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134 Cards in this Set
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half life as a function of Vd and Cl
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halflife = (Vd*ln2/Cl
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what drug is used for long term anticoag to prevent DVT?
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WARFARIN -- inhibits vit K-dependent carboxylation of glutamic acid residues on factors 2,7,9,10
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give an example of a direct thrombin inhibitor
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lepirudin
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role of alpha and beta adrenergic receptos in insulin control
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alpha receptors --> INHIBIT insulin release; beta --> STIMULATE insulin secretion
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TMP vs MTX vs pyrimethamine
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all --| DHFR ==> inhibit folic acid synthysis; TMP used for microbials, MTX for cancer, and pyrimethamine for malaria / toxo (parasites)
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tx of hyperpyrexia (temp > 40'C)
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emergently: facilitate heat loss (cooling blankets, saline bags, cold water enemas); also give oral antipyretics (NSAIDs to adults, acetaminophen to kids) --| PGE2
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chance of causing EPS among atypical antipsychotics
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RISPERIDONE: greatest risk; CLOZAPINE: least risk (but a/w agranulocytosis --> last resort)
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chronlogic evolution of EPS w/ neuroleptics
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4h: dystonia; 4d: akinesia; 4d: akathisia; 4m: tardive dyskinesia
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side effect profile of high potency vs low potency antipsychotics
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high potency (eg HALOPERIDOL, FLUPHENAZINE) cause more EPS, fewer anticholinergic/antihistamine; low potency (eg CHLORPROMAXINE) are opposite: fewer EPS, more anticholinergic/antihistamine
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effectiveness of typical vs atypical neuroleptics
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typical good only for positive sx (hallucinations, delusions, disorganized speech/behavior): Atypical also good for negative sx (dec emotional range, poverty of sleepch, loss of interest in living)
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systemic side effects of general anesthesia
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shuts tihings down (myocardial depression --> hypotension; respiratory depression --> hypercapnia; dec mucociliary clearance --> postop atelectasis; dec cerebral vascular resistance -> inc cerebral blo blood flow --> inc ICP; kidney: dec GFR and RPF; liver: dec hepatic blood flow
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chlorpromazine s/e
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anti-muscarinic (dry mouth, VISION [probs w/ accomodation]), anti-alph1 (orthostatic hypotension), anti-histaminic (sedation)
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muscarinic receptors on endothelial cells
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M3 -- normally not innervated, but can be stimed by cholinergic agonsits; cause relase of NO (EDRF) --> vasodilation
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what is No mechanism of endothelial relaxtiaion?
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NO --> guanylate cyclase --> inc cGMP -- Ca pump --> Ca efflux --> dec MLCK --> myosin dephosphorylation
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how is acetaminophen metablolized in the liver?
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sulfation and glucorn
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how is acetaminophen metabolized?
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1) sulfation/glucornide conjugationo in liver; 2) p450 in liver; 3) urinary excretion (un-metabolized)
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what anti-arrhythmic is associated with "chest burning"
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adenosine (also flushing)
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dobutamine
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selective B1 agonist; increass heart rate, contractility, conduction, and myocardial oxygen consumption
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what routine workup with carbemazepine?
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LFTs
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examples of zero-order drugs
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EtOH, phenytoin, aspirin (at high conc)
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what reactions constitute Phase II metabolism?
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acetylation, sulfation, glucoronidation
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phase 1 to phase 4 clinical trials
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1: pharmacokinetics, safety; 2: efficacy; 3: double blind studies; 4: postmarketing surveillance
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methscopolamine, oxybutin, glycopyrrolate
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same mech as SCOPOLAMINE (central antimuscarinic used for motion sickness), but diff USE (tx urinary urgency in mild cystitis, reduces bladder spasms)
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how to tx bladder urgency in cystitis?
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ATROPINE, METHSCOPOLAMINE, oxybutin, glycopyrrolate
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effects of D1 receptor, application
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D1: relaxes renal vasculature; ==> Dopamine (D>B>a) can be used to protect kidneys in shock (increases renal perfusion)
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name two alpha blockers and the difference between them
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phenoxybenzamine (irreversible), phentoalmine (reversible)
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alpha2 blocker, use, tox
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mirtazapine; USE: depression; TOX: sedation(??), inc serum cholesterol, inc appetite
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beta-1 selective beta blockers
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BEAM: betaxolol, esmolol (short acting), atenolol, metoproplol
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beta blocker effect on AV node
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decreases conduction speed --> used for SVTs, tox can cause AV BLOCK
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which beta blockers are partial agonists
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pindolol. Labetalol -- useful in hypertension with bradycardia (prevents complete cardiac depression)
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what agents are used in glaucoma to reduce aqueous humor production and secretion?
