2014-04-14 First Aid Pharm Cards - First Aid Pharm Cards Flashcards
Cimetidine
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.
Omeprazole
PPI
M: Irreversibly inhibit H+/K+ -ATPase in stomach parietal cells
C: Peptic ulcer, gastritis, esophageal reflux, Zollinger-Ellison
Omeproazle, lansoprazole
Sucrulfate
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
Misoprostol
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)
Muscarininc antagonists
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
Antacids
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
Infliximab
M:Anti-TNF antibody.
C: Crohn’s, rheumatoid arthritis.
T: Respiratory infection, fever, hypotension
Sulfasalazine
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
Ondansetron
M:5-HT3 antagonist. Powerful central acting anti-emetic
C: Control vomiting post-op and in chemo patients
T: Headache, constipation
“Zofran”
Cisapride
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
Metoclopramide
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.
Insulin
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)
Sulfonylureas
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
Metformin
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
Glitazones
Pioglitazone, Rosiglitazone
M: Incr target cell response to insulin
C: Monotherapy or combo-therapy in DM2
T: Weight gain, edema. Hepatotoxicity, CV toxicity.
alpha-glucosidase inhibitors
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
Orlistat
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.
Sibutramine
M: Sympathomimetic serotonin and NE reuptake inhibitor.
C: Short-term and long-term obesity management.
T: Hypertension, tachycardia.
Propylthiouracil
Inhibit organification and coupling of thyroid hormone synthesis. Dec. peripheral conversion of T4 to T3.
C: Hyperthyroidism
T: Skin rash, agranulocytosis (rare), aplastic anemia.
Methimazole
Inhibit organification and coupling of thyroid hormone synthesis.
C: Hyperthyroidism
T: Skin rash, agranulocytosis (rare), aplastic anemia.
GH
GH deficiency, Turner’s syndrome
Octreotide
Somatostatin analog.
Acromegaly, carcinoid, gastrinoma, glucagonoma
Oxytocin
Stimulates labor, uterine contractions, milk let-down; controls uterine hemorrhage
Desmopressin
ADH analog.
Pituitary (central, not nephrogenic) Diabetes insipidus.
Levothyroxine
M: Thyroxine replacement
C: Hypothyroidism, myxedema
T: Tachycardia, heat intolerance, tremors, arrhytmias
Triiodothryonine
Glucocorticoids
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.
Leukotrienes
LTB, LTC, LTD: increase bronchial tone
Zileuton inhibits lipoxygenase.
Zafirlukast inhibits leukotrienes directly.
Prostacyclin (PGI)
Decrease platelet aggregation
Decrease vascular tone
Decrease bronchial tone
Decrease uterine tone
Prostaglandins
PGE, PGF
Decrease vascular tone
Decrease bronchial tone
Increase Uterine Tone
Thromboxane (TXA)
Increase platelet aggregation
Increase vascular tone
Increase bronchial tone
NSAIDS
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.
Celecoxib
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.
Acetominophen
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.
Colchicine
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.
Probenecid
M: Inhibits reabsorption of uric acid in PCT
C: Chronic gout
T: Inhibits secretion of penicillin. Not used acutely. No salicylates.
Allopurinol
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.
Etanercept
M: Recombinant TNF receptor (decoy)
C: Rheumatoid arthritis, psoriasis, ankylosing spondylitis.
Methotrexate
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.
Heparin
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.
LMWH
Acts more on Xa, better bioavailability, 2-4x longer half life. Sub Q w/o lab monitoring. Not reversible.
Lepirudin/bivalirudin
Hirudin derivatives; directly inhibits thrombin. Alternative to heparin for anticoagulating pts with HIT
Warfarin
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.
Thrombolytics
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.
Aspirin
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.
Clopidogrel
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.
Abciximab
M: Monoclonal Ab to GPIIa/IIIb on activated platelets. Prevents aggregation.
C:Acute coronary symptoms. Angioplasty.
T: Bleeding, throbocytopenia.
5-fluorouracil
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.
6-mercaptopurine
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.
Cytarabine
M: Inhibits DNA polymerase
C: AML
T: Leukopenia, thrombocytopenia, megaloblatic anemia
Cyclophosphamide
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)
Nitrosoureas
M: Alkylate DNA. Require bioactivation. Cross BBB.
