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USMLE Pharmacology
| Question | Answer | More? |
|---|---|---|
| Examples of Typical Anti-psychotics | Thiorodazine, Haloperidol, Fluphenazine, Chlorpromazine | |
| Examples of Atypical Anti-psychotics | Clozapine, Olanzapine, Risperidone | |
| Mechanism of Action for Typical Anti-psychotics and side effects | Blocks D2 receptors | Neuroleptic Malignant Syndrome(muscle rigidity, altered mental status) Tx with Dantrolene or bromocriptine |
| Mechanism of Action for Atypical Anti-psychotics and side effects | Blocks Dopamine & 5-HT2 Receptors | Anticholinergic, weight gain, extra pyrimidal symptoms |
| Drug that may be used for EPS in anti-psychotics and why | Amantadine | increases the release of dopamine |
| Examples of Benzodiazepines | Diazepam, Lorazepam, Midazolam, Triazolam, Chlordiazepoxide | |
| MOA of Benzodiazepines and side effects | GABA- mediated inhibitory effects; Increases frequency of Cl channel opening * FRENZOdiazepines- Increases frequency | CNS depression, Dependence |
| Examples of Barbituates | Phenobarbital, Pentobarbital, Thiopental | |
| MOA of Barbituates and side effects | GABA- mediated inhibitory effects; Increases duration of Cl channel opening * barbitDURATES- Increases duration | CNS depression, respiratory failure, dependence |
| Flumazenil | Competitive antagonist at GABA receptors; Antidote for benzodiazepine overdose | |
| Examples of Full Opioid Agonists | Morphine, Meperidine, Fentanyl, Methadone, Heroin | CNS depression, respiratory depression, constipation |
| Examples of Partial opioid Agonists | Codeine, Hydrocodone, Oxycodone | CNS depression, respiratory depression, constipation |
| Examples of and receptor properties of mixed opioid agonists | Pentazocine, Nalbuphine, Butorphanol Agonists @ Kappa/Delta receptors, Antagonists at Mu receptors | CNS depression, respiratory depression, constipation, hallucinations |
| Used for opioid overdose | Naloxone/Naltrexone | can induce withdrawal symptoms |
| Selegiline MOA and use | Mono amine oxidase-B inhibitor; Increases availability of dopamine | Use: Parkinson's Disease Orthostasis, insomnia |
| Levodopa MOA and use | Precursor of Dopamine | Use: Parkinson's Disease Arrhythmias, anorexia |
| Carbidopa MOA and use | Peripheral decarboxylase inhibitor, increases availability of dopamine | Use: Parkinson's Disease |
| Local Anesthetics Esters | Procaine, Tetracaine Esters have one "I" | |
| Local Anesthetics Amides | Lidocaine, Bupivicaine AmIdes have 2 "I" | |
| Triptan examples and use | Sumatriptan, Frovatriptan, Eletriptan | Use: Migraine headaches S.E.:Chest pain |
| MOA of Triptans | 5-HT1D and 5-HT1B agonists. Causes vasoCONSTRICTION | |
| Succinylcholine | Blocks Neuromuscular junction AFTER INITIAL DEPOLARIZATION Phase 1: Prolonged depolarization Phase 2: Repolarized, but blocked | |
| Antidote for Phase 1 neuromuscular block | No Antidote | |
| Antidote for Phase 2 neuromuscular block | Cholinesterase Inhibitors: Neostigmine | |
| Tubocurarine, Pancuronium | Blocks NMJ, NO INITIAL DEPOLARIZATION Compete for ACh receptors | |
| Reversal of nondepolarizing blockade | Cholinesterase Inhibitors: Neostigmine, Edrophonium | |
| Phenytoin MOA and use | Decrease influx of sodium ions Use: Partial, tonic-clonic seizures and status epilepticus | |
| Carbamazepine MOA and use | stabilizes closed sodium channels | Use: Partial and tonic-clonic seizures |
| Treatment for Absence Seizures | Ethosuximide | |
| Valproic Acid MOA and use | Decreases sodium channel activation | Use: Myoclonic and Absence seizures |
| Bethanechol MOA | direct acting cholinergic agonist Stimulates bladder and GI motility | |
| Pilocarpine MOA and use | direct acting cholinergic agonist | Topical use for glaucoma, acts on M3 receptor |
| Edrophonium | Indirect cholinergic agonist via inhibiting acetylcholinesterase Use: Myasthenia Gravis diagnosis | |
