Drugs PHAR2210 PDF

Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 1. Adrenaline Acts via ²-adrenoceptor for increased contractility 2. action of: activate phospholipase C - a1 adrenoceptors inhibit adenylate cyclase - a2 adrenoceptors...

Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 1. Adrenaline Acts via ²-adrenoceptor for increased contractility 2. action of: activate phospholipase C - a1 adrenoceptors inhibit adenylate cyclase - a2 adrenoceptors activate phospholipase C - Muscarinic acetyl- activate adenylate cyclase choline receptors - B-adrenoceptors 3. Acetylcholine Acts on muscarinic receptors, stimulant of nicotinic re- ceptors 4. Noradrenaline Acts on ±- adrenoceptors, mimics endogenous ligands 5. Phenylephrine ±- adrenoceptor activator in vascular smooth muscle cell for vasoconstriction 6. Diphenhydramine Binds to histamine receptors (decongestant) and mus- carinic acetylcholine receptors (dry mouth) 7. What is the action Agonist at ²2-adrenoceptors for bronchospasm relief of Salbutamol? 8. What is the mecha- Salbutamol (agonist) -> ²2-adrenoceptor -> Gs (stimula- nism of Salbutamol tory G protein) -> adenylate cyclase (transduction/effec- action at a cellular tor protein) -> cyclic AMP (2nd messenger) -> relaxation level? (effect) 9. Pancuronium Nicotinic receptor antagonist for muscle paralysis dur- ing anaesthesia 10. Insulin Activates insulin receptor to lower blood glucose 11. Prednisolone Glucocorticoid drug activating nuclear receptors - anti-inflammatory agent 12. Nifedipine Ca2+ channel blocker for hypertension treatment 13. Benzodiazepines Enhance GABA-activated Cl- channel opening for anx- iety 1/7  Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 14. Paracetamol - en- an analgesic that Inhibits cyclooxygenase zyme as drug tar- gets 15. Fluorouracil Blocks DNA synthesis by replacing uracil in purine biosynthesis (anti-cancer drug) 16. Ciclesonide Prodrug converted to active metabolite in the lung 17. Fluoxetine Inhibits serotonin re-uptake for antidepressant effect 18. Amphetamine CNS stimulant using noradrenaline transporter to enter nerve terminals and replace/release the neurotransmit- ters noradrenaline and serotonin 19. Ethanol increased drug metabolism leading to lower plasma concentrations 20. which drug is ev- alcohol idence of toxicity acute toxicity - CNS depression from duration and chronic toxicity - alcohol-related liver disease frequency of expo- sure 21. Barbiturates Increase metabolism resulting in lower drug response 22. ³-aminobutyric acid activates ion channel receptors, Inhibitory transmitter (GABA) formed from glutamate types: GABAa, GABAb (GPCR), GABAc (ion channel receptors) 23. Glycine activates ion channel receptors, stimulates glycine re- ceptors, Inhibitory neurotransmitter mainly in the spinal cord - surmountable antagonist 24. Glutamate activates ion channel receptors, stimulates glutamate receptors, Fast-acting excitatory neurotransmitter in the CNS 2/7  Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 25. 5-hydroxytrypta- activates ion channel receptors, Increases motility, va- mine (5HT) sodilation, and platelet aggregation 26. Suxamethonium Long-acting agonist causing neuromuscular block, short-acting muscle relaxant/paralysis 27. GR± Glucocorticoid receptor encoded by NR3C1 gene 28. Morphine, Codeine linked to pharmacological effects of a drug and show a - Type A ADR dose-response relationship - respiratory depression 29. Penicillin - Type B Idiosyncratic, unpredictable adverse drug reactions ADR - anaphylaxsis 30. Teratogens - Type D time related - occurs after use ADR - Agents causing birth defects by altering fetal growth 31. Antibiotic resis- Unexpected failure of drug to produce therapeutic ef- tance - Type F ADR fects 32. TOCP Organophosphate causing delayed neuropathy - mus- cle weakness ataxia - human teratogen 33. Diethylstilbestrol Synthetic estrogen linked to severe birth defects - clear-cell adenocarcinoma in vagina of female offspring of DES treated mothers - human teratogen 34. Thalidomide Sedative causing severe birth defects - human teratogen 35. Fetal alcohol syn- Effects from prenatal alcohol exposure including facial drome defects 36. Paracetamol - DILI Intrinsic DILI - predictable, common, dose-related, re- type producible in animal models 37. NSAIDs - DILI type 3/7  Drugs PHAR2210 Study online at https://quizlet.com/_fd374h causing idiosyncratic liver injury - rare, unpredictable, not dose-related and not reproducible in animal models 38. Diclofenac Causes idiosyncratic liver injury - reactive metabolites cause mitochondrial injury and oxidative stress 39. Penicillin Inhibits bacterial cell wall synthesis 