Pharmacology Basics
348 Questions
0 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which type of drug bond usually results in irreversible action?

  • Ionic bonds
  • Hydrogen bonds
  • Covalent bonds (correct)
  • Van der Waals interactions

    • Which of the following is not a form of drug classification according to use?

  • Diagnostic agents
  • Enzyme inhibitors (correct)
  • Analgesic agents
  • Functional modifiers

    • What type of drug would be used to replenish substances that are lacking in the body?

  • Diagnostic agents
  • Hormones (correct)
  • Analgesic drugs
  • Chemotherapeutic agents

    • Which agent is specifically used to determine the presence or absence of a condition or disease?

    <p>Diagnostic agents</p> Signup and view all the answers

    Pernicious anemia may require treatment with which vitamin due to lack of intrinsic factor?

    <p>Vitamin B12</p> Signup and view all the answers

    Which of the following examples is used in stress testing for coronary artery disease (CAD) and myocardial infarction (MI)?

    <p>Dobutamine</p> Signup and view all the answers

    What is the primary purpose of conducting a stress test?

    <p>To assess heart function before, during, and after exercise</p> Signup and view all the answers

    Which of the following is a characteristic of chemotherapeutic agents?

    <p>It specifically targets foreign cells or nucleic acids</p> Signup and view all the answers

    What is a common use of histamine in medical treatments?

    <p>To treat allergic reactions</p> Signup and view all the answers

    Which of the following inhibitors targets the enzyme xanthine oxidase?

    <p>Allopurinol</p> Signup and view all the answers

    What is the primary function of GABA receptors in the nervous system?

    <p>They control chloride ion movement.</p> Signup and view all the answers

    Which class of receptor is associated with the activation of G-protein linked signaling?

    <p>Type II Receptor</p> Signup and view all the answers

    Which enzyme is targeted by NSAIDs for their pain-relieving effects?

    <p>Cyclooxygenase</p> Signup and view all the answers

    What distinguishes Type I receptors from other receptor types?

    <p>They act as ion channels.</p> Signup and view all the answers

    Which type of drug would likely inhibit the function of acetylcholinesterase?

    <p>Edrophonium</p> Signup and view all the answers

    What is the function of a ligand in the context of receptor interactions?

    <p>To bind specifically to a receptor.</p> Signup and view all the answers

    What is the primary function of Gs proteins in cellular signaling?

    <p>Stimulates adenylyl cyclase</p> Signup and view all the answers

    Which type of receptor is classified as a Type III receptor?

    <p>Tyrosine kinase-linked receptors</p> Signup and view all the answers

    What is the typical onset time for Type IV receptors?

    <p>Hours</p> Signup and view all the answers

    Which of the following is an example of a second messenger?

    <p>Cyclic guanosine monophosphate (cGMP)</p> Signup and view all the answers

    Which drug acts on Type IV receptors involved in gene transcription?

    <p>Corticosteroids</p> Signup and view all the answers

    What is the role of glucokinase in cellular metabolism?

    <p>Converts glucose to glucose-6-phosphate</p> Signup and view all the answers

    What is the primary focus of pharmacodynamics?

    <p>Study of the biochemical and physiological effects of drugs</p> Signup and view all the answers

    Which of the following mechanisms is NOT a way drugs can exert their effects?

    <p>Bioenergetic mechanism</p> Signup and view all the answers

    Which type of channel is involved in transmembrane signaling related to drug action?

    <p>Voltage-gated Ca channel</p> Signup and view all the answers

    Which drug is known for inhibiting microtubule synthesis?

    <p>Griseofulvin</p> Signup and view all the answers

    What kind of drug action is associated with receptor-mediated mechanisms?

    <p>Endogenous signal modulation</p> Signup and view all the answers

    Which of the following is a target for calcium channel blockers?

    <p>Voltage-gated Ca channel</p> Signup and view all the answers

    What is the term for the way the body handles drugs in pharmacokinetics?

    <p>Drug disposition</p> Signup and view all the answers

    Which of the following correctly identifies a type of chemical reaction involved in drug action?

    <p>Neutralization</p> Signup and view all the answers

    Which drugs act on voltage-gated ion channels?

    <p>Both A and B</p> Signup and view all the answers

    Which drug works by binding to tubulin and inhibiting its function?

    <p>Colchicine</p> Signup and view all the answers

    What type of protein does Digitalis glycosides primarily target in the heart?

    <p>Transporters</p> Signup and view all the answers

    What substrate does Adenylyl Cyclase use to generate cAMP?

    <p>ATP</p> Signup and view all the answers

    Which characteristic is true for nicotinic, GABA-A, and glutamate receptors?

    <p>They regulate ion flow across the membrane</p> Signup and view all the answers

    Stimulation of Beta-adrenoceptors involves the generation of which secondary messenger?

    <p>cAMP</p> Signup and view all the answers

    What is the primary focus of pharmacokinetics?

    <p>The movement and transformation of drugs within the body</p> Signup and view all the answers

    Which of the following describes the role of physicochemical properties in pharmacology?

    <p>They influence the method of drug administration.</p> Signup and view all the answers

    Which statement accurately reflects the relationship between drug absorption and kinetics?

    <p>Kinetics examines the rate and extent of drug absorption.</p> Signup and view all the answers

    What does the term 'dosage form' refer to in pharmacology?

    <p>The physical form in which a drug is given</p> Signup and view all the answers

    What is the significance of understanding the interrelationship of physicochemical properties and the route of administration?

    <p>It aids in predicting the drug's pharmacological effects.</p> Signup and view all the answers

    How does the science of pharmacology relate to drug kinetics?

    <p>It examines how drugs alter physiological processes.</p> Signup and view all the answers

    What aspect does pharmacodynamics primarily address?

    <p>How drugs interact with their targets</p> Signup and view all the answers

    Which factor is crucial in determining the rate of drug absorption?

    <p>The crystallinity of the drug</p> Signup and view all the answers

    What distinguishes a full agonist from a partial agonist?

    <p>A full agonist produces the maximal possible response.</p> Signup and view all the answers

    Which type of antagonist directly prevents the binding of an agonist?

    <p>Pharmacologic antagonist</p> Signup and view all the answers

    What is an example of a chemical antagonist?

    <p>Protamine inactivating heparin</p> Signup and view all the answers

    How does a competitive antagonist function?

    <p>It can be overcome by increasing agonist concentration.</p> Signup and view all the answers

    Which statement accurately describes a physiological antagonist?

    <p>It acts on different receptors to yield opposing actions.</p> Signup and view all the answers

    In terms of pharmacologic effects, what describes the addition of two different drugs with similar effects?

    <p>An additive interaction</p> Signup and view all the answers

    What characterizes non-competitive antagonism?

    <p>It modifies the receptor to inhibit the agonist's function.</p> Signup and view all the answers

    Which of the following concepts most accurately describes how chelating agents work?

    <p>They bind to and inactivate their specific target, forming an inactive compound.</p> Signup and view all the answers

    What term describes a decreased responsiveness to a drug due to continuous administration?

    <p>Tolerance</p> Signup and view all the answers

    Which type of hypersensitivity is characterized by an immediate allergic reaction?

    <p>Type I</p> Signup and view all the answers

    What does hyporeactivity refer to in drug responses?

    <p>Decreased effect of a drug</p> Signup and view all the answers

    What is tachyphylaxis?

    <p>Rapidly developing tolerance</p> Signup and view all the answers

    Which term refers to a decrease in receptor sensitivity following prolonged exposure to a drug?

    <p>Desensitization</p> Signup and view all the answers

    Which type of hypersensitivity involves immune complex disease?

    <p>Type III</p> Signup and view all the answers

    What is the effect of down-regulation of receptors on drug response?

    <p>Decreased drug efficacy</p> Signup and view all the answers

    What does hyperreactivity indicate in terms of drug response?

    <p>Increased drug effect</p> Signup and view all the answers

    What is one of the primary uses of H2-receptor antagonists?

    <p>Treatment of gastrointestinal disorders</p> Signup and view all the answers

    Which of the following statements about Nizatidine is correct?

    <p>It has almost 100% bioavailability.</p> Signup and view all the answers

    What side effect can result from the anti-androgen activity of Cimetidine in men?

    <p>Breast enlargement (gynecomastia)</p> Signup and view all the answers

    How does Cimetidine affect drug metabolism in the liver?

    <p>It inhibits metabolism of specific drugs.</p> Signup and view all the answers

    What is a common route of administration for Cromolyn and Nedocromil Sodium?

    <p>Inhalation</p> Signup and view all the answers

    Which condition is treated by H2-receptor antagonists that involve excessive gastric acid secretion?

    <p>Zollinger-Ellison syndrome</p> Signup and view all the answers

    What characteristic distinguishes autacoids from traditional hormones?

    <p>They are produced at the site of action.</p> Signup and view all the answers

    Which of the following is NOT classified as a lipid-derived autacoid?

    <p>Histamine</p> Signup and view all the answers

    What enzyme catalyzes the decarboxylation process to produce histamine?

    <p>L-Histidine Decarboxylase</p> Signup and view all the answers

    What process is responsible for the immunologic release of histamine?

    <p>Energy- and Ca2+-dependent degranulation</p> Signup and view all the answers

    Which of the following statements about histamine release mechanisms is accurate?

    <p>Chemical release does not require energy.</p> Signup and view all the answers

    Which classification of autacoids includes serotonin?

    <p>Biologically active amines</p> Signup and view all the answers

    Histamine is stored primarily in which types of cells?

    <p>Mast cells and basophils</p> Signup and view all the answers

    What role does R-alpha methylhistamine play in relation to histamine?

    <p>It is an H3-specific agonist.</p> Signup and view all the answers

    Which antihistamine is primarily associated with a strong sedative effect?

    <p>Doxylamine</p> Signup and view all the answers

    What is the primary mechanism by which antihistamines act?

    <p>Inhibition of H1 receptors</p> Signup and view all the answers

    Which of the following is a potential side effect of 1st generation antihistamines?

    <p>Increased CNS penetration</p> Signup and view all the answers

    How long do the effects of 2nd generation antihistamines typically last?

    <p>3-24 hours</p> Signup and view all the answers

    What is a defining feature of the antihistamine Terfenadine?

    <p>It is metabolized to fexofenadine.</p> Signup and view all the answers

    Which of the following second-generation antihistamines is least associated with sedation?

    <p>Loratadine</p> Signup and view all the answers

    Which agent has a very high H2:H1 receptor activity ratio of about 10,000?

    <p>Impromidine</p> Signup and view all the answers

    What is a common non-allergic application for antihistamines?

    <p>Appetite suppression</p> Signup and view all the answers

    What type of receptor antagonists are Ondansetron and Granisetron primarily classified as?

    <p>5HT3-receptor antagonists</p> Signup and view all the answers

    Which drug is known to lower blood pressure in cases of experimentally induced hypertension?

    <p>Ketanserin</p> Signup and view all the answers

    What serious side effect is associated with the use of Clozapine?

    <p>Agranulocytosis</p> Signup and view all the answers

    Risperidone is primarily used to treat which psychiatric condition?

    <p>Schizophrenia</p> Signup and view all the answers

    What is the primary metabolic responsibility of MAO-A?

