Drug Name Category Comments
Metformin Diabetes

Biguanide

Mechanism of action unknown. Their hypoglycemic activity does not depend on the presence of functional beta-cells.
Isophane (NPH) Insulin Diabetes

Insulin

Intermediate-acting

Cloudy solution. Protease reacts with the protamine to release the insulin. Later onset and longer duration.
Lente Insulin Diabetes

Insulin

Intermediate-acting

Cloudy solution. Insulin precipitated with Zinc in acetate buffer.
Ultralente Insulin Diabetes

Insulin

Long-acting

Cloudy solution. Poorly soluble complex of zinc and insulin. Due to poor manageability, used only with Type I Diabetics.
Bovine Insulin Diabetes

Insulin

Short-acting

Regular insulin, clear solution. Rapid onset and duration of a few hours. It is taken before meals for its immediate effects.
Humulin Diabetes

Insulin

Short-acting

Regular insulin, clear solution. Rapid onset and duration of a few hours. It is taken before meals for its immediate effects.
Porcine Insulin Diabetes

Insulin

Short-acting

Regular insulin, clear solution. Rapid onset and duration of a few hours. It is taken before meals for its immediate effects.
Acetohexamide Diabetes

Sulfonylurea

Relatively long-acting.

Adverse Effects: Disulfarim-like reaction.

Chlorpropamide Diabetes

Sulfonylurea

Very long-acting.

Adverse Effects: Disulfarim-like reaction.

Glipizide Diabetes

Sulfonylurea

"Second-generation" sulfonylurea. More potent ad fewer side-effects (no disulfarim reaction)

Adverse Effect: Hypoglycemia (over-extension of drug's principle action).

Glyburide Diabetes

Sulfonylurea

"Second-generation" sulfonylurea. More potent ad fewer side-effects (no disulfarim reaction). Short half-life, yet it has a long action of about 24 hrs.

Adverse Effect: Hypoglycemia (over-extension of drug's principle action). Contraindicated in hepatic or renal impairment.

Tolazamide Diabetes

Sulfonylurea

Relatively long-acting.

Adverse Effects: Disulfarim-like reaction.

Tolbutamide Diabetes

Sulfonylurea

Relatively long-acting.

Adverse Effects: Disulfarim-like reaction.

Demeclocycline Diuretic

ADH Antagonist

Indicated for hyper-ADH conditions, such as an ADH-secreting tumor.
Acetazolamide Diuretic

Carbonic-Anhydrase Inhibitor

Causes mild alkaline diuresis and metabolic acidosis. Used to increase urinary excretion of weak acids: counteract salicylate and phenobarbitol poisoning.

Also can be used to stimulate respiration in acute mountain sickness.

Methazolamide Diuretic

Carbonic-Anhydrase Inhibitor

Causes mild alkaline diuresis and metabolic acidosis. More lipid soluble, longer T1/2, less plasma-protein binding all favor entry into aqueous humor and CSF. Therefore used in prophylaxis of Glaucoma.
Amiloride Diuretic

K+-sparing Diuretic

It inhibits Na+/K+-ATPase in collecting ducts.
Triamterene Diuretic

K+-sparing Diuretic

It inhibits Na+/K+-ATPase in collecting ducts. Also has an active (hydroxylated) metabolite. Both are excreted in kidney. T1/2 = 3-5 hrs

Adverse Effect: Hyperkalemia, Metabolic Acidosis, renal stones

Spironolactone Diuretic

K+-sparing Diuretic

Aldosterone Antagonist

24-48 hours required to achieve maximal natriuresis.

Indicated for primary or secondary hyperaldosteronism.

Adverse Effects: Gynecomastia, hirsutism, post-menopausal bleeding

Glycerine Diuretic

Osmotic Diuretic

Mannitol Diuretic

Osmotic Diuretic

Indications: (1) Prophylaxis of acute renal failure, (2) cerebral edema, and (3) used with furosemide to prevent cisplatin toxicity.
Urea Diuretic

Osmotic Diuretic

Ethacrynic Acid Diuretic; Anti-CHF

Loop Diuretic; phenoxyacetic acid

Slow-onset, partially irreversible inhibition of channels.
Bumetanide Diuretic; Anti-CHF

Loop Diuretic; sulfonamide

Fast, reversible diuresis. Also inhibits Na3PO4 cotransporter.
Furosemide

(Lasix)

Diuretic; Anti-CHF

Loop Diuretic; sulfonamide

Fast, reversible diuresis. Also has a carbonic anhydrase inhibitory effect.
Torsemide Diuretic; Anti-CHF; Anti-HTN

Loop Diuretic; sulfonamide

Fast, reversible diuresis. Long-acting. Once daily dosage for HTN: good side-effect profile, no hypokalemia or dyslipidemia.
Benzoflumethiazide Diuretic; Anti-HTN

Thiazide Diuretic

Lipid soluble, more potent and longer acting. Extensively metabolized.
Chlorothiazide Diuretic; Anti-HTN

Thiazide Diuretic

Chlorthalidone Diuretic; Anti-HTN

Thiazide Diuretic

Used to treat HTN.
Hydrochlorothiazide Diuretic; Anti-HTN

Thiazide Diuretic

Water-soluble. Most popular thiazide diuretic for treating HTN. Cheap.
Hydroflumethiazide Diuretic; Anti-HTN

