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240 Cards in this Set
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Cimetidine
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M: Reversible block of histamine H2 receptors. Leads to decreased secretion by parietal cells.
C: Peptic Ulcer, gastritis. mild esophageal reflux T: Cimetidine is potent inhibitor of p-450; also has antiandrogenic effects. (prolactin release, gynecomastia, impotence, dec. libido in males); can cross BBB (confusion, dizziness, headaches) and placenta. Cimetidine and ranitidine dec. renal excretion of creatinine. Other blockers free of these effects. |
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Omeprazole
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PPI
M: Irreversibly inhibit H+/K+ -ATPase in stomach parietal cells C: Peptic ulcer, gastritis, esophageal reflux, Zollinger-Ellison Omeproazle, lansoprazole |
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Sucrulfate
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M: bind to ulcer base, provide physical protection, allow HCO3- secretion to reestablish pH gradient in mucous layer.
C: Quicken ulcer healing, traveler's diarrhea. Bismuth |
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Misoprostol
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M: PGE1 analog. Increase production and secretion of gastric mucous barrier, dec. acid production.
C: Prevent NSAID ulcers; maintenance of a patent ductus arteriosus; used to induce labor. T: Diarrhea. Contraindicated in childbearing women. (Abortificant) |
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Muscarininc antagonists
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Pirenzepine, propantheline
M: Block M1 receptors on ECL cells (dec histamine secretion) and M3 receptors on parietal cells (dec. H+ secretion) C: Peptic Ulcer T: Tachycardia, dry mouth, difficulty focusing eyes |
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Antacids
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Can affect absorption, bioavailability, or urinary excretion of other drugs by altering gastric/urinary pH or by delaying gastric emptying.
Aluminum Hydroxide: constipation and hypophosphatemia; proximal muscle weakness, osteodystrophy, seizures Magnesium hydroxide: diarrhea, hyporeflexia, hypotension, cardiac arrest Calcium Carbonate: hypercalcemia, rebound acid increase. All can cause hypokalemia |
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Infliximab
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M:Anti-TNF antibody.
C: Crohn's, rheumatoid arthritis. T: Respiratory infection, fever, hypotension |
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Sulfasalazine
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M: Combination of sulfapyridine (antibacterial) and mesalamine (anti-inflam). Activated by colonic bacteria
C: Ulcerative colitis, Crohn's T: Malaise, nausea, sulfonamide toxicity, reversible oligospermia |
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Ondansetron
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M:5-HT3 antagonist. Powerful central acting anti-emetic
C: Control vomiting post-op and in chemo patients T: Headache, constipation "Zofran" |
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Cisapride
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Pro-kinetic agent
M: Acts on serotonin receptor to incr. ACh release at myenteric plexus. Inc. esophageal tone; inc. gastric and duodenal contractility, improving transit time (including colon) T: No longer used. Serious interactions (torsades des pointes) with erythromycin, ketoconazole, nefazodone, fluconazole |
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Metoclopramide
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Prokinetic agent
M: D2 receptor antagonist. Incr. resting tone, contractility, LES tone, motility. Does not influence colon transport time. C: Diabetic and post-surgery gastroparesis. T: Parkinsonian effects. Restlessness, drowsiness, fatigue, depression, nausea, diarrhea. Drug interaction with digoxin and diabetic agents. Contraindicated in SBO. |
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Insulin
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M: Bind insulin receptor (tyrosine kinase activity). Liver: glucose stored as glycogen. Muscle: Incr. glycogen and protein synthesis, K+ uptake. Fat: aids TG storage.
C: Type 1 DM; dangerous kyperkalemia and stress-induced hyperglycemia. T: Hypoglycemia, hypersensitivity reaction (rare) Lispro (short); Aspart (short: NPH (intermediate) Lente, Ultralente (long) |
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Sulfonylureas
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M: Close K+ channel in B-cell membrane, cell depolarizes. This triggers insulin release via Ca2+ influx.
C: Stimulate endogenous insulin in type 2 DM. Requires islet function, no good in DM 1. T:Disulfiram effects (1st gen). Hypoglycemia (2nd gen) 1st gen: tolbutamide, chlorpropamide. 2nd gen: Glyburide, Glimepiride, glipizide |
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Metformin
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Biguanides
M: Unknown. Maybe dec. gluconeogenesis, inc. glycolysis, dec. serum glucose levels. C: Oral hypoglycemic. Can be used even without islet function. T:Lactic acidosis |
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Glitazones
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Pioglitazone, Rosiglitazone
M: Incr target cell response to insulin C: Monotherapy or combo-therapy in DM2 T: Weight gain, edema. Hepatotoxicity, CV toxicity. |
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alpha-glucosidase inhibitors
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Acarbose, Miglitol
M: Inhibit intestinal brush-border a-glucosidases. Delayed sugar hydrolysis and glucose absorption dec. postprandial hyperglycemia C: Mono/combo therapy for DM2 T: GI disturbances |
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Orlistat
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M: Alters fat metabolism by inhibiting pancreatic lipases
C: Long-term obesity management (w/ modified diet) T: Steatorrhea, GI discomfort, reduced absorption of fat-soluble vitamins, headache. |
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Sibutramine
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M: Sympathomimetic serotonin and NE reuptake inhibitor.
C: Short-term and long-term obesity management. T: Hypertension, tachycardia. |
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Propylthiouracil
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Inhibit organification and coupling of thyroid hormone synthesis. Dec. peripheral conversion of T4 to T3.
C: Hyperthyroidism T: Skin rash, agranulocytosis (rare), aplastic anemia. |
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Methimazole
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Inhibit organification and coupling of thyroid hormone synthesis.
C: Hyperthyroidism T: Skin rash, agranulocytosis (rare), aplastic anemia. |
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GH
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GH deficiency, Turner's syndrome
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Octreotide
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Somatostatin analog.
Acromegaly, carcinoid, gastrinoma, glucagonoma |
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Oxytocin
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Stimulates labor, uterine contractions, milk let-down; controls uterine hemorrhage
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Desmopressin
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ADH analog.
Pituitary (central, not nephrogenic) Diabetes insipidus. |
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Levothyroxine
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M: Thyroxine replacement
C: Hypothyroidism, myxedema T: Tachycardia, heat intolerance, tremors, arrhytmias Triiodothryonine |
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Glucocorticoids
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M: Dec. production of leukotrienes and prostaglandins bu inhibiting phospholipase A2 and expression of COX-2
C: Addison's disease, inflammation, immune suppression, asthma T: Iatrogenic Cushing's - buffalo hump, moon facies, truncal obesity, muscle wasting, thin skin, easy bruising, osteoporosis, adrenocortical atrophy, peptic ulcers, diabetes (if chronic) Hydrocortisone, prednisone, triamcinolone, dexamethasone, beclomethasone. |
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Leukotrienes
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LTB, LTC, LTD: increase bronchial tone
Zileuton inhibits lipoxygenase. Zafirlukast inhibits leukotrienes directly. |
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Prostacyclin (PGI)
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Decrease platelet aggregation
Decrease vascular tone Decrease bronchial tone Decrease uterine tone |
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Prostaglandins
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PGE, PGF
Decrease vascular tone Decrease bronchial tone Increase Uterine Tone |
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Thromboxane (TXA)
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Increase platelet aggregation
Increase vascular tone Increase bronchial tone |
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NSAIDS
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M: Reversibly inhibit COX-1, COX-2. Block prostaglandin synthesis
C: Antipyretic, analgesic, anti-inflamm. Indomethacin closes patent PDA. T: Renal damage, aplastic anemia, GI distress, ulcers. Ibuprofen, naproxen, indomethacin, ketorolac. |
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Celecoxib
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M: Reversibly inhibits COX-2 isoform, found in inflamm cells and mediates inflammation/pain. Spares COX-1, which maintains gastric mucosa.
C: Rheumatoid and osteoarthritis. T: Inc. risk of thrombosis. Sulfa allergy. Less toxicity to GI mucosa. |
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Acetominophen
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M: Reversibly inhibits COX, mostly in CNS. Inactivated peripherally.
C: Antipyretic, analgesic, no anti-inflamm effects. T: Overdose causes hepatic necrosis; metabolite depletes glutathione and forms toxic tissue adducts in liver. N-acetylcysteine is antidode, regenerates glutathione. |
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Colchicine
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M: Depolymerizes microtubules, impairing leukocyte chemotaxis and degranulation.
