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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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2019 Price of Synarel

$2,816.571 nasal spray (8ml) 2mg/ml
price without discount in nearest pharmacy. Price may vary.

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Nafarelin volume of distribution

Rapidly absorbed into the systemic circulation after intranasal administration. Bioavailability from a 400 µg dose averaged 2.8% (range 1.2 to 5.6%). Not absorbed after oral administration.

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2018 Statistics

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Discount Cards 16,000+

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Clients Benefit 29%

savings

Total savings $4,735,080

What is Nafarelin

A potent synthetic agonist of gonadotropin-releasing hormone with 3-(2-naphthyl)-D-alanine substitution at residue 6. Nafarelin has been used in the treatments of central precocious puberty and endometriosis.

Nafarelin mechanism of action

Like GnRH, initial or intermittent administration of nafarelin stimulates release of the gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland, which in turn transiently increases production of estradiol in females and testosterone in both sexes. However, with continuous daily administration, nafarelin continuously occupies the GnRH receptor, leading to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes. This causes a significant and sustained decline in the production of LH and FSH. A decline in gonadotropin production and release causes a dramatic reversible decrease in synthesis of estradiol, progesterone, and testosterone by the ovaries or testes. Like normal endometrium, endometriotic implants contain estrogen receptors. Estrogen stimulates the growth of endometrium. Use of nafarelin induces anovulation and amenorrhea and decreases serum concentrations of estradiol to the postmenopausal range, which induces atrophy of endometriotic implants. However, nafarelin does not abolish the underlying pathophysiology of endometriosis. In children with central precocious puberty receiving nafarelin, serum LH, testosterone, and estradiol concentrations return to prepubertal levels. This results in the supression of secondary sexual characteristics and decrased rate of linear growth and skeletal maturation. Following disconinuation of nafarelin, the effects of the drug is reversed, meaning FSH and LH concentrations usually return to pretreatment levels.

Dosage forms of Nafarelin

FormRouteStrength
Metered-dose aerosolnasal2 mg
Spray, meterednasal2 mg/mL
Liquidnasal2 mg

Prescription Generics

false

International Brands

Synarel

Synonyms

Nafarelin Nafarelina

Manufacturers

G.D. Searle LLC Division of Pfizer Inc

CAS number

76932-56-4

UNII

1X0094V6JV

State

solid

Affected organisms

Humans and other mammals

Indication of Nafarelin

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.

Toxicity of Nafarelin

In experimental animals, a single subcutaneous administration of up to 60 times the recommended human dose (on a micro;g/kg basis, not adjusted for bioavailability) had no adverse effects. At present, there is no clinical evidence of adverse effects following overdosage of GnRH analogs.

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