Nafarelin

Indications
 Nasal
Endometriosis
Adult: 200 mcg (into each nostril) bid starting on days 2-4 of the menstrual cycle; may be continued for up to 6 mth. Double dose after 2 mth if amenorrhoea is not achieved.
Nasal
Central precocious puberty
Child: 800 mcg (400 mcg into each nostril) bid. Dose may be increased to 600 mcg tid into alternate nostrils depending on response.
Nasal
Adjunct to induce ovulation with gonadotrophins in the treatment of infertility
Adult: 400 mcg intranasally bid starting either in the early follicular phase (day 2) or midluteal phase (day 21) of the menstrual cycle. Continue treatment until downregulation is achieved; withdraw therapy if this does not occur within 12 wk. Once downregulation is achieved, add gonadotrophin treatment to nafarelin therapy until an appropriate stage of follicular development, then both are discontinued and chorionic gonadotrophin is given to induce ovulation.
Contraindications
 Undiagnosed abnormal vaginal bleeding. Pregnancy and lactation.
Warnings / Precautions
 Patients with risk factors for decreased bone mineral density. Ovarian cysts may occur during the first 2 mth of therapy, more commonly in women with polycystic ovarian disease. Monitor patient regularly, especially during the first 6-8 wk of therapy to ensure patient compliance and adequate response. Determine bone age and growth velocity within 3-6 mth of initiation of therapy and periodically thereafter. Do not use topical nasal decongestant for at least 2 hr after nafarelin admin.
Adverse Reactions
 Shortness of breath, chest pain, urticaria, rash, pruritus. Women: Hot flushes, decreased libido, vaginal dryness, headache, emotional lability, acne, myalgia, decrease in breast size, nasal irritation. Decreased bone mineral density. Children: Acne, transient breast enlargement, emotional lability, transient increases in pubic hair, body odour, seborrhoea, hot flushes, rhinitis, vaginal bleeding, white or brown vaginal discharge.
Lab Interactions
 May interfere with diagnostic tests for pituitary gonadotrophic and gonadal functions if done during or up to 4-8 wk after discontinuation of drug.
Mechanism of Actions
 Nafarelin is a gonadotrophin-releasing hormone (GnRH) analogue which exhibits greater potency in terms of pituitary release of luteinising hormone (LH) and follicle-stimulating hormone (FSH). It subsequently stimulates the secretion of sex hormones from the gonads. Nafarelin causes stimulation of gonadotrophin release in the initial phase (single dose). However, with continued admin, stimulation is reversed resulting in the inhibition of gonadotrophin release.
Absorption: Rapidly absorbed (intranasal). Peak plasma concentrations within 20 min; bioavailability: About 3%.
Distribution: Protein-binding: 80%.
Metabolism: Metabolised by peptidases.
Excretion: SC admin: Via urine (as metabolites) and faeces (as unchanged drug).
Storage Conditions
 Nasal: Store at 15-30°C (59-86°F). Protect from light.
ATC Classification
 H01CA02 - nafarelin ; Belongs to the class of gonadotropin-releasing hormones. Used in hypothalamic hormone preparations.
Storage
 Nasal: Store at 15-30°C (59-86°F). Protect from light.
Available As
  • Nafarelin 2 mg

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