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

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