Thiazide Diuretic

Indapamide Diuretic; Anti-HTN

Thiazide Diuretic

Used to treat HTN. Both a thiazide diuretic and a direct vasodilator.
Carbidopa Dopamine Antagonist, Indirect

Dopamine-Decarboxylase Inhibitor

Prevents the formation of Dopamine in the periphery. Used in conjunction with L-DOPA in treatment of Parkinson's.
Diphenoxylate GI; Anti-diarrheal Related to opiates; suppress diarrhea in a manner similar to meperidine.
Loperamide GI; Anti-diarrheal Related to opiates; suppress diarrhea in a manner similar to meperidine.
Diphenoxylate GI; Anti-Diarrheal Opioid derivative that is specific to GI-tract, used to treat diarrhea.
Loperamide GI; Anti-Diarrheal Opioid derivative that is specific to GI-tract, used to treat diarrhea.
Hydroxyzine GI; Anti-Emetic Has several sub-cortical CNS effects, of which anti-emesis is the most prominent. Also anxiolytic, analgesic.
Attapulgite GI; Anti-emetic; adsorbent
Kaolin & Pectin GI; Anti-emetic; adsorbent
Viscous Lidocaine GI; Anti-emetic; adsorbent
Scopolamine GI; Anti-emetic; central

Anti-muscarinic

Skin-patch applied to hairless area behind ear; indicated for motion sickness.

Given as pre-anesthetic medication, to counteract vomiting and bradycardia.

Metoclopramide GI; Anti-emetic; central

Pro-kinetic

MECH: Blocks dopamine in brain (anti-emetic) and in GI tract (pro-kinetic).

Indications: (1) Diabetic gastroparesis, (2) nausea and vomiting with cancer chemotherapy, (3) anorexia nervosa.

Chenodiol GI; Gallstones Natural bile salt reduces cholesterol secretion and increases bile salts, thereby solubilizing the bile. Administered for 9-12 months.
Monoctanoin GI; Gallstones Used when pigment stones are refractory to treatment by chenodiol. Administered through a nasobiliary catheter; only effective when in direct contact with the stones.
Ursodiol GI; Gallstones Natural bile salt. Suppresses hepatic synthesis of cholesterol, and inhibits absorption of cholesterol. Months of therapy required.
Mesalamine GI; Inflammatory bowel disease Used in Ulcerative Colitis. Mechanism unknown; thought to locally inhibit cyclooxygenase in bowel mucosa. Adverse Effects = mild ones, except occasional hypersensitivity
Olsalazine sodium GI; Inflammatory bowel disease Used to maintain remission of Ulcerative Colitis.

Contraindicated in persons with salicylate hypersensitivity.

Sulfasalazine GI; Inflammatory bowel disease For mild to moderate Ulcerative Colitis. Active metabolite = 5-aminosalicylic acid.

Adverse Effects: Anorexia, headaches, rash, hemolytic anemia, impaired folate absorption, abnormalities of sperm.

Calcium polycarbophil GI; Laxative

Bulk-forming agent

Methylcellulose GI; Laxative

Bulk-forming agent

Plantago seed GI; Laxative

Bulk-forming agent

Bisacodyl GI; Laxative

Contact-stimulant

Synthetic agent. Treat constipation. Evacuate colon before surgery.

Frequently gives as suppository; may cause GI irritation if given PO.

Cascara Sagrada

(Castor oil)

GI; Laxative

Contact-stimulant

From cascara plant. They stimulate GI mucosa ------> increase motility and secretions.

It is not active unless hydrolyzed.

Phenolphthalein

(Ex-lax)

GI; Laxative

Contact-stimulant

Senna GI; Laxative

Contact-stimulant

From senna plant. They stimulate GI mucosa ------> increase motility and secretions.
Docusate Sodium

Docusate Potassium

Docusate Magnesium

GI; Laxative

Fecal softener

Ca+2 is thought to be the superior product. Administered at bedtime, and it takes 1-2 days for the softened feces to pass through. They have no cathartic effect (don't add bulk or water). They only soften the feces and are used for constipation.
Mineral Oil GI; Laxative

Lubricant laxative

Action 6-8 hours after administration. Indications: (1) Tearing of hemorrhoids or fissures, (2) temporary relief of constipation.

Adverse Effects: (1) bowel granulomas, (2) may cause aspiration pneumonia in infants, (3) leaks through the anal sphincter, (4) interferes with absorption of fat-soluble vitamins

Glycerine Suppositories GI; Laxative

Miscellaneous

Promote peristalsis by locally irritating mucous membranes of the rectum.
Lactulose Syrup GI; Laxative

Miscellaneous

It acidifies the colon, pulling NH3 into the bowel. Thus it is used to increase excretion of NH3 in patients with hepatic encephalopathy.
Magnesium Citrate

Magnesium Sulfate

Sodium Phosphate

Sodium Tartrate

GI; Laxative

Osmotic / Saline Agents

Fast and powerful cathartics, act in 2-6 hrs. Indicated for (1) before diagnostic tests, (2) flushing entire GI tract of poisons or parasites.
Aluminum Hydroxide

Al(OH)3

GI; Peptic Ulcer

Antacid

Local antacid; not absorbed. Weakest antacid. Has constipation as side-effect. Give it with Magnesium (as in Mylanta) to minimize side-effect.

