Term
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Definition
| Anti convulsant, anti epileptic, slow down break down of GABA |
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Term
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Definition
| Binds irreversibly to GABA T, GABA levels go down only when new GABA T formed |
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Term
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Definition
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Term
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Definition
| Competitive GABA antagonist |
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Term
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Definition
| Non competitive GABA antagonist-binds inside Cl-channel. Channel can still open, but GABA can't enter. |
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Term
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Definition
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Term
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Definition
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Term
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Definition
| GABA B receptor agonist, muscle relaxant, spasmolytic drug |
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Term
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Definition
| GABA B antagonist-competitive |
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Term
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Definition
| Phenylalkylamine, rate slowing, cardiac and smooth, for SVT and AF |
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Term
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Definition
| Benzothiazepines, rate slowing, cardiac and smooth |
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Term
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Definition
| only smooht uscle, don't slow rate, eg:amlodipine, for hypertension |
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Term
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Definition
| Acts on A1 receptors, hyperpolarize cardiac tissue, slow conduction through AV node. Used to treat SVT, safer than verapamil |
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Term
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Definition
| Antidysrhythmic. Treat SVT as well as Ventricular Tachycardia |
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Term
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Definition
| inhibits Na-K-ATPase,central vagal stimulation. Slow ventricular rate in AF, used in chronic heart failure. |
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Term
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Definition
| Blocks if channel in the SAN. Used for angina. Contraindicated if sick sinus/heart block/post MI/cardiogenic shock |
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Term
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Definition
| inhibitor of phosphodiesterase in cardiac myocytes |
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Term
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Definition
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Term
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Definition
| Insurmountable AT1 antagonist |
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Term
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Definition
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Term
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Definition
| release NO within smooth muscle cells, or stimulate guanylate cylcase, reduce venous return |
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Term
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Definition
| Irreversible alpha blocker |
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Term
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Definition
| Agonist at 5HT1 receptors, constricts large arteries, inhibit trigeminal nerve transmission |
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Term
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Definition
| Emergency hormone, hypotensive crisis, breathing crisis |
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Term
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Definition
| selectivity for alpha receptors, vasoconstrictor, nasal decongestant, mydriatic |
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Term
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Definition
| Alpha 2 adrenoceptor agonist |
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Term
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Definition
| Beta selective (B1, B2) agonist. Important side effect, reflex tachycardia |
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Term
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Definition
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Term
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Definition
| B2 selective agonist. Treat asthma, threatened uncomplicated labour. Caution with cardiac patients, hyperthyroidism and diabetes. |
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Term
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Definition
| Inhibit uptake 1 in NA terminals |
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Term
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Definition
| Act as false neurotransmitter, normally broken down by MaO. Cheese reaction in ppl who takes MaO inhibitors. |
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Term
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Definition
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Term
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Definition
| Important for the synthesis of factor 2,7,9,10. Addition of carboxyglutamic acid. Post-translational modification |
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Term
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Definition
| Activated by thrmobin, inactivates factor V and VII |
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Term
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Definition
| Activated by heparin, inactivates thrombin, as well as factor 10a |
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Term
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Definition
| Prevents action of vitamin K, strong binding to plasma protein, metabolized by hepatic mix function P450, anti-coagulant properties monitored by INR |
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Term
| Warfarin-drugs that inhibit p450 |
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Definition
| antibacterial, antifungal-erythromycin, fluconozole |
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Term
| Warfarin-drugs which displace warfarin |
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Definition
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Term
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Definition
| phenobarbital, rifampicin, St John's wart |
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Term
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Definition
| Activates antithrombin 3, given subcutaneous/IV |
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Term
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Definition