C: Acute gout T: GI side effects, especially orally. (Indomethacin used in accute gout, less toxic.) No salicylates. |
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Probenecid
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M: Inhibits reabsorption of uric acid in PCT
C: Chronic gout T: Inhibits secretion of penicillin. Not used acutely. No salicylates. |
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Allopurinol
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M: Inhibits xanthine oxidase, dec. conversion of xanthine to uric acid.
C: Chronic gout. Lymphoma and leukemia (prevent tumor-lysis associated urate nephropathy.) T: Interacts with azothioprine and 6-MP. Not used acutely. No salicylates. |
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Etanercept
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M: Recombinant TNF receptor (decoy)
C: Rheumatoid arthritis, psoriasis, ankylosing spondylitis. |
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Methotrexate
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M: S-phase specific antimetabolite. Folic acid analogue/inhibits DHF reductase, dec. dTMP and dec. DNA.
C: Leukemia, lymphoma, choriocarcinoma, sarcoma. Abortion, ectopic, RA, psoriasis. T: Myelosuppresion, reversible with LEUCOVORIN "rescue." Macrovesicular fatty change in liver. Mucositis. |
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Heparin
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M: Catalyze activation of ATIII, decr thrombin and Xa. Short half life.
C: Immediate anticoag for PE, stroke, angina, MI, DVT. Used during pregnancy. Follow PTT. T: Bleeding, HIT, osteporosis, drug interactions. Protamine sulfate for reversal. |
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LMWH
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Acts more on Xa, better bioavailability, 2-4x longer half life. Sub Q w/o lab monitoring. Not reversible.
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Lepirudin/bivalirudin
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Hirudin derivatives; directly inhibits thrombin. Alternative to heparin for anticoagulating pts with HIT
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Warfarin
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M: Interrupts synth. and g-carboxylation of Vit k-dep factors II, VII, IX, X, C S. Metabolized by p450. Long half life, affects PT.
C: Chronic anticoag. Not used in pregnant women. Follow PT/INR. T: Bleeding, teratogenic, skin/tissue necrosis, drug-drug interaction. |
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Thrombolytics
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Streptokinase, urokinase, tPA
M: Direclty/indirectly help convert plasminogen to plasmin. high PT and PTT, no platelet change. C: Early MI, early stroke. T: Bleeding. Contraindicated in pts with active bleeding, history of intracranial bleed, recent surgery, known bleeding diatheses, or HTN. Aminocaproic acid inhibits fibrinolysis. |
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Aspirin
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M: Acetylates, irreversibly inhibits COX1,2 to prevent TXA2 synthesis. Increase bleeding time. No PT/PTT effect.
C: Antipyretic, analgesic, anti-inflamm, anti-platelet. T: Gastric ulcers, bleeding, hyperventilation, Reye's, tinnitus. |
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Clopidogrel
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M: Inhibit platelet aggregation by irreversibly blocking ADP receptors. Inhibit fibrinogen binding by preventing GPIIb/IIIa expression.
C: Acute coronary syndrome; coronary stenting. Dec. incidence/recurrence of stroke. Ticlopidine has neutropenia. |
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Abciximab
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M: Monoclonal Ab to GPIIa/IIIb on activated platelets. Prevents aggregation.
C:Acute coronary symptoms. Angioplasty. T: Bleeding, throbocytopenia. |
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5-fluorouracil
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M: S-phase specific. Pyrimidine analog activated to 5F-dUMP, convalently complexes folic acid. Inhibits thymidylate synthase, dec dTMP, similar to MTX.
C: Colon cancer, solid tumors, basal carcinoma (topical.) Synergy with MTX T: Myelosuppresion, NOT reversible by leucovorin; photosensitivity. Thymidine rescue. |
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6-mercaptopurine
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M: Blocks de novo purine synthesis. Activated by HGPRTase.
C: Leukemias, lymphomas (not CLL or Hodkins) T: Bone marrow, GI, Liver. Metabolized by xanthine oxidase, so incr tox. with allopurinol. |
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Cytarabine
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M: Inhibits DNA polymerase
C: AML T: Leukopenia, thrombocytopenia, megaloblatic anemia |
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Cyclophosphamide
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M: Alkylating agent, covalently x-link (interstrand) DNA at guanine N-7. Requires bioactivation by liver.
C: Non-Hodg L, breast/ovarian carcinoma. Immunosuppresion. T: Myelosuppresion; hemorrhagic cystitis (prevent with mesna) |
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Nitrosoureas
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M: Alkylate DNA. Require bioactivation. Cross BBB.
C: Brain tumors (like GBM) T: CNS toxicity (dizziness/ataxia) Carmustine, lomustine, streptozocin. |
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Cisplatin / Carboplatin
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M: Like alkylating agent
C: Testicular, bladder, ovary, lung carcinoma T: Nephrotixicity, acoustic nerve damage |
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Busulfan
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M: Alkyates DNA
C: CML T: Pulmonary fibrosis, hyperpigmentation |
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Doxorubicin (adriomycin)
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M: Generate free radicals, intercalate in DNA (create breaks, decr replication)
C: part of Abvd combo for Hodkins and myleomas, sarcomas, solid tumors T: Cardiotoxicity; myelosuppresion and marked alopecia. |
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Dactinomycin
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M: Intercalates in DNA
C: Wilm's tumor, Ewings sarcoma, rhabdomyosarcoma T: Myelosuppresion Childhood tumors |
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Bleomycin
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M: Induces free radical formation, breaks in DNA strands
C: Testicular cancer, lymphomas (aBvd) T: Pulmonary fibrosis, skin changes, minimal myelosuppresion |
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Hydroxyurea
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M: Inhibits Ribonucleotide Reductase - decr DNA synthesis
C: Melanoma, CML, sickle cell T: Bone marrow suppression, GI upset |
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Etoposide
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M: G2 phase specific, inhibits topisomerase II, incr DNA degradation
C: Small cell carcinoma of lung and prostate, testicular carcinoma T: Myelosuppression, GI irritation, alopecia |
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Prednisone (cancer)
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M: May trigger apoptosis/work on nondividing cells
C: CLL, Hodkings, immunosuppresant. T: Cushing like symptoms; immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis |
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Tamoxifen
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M: Estrogen-receptor antagonist in breast, agonist in bone
C: Breast cancer. Osteoporosis. T: May incr risk of endometrial cancer via partial agonist effects. Hot flashes. Raloxifene does not cause endometrial carc. |
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Trastuzumab (Herceptin)
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M: Mab against HER2.
C: Metastatic breast cancer for overexpressing HER2 tumors T: Cardiotoxicity |
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Imatinib
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GLEEVEC
M: BCR-ABL tyrosine kinase inhibitor C: CML, GI stromal tumors T: Fluid retention |
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Vincristine
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M: M-phase specific alkaloids bind to tubulin, block polymerization of mts so spindle can't form.
C: Lymphoma, Wilms' tumor, choriocarcinoma T: Neurotoxicity (areflexia, peripheral neuritis,) paralytic ileus. Vinblastine: myelosuppresion |
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Paclitaxel
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M: M-phase specific agents bind to tubulin, and prevent spindle break down
C: Ovarian, breast cancer T: Myelosuppresion and hypersensitivity |
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Cyclosporine
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M: Binds cyclophilins. Complex inhib. calcineurin, prevents production of IL-2/receptor, blocks activation/diff of T-cells.
