Disease Class/Type of Drug Drugs Mode of action

Proton Pump Inhibitors Omeprazole
H2 Antagonists
Antacids
Peptic Ulcer Disease
Fiber/Bulk Forming Laxatives
Osmotic Laxatives
Constipation
Contact Stimulant Laxatives
Emollient Laxatives
Glycerin Suppository
Diarrhea
Anti-Emetics
Statins
Fibrates
Dyslipidemia Agents
Bile Acid Sequestrants
Nicotinic Acid
Irriversibly binds H+/K+ ATPase. CI: pregnancy
Ranitidine, Cimetidine Competitive inhibition of H2 receptors (histamine)
Magnesium Diarrhea, muscle weakness, cramping, accumulation in renal failure
Aluminum Binds phosporus. Constipation. Osteomalacia.
Calcium Constipation. Alkalosis. Milk alkali syndrome.
Sodium Alkalosis. Sodium overload --> hypertension
Sucralfate Binds proteins forming protetive lining (mucosa).
Misoprostol Prostaglandin analog. Avoid in pregnancy. Increase bicarb, increase mucus. Decrease gastric acid.
H. pylori eradication Triple therapy: e.g. PPI, clarithromycin, amoxicillin --> LOSEC 123A
Prodium (psyllium) Absorb and retain large amounts of fluid, increasing bulk. 24+ hours.
Metamusil
Fiber tables
Magnesium hydroxide (MOM) Potent osmotic effect, retaining fluid in bowel lumen and softening stool. 3-24 hours.
Lactulose
Epsom salts
Bisacodyl Act on GI mucosa resulting in effect on GI motility and absorption of electrolytes and water. 6-12 hours.
Anthraquinones Rectally: 0.5-1 hour. Can cause fluid and electrolyte imbalances.
Phenolpthalien Ostomalacia. Local irritation (Bisacodyl)
Docusate Reduces surface tension of the oil-water interface of stool. 12-72 hours.
Stim rectal mucosa and may soften the stool. Well tolerated. 15-30 minutes.
Loperamide Inhibits peristalsis. Prolong transit time.
Bismuth Compounds ??? Salicylate component. As effective as loperamide. Can cause black tongue.
Diphenoxylate Inhibites excessive GI motility and GI propulsion. Abuse potential --> euphoria.
Blocks dopamine receptors at the CTZ. Enhances response to ACH (enhanced motility, inc gastric
Metoclopramide
emptying). May worsen Parkinson's
Scopolamine Blocks action of Ach at PNS sites in smooth mucle & secretory glands.
Ondansetron Selective seretonin receptor antagonist (vomit reflex). $, good for chemo. CYP enzyme substrate.
Dimenhydinate Anticholinergic effect. Drowsiness.
Blocks post-synaptic dopamine receptors in brain including CTZ. Caution - wear SPF. May worsen
Procholoperazine
Parkinson's, CI: glaucoma. Difficulty with urination.
Atorvastatin, Pravastatin,
Simvastatin, Rosouvastatin, Reduces hepatic cholesterol synthesis. Rhabomyolysis. Inhibitors: grapefruit juice, CYP p450 inhibitors
Fluvastatin, Lovastatin
Fenofibrate Decreased production of TG and increase clearance of TG rich lipoproteins
Gemfibrozil Dyspepsia, gallstones, myopathy. GI: severe renal or hepatic disease.
Cholestyramine
May increase TG. GI distress/constipation/may inhibit absorption of other meds/vitamins
Colestipol
Niacin Inhibition of synthesis and esterification of fatty acids (hepatic production of VLDL and apoB) Flushing,
Niaspan hyperglycemia, hyperuricemia, GI distress. GI: liver disease, gout, peptic ulcer.

Diuretics
Centrally acting sympatholytics
Peripherally acting sympatholytics
B Blockers (BB)
Hypertension
ACE inhibitors (ACE -)
Angiotensin Receptor Blockers (ARB)
Direct acting vasodilators
Ca++ Channel Blockers (CCB)
Increases Na+ and H2O excretion (inhibits Na/K/2Cl cotransporter in DCT). Often 1st choice with
hypertension - useful in combo (BB and ACE-). Decresed excrection of Ca++ and uric acid. Inc
Thiazides
excretion of Mg+, K+, Na+. --> hypokalemia (ht palpitation), hyperuricemia. CI: diabetics, elevated
chol, pregnancy. CYP p450 interactions.
