| Term 
 | Definition 
 
        | PGE1 drug; used to treat congenital heart defects (inc pulmonary flow) and erectile dysfunction
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | PGE1 drug; tx gastric ulcers
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | PGE1 drug; tx gastric ulcers
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | PGI2 drug; stable;
 tx gastric ulcers;
 heparin substitute in renal disease
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | PGI2 drug; stable;
 tx gastric ulcers, pulmonary HTN;
 heparin substitute in renal disease;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 15-methyl-PGF2-alpha drug; induce labor and abortion
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | recombinant BNP; tx dyspnea due to CHF;
 diuresis, natriuresis, vasodilation, dec aldosterone
 SE- hypotension
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Endothelin-1 receptor antagonist; vasodilation;
 tx CHF, pulmonary HTN;
 SE teratogenic, hepatotoxicity, peripheral edema;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Carbonic Anhydrase inhibitor; HCO3-, Na lost in urine, alkaline;
 Cl reabsorbed;
 limited use as diuretic;
 tx cysteinuria, glaucoma, seizures;
 SE- metabolic acidosis, hypercholoremia, drowsiness, inc sensitivity to thiazides
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | inhibits Na-K-Cl symporter, inhibits NaCl reabsorption; inc renin;
 tx: edema, hypercalcemia, prophylaxis for renal failure, CHF, HTN;
 "loops lose Ca";
 SE- inc BUN, hypokalemia, alkalosis, ototoxicity, warfarin interactions
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | inhibits Na-K-Cl symporter, inhibits NaCl reabsorption; 40x more potent than furosemide and no Warfarin interaction
 inc renin;
 tx: edema, hypercalcemia, prophylaxis for renal failure, HTN;
 "loops lose Ca";
 SE- inc BUN, hypokalemia, alkalosis, ototoxicity, drug interactions
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | inhibits Na-K-Cl symporter, inhibits NaCl reabsorption; long half-life;
 inc renin;
 tx: edema, hypercalcemia, prophylaxis for renal failure, HTN;
 "loops lose Ca";
 SE- inc BUN, hypokalemia, alkalosis, ototoxicity, drug interactions
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Osmotic diuretic; tx prophylaxis of acute renal failure (LOW GFR-ready);
 SE- volume overload may lead to heart failure
 |  | 
        |  | 
        
        | Term 
 
        | Hydrochlorothiazide (Esidrex) |  | Definition 
 
        | class 1 thiazide diuretic (high GFR); inhibits Na/Cl symporter in aldo insensitive segment;
 see SE of thiazide related drugs;
 short acting;
 tx HTN, nephrogenic diabetes insipidus;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | class 2 thiazide diuretic (GFR 20-40); high potency;
 inhibits Na/Cl symporter in aldo insensitive segment;
 tx HTN even if renal insufficiency, CHF
 |  | 
        |  | 
        
        | Term 
 
        | Thiazide SE Depletion Phenomena (4)
 |  | Definition 
 
        | hypokalemia; dilutional hyponatremia;
 hypochloremic alkalsosis;
 hypomagnesemia
 |  | 
        |  | 
        
        | Term 
 
        | Thiazide SE Retention Phenomena (2)
 |  | Definition 
 
        | hyperuricemia; hypercalcemia
 |  | 
        |  | 
        
        | Term 
 
        | Thiazide SE Metabolic changes (3)
 |  | Definition 
 
        | hyperglycemia; hyperlipidemia;
 hypersecretion of renin and aldo
 |  | 
        |  | 
        
        | Term 
 
        | Thiazide SE Hypersensitivities (5)
 |  | Definition 
 
        | fever; rash;
 purpurea;
 pancreatitis;
 withdrawal edema
 |  | 
        |  | 
        
        | Term 
 
        | Spirinolactone (Aldactone) |  | Definition 
 
        | aldosterone antagonist, K-sparing diuretic; inhibit Na reabsorption in DCT;
 tx HTN alongside HCTZ (not used alone), CHF;
 SE- hyperkalemia, megaloblastic anemia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | K-sparing diuretic; inhibit Na reabsorption in DCT;
 tx HTN alongside HCTZ (not used alone);
 SE- hyperkalemia, megaloblastic anemia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | K-sparing diuretic; inhibit Na reabsorption in DCT;
 tx HTN alongside HCTZ (not used alone);
 SE- hyperkalemia, megaloblastic anemia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | alpha-2 agonist RVLM; tx dec sympathetic output;
 analgesic;
 SE sedation, drowsiness, fatigue, anxiety, water retention, xerostomia;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Acts centrally (post-synaptic a2) on RLVM to tx severe HTN (ex. preeclampsia); Also acts on presynaptic a2 receptors to reduce NE release;
 Tx - preeclampsia
 SE - sedation, sleep disturbance water retention, immunological dysfunction (Positive Coombs, "lupus-like")
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | inhibits DA and NE movement into synaptic vesicles; DEC EPI, NE, AND DA in periphery
 tx HTN;
 contraindicated for patients with peptic ulcers or hx of depression
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | alpha-1 antagonist; tx HTN;
 short acting;
 inc HDL, improves insulin resistance
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Beta-1 and 2 antagonist; direct effect on Na channels, anti-arrythmias;
 tx HTN, esp with CHF or prev MI;
 SE see BB SEs
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Beta-1 and 2 + alpha-1 antagonist; tx HTN, primary drug for CHF;
 dec ROS production
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | beta-1 and 2 antagonist; tx glaucoma, migraines;
 slight ISA
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | beta-1 antagonist; tx HTN, esp associated w/ CHF
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | beta-1 antagonist; tx HTN, esp associated w/ CHF
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | beta 1 antagonist; antiarrthymic;
 very short half-life;
 tx tachycardia, HTN
 |  | 
        |  | 
        
