PGE1 drug; 

Vasodilatory;

Tx: congenital heart defects (↑ pulmonary blood flow/oxygenation+maintains a patent ductus), also tx erectile dysfunction

PGE1 drug;

Tx: gastric ulcers (↓ gastrin secretion)/suppress gastric ulceration

PGE1 drug;

Tx gastric ulcers (↓ gastrin secretion)/suppress gastric ulceration;

SE: Dose-limiting diarrhea (given only to pt who must be on NSAIDs to protect the stomach)

PGI2 drug; stable;

Tx gastric ulcers;

Heparin substitute in renal disease (antithrombotic)*

PGI2 drug; stable;

Tx gastric ulcers, pulmonary HTN;

Heparin substitute in renal disease, antithrombotic;

15-methyl-PGF2-alpha drug;

Contracts the preg and non-preg uterus → Induces labor and abortion.

[Latisse]

PG-F2-alpha analog, drop formulation

Tx: Glaucoma (↓ IOP by ↑ outflow of aqueous humor), cosmetically to lengthen eyelashes (mechanism unknown).

(Diamox)

Carbonic Anhydrase inhibitor;

HCO3-, Na lost in urine, alkaline;

Cl reabsorbed; limited use as diuretic;

Tx cysteinuria (alkalinizes urine), glaucoma, seizures;

SE- metabolic acidosis, hyperchloremia, drowsiness, ↑ sensitivity to thiazides

Vasopressin/ADH receptor (V2 receptor, on the kidney tubules) antagonist;

Tx: SIADH

Loop Diuretic; inhibits Na-K-Cl symporter, inhibits NaCl reabsorption in the ascending LoH;

40x more potent than furosemide and no Warfarin interaction, ↑ renin;

Tx: edema, hypercalcemia, prophylaxis for renal failure, HTN; "loops lose Ca";

SE: ↑ BUN, hypokalemia, alkalosis, ototoxicity, drug interactions

Loop Diuretic: inhibits Na-K-Cl symporter, inhibits NaCl reabsorption;

Long half-life; ↑ renin;

Tx: edema, hypercalcemia, prophylaxis for renal failure, HTN; "loops lose Ca";

SE- inc BUN, hypokalemia, alkalosis, ototoxicity, drug interactions

Osmotic diuretic;

Tx: prophylaxis of acute renal failure (LOW GFR-ready) and glaucoma (↓ IOP);

SE- volume overload may lead to heart failure, hyponatremia, pulmonary edema

Class 1 thiazide diuretic (high GFR);

Inhibits Na/Cl symporter in aldo-insensitive segment of the DCT; 

Short acting;

Tx HTN, nephrogenic diabetes insipidus;

see SE of thiazide related drugs;

Class 2 thiazide diuretic (Low GFR 20-40);

High potency;

Inhibits Na/Cl symporter in aldo insensitive segment of the DCT;

Tx: HTN even if renal insufficiency, CHF

Hypokalemia;

Dilutional hyponatremia;

Hypochloremic alkalsosis;

Hypomagnesemia

Hyperuricemia;

Hypercalcemia

Hyperglycemia;

Hyperlipidemia;

Hypersecretion of renin and aldosterone

Fever;

Rash;

Purpura;

Pancreatitis;

Withdrawal edema

Aldosterone antagonist, K-sparing diuretic;

Inhibits Na reabsorption in DCT;

Tx HTN alongside HCTZ (not used alone), CHF;

SE- hyperkalemia, megaloblastic anemia*

Shown to prolong life in pt with CHF*

K-sparing diuretic;

Inhibits Na reabsorption in DCT;

Tx HTN alongside HCTZ (not used alone);

SE- hyperkalemia, megaloblastic anemia*

K-sparing diuretic;

Inhibits Na reabsorption in DCT;

Tx HTN alongside HCTZ (not used alone);

SE- hyperkalemia, megaloblastic anemia*

Alpha-2 agonist, presynaptically in the RVLM;

Tx: ↓ sympathetic output, Analgesic;

SE: CNS (sedation/drowsiness/fatigue/anxiety), water retention, xerostomia;

Centrally acting (post-synaptic a2) at the RLVM to tx severe HTN (ex. preeclampsia);

Also acts on presynaptic a2 receptors to ↓ NE release;

Tx - preeclampsia

SE - sedation, sleep disturbance water retention, immunological dysfunction

(Positive Coombs, "lupus-like syndrome")*

Selective alpha-1 antagonist;

Tx: HTN, BPH/urinary retention;

SE: Orthostatic HypoT

[Minipress]

Alpha-1 antagonist;

Tx: HTN (short acting), ↑ HDL, improves insulin resistance

(Inderal)

Beta-1 and 2 antagonist; direct effect on Na channels, anti-arrythmic;

Tx: HTN (esp in CHF or prev MI), migraine prophylaxis in kids.

SE see BB SEs

Beta-1 and 2 + alpha-1 antagonist;

Tx HTN, primary drug for CHF*;

↓ ROS production

Beta-1 and 2 antagonist (some partial agonist/ISA activity = no bradycardia);

Tx: Glaucoma, migraines; slight ISA

(Lopressor)

Beta-1 antagonist;

Tx HTN, esp associated w/ CHF

Beta-1 antagonist;

Tx HTN, esp associated w/ CHF

Beta 1 antagonist;

Antiarrthymic;

IV only, Very short half-life;

Tx: tachycardia, HTN

Raynaud's,

Bradycardia,

Bronchospasm,

Depression,

Drug interaction with conduction blockers,

Fatigue,

Decreased GFR

[Rogaine]

Direct vasodilator;

Pro-drug, opens K/ATP channels in SM;

Dilates arterioles only, not veins;

SE reflex tachycardia, hirsutism

Vasodilator and venodilator;

Prodrug for NO;

Dilates arteries and veins (↑ cGMP);

Tx HTN crisis, L sided heart failure;

SE - hypotension, tachycardia, palpitations, cyanide production*, nausea

ACE inhibitor;

Improves prognosis for CHF by ↓ afterload;

 ↑ synthesis of prostaglandins to ↑ vasodilation (vascular and renal); Short half-life;

SE - ortho hypotension, hyperK, dry cough!, angioedema (↑ bradykinins), fetotoxity;

CI in pregnant and nursing women

ACE inhibitor; improves prognosis for CHF by ↓ afterload; Prodrug, (de-esterification) converted into elanaprilat (activE);

SE - ortho hypotension, hyperK, dry cough!, angioedema (↑ bradykinins), fetotoxity;

CI in pregnant and nursing women

Angiotensin II Receptor Blocker (ARB);

