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241 Cards in this Set
- Front
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time it takes for amount of drug to fall to half its value; this is a constant in first order kinetics (majority of drugs)
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half life
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this step of metabolism makes a drug more hydrophilic and hence augments elimination
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phase 1
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inducers of cytochrome P450
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barbituates, phenytoin, carbamazapine, rifampin
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inhibitors of CYP 450
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cimetidine, ketoconazole, erythromycin, isoniazid, grapefruit
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strength of interaction between drug and its receptor
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affinity
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maximum response achievable from a drug
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efficacy
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a hormone whose mechanism of action utilizes intracellular receptors
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thyroid and steroid hormones
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a hormone whose MOA utilizes transmembrane receptors
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insulin
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antidote used for anticholinergic poisoning
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physostigmine
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antidote used for organophosphate / anticholinesterase poisoning
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atropine, pralidoxime
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antidote used for acetaminophen toxicity
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N acetyl cysteine
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antidote used for heparin overdose
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protamine
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antidote used for warfarin toxicity
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vitamin K and fresh frozen plasma
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antidote for tissue plasminogen activator, streptokinase
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aminocaproic acid
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antidote used for opioid toxicity
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naloxone (IV), naltrexone (PO)
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antidote used for benzo toxicity
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flumazenil
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interaction with this drug requires dose reduction of 6-MP
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allopurinol
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may protect against doxorubicin toxicity by scavenging free radicals
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dexrazoxane
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blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
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bleomycin
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regimen used for non-hodgkin's lymphoma
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CHOP (cyclophosphamide, doxorubicin,
vincristine, and prednisone) plus rituximab |
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interact with microtubules (but unlike vinca which prevent disassembly of tubules) it stabilizes tubulin and cells remain frozen in metaphase
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paclitaxel
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used for hairy cell luekemia; it stimulates NK cells
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interferon alpha
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anti estrogen ued for estrogen receptor and breast cancer
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tamoxifen
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anti emetics used in association with anti cancer drugs that are 5-HT3 (serotonin receptor subtype) antagonists
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ondansetron, granisetron
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ACTH analog used for diagnosis of patients with corticosteroid abnormality
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cosyntropin
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synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
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desmopressin (DDVAP)
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most widely used thyroid drugs such as synthroid and levoxyl contain
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L thyroxine [T4]
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PTU (propylthiouracil) MOA
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inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
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dose may need to be increased during pregnancy or with OCs due to increased TBG in plasma
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thyroxine
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some side effects of corticosteroids
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osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria thinning of skin
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inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
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aminoglutethimide
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antifungal agent used for inhibition of all gonadal and adrenal steroids
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ketoconazole
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diuretic used to antagonize aldosterone receptors
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spironolactone
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common SE of spironolactone
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gynecomastia and hyperkalemia
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selective estrogen receptor modulator [SERM] used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
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raloxifene
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non steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
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diethylstilbestrol [DES]
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converted low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
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combination oral contraceptives [OC]
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converted to more active form DHT by 5 alpha reductase
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testosterone
