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Mechanisms of action
| Question | Answer |
|---|---|
| What is the mechanism of action of amiodarone? | Amiodarone blocks potassium channels, prolonging phase 3 repolarization and increasing action-potential duration and refractory period. It also has sodium-channel, calcium-channel, and noncompetitive β-blocking effects, |
| What is the mechanism of action of epinephrine? | Epinephrine is a potent α- and β-adrenergic agonist that causes peripheral vasoconstriction via α1, increases heart rate and contractility via β1, and produces bronchodilation via β2 activation. |
| How does ephedrine work? | Ephedrine indirectly increases norepinephrine release from sympathetic nerve terminals and also weakly stimulates α and β receptors directly, increasing heart rate, blood pressure, and bronchodilation. |
| What is the mechanism of action of atropine? | Atropine is a competitive muscarinic acetylcholine receptor antagonist that blocks parasympathetic activity. In the heart, it increases SA node firing and AV conduction by inhibiting vagal tone. |
| How does albuterol cause bronchodilation? | Albuterol selectively stimulates β2-adrenergic receptors in bronchial smooth muscle, increasing cAMP via adenylate cyclase activation and causing smooth-muscle relaxation. |
| What is the mechanism of action of aspirin? | Aspirin irreversibly inhibits COX-1 and COX-2, blocking prostaglandin and thromboxane synthesis. Platelet inhibition lasts for the platelet’s entire lifespan because platelets cannot regenerate COX-1. |
| Why is esmolol useful in acute cardiac settings? | Esmolol is an ultra-short-acting, cardioselective β1-blocker that reduces heart rate, contractility, and AV nodal conduction. It is rapidly metabolized by red-blood-cell esterases, allowing tight titration. |
| What receptors does labetalol block? | Labetalol blocks β1, β2, and α1 receptors, decreasing heart rate and systemic vascular resistance. α1 blockade lowers blood pressure with minimal reflex tachycardia. |
| How does lidocaine act as an antiarrhythmic? | Lidocaine is a class Ib antiarrhythmic that blocks fast sodium channels, shortening action-potential duration in ventricular myocardium and preferentially suppressing ischemic or depolarized tissue. |
| What are the key pharmacologic effects of diphenhydramine? | Diphenhydramine is a first-generation H1 antagonist that blocks histamine-mediated allergic responses and has anticholinergic effects, causing sedation and drying of secretions. |
| What is the mechanism of action of dexamethasone? | Dexamethasone is a potent glucocorticoid that binds intracellular receptors to alter gene transcription, reducing inflammatory cytokines, capillary permeability, and tissue edema. |
| How does naloxone reverse opioid overdose? | Naloxone is a competitive μ-opioid receptor antagonist that rapidly reverses opioid-induced respiratory depression and CNS effects; repeat dosing may be needed due to its short duration. |
| What is the mechanism of action of flumazenil? | Flumazenil competitively inhibits benzodiazepine binding at the GABA-A receptor, reversing sedation and respiratory depression; its short half-life may require redosing. |
| How does adenosine terminate supraventricular tachycardia? | Adenosine activates A1 receptors in the AV node, opening potassium channels and hyperpolarizing tissue, transiently blocking AV conduction and interrupting re-entrant SVTs. |