Prodrug, active metabolite is non-competitive inhibitor;

Tx: CHF, HTN;

No cough/angioedema as compared to ACEI; unique ↑ uric acid secretion* (think gout) and inhibits CYP450;

SE - hypotension, hyperK, hepatic dysfunction, fetotoxicity;

CI in pregnancy

Angiotensin II Receptor Blocker (ARB);

No cough/↓ angioedema as compared to ACEI;

SE - hypotension, hyperK, hepatic dysfunction, fetotoxicity;

CI in pregnancy

Renin inhibitor, nonpeptide;

Blocks the conversion of angiotensinogen to AT-I by renin;

Never used alone, usually with ARB

L-type Ca Channel Blocker (CCB);

Tx HTN w/ angina and arrhythmias - ↓ contractility and AV conduction;

SE: peripheral edema, reflex tachy, hypoT, constipation, depression of SA/AV nodes, myocardial depression, nausea, HA

DHP Calcium Channel Blocker (CCB);

Systemic vasodilation, Selective for vascular SM, not cardiac;

Long-acting;

Tx HTN, use with diuretic;

SE - peripheral edema, reflex tachy, hypoT, constipation

(Norvasc)

DHP Calcium Channel Blocker (CCB);

Short-acting;

Tx HTN, use with diuretic; selective for vascular SM, not cardiac; 

SE - peripheral edema, reflex tachy, hypoT, constipation

L-type Calcium Channel Blocker (non-DHP);

Ltd reflex tachycardia;

Tx: HTN, angina, Class IV antiarrhythmic;

SE: Depression of SA/AV nodes, myocardial depression, peripheral edema, rashes, nausea, HA;

CYP3A4 inhibitor

L-type AND Na channel inhibitor;

Tx HTN;

SE- arrhythmias, agranulocytosis*

Digitalis glycoside; 

↑  intracellular Ca: Blocks Na/K-ATPase → ↑ intracellular Na→ ↑ activity Na/Ca exchanger → ↑ Ca → ↑ contractility;

Tx severe CHF with low EF; ↓ in AV conduction velocity (inc PR interval);

SE: interactions with diuretics, Warfarin

Direct arterial vasodilator;

Tx CHF; stimulates RAS;

SE - edema/↑ volume, nausea, anorexia, +FANA* (lupus-like syndrome), exacerbates angina (reflex tachy)

Vasodilator (Veins more than arteries);

↓ preload in tx of CHF; ↓ pulmonary arterial pressure, congestion; reduces LV filling Pressure

Veno- and vasodilator;

Reduces preload in tx of CHF; reduces pulmonary arterial pressure, congestion; reduces LV filling P

Beta-agonist, mostly B1 (also B2, a1);

Inotrope, Vasodilator (prevented by Bblocker), vasoconstrictor (unopposed a1 effect);

Tx: CHF

Depolymerizes MT;

Tx: gouty arthritis (terminates acute attacks and used prophylactically) and Familial Mediterranean Fever;

SE GI disturbance, blood dyscrasias

COX 1/2 inhibitor;

Analgesic and antipyretic + Inhibits leukocyte motility;

Very Potent

Tx: acute attack of gout and is used to close patent ductus in neonates;

SE: GI (N/V), CNS (HA), hematopoietic disorders;

Antagonizes furosemide and HCTZ

Competitive inhibitor of xanthine oxidase;

Metabolized to oxypurinol (a non-competitive inhibitor) = Suicide Inhibitor;

Reduces plasma levels and urinary excretion of UA, ↑ precursors of UA;

Dissolves UA crystals, prevents UA kidney stones;

Tx: Gout due to enzyme abnormalities (HGPRT/PPRP)or hematologic disorders (less common cause of gout) and Hyperuricemia. Does not treat acute gout flares;

SE: Acute gout flares, hypersensitivity rxn, liver fxn;

Interactions/CI: Interacts with 6-MP, Ampicillin, Azithroprine*

Uricosuric Agent;

Interferes with UA reabsorption by the organic acid ion transporter in Proximal Tubule → ↑ UA excretion; dissolution of UA crystals;

SE: Salicylates (asprins) inhibit uricosuric action of probenecid*

Class 1A Prototype- intermed. dissociation rate;

Na+ channel blocker (ganglionic blockade) = ↓ membrane responsiveness, ↓ conduction velocity, ↑ effective refractory period;

IV only;

Tx: Acute Atrial and Ventricular arrhythmias;

SE - (+)FANA, drug induced lupus, GI intolerance, bone marrow aplasia, QT prolongation*, Torsades*

Class III - K channel blocker; also blocks Na (I), Ca, and B-adrenergics (II);

Interacts with Thyroid hromone receptors; prolongs AP, effective refractory period; inhibits abnormal automaticity;

Tx: Vtach, Vfib, Afib, IV for cardiac rescuscitation, PO for chronic atrial, ventricular, and AVN arrhythmias;

SE: Pulmonary fibrosis (Amiodarone Pulmonary Toxicity), hypo- hyper-thyroid, blindness, hepatitis (Torsades rare!);

Inhibits CYP3A4

Class III - K channel blocker (prolongs AP);

Non-selective beta-blocker (1/3 the potency);

Tx: atrial, vententricular, and AVN reentry, Vtach;

SE - Torsades;

CI - long QT, renal insufficency, COPD, CHF, AV block, bradycardia;

Class III prototype - K channel blocker;

Prolong repolarization which ↑ effective refractory period; interrupts reentry, ↑ fibrillation threshold (↓ fib's);

Tx: IV for acute atrial arrhythmias (Afib, Aflutter)

(Diff from Nagle notes);

SE - Torsades

Very short half-life, IV only;

Blocks the AV node;

Tx: acute PSVT;

SE: Chest tightness, flushing, recurrence* of PSVT;

CI - methylxanthines, Dypyridamole (potentiation), WPW

(Aspirin)

Acetylates and irreversibly inhbits COX (1&2);

Inhibits platelet aggregation;

Tx: inflammation, fever, pain, HA, arthritis, dysmenorrhea, RA (large dose);

SE - GI ulcer, tinnitus, hearing loss, hepatic injury, Reyes', asthma, inc bleeding time;

CI with bleeding disorders

(Tylenol)

Inhibits of COX-1,2,(3);

Analgesic and antipyretic; NOT anti-inflammatory*;

SE - HEPATOTOXICITY;

No effects on platelets, NO GI irritation, Ok in Pregnancy*

(Advil, Motrin)

NSAID - reversible COX inhibitor;

