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year 3 formulary

TermDefinition
allopurinol <synthesis of uric acid by competitive inhibition of xanthine oxidase. Some inhibition of de novo purine synthesis.Converted to alloxanthine by xanthine oxidase,is effective noncompetitive inhibitor of the enzyme&produces most of therapeutic effect.
methotrexate Immunomodulator and inhibitor of tetrahydrofolate dehydrogenase, thus preventing formation of tetrahydrofolate that is necessary for synthesis of thymidylate, an essential component of DNA.
cetirizine Competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. Penetrates CNS less well than chlorpheniramine so less sedating.
dexamethasone Binds with high affinity to specific cytoplasmic receptors to produce inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, and suppression of humoral immune responses
charcoal, activated Adsorbs several drugs and toxins, and used in treatment of poisoning with certain agents
amoxicillin + clavulanic acid (co-amoxiclav) Clavulanate competitively and irreversibly inhibits wide variety of beta-lactamases produced by certain bacteria, making drug combination more potent.
flucloxacillin Flucloxacillin stable against hydrolysis by variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases
Cefotaxime Inhibition of cell wall synthesis via a penicillin-binding proteins. Displays resistance to penicillinases so useful to treat penicillin resistant
nitrofurantoin Inhibits bacterial acetyl-coenzyme A, interfering with organism's carbohydrate metabolism. Can also disrupt bacterial cell wall formation
oxytetracycline Reversibly binds to 30S ribosomal subunit and prevents amino-acyl tRNA from binding to the A site of the ribosome, inhibiting translation and thus cell growth
vancomycin glycopeptide antibiotic which acts by inhibiting cell wall synthesis.
ethambutol Inhibits transfer of mycolic acids into cell wall of tubercle bacillus
isoniazid Prodrug, which once activated, inhibits synthesis of mycolic acids (essential component bacterial cell wall)
pyrazinamide Mechanism unclear. Metabolite (pyrazinoic acid) may lower intrabacterial pH to level that could inactivate vital target enzyme (e.g. fatty acid synthase.
rifampicin inhibits DNA-dependent RNA polymerase activity in bacillus
nystatin Binds to sterols in cell membrane of susceptible species, resulting in increased membrane permeability and subsequent leakage of intracellular components.
aciclovir As triphosphate, competitively inhibits viral DNA polymerase and competes with natural deoxyguanosine triphosphate for incorporation into viral DNA, thus acting as chain terminator
ciclosporin Binds to cyclophillin to form complex that inhibits calcineurin, the enzyme that activates of transcription of
ferrous salt Essential element in synthesis of haemoglobin (as well as myoglobin, cytochromes and other enzymes).
folic acid Critical cofactor in enzymatic reactions required for DNA synthesis. Acts as carbon donor in the conversion of deoxyuridine to deoxythymidine.
hydroxocobalamin Analogue of vitamin B12, which is converted to cobalamin, cofactor for homocysteine-methionine methyltransferase, which transfers methyl group from methyltetrahydrofolate to homocysteine to make methionine and thus ensure normal activation of folate.
clopidogrel Prodrug, active metabolite of which prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex
dipyridamole Inhibits both adenosine deaminase and phosphodiesterase, preventing degradation of cAMP, an inhibitor of platelet function. Elevation in cAMP blocks release of arachidonic acid from membrane phospholipids and reduces thromboxane A2 activity.
Glycerl trinitrate Converted to NO,activates guanylate cyclase.Stimulates guanosine 3', 5’-monophosphate (cGMP) which activates kinase phosphorylations in SM cells= dephosphorylation of SM myosin light chains. release of CA = relaxation of SM cells&vasodilation.
isosorbide mononitrate Converted to NO,activates guanylate cyclase.Stimulates guanosine 3', 5’-monophosphate (cGMP) which activates kinase phosphorylations in SM cells= dephosphorylation of SM myosin light chains. release of CA = relaxation of SM cells&vasodilation.
nicorandil Combines KATP channel activation with NO donor activity, and is used in refractory angina
adenosine Slows conduction time through AVN, interrupting re-entry pathways through A-V node, and thus restoring normal sinus rhythm in patients with paroxysmal supraventricular tachycardia (PSVT), including PSVT associated with Wolff-Parkinson-White Syndrome
amiodarone Prolongs myocardial cell AP, (phase 3)duraion and refractory period and acts as a non-competitive a and B adrenergic inhibitor.