        | Term 
 
        | Beta-blocker side effects (7) |  | Definition 
 
        | Raynaud's bradycardia
 bronchospasm
 depression
 drug interaction with conduction blockers
 fatigue
 dec GFR
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | direct vasodilator; pro-drug, opens K/ATP channels in SM;
 dilates arterioles, not veins;
 SE reflex tachycardia, hirsutism (Rogaine)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Vasodilator and venodilator; Prodrug for NO;
 Dilates arteries and veins (inc cGMP);
 Tx HTN crisis, L sided heart failure;
 SE - hypotension, tachycardia, palpitations, cyanide production, nausea
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | ACE inhibitor; improves prognosis for CHF by dec afterload;
 short half-life;
 inc synthesis of prostaglandins to inc vasodilation (vascular and renal);
 SE - ortho hypotension, hyperK, dry cough!, angioedema (inc bradykinins), fetotoxity
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | ACE inhibitor; improves prognosis for CHF by dec afterload;
 prodrug, (de-esterification) converted into elanaprilat (activE);
 SE - ortho hypotension, hyperK, dry cough!, angioedema (inc bradykinins), fetotoxity
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | ARB; tx CHF, HTN;
 no cough, dec angioedema as compared to ACEI;
 prodrug, active met is non-comp inhibitor;
 unique inc uric acid secretion (think gout) and inhibits CYP450;
 SE - hypotension, hyperK, hepatic dysfunction, fetotoxicity
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | ARB; no cough, dec angioedema as compared to ACEI;
 SE - hypotension, hyperK, hepatic dysfunction, fetotoxicity
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | ARB; tx CHF, HTN;
 no cough, dec angioedema as compared to ACEI;
 prodrug;
 SE - hypotension, hyperK, fetotoxicity
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Renin inhibitor, nonpeptide; never used alone, usually with ARB
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | L-type Ca Channel Blocker; phenylalkylamine;
 tx HTN w/ angina and arrhythmias - dec contractility and AV conduction;
 SE - peripheral edema, reflex tachy, hypotension, constipation, depression of SA/AV nodes, myocardial depression, nausea, headache
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | L-type Calcium Channel Blocker; dihydropyridine;
 tx HTN, use with diuretic;
 selective for vascular SM, not cardiac;
 long acting;
 SE - peripheral edema, reflex tachy, hypotension, constipation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | L-type Calcium Channel Blocker; dihydropyridine;
 tx HTN, use with diuretic;
 selective for vascular SM, not cardiac;
 short acting;
 SE - peripheral edema, reflex tachy, hypotension, constipation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | L-type Calcium Channel Blocker; dihydropyridine;
 tx HTN, use with diuretic;
 selective for vascular SM, not cardiac;
 SE - peripheral edema, reflex tachy, hypotension, constipation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | L-type Calcium Channel Blocker; benzothiazepine, intermediate between phenyl. and DHPs;
 limited reflex tachycardia;
 SE - depression of SA/AV nodes, myocardial depression, peripheral edema, rashes, nausea, headache
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | L-type AND Na channel inhibitor; tx HTN;
 SE- arrhythmias, agranulocytosis
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | digitalis glycoside; inc intracellular Ca; mech - blocks Na/K-ATPase, inc intracellular Na, inc activity Na/Ca exchanger;
 inc Ca - inc contractility;
 tx severe CHF with low EF;
 decrease in AV conduction velocity (inc PR interval);
 SE interactions with diuretics, warfarin
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | direct arterial vasodilator; tx CHF;
 stimulates RAS as a SE - edema, inc volume;
 SE - nausea, anorexia, +FANA, exacerbate angina (reflex tachy), "lupus-like syndrome"
 |  | 
        |  | 
        
        | Term 
 
        | Nitroglycerine (Tridil, Ismo) |  | Definition 
 
        | venodilator; reduce preload in tx of CHF;
 reduces pulmonary art P, congestion; reduces LV filling P
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | veno- and vasodilator; reduce preload in tx of CHF;
 reduces pulmonary art P, congestion; reduces LV filling P
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Oral nitrate preparation; Slow onset, med duration (4-6 hrs)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Beta-agonist, mostly B1 (also B2, a1); Inotrope, vasodilator (prevented by Bblocker), vasoconstrictor (unopposed a1 effect);
 Tx CHF
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | tx gouty arthritis and prophylaxis, terminates acute attacks; tx Familial Mediterranean Fever;
 works by depolimerization of microtubules;
 SE GI disturbance, blood dyscrasias
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | COX inhibitor, analgesic and antipyretic; inhibits leukocyte motility;
 tx acute attack of gout;
 SE GI (nausea, vomit), CNS (HA), hematopoietic disorders, antagonize furosemide and HCTZ
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | competitive inhibitor of xanthine oxidase; met to oxypurinol, non-competitive inhibitor;
 dec plasma levels and urinary excretion of UA;
 inc precursors;
 dissolution of UA crystals, prevention of UA kidney stones;
 tx gout due to enzyme abnormalities or hematologic disorders;
 SE acute gout, hypersensitivity rxn, liver function, interaction with antibiotics
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | inhibits transport of organic anions across epithelia, blocks UA reabsorption; inc UA excretion;
 dissolution of UA crystals;
 SE salicylates inhibit uricosuric action of proben.
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | inc glucose oxidation, efficiency of O2 use in heart; tx chronic stable angina (combo with amlodapine, BB, or nitrates);
 indicated for pts refractory to revascularization, BBs, nitrates, amlodapine (4th, 5th-line tx);
 SE - dizzy, HA, constapation, nausea, syncope, asthenia;
 contraindiated with CYP3A4 inhibitors, long QT, class 1a and III AAs, or Digoxin (inhibits metabolism at P-GP)
 |  | 
        |  | 
        
        | Term 
 
        | Procaineamide (Procan-SR) |  | Definition 
 
        | Class 1A prototype- intermed. dissociation rate; Decreases membrane responsiveness by binding to Na channels, dec conduction velocity, inc effective refractory period;
 IV only;
 tx acute atrial and ventricular arrhythmias;
 SE - (+)FANA, drug induced lupus, GI intolerance, bone marrow aplasia, QT prolongation, Torsades
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Class 1C prototype - SLOW dissociation rate; prolong QRS;
 Decreases membrane responsiveness by binding to Na channels, dec conduction velocity;
 suppresses automaticity, inc effective refractory period in atria, vent, AVN;
 tx supraventricular arrhythmias, WPW, A fib, A flutter;
 SE - pro-arrhythmic effect;
 contraindicated in pts with structural heart disease (incl. necrotic infarcts) - inc mortality post-MI;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Class III - K channel blocker; also blocks Na (class 1), Ca, and B-adrenergics (some class 2);
 Interacts with TH (thyroid) receptors;
 prolongs AP, effective refractory period;
 inhibits abnormal automaticity;
 tx Vtach, Vfib, Afib, IV for cardiac rescuscitation, PO for chronic atrial, vent, AVN arrhythmias;
 SE - pulmonary fibrosis, hypo- hyper-thyroid, blindness, hepatitis, (Torsades rare!);
 inhibits CYP3A4
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Class III - K channel blocker (prolongs AP); non-selective beta-blocker (1/3 the potency);
 tx atrial, vent, AVN reentry, Vtach;
 contraindications - long QT, renal insuff, COPD, CHF, AV block, bradycardia;
 SE - Torsades
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Class III prototype - K channel blocker; Prolong repolarization therefore inc effective refractory period;
 interrupts reentry, inc fibrillation threshold (dec fib's);
 tx IV for acute atrial arrhythmias (Afib, Aflutter) (Diff from Nagle notes);
 SE - Torsades
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | tx acute PSVT, blocks AV node; short half-life, IV admin;
 SE - tight chest, flushing, recurrence of PSVT;
 Contraindications - methylxanthines (think Dr. Nelson), Dypyridamole (potentiation), WPW
 |  | 
        |  | 
        