    <p>Metabolism of norepinephrine and serotonin</p> Signup and view all the answers

    Which drug is categorized as an atypical antipsychotic that antagonizes both 5HT2A- and dopamine (D2) receptors?

    <p>Clozapine</p> Signup and view all the answers

    What distinguishes Ketanserin from Ondansetron and Granisetron?

    <p>Ketanserin is a specific 5HT2-receptor antagonist</p> Signup and view all the answers

    Which of the following receptors does Risperidone antagonize?

    <p>5HT2A, 5HT2C, and D2</p> Signup and view all the answers

    What is the primary precursor for the biosynthesis of serotonin?

    <p>L-tryptophan</p> Signup and view all the answers

    Which of the following cells is responsible for the majority (90%) of serotonin distribution in the body?

    <p>Enterochromaffin cells</p> Signup and view all the answers

    Which enzyme is involved in the conversion of serotonin to hydroxyindoleacetic acid (5-HIAA)?

    <p>Monoamine oxidase (MAO)</p> Signup and view all the answers

    What type of receptor does buspirone specifically target for its anxiolytic effects?

    <p>5-HT1a receptor</p> Signup and view all the answers

    Which class of drugs includes medications like sumatriptan and rizatriptan used for treating migraines?

    <p>Triptans</p> Signup and view all the answers

    What is the primary action of trazodone in treating depression?

    <p>Activation of 5HT1B and 5HT2 receptors</p> Signup and view all the answers

    Where is MAO-A predominantly found outside the central nervous system?

    <p>Liver and gastrointestinal tract</p> Signup and view all the answers

    Which component undergoes hydroxylation during the biosynthesis of serotonin?

    <p>L-tryptophan</p> Signup and view all the answers

    Which agent is a selective reversible MAO-A inhibitor with a lesser risk of causing hypertensive crisis with tyramine foods?

    <p>Moclobemide</p> Signup and view all the answers

    What is the primary action of cisapride in the gastrointestinal tract?

    <p>Increases motility</p> Signup and view all the answers

    Which drug requires weekly WBC monitoring for the first 6 months and every 3 weeks thereafter due to the risk of agranulocytosis?

    <p>Clozapine</p> Signup and view all the answers

    What is the primary mechanism of action of Ondansetron and Granisetron?

    <p>Antagonist effect at the 5-HT3 receptor</p> Signup and view all the answers

    What is the mechanism of action of fluoxetine?

    <p>Decreases serotonin uptake</p> Signup and view all the answers

    What is the clinical use of Ondansetron and Granisetron?

    <p>Anti-emetic</p> Signup and view all the answers

    Which of the following describes dexfenfluramine's role in treating obesity?

    <p>Causes serotonin release</p> Signup and view all the answers

    What clinical use do drugs that primarily stimulate the 5-HT1B and 5-HT1D receptors serve?

    <p>Treatment of acute migraine attack</p> Signup and view all the answers

    What major adverse effect is associated with sibutramine?

    <p>Increased risk of cardiovascular events</p> Signup and view all the answers

    Which receptors does clozapine block?

    <p>5HT1 and 5HT2 receptors</p> Signup and view all the answers

    What class of drug is Rasagiline?

    <p>A selective MAO-B inhibitor</p> Signup and view all the answers

    What is the classification of cisapride?

    <p>Gastroprokinetic agent</p> Signup and view all the answers

    Which type of receptor is primarily targeted by Ondansetron and Granisetron?

    <p>5-HT3 receptor</p> Signup and view all the answers

    What type of drug is dexfenfluramine primarily considered?

    <p>Anorectic drug</p> Signup and view all the answers

    For which condition would you potentially use medications that stimulate the 5-HT1B and 5-HT1D receptors?

    <p>Acute migraine treatment</p> Signup and view all the answers

    Which drug is no longer available in the U.S. due to safety concerns?

    <p>Sibutramine</p> Signup and view all the answers

    What are eicosanoids primarily derived from?

    <p>20-carbon unsaturated fatty acids</p> Signup and view all the answers

    Which eicosanoid is primarily produced by the Prostaglandin H synthase pathway?

    <p>Thromboxane</p> Signup and view all the answers

    What is the role of dinoprostone (PGE2) in the female reproductive system?

    <p>To induce abortion</p> Signup and view all the answers

    Which eicosanoid is used to treat pulmonary hypertension?

    <p>Prostacyclin</p> Signup and view all the answers

    Which of the following eicosanoids is administered to manage peripheral vascular disease?

    <p>PGE1</p> Signup and view all the answers

    What is the primary function of TXA2 in the blood?

    <p>To promote platelet aggregation</p> Signup and view all the answers

    How many pairs of cranial nerves are part of the nervous system discussed?

    <p>12 pairs</p> Signup and view all the answers

    What type of nerve is the Trigeminal nerve classified as?

    <p>Mixed</p> Signup and view all the answers

    Which cranial nerve is primarily responsible for facial movement?

    <p>Facial</p> Signup and view all the answers

    What is the function of the Vagus nerve?

    <p>Mixed functions</p> Signup and view all the answers

    Which cranial nerve is associated with visual sensory functions?

    <p>Optic</p> Signup and view all the answers

    Which cranial nerve is involved in regulating heart rate and digestive tract functions?

    <p>Vagus</p> Signup and view all the answers

    What type of nerve is the Abducens classified as?

    <p>Motor</p> Signup and view all the answers

    Which cranial nerve is associated with hearing and balance?

    <p>Vestibulocochlear</p> Signup and view all the answers

    What is the primary focus of the autonomic nervous system?

    <p>Visceral functions</p> Signup and view all the answers

    Which of the following neurotransmitters is associated with sympathetic postganglionic fibers?

    <p>Norepinephrine</p> Signup and view all the answers

    Which statement accurately describes the origin of the autonomic nervous system divisions?

    <p>Sympathetic originates from the thoraco-lumbar region</p> Signup and view all the answers

    What describes the nature of the preganglionic nerve fibers in the parasympathetic nervous system?

    <p>Long and myelinated</p> Signup and view all the answers

    Which type of receptors are associated with the parasympathetic nervous system?

    <p>Muscarinic and nicotinic</p> Signup and view all the answers

    What is the role of the Myenteric Plexus in the gastrointestinal tract?

    <p>Controls muscular contractions</p> Signup and view all the answers

    Which of the following best describes the autonomic nervous system's control over bodily functions?

    <p>Primarily involuntary and autonomous</p> Signup and view all the answers

    What distinguishes the preganglionic fibers of the sympathetic division from those of the parasympathetic division?

    <p>Parasympathetic fibers are shorter than sympathetic fibers</p> Signup and view all the answers

    What is the primary action of the reuptake process involving norepinephrine (NE)?

    <p>Recaptures NE back to the neuron</p> Signup and view all the answers

    Which agent is known to block the synthesis of norepinephrine?

    <p>a-Methyltyrosine</p> Signup and view all the answers

    What distinguishes adrenergic agonists from other drugs?

    <p>They stimulate the sympathetic nervous system</p> Signup and view all the answers

    What is the role of cocaine in neurotransmitter management?

    <p>Inhibits reuptake of neurotransmitters</p> Signup and view all the answers

    Which process does amphetamine primarily promote?

    <p>Increase transmitter release</p> Signup and view all the answers

    How does reserpine affect adrenergic neurotransmission?

    <p>Depletes norepinephrine from storage</p> Signup and view all the answers

    What mechanism is employed by tetrodotoxin in nerve conduction?

    <p>Blocks sodium channels</p> Signup and view all the answers

    What is a characteristic of direct-acting adrenergic agonists?

    <p>They stimulate adrenergic receptors directly</p> Signup and view all the answers

    What effect does Beta-2 receptor activation have on the lungs?

    <p>Bronchodilation</p> Signup and view all the answers

    Which receptor is associated with increasing lipolysis in fat cells?

    <p>Beta-3</p> Signup and view all the answers

    What is a major consequence of combining tyramine with MAO inhibitors?

    <p>Hypertensive crisis</p> Signup and view all the answers

    Which type of drugs are categorized as nonselective agonists?

    <p>Isoproterenol</p> Signup and view all the answers

    Which of the following best describes the function of Dopa-2 receptors?

    <p>Increase dopamine release</p> Signup and view all the answers

    What is the selective agonist for Beta-2 receptors?

    <p>Albuterol</p> Signup and view all the answers

    Which agonist is known to increase renin secretion from the kidneys?

    <p>Dopamine</p> Signup and view all the answers

    What is the primary effect of Beta-3 receptor activation in adipose tissue?

    <p>Stimulate lipolysis</p> Signup and view all the answers

    Which type of drugs would antagonize the action of Beta-2 agonists?

    <p>Nonselective Beta antagonists</p> Signup and view all the answers

    What is a common property of selective Dopa-1 agonists?

    <p>Vasodilation in renal blood vessels</p> Signup and view all the answers

    What is the primary neurotransmitter of the postganglionic fiber in the parasympathetic nervous system?

    <p>Acetylcholine</p> Signup and view all the answers

    What is another name for the sympathetic nervous system?

    <p>Adrenergic system</p> Signup and view all the answers

    What is the function associated with the pre-ganglionic fibers of the parasympathetic nervous system?

    <p>Short fibers that connect to close ganglia</p> Signup and view all the answers

    Which condition is characterized by an increased heart rate?

    <p>Bradycardia</p> Signup and view all the answers

    Which plexus is also known as the submucous plexus?

    <p>Enteric plexus</p> Signup and view all the answers

    Which of the following structures is responsible for the autonomic functions in the nervous system?

    <p>Peripheral Nervous System</p> Signup and view all the answers

    What is the effect of norepinephrine on the body?

    <p>Promotes fight-or-flight response</p> Signup and view all the answers

    How many pairs of spinal nerves does the peripheral nervous system have?

    <p>31 pairs</p> Signup and view all the answers

    What is the primary effect of Alpha-1 adrenergic receptors when stimulated?

    <p>Vasoconstriction</p> Signup and view all the answers

    Which of the following agents is a selective agonist for Alpha-2 receptors?

    <p>Clonidine</p> Signup and view all the answers

    What is the mechanism of action of amphetamine in relation to adrenergic receptors?

    <p>Stimulation of NE release from nerve endings</p> Signup and view all the answers

    Which effect is associated with Beta-1 adrenergic receptor activation?

    <p>Increased heart rate</p> Signup and view all the answers

    Which of the following drugs is used as a prodrug for epinephrine to treat glaucoma?

    <p>Dipivefrin</p> Signup and view all the answers

    What is the effect of Alpha-2 receptor stimulation in fat cells?

    <p>Decreased lipolysis</p> Signup and view all the answers

    Which of the following is an antagonist for Alpha adrenergic receptors?

    <p>Yohimbine</p> Signup and view all the answers

    Which receptor subtype is primarily responsible for triggering mydriasis (pupil dilation) when activated?

    <p>Alpha-1</p> Signup and view all the answers

    What happens when Alpha-1 receptors in the bladder sphincter are stimulated?

    <p>Constriction of the sphincter</p> Signup and view all the answers

    Which drug is known for its reversible antagonist effect on Alpha receptors?