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PRODUCTION: alpha agonists (BRIMONIDINE); SECRETION: beta-blockers (TIMOLOL, BETAXOLOL, CARTEOLOL), diuretics (ACETAZOLAMIDE)
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what agents are used to increase aqueous humor outflow in glaucoma?
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alpha-agonists (EPINEPHRINE), cholinomimetics (CARBECHOL, PILOCARPINE, ECHOTHIOPHATE, PHYSOSTIGMINE), and prostaglandins (LATANOPROST)
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acidify urine to clear what drugs?
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weak bases (eg amphetamines)
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which antiepileptics cause stevens johnson?
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ethosuccimide and lamotrigine
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p450 inducers
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"Queen Barb uses Phenphen and Refuses Greasy Carbs:" QUINIDINE, BARBITURATES, PHENYTOIN, RIFAMPIN, GRISEOFULVIN, CARBEMAZEPINE, + ST.JOHN'S WORT
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p450 inhibitors
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"Inhibitors Stop Crazy Kids from Eating Grapefruit Rinds:" INH, Sulfonamides, Cimetidine, Ketoconazole, Erythromycin, Grapefruit Juice, Ritonavir
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what herbal agent can cause serotonin syndrome SSRIs?
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st. john's wort
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venous anticoag in pregnancy
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heparin/couamdin (doesn’t cross placenta -- warfarin does)
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LMWH
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enoxaparin
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abciximab
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mAb against GP IIb/IIIa --> used for acute coronary syndromes or angioplasty
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ticlodipine: mech, use, tox
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MECH: inhibits plt aggregation (blocks ADP receptors irreversibly); USE: acute coronary syndrome, stents, thrombotic stroke; TOX: NEUTROPENIA (not a s/e of clopidegrel, which has same mech)
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which chemotherapeutics cause DNA strand breaks? What phase of the cell cycle do they work in?
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ETOPOSIDE, BLEOMYCIN (also causes DNA intercalation, anytime); both in G2;
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DNA intercalating agents and cell cycle specificity
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Dactinomycin, doxorubicin, bleomycin; only bleomycin is cell-cycle specific (G2) because it also causes DNA strand breaks
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synergy w/ MTX
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5-FU: both block dTMP synthesis; MTX can be rescued by folinic acid (LEUKOVORIN); 5-FU cannot
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MTX tox
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HEPATITIS, pulm fibrosis, bone marrow suppression, stomatitis
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what chemotherapeutic is contraindicated with allopurinol?
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6-Mercaptopurine (6-MP), an antimetabolite; acts just like a purine -- activated by HGPRTase, inactivated by xanthine oxidase; ALLOPURINOL --| metabolism --> tox (GI, Liver)
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what's tox of c-ara
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used to tx AML (c-ARAMEL) ==> "must stop RBC synth" ==> MEGALOBLASTIC ANEMIA
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whats tox of cyclophosphamide, how can it be prevented?
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tox = hemorrhagic cystitis; prevent by coadministering MESNA
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tx for non-hodgkin's lymphoma
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CHOP (cyclophosphamide, doxorubicin, vincristine, prednisone)
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which DNA alkylators can cross BBB; what does that suggest about their use/tox
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NITROSOUREAS (eg. -mustine + streptozocin); USE: brain tumors, eg GLIOBLASTOMA MULTIFORME; TOX: CNS (ataxia, dizziness); ["NITROgen goes straight to your BRAIN"]
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tx for hodgkin's lymphoma
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ABVD: adriomycin (doxorubicin), bleomycin, vinblastine, dacarbazine (alkylator)
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which CTX require bioactivation?
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cyclophosphamide and nitrosoureas (both ALKYLATORS)
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CTX with cardiotox
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doxorubicin, daunorubicin, traztuzumab
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pacliaxel mech and use
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hyperstabalizes microtubles -- can't break down -- anaphase can't occur; use: breast and ovarian carcinomas
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what drug contraindicated with loop diruetics?
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NSAIDs -- in diuresis, probably have elevated ACE --> efferent vasoconstriction; if you give NSAID --| PG ==> afferent vasoconstriction --> renal failure; use ACETAMINOPHEN instead if you need anti-pyretic
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use of primaquine
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LATENT hypnozoite (liver) forms of malaria (Vivax and Ovale); for active, use quinine, mefloquine, chloroquine, etc.
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what ABx are cephalosporins contraindicated with?
