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Block 2
Asmt's 4-9 (tsweat's abbreviated drug list)
237
Pharmacology
Professional
11/17/2010

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Term
Alprostadil
Definition
PGE1 drug;
used to treat congenital heart defects (inc pulmonary flow) and erectile dysfunction
Term
Rioprostil
Definition
PGE1 drug;
tx gastric ulcers
Term
Misoprostol
Definition
PGE1 drug;
tx gastric ulcers
Term
Carbacyclin
Definition
PGI2 drug;
stable;
tx gastric ulcers;
heparin substitute in renal disease
Term
Iloprost
Definition
PGI2 drug;
stable;
tx gastric ulcers, pulmonary HTN;
heparin substitute in renal disease;
Term
Carbaprost
Definition
15-methyl-PGF2-alpha drug;
induce labor and abortion
Term
Nesiritide (Natrecor)
Definition
recombinant BNP;
tx dyspnea due to CHF;
diuresis, natriuresis, vasodilation, dec aldosterone
SE- hypotension
Term
Bosentan (Tracleer)
Definition
Endothelin-1 receptor antagonist;
vasodilation;
tx CHF, pulmonary HTN;
SE teratogenic, hepatotoxicity, peripheral edema;
Term
Acetazolamide (Diamox)
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
Furosemide (Lasix)
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
Bumetanide (Bumex)
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
Torsemide (Demadex)
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
Mannitol
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
Metolazone (Zaroxolyn)
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
Amiloride (Midamor)
Definition
K-sparing diuretic;
inhibit Na reabsorption in DCT;
tx HTN alongside HCTZ (not used alone);
SE- hyperkalemia, megaloblastic anemia
Term
Triamterene (Dyrenium)
Definition
K-sparing diuretic;
inhibit Na reabsorption in DCT;
tx HTN alongside HCTZ (not used alone);
SE- hyperkalemia, megaloblastic anemia
Term
Clonidine (Catapres)
Definition
alpha-2 agonist RVLM;
tx dec sympathetic output;
analgesic;
SE sedation, drowsiness, fatigue, anxiety, water retention, xerostomia;
Term
Methyldopa (Aldomet)
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
Reserpine
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
Prazosin (Minipress)
Definition
alpha-1 antagonist;
tx HTN;
short acting;
inc HDL, improves insulin resistance
Term
Propranolol (Inderal)
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
Carvedilol (Coreg)
Definition
Beta-1 and 2 + alpha-1 antagonist;
tx HTN, primary drug for CHF;
dec ROS production
Term
Timolol (Blocadren)
Definition
beta-1 and 2 antagonist;
tx glaucoma, migraines;
slight ISA
Term
Metoprolol (Lopressor)
Definition
beta-1 antagonist;
tx HTN, esp associated w/ CHF
Term
Atenolol (Tenormin)
Definition
beta-1 antagonist;
tx HTN, esp associated w/ CHF
Term
Esmolol (Brevibloc)
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
Minoxidil (Loniten)
Definition
direct vasodilator;
pro-drug, opens K/ATP channels in SM;
dilates arterioles, not veins;
SE reflex tachycardia, hirsutism (Rogaine)
Term
Sodium Nitroprusside
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
Captopril (Captoten)
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
Enalapril (Vasotec)
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
Losartan (Cozaar)
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
Valsartan (Diovan)
Definition
ARB;
no cough, dec angioedema as compared to ACEI;
SE - hypotension, hyperK, hepatic dysfunction, fetotoxicity
Term
Candesartan (Atacand)
Definition
ARB;
tx CHF, HTN;
no cough, dec angioedema as compared to ACEI;
prodrug;
SE - hypotension, hyperK, fetotoxicity
Term
Aliskerin (Tekturna)
Definition
Renin inhibitor, nonpeptide;
never used alone, usually with ARB
Term
Verapamil (Calan)
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
Amlodipine (Norvasc)
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
Nifedipine (Adalat)
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
Nimodipine (Nimotop)
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
Diltiazem (Cardizem)
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
Bepridil (Vascor)
Definition
L-type AND Na channel inhibitor;
tx HTN;
SE- arrhythmias, agranulocytosis
Term
Digoxin (Lanoxin)
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
Hydralazine
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
Nitroprusside (Nipride)
Definition
veno- and vasodilator;
reduce preload in tx of CHF;
reduces pulmonary art P, congestion; reduces LV filling P
Term
Isosorbide dinitrate
Definition
Oral nitrate preparation;
Slow onset, med duration (4-6 hrs)
Term
Dobutamine (Dobutrex)
Definition
Beta-agonist, mostly B1 (also B2, a1);
Inotrope, vasodilator (prevented by Bblocker), vasoconstrictor (unopposed a1 effect);
Tx CHF
Term
Colchicine
Definition
tx gouty arthritis and prophylaxis, terminates acute attacks;
tx Familial Mediterranean Fever;
works by depolimerization of microtubules;
SE GI disturbance, blood dyscrasias