40. Amoxicillin Broad-spectrum penicillin not ²-lactamase resistant 41. Clavulanic acid ²-lactamase inhibitor, semisynthetic 42. Augmentin Combination drug for penicillin resistance - amoxicillin + clavulanic acid 43. Cephalosporin Inhibits bacterial cell wall synthesis 44. Aminoglycosides Inhibit bacterial protein synthesis inhibits initiation step 45. Tetracyclines Inhibit bacterial protein synthesis inhibits tRNA binding step 46. Amphenicols Inhibit bacterial protein synthesis - inhibit transpeptidation step 47. Antibacterial Inhibit protein synthesis Macrolides - prevent tRNA transfer with the growing peptide from A site to P site 48. Echinocandin Antifungal drug inhibiting cell wall synthesis 49. Polyenes Antifungal drugs altering cell membrane integrity or per- meability 50. amphotericin B a polyene - broad spectrum 51. Allylamines Synthetic antifungal drugs altering cell membrane in- tegrity or permeability 4/7  Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 52. Terbinafine Allylamine treating fungal nail infections CYP2D6 inhibitor 53. Azoles Synthetic antifungal drugs, alters cell membrane integri- ty or permeability inhibiting ergosterol biosynthesis 54. Itraconazole Triazole (azole) antifungal drug with variable oral ab- sorption 55. Integrase inhibitors Mechanism of action for anti-HIV drugs, INSTIs -tegravir 56. Protease inhibitors Anti-HIV drugs inhibiting viral protease, PIs -navir 57. Chloramphenicol Bacterial PSI - Rapidly absorbed amphenicol with he- patic clearance (UGT2B7) 58. Tenofovir disoprox- Prodrug for HIV reverse transcriptase inhibition il fumarate 59. Tenofovir alafe- Prodrug of tennofovir with improved oral absorption for namide HIV treatment 60. Ritonavir Potent CYP3A4 inhibitor used to boost protease in- hibitors CYP3A4 inhibitor 61. Elvitegravir Integrase strand transfer inhibitor for HIV treatment 62. Cobicistat Enhances elvitegravir efficacy in HIV treatment 63. prodrug example codeine ---CYP2D6---> morphine (dealkylation) 64. what hydrolyses esterase tenofovir disoproxil (hydrolysis) to tenofovir 5/7  Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 65. morphine morphine ---UGT2B7---> morphine-3-glucuronide (ma- metabolised jor) and morphine-6-glucuronide (minor) 66. describe entero- 1. lipophilic drug - undergoes absorption hepatic recircula- 2. hepatic metabolism tion and give an ex- 3. conjugates excreted into bile ample of a drug that 4. glucuronides in the GI tract - hydrolysed by B-glu- undergoes it curonidase (expressed by GI bacteria) 5. generate unconjugated drug - back to step 1 67. what metabolises paracetamol ---GST---> NAPQI paracetamol 68. how does char- oral admin. of activated charcoal decreases aspirin ab- coal prevent as- sorption as it has pores on its surface that the drug pirin overdose molecules attach to. It is excreted from body as charcoal can't be absorbed. 69. how does sodium I.V. sodium bicarbonate alkalises urine - increases urine bicarb prevent sali- pH, increases salicylic acid ionsisation, decreases re- cylate overdose absorption - leaves body more quickly 70. name 3 important MDR1, MRP2, BCRP ATP-binding cas- sette (ABC) drug transporters 71. name 2 solute OAT1, OAT3 carrier transporters (SLC) 72. which body com- total body water partment is ethanol stored in 73. how is ethanol ethanol ---alcohol dehydrogenase--->acetalaldehyde metabolised (oxidation) 74. which drug follows ethanol zero-order kinetics 6/7  Drugs PHAR2210 Study online at https://quizlet.com/_fd374h 75. why should preg- have a high affinity for calcium - slowly accumulates in nant people or bones and teeth young children avoid tetracyclines 76. Why is thiopen- it rises quickly in the liver and brain as well perfused, tal not used for slow rise in muscles and fat. if there was continuous I.V. anesthesia mainte- infusion, there would be a 'hangover' effect because the nance? drug is highly lipophilic and stored in fat, would slowly release from fat and re-access brain when no longer required 77. what does increases the action of cephalexin when co-adminis- probenecid do tered as it is a OAT1/OAT3 inhibitor 78. name 2 important a1 acid glycoprotein drug-binding plas- human serum albumin (HAS) ma proteins 79. what does pheno- increases CYP expression, reduced drug effects due to barbital do enhances hepatic metabolism (CYP induction) 80. how's ritonavir irreversible inhibition of an enzyme due to formation of cause CYP inhibi- a complex between the enzyme and reactive metabolite tion via covalent bonding inhibits CYP3A4, increases saquinavir plasma concen- tration when co-administered (mechanism-based inhibition) 81. which CYP does CYP3A4 cobicistat inhibit 7/7