    <p>Phentolamine</p> Signup and view all the answers

    Which of the following drugs is classified as a reversible cholinesterase inhibitor?

    <p>Neostigmine</p> Signup and view all the answers

    What is the primary purpose of edrophonium in the context of medical diagnosis?

    <p>To diagnose Myasthenia gravis</p> Signup and view all the answers

    Which of the following is an example of an irreversible cholinesterase inhibitor?

    <p>Isofluorophate</p> Signup and view all the answers

    Which of the following cholinomimetics is an intermediate acting carbamate?

    <p>Carbachol</p> Signup and view all the answers

    Which of the following agents is indicated for the treatment of glaucoma?

    <p>Pilocarpine</p> Signup and view all the answers

    Which of the following statements about carbachol is true?

    <p>It can cause increased strength in muscle contractions.</p> Signup and view all the answers

    What is the primary characteristic of seizures as measured by EEG?

    <p>Excessive, hypersynchronous discharge of cortical neuron activity</p> Signup and view all the answers

    Which statement best defines epilepsy?

    <p>A group of disorders characterized by unpredictable, recurrent seizures</p> Signup and view all the answers

    What distinguishes simple partial seizures from other types of seizures?

    <p>They do not cause loss of consciousness</p> Signup and view all the answers

    What is the most common type of seizure observed in epileptic patients?

    <p>Partial seizures</p> Signup and view all the answers

    During which phase of a seizure does the actual seizure activity occur?

    <p>Ictal phase</p> Signup and view all the answers

    What are convulsions described as in the context of seizures?

    <p>Involuntary contractions of muscles</p> Signup and view all the answers

    Which substance inhibits the transport of choline during the synthesis of acetylcholine?

    <p>Hemicholinium</p> Signup and view all the answers

    What is the action of botulinum toxin in the release of neurotransmitters?

    <p>Blocks release</p> Signup and view all the answers

    Which process is NOT a method of acetylcholine removal after its action?

    <p>Amplification</p> Signup and view all the answers

    Which type of drug mimics the action of acetylcholine in the body?

    <p>Cholinergic agonists</p> Signup and view all the answers

    What is the primary effect of spider venom on neurotransmitter release?

    <p>Promotion of release</p> Signup and view all the answers

    Which mechanism is primarily responsible for the degradation of acetylcholine?

    <p>Acetylcholinesterase</p> Signup and view all the answers

    What occurs following the binding of acetylcholine to its receptor?

    <p>Activation of downstream signaling pathways</p> Signup and view all the answers

    Which class of receptor do selective cholinergic drugs primarily target?

    <p>Muscarinic</p> Signup and view all the answers

    What effect does the M-2 cholinergic receptor have on the heart?

    <p>Decreases force of contraction</p> Signup and view all the answers

    Which cholinergic receptor type is responsible for muscarinic effects in glands?

    <p>M-3</p> Signup and view all the answers

    What does stimulation of the Nm receptor in the neuromuscular junction cause?

    <p>Muscle contraction</p> Signup and view all the answers

    Which of the following effects is NOT associated with M-3 receptors?

    <p>Dilation of pupils</p> Signup and view all the answers

    Where are M-1 receptors primarily located?

    <p>Gastrointestinal tract</p> Signup and view all the answers

    What is the primary function of the Nn cholinergic receptors?

    <p>Stimulate CNS ganglia</p> Signup and view all the answers

    Which effect is associated with stimulation of M-3 receptors in the lungs?

    <p>Increased airway resistance</p> Signup and view all the answers

    Which of the following statements about cholinergic receptors is true?

    <p>Nicotinic receptors can be found at the neuromuscular junction</p> Signup and view all the answers

    Which of these best describes the primary effect of M-3 receptor stimulation on the eyes?

    <p>Miosis</p> Signup and view all the answers

    Which location is associated with M-2 receptors within the parasympathetic nervous system?

    <p>Heart</p> Signup and view all the answers

    Why is buspirone not effective in treating benzodiazepine (BZ) withdrawal symptoms?

    <p>It is not cross-tolerant with BZs.</p> Signup and view all the answers

    What is the recommended approach before switching a patient from benzodiazepines to buspirone?

    <p>Taper the benzodiazepine dose.</p> Signup and view all the answers

    For which type of patients is buspirone considered an appropriate choice?

    <p>Patients with a history of anxiety and substance abuse.</p> Signup and view all the answers

    What is the mechanism of action of ramelteon as a melatonin receptor agonist?

    <p>Activates MT1 and MT2 receptors in the CNS.</p> Signup and view all the answers

    How do propranolol and other beta-blockers primarily help anxiety patients?

    <p>They reduce cardiovascular symptoms associated with anxiety.</p> Signup and view all the answers

    What limitation do beta-blockers have when used for treating anxiety?

    <p>They do not address the psychological symptoms of anxiety.</p> Signup and view all the answers

    What is a significant advantage of ramelteon compared to traditional sleep medications?

    <p>It results in minimal rebound insomnia.</p> Signup and view all the answers

    In treating anxiety, beta-blockers are typically reserved for which group of patients?

    <p>Patients exhibiting prominent physical symptoms.</p> Signup and view all the answers

    What characterizes the prodromal phase of schizophrenia?

    <p>Onset and gradual buildup of schizophrenic symptoms</p> Signup and view all the answers

    Which of the following accurately describes the active phase of schizophrenia?

    <p>Full-blown symptoms with severe thought disturbances</p> Signup and view all the answers

    What is a characteristic symptom of schizophrenia?

    <p>Disorganized speech patterns</p> Signup and view all the answers

    What defines positive symptoms in schizophrenia?

    <p>Symptoms that are added to the individual's experience</p> Signup and view all the answers

    What typically happens during the residual phase of schizophrenia?

    <p>Prominent symptoms are often absent</p> Signup and view all the answers

    Which of the following best describes catatonic behavior in schizophrenia?

    <p>Complete withdrawal from surroundings and non-responsiveness</p> Signup and view all the answers

    Which anticholinergic drug is used in the treatment of movement symptoms associated with schizophrenia?

    <p>Benztropine mesylate</p> Signup and view all the answers

    How is complete recovery from schizophrenia commonly viewed?

    <p>It is rare, but many individuals can lead productive lives.</p> Signup and view all the answers

    Which atypical antipsychotic is classified as a dibenzodiazepine?

    <p>Clozapine</p> Signup and view all the answers

    Which adverse drug reaction is specifically associated with Clozapine?

    <p>Agranulocytosis</p> Signup and view all the answers

    What is a primary treatment approach for Extrapyramidal symptoms (EPS)?

    <p>Use anticholinergics</p> Signup and view all the answers

    Which of the following is characterized by slowness of movement and rigidity?

    <p>Bradykinesia</p> Signup and view all the answers

    Which antipsychotic is associated with the risk of cardiotoxicity?

    <p>Thioridazine</p> Signup and view all the answers

    Which type of symptoms are classified under Extrapyramidal symptoms?

    <p>Tardive dyskinesia</p> Signup and view all the answers

    What is a key characteristic of Major Depressive Disorder (MDD)?

    <p>Depressed mood most of the time for at least 2 weeks</p> Signup and view all the answers

    Which of the following symptoms is NOT typically associated with Major Depressive Disorder?

    <p>Increased appetite</p> Signup and view all the answers

    What is the main goal of the acute treatment phase for depression?

    <p>Resolve symptoms</p> Signup and view all the answers

    Which class of antidepressants primarily works by increasing serotonin levels in the brain?

    <p>Selective serotonin re-uptake inhibitors</p> Signup and view all the answers

    What is the duration of the continuation treatment phase for depression?

    <p>6-9 months</p> Signup and view all the answers

    Which of the following is a potential non-pharmacological treatment for depression?

    <p>Psychotherapy</p> Signup and view all the answers

    What is an example of a Tricyclic antidepressant (TCA)?

    <p>Amitriptyline</p> Signup and view all the answers

    What symptom is considered a major risk associated with Major Depressive Disorder?

    <p>Suicidal attempts</p> Signup and view all the answers

    Which antidepressant class can affect both serotonin and norepinephrine reuptake?

    <p>Noradrenaline reuptake inhibitors</p> Signup and view all the answers

    What is the expected duration for the maintenance treatment phase for high-risk patients with depression?

    <p>3-5 years</p> Signup and view all the answers

    Which symptom is characterized by a difficulty in initiating movement and slowness of movement in patients with Parkinson's disease?

    <p>Akinesia</p> Signup and view all the answers

    What is the primary mechanism of action for dopaminergic agents in the treatment of Parkinson's disease?

    <p>Promote activation of dopamine receptors</p> Signup and view all the answers

    Which medication combination is commonly used in the treatment of Parkinson's disease to enhance dopamine levels?

    <p>Levodopa + Carbidopa</p> Signup and view all the answers

    Which class of drugs is used to block muscarinic cholinergic receptors in the treatment of Parkinson's disease?

    <p>Anticholinergic agents</p> Signup and view all the answers

    What is a characteristic motor disability of Parkinson's disease related to stiffness and resistance to movement?

    <p>Rigidity</p> Signup and view all the answers

    Which of the following medications is a dopamine receptor agonist used in treating Parkinson's disease?

    <p>Pramipexole</p> Signup and view all the answers

    Which of the following is a common side effect associated with the use of dopaminergic therapy, particularly Levodopa?

    <p>Hypotension</p> Signup and view all the answers

    Which of these medications inhibits the enzyme monoamine oxidase B (MAO-B) to enhance dopamine levels?

    <p>Rasagiline</p> Signup and view all the answers

    What symptom is characterized by the failure to respond to questions or comments?

    <p>Alogia</p> Signup and view all the answers

    Which negative symptom is associated with a lack of pleasure in life?

    <p>Anhedonia</p> Signup and view all the answers

    Which disorganized symptom involves incoherent speech and difficulty organizing thoughts?

    <p>Loose associations</p> Signup and view all the answers

    What term describes a lack of action or goal-oriented behavior commonly seen in schizophrenia?

    <p>Avolition</p> Signup and view all the answers

    Which of the following best describes catatonia?

    <p>Repetitive gestures or wild flailing</p> Signup and view all the answers

    What is a key characteristic of inappropriate affect in schizophrenia?

    <p>Emotional responses not matching situations</p> Signup and view all the answers

    What is the most likely indication of irreversible neuronal loss in schizophrenia?

    <p>Avolition</p> Signup and view all the answers

    What type of behavior might be seen in disorganized symptoms of schizophrenia?

    <p>Agitated pacing</p> Signup and view all the answers

    Which neurotransmitter is commonly associated with the pathophysiology of schizophrenia?

    <p>Dopamine</p> Signup and view all the answers

    Which form of antipsychotic is classified as more potent and selective?

    <p>Piperazine phenothiazines</p> Signup and view all the answers

    Which of the following antihistamines belongs to the Ethanolamines category?

    <p>Diphenhydramine</p> Signup and view all the answers

    Which of the following is a characteristic of 2nd generation antihistamines?

    <p>Have antihistaminic effects without significant sedation</p> Signup and view all the answers

    Which antihistamine is classified under the Piperidine category?

    <p>Fexofenadine</p> Signup and view all the answers

    Which of the following is a common use for Promethazine?

