Nafarelin (Acetate)

Drug #1550

Nafarelin (Acetate) is an analogue of gonadorelin with similar properties. Administration of gonadorelin analogues produces stimulation and causes reduction in the release of gonadotrophins (Follicle-stimulating hormone and luteinising hormone), which ultimately leads to inhibition of androgen and estrogen synthesis. Nafarelin (Acetate) is used in the treatment of endometriosis, precocious puberty, infertility anemia due to uterine fibroidsbreast cancer, prostate cancer and prior to intra-uterine surgery.

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Primary Characteristics

It is of Synthetic origin.

Molecular Weight: 1322.5 · pK_a: 10.98 · Solubility in Water: slighty · Solubility in Alcohol: very slighty · Non-proprietary name: Nafarelin (Acetate).

Molecular structure of Nafarelin (Acetate)

Pharmacokinetics

Absorption: Nafarelin (Acetate) has an oral bioavailability is 1.4% (±1.4%).

Distribution: Nafarelin (Acetate) has a plasma protein binding is 80 %.

Elimination: plasma half-life is 4 hr, renal excretion is 3 % unchanged.

Indications

Nafarelin (Acetate) is primarily indicated in conditions like Benign prostatic hypertrophy, Endometriosis, Preparation of endometrial resection, Shrinkage of fibroids before surgery.

Nafarelin (Acetate) is also indicated for secondary conditions like Infertility, Pituitary desensitisation.

Contraindications

Nafarelin (Acetate) is contraindicated in conditions like Osteoporosis, Vaginal bleeding, Pregnancy, Lactation.

Dosage

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

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
400 mcg	400 mcg	—	IN	200 mcg (base) into one nostril in the morning and 200 mcg into the other nostril in the evening for 6 months.
800 mcg	800 mcg	—	IN	For undometriosis 400mcg each hostril.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

None recorded.

Side Effects

Nafarelin (Acetate) produces potentially life-threatening effects which include Chest pain, Urticaria, Decreased invertebral trabecular bone mass, Shortness of breath, Pruritis. Careful monitoring is needed with proper medical management.

Nafarelin (Acetate) is known to cause more or less tolerable side effects which are usually transient. These include Acne, Changes in libido , Headache, Hot flushes, Irritation of nasal mucosa, Myalgia, Ovarian cyst, Rashes , Vaginal dryness.

Warnings / Precautions

Children treated for central precocious puberty should be closely monitored by the physician, during and after nafarelin treatment for central precocious puberty. Possibility of amenorrhea or irregular menstrual periods; checking with physician if regular menstruation does not occur within 60 to 90 days after discontinuation of medication.Using a water-based vaginal lubricant if painful sexual intercourse or vaginal dryness is a problem. Medication should be stopped if pregnany is suspected.

Interference in Pathology

Nafarelin (Acetate) may interfere in the diagnosis of Pregnanediol Test , Increased Alkaline Phosphatase Levels, Gonadal function testing, Increased serum phosphate level.

Available Brands

None recorded.

Storage Conditions

Nafarelin (Acetate) should be stored Nasal Spray.

Drug Classification

1.18.6 — Ovulation stimulants