C: Suppress organ rejection, select autoimmune disorders T: Predisposes pts to viral infections and lymphoma; nephrotoxic (prevent with mannitol diuresis) |
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Tacrolimus
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M: Binds to FK-binding protein, inhibits secretion of IL-2 and others
C: Potent immunosuppresive in organ transplants T: Significant - nephrotocix, peripheral neuropathy, hypertension, pleural effusion, hyperglycemia |
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Azothiporine
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M: Antimetabolite precursor of 6-MP, interferes with metabolism and synthesis of nucleic acids. Toxic to prolif. lymphocytes
C: Kidney tranplant, autoimmune dz (including glomerulonephritis and hemolytic anemia) T: Bone marrow suppression; active metabolite 6-mp metabolized by xanthine oxidase; toxic effects may be incr. by allopurinol |
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Muromonab (OKT3)
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M: Mab binds CD3 on surface of T cells. Blocks cellular interaction with CD3 protein responsible for T-cell transduction
C: Immunosuppresion post-trasnplant T: Cytokine release syndrome, hypersensitivity reaction |
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Sirolimus
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Rapamycin
M: Binds to mTOR. Inhibits T-cell proliferation in reponse to IL-2. C: Post-kidney transplant with cyclosporine and corticosteroids T: Hyperlipidemia, thrombocytopenia, leukopenia |
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Mycophenolate Mofetil
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Inhibits de novo guanine synthesis (conversion of IMP to GMP) and blocks lymphocyte production
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Daclizumab
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Mab with high affinity for IL-2 receptor on activated T-cells
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Filgrastim / Sargramostim
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G-CSF / GM-CSF
Bone marrow recovery |
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alpha / beta / gamma interferon
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Hep B/C, Kaposi Sarcoma, Leukemia
MS Chronic granulomatous disease |
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Mannitol
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M: Osmotic diuretic, incr tubular fluid osmolarity, incr urine flow. Act at PCT, dec limb
C: Shock, drug overdose, decr intracranial/intraocular pressure T: Pulmonary edema, dehydration. Contraindicated in anuria, CHF |
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Acetazolamide
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M: Carbonic anhydrase inhib. Self-limited NaHC03 diuresis and reduction in total bicarb stores. PCT and desc limb
C: Glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness T: Hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy |
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Furosemide
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M: Loop diuretic. Inhib cotransport (Na, K, 2 CL) of TALH. Abolish hypertonicity of medulla, prevents concentration of urine. Incr Ca excretion
C: Edematous states, HTN, hypercalcemia T: Ototoxicity, hypokalemia, dehydration, sulfa allergy, interstitial nephritis, gout |
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Ethacrynic acid
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M: Non-sulfa drug acts like furosemide
C: Diuresis in pts with sulfa-allergy T: Similar to furosemide |
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Hydrochlorothiazide
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M: Thiazide diuretic. Inhib NaCl reabsorption in DCT, reducing diluting capacity of nephron. Decr Ca excretion
C: HTN, CHF, hypercaliuria, nephrogenic diabetes insipidus T: Hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia. Lassitude. Sulfa allergy. |
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Spironolactone / Amiloride
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M: (S) Competitive aldosterone receptor antagonist in cortical collecting tubule
M: (A) Block Na+ channels in CCT C: Hyperaldosteronism, K+ depletion, CHF T: Hperkalemia, endocrine effects (spironolactone causes gynecomastia, antiandrogen effects) |
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Lisinopril
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M: Inhibit ACE, reduces level of ATII and prevents inactivation of bradykinin, a potent vasodilator. Renin release is inscr due to loss of feedback inhibition.
C: HTN, CHF, diabetic renal disease T: Cough, angioedema, proteinuria, taste changes, hypotension, fetal renal damage, rash, hyperkalemia. Avoid with bilateral renal artery stenosis. ARBs - No cough |
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Finasteride / Flutamide
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5a-reductase inhibitor, decreases conversion of testosterone to DHT. Used in BPH and balding.
Flutamide: nonsteroidal competitive inhibitor of androgens at testosterone receptor. Used in prostate cancer |
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Leuprolide
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M: GnRH analog with agonist properties if used in pulsatile fashion; antagonist hen used in continuous fashion
C: Infertility (pulsatile); prostate cancer (continuous - with flutamide) uterine fibroids T: Antiandrogen, nausea, vomiting |
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Sildenafil
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M: Inhibit cGMP phosphodiesterase, increasing cGMP. Smooth mm relaxation in corpus cavernosum, incr blood flow, boners
C: ED T: Headache, flushing, dyspepsia, impaired blue-green color vision. HTN WITH NITRATES |
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Mifepristone (RU-486)
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M: Competitive inhibitor of progestins at progesterone receptor
C: Termination of pregnancy (with misoprostol) T: Heavy bleeding, nausea, vomiting, anorexia, abdominal pain |
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HRT
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Relief or prevention of menopausal symptoms and osteoporosis
Unopposed estrogen therapy incr risk of endometrial cancer, so add progesterone. Possible incr CV risk. |
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Clomiphene
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SERM. Partial agonist in pituitary. Prevents normal feedback inhibition and incr release of LH and FSH from pituitary, stimualtes ovulation.
C: Infertility and PCOS. T: Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances |
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SERMS (Tamoxifen, raloxifen)
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Tamoxifen: Antagonist on breast tissue, treat and recurring ER-positive cancer. (Incr risk of endometrial cancer)
Raloxifine: Agonist on bone. Reduced resorption of bone, treat osteoporosis. |
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H-1 Blockers
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Block H1-receptor
1st gen (diphenhydramine) C: Allergy, motion sickness, sleep aid T: Sedation, antimuscarinic, anti-alpha-adrenergic 2nd generation (loratadine) C: Allergy T: Non-sedating, can't get into BBB |
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Isoproterenol / Albuterol / Salmeterol
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I: nonspecific B-agonist. Relaxes broncial mm (b2) but also tachycardia (B1)
A: Selective B2 agonist. Acute attack. S: Long-acting agent for prophylaxis - adverse effect is tremor and arrhythmia |
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Theophylline
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Methylxanthine
M: Inhibits phosphodiesterase, decr cAMP hydrolysis. C: Asthma (not really) T: Narrow therapeutic index. Cardiotoxicity, neurotoxicity. P-450 metabolizes. |
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Ipratropium
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Muscarinic antagonist
Competitive block of muscarinic receptors, prevents bronchoconstriction. Also for COPD. |
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Cromoyln
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Prevents release of mediators from mast cells. Only effective for prophylaxis of asthma, not acute attack. Toxicity is rare.
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Zileuton / Zafirlukat, montelukast
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Zileuton: 5-lipoxygenase inhibitor. Blocks conversion of AA to leukotrienes
Z/M: Block leukotriene receptor. Especially good for aspirin induced asthma |
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Bacteriostatic / Bacteriocidal
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Static: Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol
Cidal: Vancomycin, Fluoroquinolones, Penicllin, Aminoglycosides, Cephalosporins, Metronidazole |
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Penicillin
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M: B-lactam. Bind penicillin binding protein; block transpeptidase cross-linking of cell wall; activate autolytic enzymes
C: Cidal for G+ cocci, G- rods, G- cocci, spirochetes. Not penicillinase resistant. T: Hypersensitivity rxn, hemolytic anemia, nausea, diarrhea |
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Methicillin
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Nafcillin, dicloxacillin
M: B-lactam, but penicillinase resistant. (Bulkier R Group) C: Staph aureus (except MRSA; resistant b/c altered penicillin binding protein target site) T: Hypersensitivity rxn, interstitial nephritis (methicillin), bone marrow depression |
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Ampicillin/amoxicillin
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M: same as penicillin. Wider spectrum; penicillinase sensitive. Combine with clavulanic acid (penicillinase inhib) to enhance spectrum. Amox has great oral availability
C:better g+/g- coverage. (H flu, e coli, listeria, proteus, salmonella). ENT infx; lower resp. tract infx T: Hypersensitivity rxn, ampicillin rash, psuedomembranous colitis |
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Ticarcillin, carbenicillin, piperacillin
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Antipseudomonals
M: same as penicillin c: Pseudomonas and G- rods. Use with clavulanic acid T: Hypersensitivity rxn |
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Cephalosporins
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B-lactams, inhibit cell wall synth, less resistant to penicillinase, bacteriocidal
1st: (cefazolin, cephalexin) g+ cocci, proteus, e coli, klebsiela. Surgical prophylaxis 2nd: (cefoxitin, cefaclor, cefuroxime) H Flu, Enterobacter, Neisseria, Proteus, Klebsiella, Serratia 3rd: (ceftriaxone, ceftazidime, cefotaxime) serious G- infections resistant to others; meningitis (most get thru BBB). ceftazidime for pseudomonas, ceftriaxone for gonorrhea 4th: (cefepime) incr activity against psuedomonas and gram-positives T: Hypersensitivity Rxn. Crosses with penicillin in 5-10%. Incr nephrotoxicity of aminoglycosides; disulfiram-like rxn with ethanol in some |
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Aztreonam
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M: Monobactam resistant to b-lactamases. Inhibits cell wall synth (binds PBP3). Syngergistic with aminoglycosides. No cross-allergenicity with penicillin.