    <p>As an antiemetic</p> Signup and view all the answers

    Which of the following drugs is included in the Methylpiperidine class of antihistamines?

    <p>Cyproheptadine</p> Signup and view all the answers

    Which of the following antihistamines is not classified as a 1st generation antihistamine?

    <p>Cetirizine</p> Signup and view all the answers

    What class of drugs includes Cimetidine and Famotidine?

    <p>H-2 Blockers</p> Signup and view all the answers

    Which drug is primarily used to treat chronic tophaceous gout?

    <p>Allopurinol</p> Signup and view all the answers

    Which of the following is a common bronchodilator?

    <p>Theophylline</p> Signup and view all the answers

    What is the function of Misoprostol in medical treatment?

    <p>To prevent gastric ulcers</p> Signup and view all the answers

    Which of the following is classified as a uricosuric agent?

    <p>Sulfinpyrazone</p> Signup and view all the answers

    Which drug class does Ibuprofen belong to?

    <p>Propionic Acid Derivative</p> Signup and view all the answers

    What mechanism do leukotriene modifiers, such as Montelukast, primarily target?

    <p>Leukotriene receptors</p> Signup and view all the answers

    Which of the following medications is NOT an antacid?

    <p>Famotidine</p> Signup and view all the answers

    What stage of anesthesia involves unconsciousness with normal blood pressure and respiration rate?

    <p>Surgical anesthesia</p> Signup and view all the answers

    Which of the following is a volatile liquid used as an inhalational anesthetic?

    <p>Halothane</p> Signup and view all the answers

    What is the primary characteristic of medullary paralysis in anesthesia?

    <p>Respiratory depression</p> Signup and view all the answers

    Which intravenous anesthetic is primarily used for short surgical procedures due to its rapid action?

    <p>Propofol</p> Signup and view all the answers

    Which local anesthetic is known to be the most cardiotoxic?

    <p>Bupivacaine</p> Signup and view all the answers

    Which intravenous anesthetic is classified as a benzodiazepine?

    <p>Midazolam</p> Signup and view all the answers

    What is the main characteristic of primary hypertension?

    <p>It has no obvious underlying medical cause.</p> Signup and view all the answers

    Which class of drugs primarily works by promoting the excretion of sodium and water?

    <p>Diuretics</p> Signup and view all the answers

    Secondary hypertension can be caused by conditions affecting which of the following?

    <p>The endocrine system and kidneys</p> Signup and view all the answers

    Which of these antihypertensive agents acts by blocking the production or action of angiotensin?

    <p>ACE inhibitors and ARBs</p> Signup and view all the answers

    Which group of antihypertensive agents includes beta-blockers and alpha1 blockers?

    <p>Sympathoplegic agents</p> Signup and view all the answers

    What percentage of hypertension cases are classified as primary hypertension?

    <p>90-95%</p> Signup and view all the answers

    Which of the following is a potential side effect of thiazide diuretics?

    <p>Hyponatremia</p> Signup and view all the answers

    What is a common therapeutic use of thiazide diuretics?

    <p>Moderate hypertension</p> Signup and view all the answers

    Which of the following drugs is an example of a thiazide diuretic?

    <p>Chlorothiazide</p> Signup and view all the answers

    Which electrolyte imbalance is commonly associated with thiazide diuretics?

    <p>Hyponatremia</p> Signup and view all the answers

    In which part of the kidney do thiazide diuretics primarily act?

    <p>Distal convoluted tubule</p> Signup and view all the answers

    What metabolic effect can thiazide diuretics potentially induce?

    <p>Hyperglycemia</p> Signup and view all the answers

    Which of the following conditions might be treated with thiazide diuretics?

    <p>Mild to moderate hypertension</p> Signup and view all the answers

    Which side effect would be most unexpected from thiazide diuretics?

    <p>Hypertension</p> Signup and view all the answers

    Which of the following is a common adverse drug reaction associated with mild to moderate hypertension treatment?

    <p>Hyperkalemia</p> Signup and view all the answers

    What is the primary mechanism of action of alpha2 agonists in treating hypertension?

    <p>Inhibit sympathetic outflow</p> Signup and view all the answers

    Which of these drugs is contraindicated during pregnancy due to potential fetal abnormalities?

    <p>Losartan</p> Signup and view all the answers

    What is a common side effect experienced by patients on alpha1 blockers?

    <p>Syncope</p> Signup and view all the answers

    What is a known adverse effect of ganglion-blocking agents?

    <p>Erectile dysfunction</p> Signup and view all the answers

    Which of the following is a characteristic of beta blockers?

    <p>They reduce heart rate</p> Signup and view all the answers

    Which medication is an example of an angiotensin receptor blocker (ARB)?

    <p>Candesartan</p> Signup and view all the answers

    What warning is commonly associated with the initiation of alpha1 blocker therapy?

    <p>First-dose phenomenon</p> Signup and view all the answers

    What is the primary adverse effect associated with the use of furosemide?

    <p>Ototoxicity</p> Signup and view all the answers

    Which potassium-sparing diuretic is known to cause gynecomastia as a side effect?

    <p>Spironolactone</p> Signup and view all the answers

    What is a common side effect of carbonic anhydrase inhibitors, such as acetazolamide?

    <p>Metabolic acidosis</p> Signup and view all the answers

    Which class of diuretics primarily acts at the collecting tubule?

    <p>Potassium-sparing diuretics</p> Signup and view all the answers

    Which of the following medications is classified as an osmotic agent?

    <p>Mannitol</p> Signup and view all the answers

    What is a potential side effect of using vasodilators for hypertension?

    <p>Hypotension</p> Signup and view all the answers

    Which calcium channel blocker is known for its significant protein binding?

    <p>Verapamil</p> Signup and view all the answers

    What condition is primarily treated with ACE inhibitors?

    <p>Hypertension</p> Signup and view all the answers

    What is a major side effect of using hydralazine?

    <p>Systemic lupus erythematosus (SLE)</p> Signup and view all the answers

    Which diuretic class would most likely cause hyperkalemia?

    <p>Potassium-sparing diuretics</p> Signup and view all the answers

    What is the primary role of the SA Node in the heart?

    <p>Regulating heart rhythm</p> Signup and view all the answers

    Which class of heart failure is characterized by marked limitation on physical activity that can occur even during rest?

    <p>Class 3</p> Signup and view all the answers

    What type of heart failure is commonly associated with the body's metabolic demands exceeding the heart's ability to compensate?

    <p>Low output heart failure</p> Signup and view all the answers

    Which inotropic agent is classified as a cardiac glycoside?

    <p>Digitalis</p> Signup and view all the answers

    Which symptom class of heart failure indicates that a patient is asymptomatic with no limitations on physical activity?

    <p>Class 1</p> Signup and view all the answers

    What is the primary effect of administering potassium chloride (KCl) in patients treated with digitalis?

    <p>To counteract hypokalemia</p> Signup and view all the answers

    Which type of antiarrhythmic drug primarily affects sodium channels?

    <p>Type I</p> Signup and view all the answers

    Which of the following symptoms may indicate class 4 heart failure?

    <p>Any physical activity triggers symptoms</p> Signup and view all the answers

    What is the first-line medication prescribed for acute supraventricular tachycardia?

    <p>Adenosine</p> Signup and view all the answers

    Which medication is indicated as the first-line treatment for Torsades de pointes?

    <p>Magnesium Sulfate</p> Signup and view all the answers

    Which agent is the first-line controller treatment for chronic obstructive pulmonary disease (COPD)?

    <p>Long-acting beta agonist (LABA)</p> Signup and view all the answers

    What is the primary indication for the use of levo-thyroxine?

    <p>Hypothyroidism</p> Signup and view all the answers

    Which medication is the drug of choice (DOC) for treating syphilis?

    <p>Penicillin G</p> Signup and view all the answers

    Which of the following medications is considered the drug of choice for managing status epilepticus?

    <p>Lorazepam</p> Signup and view all the answers

    What is the first-line recommendation for the treatment of type 2 diabetes mellitus, especially in obese patients?

    <p>Metformin</p> Signup and view all the answers

    In the treatment of hyperthyroidism, which medication is classified as a first-line option?

    <p>Methimazole</p> Signup and view all the answers

    What is the main cause of stable angina?

    <p>Atherosclerosis</p> Signup and view all the answers

    Which type of angina occurs unexpectedly, even at rest?

    <p>Unstable angina</p> Signup and view all the answers

    What is a common treatment for vasospastic angina?

    <p>Calcium channel blockers</p> Signup and view all the answers

    Which item serves as a phosphodiesterase inhibitor to help manage both erectile dysfunction and angina?

    <p>Sildenafil</p> Signup and view all the answers

    What is a significant risk associated with cerebral ischemia?

    <p>Stroke</p> Signup and view all the answers

    Which antianginal drug works primarily by decreasing heart rate and contractility?

    <p>Beta blockers</p> Signup and view all the answers

    Which type of ischemia directly affects the heart's oxygen supply?

    <p>Myocardial ischemia</p> Signup and view all the answers

    What type of angina is characterized by severe chest pain occurring predominantly at night?

    <p>Variant angina</p> Signup and view all the answers

    What is the drug of choice for Type I Diabetes Mellitus?

    <p>Insulin lispro</p> Signup and view all the answers

    Which medication is used as the first-line bronchodilator in acute asthma attacks?

    <p>Albuterol</p> Signup and view all the answers

    Which drug is the first-line treatment for managing chronic stable angina pectoris?

    <p>Beta blockers</p> Signup and view all the answers

    What condition is Pralidoxime used to treat?

    <p>Organophosphate poisoning</p> Signup and view all the answers

    Which drug is indicated as the first-line treatment for stress-induced ulcers in critically-ill patients?

    <p>Sucralfate</p> Signup and view all the answers

    Which class of agents includes sitagliptin?

    <p>Dipeptidyl peptidase inhibitors</p> Signup and view all the answers

    What is the primary function of Methimazole in thyroid management?

    <p>Thyroid hormone synthesis inhibition</p> Signup and view all the answers

    Which medication is NOT associated with hypertension management?

    <p>Sitagliptin</p> Signup and view all the answers

    Which agent is the first-line treatment for acute gout attacks?

    <p>Colchicine</p> Signup and view all the answers

    Which beta-blocker is commonly used as the drug of choice during chronic stable angina pectoris?

    <p>Propranolol</p> Signup and view all the answers

    What is the primary benefit of using Angiotensin Converting Enzyme inhibitors in heart failure management?

    <p>Prevent cardiac hypertrophy</p> Signup and view all the answers

    Which diuretic is commonly used to manage fluid retention in patients with heart failure?

    <p>Thiazide diuretics</p> Signup and view all the answers

    Which agent is associated with the side effect of hepatotoxicity?

    <p>Atorvastatin</p> Signup and view all the answers

    What is the primary therapeutic effect of beta blockers in chronic heart failure?

    <p>Improve exercise tolerance</p> Signup and view all the answers

    What is the main mechanism by which HMG-CoA reductase inhibitors lower cholesterol levels?

    <p>Preventing mevalonic acid synthesis</p> Signup and view all the answers

    Which of the following drugs is known for its vesodilating effect and is used to reduce LDL secretion?

