Premarin

— THERAPEUTIC CATEGORIES —
  • Bone disorders
  • Breast cancer
  • Menopause and HRT
  • Prostate and other male cancers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Premarin Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Conjugated estrogens 0.3mg, 0.45mg, 0.625mg, 0.9mg, 1.25mg; tabs.

    Pharmacological Class

    Estrogen.

    See Also

      How Supplied

      Tabs 0.3mg, 0.625mg, 1.25mg—100, 1000; 0.45mg, 0.9mg—100

      Manufacturer

      Pfizer Inc.

      Mechanism of Action

      Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these gonadotropins seen in postmenopausal women.

      Premarin Indications

      Indications

      Prevention of postmenopausal osteoporosis. 

      Premarin Dosage and Administration

      Adult

      Initially 0.3mg once daily; give continuously or cyclically (25 days on, 5 days off). Supplement diet with calcium 1.5g/day and Vit. D 400–800IU/day. Adjust as needed; periodically reassess need if dose is increased.

      Children

      Not applicable.

      Premarin Contraindications

      Contraindications

      Undiagnosed abnormal genital bleeding. Breast cancer (except in select patients being treated for metastatic disease) or other estrogen-dependent neoplasms. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders. Pregnancy.

      Premarin Boxed Warnings

      Boxed Warning

      Endometrial cancer. Breast cancer. Cardiovascular disorders. Probable dementia.

      Premarin Warnings/Precautions

      Warnings/Precautions

      Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Conditions aggravated by fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Nursing mothers: not recommended.

      Premarin Pharmacokinetics

      Distribution

      Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in the blood largely bound to SHBG and albumin.

      Metabolism

      Hepatic.

      Elimination

      Renal. Half-life: ~17 hours.

      Premarin Interactions

      Interactions

      May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

      Premarin Adverse Reactions

      Adverse Reactions

      Abdominal pain, asthenia, back pain, headache, flatulence, nausea, depression, insomnia, breast pain, endometrial hyperplasia, leucorrhea, vaginal hemorrhage, vaginitis; thromboembolism, neoplasms, anaphylaxis, angioedema (permanently discontinue if occurs).

      Premarin Clinical Trials

      See Literature

      Premarin Note

      Not Applicable

      Premarin Patient Counseling

      See Literature

      Premarin Generic Name & Formulations

      Legal Class

      Rx

      General Description

      Conjugated estrogens 0.3mg, 0.45mg, 0.625mg, 0.9mg, 1.25mg; tabs.

      Pharmacological Class

      Estrogen.

      See Also

        How Supplied

        Tabs 0.3mg, 0.625mg, 1.25mg—100, 1000; 0.45mg, 0.9mg—100

        Manufacturer

        Pfizer Inc.

        Mechanism of Action

        Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these gonadotropins seen in postmenopausal women.

        Premarin Indications

        Indications

        Treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease.

        Premarin Dosage and Administration

        Adult

        10mg 3 times daily for at least 3mos.

        Children

        Not applicable.

        Premarin Contraindications

        Contraindications

        Undiagnosed abnormal genital bleeding. Breast cancer (except in select patients being treated for metastatic disease) or other estrogen-dependent neoplasms. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders. Pregnancy.

        Premarin Boxed Warnings

        Boxed Warning

        Endometrial cancer. Breast cancer. Cardiovascular disorders. Probable dementia.

        Premarin Warnings/Precautions

        Warnings/Precautions

        Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Conditions aggravated by fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Nursing mothers: not recommended.

        Premarin Pharmacokinetics

        Distribution

        Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in the blood largely bound to SHBG and albumin.

        Metabolism

        Hepatic.

        Elimination

        Renal. Half-life: ~17 hours.

        Premarin Interactions

        Interactions

        May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

        Premarin Adverse Reactions

        Adverse Reactions

        Abdominal pain, asthenia, back pain, headache, flatulence, nausea, depression, insomnia, breast pain, endometrial hyperplasia, leucorrhea, vaginal hemorrhage, vaginitis; thromboembolism, neoplasms, anaphylaxis, angioedema (permanently discontinue if occurs).

        Premarin Clinical Trials

        See Literature

        Premarin Note

        Not Applicable

        Premarin Patient Counseling

        See Literature

        Premarin Generic Name & Formulations

        Legal Class

        Rx

        General Description

        Conjugated estrogens 0.3mg, 0.45mg, 0.625mg, 0.9mg, 1.25mg; tabs.

        Pharmacological Class

        Estrogen.

        See Also

        How Supplied

        Tabs 0.3mg, 0.625mg, 1.25mg—100, 1000; 0.45mg, 0.9mg—100; Cream—30g (w. applicator)

        Manufacturer

        Pfizer Inc.

        Mechanism of Action

        Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these gonadotropins seen in postmenopausal women.

        Premarin Indications

        Indications

        Moderate to severe vasomotor symptoms of menopause. Moderate to severe symptoms of vulvar and vaginal atrophy due to menopause. Hypoestrogenism due to hypogonadism, castration, or primary ovarian failure.

