II. Indications
-
Peptic Ulcer Disease Prevention
- See NSAID Gastrointestinal Adverse Effects
- Prevents ulcers in those on NSAIDs chronically
- Cervical Ripening agent in Pregnancy Labor Induction
- Termination of Pregnancy (<77 days)
- Early Pregnancy Loss (<84 days)
III. Contraindications
- Factors that increase risk for Uterine Rupture
- Prior Cesarean Section
- Multigravida with >=5 prior pregnancies (relative contraindication)
IV. Mechanism
- See Prostaglandin
- Misoprostol is a synthetic Prostaglandin E1 (PGE1) Analog
- Misoprostol is a pro-drug, that when taken orally is de-esterified to its active acid
- Misoprostol activity as a PGE1 Analog is local at the Uterus and gastric mucosa with non-toxic doses
- Contrast with systemic PGE1 effects absent with Misoprostol (e.g. vasodilation, bronchodilation)
-
Prostaglandin E1 (PGE1) Local Effects
- Cervical Ripening and uterine contractions
- Gastric Mucosa Protection by Prostaglandin replacement
- Inhibits gastric acid and pepsin secretion (dose dependent)
- Bolsters mucosal resistance to injury
V. Medications
- Misoprostol (Cytotec) oral tablets: 100 mcg, 200 mcg
- Oral tablets may be used intravaginally
VI. Dosing: Prevention of NSAID-induced Peptic Ulcer Disease
- See NSAID Gastrointestinal Adverse Effects
- Option 1: 100 to 200 mcg four times daily with food
- Option 2: 200 mcg orally twice daily with food
- Better tolerated than four times per day dosing
VII. Dosing: Obstetrics and Gynecology
-
Cervical Ripening
- See Cervical Ripening for complete protocol
- Misoprostol 50 mcg per vagina every 6 hours (or 25 mcg every 3 hours)
- Monitor for uterine hyperstimulation and Fetal Heart Rate
- Avoid after prior Cesarean Section, Multigravida (>=5 prior pregnancies)
- Risk of Uterine Rupture
-
Early Pregnancy Loss (<84 days) or Termination of Pregnancy (<77 days)
- See Early Pregnancy Loss (includes precautions and monitoring protocol)
- See Mifepristone and Misoprostol Protocol for Early Pregnancy Loss
- Misoprostol Dosing Protocol
- Vaginal (or rectal)
- Place 800 mcg (4 tablets) intravaginally at 24-48 hours after Mifepristone
- Lie supine for 30 minutes after dose
- Buccal Dosing may be used in place of vaginal dosing
- Place two of the 200 mcg Misoprostol tablets on each side of the mouth (total 800 mcg)
- Allow tablets to dissolve over 30 minutes
- Efficacy improves if followed by second dose Misoprostol 800 mcg 4 hours after first
- Vaginal (or rectal)
- Strong uterine cramping and heavier Vaginal Bleeding follows Misoprostol dose
- Onset within several hours
- Persists for 3-5 hours
- Lighter Vaginal Bleeding may persist for 9-16 days
- Adjunctive medications
- NSAIDs
- Heating pad
VIII. Pharmacokinetics
- Rapid oral absorption
- Serum level peaks within 30 min of oral dose
- Elimination half life (including metabolites): <2 hours
IX. Safety
- Pregnancy Category X (aside from peripartum Cervical Ripening, pregnancy loss)
- Avoid in Lactation
X. Adverse Effects
- See Misoprostol Poisoning
- When used orally (poorly tolerated)
- Diarrhea
- Nausea
- Vomiting
- Abdominal cramping
- Flatulence
- Gynecologic symptoms (800 mcg dosing)
- Strong uterine cramping
- Vaginal Bleeding heavier than typical Menses
XI. Efficacy: Peptic Ulcer Disease reduction
- Dosing four times daily: 4% Peptic Ulcer Disease recurrence
- Dosing twice daily: 8% Peptic Ulcer Disease recurrence
- Placebo: 16% Peptic Ulcer Disease recurrence
- Reference
XII. Resources
XIII. References
Images: Related links to external sites (from Bing)
Related Studies
| misoprostol (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| MISOPROSTOL 100 MCG TABLET | Generic | $0.46 each |
| MISOPROSTOL 200 MCG TABLET | Generic | $0.74 each |