Alters platelets (prolonged bleeding), Anti-inflammatory, Antipyretic, Analgesic;

Tx: Pain (400mg/6hrs), RA (3200mg);

SE- GI irritation (less than others);

CI in pregnancies

(Aleve)

NSAID - reversible COX 1/2 inhibitor;

Alters platelets (prolonged bleeding), Anti-inflammatory, Antipyretic, Analgesic;

Long half-life - 14hrs, so 2xday dosing;

SE- GI irritation

NSAID - heteroaryl acetic acid derivative;

POTENT analgesic, moderate Anti-inflammatory;

IM, oral, parenteral admin;

SHORT-TERM USE ONLY;

Tx: Post-op pain and inflammation, topical for eye inflammation (allergies or post-op);

NSAID - heteroaryl acetic acid derivative;

Potent COX inhibition;

Tx: RA, OA;

SE - GI, ↑ of hepatic aminotransferase activities;

CI in pregnancy

(Celebrex)

NSAID - selective COX2 inhibior;

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

[Rheumatrex]

DMARD anti-metabolite- inhibits DHFR to inhibit purine biosynthesis (thymidilate synthase);

Polygultamated form is active and trapped in the cell;

Tx: RA!, leukemias, psoriasis, immunosuppressor (↓ Igs, TNF, IL-1,6);

SE - hepato/renal toxicity, infections, BM hemorrage, pneumonitis, teratogenic;

CI - poor renal fxn, NSAIDs dec clearance, pregnancy (Cat X*)

(Rescue w/ Leucovorin)

DMARD - inhibits pyrimidine synthesis;

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);

DMARD - prodrug;

Metabolized to sulfapyridine (SE's) and 5-ASA (therapeutic component);

Tx: RA, UC, Crohn's;

SE - GI, ↓ WBCs, anemia, rash, impotence

(Enbrel)

DMARD - TNF inhibitor;

Soluble TNF receptor fused to human IgG and produced in CHO cells (hamster);

Reduces circulating TNF-a and blocks action at receptor;

SC injection 2x a week (3-4 day half life);

Tx: RA (those that don't respond to other DMARDs), psoriatic arthritis, AS, plaque psorisis, IBD;

SE - injection site rxn, ↑ risk of infection

DMARD - TNF inhibitor;

↓ circulating TNF-a and blocks action at its 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 arthritis, AS, UC, plaque psoriasis;

SE: Infusion site rxn, risk of infection

DMARD;

T-cell costimulation blocker;

CTLA4 conjugated w/ IgG, binds CD28 on Tcell, blocks response and cytokine (TNF) release;

IV admin first 0,2,4 weeks then once a month;

Used after failed TNF-inhibitor therapy;

SE: Risk of infections (immunocompromised)

DMARD;

Depletes B cells;

Monoclonal Ab against CD20 on Bcells, ↓ cytokine production;

Tx: RA who failed to respond to other TNF antagonists

Prototype Opiate: MOR Agonist;

Active but converted to M-6-glucaronide (100x higher potency);

Tx: mod/severe pain;

4 hr half life - accumulation; extensive (70%) first pass metabolism;

OK in pts taking MAO-Is;

SE: Tolerance, respiratory depression, N/V/constipation

MOR agonist (morphine-like);

Oral and parenteral admin;

Tx mod/SEVERE pain;

SE: Respiratory depression, N/V/constapation, sedation

(OxyContin)

MOR agonist (morphine-like);

Long acting;

Tx mod/severe pain; high abuse potential*

SE: Respiratory depression, N/V/constapation, sedation

(Demerol)

MOR agonist (morphine-like);

Tx mod/severe pain;

50% inactivated, first pass;

Toxic metabolite (normeperidine) can accumulate and cause CNS excitement (inhibits 5-HT/NE reuptake) = seizure risk;

Peripheral anticholinergic effects → dilation of pupils, Exception to the opiate OD triad (pinpoint pupils, respiratory depression, and coma*);

SE: Respiratory depression, N/V/constapation (less), sedation, seizures;

CI: lethal w/ MAO-inhibitors, CHILDREN**

MOR agonist (morphine-like);

po admin;

Long half life; Strongly binds and occupies opoid receptors but does not produce euphoria;

Tx: Abuse withdrawl/cravings, dampens the peaks/troughs of withdrawl sx during weaning;

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)

Opiate for MODERATE pain;

SE: Respiratory depression, N/V/constapation, sedation

MOR partial agonist (low action), KOR antagonist;

↓ abuse potential;

PO admin;

Tx: addiction/abuse;

SE - Abstinence syndrome (if morph-dependent)

Opioid mixed agonist/antagonist;

Binds and inactivates MOR; activates KOR;

Tx: mod/severe pain, but analgesic effect is slightly;

No constipation, no respiratory depression!;

SE - abstinence syndrome;

Opioid receptor antagonist;

Long Duration of action, but not a good choice for emergency OD;

PO admin, extensive first pass metabolism;

Tx: alcohol and opiod abuse (craving and relapse)

Opioid receptor antagonist;

IV only;

Rapid onset, short duration (esp compared to morhphine), Must give multiple doses accordingly;

Useful for acute OD;

First pass metabolism is extensive;

Tx: Opioid OD, reverses respiratory depression; can cause opioid withdrawal; start low, go slow*

(Imodium)

Opiate derivative;

Antidiarrheal:

↓ GI motility, peristalsis and secretion = ↑ absorption;

Tx diarrhea;

No CNS effects - doesn't cross BBB

(Benadryl)

1st Gen antihistamine;

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

(Dramamine)

1st Gen antihistamine;

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

(Claritin)

2^nd Gen antihistamine;

Longer duration, non-sedating (doesn't cross BBB) than 1^st gen, no anticholinergic fxn, SAFE for asthmatics;

Tx: allergy, hayfever, rhintis, urticaria, insect bites, contact flora;

SE: mild congnitive disturance, appetite stimulation

(Zyrtec)

2^nd Gen antihistamine; 

Longer duration of action, less sedating, no anticholinergic fxn, SAFE for asthmatics;

Tx: allergy, hayfever, rhintis, urticaria, insect bites, contact flora;

SE: Some sedation, appetite stimulation, mild congnitive disturance

(Clarinex)

2^nd/3^rd Gen antihistamine;

High specificity for H1, some muscarinic activity;

LONG HALF LIFE (27hrs);

2^nd/3^rd Gen antihistamine;

Inhibits histamine, LTs activity, blocks Ca2+ mobilization, and the 5-lipoxygenase pathway (production of LTs), inhbits PAF activity*;

LONG HALF LIFE;

