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

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