C: G- rods - klebsiella, pseudomonas, serratia. No activity against G+ or anaerobes. For penicillin-allergic pts and those with renal failure T: Usually nontoxic. Occasional GI upset. No cross-sensitivity with pen or ceph. Skin rashes, elevated LFTs |
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Imipenim/cilastatin
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M: Broad spectrum, b-lactamase resistant carbapenem. Always w/ cilastatin (inhibitor of rehnal dihydropeptidase I) to dec inactivation in renal tubules
C: G+ cocci, g- rods, and anaerobes. Best for enterobacter. Only if life-threating infx, or others have failed. T: GI distress, skin rash, CNS toxicity (seizures.) Meropenem-reduced CNS risk, stable to dihydropeptidase. |
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Vancomycin
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M: Inhibits cell wall mucopeptide formation, binding D-ala D-ala portion of cell wall precursors. Cidal. Resistance occurs with amino acid change to D-ala D-lac.
C: For serious, G+ multidrug resistant infx, incl s. aureus, and c-diff. T: Nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing ("red man synd") prevent with antihistamines, slow infusion. Chills, fever. |
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Protein synthesis inhibitors
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30S: Aminoglycosides/Tetracyclines
50S: Chloramphenicol, clindamycin, erythromycin, lincomycin, linezolid |
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Aminoglycosides
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Gentamicin, Tobramycin, Streptomycin etc
M: Cidal. Inhibit formation fo initiation complex and cause misreading of mRNA. Require 02 for uptake; ineffective against anaerobes. C: Severe G- rod infx. Synergistic w/ B-lactam abx. Neomycin used for bowel surgery. T: Nephrotoxicity (esp w/ cephalosporins) ototoxicity (esp w/loop diuretics); Teratogen. Optic nerve tox with streptomycin. Neuromuscular blockade (rare) |
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Tetracyclines
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Tetra/doxy/demeclocycline
M: Static; bind 30S, prevent attachment of tRNA; limited CNS penetration. Doxy is fecally eliminated, used in renal failure. NOT take with milk, antacids, or iron-containing preps because divalent cations inhibit its absorption in gut. C: Vibrio, Acne, Chlamydia, Ureplasma, Urealyticum, Mycoplasma pneumo, Tularemia, H Pylori, Borrelia burdorferi, Rickettsia T: GI Distress, discolored teeth, inhibits bone growth in kids, photosensitivity. Contraindicated in pregnancy |
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Macrolides
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Erythro/azithro/clarithromycin
M: Inhibit protein synth by blocking translocation; bind to 23S rRNA of 50S subunit. Static. C: UTIs, pneumonias, STDs - G+ cocci (strep in pts w/ penicillin allergy), Mycoplasma, Legionella, Chlamydia, Neisseria T: GI discomfort (common cause of non-compliance), acute cholestatic hepatitis, eosinophilia, skin rashes. Incr serum conc. of theophyllines, oral anticoags. |
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Chloramphenicol
|
M: Inhibits 50S peptidyltransferase activity. Static.
C: Meningitis (H Flu, Neisseria, S pneumo). Conservative use, due to toxicity. T: Anemia (does dependent); aplastic anemia (dose independent); gray baby syndrome (in premi infants b/c they lack liver UDP glucuronyl transferase |
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Clindamycin
|
M: Blocks translocation at 50S. Static.
C: Anaerobic infx, above diaphragm (Bacteroides fragilis, clostridium perfingens.) T: Pseudomembranous colitis, fever, diarrhea. |
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Sulfonamides
|
Sulfamethoxazole, sulfadizine
M: PABA antimetabolites inhibit dhydropteroate synthetase. Static. C: G+, G-, Nocardia, Chlamydia. Triple or SMX for UTIs T: Hypersensitivity rxn, hemolysis if G6PD, nephrotoxic (tubulointerstitial nephritis), photosensitivity, kernicterus in infants, displace other drugs from albumin. Vomiting, diarrhea, stevens-johnson |
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Trimethoprim
|
M: Inhibits bacterial dihydrofolate reductase. Static.
C: Use w/ sulfonamides (TMP-SMX.) causing sequential block of folate synth. Combo used for recurrent UTIs, shigella, salmonella, pneumocystis jiroveci T: Megaloblastic anemia, leukopenia, granulocytopenia. (May alleviate with supp. folinic acid). N/V/D. Rash. CNS disturbance. |
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Fluoroquinolones
|
Cipro/nor/ofloxacin
M: Inhibit DNA gyrase (topoisomerase II). Cidal. Not taken with antacids. C: G- rods of urinary and GI tracts (incl pseudomonas), neisseria, some G+ orgs. T: GI upset, superinfx, skin rashes, headache, dizziness. Contraindicated in pregnant women and children b/c animal studies show damage to cartilage. Tendonitis and tendon rupture in adults; leg cramps/myalgias in kids. |
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Metronidazole
|
M: Forms toxic metabolites in the bacterial cell that damages DNA. Cidal.
C: Antiprotozoal. Giardia, Entamoeba, Trichomonas, Gardnerella, Anaerobes. Use with bismuth and amoxicillin (or tetracycline) for 'triple therapy' against H Pylori T: Disulifram-like rxn w/ alcohol; headache; metallic taste |
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Polymyxins B, E
|
M: Bind to cell membranes of bacteria and disrupt their osmotic properties. Are cationic, basic proteins that act like detergents
C: Resistant G- infx T: Neurotoxicity, ATN |
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Antimycobacterial:
M. Tuberculosis M. avium-intracellulare M. leprae |
M. tub: Isoniazid (prophylaxis) plus rifampin, ethambutol, pyrazinamide, streptomycin
M. ai: Azithromycin (prophylaxis) plus rifampin, ethambutol, streptomycin M: Lep: no prophylaxis, use dapsone, rifampin, clofazimine |
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Isoniazid (INH)
|
M: Decr synth of mycolic acids
C: M. tuberculosis. Only agent used as solo-prophylaxis against TB. T: Hemolysis if G6PD, neurotoxicity, hepatotoxicity, SLE-like syndrome. Pyridoxine (Vit B6) can prevent neurotoxicity. |
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Rifampin
|
M: Inhibits DNA-dependent RNA polymerase.
C: M. tuberculosis; delays resistance to dapsone in leprosy treatment. Meningococcal prophylaxis and chemoprophylaxis in contacts of kids w/ H Flu. T: Minor hepatotoxicity and drug interactions (incr P-450); orange body fluids (non-hazardous.) |
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Prophylaxis:
Meningococcal infx Gonorrhea Syphillis |
Mening: Rifampin, or minocycline
Gonor: Ceftriaxone Syph: Benzathine penicillin G |
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Prophylaxis:
Recurrent UTIs Pneumocystis jiroveci Endocarditis w/ surgical, dental |
UTIs: TMP-SMX
P jiro: TMP-SMX, or aerosolized pentamidine Endocar: Penicillins |
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Amphotericin B
|
M: Binds ergosterol; forms membrane pores, leakage of electrolytes
C: Wide spectrum of systemic mycoses. Cryptococcus, Blastomyces, coccidioides, aspergillus, histoplasma, candida, mucor. Intrathecal for fungal meningitis. Doesnt cross BBB T: Fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis. Hydration reduced nephrotoxicity. Liposomal amph. reduced toxicity. |
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Nystatin
|
M: Binds to ergosterol, disrupting fungal membranes. Too toxic for systemic use
C: Swish and Swallow for oral candidiasis; topical for diaper rash or vaginal candida |
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Azoles
|
Fluconazole, ketoconazole, miconazole
M: Inhibits ergosterol synthesis C: Systemic mycoses. Fluconazole for cryptococcal meningitis in AIDS patients (can cross BBB) and candidal infx. Ketoconazole for blastomyces, coccidiodes, histoplasma, candida; hypercortisolism. T: Hormone synthesis inhibition (gynecomastia); liver dysfunction (inhibits P-450), fever, chills |
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Flucytosine
|
M: Inhibits DNA synthesis by conversion to fluorouracil, which competes with uracil
C: Systemic fungal infx (candida, cryptococcus) in combo w/ amphotericin b T: Nausea, vomiting, diarrhea, bone marrow supression |
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Caspfungin
|
M: Inhibits cell wall synthesis
C: Invasive aspergillosis T: GI upset, flushing |
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Terbinafine
|
M: Inhibits fungal enzyme squalene epoxidase
C: Used to treat dermatophytoses (especially onychomycosis) |
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Griseofulvin
|
M: Interferes with mt formation; disrupts mitosis. Deposits in keratin-containing tissues (e.g. nails)
C: Oral treatment of superficial infx; inhibits growth of dermatophytes (tinea, ringworm) T: Teratogenic, carcinogenic, confusion, headaches, incr P-450 and warfarin metabolism |
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Amantadine
|
M: Blocks viral penetration/uncoating (M2 protein); may buffer pH of endosome. Also causes release of dopamine from intact nerve terminals.
