Misoprostol

Misoprostolis aprescription drugused to reducing the risk ofNSAID(nonsteroidalanti-inflammatory drugs, includingaspirin)–inducedgastriculcersinpatients at high risk of complications fromgastric ulcer, such as the elderly and patients with concomitant debilitatingdisease, as well as patients at high risk of developing gastriculceration, such as patients with a history ofulcer.

• Misoprostol has not been shown to reduce the risk ofduodenalulcers in patients takingNSAIDs.
• Misoprostol should be taken for the duration of NSAIDtherapy.
• Misoprostol has been shown to reduce the risk of gastric ulcers in controlled studies of 3 months duration. It had no effect, compared toplacebo, ongastrointestinalpainor discomfort associated with NSAID use.

Misoprostol is available under the following different brand names:Cytotec.

Dosages of Misoprostol:

Adult andPediatricDosage

Tablet

• 100 mcg
• 200 mcg

Dosage Considerations– Should be Given as Follows:

NSAID-Induced Ulcer

Adult

Prophylaxis

• 200 mcg orally every 6 hours withfood; may be decreased to 100 mcg every 6 hours if higher dose is not tolerated; last dose to be administered at bedtime
• Should take therapy for duration of therapy

Geriatric

• To avoid possibility ofdiarrhea, dosing may be initiated at 100 mcg every 6 hours and increased by 100 mcg/day every 3 days until desired dose is achieved

PregnancyTermination

• Seemifepristone(Mifeprex) drug monograph forFDAapproved dosageregimen

StressUlcer Prophylaxis (off-label)

• 100-200 mcg orally every 4-6 hours

Induction ofLabor(off-label)

• 25 mcg (1/4 of 100 mcgoraltablet) intravaginally initially, thenrepeatat intervals not to exceed every 3-6 hours

Not to be used in patients with previous cesarean delivery ormajoruterinesurgery

PostpartumHemorrhage(off-label)

• Prophylaxis: 600 mcg orally within 1 minute of delivery
• Treatment: 800 mcg orally once; use caution ifprophylacticdose already given and adverse effects present or observed
• Use only in settings whereoxytocinnot available

Treatment of IncompleteAbortion(off-label)

• 600 mcg buccally (dissolved in themouth) once

FatAbsorptioninCystic FibrosisPatients (off-label)

Pediatric

• Children under 8 years: safety and efficacy not established
• Children 8 years and older: 100 mcg orally every 6 hours

Dosage Modifications

Renalimpairment

• Use with caution; peakplasma浓度,半衰期和生物利用度be increased, but it is not clear whether these increases are of临床relevance

Side effects of misoprostol include:

• diarrhea
• abdominal pain
• headache
• severeallergic reaction(anaphylaxis)
• anemia
• abnormalheartbeat
• chest pain
• gas (flatulence)
• gastrointestinal bleeding
• hearing loss
• heart attack(myocardial infarction)
• nausea
• vomiting
• constipation
• 破裂ofuterus
• blood clots
• stroke
• spotting
• menstrual cramps
• disruption in normalmenstrualflow
• menstrual disorder
• painful periods
• aches/pains
• abnormal physical weakness
• fatigue
• fever
• chills
• sudden feeling of cold accompanied by a rise intemperature
• weight changes
• rash
• dermatitis,eczema
• hair loss
• pale appearance
• breast pain
• abnormaltaste
• abnormal vision
• pinkeye(conjunctivitis)
• ringing in the ears(tinnitus)
• earache
• upperrespiratorytractinfection
• bronchitis
• difficultybreathing
• pneumonia
• nosebleed
• swelling (edema)
• sweating
• low blood pressure(hypotension)
• high blood pressure(hypertension)
• irregular heartbeat (arrhythmia)
• inflammationofvein
• increasedcardiacenzymes
• fainting(syncope)
• rectaldisorders (hemorrhoids, abscesses, fissures orcancer)
• abnormalliverandgallbladderfunction
• 牙龈的炎症(gingivitis)
• reflux
• difficulty swallowing
• increasedbloodlevel ofamylaseenzyme
• excess sugar in theurine
• inflammatoryarthritis(gout)
• increased blood level ofnitrogen
• increased blood level ofalkaline phosphatase(ALP)
• abnormal large volume of dilute urine
• painful ordifficult urination
• blood in the urine
• urinary tract infection
• anxiety
• loss of appetite
• depression
• drowsiness
• dizziness
• thirst
• impotence
• loss of sex drive (libido)
• numbness or weakness
• neurosis(symptoms of stress: depression, anxiety, obsessive behavior,hypochondria)
• confusion
• jointpain
• musclepain
• muscle cramps
• stiffness
• back pain
• low bloodplatelets(thrombocytopenia)
• rash with purple spots on theskin
• increased红细胞sedimentation rate(ESR) in the blood

