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

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