Podcast
Questions and Answers
What is the primary action of Isoproterenol on the heart?
What is the primary action of Isoproterenol on the heart?
- Increase diastolic blood pressure
- No effect on heart rate
- Decrease heart rate and contractility
- Increase heart rate and contractility (correct)
Which receptor does Phenylephrine selectively act upon?
Which receptor does Phenylephrine selectively act upon?
- B2 receptor
- a2 receptor
- a1 receptor (correct)
- B1 receptor
What is a caution associated with the use of Phenylephrine in elderly patients?
What is a caution associated with the use of Phenylephrine in elderly patients?
- Increased risk of hypertension (correct)
- Increased risk of hypotension
- Increased risk of arrhythmias
- Lowered effectiveness as a nasal decongestant
What effect does stimulation of B2 receptors have on total peripheral resistance (TPR)?
What effect does stimulation of B2 receptors have on total peripheral resistance (TPR)?
Which of the following statements about selective drugs is accurate at high concentrations?
Which of the following statements about selective drugs is accurate at high concentrations?
What is the primary effect of MAO inhibitors in treating Parkinson's disease?
What is the primary effect of MAO inhibitors in treating Parkinson's disease?
What condition may result from consuming foods high in tyramine while on MAO inhibitors?
What condition may result from consuming foods high in tyramine while on MAO inhibitors?
What kind of adrenergic receptors does Ephedrine primarily act on?
What kind of adrenergic receptors does Ephedrine primarily act on?
Which effect is NOT associated with the use of alpha blockers?
Which effect is NOT associated with the use of alpha blockers?
Which side effect is most commonly associated with the use of non-selective alpha antagonists?
Which side effect is most commonly associated with the use of non-selective alpha antagonists?
What is the main therapeutic use of non-selective alpha antagonists like Phentolamine?
What is the main therapeutic use of non-selective alpha antagonists like Phentolamine?
How do COMT inhibitors function in regards to catecholamines?
How do COMT inhibitors function in regards to catecholamines?
Which of the following is an effect of mixed acting sympathomimetics like Ephedrine?
Which of the following is an effect of mixed acting sympathomimetics like Ephedrine?
What is a potential adverse effect of phenoxybenzamine due to its irreversible action?
What is a potential adverse effect of phenoxybenzamine due to its irreversible action?
What mechanism does Selegiline utilize in treating depression?
What mechanism does Selegiline utilize in treating depression?
What is the primary mechanism of action of artemisinin compounds in treating malaria?
What is the primary mechanism of action of artemisinin compounds in treating malaria?
Which condition can result from the use of sulfadoxine in Fansidar?
Which condition can result from the use of sulfadoxine in Fansidar?
Which antibiotic is commonly used in combination with quinine for treating malaria?
Which antibiotic is commonly used in combination with quinine for treating malaria?
What is the primary effectiveness of primaquine in malaria treatment?
What is the primary effectiveness of primaquine in malaria treatment?
What is a notable side effect of atovaquone?
What is a notable side effect of atovaquone?
Which drug combination is the recommended first line treatment for multidrug-resistant falciparum malaria?
Which drug combination is the recommended first line treatment for multidrug-resistant falciparum malaria?
Which of the following statements about proguanil is true?
Which of the following statements about proguanil is true?
Why is doxycycline not recommended for children?
Why is doxycycline not recommended for children?
What stage of malaria does primaquine specifically target?
What stage of malaria does primaquine specifically target?
Which statement about Fansidar is correct?
Which statement about Fansidar is correct?
What is the primary mechanism of action of Dantrolene?
What is the primary mechanism of action of Dantrolene?
Which of the following is a significant side effect of Tizanidine?
Which of the following is a significant side effect of Tizanidine?
Which adrenergic receptor subtype primarily results in bronchial dilation when stimulated?
Which adrenergic receptor subtype primarily results in bronchial dilation when stimulated?
In which clinical situation is adrenaline primarily utilized?
In which clinical situation is adrenaline primarily utilized?
What effect does Noradrenaline have on heart rate?
What effect does Noradrenaline have on heart rate?
What is the function of b3 adrenergic receptors?
What is the function of b3 adrenergic receptors?
What condition is associated with the use of Dopamine at low concentrations?
What condition is associated with the use of Dopamine at low concentrations?
What adverse effect can be anticipated from using Dantrolene?
What adverse effect can be anticipated from using Dantrolene?
Which of the following effects is associated with alpha 1 adrenergic receptors?
Which of the following effects is associated with alpha 1 adrenergic receptors?
Which neurotransmitter is responsible for activating b1 receptors to stimulate the heart?
Which neurotransmitter is responsible for activating b1 receptors to stimulate the heart?