This document does not contain all possible side effects and others may occur. Check with yourphysicianfor additional information about side effects.

If yourdoctorhas directed you to use thismedication, your doctor or药剂师may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor,healthcare provider or pharmacist first.

Misoprostol has no known severe interactions with other drugs.

Misoprostol has no known serious interactions with other drugs.

Moderate interactions of misoprostol include:

• croelemer
• eluxadoline

Misoprostol has no known mild interactions with other drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

Warnings

• Bacterialinfections reported after use
• Patients must seek medicalattentionif excessive bleeding occurs
• Administration topregnantwomen can cause abortion,premature birth, or birth defects
• Uterine rupturehas been reported when drug is administered to pregnant women to induce labor; risk of uterine rupture increases with advancing gestational ages and prior uterine surgery, including cesarean delivery
• Contraindicated in pregnant women to reducepeptic ulcerrisk from nonsteroidal anti-inflammatory drugs (NSAIDs)
• Warn patients of risk for abortion, and warn them not to give drug to others
• Use in women of childbearing potential:
• Do not use for reducing risk of NSAID-induced ulcers in women of childbearing potential unlesspatientis at high risk forcomplicationfrom gastric ulcers; may be prescribed in the following situations:
• Patient has negativeserumpregnancy test result within 2 weeks before initiation of therapy
• Patient is capable of complying with effective contraceptive measures
• Patient has received both oral and written warnings about misoprostol hazards, risk of possible contraception failure, and danger to other women of childbearing potential should drug be taken by mistake
• Patient will begin misoprostol only on day 2 or 3 of next normal menstrual period

This medication contains misoprostol. Do not take Cytotec if you are allergic to misoprostol or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact aPoison Control Centerimmediately.

Contraindications

• Pregnancy when used to reduce risk of NSAID-induced ulcers.
• Hypersensitivity to misoprostol, prostaglandins, orprostaglandinanalogues

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Misoprostol?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Misoprostol?"

Cautions

• May cause diarrhea; should not be coadministered with other drugs that cause diarrhea (magnesium-containing antacids)
• Adequate contraception is required in women of childbearing age
• May cause severe allergic (anaphylactic) reaction
• May cause chills
• Unknown whether drug is safe for use in women with severe anemia
• Misoprostol may cause birth defects, abortion (sometimes incomplete), premature labor or rupture of the uterus if given to pregnant women
• Safety and efficacy in patients withcardiovascular disease,diabetes,kidney(renal) impairment, or respiratory disease are not established
• Use with caution in women over 35 years or heavy smokers (these patients were not included in临床trials)

Off-label use

• Forhospitaluse only if used off label forcervicalripening, induction of labor, or treatment of serious postpartum hemorrhage
• Uterine activity and fetal status should be monitored by trained obstetric personnel in hospital setting
• May be associated withmeconiumpassage, meconium staining ofamniotic fluid, and cesarean delivery
• Maternalshock, maternaldeath, fetalbradycardia, and fetal death have been reported

Pregnancy andLactation

• Do not use misoprostol during pregnancy
• The risks involved outweigh potential benefits
• Safer alternatives exist
• Breastfeeding: misoprostol is rapidly metabolized inmotherto misoprostol acid, which is biologically active and is excreted inbreast milk; although no published reports of adverse effects of misoprostol in breastfeeding infants exist, caution should be exercised when misoprostol is administered to breastfeeding women