BMSC2 drug list
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- What types of receptors does acetylcholine interact with?
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this neurotransmitter interacts with
-nicotinic receptors
-muscarinic receptors - Which muscarinic/nicotinic agonists are acetylcholinesterase substrates? (short action duration) Why?
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-acetylcholine
-methacholine
both have an ester group - Which muscarinic/nicotinic agonists are not acetylcholinesterase substrates? (long action duration) Why?
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-carbachol
-bethanechol
both have an amide group instead of an ester group - What is edrophonium?
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this drug is:
-reversible competitive inhibitor of cholinesterase (very short duration)
-used in diagnosis of myasthenia gravis - What is DFP (diisopropyl-fluorophosphate)?
- this drug is an irreversible inhibitor of cholinesterase (long term inhibition)
- What is neostigmine?
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this drug is:
-carbamate inhibitor of cholinesterase (intermediate duration of action)
-binds covalently but bond is readily hydrolyzed - Which drugs are antimuscarinic (anticholinergic) agents?
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-atropine
-scopolamine
-methylatropine
-ipratropium - What is trimethaphan?
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this drug is:
-short acting ganglionic blocking agent
-used during surgery to produce controlled hypotension - What is atypical plasma cholinesterase?
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-lacks the ability to hydrolyze carboxylic ester bonds in drugs
-causes slowed metabolism of drugs containing carboxylic esters - Why does methacholine at low doses produce miosis in dysautonmia patients but not in normal patients?
- this disease involves small-fiber peripheral neuropathy → supersentized to methacholine (normal patients are not supersensitized)
- What are common effects of muscarinic agonists?
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this category of drugs often causes:
-bradycardia (direct effect)
-vasodilation
-reflex tachycardia (indirect effect)
-increased secretions of fluids → dehydration
-bronchoconstriction
-increase in peristaltic activity → diarrhea
-pupillary constriction
-loss of accomodation → blurred vision - What are common side effects of antimuscarinic (anticholinergic) agents?
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side effects of this type of drug:
-paralysis of accomodation to near objects (cycloplegia)
-increased heart rate
-reduced secretion of fluids
-reduced GI/bladder motility → constipation, urinary retention
-reduced bronchial mucous secretion
-bronchodilation
-CNS: sedation, memory loss, psychosis (high doses) - What types of receptors does norepinephrine interact with?
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this neurotransmitter:
-interacts with α and β1 receptors at low dose
-interacts with β2 receptors at high dose - What types of receptors does epinephrine interact with?
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this neurotransmitter:
-interacts with β1 and β2 receptors at low dose
-interacts with α receptors at high dose - What types of receptors does isoproterenol interact with?
- this drug interacts with β1 and β2 receptors only
- What is phenylephrine?
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-this drug is an α1-agonist
-causes vasoconstriction → reflex bradycardia - Which drugs are usually given as bronchodilators?
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β2 agonists are usually used for this purpose.
examples:
-terbutaline
-albuterol - What is dobutamine?
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this drug is:
-β1 agonist
-increases force and rate of heart contraction - What is the mechanism of action of amphetamine?
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-indirect acting sympathomimetic
-displaces NE, Epi, DA from storage sites in presynaptic nerve terminals - What is phentolamine?
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-direct receptor sympatholytic
-α blocker - What is propanolol?
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-direct receptor sympatholytic
-β blocker (non selective) - What is clonidine?
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-central sympathetic depressant (sympatholytic)
-α2 agonist - What is reserpine?
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-adrenergic neuronal blocking agent (sympatholytic)
-interferes with synthesis and release of NE consequent to nerve stimulation - What are two examples of MAO inhibitors? What is their effect?
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-parglyine
-tranylcypromine
this category of drugs enhances NE and Epi effects - What is the mechanism of action of cocaine?
- this drug causes strong dopamine reuptake inhibition → exaggerate adrenergic response
- What is the mechanism of action of tricyclic antidepressants?
- these category of drugs causes strong NE and/or 5-HT reuptake inhibition → exaggerate adrenergic response
- What is yohimibine?
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-indirect acting sympathomimetic
-α2 blocker
-increase NE release
-increase sympathetic tone (CNS) - What are general sympathomimetic effects on nonvascular smooth muscle?
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these drugs have the following effects on nonvascular smooth muscle:
-bronchial smooth muscle (β relax, α constrict)
-stomach and intestine (α and β, relax)
-contraction of anal sphincter
-pupil dilation
-urinary retention
-increase force and rate of heart contraction
-uterus (β2, relax) - What are general sympathomimetic effects on vascular smooth muscle?
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these drugs have the following effects on vascular smooth muscle:
-vessels of skin, brain, splanchnic, mucus membranes (α, constrict)
-vessels of visceral organs including kidney and skeletal muscles (β2, dilate) - What are side effects of all sympatholytic agents?
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side effects of this category of drugs include:
- ↓GFR → increase in blood volume and NA+ retention
-sedation and depression (if it gets in CNS) - What are side effects of α-blockers, CNS sympathetic depressants, and adrenergic neuronal blockers?
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these categories of drugs have the following side effects:
-nasal stuffiness
- ↑GI motility and diarrhea - What side effects occur only with α-blockers?
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these drugs have the following side effects:
-postural hypotension → reflex tachycardia
-impaired ability to ejaculate
-in CNS: akinesia, loss of spontaneous motion, rigidity, tremor - What are the effects of β blockers?
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these drugs have the following effects:
-bradycardia
-decreased cardiac output
-impairment of insulin release (sometimes)
-bronchoconstriction
-blocks some symptoms of hyperthyroidism
-increase in triglycerides and decrease in HDL
-cold extremities - How does digitalis increase cardiac contractility?
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this drug:
-inhibits Na/K pump
-causes higher intracellular Ca2+ - How do β adrenergic agonists increase cardiac contractility?
- these stimulate Ca channel and SR Ca pump via cAMP (G protein pathway)
- How does caffeine increase cardiac contractility? What is another drug that has the same mechanism of action?
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-this drug stimulates Ca channel and SR Ca pump via cAMP (phosphodiesterase inhibition)
-milrinone works the same way - Which types of drugs decrease MVO2 (myocardial oxygen consumption)?
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-β1 blockers (decrease cardiac output)
-nitrates (vasodilate peripheral resistance)
-diuretics (decrease afterload)
-ACE inhibitors (decrease afterload) - What is captopril?
- this drug is an example of an ACE inhibitor
- Which types of drugs increase MVO2 (myocardial oxygen consumption)?
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-β1 agonists (increase cardiac output)
-vasoconstrictors - What are furosemide and bumetanide? What is their mechanism of action and what side effects do they produce?
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-these drugs are loop diuretics; they inhibit the NKCC2 transporter in the thick ascending limb
-side effects: hypokalemic metabolic acidosis - What is the mechanism of action of thiazide diuretics? What side effects do they cause?
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-these drugs inhibit the Na-Cl transporter in the distal convoluted tubule and collecting duct
-side effects: hypokalemic metabolic alkalosis - What is acetazolamide? What are the side effects?
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-this drug blocks carbonic anhydrase in the proximal tubule → blocks absorption of HCO3-
-side effects: acidosis, urine increases in K+ and PO4- - What is aldactone? What side effects does it produce?
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-this drug blocks aldosterone in the distal tubule and collecting duct
-spares K+ and enhances Na+ loss → diuresis
-side effects: hyperkalemic metabolic acidosis