| Binds to heparin to produce inactive complex |
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Term
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Definition
| Irreversible COX1 inhibitor, side effects-GI disturbances, remember that it displaces warfain |
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Term
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Definition
| Inhibits binding of Glyp2b/3a to fibrinogen. Side effects, GI haemorrhage, dirrhoea, rash |
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Term
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Definition
| Antagonist of Glyp2b/3a receptor, used in combination with heparin and aspirin,prevent ischaemia in patient with unstable angina |
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Term
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Definition
| Activates plasminogen. Derived from Beta haemolytic streptococci. May be antigenic. |
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Term
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Definition
| Activates plasminogen, clot sensitive. |
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Term
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Definition
| Act on CB1 receptor. Inhibit vomiting center, increase food intake |
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Term
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Definition
| Combat neuropathic pain, such as multiple sclerosis, only use when other analgesic not work |
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Term
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Definition
| CB1 receptor antagonist, anti-obesity drug |
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Term
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Definition
| Inhibit aldehyde dehydrogenase |
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Term
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Definition
| Inhibit HMG CoA synthase and HMG CoA reductase |
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Term
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Definition
| Acts on PPAR, increase HDL, but not very much good in lowering LDL |
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Term
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Definition
| Inhibits cholesterol absorption, activated by intestinal glucorinidation |
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Term
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Definition
| Selective COX 2 inhibitor |
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Anti-inflammatory drug. For ulcerative colitis, no immunosuppressive effects. |
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Term
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Definition
| 1st aminosalicylate, now given active moiety such as mesalazine |
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Term
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Definition
| Choline esters, M3 AChR agonist, resistant to degradation, assist bladder emptying and enhance gastric motility. |
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Term
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Definition
| Selective muscarinic agonist, less effect on GI muscle and heart, not substrate for ACh esterase, glaucoma treatment |
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Term
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Definition
| Found at all cholinergic synapse |
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Term
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Definition
| Found in plasma and most tissues, but not cholinergic synapses, broad specificity |
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Term
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Definition
| Reversible anti-cholinesterase, compete with AcH for active site on anti cholinesterase, donate carbamyl group. Treat glaucoma, atropine poisoning. |
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Term
| Organophosphates compounds |
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Definition
| Irreversible cholinesterase drugs, react with enzymes site, stable and resistant to hydrolysis, can take week. Eg: Ecothipate,dyflos, |
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Term
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Definition
| Treat glaucoma, irreversible cholinesterase inhibitor |
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Term
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Definition
| Treat organophosphate poisoning within Few hours |
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Replacement for heroin addicts. |
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Term
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Definition
| MU,delta,brainstem, thalamus |
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Term
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Definition
| Kappa,found in spinal cord |
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Term
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Definition
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Term
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Definition
| 1,25 D3. Stimulate absorption of Ca2+ and phosphate from kidney and intestine |
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Term
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Definition
| Active against anaerobic bacteria and protozoa, interfere with alcohol metabolism |
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Term
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Definition
| broad spectrum antibiotic |
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Term
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Definition
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Term
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Definition
| Irreversible inhibitors of H+/K+ ATPase, inactive at neutral pH, accumulates in canaliculi of parietal cells. Use in peptic ulcers resistant to H2 antagonist |
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Term
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Definition
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Term
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Definition
| Strong negative charge in acid environment, binds to positively charged groups in large molecules, gel like complexes, increse PG, mucus and HCo3- secretion |
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Term
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Definition
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Term
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Definition
| Prostaglandin analogue, maintain the gastroduodenal mucosal barrier |
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Term
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Definition
| Mainly non ulcer dyspepsia, salts of Al3+, Mg2+ |
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Term
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Definition
| Osmotic diuretic, pharmacologially inert, increases osmolarity of tubular fluid, use of reducing intracranial, ocular pressure |
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Term
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Definition
