P1 Top 200 Quiz 8 Chart - Lecture notes 12222 PDF

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Description

Generic Name (Formulations)

Brand Name

Drug Class

Estrogens, Conjugated

Premarin

Estrogen Derivative

(Injection solution reconstituted, tablet, vaginal cream)

FDA Approved Indication(s) All: ● Breast cancer, metastatic ● Hypoestrogenis m (female) ● Osteoporosis prevention (female) ● Prostate cancer, advanced ● Vasomotor symptoms associated with menopause ● Vulvar and vaginal atrophy associated with menopause Injection only: ● Abnormal uterine bleeding

MOA Estrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estradiol is the principle intracellular human estrogen and is more potent than estrone and estriol at the receptor level; it is the primary estrogen secreted prior to menopause. Following menopause, estrone and estrone sulfate are more highly produced. Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormone, and follicle-stimulating hormone through a negative feedback system; estrogen replacement reduces elevated levels of these hormones in postmenopausal women.

Major Contraindications* ● ● ●

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Undiagnosed abnormal genital bleeding DVT or PE (current or history of) Active or history of arterial thromboembolic disease (eg, stroke, MI) Breast cancer (except in appropriately selected patients being treated for metastatic disease) Estrogendependent tumor (known or suspected) Hepatic impairment or disease Known protein C, protein S, antithrombin deficiency or other known thrombophilic disorders Pregnancy

Black Box Warnings (BBW)↟

Major Adverse Events

Breast cancer

Headache, breast pain, abdominal pain

Endometrial cancer: Increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Cardiovascular disease: Estrogen-alone therapy should not be used for the prevention of cardiovascular disease. There are increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women (50-79 years of age). Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease. There is increased risks of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal

women (50-79 years of age). Dementia: Estrogen-alone therapy should not be used for the prevention of dementia. There is an increased risk of developing probable dementia in postmenopausal women 65 years of age or older. It is unknown whether this finding applies to younger postmenopausal women. Estrogen plus progestin therapy should not be used for the prevention of dementia. The WHIMS estrogen plus progestin ancillary study of the WHI reported an increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily conjugated estrogens (0.625 mg) combined with medroxyprogesteron e acetate (2.5 mg), relative to placebo. It is unknown whether this finding applies to younger postmenopausal women. Risk vs benefit: In the absence of

comparable data, these risks should be assumed to be similar for other doses of conjugated estrogens (with or without medroxyprogesteron e acetate) and other dosage forms of estrogens (with or without progestins). Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman. Ethinyl Estradiol; Etonogestrel (Vaginal ring)

NuvaRing

Estrogen and Progestin Combination, Contraceptive

Contraception

Combination hormonal contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary. The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal contraceptives produce

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Breast cancer or other estrogen- or progestin-sensitive cancer (current or a history of) Hepatic tumors (benign or malignant) or hepatic disease Pregnancy Undiagnosed abnormal uterine bleeding Concurrent use of hepatitis C drug combinations containing ombitasvir/paritapr evir/ritonavir, with or without dasabuvir. Use is also contraindicated in women at high risk of arterial or venous thrombotic diseases including:

Thrombosis, bloating, Cigarette smoke and serious weight changes cardiovascular events: Cigarette smoking increases the risk of serious cardiovascular events from combination hormonal contraceptive (CHC) use. This risk increases with age, particularly in women over 35 years of age, and with the number of cigarettes smoked. For this reason, CHCs, including ethinyl estradiol/etonogestre l, should not be used by women who are over 35 years of age and smoke.

Cerebrovascular disease; coronary artery disease; diabetes mellitus with vascular disease; DVT or PE (current or history of); headaches with focal neurological symptoms; migraine headaches with aura or migraine headaches if >35 years of age; hypertension (uncontrolled); thrombogenic valvular or rhythm diseases of the heart (eg, subacute bacterial endocarditis with valvular disease, atrial fibrillation); women >35 years of age who smoke; inherited or acquired hypercoagulopathi es.

alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility.

Ethinyl Estradiol; Levonorgestrel (Tablet)

Altavera, Aviane, Lutera, Marlissa, Orsythia, Portia

Contraceptive; Estrogen and Progestin Combination

Contraception, Emergency contraception

Combination hormonal contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary.

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Breast cancer or other estrogen- or progestindependent neoplasms (current or a history of), hepatic tumors or disease, pregnancy Hepatitis C drug combinations containing ombitasvir/paritapr evir/ritonavir, with or without dasabuvir Use is also

Cigarette smoke and serious cardiovascular events: Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptives use. This risk increases with age, particularly in women over 35 years of age, and with the number of cigarettes smoked.