Inhibit electolyte tansport in ascending loop of Henle. Good for those resistant to thiazides. Pronounced
LOOP Diuretics (Furosemide)
diuresis - furosemide > thiazides. Same depletions. Ototoxicity. Inc gluc and uric acid.
K+ Sparing Diuretics Inhibit Na+ reabsorption in collecting duct. Mild. Good to help with hypokalemia induced by other
(Spironolactone) diurectics. Watch for anti-adrenergic effects.
Activate a2-adrenergic receptors (which inhibit NE). Peripheral action: lower BP by interfering with
synthesis, storage and/or release of NE from sympathetic nerve terminals (a2 ad. Agonist)
clonidine Does not decrease GFR, decreases CO. Given when not responding to diuretics.
Pro-drug. For patients with renal insufficiency and in pregnancy. - serotonin and NE. Decreases TPR, no
A-methyldopa
dec in CO.
Competitively blocks a1 adrenoreceptors of smooth muscle. Dec TPR, minimal change to CO. First dose
Prazosin
often causes fainting. CI: adults >55.
Common to all BB is the ability to competitively antagonize the effects of NE and EPI on the B1
adrenergic receptors in the heart and renin-secreting cells of the KI. Decrease CO. Inhibit Renin.
Greater effectiveness in caucations and young. Treats conditions that co-exist with HT. May mask
symptoms of hypoglycemia. CNS: depression, fatigue, cold extremeties. CV: bradycardia.
Bronchoconstriction at high doses. Decrease HDL and inc TG. CI: asthma, angina, peripheral
vasc. disease. CYT p450 sensitive. Hyperkalemia risk.
antagonist at B1 and B2, readily penetrates into CNS. Good for glaucoma, migraine, hyperthyroidism,
Propranolol
angina, migraine, MI.
Atenolol Selective for B1 subtype. Good for asthmatics/smokers/DM.
Sotalol Does not penetrate into CNS
Pindolol Partial aganost at B1 and B2. Good for athletes.
Labetalol, Carvedilol Antagonists at A1 adreneric receptors. Labetalol: no lipid/sugar effects
Second line in uncomplicated HT, first line in DM, CHF. ACE inhibitors reversibily inhibit the ACE
enzyme catalyzing angiotensin I to angiotensin II --> less aldosterone released, lowers TPR. Also
diminishes rate of bradykinin inactivation (which is a vadodilator). Adverse effects: cough,
angioedema, hyperkalemia, acute renal failure, hypotension. CI: pregnancy/ breastfeeding.
captopril Rapid onset
lisinopril No biotransformation needed to activate.
enalapril Takes hours for onset
ramipril
fosinopril
benazepril
The 'sartans' (Losartan,
Reversibly bind to the AT1 subtype of the angiotensin II receptors. Similar actions to ACE-. 90% plasma
valsartan, candesartan,
protein bound.
telmisartan)
Most powerful anti-HT drugs - direct acting smooth muscle relaxants. Increases vasodilation. When
used alone, compensatory REFLEX TACHYCARDIA, FLUID RETENTION. Saved fore severe HT
patients, not used without diuretic.
Hydralazine Moderately severe HT. can precipitate angina, lupis like syndrome.
Minoxidil severe to malignant HT. Adverse effects: volume overload, edema, CHF, hypertrichosis.
Bind when channel is inactivated, block depolarization of the cell. Dec Na, so no diuretic needed. Useful
in asthma, DM, angina, peripheral vasc dz. Short half life. Infrequent adverse effects. 10% constipation.
Myocardial ones are p450 inhibitors.
Most frequency-dependent, act on myocardial cells. Well absorbed but extensive first pass. Eliminated in
Verapamil
urine in 5 hours.
Nifedipine Acts on vascular smooth muscle --> dec TPR. Excreted in urine, 2 hours. Reflex tachycardia.
act on myocardial cells. First pass so low bioavailability. Eliminated 3.5 hours. Little or no change in
Diltiazem
heart rate.
 Reduce Na+ influx into the cell by moderate blockage of Na+ channel. Dec slope of phase 0 and 4.