        | Term 
 
        | Acetylsalicylic acid (Aspirin) |  | Definition 
 
        | acetylation of COX (1&2) enzymes, irreversible inhibition; inhibits platelet aggregation;
 tx inflammation, fever, pain, HA, arthritis, dysmenorrhea, RA (large dose);
 SE - GI ulcer, tinnitus, hearing loss, hepatic injufy, Reyes', asthma, inc bleeding time;
 CI with bleeding disorders
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhibitor of COX-1,2,(3); analgesic and antipyretic;
 NOT useful for anti-inflammatory;
 SE - HEPATOTOXICITY;
 No effects on platelets, NO GI IRRITATION
 |  | 
        |  | 
        
        | Term 
 
        | Ibuprofen (Advil, Motrin) |  | Definition 
 
        | NSAID - reversible COX inhibitor; Alter platelet (prolonged bleeding), anti-inflamm, antipyretic, analgesic;
 tx RA (3200mg), pain (400mg/6hrs);
 SE- GI irritation (less than others);
 CI in pregnancies
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | NSAID - reversible COX inhibitor; Alter platelet (prolonged bleeding), anti-inflamm, antipyretic, analgesic;
 Long half-life - 14hrs, so 2xday dosing;
 SE- GI irritation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | NSAID - heteroaryl acetic acid deriv; POTENT analgesic, moderate anti-inflamm;
 IM, oral, parenteral admin;
 SHORT-TERM USE ONLY;
 tx post-op pain and inflamm, topical for eye inflamm (alergies or post-op);
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | NSAID - heteroaryl acetic acid deriv; potent COX inhibition;
 tx RA, OA;
 SE - GI, elevation of hepatic aminotransferase activities;
 CI for pregnancy
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | NSAID - selective COX2; anti-inflamm, antipyretic, analgesic;
 tx OA, RA, acute pain, dysmenorrhea;
 SE - CV, some GI uleration, dyspepsia, inhibits labor, renal alteration, hypersensitivity rxns;
 Drug interaction- "heart meds", diuretics, coumadin
 |  | 
        |  | 
        
        | Term 
 
        | Methotrexate (*Rheumatrex*) |  | Definition 
 
        | DMARD - inhibits DHFR to inhibit purine biosynth; tx RA!, leukemias, psoriasis, immunosuppressor (dec Igs, TNF, IL-1,6);
 SE - hepatotoxicity, infections, teratogenic;
 CI - poor renal fxn, NSAIDs dec clearance, pregnancy (Cat X!)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | DMARD - inhibits pyrimidine synth; tx mild RA;
 SE - skin rash, hepatic toxicity (BLACK BOX!), long-term teratogen (1-2 yrs to clear, use cholestyramidine to conjugate), myelosuppression (bone marrow);
 |  | 
        |  | 
        
        | Term 
 
        | Sulfasalazine (Azulfidine) |  | Definition 
 
        | DMARD - prodrug; met. to sulfapyridine (SE's) and 5ASA (therapeutic);
 tx RA, UC, Crohn's;
 SE - GI, DEC. WBCs, anemia, rash, impotence
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | DMARD - TNF inhibitor; Reduce circulating TNF-a and block action at receptor;
 mech - fusion of 75 TNF receptor to human IgG;
 produced in CHO cells (hamster);
 admin SC injection 2x a week (3-4 day half life);
 tx RA who don't respond to other DMARDs, psoriatic arth, AS, plaque psorisis, IBD;
 SE - injection site rxn, infection, auto-Ab
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | DMARD - TNF inhibitor; Reduce circulating TNF-a and block action at receptor;
 chimeric IgG1 monoclonal Ab, induces lysis of activated TNF-alpha expressing cells;
 IV admin 0 and 2 weeks, every other month;
 tx RA, Crohn's, psoriatic arth, AS, UC, plaque psoriasis;
 SE - injection site rxn, infection, auto-Ab
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | DMARD; T-cell costim blocker;
 CTLA4 conjugated w/ IgG, binds CD28 on Tcell, blocks response and cytokines (TNF);
 admin IV first 0,2,4 weeks then once a month;
 Use after failed TNF-inhibitor therapy;
 SE - inc infections (immunocompromised)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | DMARD; depletion of B cells;
 monoclonal Ab against CD20 on Bcells, dec cytokine production;
 tx RA who failed to respond to other TNF antagonists
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR Agonist; active but conv to M-6-glucaronide (100x potency);
 tx mod/severe pain;
 4 hr half life - accumulation;
 extensive (70%) first pass metabolism;
 Use in pts taking MAO-Is;
 SE - tolerance, constipation, renal clearance
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR agonist (morphine-like); oral and parenteral admin;
 tx mod/SEVERE pain
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR agonist (morphine-like); long acting;
 tx mod/severe pain;
 high abuse potential
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR agonist (morphine-like); tx mod/severe pain;
 50% inactivated, first pass;
 less spasmogenic, no miosis, less constipation;
 Toxic met. (normeperidine) can accumulate to produce seizure risk;
 CI - lethal w/ MAO-inhibitors, CHILDREN
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR agonist (morphine-like); po admin;
 tx abuse withdrawl/cravings, dampen peaks/troughs of drug conc during weaning
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR agonist (morphine-like); tx mod/severe pain;
 80x potency;
 transdermal patch for chronic;
 rapid onset, short duration - anesthesia IV;
 Use in pts taking MAO-Is;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | MOR agonist (morphine-like); Low affinity, 10% conv to morphine;
 oral or parenteral admin;
 renal clearance, resistance in 10% caucasians;
 tx mild pain, cough suppressant (@brainstem)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Opiate for MODERATE pain; |  | 
        |  | 
        
        | Term 
 
        | Buprenorphine (Buprenex)(Subutex) |  | Definition 
 
        | MOR partial agonist (low action), KOR antagonist; dec abuse potential;
 po admin;
 tx addiction/abuse;
 SE - abstinence syndrome (if morph-dependent)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | opioid mixed agonist/antagonist; bind and inactivates MOR;
 activates KOR;
 tx mod/severe pain, but analgesic effect is sl. dec;
 no constipation, no respiratory depression;
 SE - abstinence syndrome;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | opioid mixed agonist/antagonist; bind and inactivates MOR;
 activates KOR;
 tx mod/severe pain, but analgesic effect is sl. dec;
 no constipation, no respiratory depression;
 SE - abstinence syndrome;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | opioid receptor antagonist; LONG DURATION (24 hrs);
 po admin, extensive first pass;
 tx alcohol abuse (craving and relapse)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | opioid receptor antagonist; IV only: rapid onset, short duration (esp compared to morhphine), dose accordingly;
 EXTENSIVE P.O. FIRST PASS METABOLISM;
 tx opioid OD, reverses respiratory depression;
 can cause opioid withdrawal; start low, go slow
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | opiate derivative; dec GI motility, peristalsis and secretion = inc absorption;
 tx diarrhea;
 no CNS effects - doesn't cross BBB
 |  | 
        |  | 
        
