Drugs MVST IB - part 1

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Can you name the drugs from MVST IB - part 1?

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DescriptionDrug nameUse
Cholinergic agonist - +-isomer hydrolysed by AChE
Causes development of new blood vessels
Potassium-sparing diuretic - blocks apical Na+ channels in late distal tubule
Arteriolar vasodilator - unknown mechanism
Irreversibly alkylates muscarinic receptor
Cardiac glycoside - inhibits Na/K-ATPase
Calcium channel agonist - dihydropyridine
Nitrovasodilator - produces NO
ACE inhibitor - prodrug, must be metabolised in liver
Calcium channel antagonist - dihydropyridine - affects L-type but not T-type channels
Local anaesthetic - uncharged
Uncompetitive inhibitor of phosphatase acting on IP1 --> inositol
Orally-acting hypoglycaemic agent - sulphonylurea
Selective beta-1 antagonist (slight effect on beta-2)
Single chain recombinant human tissue plasminogen activator
Non-peptide inhibitor of glycoprotein IIb/IIIa receptor
Selective beta-2 antagonist (slight effect on beta-1)
Nicotinic receptor antagonist - relatively non-selective between NMJ and ganglion at clinical doses
Tyrosine kinase inhibitor
Glucocorticoid receptor agonist
Phosphodiesterase III inhibitor - inodilator
Blocks If current in SA node
Reverse inhibition of AChE by organophosphorus agents
Binds to SNAREs involved in membrane fusion, preventing ACh release
Blocks release of neurotransmitter via phospholipase A2 - localises to membrane by K channel binding moiety
Calcium channel blocker - phenylalkylamine - class IV antidysrhythmic
Osmotic diuretic - filtered at glomerulus, not reabsorbed
Selective MAO-A inhibitor
Selective antagonist for M3 muscarinic receptor
Depolarising blocker selective for NMJ nicotinic receptor - very short duration of action, broken down by BuChe - deficiency in enzyme activity can lead to prolonged action
Glucocorticoid receptor antagonist
Selective alpha-1 antagonist (slight effect on alpha-2)
Anion exchange resin - prevents reuptake of bile acids from intestine
K channel opener
Reversible anticholinesterase - ionic interaction
Thiazide diuretic - blocks Na/Cl transport in early distal tubule
Inhibits intestinal absorption of cholesterol - circulates enterohepatically
Binds to neurexins, causing massive ACh release from nerve terminals
Carbonic anhydrase inhibitor
Beta-1 antagonist used in heart failure
Irreversible alpha-adrenoceptor antagonist - blocks Uptake 2 (and Uptake 1 at 10x higher concs)
ADP-ribosylates alpha-i - prevents activation of Gi in response to stimulation
Depolarising blocker at NMJ
Non-selective phosphodiesterase inhibitor
Intracellular tetravalent polyamine - helps produce inward rectification of K+ channels
Acts on imidazoline receptors
Mineralocorticoid receptor antagonist - potassium-sparing diuretic
Selective MAO-B inhibitor
Irreversible antagonist at nicotinic NMJ receptors (no effect on ganglionic receptors)
NOS inhibitor - not very selective for different forms
Alpha-2 antagonist (some effect on alpha-1)
Cholinergic agonist - not selective between nicotinic/muscarinic receptors
DescriptionDrug nameUse
Quaternary local anaesthetic analogue - only effective if perfused inside cells
Class IC antidysrhythmic
Angiotensin II partial agonist
Non-specific endothelin receptor antagonist
Estrogen receptor agonist
Inhibits clotting by inhibiting synthesis of factors II, VII, IX, IX and regulatory proteins C, S, Z
COMT inhibitor
alpha-1 antagonist most commonly used
Muscarinic receptor antagonist - very long duration of action
Calcium channel blocker - benzothiazepine
Indirectly acting sympathomimetic amine - converted to octopamine by DBH - found in various foodstuffs
Class III antidysrhythmic - prolongs AP and refractory period
Blocks uptake of choline into neurons
Blocks release of NA evoked by APs (repeated low doses/aftermath of large dose) - indirect sympathomimetic actions (large doses)
Local anaesthetic - slow onset/offset - use dependence at low rates of stimulation - class IA antidysrhythmic
Indirectly-acting sympathomimetic amine - weak inhibitor of MAO
Local anaesthetic - weak base - use-dependence and voltage-dependence
Interferes with normal function of microtubule growth
Selective non-depolarising neuromuscular blocker at NMJ - ester, broken down by spontaneous hydrolysis and plasma esterases
K channel opener - also hirsutism effects
Selective beta-2 agonist (slight effect on beta-1)
Use-dependent block of ganglionic transmission
Depolarising blocker selective for ganglion nicotinic receptor
K channel opener
Competitively inhibits plasminogen activation - inhibits severe bleeding from excessive clot lysis