        Premarin Dosage and Administration

        Adult

        Menopausal symptoms, vaginal atrophy: initially 0.3mg once daily; give continuously or cyclically (25 days on, 5 days off). Female hypogonadism: 0.3–0.625mg once daily, given cyclically (3 weeks on, 1 week off). Female castration, ovarian failure: 1.25mg once daily, cyclically. For all: adjust as needed; periodically reassess need if dose is increased.

        Children

        Not applicable.

        Premarin Contraindications

        Contraindications

        Undiagnosed abnormal genital bleeding. Breast cancer (except in select patients being treated for metastatic disease) or other estrogen-dependent neoplasms. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders. Pregnancy.

        Premarin Boxed Warnings

        Boxed Warning

        Endometrial cancer. Breast cancer. Cardiovascular disorders. Probable dementia.

        Premarin Warnings/Precautions

        Warnings/Precautions

        Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Conditions aggravated by fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Nursing mothers: not recommended.

        Premarin Pharmacokinetics

        Distribution

        Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in the blood largely bound to SHBG and albumin.

        Metabolism

        Hepatic.

        Elimination

        Renal. Half-life: ~17 hours.

        Premarin Interactions

        Interactions

        May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

        Premarin Adverse Reactions

        Adverse Reactions

        Abdominal pain, asthenia, back pain, headache, flatulence, nausea, depression, insomnia, breast pain, endometrial hyperplasia, leucorrhea, vaginal hemorrhage, vaginitis; thromboembolism, neoplasms, anaphylaxis, angioedema (permanently discontinue if occurs).

        Premarin Clinical Trials

        See Literature

        Premarin Note

        Not Applicable

        Premarin Patient Counseling

        See Literature

        Premarin Generic Name & Formulations

        Legal Class

        Rx

        General Description

        Conjugated estrogens 0.3mg, 0.45mg, 0.625mg, 0.9mg, 1.25mg; tabs.

        Pharmacological Class

        Estrogen.

        See Also

          How Supplied

          Tabs 0.3mg, 0.625mg, 1.25mg—100, 1000; 0.45mg, 0.9mg—100

          Manufacturer

          Pfizer Inc.

          Mechanism of Action

          Endogenous estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these gonadotropins seen in postmenopausal women.

          Premarin Indications

          Indications

          Treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).

          Premarin Dosage and Administration

          Adult

          1.25mg—2.5mg 3 times daily.

          Children

          Not applicable.

          Premarin Contraindications

          Contraindications

          Undiagnosed abnormal genital bleeding. Breast cancer (except in select patients being treated for metastatic disease) or other estrogen-dependent neoplasms. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Hepatic impairment or disease. Protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders. Pregnancy.

          Premarin Boxed Warnings

          Boxed Warning

          Endometrial cancer. Breast cancer. Cardiovascular disorders. Probable dementia.

          Premarin Warnings/Precautions

          Warnings/Precautions

          Increased risk of endometrial carcinoma or hyperplasia in women with intact uterus (adding progestin is essential). Not for prevention of cardiovascular disease or dementia. Increased risk of cardiovascular events (eg, MI, stroke, VTE); discontinue if occurs. Manage risk factors for cardiovascular disease and venous thromboembolism appropriately. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of breast or ovarian cancer. Risk of probable dementia in women >65yrs of age. Gallbladder disease. Severe hypercalcemia in breast cancer or bone metastases. Visual abnormalities. Permanently discontinue if papilledema or retinal vascular lesions reveals on exam. Preexisting hypertriglyceridemia. History of cholestatic jaundice. Discontinue if pancreatitis, hypercalcemia, or recurrence of cholestatic jaundice occurs. Monitor thyroid function. Conditions aggravated by fluid retention. Hypoparathyroidism. Endometriosis. Hereditary angioedema. Asthma. Diabetes. Epilepsy. Migraine. Porphyria. SLE. Hepatic hemangiomas. Do initial complete physical and repeat annually (include Pap smear, mammogram, and BP). Reevaluate periodically. Nursing mothers: not recommended.

          Premarin Pharmacokinetics

          Distribution

          Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulate in the blood largely bound to SHBG and albumin.

          Metabolism

          Hepatic.

          Elimination

          Renal. Half-life: ~17 hours.

          Premarin Interactions

          Interactions

          May be potentiated by CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, grapefruit juice). May be antagonized by CYP3A4 inducers (eg, phenobarbital, carbamazepine, rifampin, St. John’s wort). Concomitant thyroid replacement; may need to increase thyroid dose. May interfere with lab tests (eg, thyroid, PT, coagulation factors, glucose tolerance, HDL/LDL, triglycerides, hormone concentrations, other binding or plasma proteins).

          Premarin Adverse Reactions

          Adverse Reactions

          Abdominal pain, asthenia, back pain, headache, flatulence, nausea, depression, insomnia, breast pain, endometrial hyperplasia, leucorrhea, vaginal hemorrhage, vaginitis; thromboembolism, neoplasms, anaphylaxis, angioedema (permanently discontinue if occurs).

          Premarin Clinical Trials

          See Literature

          Premarin Note

          Not Applicable

          Premarin Patient Counseling

          See Literature

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