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

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Created May 3, 2010ReportNominate
Tags:description, drug