Tx: rhinitis and hay fever;

Ok for use in asthmatics;

SE - somnolence, taste, nasal burning, ST, dry mouth, TERATOGENIC

Adrenergic Agonist;

Bronchodilator; B1, [B2], a1, a2;

Stimulates AC → ↑ cAMP → broncholar dilation, inhibits release of mediators from mast cells, ↓ vasculature permiability, ↑ mucociliary transport;

Tx: asthma, COPD; 

SE: skeletal m. tremor, N/V, HA, ↓ BP/↑ HR, arrhythmias

Adrenergic Agonist;

Bronchodilator; B1, [B2], a1, a2;

Stimulates AC → ↑ cAMP → broncholar dilation, inhibits release of mediators from mast cells, ↓ vasculature permiability, ↑ mucociliary transport;

Tx: asthma, COPD; 

SE: skeletal m. tremor, N/V, HA, ↓ BP/↑ HR, arrhythmias

B2-specific Adrenergic Agonist; Bronchodilator;

 FAST - reliever or rescue tx;

Stimulates AC → ↑ cAMP → broncholar dilation, inhibits release of mediators from mast cells, ↓ vasculature permiability, ↑ mucociliary transport;

Tx: asthma, COPD; 

SE: skeletal m. tremor, N/V, HA, ↓ BP/↑ HR, arrhythmias

B2-specific Adrenergic Agonist - Bronchodilator;

FAST - reliever or rescue admin;

Stimulates AC → ↑ cAMP → broncholar dilation, inhibits release of mediators from mast cells, ↓ vasculature permiability, ↑ mucociliary transport;

Tx: asthma, COPD; 

SE: skeletal m. tremor, N/V, HA, ↓ BP/↑ HR, arrhythmias

B2-specific Adrenergic Agonist - Bronchodilator;

SLOW - prevention (esp night-time, exercise use*);

Stimulates AC → ↑ cAMP → broncholar dilation, inhibits release of mediators from mast cells, ↓ vasculature permiability, ↑ mucociliary transport;

Tx: asthma, COPD; 

SE: skeletal m. tremor, N/V, HA, ↓ BP/↑ HR, arrhythmias

Cholinergic antagonist - Bronchodilator;

Competitive M blockade; 

↓ airway SM constriction, ↓ mucous secretion;

SE - pupillary dilation (bella donna) & cycloplegia (innervation of the ciliary m is blocked-no accomodation)

Cholinergic antagonist - Bronchodilator;

Competitive M blockade;

Short acting and no systemic functions;

↓ airway SM constriction, ↓ mucous secretion;

SE - pupillary dilation (bella donna) & cycloplegia (blocked innervation of the ciliary m - no accomodation)

Methylxanthine - Bronchodilator;

Inhibits PDE → ↑ cAMP → bronchodilation;

Blocks adenosine receptors → bronchodilation;

↓ release of mediators → anti-inflamm;

Tx asthma/COPD; chronotropic, ionotropic, ↑ CNS act, gastric acid secretion, SK muscle str (diaphragm);

SE - (10-20ug/mL)- N/V, HA, nervousness, insomnia, (>20ug/mL)- hypoK*, hyperglycemia, tachycardia, arrhythmias, NM irritability, seizures

Anti-inflammatory agent;

Alters Cl- channels on: mast cells (↓ degranulation), eosinophils (↓ inflamm), Airway nn (inhibits cough), ↓ bronchial hyperactivity;

Tx: asthma,COPD;

SE - TASTE, irritation of trachea (cough/bronchospasm)

Cromolyn;

Anti-inflammatory agent;

Alters Cl- channels on: mast cells (↓ degranulation), eosinophils (↓ inflamm), Airway nn (inhibits cough), ↓ bronchial hyperactivity;

Tx: asthma,COPD;

SE - TASTE, irritation of trachea (cough/bronchospasm)

Inhaled Glucocorticoid - Anti-inflammatory;

↓ production of inflammatory cytokines, ↑ prod of anti-inflammatory proteins; ↓ mucus secretion/bronchial hyperactivity;

Tx: asthma, COPD;

SE: Candidiasis, hoarse, dry mouth, ↓ bone density, dec growth rate (kids), CUSHINGOID SYNDROME

Inhaled Glucocorticoid - Anti-inflammatory;

↓ production of inflammatory cytokines, ↑ prod of anti-inflammatory proteins; ↓ mucus secretion/bronchial hyperactivity;

Tx: asthma, COPD;

SE: Candidiasis, hoarse, dry mouth, ↓ bone density, dec growth rate (kids), CUSHINGOID SYNDROME

ORAL Glucocorticoid - Anti-inflammatory;

↓ production of inflammatory cytokines, ↑ prod of anti-inflammatory proteins; ↓ mucus secretion/bronchial hyperactivity;

Tx: asthma, COPD;

SE: Candidiasis, hoarse, dry mouth, ↓ bone density, dec growth rate (kids), CUSHINGOID SYNDROME

(Singulair)

Leukotriene receptor blocker - Anti-inflammatory;

Blocks LTD4 - ↓ bronch reactivity/constriction, ↓ mucosal secretion, ↓ airway inflamm;

Tx: Asthma (aspirin-induced, caused by excess LTs!);

SE - GI, URI, nausea, otitis

(Zyflo)

Leukotriene Synthesis inhibitor - Anti-inflammatory; Inhibits 5-lipoxygenase and LT formation (B,C,D,E -4); ↓ SM contraction, ↓ blood vessel permiability (leukocyte migration);

SE: ↑ hepatic enzymes (watch liver func tests), 

Interaction with Theophylline* via CYP1A2

Anti-IgE - Humanized antibody;

↓ severity and freq of asthma attacks;

Tx: severe allergic asthma (step 5/6 treatment, slide 32);

SE - anaphylaxis, cold symptoms

Mouse anti-CD3 Ab - Immunosuppressant;

Reversibly blocks co-stimulation in T cells of the tissues and periphery;

Neutralizing Abs can develop = TOLERANCE;

SE: Acute hypersensitivity, systemic cytokine-mediated sx; pretreat with high-dose steroids*

Calcineurin inhibitor - Immunosuppressant;

Inhibits the 1st phase of Tcell activation (blocks NFAT production) → no IL-2, IFN-gamma;

Subsequent block of B cell activation→ no IL-4;

SE: Hirsuitism*, gingivial hyperplasia*, renal toxicity, HTN, infections, secondary malignancy

Calcineurin inhibitor - Immunosuppressant;

100X more potent than cyclosporine;