losartan Competitive antagonist at angiotensin II AT1-receptor on vascular smooth muscle
doxazosin Inhibits postsynaptic alpha (1)-adrenoceptors on vascular smooth muscle. This inhibits vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilatation
bisoprolol B blocker, acts as competitive antagonist of sympathomimetic NT such as catecholamines for binding at beta (1)-adrenergic R in the heart, but to a lesser extent at beta (2)R. Lipophilic exhibits no (ISA) or membrane stabilizing activity.
dopamine Produces +ve chronotropic and inotropic effects on the myocardium,=increased HR&conractility. exerting an agonist action on beta-adrenoceptors& indirectly by causing release of norepinephrine from storage sites in sympathetic nerve endings
streptokinase Cleaves Arg/Val bond in plasminogen to form proteolytic enzyme plasmin. Plasmin in turn degrades fibrin matrix of thrombus, thereby exerting thrombolytic action (also rt-PA and tenecteplase)
tropicamide Inhibits sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium
spironolactone specific antagonist of aldosterone, acting through competitive binding of receptors at the aldosterone-dependent sodium-potassium exchange site in the DCT, thus causing increased amounts of sodium and water to be excreted, while K is retained
compound alginate preparations Allginate + anatacid increases the viscosity of the stomach contents and can protect oeophageal mucosa from reflux. Some preparations form a viscous gel (raft) that floats on the surface of stomach contents, thereby reducing reflx
omeprazole Proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+ /K+ -ATPase in the gastric parietal cell, blocking the final step in HCL production. (Lansoprazole is also widely used)
metoclopramide Dopamine antagonist which raises threshold of activity in the chemoreceptor trigger zone and decreases input from afferent visceral nerves. Also increases gastric emptying rate (domperidone similar)
ondansetron Selective antagonist of serotonin (5-HT3) receptors located on nerve terminals of vagus in periphery and centrally in the chemoreceptor trigger zone of the area postrema.
prochlorperazine Antagonist of dopamine in chemoreceptor trigger zone. Also antagonist at cholinergic and alpha-adrenergic receptors
promethazine Competes with free histamine for binding at H1-receptor sites in GIT, uterus, large blood vessels,& bronchial muscle. Relief of nausea appears related to central anticholinergic actions and may implicate activity on the medullary CTZ (cyclizine similar)
mesalazine An aminosalicylate metabolized in gut to 5- aminosalicylic acid an antioxidant traps free radicals (potentially damaging by-products of metabolism)may diminishes inflammation locally by blocking cyclooxygenase&inhibiting prostaglandin production colon.
ispaghula husk Bulk-forming laxative. Polysaccharide polymer not broken down by the normal processes of digestion in upper GI tract. Form bulky hydrated mass in gut lumen promoting peristalsis and improving faecal consistency
lactulose Semi-synthetic disaccharide,not absorbed from GIT,increases water in LI, either drawing fluid from body into bowel or retaining fluid. Produces osmotic diarrhoea of low faecal pH,discourages proliferation of NH4-producing organisms.
senna Stimulant laxative which directly stimulates the myenteric plexus, resulting in increased peristalsis and thus defecation
loperamide Non-selective calcium channel blocker that also binds to opioid mu-receptors in the myenteric plexus to reduce peristalsis.
latanoprost Prostaglandin F2 alpha analogue and prostanoid selective FP receptor agonist that is believed to reduce intraocular pressure (IOP) by increasing outflow of aqueous humor.
ipratropium bromide Anticholinergic, which blocks muscarinic cholinergic receptors, without specificity for subtypes, resulting in decrease in formation of (cGMP). This results in effect on intracellular calcium, and therefore in decreased contractility of smooth muscle
ascorbic acid Reducing agent required for collagen formation, synthesis of the biogenic sympathetic amines, norepinephrine and epinephrine, and synthesis of carnitine.
nicotinamide (B3) Precursor to nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), vital cofactors for many essential enzymes
pyridoxine (B6) In the form of coenzyme pyridoxal 5'phosphate, wide range of metabolic reactions and synthesis of Nt
thiamine (B1) Co-enzyme in several vital metabolic processes, including oxidative decarboxylation of pyruvate to acetyl CoA via pyruvate dehydrogenase.
Created by: 572650658