Peringatan Keamanan

The oral LD50 in rats is 81mg/kg and in mice is 27mg/kg.L7613 The intraperitoneal LD50 in rats is 40mg/kg and in mice is 70mg/kg.L7613

Patients experiencing an overdose may present with sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea, fever, palpitations, hypotension, and bradycardia.A181706,L7616,L7619 Hemodialysis is not expected to be useful in the treatment of misoprostol overdoseL7616 but oral activated charcoal may help reduce absorption.L7619 In the event of an overdose, treat symptoms with supportive therapy.L7616 This may include removal of undissolved tablets from the vagina or buccal cavity, intravenous fluid replacement, acetaminophen, diazepam, haloperidol, or intramuscular diclofenac depending on the symptoms that present.A181706

Misoprostol

DB00929

small molecule approved

Deskripsi

Misoprostol is a prostaglandin analog used to reduce the risk of NSAID related ulcers, manage miscarriages, prevent post partum hemorrhage, and also for first trimester abortions.L7616,L7619,A181589,A181583,A181697 The stimulation of prostaglandin receptors in the stomach reduces gastric acid secretion, while stimulating these receptors in the uterus and cervix can increase the strength and frequency of contractions and decrease cervical tone.A181586

Misoprostol was granted FDA approval on 27 December 1988.L7616

Struktur Molekul 2D

Berat 382.5341
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of an 800µg oral dose is 1.0401±0.5090h, for a sublingual dose is 0.8542±0.1170h, and for a buccal dose is 0.8365±0.1346h.[A181592]
Volume Distribusi Data regarding the volume of distribution of misoprostol is scarce. The apparent volume of distribution of the active metabolite of misoprostol was in subjects with normal renal function was 13.6±8.0L/kg, with mild renal impairment was 17.3±23.0L/kg, with moderate renal impairment was 14.3±6.8L/kg, and with end stage renal disease was 11.0±9.6L/kg.[A181610]
Klirens (Clearance) Because of the rapid de-esterification of misoprostol before or during absorption, it is usually undetectable in plasma.[A181610] Misoprostol's active metabolite, misoprostol acid, has a total body clearance of 0.286L/kg/min.[A181610] Subjects with mild renal impairment had a total body clearance of 0.226±0.073L/kg/min, subjects with moderate renal impairment had a total body clearance of 0.270±0.103L/kg/min, and subjects with end stage renal disease had a total body clearance of 0.105±0.052L/kg/min.[A181610]

Absorpsi

For an 800µg oral dose of misoprostol, the AUC was 2.0192±0.8032h\*ng/mL, the Cmax was 2.6830±1.2161ng/mL, and a tmax of 0.345±0.186h.A181592 For a 800µg sublingual dose of misoprostol, the AUC was 3.2094±1.0417h\*ng/mL, the Cmax was 2.4391±1.1567ng/mL, and a tmax of 0.712±0.415h.A181592 For a 800µg buccal dose of misoprostol, the AUC was 2.0726±0.3578h\*ng/mL, the Cmax was 1.3611±0.3436ng/mL, and a tmax of 1.308±0.624h.A181592

Metabolisme

Misoprostol is de-esterified to its active metabolite, misoprostol acid, also known as SC-30695.A181574 This metabolite is further reduced to dinor and tetranor metabolites (SC-41411), a prostaglandin F1 (PGF1) analog of SC-41411, and a ?-16-carboxylic acid derivative.A181574 However, the majority of these metabolites are not well described in the literature.A181574

Rute Eliminasi

As much as 73.2±4.6% of a radiolabelled oral dose of misoprostol is recovered in the urine.A181574,L7619

