Megestrol (Acetate)
Megestrol is a sex hormone orally active synthetic derivative of progeterone, actions and effects are similar to that of progesterone. Used to suppress oestrogen-dependent tumours of the breast and the uterus by interferingwith uptake of oestrogen into the tumours. Chemically Megestrol (Acetate) is identified as 17-hydroxy-6-methylpregne-4,6-diene-3, 20-dione acetate. Adverse effects include weight gain, hair loss, deep venous thromboses in the legs.
Primary Characteristics
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 Antineoplastic Agent, Progestin pharmacological group.
Molecular Weight: 384.5 · pKa: not relevant · Solubility in Water: <1 in 10000 · Solubility in Alcohol: 1 in 60 · Non-proprietary name: Megestrol (Acetate).
Pharmacokinetics
Absorption: Megestrol (Acetate) has an oral bioavailability is 50% (±50%).
Elimination: plasma half-life is 15-20 hr, renal excretion is 57-78%.
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Indications
Megestrol (Acetate) is primarily indicated in conditions like Breast cancer, Prostatic cancer.
Megestrol (Acetate) is also indicated for secondary conditions like Cancer cachexia, Endometrial cancer, Renal carcinoma.
Contraindications
Megestrol (Acetate) is contraindicated in conditions like Diabetes mellitus, Dysfunctional uterine bleeding, Vaginal bleeding, Thrombophlebitis.
Dosage
Megestrol (Acetate)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 160 mg | 160 mg | Every 24h | PO | breast cancer. |
| 160 mg | 160 mg | Every 24h | PO | breast cancer. |
| 180 mg | 180 mg | Every 6h | PO | For endom etrial carcinoma in divided doses |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Not indicated in this age group | |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended in 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
Megestrol (Acetate) in overdosage may give rise to further complications which include Hypertension , Heart failure , Deep vein thrombosis, Pulmonary embolism .
Megestrol (Acetate) is known to cause more or less tolerable side effects which are usually transient. These include Alopecia, Carpal tunnel syndrome, Edema, Hot flushes, Hyperglycemia, Increased appetite, Mood changes, Nausea, Tumor flare, Urticaria, Vomiting , Weight gain.
Warnings / Precautions
Interference in Pathology
Megestrol (Acetate) may interfere in the diagnosis of None well documented.
Available Brands
Storage Conditions
Drug Classification
- 1.8.3 — Hormones and antihormones