Peringatan Keamanan

In experimental animals, a single subcutaneous administration of up to 60 times the recommended human dose (on a µg/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.

Nafarelin

DB00666

small molecule approved

Deskripsi

Nafarelin is 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.

Struktur Molekul 2D

Berat 1322.496
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

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.

Metabolisme

Enzymatic hydrolysis.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting alcohol in excess may increase the risk of bone thinning associated with taking nafarelin.

Interaksi Obat

100 Data
Corifollitropin alfa The therapeutic efficacy of Corifollitropin alfa can be increased when used in combination with Nafarelin.
Choline C 11 Nafarelin may decrease effectiveness of Choline C 11 as a diagnostic agent.
Capromab pendetide Nafarelin may decrease effectiveness of Capromab pendetide as a diagnostic agent.
Leuprolide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Leuprolide is combined with Nafarelin.
Somatotropin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Somatotropin is combined with Nafarelin.
Infliximab The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Infliximab is combined with Nafarelin.
Daptomycin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Daptomycin is combined with Nafarelin.
Cyclosporine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cyclosporine is combined with Nafarelin.
Pravastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pravastatin is combined with Nafarelin.
Baclofen The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Baclofen is combined with Nafarelin.
Sildenafil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Sildenafil is combined with Nafarelin.
Indinavir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Indinavir is combined with Nafarelin.
Lovastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Lovastatin is combined with Nafarelin.
Cladribine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cladribine is combined with Nafarelin.
Phenytoin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Phenytoin is combined with Nafarelin.
Pamidronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pamidronic acid is combined with Nafarelin.
Mefloquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Mefloquine is combined with Nafarelin.
Tacrine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Tacrine is combined with Nafarelin.
Carbimazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Carbimazole is combined with Nafarelin.
Cerivastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cerivastatin is combined with Nafarelin.
Trimethoprim The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Trimethoprim is combined with Nafarelin.
Betamethasone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Betamethasone is combined with Nafarelin.
Montelukast The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Nafarelin.
Zidovudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Zidovudine is combined with Nafarelin.
Cimetidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cimetidine is combined with Nafarelin.
Ritonavir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ritonavir is combined with Nafarelin.
Lercanidipine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Lercanidipine is combined with Nafarelin.
Ciprofloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ciprofloxacin is combined with Nafarelin.
Vincristine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Vincristine is combined with Nafarelin.
Propylthiouracil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Propylthiouracil is combined with Nafarelin.
Methotrexate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Methotrexate is combined with Nafarelin.
Enalapril The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Enalapril is combined with Nafarelin.
Nizatidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nizatidine is combined with Nafarelin.
Ivermectin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Nafarelin.
Chloroquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Chloroquine is combined with Nafarelin.
Triamcinolone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Triamcinolone is combined with Nafarelin.
Niacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Niacin is combined with Nafarelin.
Alendronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Alendronic acid is combined with Nafarelin.
Clofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Clofibrate is combined with Nafarelin.
Simvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Simvastatin is combined with Nafarelin.
Stavudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Stavudine is combined with Nafarelin.
Amphotericin B The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Amphotericin B.
Mycophenolate mofetil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Mycophenolate mofetil.
Lamivudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Lamivudine.
Ibandronate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ibandronate.
Propofol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Propofol.
Terbinafine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Terbinafine.
Penicillamine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Penicillamine.
Ranitidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ranitidine.
Tacrolimus The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Tacrolimus.
Eprosartan The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Eprosartan.
Risedronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Risedronic acid.
Bumetanide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Bumetanide.
Triazolam The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Triazolam.
Ethanol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ethanol.
Salmeterol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Salmeterol.
Isoniazid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Isoniazid.
Methyldopa The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Methyldopa.
Isotretinoin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Isotretinoin.
Cytarabine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Cytarabine.
Ganciclovir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ganciclovir.
Letrozole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Letrozole.
Sulfamethoxazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Sulfamethoxazole.
Minocycline The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Minocycline.
Procainamide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Procainamide.
Fenofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Fenofibrate.
Norfloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Norfloxacin.
Atorvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Atorvastatin.
Fluvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Fluvastatin.
Rosuvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Rosuvastatin.
Amiodarone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Amiodarone.
Ofloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ofloxacin.
Procarbazine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Procarbazine.
Captopril The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Captopril.
Paclitaxel The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Paclitaxel.
Saquinavir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Saquinavir.
Metoclopramide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Metoclopramide.
Dexamethasone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Dexamethasone.
Gemfibrozil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Gemfibrozil.
Docetaxel The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Docetaxel.
Bezafibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Bezafibrate.
Colchicine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Colchicine.
Fusidic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Fusidic acid.
Trabectedin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Trabectedin.
Mevastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Mevastatin.
Raltegravir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Raltegravir.
Pitavastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Pitavastatin.
Etofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Etofibrate.
Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Acipimox.
Ciprofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ciprofibrate.
Ubidecarenone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ubidecarenone.
Tianeptine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Tianeptine.
Mebeverine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Mebeverine.
Ipecac The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ipecac.
Emetine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Emetine.
Simfibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Simfibrate.
Ronifibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Ronifibrate.
Aluminium clofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Aluminium clofibrate.
Clofibride The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Clofibride.
Fenofibric acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Fenofibric acid.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR
Putative gonadotropin-releasing hormone II receptor GNRHR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9622415
    Hugues JN, Cedrin Durnerin IC: Revisiting gonadotrophin-releasing hormone agonist protocols and management of poor ovarian responses to gonadotrophins. Hum Reprod Update. 1998 Jan-Feb;4(1):83-101.
  • PMID: 7996307
    Garner C: Uses of GnRH agonists. J Obstet Gynecol Neonatal Nurs. 1994 Sep;23(7):563-70.
  • PMID: 1531579
    Henzl MR: Gonadotropin-releasing hormone analogs: update on new findings. Am J Obstet Gynecol. 1992 Feb;166(2):757-61.
  • PMID: 1531576
    Burry KA: Nafarelin in the management of endometriosis: quality of life assessment. Am J Obstet Gynecol. 1992 Feb;166(2):735-9.
  • PMID: 1830521
    Saltiel E, Garabedian-Ruffalo SM: Pharmacologic management of endometriosis. Clin Pharm. 1991 Jul;10(7):518-31.
  • PMID: 2140979
    Chrisp P, Goa KL: Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. Drugs. 1990 Apr;39(4):523-51.
  • PMID: 2151003
    Letassy NA, Thompson DF, Britton ML, Suda RR Sr: Nafarelin acetate: a gonadotropin-releasing hormone agonist for the treatment of endometriosis. DICP. 1990 Dec;24(12):1204-9.

Contoh Produk & Brand

Produk: 3 • International brands: 4
Produk
  • Synarel
    Spray, metered • 2 mg/1mL • Nasal • US • Approved
  • Synarel
    Aerosol, metered • 200 mcg / act • Nasal • Canada • Approved
  • Synarel Nas Sol 2mg/ml
    Liquid • 2 mg / mL • Nasal • Canada • Approved
International Brands
  • Nafarelil — Fuji Yakuhin
  • Nasanyl — Pfizer
  • Synarela — Pfizer
  • Synrelina — Pfizer

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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