Term
Indomethacine (Indocin)
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
Allopurinol (Lopurin)
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
Probenecid (Benemid)
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
Ranazoline (Ranexa)
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
Flecainide (Tambocor)
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
Amiodarone (Cordorone)
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
Sotolol (Betapace)
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
Ibutilide (Convert)
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
Adenosine (Adenocard)
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
Acetaminophen (Tylenol)
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
Naproxen (Aleve)
Definition
NSAID - reversible COX inhibitor;
Alter platelet (prolonged bleeding), anti-inflamm, antipyretic, analgesic;
Long half-life - 14hrs, so 2xday dosing;
SE- GI irritation
Term
Ketorolac (Toradol)
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
Diclofenac (Voltaren)
Definition
NSAID - heteroaryl acetic acid deriv;
potent COX inhibition;
tx RA, OA;
SE - GI, elevation of hepatic aminotransferase activities;
CI for pregnancy
Term
Celecoxib (Celebrex)
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
Leflunomide (Arava)
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
Etanercept (Enbrel)
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
Infliximab (Remicade)
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
Abatacept (Orencia)
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
Rituximab (Rituxan)
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
Morphine
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
Hydromorphone (Dilaudid)
Definition
MOR agonist (morphine-like);
oral and parenteral admin;
tx mod/SEVERE pain
Term
Oxycodone (OxyContin)
Definition
MOR agonist (morphine-like);
long acting;
tx mod/severe pain;
high abuse potential
Term
Meperidine (Demerol)
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
Methadone (Dolophine)
Definition
MOR agonist (morphine-like);
po admin;
tx abuse withdrawl/cravings, dampen peaks/troughs of drug conc during weaning
Term
Fentanyl (Sublimaze)
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
Codeine
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
Hydrocodone
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
Butorphanol (Stadol)
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
Pentazocine (Talwin)
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
Naltrexone (ReVia)
Definition
opioid receptor antagonist;
LONG DURATION (24 hrs);
po admin, extensive first pass;
tx alcohol abuse (craving and relapse)
Term
Naloxone (Narcan)
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
Loperamide (Imodium)
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
Cyclizine (Marezine)
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
Loratadine (Claritin)
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
Cetirizine (Zyrtec)
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
Desloratadine (Clarinex)
Definition
2nd/3rd Gen antihistamine;
high specificity for H1, some muscarinic activity;
LONG HALF LIFE (27hrs);
Term
Azelastine (Astelin)
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
Epinephrine
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
Ephedrine
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
Albuterol (Proventil)
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
Terbutaline (Brethin)
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
Salmeterol (Serevent)
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
Atropine
Definition
Cholinergic antagonist - Bronchodilator;
Competitive M blockade;
dec airway SM constriction, dec mucous secretion;
SE - pupillary dilation & cycloplegia (X ciliary m)
Term
Ipratropium (Atrovent)
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
Theophylline
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
Cromolyn (Crolom)
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
Nedocromil (Tilade)
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
Budesonide (Pulmicort)
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
Ciclesonide (Omnaris)
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
Prednisone (Deltasone)
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
Monteleukast (Singulair)
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
Zafirlukast (Accolate)
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
Zileuton (Zyflo)
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
Omalizumab (Xolair)
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
Horse [ATGAM]
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
Rabbit [rATG]
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
Carimune
Definition
IV immunoglobulin - Immune boost;