C: Brain tumors (like GBM)
T: CNS toxicity (dizziness/ataxia)
Carmustine, lomustine, streptozocin.
Cisplatin / Carboplatin
M: Like alkylating agent
C: Testicular, bladder, ovary, lung carcinoma
T: Nephrotixicity, acoustic nerve damage
Busulfan
M: Alkyates DNA
C: CML
T: Pulmonary fibrosis, hyperpigmentation
Doxorubicin (adriomycin)
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.
Dactinomycin
M: Intercalates in DNA
C: Wilm’s tumor, Ewings sarcoma, rhabdomyosarcoma
T: Myelosuppresion
Childhood tumors
Bleomycin
M: Induces free radical formation, breaks in DNA strands
C: Testicular cancer, lymphomas (aBvd)
T: Pulmonary fibrosis, skin changes, minimal myelosuppresion
Hydroxyurea
M: Inhibits Ribonucleotide Reductase - decr DNA synthesis
C: Melanoma, CML, sickle cell
T: Bone marrow suppression, GI upset
Etoposide
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
Prednisone (cancer)
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
Tamoxifen
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.
Trastuzumab (Herceptin)
M: Mab against HER2.
C: Metastatic breast cancer for overexpressing HER2 tumors
T: Cardiotoxicity
Imatinib
GLEEVEC
M: BCR-ABL tyrosine kinase inhibitor
C: CML, GI stromal tumors
T: Fluid retention
Vincristine
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
Paclitaxel
M: M-phase specific agents bind to tubulin, and prevent spindle break down
C: Ovarian, breast cancer
T: Myelosuppresion and hypersensitivity
Cyclosporine
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)
Tacrolimus
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
Azothiporine
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
Muromonab (OKT3)
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
Sirolimus
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
Mycophenolate Mofetil
Inhibits de novo guanine synthesis (conversion of IMP to GMP) and blocks lymphocyte production
Daclizumab
Mab with high affinity for IL-2 receptor on activated T-cells
Filgrastim / Sargramostim
G-CSF / GM-CSF
Bone marrow recovery
alpha / beta / gamma interferon
Hep B/C, Kaposi Sarcoma, Leukemia
MS
Chronic granulomatous disease
Mannitol
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
Acetazolamide
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
Furosemide
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
Ethacrynic acid
M: Non-sulfa drug acts like furosemide
C: Diuresis in pts with sulfa-allergy
T: Similar to furosemide
Hydrochlorothiazide
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.
Spironolactone / Amiloride
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)
Lisinopril
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
Finasteride / Flutamide
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
Leuprolide
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
Sildenafil
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
Mifepristone (RU-486)
M: Competitive inhibitor of progestins at progesterone receptor
C: Termination of pregnancy (with misoprostol)
T: Heavy bleeding, nausea, vomiting, anorexia, abdominal pain
HRT
Relief or prevention of menopausal symptoms and osteoporosis
Unopposed estrogen therapy incr risk of endometrial cancer, so add progesterone. Possible incr CV risk.
Clomiphene
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
SERMS (Tamoxifen, raloxifen)
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.
H-1 Blockers
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
Isoproterenol / Albuterol / Salmeterol
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
Theophylline
Methylxanthine
M: Inhibits phosphodiesterase, decr cAMP hydrolysis.
C: Asthma (not really)
T: Narrow therapeutic index. Cardiotoxicity, neurotoxicity. P-450 metabolizes.
Ipratropium
Muscarinic antagonist
Competitive block of muscarinic receptors, prevents bronchoconstriction. Also for COPD.
Cromoyln
Prevents release of mediators from mast cells. Only effective for prophylaxis of asthma, not acute attack. Toxicity is rare.
Zileuton / Zafirlukat, montelukast
Zileuton: 5-lipoxygenase inhibitor. Blocks conversion of AA to leukotrienes
Z/M: Block leukotriene receptor. Especially good for aspirin induced asthma
Bacteriostatic / Bacteriocidal
Static: Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol
Cidal: Vancomycin, Fluoroquinolones, Penicllin, Aminoglycosides, Cephalosporins, Metronidazole
Penicillin
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
Methicillin
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