Nafarelin acetate Brand Name– Synarel
What is Nafarelin acetate
Nafarelin acetate is an intranasally administered synthetic analog of endogenous gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH).
Substitution of one amino acid normally found in GnRH leads to sustained activity of this drug that aids in hormonal control; in addition, nafarelin is approximately 200 times more potent than endogenous GnRH.
Nafarelin is used in the treatment of children with central precocious puberty (CPP).
Nafarelin is also used for hormone-sensitive conditions in women including endometriosis, uterine leiomyomata (fibroids), and hirsutism.
The maximum length of therapy for these indications in women is 6 months to minimize the risk of bone mineral density loss.
Nafarelin is also used for pituitary down-regulation prior to controlled ovarian hyperstimulation and subsequent in vitro fertilization.
Nafarelin has been used subcutaneously in men with benign prostatic hyperplasia (BPH) to shrink prostatic tissue; however, the subcutaneous formulation of nafarelin is not available in the US.
The manufacturer reports that for the treatment of symptoms associated with endometriosis, intranasal nafarelin at a dose of 400 mcg/day is clinically comparable to monthly IM injections of leuprolide depot 3.75 mg.
However, in one study, nafarelin use in women with severe symptoms of endometriosis was associated with less bone mineral density loss and fewer days with hypoestrogenic symptoms (including hot flashes) when compared to leuprolide; consequently, nafarelin was associated with a greater improvement in quality of life.
Intranasal nafarelin (Synarel®) was approved by the FDA in February of 1990 and is FDA-approved for the treatment of CPP in children and endometriosis in female patients >= 18 years of age.
Indications
- benign prostatic hyperplasia (BPH)
- endometriosis
- hirsutism
- infertility
- precocious puberty
- uterine leiomyomata
For the treatment of endometriosis
Side Effects
- acne vulgaris
- amenorrhea
- arthralgia
- asthenia
- breakthrough bleeding
- breast enlargement
- chest pain (unspecified)
- depression
- diabetes mellitus
- drug-induced body odor
- dyspnea
- edema
- elevated hepatic enzymes
- emotional lability
- headache
- hirsutism
- hot flashes
- hyperlipidemia
- hypertriglyceridemia
- impotence (erectile dysfunction)
- insomnia
- irritability
- libido decrease
- libido increase
- maculopapular rash
- menstrual irregularity
- myalgia
- myocardial infarction
- nasal irritation
- nausea
- ocular pain
- osteopenia
- osteoporosis
- ovarian enlargement
- ovarian hyperstimulation syndrome (OHSS)
- palpitations
- paresthesias
- pituitary apoplexy
- pruritus
- pulmonary embolism
- rash
- rhinitis
- seborrhea
- seizures
- stroke
- suicidal ideation
- thromboembolism
- thrombosis
- urticaria
- vaginal bleeding
- vaginal discharge
- visual impairment
- vomiting
- weight gain
- weight loss
Monitoring Parameters
- blood glucose
- glycosylated hemoglobin A1c (HbA1c)
- prostate-specific antigen (PSA)
- serum estradiol concentrations
- serum gonadotropin concentrations
- serum testosterone concentrations
Contraindications
- breast-feeding
- children
- depression
- Gonadotropin-Releasing Hormone (GnRH) analogs hypersensitivity
- menstruation
- osteoporosis
- pituitary insufficiency
- pregnancy
- seizure disorder
- suicidal ideation
- vaginal bleeding
Interactions
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
- Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
- Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
- Acetaminophen; Dextromethorphan; Phenylephrine
- Acetaminophen; Guaifenesin; Phenylephrine
- Androgens
- atypical antipsychotic
- Brompheniramine; Carbetapentane; Phenylephrine
- Brompheniramine; Dextromethorphan; Phenylephrine
- Carbetapentane; Chlorpheniramine; Phenylephrine
- Carbetapentane; Diphenhydramine; Phenylephrine
- Carbetapentane; Guaifenesin; Phenylephrine
- Carbetapentane; Phenylephrine
- Carbetapentane; Phenylephrine; Pyrilamine
- Carbinoxamine; Hydrocodone; Phenylephrine
- Carbinoxamine; Phenylephrine
- Chlophedianol; Guaifenesin; Phenylephrine
- Chlorpheniramine; Dextromethorphan; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Phenylephrine
- Chlorpheniramine; Hydrocodone; Phenylephrine
- Chlorpheniramine; Phenylephrine
- Chlorpromazine
- Cimetidine
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- Dextromethorphan; Diphenhydramine; Phenylephrine
- Dextromethorphan; Guaifenesin; Phenylephrine
- Dextromethorphan; Promethazine
- Diphenhydramine; Hydrocodone; Phenylephrine
- Diphenhydramine; Phenylephrine
- Fluphenazine
- Guaifenesin; Phenylephrine
- Haloperidol
- Hydrocodone; Phenylephrine
- Loxapine
- Meperidine; Promethazine
- Mesoridazine
- Molindone
- Oxymetazoline
- Perphenazine
- Perphenazine; Amitriptyline
- Phenothiazines
- Phenylephrine
- Phenylephrine; Promethazine
- Pimozide
- Prochlorperazine
- Promethazine
- Tetrabenazine
- Tetrahydrozoline
- Thiethylperazine
- Thioridazine
- Trifluoperazine
