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

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