Conjugated oestrogens + Medroxyprogesterone


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Menopausal hormone replacement therapy Continuous combined therapy: Each tab contains conjugated oestrogens (mg)/medroxyprogesterone (mg): 0.3/1.5, 0.45/1.5, 0.625/5: 1 tab/day without interruption. Continuous sequential therapy: Each tab contains conjugated oestrogens 0.625 mg and medroxyprogesterone 10 mg: 1 tab/day from pack, as directed. Moderate to severe menopausal vasomotor symptoms; Moderate to severe menopausal atrophic vaginitis Continuous combined therapy: Each tab contains conjugated oestrogens (mg)/medroxyprogesterone (mg): 0.3/1.5, 0.45/1.5, 0.625/2.5, 0.625/5: 1 tab/day without interruption. Continuous sequential therapy: Each tab contains conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg: 1 tab/day from pack, as directed. Prophylaxis of postmenopausal osteoporosis Continuous combined therapy: Each tab contains conjugated oestrogens (mg)/medroxyprogesterone (mg): 0.3/1.5, 0.45/1.5, 0.625/2.5, 0.625/5: 1 tab/day without interruption. Continuous sequential therapy: Each tab contains conjugated oestrogens (mg)/medroxyprogesterone (mg): 0.625/5, 0.625/10: 1 tab/day from pack, as directed.
Dosage Details
Oral
Menopausal hormone replacement therapy
Adult: Available preparations:
Continuous combined therapy
Conjugated oestrogens 0.3 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.45 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab 
1 tab once daily without interruption.

Continuous sequential therapy Conjugated oestrogens 0.625 mg and medroxyprogesterone
10 mg tab 1 tab once daily from pack, as directed.

Oral
Menopausal vasomotor symptoms
Adult: Available preparations:
Continuous combined therapy
Conjugated oestrogens 0.3 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.45 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 2.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab
For moderate to severe cases: 1 tab once daily without interruption.

Continuous sequential therapy
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab
For moderate to severe cases: 1 tab once daily from pack, as directed.

Oral
Menopausal atrophic vaginitis
Adult: Available preparations:
Continuous combined therapy
Conjugated oestrogens 0.3 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.45 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 2.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab
For moderate to severe cases: 1 tab once daily without interruption.

Continuous sequential therapy
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab
For moderate to severe cases: 1 tab once daily from pack, as directed.

Oral
Prophylaxis of postmenopausal osteoporosis
Adult: Available preparations:
Continuous combined therapy
Conjugated oestrogens 0.3 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.45 mg and medroxyprogesterone 1.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 2.5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab
1 tab once daily without interruption.