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anti-androgen used for hirsutism in females
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cyproterone acetate
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drug is used with testosterone for male fertility
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leuprolide
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very rapid acting insulin having fastest onset and shortest duration of action
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lispro, aspart, glulisine
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product of proinsulin cleavage used to assess insulin abuse
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C-peptide
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exogenous insulin contains
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little C peptide
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long acting insulin
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detemir
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ultra long acting insulin has over a day duration of action
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glargine
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examples of alpha glucosidase inhibitors [AGI]
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acarbose; miglitol
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amino acid derivative, active as an insulin secretagogue
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nateglinide
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most important potential SE of metformin
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lactic acidosis
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MOA of thiazolidinediones -- Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
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stimulate PPAR gamma receptor to regulate CHO and lipid metabolism
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increase bone density, also being tested for breast CA prophylaxis
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raloxifene [SERM selective estrogen receptor modulator]
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used intranasally and decreases bone resorption
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calcitonin (salmon prep)
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drug that causes contraction of the uterus
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oxytocin
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distribution of histamine receptors H1, H2, H3
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smooth muscles; stomach, heart, and mast cells; nerve endings & CNS respectively
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prototype antagonist of H1 and H2 receptors
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diphenhydramine & cimetidine
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first generation antihistamine that is highly sedating
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diphenhydramine
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second generation antihistamines
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fexofenadine, loratadine, cetirizine
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H1 antagonist used in motion sickness
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dimenhydrinate, meclizine, and other 1st generation
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H2 blocker that causes the most interactions with other drugs
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cimetidine
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HT-1d agonist used for migraine headaches
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sumatriptan, naratriptan, rizatriptan
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H1 blocker that is also a serotonin antagonist
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cyproheptadine
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agents for reduction of postpartum bleeding
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oxytocin, ergonovine, ergotamine
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agents used in treatment of carcinoid tumor
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ketanserin, cyproheptadine, phenoxybenzamine
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5HT 3 antagonist used in chemotherapeutic induced emesis
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ondansetron, granisetron, dolasetron, alosetron
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DOC to treat chemo induced nausea and vomiting
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ondansetron
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ergot alkaloid used as an illicit drug
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LSD
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dopamine agonist used in hyperprolactinemia
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bromocriptine
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mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
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bradykinin
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drug causing depletion of substance P (vasodilator)
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capsaicin
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prostaglandins that cause abortions
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PGE1 (misoprostol), PGE2, PGF2-alpha
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drug that selectively inhibits COX2
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celecoxib and rofecoxib
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inhibitor of lipoxygenase
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zileuton
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used in pediatrics to maintain patency of ductus arteriosis
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PGE1
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prostaglandin used in the treatment of impotence
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alprostadil (PGE1)
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MOA and effect of nitric oxide
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stimualtes cGMP which leads to vascular smooth muscle relaxation
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long acting beta 2 agonist used in asthma
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salmeterol
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muscarinic antagonist used in asthma
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ipratropium
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MOA of cromolyn
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mast cell stabilizer
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methylxanthine derivative used as a remedy for intermittent claudication
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pentoxifylline
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SE of long term (>5 days ) corticosteroid therapy and remedy
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adrenal suppression; wean slowly