C: Prophylaxis and treatment for influenza A; Parkinson's disease T: Ataxia, dizziness, slurred speech R: Mutated M2 protein. 90% of influenza A is resistant. Rimantidine is a derivative that doesnt cross BBB. |
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Zanamivir, oseltamivir
|
M: Inhibit influenza neuraminidase, decrease release of progeny virus
C: Influenza A and B |
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Ribavirin
|
M: Inhibit synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase
C: RSV, chronic hep C T: Hemolytic anemia. Severe teratogen. |
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Acycolvir
|
M: Monophosphorylated by HSV/VSV thymidine kinase. Triphosphate formed by cellular enzymes. Preferentially inhibits viral DNA polymerase by chain termination
C: HSV, VZV, EBV. Used for HSV-induced mucocutaneous and genital lesions as well as for encephalitis. Prophylaxis in immunocompromised pts. No affect on latent forms of HSV/VZV. T: Generally well tolerated. R: Lack of thymidine kinase. |
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Foscarnet
|
M: Viral DNA polymerase inhibitor that binds to pyrophosphate-binding site of enzyme. Doesnt require activation by viral kinase.
C: CMV retinitis in immunocompromised pts when ganciclovir fails; acyclovir resistant HSV T: Nephrotoxicity, hyper/hypo calcemia,phosphatemia, penile ulcerations R: Mutated DNA polymerase |
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Ganciclovir
|
M: 5'-monophosphate formed by CMV viral kinase or HSV/VZV thymidine kinase. Triphosphate formed by cellular kinases. Preferentially inhibits viral DNA polymerase.
C: CMV, especially in immunocompromised T: Leukopenia, neutropenia, thrombocytopenia, renal toxicity. More toxic to host enzymes than acyclovir R: Mutated CMV DNA polymerase or lack of viral kinase |
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Protease inhibitors
|
Saqui/rito/indi/nelf/"NAVIR"
M: Inhibit assembly of new virus by blocking protease in progeny virons C: HIV T: GI intolerance (nausea, diarrhea), hyperglycemia, lipodystrophy, thrombocytopenia (indinavir) |
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Reverse-transcriptase inhibitors
|
Nucleosides: Zidozudine(ZDV/AZT), didanosine (ddI), zalcitabine(ddC), stavudine(drT), lamivudine(3TC), abacavir
Non-nuclesodies: Nevirapine, Efavirenz, Delviridine M: Preferentially inhibit reverse transcriptase; prevents incorporation of DNA copy of viral genome into host C: HAART normally combos protease inhibs with RTIs. ZDV used for general prophylaxis and during pregnancy to reduce risk of fetal transmission T: Bone marrow suppression, peripheral neuropathy, lactic acidosis (nucs), rash (non nucs) megaloblastic anemia (ZDV) GM-CSF and epo can be used to reduce toxicity |
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Enfuvirtide
|
M: Bind viral gp41 subunit; inhibit conformational change required for fusion with CD4 cells. Block entry and therefore replication.
C: HIV; pts with persistent viral replication despite other therapy T: Hypersensitivity rxns, rxns at Sub-q injection site, incr risk of bacterial pneumonia |
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Interferons
|
M: Glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis. Induce ribonuclease that degrades viral mRNA.
C: IFN-a (chronic hep b and c, kaposi sarcoma); IFN-b (MS); IFN-g (chronic granulomatous disease) T: Neutropenia |
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Hydralazine
|
M: Incr cGMP-->smooth mm relax. Vasodilates arterioles > veins; afterload reduction.
C: Severe HTN, CHF. First line therapy for HTN in pregnancy, with methyldopa T: Compensatory tachycardia (contraindicated in angina/CAD), fluid retention. Lupus-like syndrome. Nausea, headache, angina. |
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Minoxidil
|
M: K+ channel opener-hyperpolarizes and relaxes vascular smooth mm.
C: Severe HTN T: Hypertrichosis, pericardial effusion, reflex tachycardia, angina, salt retention |
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Ca+ Channel blockers
|
nifedipine (dihydropyridine), verapamil, diltiazem
M: Block voltage-dependent L-type Ca channels of cardiac and smooth mm, reducing contractility. Vascular: nifedipine>diltiazem>verapamil Heart: verapamil>diltiazem>nifedipine C: HTN, angina, arrhythmia (not nifedipine), Prinzmetal's angina, Raynaud's T: Cardiac depression, peripheral edema, flushing, dizziness, constipation (verapamil), AV block (verapamil), nausea |
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Nitroglycerin
|
Also isosorbide dinitrate
M: Vasodilate veins>>arteries, by releasing NO in smooth mm, causing incr in cGMP and smooth mm relaxation. Decr preload. C: Angina, pulmonary edema. (also aphrodisiac and erection enhancer) T: Tachycardia, hypotension, flushing, headache. "Monday Disease" in industrial exposure: increasing tolerance over week, lost during weekend, tachycardia dizziness and headache on reexposure |
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Malignant HTN treatment
|
Nitroprusside: Short acting; Incr cGMP via direct NO release. Dilate arteries and veins. Cyanide toxicity.
Fenoldopam: Dopamine D1 receptor agonist - relaxes renal vascular smooth mm Diazoxide: K+ channel opener-hyperpolarizes and relaxes vascular smooth mm in periph arteriole. Hyperglycemia, reflex tachycardia. |
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HMG-Coa reductase inhibitors
|
M: Inhibit cholesterol precursor synthesis.
C: Markedly lowers LDL, somewhat raise HDL, somewhat lower TGs. T: Expensive, reversible incr in LFTs, myositis (occasional rhabdomyolysis-->liver failure) |
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Niacin
|
M: Inhibits lipolysis in adipose tissue; reduce hepatic VLDL secretion into circulation
C: lower LDL, raise HDL, somewhat lower TGs. T: Red, flushed face, which is decr by aspirin or long-term use |
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Cholestyramine / colestipol
|
M: Bile acid resins. Prevent intestinal reabsorption of bile acids; liver must use cholesterol to make more
C: Decrease LDL, slightly raise HDL and TGs T: People hate it - tastes bad, GI discomfort, decr absorption of Vit D,A,K,E |
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Ezetimibe
|
M: Prevent cholesterol from diet at small intestine brush border
C: Lower LDL T: Rare increase in LFTs |
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Gemfibrozil / fenofibrate
|
Fibrates
M: Upregulate LPL --> incrs TG clearance C: somewhat lower LDL, somewhat raise HDL, markedly lower TGs T: Myositis, incr in LFTs |
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Digoxin
|
HUGE (40 hour) half life
M: Direct inhibition of Na/K ATPase leads to indirect inhibition of Na/Ca antiporter. Leads to increase in intracellular Ca, and positive inotropy. C: CHF (incr contractility); atrial fib (decr. conduction at AV node, depression of SA node.) T: May cause incr PR, dec QT, scooping of ST segment, T-wave inversion. Also incr parasympathetic activity: nausea, vomiting, diarrhea, blurry yellow vision. Arrhythmia. Worse in renal failure, hypokalemia, and with quinidine. Antidote: Slowly normalize K, lidocaine, cardiac pacer, anti-dg Fab fragments, Mg |
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Class IA antiarrhythmics
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Quinidine, Amiodarone, Procainamide
M: Incr AP duration, incr refractory period, incr QT interval. C: Affect both atrial and ventricular arrhythmias, especially reentrant and ectopic supraventricular and ventricular tachys T: Quinidine (cinchonism-headache, tinnitus, thrombocytopenia; torsades de pointes); procainamide (reversible SLE-like syndrome) |
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Class IB antiarrhythmics
|
Na+ Channel blockers
Lidocaine, Mexiletine, Tocainide M: Decr AP duration. Affect ischemic or depolarized Purkinje and ventricular tissue C: Acute ventricular arrhytmias (esp post-MI) and in digitalis induced arrhythmias T: local anesthetic. CNS stimulation/depression, cardiovascular depression. |
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Class IC antiarrhythmics
|
Na+ channel blockers
Flecainide, encainide, propafenone M: No affect on AP duration C: Useful in V-tachs that progress to VF and in intractable SVT. Usually only a last resort in refractory tachyarrhythmias T: proarrhythmic, esp post-MI (contraindicated). Significantly prolongs refractory period in AV node. |
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Class II antiarrhythmics
|
B Blockers.