Interaksi Makanan

1 Data
  • 1. Take with food. Food decreases incidence of diarrhea.

Interaksi Obat

21 Data
Carboprost tromethamine Carboprost tromethamine may increase the uterotonic activities of Misoprostol.
Oxytocin The risk or severity of adverse effects can be increased when Misoprostol is combined with Oxytocin.
Carbetocin The risk or severity of adverse effects can be increased when Misoprostol is combined with Carbetocin.
Magnesium oxide The risk or severity of adverse effects can be increased when Magnesium oxide is combined with Misoprostol.
Magaldrate The risk or severity of adverse effects can be increased when Magaldrate is combined with Misoprostol.
Magnesium hydroxide The risk or severity of adverse effects can be increased when Magnesium hydroxide is combined with Misoprostol.
Magnesium trisilicate The risk or severity of adverse effects can be increased when Magnesium trisilicate is combined with Misoprostol.
Magnesium carbonate The risk or severity of adverse effects can be increased when Magnesium carbonate is combined with Misoprostol.
Magnesium silicate The risk or severity of adverse effects can be increased when Magnesium silicate is combined with Misoprostol.
Hydrotalcite The risk or severity of adverse effects can be increased when Hydrotalcite is combined with Misoprostol.
Magnesium peroxide The risk or severity of adverse effects can be increased when Magnesium peroxide is combined with Misoprostol.
Magnesium sulfate The risk or severity of adverse effects can be increased when Magnesium sulfate is combined with Misoprostol.
Magnesium salicylate The risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Misoprostol.
Magnesium chloride The risk or severity of adverse effects can be increased when Magnesium chloride is combined with Misoprostol.
Magnesium citrate The risk or severity of adverse effects can be increased when Magnesium citrate is combined with Misoprostol.
Magnesium aspartate The risk or severity of adverse effects can be increased when Magnesium aspartate is combined with Misoprostol.
Magnesium gluconate The risk or severity of adverse effects can be increased when Magnesium gluconate is combined with Misoprostol.
Magnesium orotate The risk or severity of adverse effects can be increased when Magnesium orotate is combined with Misoprostol.
Magnesium The risk or severity of adverse effects can be increased when Magnesium is combined with Misoprostol.
Magnesium levulinate The risk or severity of adverse effects can be increased when Magnesium levulinate is combined with Misoprostol.
Magnesium lactate The risk or severity of adverse effects can be increased when Magnesium lactate is combined with Misoprostol.

Target Protein

Prostacyclin receptor PTGIR
Prostaglandin E2 receptor EP3 subtype PTGER3
Prostaglandin E2 receptor EP2 subtype PTGER2
Prostaglandin E2 receptor EP1 subtype PTGER1
Prostaglandin E2 receptor EP4 subtype PTGER4

Referensi & Sumber

Synthesis reference: Salah Ahmed, Raj Mahajan, "Vaginal tablets comprising misoprostol and methods of making and using the same." U.S. Patent US20070071814, issued March 29, 2007.
Artikel (PubMed)
  • PMID: 3932043
    Schoenhard G, Oppermann J, Kohn FE: Metabolism and pharmacokinetic studies of misoprostol. Dig Dis Sci. 1985 Nov;30(11 Suppl):126S-128S. doi: 10.1007/bf01309397.
  • PMID: 27729972
    Turner JV, Agatonovic-Kustrn S, Ward H: Off-label use of misoprostol in gynaecology. Facts Views Vis Obgyn. 2015 Dec 28;7(4):261-264.
  • PMID: 30969695
    Krugh M, Maani CV: Misoprostol .
  • PMID: 31305043
    Speer L: Misoprostol Alone is Associated with High Rate of Successful First-Trimester Abortion. Am Fam Physician. 2019 Jul 15;100(2):119.
  • PMID: 27102981
    Frye LJ, Byrne ME, Winikoff B: A crossover pharmacokinetic study of misoprostol by the oral, sublingual and buccal routes. Eur J Contracept Reprod Health Care. 2016 Aug;21(4):265-8. doi: 10.3109/13625187.2016.1168799. Epub 2016 Apr 22.
  • PMID: 19587339
    Fjerstad M, Trussell J, Sivin I, Lichtenberg ES, Cullins V: Rates of serious infection after changes in regimens for medical abortion. N Engl J Med. 2009 Jul 9;361(2):145-51. doi: 10.1056/NEJMoa0809146.
  • PMID: 17963768
    Tang OS, Gemzell-Danielsson K, Ho PC: Misoprostol: pharmacokinetic profiles, effects on the uterus and side-effects. Int J Gynaecol Obstet. 2007 Dec;99 Suppl 2:S160-7. doi: 10.1016/j.ijgo.2007.09.004. Epub 2007 Oct 26.
  • PMID: 7650228
    Foote EF, Lee DR, Karim A, Keane WF, Halstenson CE: Disposition of misoprostol and its active metabolite in patients with normal and impaired renal function. J Clin Pharmacol. 1995 Apr;35(4):384-9.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 145 • International brands: 1
Produk
  • Act Diclo-miso
    Tablet, delayed release • - • Oral • Canada • Approved
  • Act Diclo-miso
    Tablet, delayed release • - • Oral • Canada • Approved
  • Arthrotec
    Tablet, film coated • - • Oral • US • Approved
  • Arthrotec
    Tablet, film coated • - • Oral • US • Approved
  • Arthrotec
    Tablet, film coated • - • Oral • US • Approved
  • Arthrotec
    Tablet, film coated • - • Oral • US • Approved
  • Arthrotec
    Tablet, film coated • - • Oral • US • Approved
  • Arthrotec
    Tablet, film coated • - • Oral • US • Approved
Menampilkan 8 dari 145 produk.
International Brands
  • Isprelor

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul