Medroxyprogesterone (Acetate)
Also known as: Methylacetylprogestron, Metipregnone
Medroxyprogesterone (Acetate) is oral and parenteral synthetic progestin a (sex hormone). Medroxyprogesterone (Acetate) is 15 times more potent than progesterone. Can be used for the treatment of amenorrhea, abnormal uterine bleeding, endometriosis secondary to hormonal imbalances, and endometrial and renal cell carcinomas. The IM injection is a sustained-release (i.e., "depo") product available in 2 dosage strengths: one for use as a contraceptive and the other for the treatment of endometrial and renal cell carcinoma.it may be useful as respiratory stimulants in certain pulmonary disorders such as chronic obstructive pulmonary disease (COPD). it was approved by the FDA in 1959. The primary contraceptive effect of progestins involves the suppression of the midcycle surge of LH. The exact mechanism of action, however, is unknown. At the cellular level, progestins diffuse freely into target cells and bind to the progesterone receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge, thereby preventing follicular maturation and ovulation. Overall, progestin-only contraceptives prevent ovulation in 70-80% of cycles.
Primary Characteristics
Medroxyprogesterone (Acetate) is also known as Methylacetylprogestron, Metipregnone.
It is of Synthetic origin and belongs to Steroid.
It belongs to Progesterone agonist pharmacological group on the basis of mechanism of action and also classified in Contraceptive Hormonal pharmacological group. It is also classified under Sex Hormones .
Molecular Weight: 386.5 · Solubility in Water: 1 in 10000 · Solubility in Alcohol: 1 in 800 · Non-proprietary name: Medroxyprogesterone (Acetate).
Pharmacokinetics
Absorption: Medroxyprogesterone (Acetate) has an oral bioavailability is 97.5% (±2.5%).
Distribution: Medroxyprogesterone (Acetate) has a volume of distribution is >20 litre. plasma protein binding is 94%.
Elimination: it is metabolised via Hepatic (extensive), plasma half-life is 16-30 hr, renal excretion is 5%.
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Indications
Medroxyprogesterone (Acetate) is primarily indicated in conditions like Adjunctive treatment of endometrial carcinoma, Adjunctive treatment of renal carcinoma, Breast cancer, Contraception, Dysfunctional uterine bleeding, Endometrial cancer, Endometriosis, Mild to moderate endometriosis, Progestogenic opposition of oestrogen hrt, Secondary amenorrhoea, Uterine bleeding.
Medroxyprogesterone (Acetate) is also indicated for secondary conditions like Pelvic congestion, Renal carcinoma.
Contraindications
Medroxyprogesterone (Acetate) is contraindicated in conditions like Abnormal uterine bleeding, Hepatic dysfunction, Hypersensitivity, Phlebitis, Hematuria.
Dosage
Medroxyprogesterone (Acetate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 150 mg | 150 mg | — | IM | (Depot Inj.) During first 5 days of cycle or in first 5 weeks postpartum. repeat at 3 months intervals. |
| 2250 mg | 2250 mg | — | IM | |
| 300 mg | 300 mg | Every 24h | PO | Dose vary according to indication. |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Not applicable for this age group | |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not applicable for this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Medroxyprogesterone (Acetate) in overdosage may give rise to further complications which include Hypertension , Myalgia , Thromboembolism, Urticaria , Impotence , Thrombophlebitis , Depression , Increased blood pressure , Pulmonary embolism , Hyperglycemia , Breakthrough bleeding, Jaundice , Retinal thrombosis , Decreased libido .
Medroxyprogesterone (Acetate) produces potentially life-threatening effects which include Anaphylactoid reactions . Careful monitoring is needed with proper medical management.
Medroxyprogesterone (Acetate) is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Acne, Alopecia, Amenorrhea, Anovulation , Anxiety, Appetite stimulation, Cervicitis, Cushing syndrome, Diarrhea, Dysmenorrhea, Elevation of liver enzymes, Fluid retention, Hirsutism , Insomnia, Muscle cramps, Reaction at injection site, SweatingX, Termors, Vaginal spotting, Weakness, Weight gain, Weight LossX.
Warnings / Precautions
Interference in Pathology
Medroxyprogesterone (Acetate) may interfere in the diagnosis of Liver Function Test , Gonadotrophin Test , Pregnanediol Test , Oestrogen Test , Glucose Test , Metyrapone Test , Progesterone Test , Testosterone Test , Cortisol Test .
Available Brands
Storage Conditions
Drug Classification
- 1.18.3.1 — Hormonal contraceptives
- 2.18.5 — Progestogens