        | Term 
 
        | Diphenhydramine (Benadryl) |  | Definition 
 
        | 1st Gen antihistamine - ether deriv; Sedative, anti-emetic, GI cramps, anticholinergic;
 tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
 SE - sedation, dystonia, nasal congestion;
 CI - asthma
 |  | 
        |  | 
        
        | Term 
 
        | Dimenhydrinate (Dramamine) |  | Definition 
 
        | 1st Gen antihistamine - ether deriv; Sedative, anti-emetic, GI cramps, anticholinergic;
 tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
 SE - sedation, dystonia, nasal congestion;
 CI - asthma
 |  | 
        |  | 
        
        | Term 
 
        | Brompheniramine (Dimentane) |  | Definition 
 
        | 1st Gen antihistamine - Alkylamine deriv; Sedative, anti-emetic, GI cramps, anticholinergic;
 tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
 SE - sedation, dystonia, nasal congestion;
 CI - asthma
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 1st Gen antihistamine - Piperazine deriv; Long lasting (4-24hrs);
 Sedative, anti-emetic, GI cramps, anticholinergic;
 tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
 SE - sedation, dystonia, nasal congestion;
 CI - asthma
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 2nd Gen antihistamine - piperidine deriv; Longer duration, non-sedating, no anticholinergic fxn, SAFE for asthmatics;
 tx allergy, hayfever, rhintis, urticaria, insect bites, contact flora;
 SE - mild congnitive disturance, some appetite stimulation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 2nd Gen antihistamine - piperazine deriv; appetite stimulation, some sedation;
 Longer duration, non-sedating, no anticholinergic fxn, SAFE for asthmatics;
 tx allergy, hayfever, rhintis, urticaria, insect bites, contact flora;
 SE - mild congnitive disturance, some appetite stimulation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 2nd/3rd Gen antihistamine; high specificity for H1, some muscarinic activity;
 LONG HALF LIFE (27hrs);
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 2nd/3rd Gen antihistamine; inhibits histamine, LTs, PAF activity;
 LONG HALF LIFE;
 tx rhinitis and hay fever;
 can use in asthmatics;
 SE - somnolence, taste, nasal burning, ST, dry mouth, TERATOGENIC
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Adrenergic Agonist - Bronchodilator; B1, [B2], a1, a2;
 Stim AC to inc cAMP - bronch dilation;
 tx asthma, COPD;
 inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
 SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Adrenergic Agonist - Bronchodilator; B1, [B2], (some a);
 Stim AC to inc cAMP - bronch dilation;
 tx asthma, COPD;
 inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
 SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Adrenergic Agonist - Bronchodilator; [B2] specific - FAST - reliever or rescue admin;
 Stim AC to inc cAMP - bronch dilation;
 tx asthma, COPD;
 inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
 SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Adrenergic Agonist - Bronchodilator; [B2] specific - FAST - reliever or rescue admin;
 Stim AC to inc cAMP - bronch dilation;
 tx asthma, COPD;
 inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
 SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Adrenergic Agonist - Bronchodilator; [B2]specific - SLOW - prevention (esp night-time, exercise use);
 Stim AC to inc cAMP - bronch dilation;
 tx asthma, COPD;
 inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
 SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Cholinergic antagonist - Bronchodilator; Competitive M blockade;
 dec airway SM constriction, dec mucous secretion;
 SE - pupillary dilation & cycloplegia (X ciliary m)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Cholinergic antagonist - Bronchodilator; Competitive M blockade;
 short acting and no systemic functions;
 dec airway SM constriction, dec mucous secretion;
 SE - pupillary dilation & cycloplegia (X ciliary m)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Methylxanthine - Bronchodilator; Inhibit PDE - inc cAMP - bronchodilation;
 Block adenosine recept - bronchodilation;
 Dec release of mediators - anti-inflamm;
 tx asthma/COPD;
 chronotropic, ionotropic, inc CNS act, gastric acid sec, inc SK muscle str (diaphragm);
 SE - (10-20ug/mL)- nausea, vomit, HA, nervous, insomnia, (>20ug/mL)- hypoK, hyperglycemia, tachycardia, arrhy, NM irritability, seizures
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-inflamm; Alt Cl- channel: mast cells (dec degran), eosinophils (dec inflamm), airway nn (inhibit cough), dec bronchial hyperactivity;
 tx asthma,COPD;
 SE - TASTE, irritation of trachea (cough/bronchospasm)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | a Cromolyn - Anti-inflamm; Alt Cl- channel: mast cells (dec degran), eosinophils (dec inflamm), airway nn (inhibit cough), dec bronchial hyperactivity;
 tx asthma,COPD;
 SE - TASTE, irritation of trachea (cough/bronchospasm)
 |  | 
        |  | 
        
        | Term 
 
        | Beclomethasone (Beclovent) |  | Definition 
 
        | Inhaled Glucocorticoid - Anti-inflamm; Dec production of inflamm cytokines;
 Inc prod of anti-inflamm proteins;
 Dec mucus secretion, dec bronch hyperactivity;
 tx asthma, COPD;
 SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhaled Glucocorticoid - Anti-inflamm; Dec production of inflamm cytokines;
 Inc prod of anti-inflamm proteins;
 Dec mucus secretion, dec bronch hyperactivity;
 tx asthma, COPD;
 SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhaled Glucocorticoid - Anti-inflamm; Dec production of inflamm cytokines;
 Inc prod of anti-inflamm proteins;
 Dec mucus secretion, dec bronch hyperactivity;
 tx asthma, COPD;
 SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Oral Glucocorticoid - Anti-inflamm; Dec production of inflamm proteins;
 Inc prod of anti-inflamm cytokines;
 Dec mucus secretion, dec bronch hyperactivity;
 tx asthma, COPD;
 SE - glu intolerance, inc BP and weight, dec bone density, dec growth rate (kids), cataracts, immunosuppression, CUSHINGOID SYNDROME
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Leukotriene receptor blocker - Anti-inflamm; Block LTD4 - dec bronch reactivity/constriction, dec mucosal secretion, dec airway inflamm;
 tx asthma (aspirin-induced);
 SE - GI, URI, nausea, otitis
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Leukotriene receptor blocker - Anti-inflamm; Block LTD4 - dec bronch reactivity/constriction, dec mucosal secretion, dec airway inflamm;
 tx asthma (aspirin-induced);
 SE - GI, HA, inc liver enzymes, CANCER RISK
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Leukitriene Synth inhibitor - Anti-inflamm; inhibits 5-lipoxygenase and LT formation (B,C,D,E -4);
 dec SM contraction, dec blood vessel perm (leukocyte migration);
 SE - inc hepatic enzymes (watch liver func tests), inhibits CYP1A2 (theophylline)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-IgE - Humanized antibody; Dec severity and freq of asthma attacks;
 tx severe allergic asthma (step 5/6 treatment, slide 32);
 SE - anaphylaxis, cold symptoms
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Polyclonal Ab; (use rabbit more) - immunosup; anti-thmocyte globulin;
 Nonspecific binding to T-cells, lose 80-90%;
 tx for bone marrow or organ transplant, aplastic anemia;
 Neutralizing Abs dev = tolerance;
 SE - fever, chills, hypoT, thrombocytopenia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Polyclonal Ab - immunosup; anti-thmocyte globulin;
 Nonspecific binding to T-cells, lose 80-90%;
 tx for bone marrow or organ transplant, aplastic anemia;
 Neutralizing Abs dev = tolerance;
 SE - fever, chills, hypoT, thrombocytopenia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | IV immunoglobulin - Immune boost; tx immunodeficiency;
 SE- renal failure
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Mouse anti-CD3 Ab - Immunosup; Tcells in peripheral blood, reversible;
 Neutralizing Abs can dev = TOLERANCE;
 SE - acute hypersensitivity, systemic cytokine-med symp;
 pretreat with high-dose steroids
 |  | 
        |  | 
        