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MOA of quinolones
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inhibit DNA gyrase
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drug used for MRSA
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vancomycin
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vancomycin MOA
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blocks cell wall (peptidoglycan) synthesis by
sequestration |
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meningitis prophylaxis in exposed patients
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ciprofloxacin or rifampin (for children
less than 4 yrs old) |
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technique used to diagnose perianal itching and the drug used to treat it
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scotch tape technique, mebendazole
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MOA of sulfonamides
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inhibit dihydropteroate synthase
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cheap wide spectrum antibiotic DOC for otitis media
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amoxacillin
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drug that causes gray baby syndrome and aplastic anemia
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chloramphenicol
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DOC for tx of pseudomembranous colitis
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metronidazole
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anemia caused by trimethoprim
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megaloblastic anemia
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DOC for giardia, bacterial vaginosis, and trichomonas
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metronidazole
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treatment for TB patients
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RIPE - rifampin, isoniazid, pyrazinamide, and ethambutol
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common side effect of rifampin
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red urine discoloration
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topical DOC in impetigo
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topical mupirocin (Bactroban)
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DOC for influenza A
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oseltamivir
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DOC for RSV
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ribavirin
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HIV antiviral class known to have severe drug interactions by causing inhibition of metbaolism
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protease inhibitors
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antivirals that are teratogens
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delavirdine, efavirenz, ribavirin
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HIV med used to reduce transmission during birth; HIV med used to prevent perinatal transmission
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AZT (zidovudine); nevirapine
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drug used in chagas disease
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nifurtimox
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drug used for N gonorrhea in females
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ceftriaxone
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DOC for herpes and its MOA
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acyclovir; phosphorylation, incorporation
into viral DNA, and chain termination |
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anti microbials that cause hemolysis in G6PD deficient patients
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sulfonamides
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MOA of erythromycin
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inhibition of protein synthesis at the 50s subunit of ribosome
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antibiotic frequently used for chronic UTI prophylaxis
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sulfamethoxazole / trimethoprim
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benzodiazepine used for anxiety
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alprazolam (i.e. xanax)
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non benzo used as an anxiolytic
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buspirone
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non benzo used for sleep
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zolpidem
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major effect of benzo on sleep at high doses
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rem decreased
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reason benzos are used cautiously in pregnancy
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ability to cross the placenta
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antidote to benzo overdose (antagonist that reverses the CNS effects)
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flumazenil
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benzo that has efficacy against absence seizures and in anxiety states, such as agoraphobia
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clonazepam
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DOC for status epilepticus
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diazepam
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agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol oxidizing system (MEOS)
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ethanol
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system that icnreases in activity with chronic ethanol exposure and may contribute to tolerance
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MEOS
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the most common neurologic abnormality in chronic alcoholics
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peripheral neuropathy
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drugs of choice for generalized tonic clonic and partial seizures
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valproic acid and phenytoin
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DOC for absence seizures
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ethosuximide and valproic acid
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DOC for myoclonic seizures
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valproic acid
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Drugs of choice for status epilepticus
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IV diazepam for short term; phenytoin for prolonged therapy
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anti seiure drug used also for pain of neuropathic origin
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gabapentin
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SE of phenytoin