| Carbonic anhydrase inhibitor prevent reabsroption of HC03 and Na+, increase K+ loss-unwanted effect, metabolic acidosis, alkaline urine |
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Term
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Definition
| Most powerful osmotic diuretic,inhibit Na+, Cl- reabsorption in ascending limb ( Ca2+, Mg+ also affected)-use for oedema ( heart, pulmonary, renal, hepatic), hypercalcaemia, hyperkalaemia. Side effects-metabolic alkalosis |
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Term
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Definition
| Inhibit Na+,Cl- reabsorption in early distal tubule, increase K+ loss. Increases calcium reabsorption, can treat idiopathic hypercalciuria |
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Term
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Definition
| Inhibitors of aldosterone sensitive Na+ channels |
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Term
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Definition
| Enhance action of GABA, increase affinity of GABA binding, reciprocal action, increases freqeuncy of opening Cl- channel |
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Term
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Definition
| Increase affinity of GABA binding, enhance action of GABA, action not reciprocated, less selective than BDZ |
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Term
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Definition
| Competitive benzodiazepine antagonist |
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Term
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Definition
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Term
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Definition
| Hypnotic,severe intractable insominia |
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Term
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Definition
| converted into trichlorethanol, hypnotic. LIVER |
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Term
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Definition
| Peripheral DOPA decarboxylase inhibitor |
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Term
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Definition
| Selective for MAO-B, predominates in dopaminergic areas of CNS, withotu peripheral side effects of non selective Mao-I |
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Term
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Definition
| Inhibits apoptosis of dopaminergic cells? |
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Term
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Definition
| Relatively non selective between D1 and D2, high affinity for D4 receptors. Basically dopamine antagonist |
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Term
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Definition
| Neuroleptic, anti emetic, could also have action on histamine receptors, control motion sickness |
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Term
| Removal of acute dyskinesia as side effects of neuroleptics |
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Definition
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Term
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Definition
| Involunatry movements, often of face and tongue-side effects of neuroleptics |
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Term
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Definition
| Competitive antagonist at H, M, D in descending order of potentcy. Anti-emetic, disorders of the labyrinth, hyperemesis gravidarium |
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Term
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Definition
| D2 antagonist, less potency for H1 and muscarinic, acts in GI tract, increase smooth muscle motility, increase gastric emptying. Use to treat vomitting in association with chemotherapy, radiation sickness, severe kidney failure. |
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Term
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Definition
| anti motion sickness-antimuscarinic. |
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Term
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Definition
| 5HT3 antagonist-block transmission in visceral afferents and CTZ-mainly use in anticancer drug induced vomitting |
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Term
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Definition
| B1 adrenoceptor antagonist, treat angina, post MI, cardiac dysrhythimas, chronic heart failure, thyrotoxicosis |
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Term
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Definition
| Selective serotonin reuptake inhibitor-third most prescribed anti depressants |
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Term
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Definition
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Term
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Definition
| Treat tremor in Parkinsons, muscarinic antagonist, also good for neuroleptic muscle dystonia |
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Term
| Nicotinic receptor antagonist AKA |
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Definition
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Term
| Hexamethonium, trimetaphan |
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Definition
| Nicotinic receptor antagonist. Trimetaphan used during surgery-for hypotension |
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Term
| Uses of muscarinic antagonist |
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Definition
| Examination of retina, motion sickness, Parkinson's? , sedation, airway disease, IBS |
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Term
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Definition
| Binds to SNARE complex, prevents release of ACH from ACH terminals |
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Term
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Definition
| Dual acting on B1 and alpha 1 antagonist. Lowers blood pressure via a reduction in peripheral resistance, but no change in heart rate/cardiac output |
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Term
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Definition
| non selective alpha antagonist. also blocks alpha2 , not clinically useful |
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Term
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Definition
| Highly selective for alpha 1 receptors. Postural hypotension is troublesome. Casue modest decrease in LDL and an increase in HDL |
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Term
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Definition
| Form false transmitter, alpha methyl norepinephrine, not deaminated within neuron by MAO. Less active on alpha 1, more active on alpha 2. |
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Term
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Definition
| Sulphamethazole.Structural analogue of P aminobenzoic acid. Competes for dihydropteroate. Hypersensitivity, vomit, headache. |
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Term
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Definition