        | Term 
 
        | Cyclosporine (Sandimmune) |  | Definition 
 
        | Calcineurin inhibitor - Immunosup; inhibit 1st phase of Tcell activation (block NFAT prod) so no IL-2, IFN-gamma;
 Subseq block of B cell act, no IL-4;
 SE - Hirsuitism, gingivial hyperplasia, renal tox, HTN, infections, secondary malignancy
 |  | 
        |  | 
        
        | Term 
 
        | Tacrolimus (FK506, Prograf) |  | Definition 
 
        | Calcineurin inhibitor - Immunosup; 100X more potent than cyclo;
 inhibit 1st phase of Tcell activation (block NFAT prod) so no IL-2, IFN-gamma;
 Subseq block of B cell act, no IL-4;
 SE - neurotox, CYP3A5 snps, renal tox, HTN, infections, secondary malignancy
 |  | 
        |  | 
        
        | Term 
 
        | Methylprednisolone (Medrol) |  | Definition 
 
        | Corticosteroid - Immunosup; low dose- dec inflam cytokine,
 high dose - inc anti-inflamm proteins;
 Inhibits T&B cells;
 Short-term use;
 SE - CNS confusion, psychosis, HPA suppression, steroid withdrawal syndrome
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | mTOR inhibitor - Immunosup; Prevents 2nd phase of Tcell activation (G1 arrest);
 Prevention of Bcell diff into plasma cell (dec Ig's);
 Synergistic w/ cyclo;
 SE - hyperlipid, azotemia (inc creatinine, dec GFR), TUMORS, HEPATOTOXICITY and necrosis
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Cell-cycle disrupt - Immunosup; Blocks S phase purine formation;
 Inhibits RAC1/CD28 costimulation = apoptosis of memory Tcells;
 SE - skin cancer
 CI - pregnancy cat D; low TPMT gene product (should genotype), Allopurinol
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Adjuvant for analgesia/opioids; tx neuropathic pain (damage or infiltrate)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhalation Anesthetic; Analgesia, but not full anesthetic;
 Maintenance of protective reflexes;
 cheaper - "vapor sparing";
 SE - potential teratogen, drowsiness, dizziness, vertigo, dysphorya, panic, amnesia, laughing, parasthesias
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Liquid Inhalation Anesthetic; '1st' agent of choice;
 SE - areflexia, irritant, muscle relaxation, hypovent
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Liquid Inhalation Anesthetic; '1st' agent of choice - newer;
 Accumulate and equilibrate quickly, PLUS rapid recovery;
 SE - areflexia, irritant, hypovent
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Liquid Inhalation Anesthetic; '1st' agent of choice - newer;
 Accumulate and equilibrate quickly, PLUS rapid recovery;
 SE - areflexia, hypovent, CV depression
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Induction agent; Barbiturate - prolong binding of GABA to GABA receptor;
 Shifts endogenous GABA curve L;
 No analgesic activity;
 SE - Resp depression, death, bronchospasm, interactions lead to CV effects
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Induction agent; Inc GABA activity, dec Glu activity, RAPID;
 No analgesia;
 Sedation, antiemetic, dec ICP;
 SE - dec CBF, CO, RR, P INFUSION SYNDROME
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Induction agent; Inc GABA's action, may displace endogenous antagonists;
 Potent cerebral vasoconstrictor;
 Good drug for pt with CV problems;
 SE - injection pain, inhibiton of steroidogenesis (dec HPA axis), dec CBF;
 no prolonged use
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhibits Glu receptor, specific CNS depression; Balanced anesthesia;
 IV and IM;
 Potent analgesic, stimulate Symp NS, bronchodilator;
 Dissociated state - eyes can remain open;
 SE - hallucinations (use short acting BZ to control after sedation), inc CBF, inc MAP, inc CO
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Benzodiazepine - balanced anesthesia; Inc activity of GABA receptor/channel;
 Death from OD more diff than with barbs;
 No analgesia;
 Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects, wide safety margin;
 (Flumazenil = specific BZ antagonist)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Benzodiazepine - balanced anesthesia; Inc activity of GABA receptor/channel;
 Death from OD more diff than with barbs;
 No analgesia;
 Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects, wide safety margin;
 (Flumazenil = specific BZ antagonist)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Local anesthetic - amide; Injectable;
 Block Na channels, inc refractory period;
 Most commonly used form;
 Rapid onset, intermediate duration;
 ALSO... Rapid seq intubation- dec intracranial and bronchospastic response
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Local anesthetic - amide; Injectable;
 Block Na channels, inc refractory period;
 No topical effects;
 Slow onset, intermediate duration
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Local anesthetic - ester; Injectable;
 Block Na channels, inc refractory period;
 Slow onset, short duration;
 Standard used to measure potency of other agents
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Local anesthetic - ester; Injectable;
 Block Na channels, inc refractory period;
 Slow onset, long action;
 HIGH POTENCY;
 Potentially very toxic
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Local anesthetic - ester and amide!; Injectable;Block Na channels, inc refractory period; Fast onset, intermediate duration; Dental use w/ epi; Good penetration into BONE; SE - PARASTHESIAS |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | TOPICAL local anesthetic; Causes swelling of membrane, occlusion of Na channels;
 Often for Mucous membranes (contra to Nagel);
 SE - methemoglobinemia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | TOPICAL local anesthetic; Block Na channels, inc refractory period;
 Skin use, NOT mucus membranes (contra to Nagel);
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | alpha-1,2 Antagonist; used to reverse vasoconstriction
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Non-particulate Antacid; Na- and K-citrate + citric acid;
 Neutralize existing contents of stomach
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anticholinergic; Anti-sialogogue effect (dry secretions);
 Pre-op ancillary agent for anesthesia;
 Tx reflex bradycardia, block muscarinic anticholinesterases (NM blocker OD);
 Drying of secretions
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Ancillary: post-op CV support; tx hypoT;
 beta effect on heart, maintains renal perfusion
 |  | 
        |  | 
        