| Neostigmine MOA and use | AChE inhibitor | Use: myasthenia gravis, reversal of NMJ blockade |
| Pralidoxime | Reversal of organophosphate poisoning | |
| Atropine | Anticholinergic, blocks muscarinic receptors | |
| Scopolamine | Anticholinergic, blocks muscarinic receptors | |
| Ipratropium | Blocks muscarinic receptors in the lungs, inhibiting bronchoconstriction and bronchial secretions | |
| Carbonic Anhydrase Inhibitors and MOA | Acetazolamide, Dichlorphenamide | Reversibly inhibits carbonic anhydrase |
| Loop Diuretics and MOA | Furosemide, Ethacrynic Acid, Bumetanide | Inhibits Na/K/2Cl transporter in the thick ascending limb of loop of Henle |
| Thiazides and MOA | Hydrochlorothiazide, and other -azides | Inhibits NaCl reabsorption in distal tubule |
| K- Sparing and MOA | Spirinolactone,Triamterene, Amiloride | Spirinolactone- Aldosterone receptor antagonist. Amiloride/Triamterene- Prevents Na reabsorption in collecting ducts |
| Class 1A Na channel blockers and MOA | Quinidine, Procainamide, Disopyramide | decreases Na influx during depolarization and K efflux in repolarization |
| Class 1B Na channel blockers and MOA | Lidocaine, Tocainide, Phenytoin | Binds and blocks Na channels |
| Class 1C Na blockers | Flecainide, Propafenone | High potency Na channel blocker, causing prolongation of the cardiac action potential |
| ACE Inhibitors and MOA | Captopril, Quinipril, and other -pril | prevents both formation of Angiotensin II and breakdown of bradykinin by ACE |
| Angiotensin receptor blockers and MOA | -"sartan" ie, losartan | selectively blocks the binding of angiotensin II to AT-1 receptor |
| Nitrates and MOA | Nitroglycerine, Isosorbide dinitrate; vasodilators | produce nitric oxide |
| smooth muscle relaxants and MOA | Hydralazine, Minoxidil | Directly relaxes arteriolar smooth muscle |
| Sodium Nitroprusside MOA and important toxicity | Releases nitric oxide | Cyanide toxicity |
| -Statins and MOA | Simvastatin, Atorvastatin, Lovastatin, etc. | Inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis, increases number of LDL receptors synthesized |
| Fibrates and MOA | Gemfibrozil, Clofibrate, Fenofibrate | Inhibit lipolysis and hepatic secretion of VLDL, decreases Triglycerides, and LDL, increases HDL |
| Niacin MOA and important side effect | Inhibits VLDL secretion and synthesis | skin flushing and pruritis |
| Bile acid resins and MOA | Cholestyramine, Colestipol | Bile acid sequestration. Binds bile acids in gut so they can be secreted. Plasma cholesterol then converted to bile, lowering plasma cholesterol |
| Colchicine MOA and major side effects | Binds mitotic spindles and tubulin, and inhibits the release of luekotrienes | Three A's- Agranulocytosis, Aplastic anemia, and Alopecia |
| Probenecid MOA and major side effects | Inhibits renal uric acid reabsorption in proximal tubule | headache, anorexia |
| Allopurinol MOA and major side effect | Inhibits uric acid synthesis | Skin Rash |
| Heparin MOA | Binds Anti-thrombin III, inactivating thrombin and other coagulation proteases, esp. factor 5a | |
| Alteplase (tPA), Streptokinase MOA | Converts plasminogen to plasmin | |
| Urokinase MOA | Degrades both fibrin and fibrinogen | |
| Theophylline MOA | Phosphodiesterase inhibitor, increasing cAMP | |
| Albuterol, Salmeterol, Terbutaline MOA | B2 agonists | |
| Isoproterenol MOA | B1/B2 agonist | |
| Ipratropium MOA | Muscarinic agonist | |
| Zileuton MOA | 5-lipooxygenase inhibitor | |
| Zafirlukast, montelukast MOA | blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it | |
| Cromolyn MOA | Mast cell stabilizer | |
| Sulfonylureas and MOA | 1st gen.- Tolbutamide, Chlorpropamide 2nd. gen.- Glyburide, Glipizide | close K channels in B cell membrane -> depolarization -> increase Ca influx -> insulin release * requires some B cell activity |
| Biguanide and MOA | Metformin | Inhibits liver gluconeogenesis *potential for lactic acidosis |
| Acarbose MOA | inhibits a-glucosidase @ brush border -> decrease glucose absorption | |
