DERS Drugs Flashcards
AlOH
Antacid
AE: Constipation
MgOH
Antacid
AE: Osmotic diarrhea
Calcium Carbonate
Antacid
AE: Belching, metabolic alkalosis (milk alkali)
Cimetidine
H2 Receptor Antagonist
Prototype with many AEs
AE: Gynecomastia, galactorrhea, male impotence, confusion, dizziness, headaches, CYP450 inhibition.
Inc serum concentration of Warfarin, Diazepam, Phenytoin.
Famotidine
H2 Receptor Antagonist
AE: B12 deficiency and myelosuppression with long term use.
Nizatidine
H2 Receptor Antagonist
AE: B12 deficiency and myelosuppression with long term use.
Famotidine
H2 Receptor Antagonist
AE: B12 deficiency and myelosuppression with long-term use.
Omeprazole
Proton Pump Inhibitors
AE: Diarrhea, abdominal pain, headache, Vit B12 deficiency, hypomagnesemia, osteopenia, inc risk of C Diff colitis, CYP450 inhibitor, CYP2C19 Inhibitor.
Inc serum concentration of Warfarin, Diazepam, Phenytoin, decrease effectiveness of Clopidogrel.
Esomeprazole
Proton Pump Inhibitors
AE: Diarrhea, abdominal pain, headache, Vit B12 deficiency, hypomagnesemia, osteopenia, inc risk of C Diff colitis, CYP2C19 Inhibitor.
Decrease effectiveness of Clopidogrel.
Lansoprazole
Proton Pump Inhibitors
AE: Diarrhea, abdominal pain, headache, Vit B12 deficiency, hypomagnesemia, osteopenia, inc risk of C Diff colitis, CYP2C19 Inhibitor.
Decrease effectiveness of Clopidogrel.
Pantoprazole
Proton Pump Inhibitors
AE: Diarrhea, abdominal pain, headache, Vit B12 deficiency, hypomagnesemia, osteopenia, inc risk of C Diff colitis.
Minimal inhibition of CYP2C19. Preferred in pt taking Clopidogrel.
Rabeprazole
Proton Pump Inhibitors
AE: Diarrhea, abdominal pain, headache, Vit B12 deficiency, hypomagnesemia, osteopenia, inc risk of C Diff colitis.
Minimal inhibition of CYP2C19. Preferred in pt taking Clopidogrel.
Misoprostol
PGE1 Analog
PUD treatment.
Bings EP3 receptor, decreases acid secretion, increases mucus and bicarb secretion.
Treat NSAID-induced ulcers.
Pregnancy: Widely used to treat post-partum hemorrhage. Abortifacient in combination with mifepristone. Can be used for cervical ripening but not FDA approved for this.
AE: Diarrhea, abdominal pain, cramps.
CI in pregnancy.
Sucralfate
PUD treatment.
Sucrose salt + Sulfated AlOH
Paste that binds to ulcers. Initial management of GERD in pregnancy.
Bismuth Subsalicylate
Suppress H Pylori, neutralize gastric acid, treat dyspepsia & acute diarrhea. Decrease fluid secretion in enteric tract. Anti-diarrheal and anti-acid.
AE: Harmless blackening of stool. Salicylate poisoning in combination with other salicylate products.
CI: Renal failure.
Erythromycin
Prokinetic
Antibiotic, agonist at motilin receptor.
Indication: Diabetic gastroparesis.
Use limited to short term.
Cisapride
Prokinetic
5HT4 agonist, 5HT3 antagonist. Direct muscle stimulant.
Used for GERD, gastroparesis.
No longer available due to causing ventricular arrhythmia.
Metoclopramide
Prokinetic
5HT4 agonist. Vagal + central 5HT3 antagonist. D2 antagonist in upper digestive tract.
Indication: Gastroparesis, Anti-emetic, GERD.
AE: Extrapyramidal syndrome, galactorrhea.
Scopolamine
Antimuscarinic antiemetic
Treat postop N/V and motion sickness.
Diphenhydramine
H1 Antagonist antiemetic
Treat postop N/V and motion sickness.