propranolol, esmolol, metoprolol, atenolol, timolol M: Decr. cAMP, Ca++ currents. Supress abnormal pacemakers by decr slope of phase 4. AV node particularly sensitive. Incr PR interval. Esmolol very short acting. C: V-tach, SVT, slowing ventricular rate during a-fib and a-flutter. T: Impotence, exacerbation of asthma, CV effects (bradycardia, AV block, CHF), CNS effects (sedation, sleep alteration). May mask signs of hypoglycemia. Metoprolol can cause dyslipidemia. |
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Class III antiarrhythmics
|
K+ channel blockers
Sotalol, ibutilide, betylium, amiodarone M: Incr AP duration, incr refractory period. Incr QT interval. Used when other antiarrhythmics fail. T: Sotalol - torasdes de pointes, excessive b-block; ibutilide - torsades; bretylium - new arrhythmias, hypotension; amiodarone: pulmonary fibrosis, corneal deposits, hepatotoxicity, skin deposits (photodermatitis), neurologic effects, constipation, CV effects, thyroid disregulation. |
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Class IV antiarrhthymics
|
Ca channel blockers
Verapamil, diltiazem M: Primarily affect AV nodal cells. Decr conduction velocity, incr ERP, PR interval. C: Used in prevention of nodal arrhythmias (e.g. SVT) T: Constipation, flushing, edema, CV effects (CHF, AV block, sinus node depression) |
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Other antiarrhythmics
|
Adenosine: Increase K out of cells - hyperpolarizes cell. Drug of choice in diagnosing/abolishing AV nodal arrhythmias. Short acting (15 secs) Flushing, hypotension, chest pain.
K+: depress ectopic pacemakers in hypokalemia (digoxin toxicity) Mg++: Effective in torsades do pointes and digoxin toxicity. |
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Opiod analgesis
|
morphine, fentanyl, codeine, heroine, methadone
M: Agonists at opiod receptors (mu=morphine; delta=enkephalin; kappa=dynorphin) to modulate synaptic transmission C: Pain, cough supression (dextromethorphan), diarrhea (loperamide and diphenoxylate), acute pulmonary edema, maintenance programs for addicts T: Addicton, respiratory depression, constipation, miosis (pinpoint pupils), additive CNS depression w/ other drugs. Tolerance does not develop to miosis and constipation. Toxicity treated w/ naloxone or naltrexone. |
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Carbamazepine
|
M: Blocks sodium channels
C: 1st line for tonic-clonic seizures, trigeminal neuralgia. Can use for all partials. T: Diplopia, ataxia, blood dyscrasias, liver toxicity, teratogenic, induces P-450. |
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Lamotrigine
|
M: Block voltage gated Na channels
C: All partials, tonic-clonic T: Stevens-Johnson syndrome |
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Gabapentin
|
M: Increase GABA release
C: All partials, tonic-clonic, peripheral neuropathy T: Sedation, ataxia |
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Topiramate
|
M: Block Na Channels, Incr GABA action
C: All partials, tonic-clonic T: Sedation, mental dulling, kidney stones, weight loss |
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|
Phenobarbital
|
M: Increase GABA action
C: All partials, tonic-clonic, 1st line in pregnant women, children T: Sedation, tolerance, dependence, induction of P-450 |
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|
Valproic acid
|
M: Block Na channels, incr GABA concentration
C: 1st line for tonic-clonic. Can be used for absence seizures, myoclonic seizures. All partials. T: GI distress, rare but fatal hepatotoxicity, neural tube defects in fetus, tremor, weight gain. Contraindicated in pregnancy. |
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Ethosuximide
|
M: Blocks thalamic T-type Ca Channels
C: 1st line for absence seizures T: GI distress, fatigue, headache, urticaria, Stevens-Johnson syndrome |
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|
Benzodiazepines
|
diazepam/lorazepam
M: Increase GABA action by incr frequency of Cl- opening. C: 1st line for acute status epilepticus. Also for seizures of eclampsia. (MgS04 is used to prevent those.) Anxiety, spasticity, detox, night terrors, sleepwalking. T: sedation, tolerance, dependence, CNS depression Overdoze treated with flumazenil |
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Phenytoin
|
M: Blocks Na channels; inhibition of glutamate release presynaptically
C: 1st line tonic-clonic defense. Prophylaxis of status epilepticus. Class IB antiarrhythmic. Partials. T: Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsuitism, megaloblastic anemia, teratogenesis, SLE-like syndrome, induces P-450 |
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Barbiturates
|
Pheno/pentobarbitol, thiopental
M: Incr duration of Cl- channel, facilitate GABA action C: Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental) T: Dependence, additive CNS depression effects with EtOH, respiratory or CV depression, induction of P-450 Treat overdose with symptom management |
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|
Inhaled anesthetics
|
halothane, isoflurane, sevoflurane
M: Unknown Effects: Myocardial depression, respiratory depression, nausea/emesis, incrs cerebral blood flow (decr cerebral metabolic demand) T: Hepatotoxicity (halothane), nephrotoxicity (methoxyflurane), proconvulsant (enflurane) malignant HTN (rare) |
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IV anesthetics
|
Barbiturates: Thiopental-high potency, lipid soluble, rapid brain entry. Induction of anesthesia and short procedure. Decr cerebral blood flow.
Benzo: Midazolam most common for endoscopy; used adjunctively with gas and narcotics. May cause postop resp depression, decr BP Ketamine: PCP analog, dissociative anesthetic. CV stimulant. Hallucinations. Incr cerebral blood flow. Propofol: Rapid anesthesia induction and short procedures. Les postop nausea than thiopental. |
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Local anesthetics
|
Esters: procaine, cocaine; amides:lidocaine, etc
M: Block Na channels on receptors of inner part of channel. Preferentially bind to activated Na channels, most effective in rapidly firing n. C: Minor surgical procedures, spinal anesthesia. T: CNS excitation, severe CV toxicity, HTN and arrhythmia (cocaine) Principle: In acidic infected tissue, alkaline anesthetic charged, can't penetrate. use more; effects small-myelinated > small-unmy > large my > large unmy; given with vasoconstrictors to enhance local action |
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Neuromuscular blocking drugs
|
Used for muscle paralysis in surgery of mechanical ventilation. Selective for motor nicotinic receptor.
Depolarizing: Succinylcholine. Fast acting. Can cause hypercalcemia and hyperkalemia. To reverse it, initially you can't. In Phase II, antidote is cholinesterase inhibitors (neostigmine.) Nondepolarizine (tubocurarine, the "oniums" and "curiums." Compete with ACh for receptors. Can reverse with neostigmine, edrophonium, other cholinesterase inhibs. |
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Dantrolene
|
M: Prevents release of Ca++ from sarcoplasmic reticulum of skeletal mm
C: Malignant hyperthermia, also to treat neuroleptic malignant syndrome. T: and GI CNS side effects |
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|
Bromocriptine / Amantadine / Benztropine
|
B: Ergot alkaloid, Partial agonist at dopamine receptors, used for Parkinsons. Supplement L-dopa. Treats hyperprolactinemia. GI, CV disturbances.
A: May increase dopamine release. Also an antiviral against influenz A and rubella. Initial therapy. Ataxia. Benz: Antimuscarinic used for parkinsons. |
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L-Dopa/carbidopa
|
M: Incr level of dopamine in brain. L-dopa can cross BBB and is converted by dopa-decarboxylase in CNS.