PPAR-gamma agonist
Binds very tightly to VMAT-2, preventing loading of catecholamines into vesicles
Beta-1 antagonist used in heart failure
Mild partial beta-1 agonist
Inhibits DOPA decarboxylase in periphery
Non-selective beta-adrenoceptor antagonist
Converted to alpha-methylNA - released as false transmitter - more potent at alpha-2, less potent at alpha-1
Orally-acting hypoglycaemic agent - sulphonylurea
Progestagen receptor antagonist
SSRI - blocks 5-HT transporter in Uptake 1
Inodilator used to treat canine dilated cardiomyopathy - calcium sensitiser
Double chain recombinant human tissue plasminogen activator
NSAID used to prevent thrombosis
Potassium-sparing diuretic - blocks apical Na+ channels in late distal tubule
A1 receptor antagonist - non-selective phosphodiesterase inhibitor
Selective alpha-2 agonist
Medium 'reversible' anticholinesterase - binds to esteratic site and carbamoylates ACh
Non-peptide angiotensin II antagonist - acts on AT1 receptors
Loop diuretic - blocks Na/K/2Cl transport in thick ascending limb
Competitive antagonist for ganglionic nicotinic receptors - inactive at NMJ
Potent, irreversible inhibitor of iNOS in activated macrophages
Irreversible anticholinesterase - activated by replacement of sulphur atom with oxygen, deoxified by plasma carboxylesterases
Nitrovasodilator - produces NO - taken sublingually
Non-selective alpha-adrenoceptor antagonist
Plasminogen + anisoylated streptokinase
Illegal drug - blocks NET
Acts on imidazoline receptors
DescriptionDrug nameUse
Calcium sensitiser - increases cardiac Ca2+ binding efficiency to troponin - inhibits phosphodiesterase III
Tricyclic antidepressant - blocks NET
K channel opener - also NO donor
Used experimentally to inhibit dopamine beta-hydroxylase - also inhibits aldehyde dehyddrogenase
Partial agonist at alpha-adrenoceptors - 5-HT agonist
ACE inhibitor
Non-selective phosphodiesterase inhibitor
Binds to plasminogen activator, increasing generation of plasmin
Competitive antagonist for ganglionic nicotinic receptor - inactive at NMJ
Local anaesthetic (ester, weak base) - broken down by BuChE
Blocks transport of adenosine into cells - phosphodiesterase type V inhibitor
ADP-ribosylates alpha-s - inhibits GTPase activity - sustained activation of adenylyl cyclase
Experimental cardiac glycoside
Slightly selective alpha-2 agonist (also alpha-1 actions) - omitting dose can lead to rebound hypertension
Phosphodiesterase III inhibitor - inodilator
Non-selective agonist for muscarinic receptors
Naturally occurring anticoagulant produced by basophils/mast cells - exposes active site of antithrombin III
Direct acting vasodilator - metabolised to NO or cyanide
Beta-adrenoceptor agonist
Regulates expression of multiple angiogenic genes
Non-selective agonist for muscarnic receptors
Monoclonal antibody against glycoprotein IIb/IIIa receptor - prevents platelet aggregation - also binds to vitronectin receptor
Selective inhibitor of NOS in neurons
Selective alpha-1 agonist (some action on beta-1)
Irreversible anticholinesterase - organophosphorus agent
Beta-1 agonist - weak beta-2 agonist
Mineralocorticoid receptor agonist
Co-released with NA or ACh - acts on purinoceptors (P2 > P1)
Competitive inhibitor of tyrosine hydroxylase
Selective antagonist for M1 muscarinic receptors
Involved with providing new blood flow to ischaemic tissues
Non-selective, reversible MAO inhibitor
Competitively inhibits plasminogen activation - inhibits severe bleeding from excessive clot lysis
Combined alpha- and beta-adrenoceptor antagonist
Blocks Na channels from exterior - no use-dependence
Nitrovasodilator - produces NO - metabolised in liver to active drug
Inhibits platelet activation by inhibiting binding of ADP to its receptor on platelets
Immunosuppressant drug with antiproliferative effects
Estrogen receptor antagonist
Selective inhibitor of phosphodiesterase type V (selectively breaks down cGMP)
Progestagen receptor agonist
Inhibits HMG-CoA reductase - also many pleiotropic effects
Blocks transporter carrying ACh into storage vesicles
Selective alpha-2 antagonist (slight effect on alpha-1)
Tricyclic antidepressant - blocks NET
Cyclic heptapeptide inhibitor of glycoprotein IIb/IIIa receptor
Muscarinic receptor agonist
Very potent alpha-2 agonist
Selective non-depolarising neuromuscular blocking agent at NMJ - long action, not hydrolysed
Inhibits liver triglyceride production and VLDL secretion - increases levels of tissue plasminogen activator
Lowers VLDL (and LDL) by stimulating lipoprotein lipase - may activate PPARs
Binds to synaptobrevin to prevent vesicle release from inhibitory interneuron synapses with motor neurons

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