Meclizine
H1 Antagonist antiemetic
Treat postop N/V and motion sickness.
Cyclizine
H1 Antagonist antiemetic
Treat postop N/V and motion sickness.
Promethazine
Weak D2 antagonist at chemotaxic zone. Antiemetic.
Treat CINV
Droperidol
Central D2 antagonist. Anti-emetic.
AE: Extrapyramidal syndrome, QT prolongation.
Ondansetron
5-HT3 Antagonist (prototype). Anti-emetic
DOC for prophylaxis of acute CINV. Effective against hyperemesis gravidarum. Well tolerated.
Granisetron
5-HTS Antagonist. Anti-emetic
DOC for prophylaxis of acute CINV. Effective against hyperemesis gravidarum. Well tolerated.
Dexamethasone
Anti-emetic: Effective adjuvants against nausea in metastatic cancer. Suppress peritumoral inflammation & prostaglandin production.
Acute adrenal insufficiency: Dexamethasone given to treat if AAI is suspected but not yet diagnosed. Allows for immediate treatment that doesn’t impede diagnostic cortisol assays.
Methylprednisolone
Anti-emetic: Effective adjuvants against nausea in metastatic cancer. Suppress peritumoral inflammation & prostaglandin production.
Aprepitant
NK1 antagonist ORAL. Anti-emetic
Prophylaxis against delayed CINV.
Extensive CYP3A4 metabolism- affect metabolism of warfarin and OCP
Fosaprepitant
NK1 antagonist PARENTERAL. Anti-emetic.
Prophylaxis against delayed CINV.
Extensive CYP3A4 metabolism- affect metabolism of warfarin and OCP
Benzodiazepines
Lorazepam, Alprazolam, Diazepam. Anti-emetics.
Anti-anxiety adjuncts. Facilitate GABA action.
AE: CNS depression, addiction.
Dronabinol
Delta-9-tetrahydrocannabinol. Anti-emetic.
Stimulates CB1 receptors.
Prophylaxis in patients with chemo when other drugs ineffective.
AE: Palpitations, Hypotension, Tachycardia, Vasodilation, Conjunctival injection.
Methylcellulose
Bulk-forming laxative
Non-digestible colloid, absorbs water, forms a bulky jelly that distends colon and promotes peristalsis.
CI: Immobile pt or on long-term opioids.
Psyllium
Bulk-forming laxative
Non-digestible colloid, absorbs water, forms a bulky jelly that distends colon and promotes peristalsis.
Use: Constipation predominant IBS.
CI: Immobile pt or on long-term opioids.
Bran
Bulk-forming laxative
Non-digestible colloid, absorbs water, forms a bulky jelly that distends colon and promotes peristalsis.
CI: Immobile pt or on long-term opioids.
Bisacodyl
Stimulant laxative
Directly stimulates enteric NS to increase motility.
Minimal systemic absorption, safe for acute & long-term use.
Senna
Stimulant laxative
Directly stimulates enteric NS to increase motility.
Melanosis coli with chronic use- harmless brown pigmentation of colonic mucosa.
Castor oil
Stimulant laxative. Broken down into ricinoleic acid in SI.
Directly stimulates enteric NS to increase motility.
Required on a long-term basis for neurologically impaired and bed-bound patients.
CI: Pregnancy (stimulates contraction)
Docusate
Stool softener. Laxative
Surfactant that allows water and lipids to penetrate and soften stool.
Use: Constipation predominant IBS
Glycerin
Stool softener. Laxative
Surfactant that allows water and lipids to penetrate and soften stool.
Mineral Oil
Lubricant Laxative
Coats fecal material, preventing water reabsorption.
CI: Docusate will negate action of mineral oil by absorbing it into the stool (can’t coat stool)
Lactulose
Osmotic Laxative
AE: Flatus with abdominal cramping
Magnesium Salts
Osmotic Laxative
MgOH and MgSO4
CI: Prolonged use in pt with renal insufficiency can cause hypermagnesemia
Polyethylene Glycol
Osmotic Laxative
No systemic absorption, high osmotic pressure. No flatus or cramping.