It depletes phosphate. Indicated for hyperphosphatemia: Al+3 binds with excess PO4-3 in bowel and is excreted in feces.

CaCO3 GI; Peptic Ulcer

Antacid

Local antacid; not absorbed. Most neutralizing.

Adverse effects: (1) constipation. (2) Can lead to acid-rebound when therapy is stopped, as Ca+2 can stimulate gastric secretion. (3) Hypercalcemia and hyperphosphatemia can lead to renal stones with chronic use. (4) Milk-alkali syndrome.

Magnesium Hydroxide

Mg(OH)3

GI; Peptic Ulcer

Antacid

Most potent of antacids. Local antacid; not absorbed. Has diarrhea as a side-effect. Give it with Aluminum (as in Mylanta) to minimize side-effect.

May cause CNS depression in patients with renal insufficiency.

Sodium Bicarbonate

(NaHCO3)

(Alka-Seltzer)

GI; Peptic Ulcer

Antacid

Systemic antacid. It is absorbed, increasing Na+ and HCO3- load. It may lead to systemic metabolic alkalosis, and can cause acid-rebound. It creates an alkaline urine, facilitating clearance of drugs that are weak acids.
Carbenoxolone GI; Peptic Ulcer

Cytoprotective Agent

Lots of side effects; rarely used
Colloidal Bismuth Subcitrate

(De Nol)

GI; Peptic Ulcer

Cytoprotective Agent

Cytoprotective, plus antimicrobial activity against H. Pylori
Sucralfate GI; Peptic Ulcer

Cytoprotective Agent

Sucralfate = Sucrose + Sulfate. It forms a mucus barrier that absorbs pepsin; increase mucus secretion, HCO3- secretion, and PGE2 synthesis. It is not absorbed ------> minimal adverse effects. Aluminum accumulation in blood may occur in people with renal insufficiency. It is only effective at an acidic pH: don't give with antacids or H2-blockers.

Indicated for stress-induced ulcers

Bismuth Subsalicylate

(Pepto-Bismol)

GI; Peptic Ulcer

Cytoprotective Agent

Anti-emetic

Selectively binds to ulcer, providing coating and protection. Stimulate mucus production and PGE1 synthesis. Has anti-microbial activity; often used in combination therapy with antibiotics, to fight H. Pylori
Misoprostol

(PGE1)

GI; Peptic Ulcer

Cytoprotective Agent

Autocoid; PG Analog

Analog of PGE1. Inhibits gastric acid secretion; stimulates mucus secretion and cAMP production. Cytoprotection: increased mucous, increased HCO3-.

Particularly useful in NSAID-induced ulcers.

Omeprazole GI; Peptic Ulcer

Gastric-Pump Inhibitor

Mech: Irreversibly inhibits the H+-pump by forming a covalent bond with a Cys residue. It blocks H+ transport into secretory vesicles ------> prevent acid formation.

Maximally effective when taken before meals; it requires acid in order to function, thus higher doses are required in fasting people.

Indicated for Zollinger-Ellison syndrome, GERD, and non-bleeding PUD.

Cimetidine

(Tagamet)

GI; Peptic Ulcer

H2-Blocker

First and least potent drug. Gets into breast milk. T1/2 = 2 hrs. Known to be effective with duodenal ulcers, less effective with gastric ulcers.

Adverse Effects: (1) Inhibits Phase-I oxidation (Cyt-P450) ------> increased levels of warfarin, diazepam, phenytoin, theophylline. (2) Gynecomastia and Impotence, (3) mental confusion, (4) diarrhea

Famotidine

(Pepcid)

GI; Peptic Ulcer

H2-Blocker

Most potent, newest of H2-blockers. 20-50X more potent then cimetidine.

Adverse Effects: Muscle cramps, headache, constipation

Nizatidine

(Axid)

GI; Peptic Ulcer

H2-Blocker

Adverse Effects: Minor. Greater than 90% urinary excretion, more than the other drugs.
Ranitidine

(Zantac)

GI; Peptic Ulcer

H2-Blocker

Gets into breast milk.

Inhibits Phase-I oxidation (Cyt-P450)

Paramethasone Glucocorticoid

Intermediate-acting

No salt-retaining activity.
Triamcinolone Glucocorticoid

Intermediate-acting

No salt-retaining activity.
Betamethasone Glucocorticoid

Long-acting

Very potent. No salt-retaining activity.
Dexamethasone Glucocorticoid

Long-acting

Very potent. No salt-retaining activity.
Cortisone Glucocorticoid

Short-acting

Some salt-retaining activity (i.e. Aldosterone cross-reactivity)
Hydrocortisone (same as endogenous Cortisol) Glucocorticoid

Short-acting

Meprednisone Glucocorticoid

Short-acting

Some salt-retaining activity (i.e. Aldosterone cross-reactivity)
Methylprednisolone Glucocorticoid

Short-acting

Some salt-retaining activity (aldosterone cross-reactivity)
Prednisolone Glucocorticoid

Short-acting

Some salt-retaining activity (aldosterone cross-reactivity)
Prednisone Glucocorticoid

Short-acting

Some salt-retaining activity (aldosterone cross-reactivity)
Erythropoeiten Hemopoeitic; Anemia Useful for treating the hypoproliferative anemia caused by end-stage renal disease. Produced by recombinant DNA techniques.
Ferrous Fumarate Hemopoeitic; Anemia

Iron-Deficiency Anemia

Like Ferrous Sulfate
Ferrous Gluconate Hemopoeitic; Anemia

Iron-Deficiency Anemia

Like Ferrous Sulfate
Ferrous Sulfate Hemopoeitic; Anemia

Iron-Deficiency Anemia

Take them on an empty stomach. Enteric-coated iron preparations are not used, because we want to absorb the iron in the stomach and proximal duodenum. 200-400 mg of iron daily are required to treat iron deficiency.

Adverse Effects: Black stools, constipation, nausea, epigastric discomfort, abdominal cramps, diarrhea.

Iron Dextran Hemopoeitic; Anemia

Iron-Deficiency Anemia

Parenteral iron administration, IM or IV. IM can be painful.

Indications: Parenteral iron is given for severe iron deficiency, after a bowel resection or after Inflammatory Bowel Disease involving the proximal jejunum.

Adverse Effects: Headache, light-headedness. Nausea, vomiting, back pain, fever, arthralgia, urticaria, anaphylaxis (rare), flushing.

Cyanocobalamin

(Vitamin B12)

Hemopoeitic; Anemia

Megaloblastic Anemia

IM. The drug of choice in patients who are hypersensitive to the Hydroxycobalamin-Transcobalamin-II Complex. Therapy continues for life.
Folic Acid Hemopoeitic; Anemia

Megaloblastic Anemia

Folic acid will cure dietary folate deficiency. It will not cure folate deficiency due to anti-folate drugs (such as Trimethoprim). For that you use folinic acid.

No adverse effects.

Hydroxycobalamin

(Vitamin B12)

Hemopoeitic; Anemia

Megaloblastic Anemia

IM. Highly bound to plasma proteins and remains in circulation longer than cyanocobalamin. Therapy continues for life.
Dextran Hemopoeitic; Clotting

Anti-Coagulant

Used to prevent post-operative thrombosis. Long chain sugars physically interfere with platelet function and fibrin polymerization.
Heparin Hemopoeitic; Clotting

Anti-Coagulant

IV or SQ anti-coagulant. It potentiates Antithrombin-III and is monitored using the PTT. It has a fast onset of action and short duration of action.
Warfarin

(Coumadin)

Hemopoeitic; Clotting

Anti-Coagulant

Oral anti-coagulant. It is an analog of Vitamin-K and inhibits Vit-K-dependent factors. It is monitored using the PT. It has a slow onset of action and longer duration of action. It is eliminated by P450 metabolism and has lots of drug interactions.
Acetylsalicylic Acid

(Aspirin)

Hemopoeitic; Clotting

Platelet Inhibitor

Irreversibly inhibits COX. Can cause GI disturbances, unlike other NSAID's.

Has anti-platelet activity at low doses via its inhibition of TXA2. Has anti-inflammatory properties at high doses via its inhibition of PGE1.

Dipyridamole Hemopoeitic; Clotting

Platelet Inhibitor

Inhibits phosphodiesterase ------> potentiate prostacyclin, which is a cAMP dependent factor.

In combination with warfarin, it is effective in preventing arterial embolization in patients with prosthetic heart valves.

Sulfinpyrazone Hemopoeitic; Clotting

Platelet Inhibitor

Blocks the chemical mediators of platelet aggregation. However, it also prolongs platelet survival, limiting its use in this capacity.
Ticlopidine Hemopoeitic; Clotting

Platelet Inhibitor

Inhibits ADP-Induced platelet aggregation. Effective in preventing the recurrence of arterial thrombosis in patients with a history of MI, Transient Ischemic Attacks (TIA's), stroke, unstable angina pectoris.

Adverse Effects: GI Disturbances in 20% of patients, Hemorrhage in 5% of patients, Leukopenia in 1% of patients.

Timolol Hemopoeitic; Clotting

Platelet Inhibitor

beta-blocker has been approved for the prophylaxis and prevention of first MI. It is not known whether the beneficial effects are due to inhibited platelets, beta-blocking activity, or combination of both.
Aminocaproic Acid Hemopoeitic; Clotting

Prothrombogenic

They inhibit the conversion of plasminogen to plasmin. Used as adjunctive therapy in treating hemophilias.

Indicated for tPA, streptokinase toxicity.

Desmopressin Acetate Hemopoeitic; Clotting

Prothrombogenic

Useful as an adjunct in treatment of mild Hemophilia A. It potentiates the activity of Factor VIII.
Factor IX Hemopoeitic; Clotting

Prothrombogenic

Given to treat primary Hemophilia B (Factor IX Deficiency). Administration of the blood-derived factor carries a risk of getting viral infections such as Hepatitis-C.
Factor VIII Hemopoeitic; Clotting

Prothrombogenic

Given to treat primary Hemophilia A (Factor VIII Deficiency). Administration of the blood-derived factor carries a risk of getting viral infections such as Hepatitis-C.
Phytonadione

(Vitamin-K)

Hemopoeitic; Clotting

Prothrombogenic

Given for treatment of warfarin overdose, or whenever the effects of warfarin need to be reversed, such as in preparation for surgery. The effect is delayed by about 24 hours, the time required to synthesize new clotting factors.