        | Term 
 
        | Phenylephrine (AK-Dilate) |  | Definition 
 
        | Ancillary: post-op CV support; alpha-agonist;
 tx hypoT;
 |  | 
        |  | 
        
        | Term 
 
        | Hydrocortisone think Post-op
 |  | Definition 
 
        | Ancillary: tx post-op Anaphylaxis;
 Anti-inflamm function of LT, PGs, kinins released by mast cells
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Barb for acute migraine tx; GABA enhancement - sedative function;
 SE - ANALGESIC OVERUSE SYN, CYP450 induction, CNS+resp depression, porphyria (beware of Nishimoto's vampireS)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Triptan for acute migraine tx (1st line); Cerebral vasoconstriction, Inh trigeminal n activation, Inh trigeminal cervical cortes activation;
 5-HT1b, 5-HT1d actions;
 Met by CYP450;
 Least problems with triptan SE, but..
 SE - sleepiness, dec mentition, inc HR, dizziness, VASOSPASM
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Triptan for acute migraine tx (1st line); Cerebral vasoconstriction, Inh trigeminal n activation, Inh trigeminal cervical cortes activation;
 5-HT1b, 5-HT1d actions;
 Met by MAOs;
 SE - sleepiness, dec mentition, inc HR, dizziness, VASOSPASM
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Triptan for acute migraine tx (1st line); Cerebral vasoconstriction, Inh trigeminal n activation, Inh trigeminal cervical cortes activation;
 5-HT1b, 5-HT1d actions;
 Met by MAOs;
 SE - sleepiness, dec mentition, inc HR, dizziness, VASOSPASM
 |  | 
        |  | 
        
        | Term 
 
        | Dihydroergotamine (Migranal) |  | Definition 
 
        | Ergot for acute SEVERE migraine tx; Agonist on 5-HT1&2, alpha-1&2, D2;
 Central and peripheral vasoconstriction;
 BP is unpredictable;
 SE - drug interactions, CATEGORY X, valvular heart dz;
 CI - vasospasm, triptans, vasoconstrictors, tobacco, propranolol
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anticonvulsant for chronic migraine prophylaxis; Inh Na channels, dec GABA met & reuptake;
 Highly protein bound;
 CYP2C9 substrate;
 SE - TERATOGEN, N/V, pancreatitis, hepatotoxicity, sedation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anticonvulsant for chronic migraine prophylaxis; Inh Na channels, dec GABA met & reuptake;
 Highly protein bound;
 CYP2C9 substrate;
 SE - TERATOGEN, N/V, pancreatitis, hepatotoxicity, sedation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Topical antibiotic; Prevent clean wound infection, early tx of infected dermatoses/wounds, prevent staph in nares, tx acne vulgaris, axillary deodorizer;
 Avoid in open wounds;
 SE - neuro-, nephro-toxic
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Topical antibiotic; Prevent clean wound infection, early tx of infected dermatoses/wounds, prevent staph in nares, tx acne vulgaris, axillary deodorizer;
 Limited in topical usage due to resistance fears;
 SE - neuro-, nephro-, and oto-toxic
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Topical antibiotic; Prevent clean wound infection, early tx of infected dermatoses/wounds, prevent staph in nares, tx acne vulgaris, axillary deodorizer;
 CI - pregnancy, renal, hapatic dz
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Topical/Oral antifungal agent - azole deriv; Dec production of ergosterol to compromise fungal cell wall integrity;
 Inh CYP2C19, 3A4,5,7!;
 Inh testosterone synth
 |  | 
        |  | 
        
        | Term 
 
        | Terbinafine (Desenex)(Lamisil) |  | Definition 
 
        | Topical/oral antifungal agent - allylamine; Inh squalene monooxygenase to block sterol synthesis to compromise structural integrity;
 Inh CYP2D6 as oral agent, CI - codeine, theophylline
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Oral antifungal agent; Dec production of ergosterol to compromise fungal cell wall integrity;
 Inh CYP2C9
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Oral antifungal agent; Dec production of ergosterol to compromise fungal cell wall integrity;
 Inh CYP3A4,5,7
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | IV/IM fusion protein - Immunosuppressant; Modulates CD2 response, induces apoptosis of CD2+ cells;
 Tx chronic plaque psoriasis;
 SE - lymphopenia, secondary BCC or SCC, neutralizing Abs
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 1ST Generation Retinoid - Oral; Bind RAR, inc RNA pol activity, dec epidermal cohesion, inc epidermal cell turnover;
 Tx inflamm dz's, hyperprolif dz's, skin malignancies;
 Enhance penetration of other agents (benzoyl peroxide, topical ABs);
 SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 2ND Generation Retinoid - Oral; Bind RAR, inc RNA pol activity, dec epidermal cohesion, inc epidermal cell turnover;
 Tx inflamm dz's, hyperprolif dz's, skin malignancies;
 Enhance penetration of other agents (benzoyl peroxide, topical ABs);
 SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | 3RD Generation Retinoid - TOPICAL; Bind RAR, inc RNA pol activity, dec epidermal cohesion, inc epidermal cell turnover;
 Tx inflamm dz's, hyperprolif dz's, skin malignancies;
 Enhance penetration of other agents (benzoyl peroxide, topical ABs);
 SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Topical; Oxidation of bacterial proteins, keratolytic for acne resolution;
 Tx. - P. acnes in seb. follicles and comedones;
 SE - Xerosis, skin irritation, sting, +Hydroquinone= dark staining
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Oral trichogenic; Block DHT production;
 Tx hair loss;
 SE - sexual dysfunction;
 CI w/ Saw palmetto
 |  | 
        |  | 
        