    <p>Niacin</p> Signup and view all the answers

    What is a common side effect associated with Inamrinone?

    <p>Aplastic anemia</p> Signup and view all the answers

    What is the mechanism of action of bile acid binding resins in managing cholesterol levels?

    <p>Prevent reabsorption of bile acids</p> Signup and view all the answers

    Which of the following drugs is primarily used to treat hyperthyroidism?

    <p>Methimazole</p> Signup and view all the answers

    Which medication must be taken with aspirin to mitigate flushing side effects?

    <p>Niacin</p> Signup and view all the answers

    Study Notes

    Drug Interactions and Functions

    • Study of substances that affect living systems via chemical processes by binding to regulatory molecules.
    • Drugs alter biological functions through chemical actions; can prevent, diagnose, mitigate, or treat conditions.

    Drug-Receptor Bonds

    • Drugs utilize various chemical bonds to bind to receptors:
      • Strong covalent bonds lead to irreversible effects.
      • Weaker electrostatic bonds form between cations and anions.
      • Very weak interactions include hydrogen bonds, van der Waals interactions, and hydrophobic bonds.

    Drug Classifications by Use

    • Drugs can be classified based on their functional roles:
      • Functional Modifiers: Alter or modulate normal physiological functions, e.g., analgesic, anti-pyretic, anti-inflammatory, and anti-hypertensive drugs.
      • Replenishers: Supplement endogenous substances that are deficient, such as hormones (like insulin), IV fluids, electrolytes, and multivitamins.
      • Diagnostic Agents: Determine the presence or absence of diseases/conditions, examples include Edrophonium, histamine, some radiopharmaceuticals, barium sulfate, dobutamine, and dipyridamole used in stress tests for coronary artery disease (CAD) and myocardial infarction (MI).
      • Chemotherapeutic Agents: Target and inhibit the growth of foreign cells or nucleic acids with selective toxicity, such as antineoplastics and anti-infectives.

    Specific Cases in Drug Use

    • Pernicious Anemia: Caused by autoimmune destruction of parietal cells, leading to Vitamin B12 deficiency; often treated with Vitamin B12 injections.
    • Stress Tests: Electrocardiographic assessments of heart function conducted under controlled exercise conditions to evaluate heart health.

    Pharmacokinetics

    • Study of drug fate in the body, including absorption, distribution, metabolism, and excretion.
    • Drug disposition refers to how the body processes drugs.

    Pharmacodynamics

    • Examines biochemical and physiological effects of drugs and their mechanisms of action.
    • Mechanisms can be categorized into:
      • Target protein mediated mechanisms.
      • Non-target protein mediated mechanisms, including:
        • Colligative mechanisms related to osmotic pressure.
        • Chemical reactions such as neutralization and chelation.

    Sites of Drug Action

    • Target proteins serve as biological sites where drugs exert effects.
    • Microtubules are crucial drug action sites, inhibited by:
      • Griseofulvin
      • Vinca alkaloids
      • Colchicine

    Types of Drug Action Mechanisms

    • Channels/Transport:

      • Proteins that regulate ionic composition, such as voltage-gated sodium and calcium channels.
      • Local anesthetics and drugs like carbamazepine and phenytoin interact with sodium channels, while calcium channel blockers target calcium channels.

    • Carrier Molecules:

      • Na+-K+ ATPase pump inhibited by digitalis glycosides.
      • H+-K+ ATPase pump targeted by proton pump inhibitors.

    • Enzymes:

      • Proteins acting as catalysts, e.g.:
        • Xanthine oxidase inhibited by allopurinol.
        • Cyclooxygenase targeted by NSAIDs and ACE inhibitors.
        • Monoamine oxidase inhibitors (MAOIs) include phenelzine, isocarboxazid, and tranylcypromine.

    • Receptors:

      • Macromolecular components of cells with specific binding capabilities.
      • Ligands are chemicals that bind to receptors, which exhibit specificity and selectivity.

    Types of Receptors

    • Type I Receptors:

      • Control ion movement in cell membranes, activated in milliseconds, e.g. GABA A receptors affecting chloride ions, influenced by benzodiazepines and barbiturates.

    • Type II Receptors:

      • G-protein linked receptors that modulate second messenger production. Rapid onset in seconds, includes alpha and beta receptors, and muscarinic receptors.

    • Type III Receptors/Tyrosine Kinases:

      • Catalyze the phosphorylation of tyrosine residues, affecting various biochemical processes. Slow onset (hours), examples include imatinib for GIST and gefitinib for epidermal growth factor receptor.

    • Type IV Receptors/Gene Transcription-Linked:

      • Involved in gene transcription (central dogma: replication, transcription, translation). Drugs affecting these receptors include corticosteroids, mineralocorticoids, sex steroids, vitamin D, and thyroid hormone. Slow onset in hours.

    Drug Actions on Voltage-Gated Ion Channels

    • Diltiazem and Nifedipine are calcium channel blockers affecting cardiovascular function.
    • Lidocaine and Procaine are local anesthetics that inhibit sodium channels, reducing neuronal excitability.
    • Captopril and Losartan are not primarily known for action on voltage-gated ion channels; they relate to the renin-angiotensin system.

    Tubulin-Binding Drugs

    • Colchicine binds to tubulin, inhibiting microtubule formation and affecting cellular functions.
    • Cyclosporine, Neostigmine, Glibenclamide, and Metformin do not primarily involve tubulin-binding mechanisms.

    Digitalis Glycosides Action

    • Digitalis glycosides target transporters, specifically the Na+/K+ ATPase enzyme, enhancing cardiac contractility.

    cAMP Synthesis

    • Cyclic Adenosine Monophosphate (cAMP) is synthesized from ATP by the enzyme Adenylyl Cyclase, serving as a secondary messenger in various signaling pathways.

    Ion-Channel Receptors Characteristics

    • Nicotinic, GABA-A, and Glutamate receptors are ligand-gated ion channels that control ion movement across the plasma membrane.
    • These receptors primarily exhibit excitatory effects, facilitating cellular responses; they do not act via secondary messengers.

    Stimulation of Beta-Adrenoceptors

    • Activation of Beta-adrenoceptors generates cAMP as a secondary messenger, influencing metabolic processes and cardiac function.

    Pharmacodynamics Overview

    • Pharmacodynamics studies the effects of drugs on biological systems and the interactions between drug properties and administration routes.
    • It encompasses the kinetics of drug absorption, distribution, metabolism, and elimination.
    • Describes the physiological effects drugs have on the body, focusing on the relationship between drug concentration and effect.

    Lanoxin (Digoxin) Action

    • Lanoxin, also known as Digoxin, primarily acts on cardiac tissues by inhibiting Na+/K+ ATPase, leading to increased intracellular calcium and enhanced contractility.

    Idiosyncrasy in Drug Response

    • Unusual drug responses arise from genetic differences or immunologic mechanisms affecting drug metabolism or triggering allergic reactions.
    • Hyporeactivity: Reduced intensity of drug effects at a standard dose.
    • Hyperreactivity: Enhanced intensity of drug effects compared to the typical response seen in most patients.
    • Hypersensitivity: Allergy or other immunologic drug responses, classified into five types.

    Hypersensitivity Classification

    • Type I: Immediate Allergic Reactions.
    • Type II: Cytotoxic or Antibody-dependent reactions.
    • Type III: Immune Complex Disease.
    • Type IV: Delayed-Type Hypersensitivity.
    • Type V: Autoimmune Diseases.

    Tolerance and Tachyphylaxis

    • Tolerance: Reduced responsiveness to a drug after prolonged use; develops with continued administration.
    • Tachyphylaxis: Rapidly occurring tolerance where responsiveness decreases swiftly following drug administration.

    Receptor Interaction and Alterations

    • Down-regulation: Occurs due to prolonged exposure, leading to decreased receptor numbers and altered functionality.
    • Desensitization: Resulting from down-regulation, causing diminished effects from the same drug concentration upon subsequent doses.

    Drug Classification Based on Receptor Interaction

    • Agonist: Binds with affinity and exhibits intrinsic activity.

      • Full Agonist: Produces maximum response, activating all receptor variants.
      • Partial Agonist: Produces less than the expected full response.

    • Antagonist: Binds with affinity but lacks intrinsic activity, inhibiting agonist binding.

    Types of Antagonists

    • Pharmacologic Antagonist: Binds to the same receptor as an agonist, producing opposing effects (e.g., beta-blockers vs. beta-agonists).
    • Physiologic Antagonist: Operates at different receptor sites for opposing actions (e.g., histamine vs. epinephrine).
    • Chemical Antagonist: Forms an inactive compound through binding (e.g., protamine and heparin).

    Competitive vs. Non-competitive Antagonism

    • Competitive Antagonism: The antagonist's effects can be reversed by increasing the agonist concentration.
    • Non-competitive Antagonism: Also known as irreversible antagonism, cannot be overcome by increasing agonist concentration.

    Drug Interaction Effects

    • Addition: The total effect equals the sum of individual drug effects (e.g., alcohol combined with a sedative).

    Key Points

    • Responsiveness to drugs can vary significantly based on individual genetic makeup and receptor interactions.
    • Understanding these mechanisms is crucial for predicting drug responses and optimizing therapeutic strategies.

    Autacoids Overview

    • Endogenous substances with biological activity, not stored or released by glands.
    • Formed at the site of action and produce localized effects.

    Classification of Autacoids

    • Biologically Active Amines:
      • Histamine and Serotonin.
    • Lipid-Derived Autacoids (Eicosanoids):
      • Prostaglandins, Leukotrienes, Thromboxanes.
    • Ergot Alkaloids:
      • Naturally occurring compounds derived from the fungus Claviceps purpurea.

    Histamine

    • Small molecule produced from decarboxylation of histidine, catalyzed by L-histidine decarboxylase.
    • Requires pyridoxal phosphate for its synthesis.
    • Found in high concentrations in mast cells and basophils; also present in the brain.

    Histamine Release Mechanisms

    • Energy- and Ca2+-Dependent Degranulation:
      • Involves mast cells sensitized by IgE antibodies reacting with specific antigens, leading to allergic responses.
    • Energy- and Ca2+-Independent Release (Displacement):
      • Triggered by chemical or mechanical injury to mast cells, induced by drugs (e.g., morphine, amine antibiotics).

    Effects of Histamine

    • Causes flushing, hypotension, tachycardia, headache, wheals, bronchoconstriction, and gastrointestinal upset.

    Antihistamines

    • Competitive inhibitors at the H1-receptor, used to counteract histamine effects.
    • 1st Generation Antihistamines:
      • Ethanolamines: Carbonoxamine, Dimenhydrinate, Diphenhydramine, Doxylamine, Clemastine.
      • Ethylaminediamines: Pyrilamine, Tripelennamine.
      • Piperazine: Hydroxyzine, Cyclizine, Meclizine.
      • Alkylamines: Brompheniramine, Chlorpheniramine.
      • Phenothiazines: Promethazine.
      • Miscellaneous: Cyproheptadine, Piperidines.

    2nd Generation Antihistamines

    • Terfenadine (Seldane): Metabolized to active fexofenadine.
    • Loratadine (Claritin): Low CNS penetration.
    • Cetirizine (Zyrtec): Minimal cardiac effects, poor CNS penetration.