tx immunodeficiency;
SE- renal failure
Term
Muromonab (Orthoclone)
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
Sirolimus (Rapamune)
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
Azathioprine (Imuran)
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
Phenytoin (Dilantin)
Definition
Adjuvant for analgesia/opioids;
tx neuropathic pain (damage or infiltrate)
Term
Nitrous Oxide
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
Isoflurane (Forane)
Definition
Liquid Inhalation Anesthetic;
'1st' agent of choice;
SE - areflexia, irritant, muscle relaxation, hypovent
Term
Desflurane (Suprane)
Definition
Liquid Inhalation Anesthetic;
'1st' agent of choice - newer;
Accumulate and equilibrate quickly, PLUS rapid recovery;
SE - areflexia, irritant, hypovent
Term
Sevoflurane (Ultane)
Definition
Liquid Inhalation Anesthetic;
'1st' agent of choice - newer;
Accumulate and equilibrate quickly, PLUS rapid recovery;
SE - areflexia, hypovent, CV depression
Term
Thiopental (Pentothal)
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
Propofol (Diprivan)
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
Etomidate (Amidate)
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
Ketamine (Ketalar)
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
Lorazepam (Ativan)
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
Midazolam (Versed)
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
Lidocaine (Xylocaine)
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
Mepivacaine (Carbocaine)
Definition
Local anesthetic - amide;
Injectable;
Block Na channels, inc refractory period;
No topical effects;
Slow onset, intermediate duration
Term
Procaine (Novacain)
Definition
Local anesthetic - ester;
Injectable;
Block Na channels, inc refractory period;
Slow onset, short duration;
Standard used to measure potency of other agents
Term
Tetracaine (Pontocaine)
Definition
Local anesthetic - ester;
Injectable;
Block Na channels, inc refractory period;
Slow onset, long action;
HIGH POTENCY;
Potentially very toxic
Term
Articaine (Septocaine)
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
Benzocaine (Americaine)
Definition
TOPICAL local anesthetic;
Causes swelling of membrane, occlusion of Na channels;
Often for Mucous membranes (contra to Nagel);
SE - methemoglobinemia
Term
Dibucaine (Nupercainal)
Definition
TOPICAL local anesthetic;
Block Na channels, inc refractory period;
Skin use, NOT mucus membranes (contra to Nagel);
Term
Phentolamine (OraVerse)
Definition
alpha-1,2 Antagonist;
used to reverse vasoconstriction
Term
Polycitra
Definition
Non-particulate Antacid;
Na- and K-citrate + citric acid;
Neutralize existing contents of stomach
Term
Glycopyrrolate (Robinul)
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
Dopamine
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
Butalbital (Fiorinal)
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
Naratriptan (Amerge)
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
Rizatriptan (Maxalt)
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
Zolmitriptan (Zomig)
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
Divalproex (Depakote)
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
Valproic Acid (Depacon)
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
Polymixin B Sulfate
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
Gentamicin (Garamycin)
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
Tetracycline (Sumycin)
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
Ketoconazole (Nizoral)
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
Fluconazole (Diflucan)
Definition
Oral antifungal agent;
Dec production of ergosterol to compromise fungal cell wall integrity;
Inh CYP2C9
Term
Itraconazole (Sporanox)
Definition
Oral antifungal agent;
Dec production of ergosterol to compromise fungal cell wall integrity;
Inh CYP3A4,5,7
Term
Alefacept (Amevive)
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
Isotretinoin (Accutane)
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
Acitretin (Soriatane)
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
Adapalene (Differin)
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
Benzoyl peroxide
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
Finasteride (Propecia)
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
Ifosfamide (Mesnex)
Definition
Alkylating agent - nitrogen mustard;
SE - renal failure, urotoxicity (tx: MESNA), CNS TOXICITY
Term
Carmustine, BCNU
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
Lomustine, CCNU
Definition
Alkylating agent - Nitrosoureas (brain tumors);
Term
Thiotepa
Definition
Alkylating agent - aziridine;
Rapidly met to TEPA, will form interstrand DNA cross-links;
SE - neurotoxic, injection site rxn, bladder tox (if IVe)
Term
Mitomycin C (Mutamycin)
Definition
Alkylating agent - antibiotic;