Given prophylactically before gallbladder surgery.

Tranexamic Acid Hemopoeitic; Clotting

Prothrombogenic

Analog of aminocaproic acid. They inhibit the conversion of plasminogen to plasmin. Used as adjunctive therapy in treating hemophilias.

Indicated for tPA, streptokinase toxicity.

Anistreplase (APSAC) Hemopoeitic; Clotting

Thrombolytic Agent

The acylated form of the Streptokinase-Plasminogen Activated Complex (APSAC); no risk of systemic fibrinolysis. Longer lasting than the others. Infused IV for 3-5 minutes.
Streptokinase Hemopoeitic; Clotting

Thrombolytic Agent

From Streptococcus. Can cause systemic fibrinolysis and DIC. May see allergies, in patients who have anti-streptococcal antibodies. Given as IV loading dose, then 24-48 hours of infusion.
Tissue Plasminogen Activator (tPA) Hemopoeitic; Clotting

Thrombolytic Agent

Active only at the site of the clot; no risk of systemic fibrinolysis. Given as IV loading dose, then 2 hours of infusion. Particularly efficacious for post-MI treatment, and that is the only indication currently approved.

Adverse Effect: Higher risk for hemorrhagic stroke than with the other drugs.

Urokinase Hemopoeitic; Clotting

Thrombolytic Agent

Isolated from human kidney. Can cause systemic fibrinolysis and DIC. Given as IV loading dose, then 12 hours of infusion.
Finasteride Hormone

5alpha-Reductase Inhibitor

5alpha-Reductase Inhibitor. Inhibits conversion of testosterone to DHT. Useful in treatment of Benign Prostatic Hypertrophy.
Cosyntropin (Adrenal-Corticotropin Hormone (ACTH)) Hormone

ACTH

Used Diagnostically to evaluate adrenal insufficiency. If Cortisol does not respond to exogenous ACTH, then the problem is primary.
Metyrapone Hormone

Anti-Cortisol

Inhibits 11beta-Dehydroxylase, the final step in the formation of Cortisol, thus preventing formation of Cortisol.

Used diagnostically to confirm secondary adrenal insufficiency. Give Metyrapone, and look for increase in ACTH levels. No increase in ACTH indicates secondary adrenal insufficiency.

Clomiphene Hormone

Anti-Estrogen

It is used to stimulate ovulation, but the mechanism is not completely understood. Proposed mech: blocks estrogen effects on hypothalamus ------> promote GnRH ------> promotes ovulation.
Tamoxifen Hormone

Anti-Estrogen

Used to treat breast cancer. Antagonizes the action of estrogen on breast tissue.
Danazol Hormone

Anti-Gonadotropic

Has androgenic and progesterone activity, which suppresses the hypothalamic-pituitary axis. Indicated for treatment of endometriosis, fibrocystic disease of the breast, and to suppress ovarian steroid synthesis.
Spironolactone Hormone

Anti-Hirsutism

Aldosterone antagonist is used in treatment of Polycystic Ovary (Stein-Levanthal Syndrome), to prevent hirsutism. Mechanism of preventing hirsutism is unknown.
Iodide, I- Hormone

Anti-Thyroid

Exogenous I- temporarily (short-term) inhibits the proteolysis of thyroglobulin, preventing release of T4. Used to treat acute thyroid storm.

Also used before surgery, to make the Thyroid smaller and more firm.

Radio-Iodine, 131I Hormone

Anti-Thyroid

Used to treat hyperthyroidism. The 131I gets concentrated in the Thyroid, where it diffusely kills thyroid cells.

Ultimately it will lead to hypothyroidism, which can then be treated with T4.

Perchlorate (ClO4-) Hormone

Anti-Thyroid

Ionic Inhibitor

Inhibits uptake of iodide into the Thyroid.

In large doses, this drug causes aplastic anemia. Only use in small doses.

Thiocyanate (SCN-) Hormone

Anti-Thyroid

Ionic Inhibitor

Inhibits uptake of iodide into the Thyroid.
Carbimazole Hormone

Anti-Thyroid

Thionamide

Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed.
Methimazole Hormone

Anti-Thyroid

Thionamide

Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed.

This is the metabolic by-product of Carbimazole.

Propylthiouracil Hormone

Anti-Thyroid

Thionamide

Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed.

Also inhibits peripheral conversion of T4 to T3.