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gingival hyperplasia, nystagmus, diplopia, ataxia
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DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
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dantrolene
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benzo receptor antagonist; accelerates recovery from benzo overdose
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flumazenil
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opioid associted with respiratory depression, but is used in high risk patients who may not survive full general anesthesia
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fentanyl
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GABA agonist in the spinal cord
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baclofen
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DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
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dantrolene
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irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP
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drug induced parkinsonism
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MOA of neuroleptics/antipsychotics
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dopamine blockade
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SE occuring in antipsychotics that block dopamine
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hyperprolactinemia, galactorrhea, menorrhea, mood changes, decreased sexual interest, weight gain, confusion
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antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
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risperidone
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atypical antipsychotic causing high prolactin levels
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risperidone
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newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, adversely affect diabetes
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olanzapine
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drug used in neuroleptic malignant syndrome
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dantrolene
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antipsychotic having the strongest autonomic effects
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thioridazine
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agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
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clozapine
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anti-psychotic not shown to cause tardive dyskinesia
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clozapine
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major route of elimination of lithium
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kidneys
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patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
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lithium toxicity
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DOC for bipolar affective disorder
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lithium
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SE of lithium
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tremor, sedation, ataxia, aphasia, thyroid enlargement, reversible diabetes insipidus
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usual time needed for full effect of antidepressant therapy
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2-3 weeks
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TCA used in chronic pain, enuresis, and ADD
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imipramine
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antidepressant associated with seizures and cardiotoxicity
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maprotiline
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heterocyclic antidepressant least likely to affect sexual performance used for management of nictoine withdrawal, SE include diziness, dry mouth , aggravation of psychosis, and seizures
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bupropion
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side effects frequently seen with SSRIs
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CNS stimulation, GI upset
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SSRI indicated for premenstrual dysphoric disorder
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fluoxetine (sarafem)
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activation of these receptors close Ca ion channels and inhibit neurotransmitter release
|
presynaptic mu, delta, and kappa
receptors |
|
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tolerance to all effects of opioid agonists can develop except
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miosis and constipation
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opioid used in the management of withdrawal states
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methadone
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opioid available trans dermally
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fentanyl
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opiod that can be given PO, by epidural, and IV which helps to relieve the dyspnea of pulmonary edema
|
morphine
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moderate opioid agonists
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codeine, hydrocodone, oxycodone
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opoid antagonist that is given IV and had short DOA
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naloxone
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opioid antagonist that is given orally in alcohol depndency programs
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naltrexone
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readily detected markers that may assist in diagnosis of the cause of a drug overdose include
|
changes in heart rate, BP, respiration, body temperature, sweating, bowel signs, pupillary responses
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leads to respiratory depression progressing to coma and death
|
overdose of opioids
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this agent may cause more severe rapid and intense symptoms to a recovering addict
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naloxone
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date rape drug
|
flunitrazepam (rohypnol)
|
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thsese agents are CNS depressants
|
ethanol, barbituates, and benzos
|
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treatments available for nicotine addiction
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patches, gum, nasal spray, psychotherapy, bupropion
|
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this agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
|
bethanechol
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|
