| NAFARELIN ACETATE
Classifications: hormone; gonadotropin-releasing hormone analog; Therapeutic: gonadotropin-releasing hormone analog
Pregnancy Category: X
0.2 mg/spray solution
Potent agonist analog of gonadotropin-releasing hormone (GnRH). Inhibits pituitary gonadotropin secretion of LH and FSH.
Decrease in serum estradiol or testosterone concentrations results in the quiescence of tissues and functions that depend
on LH and FSH.
Endometriosis and precocious puberty.
Uterine leiomyomas, benign prostatic hypertrophy.
Hypersensitivity to GnRH or GnRH agonist analog; undiagnosed abnormal vaginal bleeding; pregnancy (category X), lactation.
Polycystic ovarian disease; osteoporosis.
Route & Dosage
Adult: Inhalation 2 inhalations/d (200 mcg/inhalation), one in each nostril, begin between days 2 and 4 of menstrual cycle; in patients with
persistent regular menstruation after 2 mo of therapy, may increase to 800 mcg/d as 2 inhalations (one in each nostril)
b.i.d.; do not exceed 6 mo of treatment
Child: Inhalation 8001200 mcg/d divided q812h
- Withhold any topical nasal decongestant, if being used, until at least 30 min after nafarelin administration.
- Store at 15°30° C (59°86° F); protect from light.
Adverse Effects (≥1%)GI: Bloating, abdominal cramps,
weight gain, nausea. Endocrine: Hot flashes, anovulation, amenorrhea, vaginal dryness,
Decreased bone mineral content (reversible). CNS:
Transient headache, inertia, mild depression
, moodiness, fatigue
Nasal irritation. Urogenital: Impotence, decreased libido,
Diagnostic Test Interference
Increased alkaline phosphatase; marked increase in estradiol in first 2 wk, then decrease to below baseline; decreased FSH and LH levels; decreased testosterone levels.
No clinically significant interactions established.
21% absorbed from nasal mucosa
4 wk. Peak:
12 wk. Duration:
3050 d after discontinuing drug. Distribution:
7884% bound to plasma proteins
; crosses placenta. Metabolism:
Hydrolyzed in kidney. Elimination:
4455% in urine over 7 d, 1944% in feces. Half-Life:
Assessment & Drug Effects
- Make appropriate inquiries about breakthrough bleeding, which may indicate that patient has missed successive drug doses.
Patient & Family Education
- Read the information pamphlet provided with nafarelin.
- Inform physician if breakthrough bleeding occurs or menstruation persists.
- Use or add barrier contraceptive during treatment.