        | Term 
 
        | Cyclophosphamide (Cytoxan) |  | Definition 
 
        | Alkylating agent - nitrogen mustard; Prodrug, converted into active Aldophosphamide;
 Also, for immunosuppression;
 SE - renal failure, urotoxicity (hemorrhagic cystitis)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alkylating agent - nitrogen mustard; SE - renal failure, urotoxicity (tx: MESNA), CNS TOXICITY
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alkylating agent - Nitrosoureas (brain tumors); 1. Alkylates O6-guanine, DNA breakage;
 2. Isocyanate protein metabolite, inh DNA repair;
 SE - injection site rxn, pulm fibrosis, CNS tox, hepatic tox (tx: Defibrotide)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alkylating agent - Nitrosoureas (brain tumors); |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alkylating agent - aziridine; Rapidly met to TEPA, will form interstrand DNA cross-links;
 SE - neurotoxic, injection site rxn, bladder tox (if IVe)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alkylating agent - antibiotic; Metabolically activated;
 Gen free radicals;
 SE - myelosuppression, injection site rxn, hemolytic anemia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alkylating agent; Intrastrand DNA links, primarily at N7-guanine;
 IV only;
 SE - ototoxic, nephrotoxic, N/V, progressive neuropathy,
 secondary malignancy (AML)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Methylating agent; At O6-guanine, w/out Cl-;
 Metabolically activated;
 IV only;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Methylating agent; At O6-guanine;
 Prodrug, activated in liver;
 SE - weak MAO inhibitor, disulfriam-like rxns (+alcohol = malaise)
 |  | 
        |  | 
        
        | Term 
 
        | Methotrexate (Trexall, Rheumatrex) |  | Definition 
 
        | Antimetabolite agent - DMARD; Inhibits DHFR, thymidylate synthase;
 Polyglutamaded form is active but can't leave cell;
 SE - BM hemorrhage, renal tox, pneumonitis;
 (Rescue w/ Leucovorin)
 |  | 
        |  | 
        
        | Term 
 
        | Fluorouracil, 5-FU (Adrucil) |  | Definition 
 
        | Antimetabolite agent - pyrimidine analog; Inh thymidylate synthase - req "triple complex," enhanced by Leucovorin;
 SE - angina, myelosuppression, Hand-Foot syndrome
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Antimetabolite agent - pyrimidine analog; Locks cell division (not S phase specific);
 SE - myelosuppression, FLU-LIKE syndrome, inc liver transaminases, interstitial pneumonitis
 |  | 
        |  | 
        
        | Term 
 
        | Mercaptopurine, 6-MP (Purinethol) |  | Definition 
 
        | Antimetabolite agent - purine analog; Unknown mech;
 Oral;
 Resistance @ HGPRT, alkaline phosphatase;
 SE - myelo, inc hepatic enzymes;
 Look at TPMT;
 Interact w/ Allopurinol
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Antimetabolite agent - purine analog; Oral prodrug met by deoxycytidine kinase to active triphosphate;
 SE - myelo, lingering immunosupp
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product" - vinca alkaloids; Bind beta-tubulin, preventing polymerization, metaphase arrest;
 NO LEUKOPENIA;
 SE - alopecia, local cellulitis, NUMBNESS AND TINGLING, LOSS OF DTR & MOTOR FUNCTION
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product" - camptothecin analog; Inh Topo-1, break strands;
 Resistance - change in Topo-1or2;
 SE - neutropenia, diarrhea, N/V, inc hepatic enzymes;
 CI - Gilbert Syndrome
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product" - camptothecin analog; Inh Topo-1, break strands;
 Resistance - change in Topo-1or2;
 SE - neutropenia, diarrhea, N/V, inc hepatic enzymes, ACH-ase INHIBITION;
 CI - Gilbert Syndrome
 |  | 
        |  | 
        
        | Term 
 
        | Etoposide, VP-16 (Toposar) |  | Definition 
 
        | "Natural product" - podophyllotoxin; Inh Topo-II, prevents resealing of DNA breaks;
 Oral;
 SE - myelo, N/V
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product" - Taxanes; Bind beta-tubulin, preventing de-polymerization, mitotic arrest;
 Needs surfactant for solubility;
 SE - +Cremaphor=HYPERSENSITIVITY, mylo, STOCKING GLOVE SENSORY NEUROPATHY
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product" - anthracycline; Inh Topo-II;
 Makes free radicals, apoptosis;
 SE - myelo, alopecia, extravasational necrosis, cardiotox, red urine
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product"; Complex w/ Fe, oxidative damage to deoxyribose, DNA breaks (sim result as Topo block);
 SE - pulm fibrosis, dry cough, cutaneous tox (hyperpig, hyperkeratosis)
 |  | 
        |  | 
        
        | Term 
 
        | Dactinomycin, Actinomycin-D (Cosmegen)
 |  | Definition 
 
        | "Natural product"; Intercalates DNA, breaks ssDNA via topo-II action;
 IV;
 SE - pancytopenia, anorexia, N/V, diarrhea, alopecia, extravasational necrosis, derm manifestations
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | "Natural product"; Dec protein synth;
 Immunosupp;
 Dec insulin, hypergly;
 SE - PANCREATITIS, hypersensitivity rxn
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Interferes with conversion of ribonucleotides by scavenging the free radical cofactor of ribonucleotide reductase; Oral admin;
 Resisted by inc reductase;
 SE - desquamative interstitial pneumonitis, hematopoietic depression, GI, myelo (prophylaxis against myeloprolif dz)
 |  | 
        |  | 
        
        | Term 
 
        | Glucocorticoids (dexamethasone or predinosone) |  | Definition 
 
        | Anti-inflamm + immunosup; Used in chemo;
 SE - cushingoid syndrome
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Blocks VEGF - anti-angiogenesis; Limits growth of tumor;
 SE - HTN!, CHF< pulm hemorrhage, GI perforation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Binds EGFR-1, HER-1; Tx colorectal cancer
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Binds CD-52 - T-cell depletion; SE - pancytopenia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | TK inhibitor; Prevents EGFR-TK from phosphorylating, blocks signal transduction;
 Rapid resistance via expansion of clones w/ mutated target;
 SE - fatigue, rash, N/V/D, anorexia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | TK inhibitor; Targets BCR-ABL;
 Oral admin;
 High lvls of resistance;
 SE - cytopenia, N/V/D, edema, muscle cramps, fatigue, rash
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | TK inhibitor; Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
 SE - cardiotox, inc hepatic enzymes, lymphopenia, thrombocytopenia, graying of hair, skin discolor
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | TK inhibitor; Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
 SE - hand-foot syn, cytopenia, diarrhea
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Proteosome inhibitor; Inh UQ-proteosome path;
 Prevents degradation of IkBa, activates caspases, inh binding of myeloma cell to stroma, dec angiogenesis, inh cytokine interactions;
 SE - thrombocytopenia, peripheral neuropathy
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Hormone-ish; GnRH agonist, hyperstimulation leads to desenitization and "castration";
 Avoid initial flare w/ AR blocker;
 SC or IM admin;
 SE - sweat, dec libido, hot flashes, nausea, dec bone and muscle;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | SERD - hormone-ish; Completely suppresses estrogen receptor expression;
 IM admin;
 Resistance - inc growth factor signals;
 SE - nausea, asthenia, vasodilation
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | SERM - hormone-ish; Estrogen agonist at bone (inc density);
 Estrogen antagonist at mammary's;
 Dec cholesterol;
 Oral admin;
 SE - endometrial hypertrophy (cancer risk), thromboembolism, retinal degen
 |  | 
        |  | 
        