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aminoglycosides (increase nephrotox); no AMP-GENT sweetness here
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trazodone tox
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priapism
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use of cromylyn
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only for PROPHYLAXIS of asthma (not useful in acute setting)
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s/e of long-term salmeterol use
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beta-agonist, so get "hyperactivity" s/e: tremor, arrhythmias
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theophylline use
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PDE inhibitor ==> prevents breakdown of cAMP ==> bronchodilation (asthma); use limited by NARROW TI: cardiotox (arrhythmias) and neurotox (seizures) ["hyperactivity" tox, just like salmeterol]
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1st line tx for asthma
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corticosteroids, esp BECLOMETHASONE and PREDNISONE
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effect of PGI on platelets and SMC
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INHIBITS aggregation, vasodilates, bronchodilates (opposite of TxA2)
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ACEi tox
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CAPTOPRIL (Cough, Angioedema, Proteinuria, Taste Changes from electrolyte shifts, hypOtension, Pregnancy problems, Rash, Increased Renin, Lower ATII)
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None
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antiandrogen used in PCOS, why?
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ketoconazole / spironolactone -- impair steroid synth (spironolactone also inhibits androgen receptor); PCOS ==> excess androgens ==> HIRSUTISM
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sildenafil tox, complications
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can cause blue-green COLOR VISION changes; life-threatening HYPOTENSION if taken with NITRATES
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drugs a/w color vision changes
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DIGOXIN: yellow; SILDENAFIL: blue-green ("van gogh painted starry starry night with epilepsy--digoxin and a massive erection--sildenefil)
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BPH vs Prostate cancer tx
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BPH: finasteride (BPH caused by inc estrogen or DHT); PROSTATE CANCER: flutamide, leuprolide
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AZT tox
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non-b12/folate macrocytic anemia
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tx for malaria
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CHLOROQUINE -- kills ACITVE form; for vivax/ovale, need to also give PRIMAQUINE -- kills LATENT form (in liver)
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tx of schistosomiasis and clonorchiasis
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praziquantel (also can tx paragonimus [all TREMATODES/FLUKES])
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uses of cephalosporins (1-3 gen)
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1: surg prophylaxis; 2: sinusitis, anaerobes; 3: meningitis, gonorrhea
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uses of fluconazole
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cryptococcal meningitis in aids; CANDIDA (all kinds, use w/ nystatin)
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most common antibiotic used to prevent endocarditis in patients w/ valvular disease
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amoxicillin (all but MVP)
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which chlamydia drug can also tx gonorrhea?
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azythromycin
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drugs that discolor skin
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QUINACRINE (antimalarial): yellow; CHLORPROMAZINE/ARSENIC: blue-grey
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best tx for open-angle glaucoma
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beta-blocker (eg timolol); can also use pilocarpine (cholinomimetic)
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tx of malignant hypertension
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nitroprusside (arterio and veno dilator)
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thioridazine: class, tox
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typical antipsychotic; can cause arrhythmias and RETINITIS PIGMENTOSA
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what is ribavirin used for?
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RSV
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how to tx seizures of eclampsia?
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benzos; prevent w/ MgSO4
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what drugs used for peripheral neuropathy
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gabapentin, amitriptyline
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phenytoin tox
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EYES (nystagmus, diplopia); FOLATE/B12 (megaloblastic anemia, teratogenesis); GROWTH (gingival hyperplasia, hirsutism); SLE-like syndrome, P450 induction
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antiepileptics and folate deficiency
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both phenytoin and valproic acid cause folate deficiency --> neural tube defects
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liver tox with which anti-epileptics?
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carbamazepine, VALPROIC ACID
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TCA tox
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"Tri-Cs:" Coma, Convulsions, Cardiotox (arrhythmias); + resp depression + hyperpyrexia
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which TCA in elderly?
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nortryptiline -- least sedating (elderly susceptible to confusion and hallucinations)
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name the 5 heterocyclics and their special toxicities
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STIMULANT: Bupropion (seizures in bulemics), Venlafaxine; SEDATION: Mirtazapine (inc appetite --> inc weight), Maprotiline, Trazodone (priapism)
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name the 5 heterocyclics and their mechanisms
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BUPROPION (mech unk., also used for smoking cessation); VENLAFAXINE (SNRI: --| 5-HTT, NET), MIRTAZAPINE (--|a2, 5-HT2R, 5-HT3R), MAPROTILINE (--|NET), TRAZADONE (--| 5-HTT, 5-HT2R)
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what opiod causes hypertensive crisis with MAOis?
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meperidine
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glitizone tox
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weight gain, hepatotox, (CARDIOVASCULAR problems)
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which hypoglycemic to use in gestational DM?
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INSULIN -- others can harm fetus
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how to tx hyperthyroidism? 3 classes
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1) ANION INHIBITORS: perchlorate, pertechnetate; block I- uptake by thyroid gland; 2) IODIDE SALTS: inhibit synthesis and release of TH; 3) THIONAMIDES: ptu, methimazole; inhibit organification of iodine
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tx of Turner syndrome
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GH (somatotropin)
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how to control uterine hemorrhage?
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oxytocin
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which h2 blocker has s/e, and what are they?