What is the primary clinical use of Dopamine?
What is the primary clinical use of Dopamine?
What effect does stimulation of b2 receptors have on the uterus?
What effect does stimulation of b2 receptors have on the uterus?
Which drug binds non-selectively to all adrenergic receptors?
Which drug binds non-selectively to all adrenergic receptors?
In addition to treating shock, what is a common use of Noradrenaline?
In addition to treating shock, what is a common use of Noradrenaline?
Which of the following pharmacological effects is primarily associated with M2 muscarinic receptors?
Which of the following pharmacological effects is primarily associated with M2 muscarinic receptors?
What is the main therapeutic use of Methacholine?
What is the main therapeutic use of Methacholine?
Which adverse effect is associated with the use of Pilocarpine?
Which adverse effect is associated with the use of Pilocarpine?
What is the mechanism of action of cholinesterase inhibitors?
What is the mechanism of action of cholinesterase inhibitors?
Which receptor type is targeted by Nicotine as a nicotinic agonist?
Which receptor type is targeted by Nicotine as a nicotinic agonist?
What is a significant pharmacological effect of M3 receptor activation?
What is a significant pharmacological effect of M3 receptor activation?
Which of the following is an example of a reversible acetylcholinesterase inhibitor?
Which of the following is an example of a reversible acetylcholinesterase inhibitor?
What is a primary clinical use of Acetylcholine as a drug?
What is a primary clinical use of Acetylcholine as a drug?
What is a characteristic of the pharmacokinetics of Acetylcholine?
What is a characteristic of the pharmacokinetics of Acetylcholine?
Which type of muscarinic receptors facilitate increased gastric secretions and motility?
Which type of muscarinic receptors facilitate increased gastric secretions and motility?
What adverse effect is commonly associated with excessive stimulation of M3 receptors?
What adverse effect is commonly associated with excessive stimulation of M3 receptors?
Which of the following drugs is an example of a nicotinic agonist used for skeletal muscle contraction?
Which of the following drugs is an example of a nicotinic agonist used for skeletal muscle contraction?
What mechanism causes the decrease in intraocular pressure (IOP) when using Pilocarpine?
What mechanism causes the decrease in intraocular pressure (IOP) when using Pilocarpine?
Why is Acetylcholine not frequently used clinically despite its effects?
Why is Acetylcholine not frequently used clinically despite its effects?
What is the primary clinical use of Prazosin?
What is the primary clinical use of Prazosin?
Which drug is preferred for the treatment of benign prostatic hyperplasia (BPH)?
Which drug is preferred for the treatment of benign prostatic hyperplasia (BPH)?
What effect do beta blockers primarily have on the heart?
What effect do beta blockers primarily have on the heart?
Which of the following is an adverse effect of Propranolol?
Which of the following is an adverse effect of Propranolol?
What is an effect of beta-3 adrenergic receptor activation?
What is an effect of beta-3 adrenergic receptor activation?
Which medication is known to have intrinsic sympathomimetic activity (ISA)?
Which medication is known to have intrinsic sympathomimetic activity (ISA)?
What action can Labetalol have during pregnancy?
What action can Labetalol have during pregnancy?
Which drug is specifically indicated for treating hypertension in diabetic patients?
Which drug is specifically indicated for treating hypertension in diabetic patients?
What condition can Chloroquine be used to treat?
What condition can Chloroquine be used to treat?
Yohimbine acts as a selective blocker for which adrenergic receptors?
Yohimbine acts as a selective blocker for which adrenergic receptors?
Which drug is contraindicated in patients with asthma?
Which drug is contraindicated in patients with asthma?
Which condition is Tamsulosin primarily used to treat?
Which condition is Tamsulosin primarily used to treat?
What is a potential adverse effect of using Atenolol?
What is a potential adverse effect of using Atenolol?
What is the mechanism of action of Chloroquine in treating malaria?
What is the mechanism of action of Chloroquine in treating malaria?
Flashcards
Muscarinic Agonists
Muscarinic Agonists
A class of drugs that act as agonists at muscarinic acetylcholine receptors (mAChRs). They mimic the actions of acetylcholine in the parasympathetic nervous system.
Muscarinic Receptors
Muscarinic Receptors
Receptors that are activated by acetylcholine in the parasympathetic nervous system and are primarily found in smooth muscles, glands, and the heart.
Muscarinic Receptor (M1)
Muscarinic Receptor (M1)
Activation of M1 receptors in gastric parietal cells leads to increased gastric secretion and motility.