    Uses of Antihistamines

    • Treat allergic rhinitis, conjunctivitis, common cold, urticaria, atopic dermatitis.
    • Used as sedatives (e.g., doxylamine, diphenhydramine), for motion sickness, and as appetite suppressants.

    Side Effects of Antihistamines

    • Sedation (caution for drivers), gastrointestinal upset, anticholinergic effects (dry mouth, blurred vision).

    H2-Receptor Antagonists

    • Include Cimetidine (Tagamet), Ranitidine (Zantac), Famotidine (Pepcid AC), Nizatidine (Axid).
    • Used for gastrointestinal disorders such as heartburn and ulcers, and in conditions like Zollinger-Ellison syndrome.

    Metabolism of H2-Receptor Antagonists

    • Cimetidine, ranitidine, and famotidine undergo significant first-pass metabolism (~50% bioavailability).
    • Nizatidine has almost 100% bioavailability with minimal first-pass metabolism.

    Cimetidine Specifics

    • Acts as a potent enzyme inhibitor, affecting drug metabolism via cytochrome P450 pathways.

    Mast Cell Stabilizers

    • Cromolyn (Intal) and Nedocromil Sodium (Tilade) are poorly absorbed, administered via inhalation.
    • Inhibit the release of histamine from mast cells, used prophylactically in asthma.

    Serotonin Overview

    • Serotonin, also known as 5-hydroxytryptamine (5-HT), is an indoleamine with a ring structure.
    • Biosynthesized from the amino acid L-tryptophan, through hydroxylation followed by decarboxylation.
    • Primarily distributed in enterochromaffin cells (90%) in the gastrointestinal tract and 10% in platelets.

    Serotonin Metabolism

    • Metabolized by monoamine oxidase (MAO) to form 5-hydroxyindoleacetaldehyde and then converted to 5-hydroxyindoleacetic acid (5-HIAA).
    • MAO-A found in the liver, gastrointestinal tract, and placenta; MAO-B primarily located in blood platelets.

    • Buspirone (Buspar): Specific 5-HT1A receptor agonist, used in managing anxiety disorders; classified as a non-benzodiazepine anxiolytic.

    • Triptans: A group of tryptamine-based drugs used for migraines and cluster headaches; includes Sumatriptan, Rizatriptan, Naratriptan, and Zolmitriptan.

    • Trazodone (Desyrel): An antidepressant metabolized to m-chlorophenylpiperazine, which activates 5-HT1B and 5-HT2 receptors.

    • Cisapride (Propulsid): A gastroprokinetic agent increasing motility in the gastrointestinal tract; acts as a 5-HT4 partial agonist.

    • Fluoxetine (Prozac): An antidepressant that inhibits serotonin uptake into neurons (SSRI).

    • Dexfenfluramine (Redux): Anorectic drug that facilitates serotonin release and reduces reuptake; used for obesity but associated with pulmonary hypertension.

    • Sibutramine (Reductil): Anorectic drug previously available in the U.S., linked to increased cardiovascular risks; currently withdrawn from the market.

    Drug Receptor Modulation

    • Ondansetron and Granisetron: 5-HT3 receptor antagonists, used to mitigate nausea and vomiting during chemotherapy and radiation therapy, available for intravenous or oral administration.

    • Ketanserin (Sufrexal): Specific antagonist of 5-HT2 receptors, investigated for lowering blood pressure in hypertension.

    • Clozapine (Clozaril): Atypical antipsychotic acting as a 5-HT2A and 5-HT2C, as well as dopamine receptor antagonist; associated with agranulocytosis.

    • Risperidone (Risperdal): Antagonist at 5-HT2A, 5-HT2C, and dopamine D2 receptors; primarily used in schizophrenia treatment.

    Key Questions for Practice

    • Identify selective reversible MAO-A inhibitors with lesser risk of hypertensive crisis related to tyramine foods.
    • Determine which drug necessitates weekly WBC monitoring due to agranulocytosis risk.
    • Recognize primary action of Ondansetron and Granisetron at the 5-HT3 receptor.
    • Understand clinical uses for medications that target 5-HT1B and 5-HT1D receptors, particularly in migraine treatments.
    • Classify Rasageline as a selective MAO-A or MAO-B inhibitor.

    Eicosanoids Overview

    • Large group of autacoids with effects on nearly all body tissues.
    • Derived from the metabolism of 20-carbon unsaturated fatty acids, predominantly arachidonic acid.
    • Released locally, functioning as local hormones, and are widely distributed throughout the body.

    Biosynthesis

    • Prostaglandin H synthase pathway (also known as COX):
      • Produces thromboxane and primary prostaglandins (PGE, PGF, PGD).
      • Also responsible for the production of prostacyclin (PGI2).

    Clinical Pharmacology in Female Reproductive System

    • Abortion Methods:
      • Dinoprostone (PGE2): Synthetic analogue administered vaginally for oxytocic effect.
      • Carboprost Tromethamine (15-methyl-PGF2a): Administered as a single 2.5 mg intra-amniotic injection.
      • Antiprogestins (Mifepristone): Combined with oral oxytocic prostaglandin (Misoprostol) for early medical abortion.

    Clinical Pharmacology in Male Reproductive System

    • Erectile Dysfunction Treatment: Alprostadil (PGE1) used as a therapeutic agent.

    Cardiovascular System Implications

    • Pulmonary Hypertension: Treated with prostacyclin.
    • Peripheral Vascular Disease: Managed with PGE and PGI2.
    • Patent Ductus Arteriosus: Alprostadil (PGE1) serves as a treatment option.

    Blood Function

    • Platelet Aggregation: Thromboxane A2 (TXA2) plays a crucial role in promoting platelet aggregation.

    Gastrointestinal System Applications

    • Ulcer Treatment: Misoprostol (PGE1) is available in Europe and the USA for managing gastric ulcers.

    Nervous System Overview

    • Collection of nerves and ganglia distributed throughout the brain.
    • Comprises 12 pairs of cranial nerves and 31 pairs of spinal nerves.

    Cranial Nerves

    • Olfactory (I): Sensory; responsible for smell.
    • Optic (II): Sensory; responsible for vision.
    • Oculomotor (III): Motor; controls eye movements and pupil constriction.
    • Trochlear (IV): Motor; innervates superior oblique muscle of the eye.
    • Trigeminal (V): Mixed; responsible for facial sensation and chewing.
    • Abducens (VI): Motor; controls lateral rectus muscle of the eye.
    • Facial (VII): Mixed; controls facial expressions and taste sensations.
    • Vestibulocochlear (VIII): Sensory; responsible for hearing and balance.
    • Glossopharyngeal (IX): Mixed; involved in taste, swallowing, and salivation.
    • Vagus (X): Mixed; interfaces with parasympathetic control of the heart, lungs, and digestive tract.
    • Accessory (XI): Motor; controls shoulder and neck muscles.
    • Hypoglossal (XII): Motor; controls tongue movements.

    Divisions of the Nervous System

    • Enteric Nervous System: Highly organized collection of neurons in the gastrointestinal tract, innervated by Myenteric and submucosal plexus.
    • Somatic Nervous System: Controls voluntary movements and posture, involving conscious control over skeletal muscles.
    • Autonomic Nervous System: Functions autonomously, regulating involuntary visceral functions such as heart rate, blood flow, and digestion.

    Autonomic Nervous System

    • Sympathetic Nervous System:

      • Originates in the thoraco-lumbar region.
      • Preganglionic fibers are short; postganglionic fibers are long.
      • Neurotransmitters: Acetylcholine (preganglionic), Norepinephrine (postganglionic).
      • Receptors: Alpha and beta adrenergic receptors.

    • Parasympathetic Nervous System:

      • Originates from cranio-sacral areas (cranial nerves III, VII, IX, X).
      • Preganglionic fibers are long; postganglionic fibers are short.
      • Neurotransmitters: Acetylcholine for both pre and postganglionic fibers.
      • Receptors: Muscarinic and nicotinic receptors.

    Peripheral Nervous System (PNS) Overview

    • Divided into autonomic (involuntary) and somatic (voluntary) systems.
    • Autonomic nervous system includes sympathetic and parasympathetic divisions, controlling involuntary bodily functions.

    Parasympathetic Nervous System Origin

    • Originates from craniosacral regions: brainstem and sacral spinal cord.

    Key Neurotransmitters

    • Primary neurotransmitter for postganglionic fibers in the sympathetic autonomic nervous system (SANS) is norepinephrine.
    • Postganglionic fibers of the parasympathetic system primarily use acetylcholine (ACh).

    Parasympathetic Receptors

    • Receptors include muscarinic and nicotinic types.
    • Muscarinic receptors are located at target organs while nicotinic receptors are found at ganglia.

    Submucous Plexus

    • Also known as the Meissner's plexus, regulates digestive system functions.

    Spinal Nerve Pairs in PNS

    • The PNS has 31 pairs of spinal nerves.

    Efferent Neurons

    • Efferent neurons, also called motor neurons, transmit signals away from the CNS.

    Alternate Names

    • Parasympathetic nervous system is sometimes referred to as the craniosacral system.
    • Norepinephrine can also be identified as noradrenaline.

    Sympathetic Nervous System Characteristics

    • Known as the adrenergic system and primarily uses norepinephrine and epinephrine as neurotransmitters.
    • Engages in the fight-or-flight response, preparing the body for stressful situations.

    Action of Sympathetic Agonists

    • Agonists can directly stimulate adrenergic receptors, indirectly promote norepinephrine release, or possess mixed actions (direct and indirect).

    Sympathetic Receptor Types

    • Alpha-1 receptors cause vasoconstriction and mydriasis.
    • Alpha-2 receptors inhibit norepinephrine release and promote platelet aggregation.
    • Beta-1 receptors increase heart rate and contraction force.
    • Beta-2 receptors promote bronchodilation and relaxation of the bladder.
    • Beta-3 receptors stimulate lipolysis in fat cells.

    Receptor Location and Effects

    • Alpha-1: Blood vessels (vasoconstriction), eyes (mydriasis).
    • Alpha-2: CNS neurons (inhibition of NE release), platelets (aggregation).
    • Beta-1: Heart (increased heart rate and contraction), kidneys (renin secretion).
    • Beta-2: Lungs (bronchodilation), uterus (tocolytic effect), liver (glycogenolysis).
    • Dopa-1: Renal blood vessels (vasodilation).
    • Dopa-2: CNS neurons (increased dopamine release).

    Norepinephrine Metabolism

    • Inactivation through MAO (monoamine oxidase) and COMT (catechol-O-methyl transferase).
    • Metabolites such as vanillyl mandelic acid (VMA) are urinary excretion products.

    Tyramine

    • By-product of tyrosine metabolism that can lead to hypertensive crises when combined with MAO inhibitors.

    Sympathetic System Interaction with Drugs

    • Various drugs can either enhance (agonists) or inhibit (antagonists) the effects of the sympathetic nervous system by acting on specific adrenergic receptors.

    Key Drugs and Effects

    • Direct agonists like isoproterenol for heart rate increase.
    • Non-selective and selective reuptake inhibitors increase effects of neurotransmitters on post-synaptic receptors.
    • Amphetamines stimulate the release of norepinephrine.