Calcimar Hormone

Calcium-regulation

Calcitonin obtained from salmon.
Calcitriol (Vitamin-D) Hormone

Calcium-regulation

Used to treat Rickets, Hypoparathyroidism, Osteomalacia.
Cibacalcin (Calcitonin) Hormone

Calcium-regulation

Used to help treat hyperparathyroidism, hypercalcemia, and Paget's Disease (characterized by increased skeletal remodeling).
Dihydrotachysterol Hormone

Calcium-regulation

Vitamin-D analogue. More effective than Vit-D because it bypasses renal mechanisms of metabolic control.
Parathyroid Hormone (PTH) Hormone

Calcium-regulation

Used diagnostically to diagnose pseudo hypothyroidism, a disorder characterized by insensitivity to PTH.
Corticotropin Releasing Hormone (CRH) Hormone

CRH

Estradiol, Estrone Hormone

Estrogen

Mixture of equine natural estrogens are used in post-menopausal hormone replacement therapy.

The equine estrogen has one extra double-bond and is hence called a "conjugated estrogen."

Urofollitropin Hormone

FSH

Natural FSH extracted from urine. Used to treat infertility.
Somatrem (Growth Hormone, GH, Somatomedin) Hormone

GH

Given as replacement therapy, only to children with open epiphyses. Contraindicated in people with closed epiphyses.

Biosynthetic, identical to endogenous GH

Sermatorelin (Growth-Hormone Releasing Hormone, GHRH) Hormone

GHRH

Given diagnostically, to diagnose primary (pituitary) or secondary (hypothalamic) GH deficiency (Dwarfism)
Gonadorelin (Gonadotropin-Releasing Hormone, GnRH) Hormone

GnRH

Very short half-life of 4 minutes. Can be given intranasally, IV, or SQ. Pulsatile administrated every 3½ or 4 hrs.

Used to treat hypogonadism in men or women, delayed puberty, and cryptorchidism.

Leuprolide Hormone

GnRH Analogue

Longer half-life of about 3 hrs. Can be given in pulsatile fashion, or continuously.

Continuous administration: used to slow down precocious puberty, or used to supress endogenous GnRH release in in-vitro fertilization. In continuous administration, it also initially induces a burst in FSH + LH activity, followed by suppression.

Indicated: Infertility, prostate cancer (with flutamide), uterine fibroids.

Nafarelin Hormone

GnRH Analogue

Longer half-life of about 3-hrs.
Human Chorionic Gonadotropin (hCG) Hormone

Menotropin

Obtained from urine of pregnant women. Closely related to LH. Given IM at mid-cycle (or whenever follicle is adequate developed) to mimic the luteal surge, to try to induce ovulation and treat infertility.
Human Menopausal Gonadotropins (hMG) Hormone

Menotropin

Partially degraded mixture of both FSH + LH. They still retain some FSH + LH activity. Administered IM to promote follicular growth, treat infertility.

Can be used to treat infertility in both men and women.

Desoxycorticosterone acetate Hormone

Mineralocorticoid

Fludrocortisone Hormone

Mineralocorticoid

Used to replace Aldosterone activity in cases of adrenal insufficiency.
Oxytocin Hormone

Oxytocin

Given IV to induce labor in mild eclampsia or incomplete abortion. Given IM to control post-partum bleeding. Given intranasally as needed to induce lactation.
Prolactin Hormone

Prolactin

No therapeutic use.
Bromocriptine Hormone

Prolactin Antagonist

Dopamine Agonist

Dopamine agonist ------> suppress Prolactin. Used to treat hyperprolactinemia.
Thyroxine (T4) Hormone

Thyroxine

Given orally to treat hypothyroidism. T4 is given -- not T3, which is too potent and has cardiotoxic side-effects.
Protirelin (Thyrotropin-Releasing Hormone, TRH) Hormone

TRH

Used diagnostically to distinguish between primary and secondary hypothyroidism.
Thyroid-Stimulating Hormone (TSH) Hormone

TSH

Used to promote uptake of radioactive 131I, to treat Thyroid carcinoma. Derived from bovine pituitaries.
Vasopressin (ADH) Hormone

Vasopressin

Used to treat Diabetes Insipidus. Administered IV, IM, intranasally.

V1 Receptors: Vascular vasoconstriction. V2 Receptors: Tubular reabsorption of water.

Desmopressin Hormone

Vasopressin Analogue

Synthetic Vasopressin analogue. Longer-acting then Vasopressin.
Adjuvants

Bacille Calmette-Guerin (BCG)

Immunomodulating Agent Attenuated M. Bovis strain can be employed as immunostimulant in cancer therapy. It activates macrophages, making them more apt at killing tumor cells.
Inosiplex Immunomodulating Agent Enhanced T-Cell and monocyte activities. Potentially useful in AIDS.
Thymosin Immunomodulating Agent 10 kDa protein. Thymic hormone that induces and stimulates the maturation of lymphoid stem-cells and pre-T-Cells into T-Cells. Indications: DiGeorge Syndrome, other conditions of T-Cell Deficiency.
Levamisole Immunomodulating Agent

Anti-Inflammatory; Anti-RA

It is an immunostimulatory drug that has paradoxical effect in treating RA. Treament has not yet been approved by FDA. Latency period of 3 - 4 months. May also be useful for Hodgkin's Disease.
Corticosteroids

(Prednisone, etc.)

Immunosuppressant Actions: (1) They inhibit Phospolipase-A2, (2) They inhibit the induction of COX-2

Indicated for organ transplants, auto-immune diseases.