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cimetidine, p-450 inhibitor, antiandrogen effects, dec creatinine excretion
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drug used n/v following chemotx; + mech
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ondansetron (5-HT3 antagonist)
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pirenzapine, propantheline
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muscarinic antagonists used for peptic ulcers (--| M1 on ECL cells ==> dec histamine; --| M3 on parietal cells ==> dec gastrin)
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opiods used as anti-diarrheals
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lopiramide, diphenoxylate
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mech and use of etanercept
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soluble tnf-a receptor; used in RA + seronegative arthritides (HLA-B27): psoriasis, ankylosing spondylitis
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infliximab: mech, use, and drugs used with
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monoclonal Ab against tnf-a; used in IBD, RA, ankylosing spondylitis; often used w/ MTX
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what are the s/e of cyclosporine and how can they be prevented?
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immunosuppression --> viral infections, lymphoma; nephrotoxicity (PREVENTABLE w/ MANNITOL diuresis)
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aldesleukin
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recombinant IL-2, used for RCC and metastatic melanoma
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uses of alpha-interferon
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HBV, HCV, Kaposi's sarcoma, leukemias, malignant melanoma
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use of gamma-interferon
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chronic granulomatous disease
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what are uses and risks of mannitol diuresis?
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used for shock (pulls fluid out of third space), drug OD, and to decrease intracranial pressure; can also be used to prevent cyclosporine nephrotox; should NOT be used in CHF (can cause pulmonary edema)
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which diuretics are sulfa derivatives?
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acetazolamide, HCTZ, furosemide;
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what loop diuretic is not a sulfa derivative?
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ethacrynic acid (otherwise almost identical to furosemide)
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when to use thiazides vs ACEi?
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thiazides normally used for essential HTN, unless CHF/DM present -- in that case, use ACEi (mortality benefit + nephroprotective)
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use, s/e of methyldopa
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alpha2 agonist, used for HTN in renal failure; interesting s/e -- causes positive coombs test
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reserpine sfx
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opposite of cocaine (sedation, depression)
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what cardiac drugs can cause headache?
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vasodilators (esp nitroglycerin)
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beta blockers vs nitrates
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beta-blockers decrease AFTERLOAD; nitrates decrease PRELOAD; both decrease BP
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what precipitates digoxin tox?
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1) hypokalemia; 2) renal failure; 3) quinidine
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amiodarone tox
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Check PFTs, LFTs, and TFTs (lung, liver, thyroid)
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class III antiarrhythmics and TDP
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sotalol (also a class II agent) carries TDP risk, amiodarone does not
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drug of choice for tx of anaphylactic shock
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epinephrine (stims a1 --> inc BP; stims B1 --> inc contractility; stims B2 --> bronchodilation)
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why are elderly pts at increased risk of atropine tox?
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inc half life due to reduced clearance
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rare s/e of hyperthyroid tx
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PTU and methimazole can (rarely) cause agranulocytosis / aplastic anemia (Abs against neutrophils)
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alpha1 selective vs nonselective alpha blockers
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alpha1 selective blockers cause less reflex tachycardia (alpha2 blockers increase NE)
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what drugs cause lipid redistribution from extremities to trunk (lipodystrophy)
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protease inhibitors and glucocorticoids -- buffalo hump
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why is tolcapone useful in parkinson's?
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used as an adjunct to L-dopa / carbidopa; prevents PERIPHERAL L-dopa degradation
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sfx of tolcapone
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severe hepatitis (must monitor LFTs); ("capone = organized crime = prohibition LIQUOR --> hepatotox")
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amantadine use in parkinson's
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main role is anti-influenza (prevents uncoating); in PD, enhances endogeneous DA (inc synth, release, and reuptake)
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tolcapone vs selegeline in PD
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tolcapone inhibits PERIPHERAL degradation of L-dopa; selegeline prevents CENTRAL degradation of DA
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which benzo to give to help with sleep disturbance in elderly?
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SHORT ACTING (wears off by morning, prevents daytime drowsiness --> fall risk); short acting benzos: TOM (triazolam, oxazepam, midazolam)
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PABA sunscreens protect against which kind of UV light?
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UVB
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what drug to give in pt with angina with aspirin allergy?
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clopidogrel
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rifampin used as prophylaxis for what bugs?
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meningococcus, HIB
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definition of premature menopause
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menopause < 35yo
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usu age of onset of PCOS
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teens
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NO mechanism
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NO --> guanylate cyclase --> inc cGMP -- Ca pump --> Ca efflux --> decreased activity of myosin light chain kinase --> myosin dephosphorylation
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what class of drugs is sertraline?
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SSRI
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name 4 SSRIs
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Fluoxetine, Sertraline, Paroxetine, Citalopram
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