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

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Created May 3, 2010ReportNominate
Tags:description, drug