Cyclophosphamide Immunosuppressant Indicated for bone marrow transplants (but it does not prevent GVHD), autoimmune disorders (PRCA, Wegener's Granulomatosis). Adverse Effect: Hemorrhagic cystitis, higher incidence of alopecia than other drugs.
Cyclosporin A Immunosuppressant From the fungus, Tolypocladium Inflatum. Binds to cyclophillins ------> inhibit IL-2 production in T-Cells ------> inhibit T-Cell differentiation and activation. Extensive Cyt-P450 metabolism.

Indications: Suppress organ rejection after transplantation, IDDM.

Adverse Effects: Viral infections, lymphoma. Nephrotoxicity, but it can be prevented with mannitol.

Methotrexate Immunosuppressant Inhibits dihydrofolate reductase. Well absorbed orally, or intrathecal. Polyglutamic-acid conjugates of methotrexate are retained intracellularly, where they have activity.

Indications: GVHD, psoriasis.

Adverse Effects: Oral, gastric ulcerations, and liver cirrhosis with long-term use. High dose methotrexate may be followed by high-dose folinic acid in order to "rescue" the anti-folate effects of the drug.

Tacrolimus (FK-506) Immunosuppressant

Anti-Bacterial; Macrolide

Macrolide antibiotic of fungal origin, similar in use to Cyclosporin. Used in situations where Cyclosporin is ineffective, toxic, or cannot otherwise be used.
Anti-Lymphocyte Globulin Immunosuppressant

Antibody

It activates complement-mediated destruction of lymphocytes ------> decreased cellular immunity. There is little effect on humoral immunity. Indications: Organ transplantations, GVHD.

Adverse Effects: Pain, erythema, possibly lymphoma at site of injection. Anaphylactic shock, serum sickness.

Anti-T-Cell Antibody OKT3 Immunosuppressant

Antibody

Mouse monoclonal antibody against the CD3 T-Cell Receptor.It inhibits the interaction between antigen-presenting cells and T-Cells.

Indications: Kidney transplantation.

Anti-Thymocyte Globulin Immunosuppressant

Antibody

Indications: Idiopathic aplastic anemia, or to counter the auto-immune effects of gamma-Interferon, secondary to hemopoeitic suppression.
Rh0(D) Globulin

(Rhogam)

Immunosuppressant

Antibody

For the primary prevention of Erythroblastosis Fetalis (hemolytic anemia of newborn). It is given to Rh- mothers, 72 hours after first childbirth of an Rh+ fetus, to prevent formation of anti-Rh antibodies in the mother.
Azathioprine Immunosuppressant

Chemotherapy; Miscellaneous

Pro-drug, it is converted by glutathione S-transferase to 6-Mercaptopurine, active form of drug. It is toxic to proliferating T-Cells and B-Cells, after antigen exposure. Allopurinol, renal disease raise its blood levels.

Indications: kidney transplants, autoimmune diseases (glomerulonephritis, hemolytic anemia).

Adverse Effects: Nausea, vomiting, diarrhea. Bone marrow suppression. Fever, skin rashes. Liver dysfunction and jaundice, ocassionally.

Bupivacaine Local Anesthetic; Amide Used for infiltration anesthesia, peripheral nerve block, epidural block.
Lidocaine

(Xylocaine)

Local Anesthetic; Amide Anti-Arrhythmic: Administered IV to avoid first-pass effect. Indications: Ventricular Arrhythmias. (1) reentry dysrhythmias. Reduces action potential duration and shortens refractory period in purkinje fibers ------> improve slow conduction. (2) Suppress ectopic pacemakers. (3) Early onset arrhythmias post-MI.
Mepivacaine Local Anesthetic; Amide Used for infiltration anesthesia, peripheral nerve block, epidural block.
Benzocaine Local Anesthetic; Ester Effective as topical agent; it penetrates mucous membranes
Chloroprocaine Local Anesthetic; Ester
Cocaine Local Anesthetic; Ester Effective as topical agent; it penetrates mucous membranes
Procaine Local Anesthetic; Ester Close to ideal as a local anesthetic. Used only for infiltration anesthesia or as spinal block.
Tetracaine Local Anesthetic; Ester Close to ideal as a local anesthetic.
Atracurium Muscle-Relaxant; Competitive
Doxacurium Muscle-Relaxant; Competitive
Gallamine Muscle-Relaxant; Competitive
Metocurine Muscle-Relaxant; Competitive
Mivacurium Muscle-Relaxant; Competitive
Pancuronium Muscle-Relaxant; Competitive
Pipecuronium Muscle-Relaxant; Competitive
Rocuronium Muscle-Relaxant; Competitive
Tubocurarine Muscle-Relaxant; Competitive Used in Multiple Sclerosis. Acidosis increases its potency; alkalosis decreases its potency.
Vecuronium Muscle-Relaxant; Competitive
Decamethonium Muscle-Relaxant; Depolarizing
Succinylcholine Muscle-Relaxant; Depolarizing Used in electroconvulsive therapy, ETC.
2-PAM

(Pralidoxime)

Toxicity Organophosphate poisoning: Only effective within the first few minutes of exposure. It is a strong nucleophile that can bind with the organophosphate, releasing it from cholinesterase, before the bond has aged.
4-methylpyrazole Toxicity A specific inhibitor of alcohol dehydrogenase that may be used instead of ethanol, for methanol and ethylene glycol poisoning.
Aminocaproic Acid Toxicity They inhibit the conversion of plasminogen to plasmin. Used as adjunctive therapy in treating hemophilias.

