misoprostol (Cytotec)
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Introduction
Tradename: Cytotec.
Indications
- prevention of NSAID-induced ulcers[6]
- short term treatment of more active duodenal & peptic ulcers
- tablets may be used vaginally to induce labor[5]
- cervical ripening[7]
- postpartum hemorrhage[7]
- tablets may be used by buccal route in combination with mifepristone to induce abortion
Contraindications
Dosage
- 200 ug PO QID with food
- 400 ug buccal once in combination with mifepristone to induce abortion
Tabs: 100 ug, 200 ug.
Pharmacokinetics
- completely absorbed from the GI tract
- undergoes extensive 1st pass metabolism to an active metabolite misoprostol acid
- elimination 1/2life is 20-40 minutes, increased in patients with renal insufficiency
- NO dosage adjustment necessary with renal insufficiency or in geriatric patients
elimination via liver
elimination via kidney
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- nausea/vomiting, uterine stimulation, vaginal bleeding
Mechanism of action
- prostaglandin E1 analog that inhibits gastric acid secretion by inhibiting activation of adenylate cyclase in gastric parietal cells by histamine
- protects the gastric mucosa from irritants
- produces uterine contraction which may be harmful during pregnancy
- may inhibit the ability of human CML stem cells to self-renew[2]
More general terms
Additional terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 2.0 2.1 O'Neil A. Evidence for New Method of Eradicating Residual CML Precursors. Targeting mitochondrial oxidative phosphorylation may help prevent CML relapse. MedPage Today. Jan 31, 2018 https://www.medpagetoday.com/reading-room/asco/hematologic-malignancies/70855
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 5.0 5.1 Prescriber's Letter 13(10): 2006 Alternative or 'Off-label' Routes of Drug Administration Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=221012&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 Fujimori S et al Prevention of nonsteroidal anti-inflammatory drug-induced small-intestinal injury by prostaglandin: A pilot randomized controlled trial evaluated by capsule endoscopy. Gastrointest Endosc 2009 Jun; 69:1339. PMID: https://www.ncbi.nlm.nih.gov/pubmed/19243767
- ↑ 7.0 7.1 7.2 Deprecated Reference