Inhibits 1st phase of Tcell activation (blocks NFAT production)→ no IL-2, IFN-gamma;

Blocks B cell activation → no IL-4;

SE: Neurotoxicity, CYP3A5 snps, renal toxicity, HTN, infections, secondary malignancy

Corticosteroid - Immunosuppressant;

@ Low dose: ↓ inflammatory cytokines,

@ high dose: ↑ anti-inflammatory proteins, Inhibits T&B cells, and acts as a Nuclear transcription inhibitor (histone deacetylator);

Short-term use;

SE: CNS confusion, psychosis, H-P Axis suppression, steroid withdrawal syndrome

mTOR inhibitor - Immunosuppressant;

Prevents 2^nd phase of Tcell activation → G1 arrest; Prevents B cell differentiation into plasma cells → ↓ dec Ig;

Synergistic w/ cyclo;

SE - hyperlipidemia, azotemia (↑ creatinine, ↓ GFR), TUMORS, HEPATOTOXICITY and necrosis

Cell-cycle Disruptor - Immunosuppressant;

Blocks S phase purine formation;

Inhibits RAC1/CD28 costimulation → apoptosis of memory T cells;

SE - skin cancer

CI - pregnancy cat D; low TPMT gene product (should genotype*), in pt taking Allopurinol

Inhalation Anesthetic and Analgesic (not full anesthetic); Maintenance of protective reflexes;

Cheaper - "vapor sparing";

SE - potential teratogen, drowsiness, dizziness, vertigo, dysphorya, panic, amnesia, laughing, parasthesias

Liquid Inhalation Anesthetic; '1st' agent of choice;

SE: Areflexia, irritant, muscle relaxation, rapid, shallow breathing

Liquid (at room temp, vaporizes easily) Inhalation Anesthetic;

'1st' agent of choice - newer;

Accumulates and equilibrates quickly, PLUS rapid recovery;

SE - areflexia, ↑RR/↓ TV, CV depression

Barbiturate - Induction agent;

Prolongs binding of GABA to GABA receptor, shifting the endogenous GABA curve L;

CNS Depressant - sedation and anesthesia, No analgesic activity*;

SE: Respiratory depression/death, bronchospasm, interactions lead to CV effects

Induction agent;

↑ GABA activity, ↓ Glu activity,

RAPID induction but No analgesia;

Sedation, antiemetic, ↓ ICP;

SE: ↓ CBF, CO, RR,

Propofol Infusion Syndrome* (assoc w high doses and long term use. Features: HyperK, hypertriglyceridemia and hepatomegaly. Can lead to cardiac failure, rhabdomyolysis, metabolic acidosis, renal failure and is often fatal).

Induction agent;

↑ GABA's action, may displace endogenous antagonists; Potent cerebral vasoconstrictor;

Good drug for pt with CV problems;

SE - injection pain, inhibiton of steroidogenesis (depresses HPA axis), ↓ CBF; 

Not for prolonged use

Inhibits Glu receptor, specific CNS depression;

Balanced anesthesia;

Potent analgesic, stimulates Symp NS, Bronchodilator; Induces a dissociated state - eyes can remain open;

IV and IM;

SE - hallucinations (use short acting BZ to control after sedation), ↑ CBF/MAP/CO

(Ativan)

Benzodiazepine - balanced anesthesia;

↑ activity of GABA receptor/channel; Sedative, hypnotic, anticonvulsant and anteretrograde Amnesic but Not analgesic, balancing sympathomimetic effects;

wide safety margin;

(Flumazenil = specific BZ antagonist)

Local anesthetic (MC used form) - Amide (hepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 Rapid onset, intermediate duration;

ALSO... Used in Rapid Sequence Intubation to ↓ intracranial and bronchospastic responses*

Local anesthetic - Amide (hepatic metabolism);

Injectable, no topical effects;

Blocks Na channels, ↑ refractory period;

Slow onset, intermediate duration

Local anesthetic - Ester (systemic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

Slow onset, long action;

HIGH POTENCY; Potentially very toxic

Local anesthetic - ester and amide!;

Injectable;

Blocks Na channels, ↑ refractory period;

Fast onset, intermediate duration;

Dental use w/ epi;

Good penetration into BONE;

SE - PARASTHESIAS

TOPICAL local anesthetic;

Causes swelling of membrane, occlusion of Na channels; 

SE: Methemoglobinemia*

Alpha-1,2 Antagonist;

Used to reverse vasoconstriction

Non-particulate Antacid;

Na- and K-citrate + citric acid;

Used to neutralize the existing contents of the stomach (as in surgery prep)

Anticholinergic;

Anti-sialogogue effect (dry secretions);

Pre-op ancillary agent for anesthesia;

Tx: reflex bradycardia, blocks muscarinic anticholinesterases (NM blocker OD), dries out secretions

Ancillary: post-op CV support;

Tx hypoT;

beta effect on heart, maintains renal perfusion*

Ancillary: post-op CV support;

Alpha-agonist;

Tx hypoT;

Ancillary: Tx post-op Anaphylaxis;

Anti-inflammatory: blocks function of LT, PGs, kinins released by mast cells

Barbituate;

GABA enhancement - sedative function;

Acute Tx for migraines;

SE - Strong possibility of causing Analgesic Overuse Syndrome, CYP450 induction, CNS+respiratory depression, porphyria

Triptan;

Causes cerebral vasoconstriction, Inhibits trigeminal n activation, Inhibits trigeminal cervical cortical activation; 5-HT1b, 5-HT1d actions;

  Tx: acute migraine (1st line);

Metabolized by CYP450; Least problems (of all the triptans w SE), but still causes sleepiness, dec mentition, inc HR, dizziness, VASOSPASM

[Imitrex]

Triptan;

Agonist at 5-HT1b, 5-HT1d - Inhibits the release of CGRP and Substance P→ Causes cerebral vasoconstriction, Inhibits trigeminal n activation, Inhibits trigeminal cervical cortical activation;

  Tx: acute migraine (1st line);

 SE: sleepiness, ↓ mentition, ↑ HR, dizziness, VASOSPASM

Ergot alkaloid;

Agonist on 5-HT1&2, alpha-1&2, D2;

Central and peripheral vasoconstriction;

Changes in BP are unpredictable;

Tx: acute SEVERE migraine;

SE - drug interactions, CATEGORY X, valvular heart dz;

CI - vasospasm, triptans, vasoconstrictors, tobacco, propranolol

Topical antibiotic;

Prevents clean wound infection, early tx of infected dermatoses/wounds, prevention of staph in nares,

Tx acne vulgaris, axillary deodorizer;