Indicated for tPA, streptokinase toxicity.

Atropine Toxicity Treatment of choice after the bond has aged and become irreversible, in organophosphate poisoning. First-line treatment for carbamate poisoning.
Cyanocobalamin

(Vitamin B12)

Toxicity Cyanide Toxicity: Co2 EDTA + Hydroxycobalamin takes up free cyanide, neutralizing it and forming cyanocobalamin (Vit B12).
Deferoxamine (Desferal) Toxicity IM or IV to chelate iron in blood, for iron toxicity.
Digoxin-specific antibody fragments. Toxicity Indicated for Digitalis toxicity.
Ethanol Toxicity It is given to displace the substrates and prevent their metabolism, in methanol and ethylene glycol poisoning. Prevent methanol from going to formic acid, and prevent ethylene glycol from going to oxalic acid.
Factor IX Toxicity Given for treatment of warfarin overdose, whenever immediate coagulation needs to take effect.
Factor IX Toxicity Used for immediate coagulation, in the event of warfarin toxicity.
Fluazenil Toxicity Indicated for Benzodiazepine toxicity.
Methylene Blue Toxicity Indicated for treatment of methemoglobinemia, such as that due to nitrite poisoning. Methylene Blue speeds the conversion of methemoglobin back to hemoglobin.
N-Acetylcysteine Toxicity Indicated for Acetominophen toxicity. It provides reduced sulfhydryl groups and restores glutathione to its reduced form.
Nalorphine Toxicity Indicated for opioid overdose, alternative to naloxone.
Naloxone Toxicity Opioid antagonist, indicated for acute opioid toxicity.
Nitrite Toxicity It causes methemoglobinemia which can then bind up all of the extra cyanide, driving it away from the cytochrome oxidase. For cyanide poisoning.
Phytonadione

(Vitamin-K)

Toxicity Given for treatment of warfarin overdose, or whenever the effects of warfarin need to be reversed, such as in preparation for surgery. The effect is delayed by about 24 hours, the time required to synthesize new clotting factors.

Given prophylactically before gallbladder surgery.

Phytonadione (Vitamin-K) Toxicity Given to reverse the effects of warfarin toxicity, but it takes 24 hours to take effect.
Protamine Sulfate Toxicity Given IV for treatment of heparin overdose. It is a basic peptide that binds to heparin. Must dose it carefully, as protamine sulfate is itself an anti-coagulant!
Prussian Blue Toxicity Thallium poisoning: It interrupts the enterohepatic circulation of Thallium, enhancing its excretion.
Pyridoxine (Vit B6) Toxicity Can reverse convulsions and peripheral neuritis associated with Isoniazid toxicity.
Sodium Bicarbonate

(NaHCO3)

Toxicity Generally promotes the excretion of acidic drugs. Indicates for treatment of tricyclic-antidepressant (TCA) induced arrhythmias.
Thiosulfate Toxicity Given to promote the formation of thiocyanate and its subsequent excretion, in cyanide poisoning.
Tranexamic Acid Toxicity Analog of aminocaproic acid. They inhibit the conversion of plasminogen to plasmin. Used as adjunctive therapy in treating hemophilias.

Indicated for tPA, streptokinase toxicity.

D-Penicillamine Toxicity

Metal Chelator

It chelates copper, mercury, zinc, lead.

Indicated for Wilson's Disease. Used as adjunct in lead, mercury, gold, arsenic poisoning. Indicated for gold salt toxicity. Indicated for Cystinuria: Forms a soluble penicillamine-cysteine complex, promoting the excretion of cysteine.

Serious adverse effects: Leukopenia, thrombocytopenia, aplastic anemia.

Dimercaprol

(British Anti-Lewisite, BAL)

Toxicity

Metal Chelator

Administered in oil by deep IM injection. Fast-acting and short half-life. Enters tissues more readily than does EDTA.

Forms stable complexes with mercury, arsenic, gold. It can free the sulfahydral compounds bound by the metals, but it is better at primary prevention. Adverse Effects: It can cause transient hypertension.

Used in combination with CaNa2 EDTA for lead poisoning, particularly when there are signs of Lead Encephalopathy.

Edetate Calcium Disodium

(CaNa2 EDTA)

Toxicity

Metal Chelator

Poor oral absorption. Usually administered IV or IM. Half-life 20 - 60 minutes. Urinary excretion. Water soluble; does not easily enter tissues or get into cells.

Indications: Primarily used for lead poisoning. Not effective against mercury, arsenic, most other metals.

Succimer Toxicity

Metal Chelator

New drug that can be given PO. Both urinary and biliary excretion, with enterohepatic circulation.

Chemically similar to Dimercaprol.

Indications: Severe Lead Poisoning: Used to treat children with lead poisoning above 45 µg / dL. It does not metabolize essential minerals like zinc, copper, iron, making it more attractive. Has been shown in labs to chelate arsenic, cadmium, mercury.


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Copyright 1999, Scott Goodman, all rights reserved