        | Term 
 
        | 2-Mercaptoethanesulfonate, Mesna (Mesnex)
 |  | Definition 
 
        | Chemoprotectant against hemorrhagic cystitis; Administer prior to chemo!;
 Problem drugs - cyclophosphamide, ifosfamide
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Tx nephrotoxic effect of cisplatin, carboplatin |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Rescue for methotrexate; Enhancement of 5-FU function
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Dec cardiotox of Anthracyclines ("-rubicin") |  | 
        |  | 
        
        | Term 
 
        | Methyl psyllium (Metamucil) |  | Definition 
 
        | Bulk-forming laxative; Dissolves in water to form a gel;
 Swell as the cmpd accumulates water;
 SE - allergic rxns, gas, intestinal obstruction, inhibits coumarin absorption
 |  | 
        |  | 
        
        | Term 
 
        | Methyl cellulose (Citrucel) |  | Definition 
 
        | Bulk-forming laxative; Dissolves in water to form a gel;
 Swell as the cmpd accumulates water;
 SE - dec absorption of other drugs/nutrients
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Surfactant laxative - stool softener; Dec water tension b/t stool and GI tract, allows for easier stool passage;
 Non-ionic surfactant;
 CI - abdominal pain, N/V
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Stimulant laxative - MOST POTENT; [3 MOAs @ colon] (1)inc perm of intestinal mucosa for back diffusion, (2)stimulate myenteric plexus to inc peristalsis, (3)inc PG synthesis and intestinal secretions;
 Natural product, gentle;
 SE - abdominal pain, nephritis, pigmentation of colon, pink urine
 |  | 
        |  | 
        
        | Term 
 
        | Magnesium sulfate: Epsom salt |  | Definition 
 
        | Osmotic laxative +Magnesium; (1) Non-absorble w/ osmotic activity;
 (2) Release of CCK leads to inc intestinal motility and secretions
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Osmotic laxative; Osmotic activity, non-absorbed;
 Conversion to organic acids make it a fecal acidifier;
 Hepatic failure - Can aid in ammonia clearance by dec absorption in colon;
 Prevents/tx encephalopathy in portal HTN
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Osmotic laxative; Osmotic and lubricant effects;
 Suppository
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-Diarrheal and cytoprotective; Absorbs hermful bacteria, viruses, toxins;
 Inc secretion of mucous and HCO3, inh Pepsin, chelates w/ proteins at base of ulcer forming protective barrier, inh H. pylori;
 Tx travellers diarrhea and H. Pylori infection
 |  | 
        |  | 
        
        | Term 
 
        | Attapulgite, Magnesium aluminum disilicate (Diasorb)
 |  | Definition 
 
        | Not in notes (?) Anti-Diarrheal: Binds to acids, toxins, bacteria in the GI;
 (previously included in Kaopectate)
 |  | 
        |  | 
        
        | Term 
 
        | Propantheline (Pro-Banthine) |  | Definition 
 
        | Anti-cholinergic as Anti-Diarrheal; Block vagal Ach to inhibit GI motility and secretions;
 Anti-spasmodic for cramps;
 Also tx urinary incontinence
 |  | 
        |  | 
        
        | Term 
 
        | Scopolamine (Transderm-Scop) |  | Definition 
 
        | Anti-Emetic - Anti-cholinergic; Blocks muscarinic receptors on CN VIII (vestibular afferents);
 Transdermal patch behind ear;
 Tx prophylaxis for motion sickness;
 SE - sedation, drowsiness, dry mouth
 |  | 
        |  | 
        
        | Term 
 
        | Prochlorperazine (Compazine) |  | Definition 
 
        | Anti-emetic - anti-dopaminergic; Also has anti-cholinergic functions;
 Tx N/V and intractable hiccups;
 Poor antipsychotic, useful antiemetic
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-emetic - anti-dopaminergic, Prokinetic; Blocks D2 receptors, inc ACH - inc gastric emptying;
 Inc LES pressure, inc esophageal peristalsis;
 Tx chemo-induced and post-op N/V, GERD, given prophylactically;
 SE - tardive dyskinesia
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-emetic - Serotonin antagonist; Block receptors in GI (dec vagal afferents), block receptors in CTZ;
 MOST EFFECTIVE ANTI-EM - use for chemo tox;
 Inc potency w/ dexamethasone;
 IV or oral
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-emetic - Serotonin antagonist; Block receptors in GI (dec vagal afferents), block receptors in CTZ;
 MOST EFFECTIVE ANTI-EM (and most potent in class) - use for chemo tox;
 Inc potency w/ dexamethasone;
 Oral
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Anti-emetic adjuvant; Substance P and neurokinin 1 antagonist;
 Crosses BBB to act on CTZ;
 Useful in cytotoxic chemos
 |  | 
        |  | 
        
        | Term 
 
        | Magnesium-aluminum hydroxide (Maalox) |  | Definition 
 
        | Antacid; Weak bases neutralize HCl, prevents pepsin activation;
 Tx reflux, adjunct w/ H2 block or PPIs in PUD;
 SE - dec drug absorption
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | H2 antagonist - PUD, GERD; Competitively inh H2 receptors in stomach, dec acid secretion;
 Least potent in class, short half life;
 SE - @CYP450; avoid by using other drugs
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | H2 antagonist - PUD, GERD; Competitively inh H2 receptors in stomach, dec acid secretion;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | H2 antagonist - PUD, GERD; Competitively inh H2 receptors in stomach, dec acid secretion;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | H2 antagonist - PUD, GERD; Competitively inh H2 receptors in stomach, dec acid secretion;
 Most potent and longest 1/2 life
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | PPI - PUD, GERD; Irreversible mod of H/K-ATPase - drug trapping;
 Req acidic pH for activation;
 Tx also - Z-E syndrome, refractory ulcers;
 Oral, long 1/2 life;
 More powerful than H2 blocker in inhibiting HCl production;
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | PPI - PUD, GERD; Irreversible mod of H/K-ATPase - drug trapping;
 Req acidic pH for activation;
 Tx also - Z-E syndrome, refractory ulcers;
 Less effective
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Cytoprotective - PGE1 analog; Inc secretion of mucous and HCO3;
 SE - dose-limiting diarrhea;
 Use - pts that require NSAID use
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Antibiotics - H.pylori infection; Inh microbe protein synthesis;
 Resistance - 8%
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Antibiotic; Give enema to dec colonic bacteria;
 Tx - portal HTN, encephalopathy
 |  | 
        |  |