Continuous sequential therapy
Conjugated oestrogens 0.625 mg and medroxyprogesterone 5 mg tab
Conjugated oestrogens 0.625 mg and medroxyprogesterone 10 mg tab
1 tab once daily from pack, as directed.
Hepatic Impairment
Contraindicated.
Contraindications
Hypersensitivity to conjugated oestrogens or medroxyprogesterone. History, suspected or current breast cancer, oestrogen-dependent tumour (e.g. endometrial cancer) and thromboembolic disease (e.g. DVT, pulmonary embolism, stroke, MI). Undiagnosed genital bleeding, untreated endometrial hyperplasia, severe uncontrolled hypertension, thrombophilic disorders (e.g. protein C or S and antithrombin deficiency). Hepatic impairment. Pregnancy and lactation.
Special Precautions
Patient with history of endometrial hyperplasia, risk factors for CV disorders (e.g. family history, obesity, hypercholesterolaemia, diabetes mellitus, hypertension, SLE), oestrogen-dependent tumour; hypertriglyceridaemia, hypoparathyroidism, otosclerosis, migraine, epilepsy, asthma, cholelithiasis, leiomyoma or endometriosis, bone cancer, porphyria, cardiac impairment; to undergo surgery. Renal impairment.
Adverse Reactions
Significant: Increased risk of breast, endometrial and ovarian cancers, CV disorders (e.g. DVT, pulmonary embolism, stroke, MI), dementia, gallbladder disease; hypersensitivity reactions, retinal vascular thrombosis (manifested by partial or complete loss of vision, diplopia, proptosis, migraine), hypertension.
Cardiac disorders: Palpitation, chest pain.
Gastrointestinal disorders: Nausea, diarrhoea, dyspepsia, eructation, flatulence, abdominal pain.
General disorders and administration site conditions: Asthenia, back or pelvic pain.
Infections and infestations: Flu syndrome, moniliasis.
Investigations: Increased triglycerides, decreased glucose tolerance.
Metabolism and nutrition disorders: Weight gain/loss, increased appetite, oedema.
Musculoskeletal and connective tissue disorders: Leg cramp, arthralgia, hypertonia.
Nervous system disorders: Headache, migraine, dizziness.
Psychiatric disorders: Depression, emotional lability, nervousness, insomnia.
Renal and urinary disorder: Urinary incontinence.
Reproductive system and breast disorders: Breast pain, tenderness, enlargement or discharge; cervix disorder, menstrual disorder, metrorrhagia, menorrhagia, dysmenorrhoea, breakthrough bleeding or spotting, leucorrhoea, vaginitis.
Skin and subcutaneous tissue disorders: Acne, dry skin, diaphoresis, rash, pruritus.
Vascular disorders: Vasodilation.
Potentially Fatal: Anaphylaxis.
MonitoringParameters
Assess personal and family medical history prior to start of treatment and at regular intervals thereafter. Include blood pressure, breast examinations (e.g. mammography) and Papanicolaou smear. Monitor for signs and symptoms of breast, endometrial and ovarian cancers and CV disorders. Periodically evaluate the need to continue treatment.
Overdosage
Symptoms: Nausea, vomiting, abdominal pain, drowsiness, fatigue, breast tenderness and withdrawal bleeding. Management: Symptomatic treatment.
Drug Interactions
Decreased effect with CYP enzyme system inducers (e.g. carbamazepine, phenobarbital, rifampicin). Increased adverse reactions with CYP enzyme system inhibitors (e.g. erythromycin, ketoconazole, ritonavir). May decrease effect of metyrapone. Conjugated oestrogens: Decrease the effect of thyroid hormone replacement therapy. Medroxyprogesterone: Decreased exposure with aminoglutethimide.
Food Interaction
Decreased effect with St. John’s wort. Increased adverse reactions with grapefruit juice.
Lab Interference
Decreased prothrombin time, partial thromboplastin time, platelet aggregation time. Increased platelet count. Increases thyroid-binding globulin, corticosteroid binding globulin and sex hormone-binding globulin.
Action
Description: Conjugated oestrogens is a mixture of synthetic sex hormones including estrone sulfate, equilin sulfate, 17α-estradiol, 17α-dihydroequilin and 17β-dihydroequilin. During menopause, these hormones substitutes for oestrogen production and alleviates its symptoms. These hormones also prevent bone loss following menopause or ovariectomy. Medroxyprogesterone reduces the oestrogen-induced risk of endometrial hyperplasia in non-hysterectomised women.
Pharmacokinetics:
Absorption: Conjugated oestrogens: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 7 hours (estrone). Medroxyprogesterone: Well absorbed from the gastrointestinal tract. Bioavailability: 0.6-10%. Time to peak plasma concentration: 2-4 hours.
Distribution: Conjugated oestrogens: Widely distributed. Mainly bound to sex hormone binding globulin and albumin. Medroxyprogesterone: Enters breast milk. Plasma protein binding: Approx 90%, mainly to albumin.
Metabolism: Conjugated oestrogens: Estradiol is metabolised in the liver by CYP enzyme system into estrone and estriol; estrone into estradiol and estriol; estriol into estradiol. Undergoes enterohepatic recycling via sulfate and glucuronide conjugation. Medroxyprogesterone: Extensively metabolised in the liver via hydroxylation and conjugation.
Excretion: Conjugated oestrogens: Via urine (mainly as estriol; as estradiol, estrone and conjugates). Elimination half-life: Approx 27 hours (estrone). Medroxyprogesterone: Via urine. Elimination half-life: Approx 16-30 hours.
Storage
Store between 20-25°C.
ATC Classification
G03FB06 - medroxyprogesterone and estrogen ; Belongs to the class of progestogens and estrogens in sequential preparations.
G03FA12 - medroxyprogesterone and estrogen ; Belongs to the class of progestogens and estrogens in fixed combinations.
References
Anon. Estrogens (Conjugated/Equine) and Medroxyprogesterone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/03/2018.

Anon. Estrogens (Conjugated/Equine, Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/03/2018.

Anon. Medroxyprogesterone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/03/2018.

Buckingham R (ed). Conjugated Oestrogens. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/03/2018.

Buckingham R (ed). Medroxyprogesterone Acetate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/03/2018.

Premique 0.625 mg/5 mg Coated Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk/. Accessed 14/03/2018.

Premique Cycle 0.625 mg/10 mg Coated Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk/. Accessed 14/03/2018.

Premique Low Dose 0.45 mg/1.5 mg Modified Release Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk/. Accessed 14/03/2018.

Prempro Tablet, Sugar Coated (A-S Medication Solutions). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/03/2018.

Disclaimer: This information is independently developed by MIMS based on Conjugated oestrogens + Medroxyprogesterone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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