Avoid in open wounds (systemic toxicity*);

SE - neuro-, nephro-toxic

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 ototoxic

Topical/oral antifungal agent - allylamine;

Inhibits squalene monooxygenase activity to block sterol synthesis = compromised structural integrity;

Inhibits CYP2D6 as oral agent;

CI - codeine, theophylline*

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

(Accutane)

1ST Generation Retinoid - Oral;

Binds RAR, ↑ RNA pol activity, ↓ epidermal cohesion, ↑ epidermal cell turnover;

Tx: inflammory dz's, hyperproliferative dz's, skin malignancies;

Enhances penetration of other agents (benzoyl peroxide, topical ABs);

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

(Differin)

3RD Generation Retinoid - TOPICAL;

Binds RAR, ↑ RNA pol activity, ↓ epidermal cohesion, ↑ epidermal cell turnover;

Tx: inflammatory and hyperproliferative dz's, skin malignancies;

Enhances penetration of other agents (benzoyl peroxide, topical ABs);

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

Topical;

Oxidizes bacterial proteins, keratolytic agent for acne resolution;

Tx: P. acnes in sebaceous follicles and comedones;

SE - Xerosis, skin irritation, sting,

+Hydroquinone= dark staining

(Propecia)

Oral trichogenic;

Blocks DHT production;

Tx: hair loss;

SE - sexual dysfunction;

CI w/ Saw palmetto

Alkylating agent;

Prodrug, converted into active Aldophosphamide;

Also, for immunosuppression;

SE - renal failure, urotoxicity (hemorrhagic cystitis*)

Alkylating agent - (brain tumors);

1. Alkylates O6-guanine, DNA breakage;

2. Isocyanate protein metabolite, inhibits DNA repair;

SE - injection site rxn, pulm fibrosis, CNS toxicity, hepatic tox (tx: Defibrotide*)

Alkylating agent;

Rapidly metabolized to TEPA, will form interstrand DNA cross-links;

SE: Neurotoxic, injection site rxn, bladder tox (if IVe)

Alkylating agent - antibiotic;

Metabolically activated;

Generates free radicals;

SE: Myelosuppression, injection site rxn, hemolytic anemia*

Alkylating agent;

Causes intrastrand DNA links, primarily at N7-guanine;

IV only;

SE: Ototoxic, nephrotoxic, N/V, progressive neuropathy, secondary malignancy (AML);

Give with Amifostine to protect the kidneys*

(DTIC)

Methylating agent;

At O6-guanine, w/out Cl-;

Metabolically activated;

IV only;

Resistance arises due to gulcuronide transferases (AGT)

Methylating agent;

At O6-guanine;

Prodrug, activated in liver;

SE - weak MAO inhibitor, disulfriam-like rxns (+alcohol = malaise)

Antimetabolite agent - pyrimidine analog;

Inhibits thymidylate synthase - requires "triple complex;"

Actions enhanced by Leucovorin;

SE - angina, myelosuppression, Hand-Foot syndrome

Antimetabolite - pyrimidine analog;

Locks cell division (not S phase specific);

SE: myelosuppression, FLU-LIKE syndrome, ↑ liver transaminases, interstitial pneumonitis

Antimetabolite - purine analog;

Unknown mechanism;

Oral;

Resistance @ HGPRT, alkaline phosphatase;

SE: myelosuppression, ↑ hepatic enzymes;

Look at TPMT;

Interactions w/ Allopurinol

"Natural product" - Vinca alkaloid;

Binds beta-tubulin, preventing MT assembly and causing metaphase arrest;

NO LEUKOPENIA;

SE - alopecia, local cellulitis, NUMBNESS AND TINGLING, LOSS OF DTR & MOTOR FUNCTION

"Natural product" - camptothecin analog;

Inhibits Topo-1, strand breaks;

Resistance - change in Topo-1or2;

SE: neutropenia, N/V/D, ↑ hepatic enzymes;

CI - Gilbert Syndrome

Anti-cancer drug;

"Natural product" - podophyllotoxin;

Inhibits Topo-II, prevents resealing of DNA breaks;

Oral;

SE - myelo, N/V

(Taxol) "Natural product" - Taxanes;

Binds beta-tubulin, preventing de-polymerization and leading to mitotic arrest;

Needs surfactant for solubility;

SE: +Cremaphor=Hypersensitivity, mylosuppression, Stocking Glove Sensory Neruopathy*

"Natural product" - anthracycline, Abx;

Inhibits Topo-II, Intercalates DNA, generates Free Radicals, induces apoptosis;

SE - myelo, alopecia, extravasational necrosis, cardiotoxicity*, red urine

"Natural product";

Complexes with Fe → oxidative damage to deoxyribose → DNA breaks (as with Topo block);

SE: pulmonary fibrosis, dry cough, cutaneous toxicity (hyperpigmentation, hyperkeratosis)

"Natural product";

Intercalates DNA, breaks ssDNA via topo-II action;

IV;

SE - pancytopenia, anorexia, N/V, diarrhea, alopecia, extravasational necrosis, derm manifestations

"Natural product" Immunosuppressant;

Breaks down asparagine depriving cancer cells of Asp and decreasing protein synthesis. Also ↓ insulin levels;

Tx: Leukemias;

SE - PANCREATITIS, hypersensitivity rxn, hyperglycemia

Interferes with conversion of ribonucleotides by scavenging the free radical cofactor of ribonucleotide reductase;

Oral admin;

Resisted by ↑ reductase;

SE - desquamative interstitial pneumonitis, hematopoietic depression, GI, myelo (prophylaxis against myeloprolif dz)

Anti-inflammatory + immunosuppressive;

Used in chemo;

SE - cushingoid syndrome

Blocks VEGF - anti-angiogenesis;

Limits growth of tumor;

SE - HTN*, Pulmonary hemorrhage>CHF, GI perforation

Binds CD-52 - T-cell depletion;

SE - pancytopenia

EGFR - 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

(Gleevec)

TK inhibitor to BCR-ABL;

Oral admin;

High levels of resistance;

SE: cytopenia, N/V/D, edema, muscle cramps, fatigue, rash

TK inhibitor; Multi-inhibitor incl VEGFR, PDGFR, KIT, FLT;

SE: Cardiotoxicity (Prolonged QT), ↑ hepatic enzymes, lymphopenia, thrombocytopenia, graying of hair, skin discoloration

Proteosome inhibitor;

Inhibits the UQ-proteosome path;

Prevents degradation of IkBa, activates caspases, inhibits binding of myeloma cell to stroma, ↓ angiogenesis, inhibits cytokine interactions;

SE - thrombocytopenia, peripheral neuropathy

Hormone-ish; GnRH agonist;

Hyperstimulation leads to desenitization and "castration" of testosterone levels;

Avoid initial flare w/ AR blocker;

SC or IM admin;

SE - sweat, decreased libido, hot flashes, nausea, decreased bone and muscle mass;

SERM - hormone-ish;

Estrogen agonist/antagonist: agonist @ bone (↑ density), antagonist @ mammary glands and in tumors, ↓ cholesterol;

Oral admin;

Tx: Breast Cancers;

SE: Endometrial hypertrophy (cancer risk), Thromboembolism, retinal degeneration

(Mesenex)

Chemoprotectant against hemorrhagic cystitis; Administer prior to chemo!;

Problem drugs - cyclophosphamide, ifosfamide

Dec cardiotox of Anthracyclines ("-rubicin")

Iron chelator.