Muscarinic Receptor (M2)
Muscarinic Receptor (M2)
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Muscarinic Receptor (M3)
Muscarinic Receptor (M3)
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Acetylcholinesterase (AChE)
Acetylcholinesterase (AChE)
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Cholinesterase Inhibitors
Cholinesterase Inhibitors
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Edrophonium
Edrophonium
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Pilocarpine
Pilocarpine
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Nicotinic Agonists
Nicotinic Agonists
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Nicotine
Nicotine
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Suxamethonium Chloride
Suxamethonium Chloride
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Nicotinic Receptor (NM)
Nicotinic Receptor (NM)
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Nicotinic Receptor (NN)
Nicotinic Receptor (NN)
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Indirect Acting Cholinergic Agents
Indirect Acting Cholinergic Agents
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Selective Alpha-1 Receptor Agonist
Selective Alpha-1 Receptor Agonist
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Phenylephrine
Phenylephrine
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Isoproterenol
Isoproterenol
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Decrease in Total Peripheral Resistance (TPR)
Decrease in Total Peripheral Resistance (TPR)
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Tachycardia
Tachycardia
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Direct Acting Sympathomimetics
Direct Acting Sympathomimetics
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Adrenergic Agonist (Sympathomimetic)
Adrenergic Agonist (Sympathomimetic)
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Adrenergic Receptor
Adrenergic Receptor
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Beta-1 Receptors (β1)
Beta-1 Receptors (β1)
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Beta-2 Receptors (β2)
Beta-2 Receptors (β2)
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Alpha-1 Receptors (α1)
Alpha-1 Receptors (α1)
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Alpha-2 Receptors (α2)
Alpha-2 Receptors (α2)
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Non-selective Adrenergic Agonist
Non-selective Adrenergic Agonist
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Adrenaline (Epinephrine)
Adrenaline (Epinephrine)
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Noradrenaline (Norepinephrine)
Noradrenaline (Norepinephrine)
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Dopamine
Dopamine
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Catechol-O-Methyltransferase (COMT)
Catechol-O-Methyltransferase (COMT)
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Monoamine Oxidase (MAO)
Monoamine Oxidase (MAO)
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Dental procedures
Dental procedures
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Anaphylactic Shock
Anaphylactic Shock
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MAO inhibitors (MAOIs)
MAO inhibitors (MAOIs)
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MAO-B inhibitors
MAO-B inhibitors
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COMT inhibitor
COMT inhibitor
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Mixed acting sympathomimetics
Mixed acting sympathomimetics
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Alpha blockers
Alpha blockers
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Non-selective reversible alpha blockers
Non-selective reversible alpha blockers
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Non-selective irreversible alpha blockers
Non-selective irreversible alpha blockers
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Beta blockers
Beta blockers
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Beta-1 selective blockers
Beta-1 selective blockers
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Non-selective beta blockers
Non-selective beta blockers
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Artemisinin Compounds
Artemisinin Compounds
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Prazosin
Prazosin
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Artemisinin-based Combination Therapies (ACTs)
Artemisinin-based Combination Therapies (ACTs)
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Fansidar (Sulfadoxine + Pyrimethamine)
Fansidar (Sulfadoxine + Pyrimethamine)
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Tamsulosin
Tamsulosin
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Antibiotics (Tetracycline, Doxycycline, Clindamycin)
Antibiotics (Tetracycline, Doxycycline, Clindamycin)
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Yohimbine
Yohimbine
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Group II Antimalarials (Proguanil, Atovaquone)
Group II Antimalarials (Proguanil, Atovaquone)
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Primaquine
Primaquine
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Propranolol
Propranolol
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Metoprolol
Metoprolol
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Blood Schizonticides
Blood Schizonticides
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Hemoglobinemia
Hemoglobinemia
