Nafarelin

DEA Class; Rx

Common Brand Names; Synarel

  • Gonadotropin Releasing Hormone Agonists

Intranasal synthetic analog of GnRH used for treatment of central precocious puberty in children and for endometriosis, uterine fibroids, and hirsutism in women. Maximum recommended length of therapy in women is 6 months due to risk of osteoporosis. Also used for female infertility.

Indicated for the treatment of endometriosis.

For the treatment of precocious puberty.
For the treatment of uterine leiomyomata.
For the treatment of hirsutism.
For inhibiting premature leuteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation and subsequent in vitro fertilization (IVF) or other assisted reproductive technology (ART) for the treatment of infertility.
For the treatment of benign prostatic hyperplasia (BPH).

Pregnancy, hypersensitivity, lactation, undiagnosed abnormal vaginal bleeding

  • Acne (10%)
  • Breast enlargement (8%)
  • Vaginal bleeding (8%)
  • Seborrhea (3%)
  • Emotional lability (6%)
  • Vaginal discharge (3%)
  • Rhinitis (5%)
  • Body odor (4%)
  • Increase in pubic hair (5%)
  • Arthralgia
  • Breast engorgement
  • Chloasma
  • Maculopapular rash
  • Paresthesia
  • Weakness
  • Palpitation
  • Eye pain
  • Liver injury
  • Pituitary apoplexy
  • Seizures
  • Pituitary gland changes
  • Liver injury (rare)
  • Ovarian hyperstimulation syndrome

Goal in adult females is to suppress menstruation; max treatment period 6 mth

May cause increase in bone turnover & decrease in bone mineral content

Ovarian cysts may develop within first 2 months of therapy and occur more commonly in women with polycystic ovarian disease

Cases of pituitary apoplexy reported

Use caution in patients with risk factors for decreased bone mineral density

Irregular or incomplete daily doses may result in stimulation of the pituitary-gonadal axis; counsel caregivers to assure full compliance

During first month of treatment, may initially expect some signs of puberty, e.g., vaginal bleeding or breast enlargement, may occur; such changes should resolve soon after first month; if such resolution does not occur within first two months of treatment, this may be due to lack of compliance or presence of gonadotropin independent sexual precocity; if both possibilities excluded, the dose omay be increased to 1800 mcg/day administered as 600 mcg tid

Patients with intercurrent rhinitis should consult their physician for use of topical nasal decongestant; if use of topical nasal decongestant required during treatment decongestant should not be used until at least 2 hr after administering therapy; sneezing during or immediately after administering therapy should be avoided, if possible, since may impair drug absorption

Convulsions reported in patients receiving GnRH agonists; reports with GnRH agonists have included patients with a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies or tumors, and patients on concomitant medications that have been associated with convulsions such as bupropion and SSRIs; convulsions also reported in patients in the absence of any of the conditions listed

Psychiatric events reported in patients taking GnRH agonists; postmarketing reports with this class of drugs include symptoms of emotional lability, such as crying, irritability, impatience, anger, and aggression; monitor for development or worsening of psychiatric symptoms during treatment

Pseudotumor cerebri (idiopathic intracranial hypertension) reported in pediatric patients receiving GnRH agonists, including leuprolide acetate; monitor patients for signs and symptoms of pseudotumor cerebri, including headache, papilledema, blurred vision, diplopia, loss of vision, pain behind the eye or pain with eye movement, tinnitus, dizziness, and nausea; inform patients and caregivers that reports of pseudotumor cerebri have occurred

Pregnancy Category: X

Lactation: Excretion in milk unknown, contraindicated

Adults

Males: 400 mcg/day SC.
Females: 800 mcg/day intranasally.

Adolescents

1800 mcg/day intranasally.

Children

1800 mcg/day intranasally.

Nafarelin Acetate

nasal spray

  • 2mg/mL

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