C: Parkinsons T: Arrhythmias from peripheral conversion. Long-term use:dyskinesia following administration, akineseia b/t doses. Carbidopa, a peripheral decarboxlase inhib, given to incr bioavailability of L-dopa in brain, limit peripheral side effects. |
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Selegiline
|
M: Selectively inhibits MAO-B, thereby incr availability of dopamine
C: Adjunctive agent to L-dopa in parkinsons T: May enhance adverse effects of L-dopa |
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|
Sumatriptan
|
M: 5-HT agonist. Causes vasoconstriction. Half-life < 2 hours.
C: Acute migrane, cluster headache attacks. T: Coronary vasospasm, mild tingling (contraindicated in CAD or Prinzmetals pts), HTN emergencies |
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|
Anti-psychotics (neuroleptics)
|
Haloperidol + the "azines"
M: Most block D2 dopamine receptors C: Schizophrenia (mostly positive symptoms), psychosis, acute mania, Tourette's T: Extrapyramidal side effects, endocrine side effects (hyperprolactinemia) and SE from blocking muscarinic (dry mouth, constipation), a (hypotension) and histamine (sedation) receptors. Tardive dyskinesia (parkinsons like effects.) Neuroleptic malignant syndrome: rigidity, myoglobinuria, autonomic instability, hyperpyrexia (treat with dantrolene and dopa agonists.) |
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|
Atypical anti-psychotics
|
Clozapine, olanzapine, risperidone, aripiprazole
M: Block 5-H2 and dopaminic receptors. Variable M, alpha1, H1 blockade. C: Schizophrenia; useful for positive and negative symptoms. Olanzapine also used for OCD, anxiety disorder, depression, mania, Tourettes. T: Fewer extrapyramidal and anticholinergic effects. Clozapine may cause agranulocytosis. |
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Lithium
|
M: Not established. Possibly inhibits phosphoinositol cascade.
C: Mood stabilizer for bipolar; blocks relapse and acute manic events. T: Tremor, hypothyroidism, polyuria (ADH antagonist) teratogenic. Narow therapeutic window. |
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|
Buspirone
|
M: Stimulates 5-HT receptors.
C: Anxiolysis for GAD. Does not cause sedation or addiction. Does not interact with EtOH. |
|
|
SSRIs
|
fluoxetine, sertraline, paroxetine, citalopram
M: Seratonin reuptake inhibitors C: Endogenous depression, OCD T: Fewer than TCAs. GI distress, sexual dysfunction. "Serotonin syndrome" with MAO inhibitors - hyperthermia, muscle rigidity, CV collapse |
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|
Tricyclics
|
Imipramine, amitriptyline, clomipramine, nortryptyline, desipramine, doxepin, amoxapine
M: Blocks reuptake of NE and serotonin C: Major depression, bedwetting (imipramine), OCD (clomipramine) T: Sedation, alpha blocking effects, atropine-like effects. Convulsions, Coma, Cardiotoxicity; respiratory depression, hyperpyrexia. |
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Other antidepressants
|
Bupropion: smoking cessation too. Mech not known. Stimulant effects (tachycardia, insomnia), headache, seizures in bulemics. No sexual side effets
Venlafaxine: Also in GAD. Inhibit serotonin, NE, and dopamine. Stimulant effects, sedation, nausea, constipation, HTN. Mirtazapine: alpha2 antagonist and 5-HT antagonist. Sedation, hyperphagia, weight gain, dry mouth. Maprotiline: Blocks NE uptake. Sedation, orthostatic hypertension. Trazodone: Serotonin reuptake inhib. Sedation, nausea, priapism, postural hypotension. |
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|
MAO inhibitors
|
Phenelzine, tranylcypromide
M: Nonselective irreversible MAO inhibition, incr levels of amine neurotransmitters. C: Atypical depression, anxiety, hypochondriasis T: Hypertensive crisis with tyramine ingestion (wine and cheese) and B-agonists; CNS stimulation. Contraindicated with SSRIs or meperidine (to prevent serotonin syndrome.) |
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|
Bethanecol
|
M: Direct cholinergic agonist. Favors M3 receptors. Acts on Bladder and Bowel.
C: Post-op and neurogenic ileus and urinary retention. T: DUMBLESS. Contraindicated in asthma, hyperthyroidism, coronary insufficiency, PUD |
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|
Carbachol
|
M: Direct cholinergic agonist. Contracts ciliary mm to open canal of schlemm.
C: Wide-angle glaucoma, release of intraocular pressure, pupillary constriction. T: DUMBLESS. Contraindicated in asthma, hyperthyroidism, coronary insufficiency, PUD |
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|
Pilocarpine
|
M: Direct cholinergic agonist. Favors M receptors. Potent stimulator of sweat, tears, saliva
C: Wide-angle glaucoma, and xerostomia in head and neck cancers. T: DUMBLESS. Contraindicated in asthma, hyperthyroidism, coronary insufficiency, PUD |
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|
Methacholine
|
M: Direct cholinergic agonist. Stimulates muscarinic receptors in airways when inhaled.
C: Challenge test for asthma. |
|
|
Neostigmine
|
M: Indirect cholinergic agonist (anti-acetycholinesterase)
C: Post-op and neurogenic ileus and urinary retention; myasthenia gravis; post-op reversal of neuromuscular blockade. T: DUMBLESS |
|
|
Pyridostigmine
|
M: Indirect cholinergic agonist (anti-acetycholinesterase)
C: Myasthenia Gravis (long acting); doesn't penetrate CNS T: DUMBLESS |
|
|
Edrophonium
|
M: Indirect cholinergic agonist (anti-acetycholinesterase)
C: Diagnosis of Myasthenia gravis. (Extremely short acting) T: DUMBLESS |
|
|
Physostigmine
|
M: Indirect cholinergic agonist (anti-acetycholinesterase)
C: Applied topically for wide-angle glaucoma. Crosses BBB. Used in atropine overdose. T: DUMBLESS |
|
|
Echothiopate
|
M: Irreversibly binds acetylcholinesterase.
C: Second line glaucoma agent. T: DUMBLESS |
|
|
DUMBLESS (organophosphate poisoning)
|
Diarrhea, Urination, Miosis, Bronchoconstriction, Lacrimation, Excitation (skeletal mm and CNS), Salivation, Sweating. And abdominal cramps.
Atropine (muscarinic antagonist) and pralidoxine (chemical antagonist that regnerates active cholinesterase) for overdose. |
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|
Atropine
|
M: Muscarinic antagonist (competitive inhib)
C: Blocks DUMBLESS. Mydriasis. Cardiac arrest. T: Hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter |
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|
Scopolamine
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M: Muscarinic antagonist. (Competitive inhib.) Acts on CNS.
C: Motion sickness. T: Anti-DUMBLESS. "Dry as a bone..." |
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Ipratropium
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M: Muscarinic antagonist. Competitive inhib.
C: Inhaled, used as bronchodilator in COPD. T: Poor distribution, less risk of side effects |
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Methoscopolamine, oxybutynin, glycopyrrolate
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M: Muscarinic antagonist
C: Genitourinary. Reduce urgency in mild cystitis and reduce bladder spasms. |
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Pirenzepine, propantheline
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M: Muscarinic antagonist
C: Gastrointestinal. Decrease secretion in patients with PUD |
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Glaucoma drugs (condensed)
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alpha agonists and beta blockers can lead to mydriasis, but the vasoconstriction also decr aqueous humor synthesis.
acetozolamide decr HCO3 and leads to decr of aqueous humor Cholinomimetics contract ciliary mm, incr outflow of aqueous humor Prostaglandin (latanoprost PGF2) increases outflow of aqueous humor) |
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Hexamethonium
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M: Nicotinic antagonist
C: Ganglionic blocker. Used in experimental models to prevent vagal reflux responses to changes in blood pressure - eg. prevents reflex bradycardia caused by NE T: Severe orthostatic hypotension, blurred vision, constipation, sexual dysfunction |
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Epinephrine
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M: Nonselective sympathomimetic.