    Important Considerations

    • Understanding the dual role of the autonomic nervous system is crucial for pharmacological interventions in various clinical settings.

    Neurotransmitter and Cholinergic Receptors

    • Acetylcholine (Ach) is a key neurotransmitter influencing various body functions.
    • Cholinergic receptors are sites on effector organs that respond to Ach, categorized into muscarinic and nicotinic receptors.

    Parasympathetic Nervous System Receptors

    • Muscarinic Receptors:

      • M-1: Located in the upper gastrointestinal tract, stimulates acid secretion.
      • M-2: Found in the heart, inhibits inotropic and chronotropic effects.
      • M-3: Present in exocrine glands (salivary, sweat), bronchial pathways, and eyes; promotes secretions, bronchoconstriction, intestinal motility, and miosis.

    • Nicotinic Receptors:

      • Nm: Neuromuscular junction, responsible for muscle contraction.
      • Nn: Located in the CNS ganglia, facilitates stimulation.

    Synthesis and Release of Acetylcholine

    • Choline transport is inhibited by hemicholinium, affecting Ach synthesis.
    • Storage vesicles protect Ach from degradation; this process is blocked by vesamicol.
    • Ach release can be inhibited by botulinum toxin or promoted by spider venom.
    • Ach degradation is mediated by acetylcholinesterase, yielding acetate and choline.

    Parasympathomimetic and Parasympatholytic Drugs

    • Parasympathomimetic (Cholinergic Agonists): Stimulate the parasympathetic nervous system, mimicking Ach.
    • Parasympatholytic (Anticholinergic): Inhibit parasympathetic actions.

    Symptoms of Parasympathetic Activation

    • Associated with the acronym DUMBBELS: Diarrhea, Urination, Miosis, Bradycardia, Bronchoconstriction, Emesis, Lacrimation, Salivation.

    Classes of Cholinergic Drugs

    • Direct Acting Cholinergic Agonists:

      • Includes carbamates and esters of choline, such as acetylcholine, betanechol, methacholine, and carbachol.

    • Reversible Cholinesterase Inhibitors:

      • Edrophonium for myasthenia gravis and diagnostics.
      • Carbamates like physostigmine and neostigmine for symptom relief.

    • Irreversible Inhibitors: Organophosphates like isofluorophate.

    Seizures and Epilepsy

    • Seizures: Excessive, hypersynchronous discharges of cortical neurons measured via EEG.

    • Convulsions: Involuntary muscle contractions associated with seizures.

    • Epilepsy: A chronic disorder characterized by recurrent seizures without consistent provoking factors.

    Phases of Seizures

    • Prodrome: Early symptoms preceding a seizure.
    • Ictal: The seizure activity itself.
    • Post-ictal: Recovery phase following a seizure.

    Types of Seizures

    • Partial Seizures: Most common, occurring in about 80% of patients. Initial neuronal activation may spread to other brain areas.
    • Simple Partial Seizures: Do not cause a loss of consciousness; symptoms vary including motor, sensory, and autonomic effects.

    Anxiolytic Treatments

    • Ramelteon (Rozerem): A melatonin receptor agonist with rapid onset and minimal rebound insomnia.
    • Beta-blockers (e.g., Propranolol): Used for anxiety symptoms, particularly cardiovascular, but less effective than benzodiazepines.

    Parkinson's Disease

    • Also known as Paralysis Agitans, named after Dr. James Parkinson (1817).
    • Neurodegenerative condition linked to the degeneration (depigmentation) of the substantia nigra.
    • Results in loss of dopaminergic input to the basal ganglia, leading to motor disabilities.

    Symptoms of Parkinson's Disease

    • Tremors: Usually starts on one side of the body, often in the hand or finger.
    • Rigidity: Increased muscle tightness, reducing flexibility.
    • Akinesia: Difficulty initiating movement and slowness.
    • Postural instability: Trouble maintaining balance.

    Drug Therapy for Parkinson's Disease

    • Two major classifications of drugs:
      • Dopaminergic agents: Enhance dopamine receptor activation.
      • Anticholinergic agents: Block cholinergic receptor activation.

    Mechanisms of Action

    • Involve enhancing dopamine synthesis, activating dopamine receptors directly, and preventing dopamine degradation.
    • May also promote dopamine release and block muscarinic cholinergic receptors in the striatum.

    Antiparkinsonian Drugs

    • Levodopa + Carbidopa: Common first-line treatment.
    • Dopamine receptor agonists: Includes Bromocriptine, Pergolide, Pramipexole, Ropinirole.
    • MAO-B Inhibitors: Such as Selegiline, Rasagiline.
    • COMT Inhibitors: Includes Entacapone, Tolcapone.
    • Amantadine: Provides symptomatic relief.
    • Anticholinergics: Like Benztropine, Biperiden, Trihexyphenidyl.

    Schizophrenia

    • Denotes various mental disorders with clear sensorium but marked disturbances in thinking.

    Phases of Schizophrenia

    • Prodromal Phase: Gradual onset of symptoms.
    • Active Phase: Full-blown symptoms such as severe thinking disturbances and affect issues.
    • Residual Phase: Symptoms decrease but full recovery is rare; many can still lead productive lives.

    Symptoms of Schizophrenia

    • Must exhibit two or more symptoms for at least one month.
    • Positive symptoms: Include hallucinations, disorganized speech, and inappropriate affect.
    • Negative symptoms: Include flat affect, alogia, avolition, and social withdrawal.

    Disorganized Symptoms

    • Disorganized speech and behavior, characterized by incoherence and odd actions.

    Other Symptoms of Schizophrenia

    • Catatonia: Involves motor abnormalities, such as unusual postures and waxy flexibility.
    • Inappropriate affect: Emotional responses inconsistent with the situation.

    Pathophysiology

    • Key neurotransmitter changes involve dopamine, glutamate, and serotonin.

    Antipsychotics

    • Phenothiazines: Include Chlorpromazine and Thioridazine; categorized based on potency.
    • Atypical Antipsychotics: Include Clozapine, Risperidone, and Olanzapine.

    Adverse Drug Reactions (ADRs) - Antipsychotics

    • Risk of seizures, agranulocytosis (especially with Clozapine), cardiotoxicity, and neuroleptic malignant syndrome.
    • Extrapyramidal symptoms (EPS) such as tremors and rigidity common, particularly with high-potency drugs.

    Affective Disorders

    • Characterized by significant mood alterations.
    • Unipolar Disorders: Mainly depression.
    • Bipolar Disorder: Manic-depressive illness involving episodes of mania and depression.

    Major Depressive Disorder (MDD)

    • Depressed mood or loss of interest/pleasure predominant for two weeks or more.
    • Symptoms include low self-worth, disturbed sleep/appetite, and potential suicidal thoughts.

    Treatment for Depression

    • Non-pharmacological options include psychotherapy and Electroconvulsive Therapy (ECT).
    • Treatment phases include acute (6 weeks), continuation (6-9 months), and maintenance (3-5 years).

    Antidepressants

    • SSRIs: Fluoxetine, Sertraline, Citalopram.
    • TCAs: Imipramine, Amitriptyline, Desipramine.
    • MAOIs: Phenelzine, Isocarboxazid.
    • SARIs: Trazodone, Nefazodone.
    • NDRIs: Bupropion is notably included.
    • NaRIs: Reboxetine for noradrenaline reuptake inhibition.

    Anti-Ulcer Drugs

    • H-2 Blockers: Reduce stomach acid secretion. Key agents include:

      • Cimetidine
      • Ranitidine
      • Famotidine
      • Nizatidine

    • Proton Pump Inhibitors (PPIs): Inhibit the proton pump to decrease gastric acid production. Noteworthy examples:

      • Omeprazole
      • Esomeprazole
      • Lansoprazole
      • Pantoprazole
      • Rabeprazole

    • Antacids: Neutralize stomach acid. Common formulations include:

      • Sodium bicarbonate (NaHCO3)
      • Calcium carbonate (NaCO3)

    • Sucralfate: Forms a protective barrier on stomach mucosa and aids in healing ulcers.

    • Bismuth Compounds: Used in treating ulcers, includes:

      • Bismuth subsalicylate
      • Often combined with antibiotics like tetracycline and metronidazole.

    • Misoprostol: A prostaglandin analogue that protects the stomach lining and prevents ulcer formation.

    NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)

    • Drug Classes and Examples:
      • Propionic Acid Derivatives: ibuprofen
      • Pyrrolealkanoic Acid Derivatives: tolmetin
      • Phenylalkanoic Acid Derivatives: flubiprofen
      • Indole Derivatives: indomethacin
      • Pyrazolone Derivatives: phenylbutazone
      • Phenylacetic Acid Derivatives: diclofenac
      • Fenamate: meclofenamate
      • Oxicam: piroxicam
      • Naphthylacetic Acid Prodrug: nabumetone
      • Salicylate: Acetylsalicylic Acid (ASA)

    Drugs Used in Gout

    • Colchicine: Effective for acute gouty arthritis.
    • Indomethacin: Non-steroidal anti-inflammatory for gout management.
    • Oxaprozin: Treats pain and inflammation in gout.
    • Allopurinol: Used for chronic tophaceous gout; it reduces uric acid production.
    • Uricosuric Agents:
      • Probenecid: Increases uric acid excretion.
      • Sulfinpyrazone: Another uricosuric agent.

    Anti-Asthma Drugs

    • Bronchodilators: Facilitate airway relaxation.

      • β2 Agonists: Mainstay for quick relief.
      • Methylxanthines: Theophylline as a classic example.
      • Anticholinergics/Antimuscarinics: Help relax bronchial muscles.

    • Anti-inflammatory Agents:

      • Leukotriene Modifiers: Zileuton, Zafirlukast, Montelukast reduce inflammation.
      • Glucocorticoids: Potent steroids for reducing airway inflammation.

    • Mast Cell Stabilizers: Prevent mast cell degranulation.

      • Nedocromil
      • Cromolyn

    Antihistamines

    • 1st Generation Antihistamines: Cause sedation and include:

      • Ethanolamines: Carbonoxamine, Dimenhydrinate, Diphenhydramine, Doxylamine.
      • Ethylaminediamines: Pyrilamine, Tripelennamine.
      • Piperazines: Hydroxyzine, Cyclizine, Meclizine.
      • Alkylamines: Brompheniramine, Chlorpheniramine.
      • Phenothiazines: Promethazine.
      • Methylpiperidine: Cyproheptadine.

    • 2nd Generation Antihistamines: Less sedating and include:

      • Piperidines: Fexofenadine.
      • Miscellaneous: Loratadine, Cetirizine.

    Stages of Anesthesia: Guedel's Signs

    • Stage I: Analgesia and amnesia; occurs from general anesthesia induction until loss of consciousness.
    • Stage II: Excitement phase; characterized by delirium, increased blood pressure (BP), and respiratory rate (RR).
    • Stage III: Surgical anesthesia; patient is unconscious, exhibits normal BP and RR, muscle relaxation, and absence of eye reflexes.
    • Stage IV: Medullary paralysis; involves respiratory depression and can lead to death.

