Peringatan Keamanan

Serious or life-threatening adverse effects include coronary spasms with subsequent myocardial infarctions and uterine rupture following prolonged uterine hypertonia or abnormal uterine pain. More common adverse effects are nausea, vomiting, loose stools, diarrhea, lower abdominal or back pain, headache, mild pyrexia and flushing. Less common side effects include hypotension, chest pain palpitations, tachycardia, muscle weakness, dyspnea, chills and headache. Oral LD50 is 300 mg/kg in mouse, 980 mg/kg in rat and 3200 mg/kg in rabbit MSDS.

Gemeprost

DB08964

small molecule approved withdrawn

Deskripsi

Gemeprost is a prostaglandin E1 (PGE1) analog and antiprogestogen used for preoperative dilation of the cervix before surgical abortion. It is available as vaginal suppositories and also used in combination with the antiprogestin and mifepristone for termination of 1st- and 2nd-trimester pregnancy A19726. It is not FDA-approved but available in Japan marketed as Preglandin.

Struktur Molekul 2D

Berat 394.552
Wujud liquid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

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

Absorpsi

Systemic absorption of gemeprost is limited with about 12-28% of administered dose of gemeprost reaching the systemic circulation L878. Following vaginal administration, peak plasma concentration is reached after 2-3 hours A19726.

Metabolisme

After intravenous administration, gemeprost is rapidly metabolized via hydrolysis to the free acid with half life of 10-15 minutes. The free acid is then inactivated by ?- and ?-oxidation A19726.

Rute Eliminasi

About 50% of the dose eliminated as metabolites in the urine during the first 24 hours.

Interaksi Obat

1 Data
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Gemeprost.

Target Protein

Prostaglandin E2 receptor EP3 subtype PTGER3
Prostaglandin E2 receptor EP2 subtype PTGER2

Referensi & Sumber

Synthesis reference: U.S. Patent 4,052,512.
Artikel (PubMed)
  • PMID: 12972009
    Bygdeman M: Pharmacokinetics of prostaglandins. Best Pract Res Clin Obstet Gynaecol. 2003 Oct;17(5):707-16.
  • PMID: 12452468
    Bartley J, Baird DT: A randomised study of misoprostol and gemeprost in combination with mifepristone for induction of abortion in the second trimester of pregnancy. BJOG. 2002 Nov;109(11):1290-4.
  • PMID: 9866000
    Wong KS, Ngai CS, Wong AY, Tang LC, Ho PC: Vaginal misoprostol compared with vaginal gemeprost in termination of second trimester pregnancy. A randomized trial. Contraception. 1998 Oct;58(4):207-10.
  • PMID: 2996248
    Husslein P: Causes of labor initiation in man: role of oxytocin and prostaglandins. Z Geburtshilfe Perinatol. 1985 May-Jun;189(3):95-102.

Contoh Produk & Brand

Produk: 0 • International brands: 4
International Brands
  • Cergem — MSD Merck Sharp & Dohme
  • Cervagem — Sanofi
  • Cervagème — Sanofi-Aventis
  • Cervidil — Merck Serono

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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