Thrombosis, bloating, weight changes

Ethinyl Estradiol; Norethindrone (__Tablet_____, Therapy pack_____, ___chewable Tablet_____)

Estrostep Fe, Tilia Fe, TriLegest Fe, femhrt, Jevantique Lo, Jinteli, Junel 1.5/30, Lo Loestrin Fe, Microgestin 1.5/30, Nortrel 0.5/35

Estrogen and Progestin Combination, Contraceptive

All: Contraception Estrostep Fe, Tilia Fe, Tri-Legest Fe: Acne vulgaris femhrt, Jevantique Lo, Jinteli: Osteoporosis prevention (female), Vasomotor symptoms associated with menopause

The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility.

contraindicated in women at high risk of arterial or venous thrombotic diseases including: Cerebrovascular disease, coronary artery disease, diabetes mellitus with vascular disease, DVT or PE (current or history of), hypercoagulopathi es (inherited or acquired), headaches with focal neurological symptoms, hypertension (uncontrolled), migraine headaches if >35 years of age, thrombogenic valvular or rhythm diseases of the heart (eg, subacute bacterial endocarditis with valvular disease or atrial fibrillation), women >35 years of age who smoke

Combination oral contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing

Combination hormonal contraceptives: ● Breast cancer, or other estrogen- or progestin-sensitive cancer (current or a history of) ● Hepatic tumors (benign or malignant) or hepatic disease ● Pregnancy; undiagnosed

For this reason, combination oral contraceptives should not be used by women who are over 35 years of age and smoke.

Breast cancer Cigarette smoke and serious cardiovascular events: Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive use. This risk increases

Headache, abdominal pain, nausea

hormone by the anterior pituitary. ● The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal ● contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility. In postmenopausal women, exogenous estrogen is used to replace decreased endogenous production. The addition of progestin reduces the incidence of endometrial hyperplasia and risk of endometrial

abnormal uterine bleeding Concomitant use of hepatitis C drug combinations containing ombitasvir/paritapr evir/ritonavir, with or without dasabuvir Women at high risk of arterial or venous thrombotic diseases for example, women with: Cerebrovascular disease; coronary artery disease; diabetes mellitus with vascular disease; DVT or PE (current or history of); hypertension (uncontrolled); headaches with focal neurological symptoms; migraine headaches with aura or migraine headaches if >35 years; women >35 years who smoke; hypercoagulopathi es (inherited or acquired); thrombogenic valvular or thrombogenic rhythm diseases of the heart (eg, subacute bacterial endocarditis with valvular disease, atrial fibrillation)

Products used for postmenopausal

with age, particularly in women over 35 years of age, and with the number of cigarettes smoked. For this reason, combination oral contraceptives should not be used in women who are over 35 years and smoke. Endometrial cancer: There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Adequate diagnostic measures, including directed or random endometrial sampling when indicated, should be taken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal genital bleeding. Cardiovascular disease: Estrogen-alone therapy should not be used for the prevention of cardiovascular

cancer in women indications: with an intact uterus. ● Undiagnosed abnormal genital bleeding ● DVT or PE (current or history of) ● Active or history of arterial thromboembolic disease (eg, stroke, MI) ● Breast cancer (known, suspected or history of) ● Estrogendependent tumor (known or suspected) ● Hepatic impairment or disease ● Known protein C, protein S, antithrombin deficiency or other known thrombophilic disorders ● Pregnancy

disease. There are increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women (50-79 years of age). Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease. There is increased risks of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal women (50-79 years of age). Dementia: Estrogen-alone therapy should not be used for the prevention of dementia. There is an increased risk of developing probable dementia in postmenopausal women 65 years of age or older. It is unknown whether this finding applies to younger postmenopausal women. Estrogen plus progestin therapy should not be used for the prevention of dementia. The WHIMS estrogen plus progestin ancillary study of the WHI reported an increased risk of

developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily conjugated estrogens (0.625 mg) combined with medroxyprogesteron e acetate (2.5 mg), relative to placebo. It is unknown whether this finding applies to younger postmenopausal women. Risk vs benefit: In the absence of comparable data, these risks should be assumed to be similar for other doses of conjugated estrogens (with or without medroxyprogesteron e acetate) and other dosage forms of estrogens (with or without progestins). Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman. Ethinyl Estradiol; Norgestimate (Tablet)

Estarylla, Femynor, Mili, MonoNessa, Ortho TriCyclen, Previfem,

Estrogen and Progestin Combination, Contraceptive

Acne vulgaris Contraception

Combination hormonal contraceptives inhibit ovulation via a negative feedback

Breast cancer or other estrogen- or progestin-dependent neoplasms (current or a history of), hepatic tumors (benign or