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Atenolol
Atenolol
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Pindolol
Pindolol
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Slow Acting Blood Schizonticides
Slow Acting Blood Schizonticides
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Labetalol
Labetalol
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Prophylaxis
Prophylaxis
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Plasmodium Falciparum
Plasmodium Falciparum
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Plasmodium Vivax and Ovale
Plasmodium Vivax and Ovale
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Clinical Cure
Clinical Cure
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Radical Cure
Radical Cure
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Chloroquine
Chloroquine
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Study Notes
Cholinergic Drugs (Parasympathetic)
- Cholinergic drugs mimic the parasympathetic nervous system
- Direct-acting muscarinic agonists:
- Increase secretions (salivation, gastric)
- Bronchoconstriction, miosis (pupil constriction)
- Lower intraocular pressure
- Myocardial suppression
- Acetylcholine:
- Primarily controlled by inhibitory Gi-coupled M2 and excitatory Gq-coupled M3 muscarinic acetylcholine receptors (mAChRs)
- Short duration of action
- Methacholine:
- Non-selective muscarinic receptor agonist
- Increases gastric secretions, suppresses myocardial contraction
- Used to diagnose bronchial hyperreactivity
- Side effects: Bradycardia, hypotension, sweating, flushing
- Pilocarpine:
- Applied locally to eye to induce miosis, lower intraocular pressure, increase secretions
- Used to diagnose bronchial hyperreactivity, and in surgeries requiring miosis
- Side effects: Local irritation, blurred vision, GIT hyperreactivity
- Direct-acting Nicotinic agonists:
- NM (neuromuscular junction) - skeletal muscle contraction
- NN (autonomic ganglia) - facilitate neurotransmission
- Examples: Nicotine, Suxamethonium chloride
Indirect Acting: Cholinesterase Inhibitors
- Inhibit acetylcholinesterase (AChE), causing acetylcholine accumulation
- Reversible short acting: Edrophonium
- Used to diagnose myasthenia gravis
- Increases muscle strength
- Reversible medium acting: Neostigmine
- Treats myasthenia gravis, and paralytic ileus
- Increases strength for hours
- Reversible long acting: Physostigmine
- Treats myasthenia gravis, glaucoma, anticholinergic poisoning
- Longer duration of action
- Irreversible:
- Organophosphates (nerve gases):
- Binds to AChE permanently
- Causes accumulation of acetylcholine
- Organophosphates (nerve gases):
Cholinergic Blockers
- Inhibit the effects of acetylcholine
- Muscarinic antagonists:
- Atropine:
- Reduces secretions (dry mouth)
- Pupil dilation (mydriasis)
- Scopolamine:
- Motion sickness
- Anti-cholinergic toxicity
- Ipratropium:
- Used in COPD
- Side Effects: Restlessness, blurred vision, increased IOP, inhibition of sweat, dry mouth
- Atropine:
- Ganglion blocking agent:
- Hexamethonium:
- Reduces secretions
- Causes muscle weakness and paralysis (at high doses)
- Hexamethonium:
Neuromuscular Blockers
- Non-depolarizing: Tubocurarine
- Used for endotracheal intubation and surgery
- Competitive antagonist, preventing Ach binding
- Blocks ACh receptors, inhibiting neuromuscular transmission
- Depolarizing: Succinylcholine
- Causes initial depolarization, followed by desensitization
- Used for intubation, and muscle relaxation during surgery
Spasmolytics
- Baclofen:
- GABA agonist
- Relieves excitation, relieving muscle spasms
- Tizanidine:
- Acts on alpha-2 receptors to reduce spasticity
- Reducing muscle spasms and pain from multiple sclerosis
Adrenergic Agonists
- a1 receptors:
- Excitatory
- Vasoconstriction, contraction, mydriasis
- a2 receptors:
- Inhibitory
- Inhibition of transmitter release
- b1 receptors:
- Excitatory
- Myocardial stimulation, renin secretion
- b2 receptors:
- Inhibitory
- Muscle relaxation, vasodilation
- b3 receptors:
- Excitatory
- Lipolysis
Adrenergic Antagonists
-
Alpha antagonists:
- Non-selective (phenoxybenzamine, phentolamine):
- Relaxes muscles around prostate
- Used to diagnose and treat pheochromocytoma
- Selective (prazosin, tamsulosin):
- Treats benign prostatic hyperplasia (BPH)
- Selective (Yohimbine):
- Non-selective (phenoxybenzamine, phentolamine):
-
Beta antagonists:
- Non-selective (propranolol):
- Treats hypertension, angina, tremor
- Cardio-selective (metoprolol, atenolol):
- Treats hypertension, angina
- Intrinsic sympathomimetic activity (ISA) (pindolol, acebutolol):
- Non-selective (propranolol):
Drugs for Malaria
-
Chloroquine:
- Effective against erythrocytic stages
- Large Vd and extensive tissue binding
- Blocks parasite's food source
-
Quinine:
- Treats severe and resistant P. falciparum malaria, RA
- Higher sensitivity in CQ resistant parasites
-
Artemisinin compounds:
- Generates highly reactive free radicals, effective against all stages
-
Sulfadoxine-pyrimethamine:
- Effective against all stages
- Inhibits DHPS and DHFR
Antibiotics (for Malaria, not for general infection)
- Group II:
- Tetracycline/doxycycline/clindamycin
- Inhibit protein synthesis
- Group III
- Primaquine (Inhibits respiratory processes, effective against primary and latent hepatic stages)
- Proguanil (Blocks parasite reproduction)
- Atovoquone (Interferes with parasite mitochondrial function; effective against the primary liver forms)
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