Use: Complete bowel prep before GI endoscopy. Management of chronic constipation. Constipation predominant IBS.
Lubiprostone
Laxative
Stimulates Cl channels in SI
Use: Chronic constipation, IBS with predominant constipation.
AE: Diarrhea
CI: Children
Alvimopan
Laxative
Selective mu-opioid receptor antagonist
Do not cross BBB
Methylnaltrexone
Laxative
Selective mu-opioid receptor antagonist
Do not cross BBB
Loperamide
Antidiarrheal Opioid Agonist.
Presynaptic mu-opioid receptors inhibit ACh release and decrease gut peristalsis.
Doesn’t cross BBB- no analgesic properties or addiction potential.
Use: Diarrhea predominant IBS
CI: Children, severe colitis.
Diphenoxylate
Antidiarrheal Opioid Agonist
Presynaptic mu-opioid receptors inhibit ACh release and decrease gut peristalsis.
Can cross BBB- high prolonged doses can cause opioid dependence.
CI: Children, severe colitis.
Octreotide
Somatostatin Analog
Synthetic Octapeptide with longer half-life.
Antidiarrheal: Treat diarrhea due to neuroendocrine tumors, vagotomy, short bowel syndrome, dumping syndrome, AIDS.
AE: Reduce pancreatic exocrine function –> steatorrhea, fat-soluble vitamin deficiency. Reduce gallbladder contractility –> gallstones.
Alosetron
Afferent 5-HT3 antagonist. Anti-diarrheal.
Reduce noxious visceral sensations such as bloating, nausea, pain
Use: Diarrhea predominant IBS.
Hyoscyamine
Anticholinergic antidiarrheal
Anti-spasmodic affects on GI tract. Limited to short term relief of acute diarrhea due to unpleasant side effects from cholinergic blockade.
Used in Diarrhea predominant IBS
Dicyclomine
Anticholinergic antidiarrheal
Anti-spasmodic affects on GI tract. Limited to short term relief of acute diarrhea due to unpleasant side effects from cholinergic blockade.
Used in Diarrhea predominant IBS
Glycopyrrolate
Anticholinergic antidiarrheal
Anti-spasmodic affects on GI tract. Limited to short term relief of acute diarrhea due to unpleasant side effects from cholinergic blockade.
Used in Diarrhea predominant IBS
Methscopolamine
Anticholinergic antidiarrheal
Anti-spasmodic affects on GI tract. Limited to short term relief of acute diarrhea due to unpleasant side effects from cholinergic blockade.
Used in Diarrhea predominant IBS
Sulfasalazine
Aminosalicylate. IBD treatment.
Active ingredient: 5-ASA: Modulation of COX & LOX pathways. Inhibition of NF-kB. Inhibition of cellular immunity mechanism. ROS scavenging.
Maintain IBD remission, treat Mild IBD.
2ndary ingredient: Sulfapyridine
AE: Nausea, GI upset, Headache, Arthalgia, Myalgia, BM suppression, hypersensitivity reactions.
Balsalazide
Aminosalicylate. IBD treatment.
Active ingredient: 5-ASA: Modulation of COX & LOX pathways. Inhibition of NF-kB. Inhibition of cellular immunity mechanism. ROS scavenging.
Maintain IBD remission, treat Mild IBD.
2ndary ingredient: Inert carrier molecule
Mesalamine
Aminosalicylate. IBD treatment.
Active ingredient: 5-ASA: Modulation of COX & LOX pathways. Inhibition of NF-kB. Inhibition of cellular immunity mechanism. ROS scavenging.
Maintain IBD remission, treat Mild IBD.
Extended release/pH sensitive 5-ASA
Prednisone
Glucocorticoid
IBD Treatment: Induce remission of acute IBD exacerbation. Oral corticoid. Used for Moderate IBD.
Prednisolone
Glucocorticoid
IBD Treatment: Induce remission of acute IBD exacerbation. Oral corticoid. Used for Moderate IBD.
Budesonide
Glucocorticoid
IBD Treatment: Induce remission of acute IBD exacerbation. Oral corticoid that acts topically. Used for Mild IBD.