(Metamucil/Citrucel)

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

[Senokot]

Stimulant laxative - MOST POTENT;

[3 MOAs @ colon]

(1) ↑ perm of intestinal mucosa for back diffusion,

(2) Stimulate myenteric plexus to ↑ peristalsis,

(3) ↑ PG synthesis and intestinal secretions;

Natural product, gentle;

SE - abdominal pain, nephritis, pigmentation of colon, pink urine

Osmotic laxative and Fecal Acidifier;

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

[Pepto Bismol]

Anti-Diarrheal and Cytoprotective agent;

Absorbs harmful bacteria, viruses, toxins;

↑ secretion of mucous and HCO3, inhibits Pepsin, chelates proteins at base of ulcer forming protective barrier, inhibits H. pylori;

Tx: travellers diarrhea and H. Pylori infection

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

Anti-emetic - anti-dopaminergic;

Also has anti-cholinergic functions;

Tx: N/V and intractable hiccups;

Poor antipsychotic, useful antiemetic

Anti-emetic - anti-dopaminergic, Prokinetic;

Blocks D2 receptors, ↑ ACH = ↑ gastric emptying; ↑ LES pressure, ↑ esophageal peristalsis;

Tx: chemo-induced and post-op N/V, GERD, given prophylactically;

SE: Tardive dyskinesia

(Zofran)

Serotonin antagonist;

Anti-emetic - Blocks receptors in GI (↓ vagal afferents), blocks receptors in CTZ;

MOST EFFECTIVE anti-emetic;

IV or Oral;

Tx: N/V with chemo tox;

Increased potency w/ dexamethasone;

Serotonin antagonist;

Anti-emetic - Blocks receptors in GI (↓ vagal afferents), blocks receptors in CTZ;

MOST EFFECTIVE ANTI-EM (and most potent in class);

Oral;

Tx: N/V with chemo tox;

Increased potency w/ dexamethasone;

Anti-emetic adjuvant;

Substance P and neurokinin 1 antagonist;

Crosses BBB to act on CTZ;

Useful in tx emesis with cytotoxic chemos

(Maalox) Antacid;

Weak bases neutralize HCl, prevents pepsin activation;

Tx reflux, adjunct w/ H2 block or PPIs in PUD;

SE: decreased absorption of other drugs

(Zantac)

H2 antagonist;

Competitively inhibits H2 receptors in stomach, decreases acid secretion;

Tx: PUD, GERD

H2 antagonist; 

Competitively inhibits H2 receptors in stomach, ↓ acid secretion;

Tx: PUD, GERD;

(Pepcid AC)

H2 antagonist;

Competitively inhibits H2 receptors in stomach, decrease acid secretion;

Most potent and longest 1/2 life in its class;

Tx: PUD and GERD

(Prilosec) PPI;

Irreversible modification of H/K-ATPase - drug trapping; Requires acidic pH for activation;

Oral admin, long half life;

Tx: PUD, GERD, Z-E syndrome, refractory ulcers;

More powerful than H2 blocker in inhibiting HCl production;

PPI;

Irreversible modification of H/K-ATPase - drug trapping; Requires acidic pH for activation;

Tx: PUD, GERD, Z-E syndrome, refractory ulcers;

Less CYP metabolism = lasts longer!

PGE1 analog;

Cytoprotective agent - Increases secretion of mucous and HCO3;

SE - dose-limiting diarrhea;

Use - pts that require NSAID use

Doscusates

Osmotic laxative +Phosphate;

Cathartic

Osmotic laxative;

Mass evac for colonoscopy pre-op;

Dissolve into 4L and chug

Anti-emetic - anti-dopaminergic;
Also has anti-cholinergic functions;

Tx N/V and intractable hiccups

Phosphodiesterase 3 inhibitor (PDE-3)that potentiates the effect of (cAMP) + enhances contraction of LV by ↑ Ca²⁺ ATPase activity on the cardiac SR which ↑ Ca²⁺ uptake.

It has +inotropic, vasodilatory and min chronotropic effects;

Short half life, withdrawl effects;

Tx: CHF (only when conventional treatment w Vasodilators and Diuretics has proven insufficient);

SE: Ventricular Arrhythmias

Xanthine Oxidase inhibitor (inhibits both the oxidized and reduced forms);

Tx: hyperuricemia, gout;

SE: nausea, diarrhea, arthralgia, HA, increased hepatic enzymes and rash

Immunosuppressant;

Monoclonal Ab to IL-2 on T-cells, Blocks IL-2Ra/CD25 interaction;
Does not change lymphocyte #, just prevents proliferation;
Long half life - weeks;
No neutralizing Abs develop;

SE - severe acute hypersensitivity

Cell-cycle disruptor - Immunosuppressant;
Inhibits IMPDH - ↓ purines, cGMP;

Acts T and B cells - selective to lymphocytes;
Blocks memory B cell response;

SE - GI, infections, tumors

B2-specific Adrenergic Agonist;

Bronchodilator;
SLOW -prophylaxis (esp night-time, exercise);
Stimulates AC to ↑ cAMP → bronchodilation, Inhibits release of mediators from mast cells, ↓ vasculature permiability, promotes mucociliary transport;

Tx asthma, COPD;

SE: skeletal m. tremor, N/V, HA, ↓ BP, ↑ HR, arrhythmias

(Amcort)

Inhaled Glucocorticoid - Anti-inflammatory;
   ↓ production of inflammatory cytokines, ↑ anti-inflammatory proteins, ↓ mucus secretion, ↓ bronchial hyperactivity;

Tx asthma, COPD;

SE - Candidiasis, hoarseness, dry mouth, ↓ bone density, ↓ growth rate (kids), CUSHINGOID SYNDROME