| Dihydrofolate reductase inhibitor in bacteria. Hypersensitivity, vomit. |
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Term
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Definition
| Inhibit formation of peptidoglycan by inhibiting transpeptidase. Main unwanted effect in hypersensitivity. Don't cross BBB unless meninges inflamed. |
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Term
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Definition
| Beta lactamase production ( impt in staphylococcus), reduction in permeability of outer membrane, modified penicillin binding sites |
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Term
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Definition
| A type of beta lactam-drug of choice for meningitis, some can cross BBB |
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Term
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Definition
| Wide spectrum, polycyclic, inhibits tRNA binding to A site. Side effect is phototoxicity, chelation in growing bones and teeth ( child). Will accumulate if renal fuction impaired. Doxycycline won't accumulate. Chelate metal ions. |
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Term
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Definition
| Inhibition of protein synthesis, binds to 50S subunit of ribosome and inhibits transpeptidation. Resistance due to chloramphenicol acetyl transferase. Unwanted effect-bone marrow suppression. Gray baby syndrome, vomiting, diarrhoea, flacidity. |
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Term
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Definition
| Inhibit bacterial protein synthesis, bind to 30S subunit of the ribosome. ALeration to codon anticodon recognition. Defective bacterial proteins. Bacteriacidal. Minimal action against anaerobic organism. Highly polar, not absorbed in the GI tract.Ototoxicity, nephrotoxicity. |
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Term
| Main mycobacteria infections. Therapy |
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Definition
| Tuberculosis, Leprosy. First phase of 2 months, 3 drugs. Second phase of 4 months. |
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Term
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Definition
| Superficial, systemic (deeper tissue and organs), dermatomycoses ( cause by dermatophytes), candidaisis (mucuous membrane) |
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Term
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Definition
| Anti mycobacterial. Penetrates well into the necrotic tuberculous lesion. Inhibit mycolic acids? |
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Term
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Definition
| Inhibits DNA-dependent RNA polymerase in prokaryotes but not eukaryotes.Anti mycobacterial. |
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Term
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Definition
| Inactive at neutral pH but tuberculostatic at acidic pH. Effctive against the intracellular organism in macrophages. |
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Term
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Definition
| Polyene macrolide. No absorption from mucous membrane or from skin. Use limited to fungal infection of skin and GI. Binds to cell membrane, interferes with permeability and transport function. Greater avidity for ergosterol. |
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Term
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Definition
| Block syntehsis of ergosterol ( from lanosterol)-alters fluidity of membrane, interferes with action of membrane associated enzymes, overall effect, inhibit replication |
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Term
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Definition
| Muscarinic inhibitor in the lung |
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Term
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Definition
| Immunosuppressive. Effective in Crohn's disease. Active form is 6mercaptopurine. |
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Term
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Definition
| Prevents breakdown of dopamine in brain ( CNS). Perippheral, inhibits peripheral COMT |
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Term
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Definition
| High specificy fo herpes simplex. Converted to monophosphate by thymidine kinase ( virus), then converted to triphosphate (host). Inhibits viral DNA polymerase. |
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Term
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Definition
| Analogue of thymidine. Active inhibitor of reverse transcriptase. Eg: in HIV. Reduces incidences of opportunistic infections, prolong life expectancy, PEP. |
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Term
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Definition
| Highly protein bound, can be displaced by Valproate, aspirin. Block voltage gated Na channel. OCP efficacy reduced. Increase concentration of warfarin. p450 enzyme inducer. |
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Term
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Definition
| Carbamezepine, Valproate, Lamotrigine |
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Term
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Definition
| Inhibit some forms of CYP450-major side effects, severe hepatic toxicity, pancreatitis |
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Term
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Definition
| Adverse effects-ataxia, hypersensitivity, rash, dizziness |
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Term
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Definition
| Metabolism inhibited by valproate. Dizziness sedation, diplopia |
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Term
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Definition
| Intercalates DNA and interferes with topoisomerase 2, can cut DNA, but cannot wind it back |
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Term
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Definition
| Inhibit DNA and RNa synthesis, though inhibition of topoisomerase 2 |
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Term
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Definition
| Generates reactive 02, chops up DNA, lung particularly susceptible due to high 02 tension, can attack non dividing cells. |
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Term
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Definition
| Binds to tubulin, inhibit polymerization into microtubules |
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Term
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Definition
| Interalating agent, cause guanine intrastrand cross links |
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Term
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Definition
| Inhibits DNA and RNA synthesis and interferes with mitosis at interphase |
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Term
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Definition
| Inhibits ribonuclease reductase |
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