Contents

Search

misoprostol (Cytotec)

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 - used alone to induce abortion [8] Contraindications: pregnancy (abortifacient) Dosage: - 200 ug PO QID with food - 400 ug buccal once in combination with mifepristone to induce abortion - misoprostol 800 ug alone administered buccally, sublingually vaginally every 3 hours for >= 3 doses [8] Tabs: 100 ug, 200 ug. Pharmacokinetics: 1) completely absorbed from the GI tract 2) undergoes extensive 1st pass metabolism to an active metabolite misoprostol acid 3) elimination 1/2life is 20-40 minutes, increased in patients with renal insufficiency 4) NO dosage adjustment necessary with renal insufficiency or in geriatric patients Adverse effects: 1) common (> 10%) - diarrhea, abdominal pain 2) less common (1-10%) - constipation, flatulence, headache 3) uncommon (< 1%) - nausea/vomiting, uterine stimulation, vaginal bleeding Mechanism of action: 1) prostaglandin E1 analog that inhibits gastric acid secretion by inhibiting activation of adenylate cyclase in gastric parietal cells by histamine 2) protects the gastric mucosa from irritants 3) produces uterine contraction which may be harmful during pregnancy 4) may inhibit the ability of human CML stem cells to self-renew [2]

Related

alprostadil (Muse, Caverject, Edex, Prostin VR pediatric, Topiglan, Befar)

General

antiulcer agent prostaglandin E1

Properties

SIZE: MW = 306.5 G/MOL COMPARTMENT: membrane MISC-INFO: elimination route LIVER KIDNEY pregnancy-category X safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. 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
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Prescriber's Letter 13(10): 2006 Alternative or 'Off-label' Routes of Drug Administration Detail-Document#: 221012 (subscription needed) http://www.prescribersletter.com
  6. 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: 19243767
  7. Deprecated Reference
  8. Moseson H et al How Effective Is Misoprostol Alone for Medication Abortion? NEJM Evid. 2024 Jun;3(6):EVIDccon2300129 PMID: 38804786 Review. https://evidence.nejm.org/doi/full/10.1056/EVIDccon2300129

Component-of

diclofenac/misoprostol (Arthrotec)