C: Anaphylaxis, glaucoma (open angle), asthma, hypotension T: HR increases, Pulse Pressure increases, TPR decreaes slightly |
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Norepinephrine
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M: alpha > Beta
C: Hypotension (causs vasoconstriction) T: Decreased renal perfusion. HR deceases (reflex bradycardia), BP increases, TPR increases |
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Isoproterenol
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M: Beta>Alpha
C: AV block (rare); bronchodilator for asthma T: HR increases, BP decreases (pulse pressure increases), TPR decreases |
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Dopamine
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M: D > beta > alpha; inotropic and chronotropic
C: Tx or cardiogenic shock, CHF, acute renal failure - important b/c it can maintain renal blood flow T: High doses can lead to vasoconstriction through alpha stimulation |
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Dobutamine
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M: B1 > B2; inotropic but not chronotropic
C: Shock, heart failure, cardiac stress testing |
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Phenylephrine
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M: alpha 1 > alpha 2
C: Pupillary dilation, vasoconstriction, nasal decongestion |
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Albuterol
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MAST: Metaproterenol, albuterol, salmeterol, terbutaline
M: Selective b2 agonist. C: salmeterol is longer acting - better for prophylaxis. T: Minimal side effects. |
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Amphetamine
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M: Indirect general sympathetic agonist, release stores catecholamines.
C: Narcolepsy, obesity, ADD T: Restlessness, tremor, insomnia, anxiety, tachycardia |
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Ephedrine
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M: Indirect general sympathetic agonist, releases stored catecholamines
C: Nasal decongestion, urinary incontinence, hypotension T: Restlessness, tremor, insomnia, anxiety, tachycardia |
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Cocaine
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M: Indirect general sympathetic agonist. Uptake inhibitor.
C: vasoconstriction and local anesthesia. T: Acting like a dick. |
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Clonidine / methyldopa
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M: Act as alpha-2 receptor agonists, reduce sympathetic tone. (decr. peripheral resistance, HR, and plasma renin activity)
C: HTN (especially in renal disease), CHF T: Mild edema, bradycardia, drowsiness, dizziness, headache. HTN with high dose. |
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Phenoxybenzamine
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M: Irreversible non-selective alpha-adrenergic antagonist.
C: Pheochromocytoma, peripheral vasodilation in Raynaud's T: Enters CNS (sedation and fatigue), orthostatic hypotension |
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Phentolamine
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M: Reversible, non-selective alpha-blocker
C: Hypertensive emergencies, once used with pheos, peripheral vasodilation in Raynauds T: Reflex tachycardia, arrhytmias, orthostatic hypotension |
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Prazosin, Terazosin, doxazosin
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M: selective alpha-1 blocker. Relaxes arterial and venous smooth mm
C: BPH, HTN T: 1st dose orthostatic hypotension (take before bedtime), dizziness, headache |
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Mirtazapine
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M: selective alpha-2 blocker
C: Depression T: Sedation, incr serum cholesterol, incr appetite |
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Non-selective Beta blockers
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Propranolol, timolol, nadolol, pindolol, sotalol
M: Blocks Beta1,2 receptors C: HTN, Angina, hyperthroidism, arrhythmias, CHF (not acute) T: Impotence, exacerbation of asthma, cardiovascular (bradycardia, AV block, CHF), CNS (sedation, sleep alterations), cold extremeties; use in caution with diabetics. |
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Selective Beta-1 blockers
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Acebutolol (partial agonist) Betaxolol, Esmolol (short acting), Atenolol, Metoprolol
M: Selective Beta-1 blockade C: HTN, angina, hyperthyroidism T: Impotence, exacerbation of asthma, cardiovascular (bradycardia, AV block, CHF), CNS (sedation, sleep alterations); use in caution with diabetics. |
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Nonselective alpha/beta antagonists
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Carvedilol, Labetalol
M: Non-selective beta blocker, with alpha-1 blockade C: HTN, CHF T: Postural hypotension, dizziness, fatigue |
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Antidotes
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Acetaminophen: N-acetylcysteine
Salicylates: NaHC02 (alkalinyze urine), dialysis Amphetamines: NH4CL (acidify urine) Beta Blockers: Glucagon Digitalis: Stop dig, normalize K+, lidocaine, andi-dig Fab fragments, Mg2+ |
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Antidotes
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Iron: Deferoxamine
Lead: EDTA, dimercaprol, penicillamine Arsenic, mercury, gold: Dimercaprol (BAL), succimer Copper, arsenic, gold: Penicillamine |
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Antidotes
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Cyanide: Nitrite, hydroxocobalamin, thiosulfate
Methemoglobin: Methylene blue CO: 100% and hyperbaric 02 Methanol, antifreeze: ethanol, dialysis, fomepizole Opioids: Naloxone, naltrexone |
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Antidotes
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Benzos: Flumazenil
TCAs: NaHC03 (serum alkalinization) Heparin: Protamine sulfate Warfarin: Vit K, FFP tPa, streptokinase: Aminicaproic acid |
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Lead poisoning
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Lead lines on gingivae and epiphyseal xray
Encephalopathy and RBC basophilic stippling Abdomninal colic and sideroblastic anemia Foot and wrist drop. Dimercarpol and EDTA 1st line treatment. Succimer for kids. |
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Iron poisoning
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Iron overdose is one of leading toxicology fatalities in kids
Cell death due to peroxidation of membrane lipids Acute - gastric bleeding Chronic - metabolic acidosis, scarring leading to GI obstruction |
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P450 inducers
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Quinidine, Barbituates, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, St John's Wort
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P450 inhibitors
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Isoniazid, Sulfonamides, Cimetidine, Ketoconazole, Erythromycin, Grapefruit juice
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Reserpine
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M: Blocks reuptake of NE, DA, and 5-HT into pre-synaptic vesicles.
C: Mild to Moderate HTN. Has Anti-psychotic effects. T: Diarrhea, Parkinson-like syndrome, sedation, severe depression. |
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Guanethidine
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M: Prevents NE release from peripheral nerve terminals
C: HTN T: Rarely used due to side effects. Orthostatic hypotension, severe diarrhea, sexual dysfunction |
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Metyrosine
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M: Blocks tyrosine hydroxlase, interferes with DA synthesis. So, less NE and Epi secreted
C: Treatment of pheos, especially in pts with metastatic/inoperable disease T: Crystalluria, sedation, diarrhea, anxiety |
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Hemicholinium / Vesamicol
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Experimental anticholinergic drugs.
Hemicholinium: Blocks reuptake of choline into presynaptic terminal Vesamicol: Blocks ACh uptake into presynaptic vesicles |
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Echinecea
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C: Common Cold
T: GI distress, dizziness, headache |
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Ephedra
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C: Like ephedrine
T: CNS and CV stimulation; arrhythmias, stroke, seizures at high doses |
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Feverfew
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C: Migraine
T: GI distress, mouth ulcers, anitplatelet actions |
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Ginkgo
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C: Intermittent claudication
T: GI distress, anxiety, insomnia, headache, antiplatelet actions |
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Kava
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C: Chronic anxiety
T: GI distress, sedation, ataxia, hepatotoxicity, phototoxicity, dermatotoxicity |
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Milk Thistle
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C: Viral Hepatitis
T: Loose stools |
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Saw palmetto
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C: BPH
T: GI distress, decreased libido, HTN |
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St John's Wort
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C: Mild to moderate depression
T: GI distress and phototoxicity; serotonin syndrome with SSRIs; induced P-450 system. |
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Dehydroepiandrosterone
|
C: Symptomatic improvement in females with SLE or AIDS
T: Androgenization (premenopausal women), estrogenic effects (postmenopausal), feminization (young men) |
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Melatonin
|
C: Jet lag, insomnia
T: Sedation, suppresses midcycle LH, hypoprolactinemia |
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Alzheimers Treatment
|
Acetylcholinesterase inhibs used initially to slow progression. (Physostigmine, Tacrine, Donepezil, Rivastigmine)
As efficacy decreases, treatment shifts to symptomatic approach, including standard psych drugs like antidepressants and antipsychotics. |
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General Anesthetics Principles
|
CNS drugs must be lipid soluble to cross BBB, or be actively transported.
Drugs with decr solubility in blood = rapid induction and recovery times. Drugs with incr solubility in lipids = incr potency = 1/MAC Ex: N20 has low blood and lipid solubility, and thus fast induction and low potency. Halothane has high lipid and blood solubility, and thus high potency and slow induction. |