Mercaptopurine (6-MP)
Purine analog, Immunosuppressant.
IBD: Treat moderate IBD. Induction & maintenance of IBD remission. Steroid sparing effect.
AE: N/V, BM sup, Hepatotoxicity. Allopurinol increases serum concentration and thus AE.
Azathioprine
Purine analog, Immunosuppressant.
IBD: Treat moderate IBD. Induction & maintenance of IBD remission. Steroid sparing effect.
AE: N/V, BM sup, Hepatotoxicity. Allopurinol increases serum concentration and thus AE.
Methotrexate
Folate Analog, Immunosuppressant
IBD: Treat moderate IBD
Pregnancy: Used off-label for early abortion.
AE: BM sup, megaloblastic anemia (need folate supplementation), mucositis
Cyclosporine
Calcineurin inhibitor, Immunosuppressant
Forms complex with cyclophillin, inhibits calcineurin, reduces activation of NFAT.
IBD: Treat severe IBD.
AE: Nephrotoxic, neurotoxic, htn, gingival hyperplasia, hirsutism, hyperkalemia, GI disturbance, hyperglycemia, osteoporosis.
Infliximab
Anti-TNFa, Immunosuppressant
IBD: Treat moderate-severe IBD. Acute & Chronic treatment.
AE: BM suppression, hypersensitivity reactions. Inc risk of hepatic failure, CHF.
Adalimumab
Anti-TNFa, Immunosuppressant
IBD: Treat moderate-severe IBD. Acute & Chronic treatment.
AE: BM suppression, hypersensitivity reactions. Inc risk of hepatic failure, CHF.
Natalizumab
Anti-integrin, Immunosuppressant.
IBD: Treat severe IBD.
AE: Infusion reactions, immunosuppression, reactivation of human polyomavirus (JC virus) resulting in progressive multifocal leukoencephalopathy.
Pancrelipase
Pancreatic enzyme supplement. Treat pancreatic exocrine deficiency.
AE: Diarrhea, abdominal pain, renal stones, colonic strictures, hyperuricosuria.
Insulin Lispro
Rapid-acting Insulin
Given SC or IV. 15 minutes before a meal.
Insulin Aspart
Rapid-acting Insulin
Given SC or IV. 15 minutes before a meal.
Insulin Glulisine
Rapid-acting Insulin
Given SC or IV. 15 minutes before a meal.
Regular Insulin
Short-acting Insulin- Soluble crystalline zinc insulin
Given SC or IV. 30 minutes before a meal. Insulin of choice for emergencies.
Neutral protamine Hagedorn
aka Isophane Insulin. Intermediate-acting insulin.
Suspension of crystalline zinc insulin with protamine. Cloudy.
Given only SC. Used for basal control.
Insulin Glargine
Long-acting insulin
Used for basal control, given once daily.
Given SC.
Insulin Degludec
Long-acting insulin
Used for basal control, given once daily.
Given SC.
Insulin Detemir
Long-acting insulin
Used for basal control, given once daily.
Given SC.
Chlorpropamide
1st Gen Sulfonylurea
Binds SUR1 receptor, block ATP-sensitive K channel, depolarization, insulin release.
AE: Hypoglycemia, weight gain, hyperemic flush, SIADH (potentiates ADH).
CI: Elderly, hepatic or renal insufficiency.
Glyburide
2nd Gen Sulfonylurea
Binds SUR1 receptor, block ATP-sensitive K channel, depolarization, insulin release.
AE: Hypoglycemia (highest risk), weight gain, rapid tolerance (tachyphylaxis).
Glipizide
2nd Gen Sulfonylurea
Binds SUR1 receptor, block ATP-sensitive K channel, depolarization, insulin release.
AE: Hypoglycemia, weight gain, rapid tolerance (tachyphylaxis).
Glimepiride
2nd Gen Sulfonylurea
Binds SUR1 receptor, block ATP-sensitive K channel, depolarization, insulin release.
AE: Hypoglycemia (lowest risk), weight gain, rapid tolerance (tachyphylaxis).