"Broad specturm antiarrhythmic agents" (both SV and V arrhythmias). Problems with negative inotropic
effects with CHF. Can cause torsade de pointes (polymorphic ventricular tachycardia).
Class I: Sodium channel Blockers
1A: Quinidine, Procainamide
1B: Lidocaine
1C: Propafenone
Blocks B1 receptor at the SA node. Direct membrane stabilizing effect slows AV nodal conduction.
Class II: Beta Blockers Carvedilol
Slows phase 4 depolarization at the SA node. Used for superventricular arrhythmias.
Arrythmia Reduce K+ efflux out of the cell by blocking K+ channels (increases refractoriness). Ventricular action
Class III: Potassium Channel Blockers Amiodarone potential is lengthened. It also blocks Na+, Ca+ channels and is an alpha and beta adrenergic
antagonist. For both SV and V arrhythmias. Interacts with warfarin, digoxin, BB/CCBs.
Block Ca+ channels in the heart - affect SA and AV nodes. Slows SA node automaticity, increased
Class IV: Calcium Channel Blockers
refractoriness (decreases phase 0 depolarization). Used for superventricular arrhythmias.
Increase the force of myocardial contraction, only orally effective inotropic agents in NA. MOA: direct
inhibition of membrane Na/K ATPase and an indiret increase in vagal tone. Slows AV conduction
Cardiac Glycosides Digoxin/Digitalis and increases refractoriness by enhancing vagal activity. Used for Superventricular arrhythmias and
CHF. Narrow TI. Toxicity = arrhythmias. K+ is often effective against glycoside-induced arrhythmias.
Toxicity = increased automaticity.
Inhibit the ADP pathway for platelet activation; interact with platelet glycoprotein, inhibiting the binding of
Thienopyridines Clopidogrel fibrinogen to activated platelets and thus inhibiting aggregation. Is a prodruct (metabolized by p450 3A to
Agents Affecting an active metabolite.) Often given with aspirin. Mainstay tx for CAD.
Platelet Function
Inhibit ADP release reaction by inhibiting platelet cyclooxygenase, thus preventing synthesis of
NSAIDS Aspirin
thromboxane (THA2).
Nitrate produce relaxation of vascular smooth muscle by production of NO --> cGMP --> vascular
Nitrates Nitrates Nitroglycerin relaxation. Vanodilation: nitrates produce venous dilation --> reduced preload --> reduced ischemia.
Gradual diminished effectiveness with each dose - need intermittent dosing. Can get hypotension.
Used for thrombosis/embolism and post MI. Individualize dose based on INR. Older patients have
Warfarin increased response to warfarin. CI: pregnancy. Inhibits synthesis of vit K dependant clotting factors
Anticoagulation Anticoagulants (is a vitamin K antagonist)
Binds to antithrombin and inhibits serine protease clotting enzymes. Immediate anticoagulant vs.
Heparin
warfarin (3-7 days). NOT plasma protein bound (unlike warfarin). IV.

Bind to dietary phosphate in gut. Taken with meals.

Aluminum Very effective, not too costly. Accumulation: osetomalacia, anemia, encephalopathy. Alzheimer's risk!
Phosphate binders
Magnesium Accumulation, diarrhea. Not really used
Renal Osteodystrophy Calcium Most widely used, cheap, helps hypocalcemia. Risk of hypercalcemia.
Management Non Ca, Mg, Al containing polymer resin that binds phosphate in the gut. Used if: hyperCa +
Sevelamer (renagel)
hyperPhosphate. May help with chol but may impair absorption of other medications. Costly.
Directly suppresses PTH secretion. OTC vitamin D ineffective - requres activation by the kidney!
Enhances calcium absorption from the gut - can lead to hypercalcemia.
Vitamin D Supplementation
Alfacalcidiol Requires activation by liver
Calcitriol 1,25-OH active
Caused mainly by iron deficiency and diminished EPO secretion. Normocytic, normochromic.
Eprex Recombinant human Epo.
Erythropoietin Supplementation Altered chemical structure with longer half life; allows for less frequent dosing. Risk of agg. HT, seizures,
Anemia and Renal Darbepoetin Alfa
Failure hemodialysis access clotting.