Cigarette smoke and serious cardiovascular events: Cigarette smoking increases the risk of

Thrombosis, bloating, weight changes

Sprintec, TriNessa

Ezetimibe (Tablet)

Zetia

mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary. The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility. Antilipemic Agent, 2Azetidinone

Homozygous familial hypercholesterolemi

malignant) or hepatic disease, pregnancy, undiagnosed abnormal uterine bleeding; concomitant use of hepatitis C drug combinations containing ombitasvir/ritonavir, with or without dasabuvir. Use is also contraindicated in women at high risk of arterial or venous thrombotic diseases for example, women with: Cerebrovascular disease, coronary artery disease, diabetes mellitus with vascular disease, DVT or PE (current or history of), hypercoagulopathies (inherited or acquired), hypertension (uncontrolled), headaches with focal neurological symptoms, migraine headaches with aura or migraine headaches if >35 years of age, thrombogenic valvular or rhythm diseases of the heart (eg, subacute bacterial endocarditis with valvular disease or atrial fibrillation), women >35 years who smoke.

Inhibits absorption ● of cholesterol at the brush border of

Concomitant use with an HMG-CoA reductase inhibitor

serious cardiovascular events from combination oral contraceptive (COC) use. This risk increases with age, particularly in women older than 35 years, and with the number of cigarettes smoked. For this reason, COCs are contraindicated in women who are older than 35 years and smoke.

N/A

Diarrhea, upper respiratory tract infection, arthralgia

Famotidine

Pepcid

Histamine H2 Antagonist

(Intravenous solution, oral reconstituted suspension, tablet)

a, homozygous sitosterolemia, primary hyperlipidemia

the small intestine via the sterol transporter, Niemann-Pick C1Like1 (NPC1L1). This leads to a decreased delivery of cholesterol to the liver, reduction of ● hepatic cholesterol stores and an increased clearance of cholesterol from the blood; decreases total C, LDL-cholesterol (LDL-C), ApoB, and triglycerides (TG) while increasing HDL-cholesterol (HDL-C).

All: Duodenal ulcer, gastric ulcer, gastroesophageal reflux disease (GERD), pathological hypersecretory conditions

Competitive inhibition of histamine at H2 receptors of the gastric parietal cells, which inhibits gastric acid secretion

OTC only: Heartburn Fenofibrate (Capsule, DR capsule, tablet)

Antara; Fenoglide; Fibricor; Lipofen; Lofibra [DSC]; Tricor; Triglide; Trilipix

Fibric acid, antilipemic agent

Hypercholesterolemi a or mixed dyslipidemia, Hypertriglyceridemia

(statin) in patients with active hepatic disease or unexplained persistent elevations in serum transaminases Pregnancy and breast-feeding (when used concomitantly with a statin)

OTC labeling: When used for selfmedication (OTC), do not use if trouble or pain when swallowing food, vomiting with blood, or bloody or black stools; allergic to other acid reducers; renal impairment; co administration with other acid reducers.

● Fenofibric acid, an agonist for the nuclear transcription factor peroxisome proliferator-activated receptor-alpha (PPAR-alpha), downregulates ● apoprotein C-III (an inhibitor of lipoprotein lipase) and upregulates the synthesis of apolipoprotein A-I, ● fatty acid transport

Active liver disease, including primary biliary cirrhosis and unexplained, persistent liver function abnormality Severe renal impairment or endstage renal disease (ESRD), including those receiving dialysis Preexisting gallbladder

N/A

Agitation, headache, diarrhea

N/A

Increased serum transaminases, abnormal hepatic function tests, dyspepsia

protein, and ● lipoprotein lipase resulting in an increase in VLDL catabolism, fatty acid oxidation, and elimination of triglyceride-rich particles; as a result of a decrease in VLDL levels, total plasma triglycerides are reduced by 30% to 60%; modest increase in HDL occurs in some hypertriglyceridemic patients.

Ferrous Sulfate (Oral elixir, oral liquid, oral solution, oral syrup, IR tablet, DR tablet, ER tablet) Finasteride (Tablet)

disease Breastfeeding

Fer-In-Sol, FeroSul, FerrouSul, Slow Fe, Slow Iron

Iron salt

Iron-deficiency anemia

Replaces iron, found ● in hemoglobin, myoglobin, and other enzymes; allows the transportation of oxygen via hemoglobin

Hemochromatosis, hemolytic anemia

N/A

Constipation, darkening of stools, epigastric pain

Propecia, Proscar

5 AlphaReductase Inhibitor

Propecia: Androgenetic alopecia

Finasteride ● competitively inhibits type II 5-alpha ...