Pharmacology Basics
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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).

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    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.

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