Leuprolide (Acetate)

Also known as: Leuprorelin Acetate

Drug #1562

Leuprolide (Acetate) is a gonadorelin analogue. Leuprolide (Acetate) is used for the supression of gonadal sex hormone secretions, in the treatment of advanced prostate cancera and breast cancer. Leuprolide (Acetate) is used as hormonal therapy in the treatment of endometriosis. Leuprolide is administered parenterally. It was approved by the FDA in April 1985 and came off patent in 1996. The depot formulation of leuprolide is indicated for treating uterine fibroid tumors, endometriosis, and advanced prostate cancer.

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Primary Characteristics

Leuprolide (Acetate) is also known as Leuprorelin Acetate.

It is of Synthetic origin and belongs to Hormone.

Molecular Weight: 1269.5 · pK_a: 6, 10, 13 · Solubility in Water: readily soluble · Solubility in Alcohol: readily soluble · Non-proprietary name: Leuprolide (Acetate).

Molecular structure of Leuprolide (Acetate)

Pharmacokinetics

Distribution: Leuprolide (Acetate) has a volume of distribution is 32 litre. plasma protein binding is 46%.

Elimination: plasma half-life is 2.6-3.8 hr.

Indications

Leuprolide (Acetate) is primarily indicated in conditions like Breast cancer, Endometriosis, Intractable premenstrual syndrome, Prostatic cancer, Shrinkage of fibroids before surgery.

Leuprolide (Acetate) is also indicated for secondary conditions like Uterine fibroids.

Contraindications

Leuprolide (Acetate) is contraindicated in conditions like Vaginal bleeding, Hypersensitivity, Lactation.

Dosage

Leuprolide (Acetate)'s dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
3.75 mg	3.75 mg	—	IM	Endometriosis This dose should be administer monthly or 11.25 mg should be given every 3 months. (depot preparation).
300 ug/kg	300 ug/kg	—	IM	Every 4 week adfuried according to responce.
1 mg/day	1 mg/day	—	SC	Advanced Prostate Cancer
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

Leuprolide (Acetate) in overdosage may give rise to further complications which include Leucopenia, Urinary retention, Angina , Bone pain , Myocardial infarction , Flare phenomenon, Urinary retention, Increased size of uterine myomata, Bowel obstruction, Bowel obstruction.

Leuprolide (Acetate) is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Acne, athralgia, Body hair, Change in scalp, Decrease in libido, Diarrhea, Dry skin, Gynecomastia, Headache, Hot flushes, Impotence, Light-headedness, Mood changes, Nausea, Nervousness, Palpitation, parasthesia, Peripheral edema, Vomiting , Weight gain.

Warnings / Precautions

Leuprolide injection (not the depot) formulation use with caution in the patients hypersensitive to benzyl alcohol. Long-term safety of leuprolide in children has not been established. At the initiation of the therapy tumor flare, bone pain and urinary tract obstruction may occur. Patient with life threatening diseases in which the rapid symptomatic relief is essential should be treated extremely cautiously with leuprolide. The drug should not be administered during pregnancy.

Interference in Pathology

Leuprolide (Acetate) may interfere in the diagnosis of Interfere with the diagnostic test of pituitary gonadotropic and the gonad function.

Available Brands

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Single Ingredient

Caps

3.75 mg

Inj

11.25 mg 3.75 mg 7.5 mg

Storage Conditions

Leuprolide (Acetate) should be stored Inj.

Drug Classification

1.8.3 — Hormones and antihormones
2.29 — Drugs used in renal, bladder, and prostatic disorders

Manufacturers

Manufacturers of Leuprolide (Acetate) in Pakistan:

Abbott Medisure Novartis Paramount