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

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