Repaglinide
Meglitinide
Binds SUR1 receptor (different site from sulfonylurea), block ATP-sensitive K channel, depolarization, insulin release.
Less effective at reducing BGL & HbA1C than sulfonylurea.
Used in pt with sulfonylurea or sulfur allergy.
AE: Hypoglycemia (higher risk), weight gain.
Nateglinide
Meglitinide
Binds SUR1 receptor (different site from sulfonylurea), block ATP-sensitive K channel, depolarization, insulin release.
Less effective at reducing BGL & HbA1C than sulfonylurea.
Used in pt with sulfonylurea or sulfur allergy.
AE: Hypoglycemia, weight gain.
Metformin
Biguanide
Activates AMPK –> alters gene expression –> reduces gluconeogenesis, increases glucose utilization.
Equal to sulfonylurea in reducing BGL & HbA1c. Also reduces plasma triglycerides & body weight.
First-line drug against Type 2 DM.
AE: GI upset. B12 deficiency. Lactic acidosis.
CI: Renal disease, hepatic disease, hypoxia, alcoholism.
Pioglitazone
Thiazolidinedione (TZD)
Binds PPAR-y receptor –> alters gene expression –> increases glucose uptake.
Acts over weeks-months.
AE: Fluid retention, weight gain, edema. LFT needs to be monitored. Osteoporosis.
CI: Heart failure.
Rosiglitazone
Thiazolidinedione (TZD)
Binds PPAR-y receptor –> alters gene expression –> increases glucose uptake.
Acts over weeks-months.
AE: Fluid retention, weight gain, edema. LFT needs to be monitored. Osteoporosis.
CI: Heart failure.
Acarbose
a-glucosidase inhibitor
Inhibits upper intestinal carb absorption. Decreases postprandial hyperglycemia & hyperinsulinemia.
AE: Flatulence diarrhea abd pain, hypoglycemia (in combo with metformin), reversible hepatic enzyme elevation.
CI: IBS or any intestinal condition worsened by gas and distension.
Exenatide
GLP-1 Analog
Enhances glucose-dependent insulin secretion, suppresses glucagon, slows gastric emptying, decreases appetite.
AE: N/V, diarrhea, acute pancreatitis.
CI: Gastroparesis.
Sitagliptin
DPP-4 inhibitor
Increases GLP-1 and insulin levels.
AE: Predispose to URTI, hypersensitivity, pancreatitis.
Pramlintide
Injectable Amylin Analog
Inhibits food intake, gastric emptying, glucagon secretion.
AE: N/V, anorexia.
CI: Gastroparesis.
Colesevelam
Oral Bile Acid Sequestrant
Lowers LDL-C. Unknown mechanism for treating DM.
Hyperthyroidism: Reduce enterohepatic recycling of thyroid hormone.
Canagliflozin
Oral SGLT2 inhibitor.
Increases renal glucose excretion.
AE: Inc risk of UTI, volume depletion, hyperkalemia, hyperMg, hyperPO4, hypotension, increased creatinine.
Levothyroxine
Synthetic T4 Analog
Treat hypothyroidism. Decreased effectiveness in presence of CYP450 Inducer.
Propylthiouracil
Blocks Thyroid Peroxidase. Blocks peripheral deiodination of T4.
Preferred in severe hyperthyroid states or thyroid storm. Preferred in first trimester of pregnancy.
AE: Pruritic rash, agranulocytosis, severe hepatitis.
Methimazole
Blocks Thyroid Peroxidase.
DOC for Graves disease.
AE: Pruritic rash, agranulocytosis
CI: First trimester of pregnancy.
Amiodarone
Can cause hypo & hyperthyroidism.
Hypothyroidism- drug contains iodine, blocks TH synthesis. Usually in pt with autoimmune thyroiditis.
Hyperthyroidism Type 1: Inc T3, T4 synthesis from iodine. Usually in pt with pre-existing goiter
Type 2: Direct toxic effect of Amiodarone on Thyroid follicles causes excess T3/T4 release.