Opiate derivative Antitussive agent;

Acts on non-opioid receptors;

Tx: Cough (no analgesia);

(Flurothane)
Liquid Inhalation Anesthetic;
3rd (of 3) agent of choice;

SE: Arrhythmias (esp w/ CA), hepatotoxicity (Halothane Hepatitis), loss of reflexes, rapid shallow breathing, CV depression

(Valium)
Benzodiazepine - balanced anesthesia;
  ↑ activity of GABA receptor/channel;

No analgesia;
Tx: Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects;

Wide safety margin, less death than with Barbituates;

SE - prolonged sedation, long 1/2 life;
(Flumazenil = specific BZ antagonist)

(Novacain)
Local anesthetic - ester;
Injectable;

Blocks Na channels, ↑ refractory period;
Slow onset, short duration;

Standard used to measure potency of other agents

Local anesthetic - amide;
Injectable;
Block Na channels, ↑ refractory period;

Slow onset, LONG duration;
Very potent due to long binding

TOPICAL local anesthetic;
Block Na channels, ↑ refractory period;

Often used on Mucous membranes (contra to Nagel);

Non-particulate Antacid;
Na- and K-citrate + citric acid;

Neutralize existing contents of stomach;

Reduces risk of aspiration pneumonia by using a non-particulate.

Topical antifungal agent - azole derivative;

 ↓ production of ergosterol to compromise fungal cell wall integrity;

Topical antifungal agent - azole derivative;

 ↓ production of ergosterol to compromise fungal cell wall integrity;

Topical antifungal agent - allylamine;

Inhibits squalene monooxygenase to block sterol synthesis and compromise structural integrity of the fungal cell wall.

TOPICAL immunosuppresant;
Unknown mechanism;

Tx: external genital or perianal HPV warts;

Topical Anti-trichogenic;

Unknown mechanism, releated to ODC levels;

Tx unwanted facial hair

Anti-Cancer, Alkylating agent;
Oral or IV, hepatic metabolism;

SE - Addison-like, hepatic toxicity (Veno-occlusive Liver Disease*)

↑ NK cells, inhibits anti-apoptosis signals, ↓ angiogenesis;
Prevents tumor cell adhesion;

SE - sedation, constipation, peripheral sensory neuropathy,

Teratogen (this was the drug given for morning sickness where all the birth defects resulted)

(Herceptin)
Binds EGFR-2, HER-2/NEU;

Tx breast cancer;

SE - cardiomyopathy

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

TK inhibitor;
Targets BCR-ABL;
Oral admin;

SE - cytopenia, N/V/D, edema, muscle cramps, fatigue, rash

 Anti-viral, anti-neoplastic;

Mimics endogenous INF triggering Cell cycle arrest in Go and apoptosis, ↑ immunological response;

SE - Neuropsychiatric, flu-like symptoms,

CYP450 inhibition

Hormone-ish;
GnRH agonist, hyperstimulation leads to desenitization and "castration" of Testosterone levels;
Avoid initial flare w/ AR blocker;
SC or IM admin;

SE - sweat, ↓ libido, hot flashes, nausea, ↓ bone/muscle

Hormone-ish - AR blocker;
Inhibits androgen binding, reflex ↑ levels of testosterone and androgens after GnRH drug admin;
Oral admin;

SE - gynecomastia, vasomotor flushing, mastodynia, ↓ libido

SERM - hormone-ish;
Estrogen agonist at bone (↑ density), Estrogen antagonist at mammary's, ↓ cholesterol;
Oral admin;

SE - endometrial hypertrophy (cancer risk), thromboembolism, retinal degeneration

Aromatase Inhibitor;

Aromatase is involved in hormone conversion to estrone & estrodiol in periphery;
Non-steroidal - competitive inhibition, Steroidal - non-competitive inhbition;
Oral admin;

SE: Arthralgia, diarrhea, nausea, hot flashes

Aromatase Inhibitor;

Aromatase is involved in hormone conversion to estrone & estrodiol in periphery;
Non-steroidal - competitive inhibition;
Oral admin;

SE - arthralgia, diarrhea, nausea, hot flash

(Aromasin)
Irreversible Aromatase Inhbitor;

Aromatase is involved in hormone conversion to estrone & estrodiol in periphery;

Steroidal=irreversible inhibition, non-steroidal=reversible;
Oral admin;

SE - arthralgia, diarrhea, nausea, hot flashes

Increases Urate Oxidase - converts uric acid to soluble allatoin for excretion;

Tx: Tumor Lysis Syndrome

Active ingrediant in Asprin;

Used as a topical tx for dandruff.

1st Gen Retinoid - Oral;
Binds RAR, ↑ RNA pol activity, ↓ epidermal cohesion, ↑ epidermal cell turnover;

Tx: inflammatory dz's, hyperproliferative dz's, and skin malignancies;
Enhances penetration of other agents (benzoyl peroxide, topical ABs);

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

[Lasix];

Loop Diuretic: inhibits Na-K-Cl symporter, inhibits NaCl reabsorption in the ascending loop of Henle;

Tx: edema, hypercalcemia, prophylaxis for renal failure, HTN; "loops lose Ca";

SE: ↑ BUN, hypokalemia, alkalosis, ototoxicity, drug interactions, Gout;

↓ efficacy of Warfarin*

Adalimumab

Immunosuppressant;

Human IgG McAb to TNF-alpha → clears membrane bound and soluble TNF in the body;

SE: ↑ risk of infections

Docusates

Anionic surfactant laxative;

Stool softener;

Short-term use only, causes irritation of the mucosa.

Exemestane

Irreversible inhibitor of aromatase, prevents conversion of estrogen to testosterone by CYP 19A1;

SE: hot flashes, diarrhea, arthralgia, thinning of the hair,

has fewer GYN sx than SERMs.

Phosphodiesterase inhibitor;

Ionotropic Agent;

IV only;

Used in CHF (short-term use only)

Prilocaine

Amide (hepatic metabolism) Local Anesthetic;

Blocks activated + inactivated V-gated Na+ channels from within the nerve fiber (prefers smaller fibers, mylenated and not), ↑ threshold for activation;

Must be unionized to be absorbed;

Block and recovery rate is Proximal → Distal*;

Slow onset, short duration of action;

SE: Hypersensitivity rxns.

1st Generation Anti-histamine;

Antichoinergic activity;

Anti-emetic

SE: Heavy sedation

Vincristine

Vinca Alkaloid, cancer drug;

Binds to beta-tubulin to prevent MT assembly.

SE: neurotoxicity

Resistance: Beta tubulin mutations.