|
This information has been developed and provided by an independent third-party source. Merck & Co., Inc. does not endorse and is not responsible for the accuracy of the content, or for practices or
standards of non-Merck sources.
ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Medication Safety Issues
Sound-alike/look-alike issues:
Cytotec® may be confused with Cytoxan®, Sytobex®
Misoprostol may be confused with metoprolol, mifepristone
Pronunciation
(mye soe PROST ole)
U.S. Brand Names
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Prevention of NSAID-induced gastric ulcers; medical termination of pregnancy of ?49 days (in conjunction with mifepristone)
Use: Unlabeled/Investigational
Cervical ripening and labor induction; NSAID-induced nephropathy; fat malabsorption in cystic fibrosis
Pregnancy Risk Factor
X
Pregnancy Considerations
[U.S. Boxed Warning]: Not to be used in women of childbearing potential unless woman is capable of complying with effective contraceptive measures; therapy is normally begun on the second or third day of next normal menstrual period. Misoprostol is an abortifacient. During pregnancy, use to prevent NSAID-induced ulcers is contraindicated. Reports of fetal death, congenital anomalies, uterine perforation, and abortion have been received after the use of misoprostol in pregnancy.
Lactation
Excretion in breast milk unknown/contraindicated
Breast-Feeding Considerations
It is not known if misoprostol is excreted in human milk, however, because significant diarrhea may occur in a nursing infant, breast-feeding is contraindicated
Contraindications
Hypersensitivity to misoprostol, prostaglandins, or any component of the formulation; pregnancy (when used to reduce NSAID-induced ulcers)
Warnings/Precautions
Boxed warnings:
• Women of childbearing potential: See “Special populations” below.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease.
• Renal impairment: Use with caution in patients with renal impairment.
Special populations:
• Elderly: Use with caution in the elderly.
• Pediatrics: Safety and efficacy have not been established in children.
• Pregnancy: Uterine perforation and/or rupture have been reported in association with intravaginal use to induce labor or with combined oral/intravaginal use to induce abortion. The manufacturer states that Cytotec® should not be used as a cervical-ripening agent for induction of labor. However, The American College of Obstetricians and Gynecologists (ACOG) continues to support this off-label use.
• Women of childbearing potential: [U.S. Boxed Warning]: Not to be used in women of childbearing potential unless woman is capable of complying with effective contraceptive measures; therapy is normally begun on the second or third day of next normal menstrual period.
Adverse Reactions
>10%: Gastrointestinal: Diarrhea, abdominal pain
1% to 10%:
Central nervous system: Headache
Gastrointestinal: Constipation, flatulence, nausea, dyspepsia, vomiting
<1%: Cramps, uterine stimulation, vaginal bleeding
Postmarketing and/or case reports: Abnormal taste, abnormal vision, alkaline phosphatase increased, alopecia, anaphylaxis, anemia, amylase increase, anxiety, appetite changes, arrhythmia, arterial thrombosis, arthralgia, back pain, breast pain, bronchospasm, cardiac enzymes increased, chest pain, confusion, deafness, depression, dermatitis, diaphoresis, drowsiness, dysphagia, dyspnea, earache, edema, epistaxis, ESR increased, fetal or infant death (when used during pregnancy), fever, GI bleeding, GI inflammation, gingivitis, glycosuria, gout, hyper-/hypotension, impotence, loss of libido, MI, muscle cramps, myalgia, neuropathy, neurosis, nitrogen increased, pallor, phlebitis, pulmonary embolism, purpura, rash, reflux, rigors, stiffness, syncope, thirst, thrombocytopenia, tinnitus, uterine rupture, weakness, weight changes
Drug Interactions
Oxytocin: Misoprostol may enhance the therapeutic effect of Oxytocin. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Food: Misoprostol peak serum concentrations may be decreased if taken with food (not clinically significant).
Storage
Store at or below 25°C (77°F).