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this agent used to treat dry mouth in Sjogrens syndrome
|
cevimeline
|
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|
treatment of atropine overdose and glaucoma (beause lipid soluble); enters CNS rapidly and has a stimulant effect, which may lead to convulsions
|
physostigmine
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treatment of myasthenia gravis
|
pyridostigmine
|
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toxicity of organophosphate
|
DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacriation, salivation, and sweating)
|
|
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treatment of choice for organophosphate overdose
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atropine & pralidoxime
|
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treat manifestations of parkinson's disease and EPS
|
benztropine; trihexyphenidyl
|
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treatment of motion sickness
|
scopolamine, meclizine
|
|
|
produce mydriasis and cycloplegia
|
atropine, hematropine, C1208 tropicamide
|
|
|
bronchodilation in asthma and COPD
|
ipratropium
|
|
|
used to treat patients exposed to insecticides such as parathion
|
pralidoxime, atropine
|
|
|
mnemonic for beta receptors
|
you have 1 heart (Beta 1) and 2 lungs
(Beta 2) |
|
|
this is the drug of choice for anaphylactic shock
|
epinephrine
|
|
|
longer acting beta 2 agonist is recommended for prophylaxis of asthma
|
salmeterol
|
|
|
these agents decrease blood flow or increase blood pressure, are local decongestants, and used in therapy of spinal shock (temporary maintanence of blood pressure which may help maintain perfusion)
|
alpha 1 agonists
|
|
|
alpha 1 agonist toxicity
|
hypertension
|
|
|
selective alpha 1 blocker used for hypertension BPH, may cause first dose orthostatic hypotension
|
prazosin, terazosin, doxazosin
|
|
|
selective B1 receptor blockers that may be useful in treating patients even though they have asthma
|
acebutolol, atenolol, esmolol, metoprolol
|
|
|
this beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
|
timolol
|
|
|
these beta blockers decrease aqueous secretion
|
timolol (nonselective), betaxolol (selective)
|
|
|
inhibit angiotensin converting enzyme (ACE)
|
ACE inhibitors
|
|
|
captopril and enalapril (-OPRIL ending) are
|
ACE inhibitors
|
|
|
SE of ACE inhibitors
|
dry cough, hyperkalemia
|
|
|
ACE inhibitors are contraindicated in
|
pregnancy and with K+
|
|
|
losartan and valsartan block
|
angiotensin receptor
|
|
|
angiotensin receptor blockers do NOT cause
|
dry cough
|
|
|
CCB contraindicated in CHF
|
verapamil
|
|
|
SE of CCB
|
constipation, edema, headache
|
|
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agents that reduce heart rate, contractility, and O2 demand
|
beta blockers
|
|
|
cardioselevtive beta 1 blockers
|
atenolol, acebutolol, metoprolol
|
|
|
SE of beta blockers
|
bradycardia, Sexual dysfunction, decrease in HDL, and increased in TGs
|
|
|
alpha 1 selective blockers
|
prazosin, terazosin and doxazosin (-AZOSIN ending)
|
|
|
A1a selective blcoker with no effects on HTN used for BPH
|
tamsulosin (flomax)
|
|
|
SE of alpha blockers
|
orthostatic hypotension (especially with first dose) and reflex tachyardia
|
|
|
methyldopa is contraindicated in
|
geriatrics due to its CNS (depression) effects
|
|
|
SE of hydralazine
|
lupus like syndrome
|
|
|
diuretic used for mountain sickness and glaucoma
|
acetazolamide
|
|
|
SE of acetazolamide
|
acidosis, alkalization of the urine (which may ppt. Ca salts), hypokalemia, paresthesias, and encephalopathy in patients with hepatic impairment
|
|
|
site of action of loop diuretics
|
thick ascending limb
|
|
|
SE of loop diuretics
|
hyperuricemia, hypokelmia, and ototoxicity
|
|
|
loops lose and thiazide diuretics retain
|
calcium
|
|
|
site of action of thiazide diuretics
|
work at early distal convoluted tubule
|
|
|
class of drugs that may cause cross sensitivity with thiazide diuretics
|
sulfonamides
|
|
|
SE of thiazide diuretics
|
hyperureicemia, hypokalemia, hyperglycemia
|
|
|
potassium sparing diuretics inhibit
|
NA/K exchange
|
|
|
diuretic used to treat primary aldosteronism
|
spironolactone
|
|
|
SE of spironolactone
|
gynecomastia, impotence, hyperkalemia,
|
|
|
osmotic diuretic used to treat increased intracranial pressure
|
mannitol
|
|
|
ADH agonist used for pituitary dibaetes inspidus
|
desmopressin
|
|
|
MOA of class I A (procainamide), class Ib (lidocaine) and class Ic (flecainide) antiarrhythmics
|
sodium channel blockers
|
|
|
SE of procainamide
|
lupus like syndrome
|
|
|
limiting side effect of quinidine
|
prolongs QT interval
|
|
|
DOC for management of acute ventricular arrhythmias
|
amiodarone
|
|
|
side effect of sotalol
|
prolongs QT and PR interval
|
|
|
life threatening cardiac event that prolonged QT leads to
|
torsades de pointes
|
|
|
MOA of sildenafil
|
inhibits phosphodiesterase 5, enhancing effects of nitric oxide activated increases in cGMP
|
|
|
MOA of nitrates
|
relax vascular smooth muscle: at low doses dilate veins and at high doses dilate arterioles
|
|
|
vitamin K dependent anticoagulant
|
warfarin
|
|
|
heparin (PTT) increases activity of
|
antithrombin 3
|
|
|
antidote to reverse actions of heparin
|
protamine sulfate
|
|
|
SE of aspirin
|
GI bleeding
|
|
|
prevents thrombosis in patients with artificial heart valve
|
dipyridamole
|
|
|
MOA of thombolytics
|
degredation of fibrin clots and are administered IV
|
|
|
thrombolytics are used for
|
pulmonary embolism and DVT
|
|
|
agent for pernicious anemia
|
vitamin B12/cyanocobalamin
|
|
|
agent used for megablastic anemia (but does NOT reverse neurologic symptoms) and decreases neural tube defects during pregnancy
|
folic acid
|
|
|
agent used for anemias associated with renal failure
|
erythropoietin
|
|
|
MOA of drug or foods (grapefruit juice) that increase statin effect
|
inhibit cytochrome P450 3A4
|
|
|
monitoring paramter to obtain before initiations of statins
|
LFTs
|
|
|
decreases liver triglycerol synthesis
|
niacin
|
|
|
SE of niacin
|
cutaneous flush
|
|
|
fibrates (gemfibrozil) increase activity of
|
lipoprotein lipase
|
|
|
agent used for closure of patent ductus arteriosus
|
indeomethacin
|
|
|
acetaminphen only has
|
antipyretic and analgesic activity
|
|
|
antidote for acetaminphen toxicity
|
N acetylcystine
|
|
|
DMARDS are slow acting drugs for
|
rheumatic disease
|
|
|
NSAID used in gout
|
indomethacin
|
|
|
MOA of colchicine (used in acute gout)
|
selective inhibitor of microtubule assembly
|
|
|
rapid acting insulins that do not self aggregate
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lispro insulin, aspart insulins, glulisine insulin
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|
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peakless long acting insulin
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insulin glargine
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|
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allpurional treats chronic gout by decreasing uric acid production by inhibiting
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xanthine oxidase
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