Hydrocortisone
Cortisol preparation
Short-acting, diffuses well across mucus membranes, some salt retaining effects
Fludrocortisone
Synthetic mineralocorticoid (aldosterone analog)
Increase expression of Na/K ATPase & ENaC.
Given in hypo-aldosteronism. Given in acute adrenal insufficiency when hydrocortisone dosage is reduced to below 50mg/day.
AE: Hypokalemia, metabolic alkalosis, Hypertension.
Betamethasone
Synthetic glucocorticoid
Reduced salt-retaining effects compared to hydrocortisone/cortisol.
Given IM to mother in pre-term labor to induce fetal lung surfactant production prior to birth.
Mifepristone
Glucocorticoid & Progesterone Receptor Antagonist
Use: Inoperable Cushing’s syndrome
Can be given with Misoprostol to induce early abortion.
Spironolactone
Aldosterone Antagonist
Use: Treat Hyperaldosteronism, Treat hirsutism in women (androgen antagonist effects), K-sparing diuretic.
AE: Hyperkalemia, cardiac arrhythmia, impotence, menstrual abnormalities, gynecomastia, GI upset, rashes, sedation, headaches.
Ketoconazole
Non-selective inhibitor of adrenal & gonadal steroid synthesis.
Use: DOC for Cushing’s syndrome. Prostate Cx.
AE: Hepatotoxicity, irregular menses, decreased libido, impotence, gynecomastia.
Aminoglutethimide
Inhibitor of all steroid hormone synthesis by blocking pregnenolone synthesis from cholesterol
Use: Cushing’s syndrome due to adrenal carcinoma
AE: Lethargy & skin rash
Metyrapone
Inhibitor of 11-hydroxylase: Inhibits cortisol synthesis
Use: Test adrenal function. DOC for Cushing’s in pregnancy.
AE: Hirsutism, salt/water retention.
Dinoprostone
PGE2 Analog
Ripens Cervix. Vaginal Insert & Cervical Gel.
Oxytocin
Induce Labor. DOC to treat post-partum hemorrhage.
Activates Gq receptor –> PLC –> SM contraction
also activates MAPK –> cPLA2 –> increased prostaglandin synthesis.
Given IV or IM.
AE: Excess uterine contractions. Vasopressin activation (SIADH).
Methylergonovine
Ergot Alkaloid
Partial agonist at a-adrenergic & some 5-HT receptors. Stimulates uterine contraction.
Use: treat post-partum bleeding.
AE: Htn, headache, seizures, N/V, chest pain, SOB, leg cramps.
CI: Angina pectoris, MI, pregnancy, hx of CVA/TIA/Htn.
Can be found in breast-milk so don’t use too long –> can give nursing infant ergot poisoning (gangrene)
Carbaprost Tromethamine
PGF2a analog. Given IM.
Helps treat post-partum bleeding.
Magnesium Sulfate
Uterine Relaxant
Inhibits myometrial action potential.
AE: Maternal flushing, nausea, headache, drowsiness, blurred vision. In both maternal & fetus: respiratory depression & cardiac arrest at doses that are way too high.
Given IV continuously.
Indomethacin
NSAID- Prostaglandin inhibitor. Uterine relaxant.
AE: Can cross placenta and cause oligohydraminos by decreasing fetal renal blood flow if used for more than 48 hours. Can cause premature ductus arteriosus closing if pregnancy over 32 weeks.
CI: Pregnancy after 32 weeks gestation.
Given orally or rectally.
Nifedipine
Ca Channel Blocker. Uterine Relaxant.
AE: Maternal tachycardia, palpitations, flushing, headaches, dizziness, nausea.
Given orally.
Atosiban
Competitive Antagonist at oxytocin receptor. Uterine relaxant.
Not available in USA.
Terbutaline
B2 agonist. Uterine relaxant.
AE: Palpitations, hyperglycemia, hypokalemia, hypotension. Serious: Pulm edema, cardiac insufficiency, arrhythmia, MI, maternal death.
Oral terbutaline no longer used.
IV terbutaline limited to 72 hours.
Ethinyl Estradiol
Estrogen component of oral contraceptive, transdermal patch, contraceptive ring.
Works through preventing ovulation.