Mechanism of Action
Misoprostol is a synthetic prostaglandin E1 analog that replaces the protective prostaglandins consumed with prostaglandin-inhibiting therapies (eg, NSAIDs); has been shown to induce uterine contractions
Pharmacodynamics/Kinetics
Absorption: Rapid
Metabolism: Hepatic; rapidly de-esterified to misoprostol acid (active)
Half-life elimination: Metabolite: 20-40 minutes
Time to peak, serum: Active metabolite: Fasting: 15-30 minutes
Excretion: Urine (64% to 73%) and feces (15%) within 24 hours
Dosage
Oral:
Children 8-16 years: Fat absorption in cystic fibrosis (unlabeled use): 100 mcg 4 times/day
Adults:
Prevention of NSAID-induced gastric ulcers: 200 mcg 4 times/day with food; if not tolerated, may decrease dose to 100 mcg 4 times/day with food or 200 mcg twice daily with food; last dose of the day should be taken at bedtime
Medical termination of pregnancy: Refer to Mifepristone monograph.
Intravaginal: Adults: Labor induction or cervical ripening (unlabeled uses): 25 mcg (1/4 of 100 mcg tablet); may repeat at intervals no more frequent than every 3-6 hours. Do not use in patients with previous cesarean delivery or prior major uterine surgery.
Administration: Oral
Incidence of diarrhea may be lessened by having patient take dose right after meals. Therapy is usually begun on the second or third day of the next normal menstrual period.
Dietary Considerations
Should be taken with food; incidence of diarrhea may be lessened by having patient take dose right after meals.
Patient Education
Take as directed; continue taking your NSAIDs while taking this medication. Take with meals or after meals to prevent nausea, diarrhea, and flatulence. Avoid using antacids. You may experience increased menstrual pain, or cramping; request analgesics. Report abnormal menstrual periods, spotting (may occur even in postmenstrual women), or severe menstrual bleeding. Pregnancy/breast-feeding precautions: When used to prevent NSAID-induced ulcers: Inform prescriber if you are pregnant. This drug should not be used in the 2nd or 3rd trimester of pregnancy. Do not get pregnant during or for 1 month following therapy. Male: Do not cause a female to become pregnant. Male/female: Consult prescriber for instruction on appropriate contraceptive measures if necessary or if you suspect you might be pregnant. This drug may cause severe fetal defects, miscarriage, or abortion; do not share medication with others. Do not breast-feed.
Geriatric Considerations
Elderly, due to extensive use of NSAIDs and the high percentage of asymptomatic hemorrhage and perforation from NSAIDs, are at risk for NSAID-induced ulcers and may be candidates for misoprostol use. However, routine use for prophylaxis is not justified. Patients must be selected upon demonstration that they are at risk for NSAID-induced lesions. Misoprostol should not be used as a first-line therapy for gastric or duodenal ulcers.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
None reported
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Assess knowledge/teach appropriate antiulcer diet and lifestyle. Monitor renal function and fluid balance. Pregnancy risk factor X: Determine that patient is not pregnant before beginning treatment and do not give to women of childbearing age or to males who may have intercourse with women of childbearing age unless both male and female are capable of complying with contraceptive measures during therapy and for 1 month following therapy.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 100 mcg, 200 mcg
Pricing: U.S. (www.drugstore.com)
Tablets (Cytotec)
100 mcg (60): $72.76
200 mcg (60): $104.99
Tablets (Misoprostol)
100 mcg (60): $39.99
200 mcg (60): $56.99
References
“Induction of Labor,” American College of Obstetricians and Gynecologists, ACOG Practice Guidelines Bulletin 10, Washington, DC; ACOG, 1999.
“Induction of Labor With Misoprostol,” American College of Obstetricians and Gynecologists, ACOG Committee Opinion 228, Washington, DC; ACOG, 1999.
Cleghorn GJ, Shepherd RW, and Holt TL, “The Use of a Synthetic Prostaglandin E1 Analogue (Misoprostol) as an Adjunct to Pancreatic Enzyme Replacement in Cystic Fibrosis,” Scand J Gastroenterol Suppl, 1988, 143:142-7.
Robinson PJ, Smith AL, and Sly PD, “Duodenal pH in Cystic Fibrosis and Its Relationship to Fat Malabsorption,” Dig Dis Sci, 1990, 35(10):1299-304.
Walt RP, “Misoprostol for the Treatment of Peptic Ulcer and Anti-inflammatory Drug-Induced Gastroduodenal Ulceration,” N Engl J Med, 1992, 327(22):1575-80.
Wing, DA, “Labor Induction With Misoprostol,” Am J Obstet Gynecol, 1999, 181(2):339-45.
International Brand Names
Lexi-Comp.com
Last full review/revision February 2009
|
