Gestrinone

Drug #1462

Gestrinone is a synthetic steroidal hormone that exhibits androgenic, anti-oestrogenic and anti-progestogenic properties. it reduces the size of endometrial tissue fragments and leads to their regression, therefore Gestrinone is used mainly for treatment of endometriosis. It may inhibit ovulation and menstrual irregularities such as breakthrough bleeding may occur during treatment.

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Primary Characteristics

It is of Synthetic origin and belongs to Trienic 19-Nortestosterane.

Molecular Weight: 308.4 · Solubility in Water: Insoluble · Solubility in Alcohol: 1 in 10 · Non-proprietary name: Gestrinone.

Pharmacokinetics

Absorption: Gestrinone has an oral bioavailability is 30% (±30%).

Distribution: Gestrinone has a volume of distribution is 152 litre (high).

Elimination: it is metabolised via Hydroxylation in liver, plasma half-life is 24 hr, renal excretion is < 1 %.

Indications

Gestrinone is primarily indicated in conditions like Endometriosis.

Gestrinone is also indicated for secondary conditions like Benign breast disease, Fibroids, Intracranial meningiomas, Menorrhagia.

Contraindications

Gestrinone is contraindicated in conditions like Cardiac insufficiency, Renal insufficiency, Hepatic insufficiency, Pregnancy, Lactation, Metabolic or vascular disorders.

Dosage

Gestrinone's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
2.5 mg	2.5 mg	—	PO	Twice a week
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Gestrinone is known to cause more or less tolerable side effects which are usually transient. These include Acne, changes in libido, Cramps , Deepening of voice, Depression, Fluid retention, GI disturbance, Headache, Hirsutism , Hot flushes, Irregular bleeding, Light vaginal bleeding, Nervousness, Oily skin, Voice changes, Weight gain.

Warnings / Precautions

It should not be used during pregnancy or lactation. It should be used with caution in-patients with migraine headaches, heart, liver or kidney disease, a history of seizures, breast cancer, abnormal bleeding, previous strokes, prostate cancer or any other diseases. Extreme caution is advised for use in children. Pediatric specialist consultation is also advised. Geriatric men are at increased risk of developing enlarged prostate and prostate cancer with the use of androgen-like drugs, so use cautiously.

Interference in Pathology

Gestrinone may interfere in the diagnosis of Decreased concentration of thyroid binding globulin,decreased in serum total thyroxine level.

Available Brands

None recorded.

Storage Conditions

Gestrinone should be stored . Caps.

Drug Classification

1.18.2 — Androgens