| Levothyroxine use and MOA | Hypothyroidism | T4 hormone |
| Methimazole and Propylthiouracil use and MOA | Hyperthyroidism | blocks thyroid peroxidase, Inhibiting oxidation and coupling -> decrease peripheral conversion of T4 to T3 |
| Misoprostal and MOA | PGE1 analog | Stimulates the secretion of gastric mucus and bicarbonate |
| Sucralfate use and MOA | Gastric and duodenal ulcers | create a barrier that prevents degradation of mucus by pepsin |
| Diphenoxylate, Loperamide use and MOA | Diarrhea | Activate opioid receptors -> decrease peristalsis |
| Docusate | Stool Softener | Hyperosmotic agent |
| Prochlorperazine, metoclopramide use and MOA | anti-emetic | Dopamine antagonist |
| Ondansetron use and MOA | anti-emetic | Block 5-HT3 receptors *not nauseous, keep ONDANcing |
| Dronabinol use and MOA | anti-emetic | CB1 (G-protein) blocker in the brain |
| major side effect of Alkylating Agents, what part of the cell cycle do they work, and MOA? | SE: Myelosuppression MOA: Cross link DNA | All are non- cell cycle specific |
| Alkylating Agent: Platinum analogs and side effects | Cisplatin, Carboplatin | Nephro-, oto-, neurotoxicities |
| Alkylating Agent: Nitrogen mustards and side effects | Cyclophosphamide, Mechlorethamine | Hemorrhagic cystitis (treat with MESNA), SIADH |
| Alkylating Agent: Nitrosureas and side effects | Carmustine, Streptozocin | Hemorrhagic cystitis, SIADH |
| Alkylating Agent: Busulfan side effect | Pulmonary fibrosis | |
| Antimetabolites act at what point of cell cycle? | S Phase | |
| Antimetabolites: Folate antagonist and MOA | Methotrexate | Inhibits dihydrofolate reductase |
| Antimetabolites: Purine analog and MOA | 6- Mercaptopurine | Functionally incorporated into DNA/RNA |
| Antimetabolites: Pyrimidine analog | 5- Fluorouracil | Functionally incorporated into DNA/RNA |
| Antimetabolites: Pyrimidine antagonists and MOA | Cytarabine, Arabinoside | Incorporate into DNA/RNA, terminate chain elongation |
| At what point in the cell cycle do Topoisomerase Inhibitors work? Major side effect | Late S and early G2 | Myelosuppression |
| Topoisomerase I inhibitor and MOA | Topotecan | Inhibits Topoisomerase I, blocks replication and transcription |
| Topoisomerase II inhibitor and MOA | Etoposide | Forms complex with topoisomerase II, blocks DNA replication, causes DNA strand breakage |
| Microtubule Inhibitors: Vinca alkaloids and MOA | Vincristine, Vinblastine | Inhibits polymerization of tubulin- M phase |
| Microtubule Inhibitors: Taxols | Paclitaxel, Docetaxol | Binds to tubulin and stabilizes microtubules- G2 and M phase |
| Antineoplastic antibiotics: Bleomycin MOA and side effects | Forms a ferrous Fe-O2 drug that complex/cleaves DNA- G2 phase | Pulmonary fibrosis, Raynaud's phenomenon |
| Antineoplastic antibiotics: Dactinomycin, Actinomycin | Intercalates with base pairs- Late S and G2 phase | myelosuppression |
| Antineoplastic antibiotics: Mitomycin C MOA and side effects | Intercalating DNA, forms reactive oxidative radicals- non cell cycle specific | Nephrotoxicity, pneumonitits, myelosuppression |
| Antineoplastic antibiotics: Doxorubicin MOA and side effect | Intercalates between DNA base pairs, inhibits DNA topoisomerases I and II | Cardiotoxicity |
| Tamoxifen MOA and side effects | Estrogen receptor antagonist | Endometrial carcinoma |
| Flutamide MOA and side effects | Inhibits androgen uptake and binding | Gynecomastia and impotence |
| Anastrozole, Letrozole | Aromatase inhibitors-> decreases conversion of androgens to estrogen | hot flashes, anorexia |
| Lueprolide | Increase LHRH release, suppressing FSH/LH | Gynecomastia, depression, weight gain |
| Rituximab | Antibody directed at CD20 surface antigen expressed on B lymphocytes | hypersensitivity, thrombocytopenia |
| Infliximab MOA and uses | Blocks TNF-a by preventing its binding to receptors | psoriasis, chron's, RA, ankylosing spondylitis |
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