    Inhalational Anesthetics

    • Gaseous anesthetic: Nitrous oxide.
    • Volatile liquid anesthetics include:
      • Halothane
      • Enflurane
      • Isoflurane
      • Desflurane
      • Sevoflurane
      • Methoxyflurane

    Intravenous Anesthetics

    • Types of intravenous anesthetics:
      • Barbiturates: Thiopental, methohexital.
      • Benzodiazepines: Midazolam, diazepam.
      • Opioid analgesics: Morphine, fentanyl, sufentanil, alfentanil, remifentanil.
      • Propofol.
      • Ketamine.
      • Miscellaneous drugs: Droperidol, etomidate, dexmedetomidine.

    Local Anesthetics

    • Routes of administration for local anesthetics:
      • Topical application.
      • Infiltration.
      • Field block.
      • Nerve block.
      • Intravenous regional anesthesia.
    • Notable local anesthetics:
      • Bupivacaine: Most cardiotoxic.
      • Lidocaine, chloroprocaine: Most neurotoxic.
      • Prilocaine: Associated with hemolytic anemia.
      • Cocaine: Limited use in practice.

    Classifications of Hypertension

    • Primary Hypertension: High blood pressure without an identifiable cause, accounts for 90-95% of cases.
    • Secondary Hypertension: Results from other medical conditions impacting kidneys, arteries, heart, or endocrine system.

    Anti-Hypertensive Agents

    • Diuretics: Promote urinary sodium excretion; various classes.
    • Sympathoplegic Agents: Include beta-blockers, alpha-1 blockers, and alpha-2 agonists that reduce sympathetic outflow.
    • Calcium Channel Blockers: Block calcium influx in cardiac and smooth muscle to lower blood pressure.
    • Direct Vasodilators: Relax blood vessels directly, reducing total peripheral resistance.
    • Agents Affecting Angiotensin: ACE inhibitors and ARBs block production/action of angiotensin.

    Diuretic Classes

    Thiazide Diuretics

    • Site: Distal convoluted tubule.
    • Examples: Bendroflumethiazide, Chlorothiazide, Hydroflumethiazide.
    • Side Effects: Hyponatremia, hypokalemia, hypercalcemia, hyperuricemia, hyperglycemia, hyperlipidemia.

    Loop Diuretics

    • Site: Thick ascending limb of the Loop of Henle.
    • Examples: Furosemide (Lasix), Torsemide, Bumetanide, Ethacrynic acid.
    • Side Effects: Ototoxicity, hyperuricemia, hypokalemia, metabolic alkalosis.

    Potassium-Sparing Diuretics

    • Site: Late distal tubule and collecting ducts.
    • Examples: Spironolactone, Eplerenone, Amiloride, Triamterene.
    • Side Effects: Hyperkalemia, menstrual abnormalities, gynecomastia.

    Aquaretics

    • Function: Increase water excretion.
    • Examples: Mannitol, Glycerin, Urea.
    • Side Effects: Dehydration, hypernatremia.

    Carbonic Anhydrase Inhibitors

    • Site: Proximal tubule.
    • Examples: Brinzolamide, Acetazolamide, Methazolamide, Dorzolamide.
    • Side Effects: GI upset, metabolic acidosis, urinary infrequency, renal calculi, drowsiness.

    Vasodilators

    • Function: Relax smooth muscle, reduce total peripheral resistance.
    • Oral long-term use: Minoxidil (hirsutism), Hydralazine (SLE).
    • Parenteral use in emergencies: Sodium nitroprusside, Diazoxide, Fenoldopam.

    Calcium Channel Blockers

    • Binding: Highly protein-bound with significant volume distribution.
    • Examples:
      • Verapamil: 5.5 L/kg
      • Diltiazem: 5.3 L/kg
      • Nifedipine: 0.8 L/kg
    • Manifestations: Hypotension and AV & SA node block.

    ACE Inhibitors

    • Function: Potent vasodilators.
    • Uses: Treat hypertension, heart failure, and diabetic nephropathy.
    • Adverse Reactions: Anorexia, hyperkalemia, polyuria, oliguria, dry cough.

    Angiotensin II Receptor Blockers (ARBs)

    • Suffix: -sartan.
    • Usage: Alone or in combination therapy.
    • Adverse Reactions: Cough, angioedema.
    • Examples: Candesartan, Irbesartan, Losartan, Telmisartan, Olmesartan, Valsartan.
    • Contraindications: Pregnancy, associated with fetal abnormalities.

    Alpha-2 Agonists

    • Effect: Decrease sympathetic outflow.
    • Examples: Methyldopa, Clonidine, Guanabenz, Guanfacine.

    Adrenoceptor Antagonists

    • Beta Blockers and Alpha-1 Blockers: Used for hypertension and BPH.
    • Side Effects: Syncope, first dose phenomenon; recommend administering small doses at night.

    Ganglion-Blocking Agents

    • Examples: Mecamylamine, Trimethaphan.
    • Mechanism: Block nicotinic cholinoceptors in postganglionic neurons.
    • Adverse Effects: Orthostatic hypotension, erectile dysfunction, constipation, blurred vision, urinary retention, dry mouth.

    Angina

    • Chest pain or discomfort resulting from coronary heart disease, primarily due to ischemia (insufficient oxygenated blood).
    • Ischemia leads to increased oxygen demand and decreased oxygen supply, affecting blood vessels.
    • Two types specifically affected:
      • Myocardial ischemia: Inadequate oxygenated blood supply to the heart.
      • Cerebral ischemia: Insufficient blood supply to the brain, potentially leading to stroke and paralysis.

    Types of Angina

    • Stable Angina:

      • Known as effort or classic angina; most prevalent form.
      • Occurs during physical exertion, common in smokers and hypertensive patients.
      • Caused mainly by atherosclerosis.

    • Unstable Angina:

      • Known as angina at rest; occurs unexpectedly, often at night.
      • Linked to atherosclerosis and thrombosis.

    • Variant Angina (Prinzmetal's Angina):

      • Severe angina occurring at rest, predominantly nighttime or early morning.

    Antianginal Drugs

    • Organic nitrates: Improve blood flow by vasodilation.
    • Calcium Channel Blockers (CCBs): Used in hypertensive patients for long-term control.
    • Beta Blockers: Manage chronic angina and reduce heart workload.
    • Ivabradine & Nicorandil: Alternative therapies for angina management.
    • Acute Treatment of Vasospastic Angina:
      • Primary drug: Nitroglycerin.
      • Alternatives: Propranolol combined with nifedipine, or verapamil/diltiazem for unstable angina.

    Sildenafil

    • A vasodilator for managing erectile dysfunction and angina.
    • Works as a phosphodiesterase type 5 inhibitor (PDE5), increasing CGMP and promoting vascular relaxation.

    Arrhythmia

    • Defined as abnormal heart rhythm, affecting the firing rate or regularity of cardiac impulses.
    • Normal rhythm ranges from 60-90 beats per minute, primarily regulated by the SA Node.

    Antiarrhythmic Drugs

    • Type I: Sodium Channel Blockers (e.g., Quinidine, Lidocaine, Flecainide).
    • Type II: Beta Blockers (e.g., Sotalol).
    • Type III: Potassium Channel Blockers (e.g., Amiodarone).
    • Type IV: Calcium Channel Blockers (e.g., Verapamil, Diltiazem).

    Heart Failure

    • Characterized by the left ventricle's inability to pump sufficient oxygenated blood.
    • Can lead to hospitalization due to inadequate blood supply.

    Heart Failure Functional Classes

    • Class I: Asymptomatic, no physical activity limitation.
    • Class II: Mild to moderate limitation, relieved at rest.
    • Class III: Marked limitation, symptoms during rest.
    • Class IV: Symptoms triggered by any physical activity.

    Forms of Heart Failure

    • Low Output Heart Failure: Most common; heart can't meet metabolic demands.
    • High Output Heart Failure: Related to metabolic disorders such as hyperthyroidism or anemia.

    Heart Failure Treatment

    • Inotropic Agents: Increase the force of heart contractions (e.g., Digoxin).
    • Diuretics: Reduce fluid overload (e.g., Thiazide or loop diuretics).
    • Vasodilators: Alleviate pulmonary congestion, particularly in left-sided heart failure (e.g., organic nitrates).
    • ACE Inhibitors: First-line treatment to prevent cardiac hypertrophy (e.g., Captopril).
    • Beta Blockers: For chronic heart failure management (e.g., Carvedilol).

    Dyslipidemia

    • Imbalance of lipoproteins, affecting cholesterol levels (LDL increases, HDL decreases).
    • Statins: Inhibit cholesterol synthesis, the cornerstone for lowering LDL levels.
    • Common statins include Atorvastatin, Simvastatin, and Rosuvastatin.

    Bile Acid Binding Resins

    • Used to prevent absorption of cholesterol; commonly includes cholestyramine and cholestipol.

    Niacin

    • Vitamin B3 reduces LDL and VLDL levels and has a vasodilatory effect.
    • Known side effect includes flushing, managed by aspirin.

    Thyroid and Antithyroid Drugs

    • Hypothyroidism: Managed with Levothyroxine as the drug of choice.
    • Hyperthyroidism: Treated with Thioamides (Methimazole, PTU) and other therapies.

    Insulin and Oral Hypoglycemic Agents

    • Types of Insulin:
      • Rapid Acting: Insulin lispro, aspart, glulisine.
      • Long Acting: Insulin glargine, detemir.
    • Oral agents: Includes sulfonylureas, meglitinides, thiazolidinediones, and others.

    Summary of Important Drugs

    • Epinephrine: First line for anaphylactic shock and cardiac stimulant.
    • Metformin: First-line for type 2 diabetes, especially in obese patients.
    • Statins: Mainstay in hypercholesterolemia management.
    • Beta Blockers: First-line for chronic stable angina pectoris (CSAP).

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Related Documents

    Pharmacology Lecture 2024 PDF
    Pharmacology Lecture Notes PDF
    Pharmacology Quiz PDF
    Drug Response & Interactions PDF
    Autacoids PDF
    Serotonin Agonists and Antagonists PDF
    Eicosanoids PDF
    Autonomic Nervous System PDF
    Neurotransmission Notes PDF
    Neurotransmitter Acetylcholine PDF
    Neurological Disorders: Parkinson's & Schizophrenia (PDF)
    Anti-Ulcer Drugs, NSAIDs, Gout, Asthma, Antihistamines PDF
    Stages of Anesthesia PDF
    Blood Pressure Categories PDF
    Angina, Heart Failure, and Related Drugs PDF

    Description

    This quiz explores the fundamental concepts of pharmacology, particularly the interactions between drugs and living systems. It covers topics such as drug-receptor bonds and the applications of pharmacology in prevention, diagnosis, and treatment. Test your understanding of how substances affect biological functions.

    More Like This

    Pharmacology Overview and Key Concepts
    12 questions

    Pharmacology Overview and Key Concepts

    TidyPermutation avatar
    TidyPermutation
    Pharmacology: Antagonists Overview
    72 questions

    Pharmacology: Antagonists Overview

    SumptuousSugilite7063 avatar
    SumptuousSugilite7063
    Use Quizgecko on...
    Browser
    Open
    Browser
    Browser