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Nafarelin

Sold under the brand name Synarel among others, is a gonadotropin-releasing hormone agonist (GnRH agonist). More

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Description

Sold under the brand name Synarel among others, is a gonadotropin-releasing hormone agonist (GnRH agonist).

Generic Name

Nafarelin

Chemical names

Nafareline; Nafarelinum; Nafarelina

Brand names

Nasarel, Synarel

IUPAC name

(2S)-N-[(2S)-1-[(2S)-2-[(carbamoylmethyl)carbamoyl]pyrrolidin-1-yl]-5-[(diaminomethylidene)amino]-1-oxopentan-2-yl]-2-[(2R)-2-[(2S)-2-[(2S)-3-hydroxy-2-[(2S)-2-[(2S)-3-(1H-imidazol-5-yl)-2-{[(2S)-5-oxopyrrolidin-2-yl]forma

Pharmacokinetics

  • Rapidly absorbed into the systemic circulation after intranasal administration.
  • Approx 80% protein binding.

Actions

It is a potent agonistic analog of GnRH (gonadotropin-releasing hormone), this drug stimulates the release of the pituitary gonadotropins, LH (luteinizing hormone) and FSH (follicle-stimulating hormone), at the onset of administration, resulting in a temporary increase of gonadal steroidogenesis.

Dosage/Dosage form

  • 200 µg two times/day starting on days 2-4 of the menstrual cycle; may continue for up to 6 month for nasal Endometriosis.
  • Precocious Puberty- 1600 µg/day. Max: 1800µg/day.
  • Uterine fibroid 200 µg two times/day.

Therapeutic uses

For treatment of central precocious puberty (true precocious puberty, GnRH-dependent precocious precocity, complete isosexual precocity) in children of both sexes and for the treatment of endometriosis.

Adverse effects/Side effects

Irritation of the nose, muscle pain, reduced breast size, depression, convulsion, stomach pain, shortness of breath, chest pain, acne, rash, severe itching, allergic reaction, osteoporosis.

Interaction

  • When used in combination with Nafarelin the therapeutic efficacy of Corifollitropin alfa can be increased.
  • Nafarelin may decrease effectiveness of Capromab pendetide as a diagnostic agent.

Contraindications

Hypersensitivity, undiagnosed abnormal vaginal bleeding, pregnancy and breastfeeding.

Storage

Store at 15-30°C (59-86°F). 

Information

Molecular weight

1322.496

Molecular formula

C66H83N17O13

CAS number

76932-56-4

Precautions

  • Regular monitoring of bone age and density is needed.
  • Don’t use nasal decongestant within two hours after Nafarelin treatment.