Increases risk of thromboembolic events. Melasma.
Activated through enterohepatic circulation.
Rifampin can decrease levels of EE in the blood by reducing enterohepatic circulation.
Mestranol
Estrogen component of oral contraceptive.
Works through preventing ovulation.
Is converted to ethinyl estradiol in the liver.
Increases risk of thromboembolic events. Melasma.
Activated through enterohepatic circulation.
Rifampin can decrease levels of EE in the blood by reducing enterohepatic circulation.
Levonorgestrel
Progestin component of oral contraceptive. Main component in intrauterine system, Plan B or Next Choice emergency contraceptive.
Highest androgenic activity. Inc risk of Hirsutism & Acne.
Breakthrough bleeding. Insulin Resistance.
Works through thickening cervical mucus & preventing implantation.
Norgestrel
Progestin component of oral contraceptive. Can be given as progestin-only pill.
Highest androgenic activity. Inc risk of Hirsutism & Acne.
Breakthrough bleeding. Insulin Resistance.
Works through thickening cervical mucus & preventing implantation.
Drospirenone
Progestin component of oral contraceptive.
Anti-androgenic activity. Lower risk of Hirsutism & Acne.
Breakthrough bleeding. Insulin Resistance.
Works through thickening cervical mucus & preventing implantation.
Norgestimate
Progestin component of oral contraceptive.
Lowest androgenic activity. Lower risk of Hirsutism & Acne.
Breakthrough bleeding. Insulin Resistance.
Works through thickening cervical mucus & preventing implantation.
Desogestrel
Progestin component of oral contraceptive.
Lowest androgenic activity. Lower risk of Hirsutism & Acne.
Breakthrough bleeding. Insulin Resistance.
Works through thickening cervical mucus & preventing implantation.
Norethindrone
Progestin component of oral contraceptive. Can be given as progestin-only pill.
Lower androgenic activity (than levonorgestrel & norgestrel). Lower risk of Hirsutism & Acne.
Breakthrough bleeding. Insulin Resistance.
Works through thickening cervical mucus & preventing implantation.
DMPA
Depot-medroxyprogesterone acetate
Progestin. IM injection once every 3 months.
AE: Osteoporosis with long-term use.
Nonoxynol-9
Spermicidal surfactant
Used in diaphragms or cervical caps
Ulipristal acetate
Main ingredient of Ella emergency contraception
Selective progesterone modulator, mainly an antagonist. Inhibits or delays ovulation.
Tamoxifen
Selective Estrogen Receptor Modulator
Antagonist in breast, agonist elsewhere.
Prevent & treat hormone-responsive breast cx.
AE: Hot flashes, nausea, endometrial hyperplasia, thromboembolism.
Raloxifene
Selective Estrogen Receptor Modulator
Antagonist in breast & uterus, agonist in bone
Prevent hormone-responsive breast cx
Prevent & treat osteoporosis in postmenopausal women.
AE: Hot flashes, nausea, leg cramps, thromboembolism.
No risk of endometrial hyperplasia.
Clomiphene
Selective Estrogen Receptor Modulator
Antagonist in hypothalamus. Prevents feedback inhibition.
Treatment of infertility associated with anovulatory cycles.
AE: Hot flashes, N/V, weight gain, breast tenderness, visual disturbances, ovarian hyperstimulation, multiple pregnancies.
Fulvestrant
Selective Estrogen Receptor Degrader
Adjuvant treatment of hormone-receptor-positive metastatic breast cx that is resistant to first-line antiestrogen therapy.
AE: Hot flashes, arthralgia, myalgia.
Anastrozole
Aromatase inhibitor
Adjuvant Treatment of Estrogen-receptor positive breast cx.
AE: Hot flashes, nausea, fatigue, alopecia, dermatitis.
Flutamide
Androgen receptor antagonist
Treat prostate cx
AE: Gynecomastia, hot flashes, reversible hepatotoxicity
Finasteride
5a-reductase inhibitor (decreases conversion of testosterone to DHT)
Use: Treat BPH & male-pattern baldness
AE: Imptence, gynecomastia