Higher need for adequate iron because of EPO administration. Oral supplements best on empty
Iron Supplementation stomach, separated from Ca and other cationic products. Better absorption if acidic (some suggest to
take with vit C). Constipation, darkens stools.
 Macrocyclic lactones. Act by binding to sterols (ergosterol - fungal form of cholesterol) in the cell
membrane and forming channels, allowing K and Mg to leak out.
Used parenterally/topically. Does not penetrate BBB well. Most toxic ABC used today. 80%
Amphotericin B -
Polyenes nephrotoxicity (azotemia, hypokalemia, hypomagnesemia). Acute Liv failure, arrhythmias. Less severe:
"amphoterrible"
N/V, chills, fever, HA.
Only used topically. Systemic fungal pathogens. Used to treat Candida. Minimal side effects. Poor
Nystatin
absorption by mucous membranes.
Inhibit synthesis of membrane sterols by inhibition incorporation or synthesis of ergosterol. Inhibit p450
3A4. May also inhibit fungal ETC.
Antifungals Clotrimazole Used only for topical treatment - poorly absorbed. Used for superficial candida. Diazole.
Azoles Water soluble, 90% bioavailable. Alters metabolism of orally administered hypoglycemic agents. 70%
eliminated unchanged. 1st drug of choice for fungal meningitis. Not active against aspergillus. Do not
Fluconazole
use with amphotericin B/nystatin - would antagonize its effects. Triazole. Used for serious candida
infections or after amphotericin treatment. Absorption decreased by cimetidine, may alter PT times.
Selectively inhibits fungal cell squalene epoxidase (the enzyme that converts squalene to squalene-
epoxide). This interferes with the biosynthesis of ergosterol (earlier step than azoles). Highly lipophilic
Allylamines Terbinafine
and keratophilic - used for superficial dermatophytic nail infections. Extensive Liv metabolism by
p450.
Kills trophozoites of E. histolytica. It is activated when reduced by ferrodoxins in protozoa/ bacteria
Amoebiasis Anti-parasitics Metronidazole (prodrug.) It causes damage to DNA of trophozoite by toxic O2 products generated from the drug by the
parasite. Disulfiram-like effect (take away from alcohol)
Prevents digestion of HgB, limiting AA supply to parasite. It inhibits the parasite's heme polymerase that
incorporates heme into an insoluble, non-toxic crystalline material. Concentrates in parasitised RBC.
Anti-Malarials Choloroquine
70% excreted unchanged. Also used in RA (higher doses!) - can result in permanent retinal
damage.

Nucleoside analogues --> prodrugs that are phosphorylated first by viral kinase (in infected host cell) and
then host cell kinases to form active triP metabolites --> compete with endogenous nucleoside triP and
competetively inhibit viral DNA polymerase. Inhibits 3 steps: Viral DNA polymerase utilization of
GTP. Terminates elongation of viral DNA strand. Inactivate DNA polymerase on DNA primer.
Selective for viral vs. host DNA replication. Resistance is due to thymidine kinase activity.
Herpes Virus Infections
Gets incorporated into viral DNA and cases chain termination. Resistance uncommon. All orally but
Acyclovir acyclovir is also iv/topical. Low bioavailability (22%). Least effective for VZV. Good safety record for
chicken pox in children.
Valacyclovir Rapidly converted to acyclovir by intestinal/hepatic enzymes. Better bioavailability (55%)
Famiciclovir Best bioavailability (80%)
NRTI (nucleoside reverse transcriptase inhibitors): converted to active triP, compete for incorporation
into viral DNA catalyzed by rT; then cause chain termination. Also inhibit host call DNA polymerase to
Anti-Virals varying degree (result in toxic effects). NNRTI (non-nucloside rT inhibitors): do not require
phosphorylation for activation. Bind directly to rT and disrupt the catalytic site. These two have
synergistic inhibition if given together. All orally, all cross BBB, KI excreted. Develop resistance.
HIV (reverse-transcriptase inhibitor)
Differ in purine/pyrimidine bases, therefore better in combo. Didanosine: purine base congener. Side
Didanosine
effects: peripheral neuropathy, pancreatitis.
Lamivudine Pyrimidine base congener, fewer side effects.