Metabolically activated;
Gen free radicals;
SE - myelosuppression, injection site rxn, hemolytic anemia
Term
Cisplatin (Platinol)
Definition
Alkylating agent;
Intrastrand DNA links, primarily at N7-guanine;
IV only;
SE - ototoxic, nephrotoxic, N/V, progressive neuropathy,
secondary malignancy (AML)
Term
Dacarbazine, DTIC
Definition
Methylating agent;
At O6-guanine, w/out Cl-;
Metabolically activated;
IV only;
Term
Procarbazine (Matulane)
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
Gemcitabine (Gemzar)
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
Cladribine (Leustatin)
Definition
Antimetabolite agent - purine analog;
Oral prodrug met by deoxycytidine kinase to active triphosphate;
SE - myelo, lingering immunosupp
Term
Vincristine (Oncovin)
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
Topotecan (Hycamtin)
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
Irinotecan (Camptosar)
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
Paclitaxel (Taxol)
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
Doxorubicin (Adriamycin)
Definition
"Natural product" - anthracycline;
Inh Topo-II;
Makes free radicals, apoptosis;
SE - myelo, alopecia, extravasational necrosis, cardiotox, red urine
Term
Bleomycin (Blenoxane)
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
L-Asparaginase (Elspar)
Definition
"Natural product";
Dec protein synth;
Immunosupp;
Dec insulin, hypergly;
SE - PANCREATITIS, hypersensitivity rxn
Term
Hydroxyurea (Hydrea)
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
Bevacizumab (Avastin)
Definition
Blocks VEGF - anti-angiogenesis;
Limits growth of tumor;
SE - HTN!, CHF< pulm hemorrhage, GI perforation
Term
Cetuximab (Erbitux)
Definition
Binds EGFR-1, HER-1;
Tx colorectal cancer
Term
Alemtuzumab (Campath)
Definition
Binds CD-52 - T-cell depletion;
SE - pancytopenia
Term
Gefitinib (Iressa)
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
Imatinib (Gleevec)
Definition
TK inhibitor;
Targets BCR-ABL;
Oral admin;
High lvls of resistance;
SE - cytopenia, N/V/D, edema, muscle cramps, fatigue, rash
Term
Sunitinib (Sutent)
Definition
TK inhibitor;
Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
SE - cardiotox, inc hepatic enzymes, lymphopenia, thrombocytopenia, graying of hair, skin discolor
Term
Sorafenib (Nexavar)
Definition
TK inhibitor;
Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;
SE - hand-foot syn, cytopenia, diarrhea
Term
Bortezomib (Velcade)
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
Leuprolide (Lupron)
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
Fulvestrant (Faslodex)
Definition
SERD - hormone-ish;
Completely suppresses estrogen receptor expression;
IM admin;
Resistance - inc growth factor signals;
SE - nausea, asthenia, vasodilation
Term
Tamoxifen (Nolvadex)
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
Amifostine (Ethyol)
Definition
Tx nephrotoxic effect of cisplatin, carboplatin
Term
Leucovorin
Definition
Rescue for methotrexate;
Enhancement of 5-FU function
Term
Dexroxazone (Zinecard)
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
Poloxamer 188
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
Senna (Senokot)
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
Lactulose (Cephulac)
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
Glycerine
Definition
Osmotic laxative;
Osmotic and lubricant effects;
Suppository
Term
Bismuth subsalicylate
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
Metoclopramide (Reglan)
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
Ondansetron (Zofran)
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
Granisetron (Kytril)
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
Aprepitant (Emend)
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
Cimetidine (Tagamet)
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
Ranitidine (Zantac)
Definition
H2 antagonist - PUD, GERD;
Competitively inh H2 receptors in stomach, dec acid secretion;
Term
Nizatidine (Axid)
Definition
H2 antagonist - PUD, GERD;
Competitively inh H2 receptors in stomach, dec acid secretion;
Term
Famotidine (Pepcid AC)
Definition
H2 antagonist - PUD, GERD;
Competitively inh H2 receptors in stomach, dec acid secretion;
Most potent and longest 1/2 life
Term
Omeprazole (Prilosec)
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
Lansoprazole (Prevacid)
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
Misoprostol (Cytotec)
Definition
Cytoprotective - PGE1 analog;
Inc secretion of mucous and HCO3;
SE - dose-limiting diarrhea;
Use - pts that require NSAID use
Term
Clarithromycin (Biaxin)
Definition
Antibiotics - H.pylori infection;
Inh microbe protein synthesis;
Resistance - 8%
Term
Neomycin (Myciguent)
Definition
Antibiotic;
Give enema to dec colonic bacteria;
Tx - portal HTN, encephalopathy
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