Pyrimidine base congener, given IV as well. Reduces utero transmission. Produces bone marrow
Zidovudine (AZT)
supression, anemia, neutropenia.
HIV (protease inhibitor) Indinavir Inhibits viral maturation. Metabolized by p450, inhibit p450 3A4. Best in combo (2 NRTIs).
Synthetic tricyclic amine compound. Prevents uncoating of influenza A particles after entering host cell.
Influenza A Amantadine Lipophilit --> crosses BBB (potential CNS side effects). Not extensively metabolized. Effective if given
prophylactically.
Hepatitis Lamivudine Inhibits replication of hepatitis B virus. Its replication is dependent on fT of an intermediate RNA.
 Precursor to testosterone (and estrogen.) Circulating levels decrease with age - considered anti-aging
Adrenal Cortex Hormone DHEA
hormone and inc NK cells. Improves mood. Melatonin stimulates its production/secretion.
Progesterone Hormone released by the corpus luteum, adrenals and placenta. Prepares the uterus for the ovum.
Injectable synthetic progesterone. Prevents ovulation. Injected every 3 months. Decreases bone and
Medroxyprogesterone
estrogen.
Progesterone Hormones - used in Spironolactone analog progestin (K+-sparing diuretic). Anti-mineralcorticoid activity (increases K, blocks
BIRTH CONTROL Drospirenone aldosterone). Therefore, decreases bloating and symptoms of water retention. Should not be used in
KI disease, hepatic dysfunction, hyperkalemia.
Norgestimate (oral)
Combined with ethinyl estradiol. Oral contraceptives, acne control.
Norelgestromin (patch)
Estradiol (E2) Strongest estrogen. 12x as potent as E1, 80x E3.
Estrone (E1) Increase in menopause. 16-OH estrone inc cancer risk. 2-OH estrone dec cancer risk.
Estrogens
Estriol (E3) Weakest estrogen but most abundant. Anti-breast cancer effects.
Conjugated estrogens Derived from urine of pregnant mare. Sodium salts of water-soluble estrogen sulfates.

Estrogen receptor agonist in CNS and GU. Fertility drug that induces ovulation in anovulatory
Clomiphene conditions. Increases LH/FSH --> ovulation. Ovarian hyperstimulation syndrome: ovarian elargement,
hepatic dysfunction, hypovolemic shock --> death. Visual spots/blurring. No drug interactions.

Endocrine Estrogen antagonist in breast tissue and CNS (used in Breast CA prevention). Estrogen agonist in
Anti-Estrogens endometrium, bone, lipids. Used in estrogen receptor positive breast CA. Inc. risk of hypercalcemia
Tamoxifen
when bone metastasis. Increase risk of endometrial CA, inc risk of DVT, other thrombo-embolytic
events. Inc risk of liver CA. Works synergistcally with melatonin. Quercitin works as well as tamoxifen.
Used to prevent postmenopausal bone loss. Estrogen agonist in bone (increase BMD) and on lipid
metabolism (decrease total and LDL chol levels, no effect on HDL or TG). Estrogen antagonist in uterine
Raloxifene
and breast tissues (may be used as a tamoxifen alternative.) As in other HRT, increases risk of DVT,
PE. Not to be used with HRT.
Synthetic T4. Many interactions. Lithium interferes with thyroid hormones, so do tricyclic anti-D,
Levothyroxine interferons. Functional hypothyroidism: interferes with conversion of T4 --> T3. This can happen with
Thyroid Hormones - Hypothyroidism propranolol, PTU, high soy diets.
(High TSH, low T4) Liothyronine Synthetic T3. Can cause thyroid storm.
Dessicated thyroid Animal thyroid gland, Natural ratio of T3 and T4. Caution: all of these drugs with cardiovascular disease.
Antagonists block throid peroxidase (catalyzes both the incorporation of iodine into the tyrosine residues
and the cloupling of the outer phenol ring to the inner)
Thyroid Hormones - Hyperthyroidism Propylthiouracil (PTU) Inhibits iodine and peroxidase from their normal interactions with thyroglobulin to form T4 and T3. PTU
(Low TSH, high T4) also interferes with the conversion of T4 to the more potent T3.
Methimazole Similar action to PTU. Both are very toxic, used just before surgery.
Radioiodine ablation therapy Hypothyroidism results.