Pharmaceutical Name

Trade (marketing or proprietary) name: Cytotec®

Generic (nonproprietary or active ingredient) name: Misoprostol

Indication and Usage

Reason the product has been approved for sale on the market.

Cytotec® (misoprostol) is indicated for reducing the risk of NSAID (nonsteroidal anti-inflammatory drugs, including aspirin)-induced gastric ulcers in patients at high risk of complications from gastric ulcer, eg, the elderly and patients with concomitant debilitating disease, as well as patients at high risk of developing gastric ulceration, such as patients with a history of ulcer. It is not approved by the FDA as a labor induction method.

Manufacturer Insert

Ingredients

Also known as “excipients” for vaccines.

Cytotec® (misoprostol) contains: 100 mcg or 200 mcg of misoprostol (a synthetic prostaglandin E1 analog), hydrogenated castor oil, hydroxypropyl methylcellulose, microcrystalline cellulose, and sodium starch glycolate.

Contraindications

Per the FDA, contraindications are conditions in a recipient that increases the risk for a serious adverse reaction. Product should not be administered when a patient has a listed contraindication.

Cytotec should not be taken by pregnant women to reduce the risk of ulcers induced by non-steroidal anti-inflammatory drugs (NSAIDs). Cytotec should not be taken by anyone with a history of allergy to prostaglandins.

Warnings and Precautions

Per the FDA, warnings are clinically significant adverse reactions or risks. According to the CDC, a precaution is a condition in a recipient that might increase the risk for a serious adverse reaction, might cause diagnostic confusion, or might compromise the effectiveness of the product. In general, a product should be deferred when a precaution is present.

Women of childbearing potential using Cytotec to decrease the risk of NSAID induced ulcers should be told that they must not be pregnant when Cytotec therapy is initiated, and they must use an effective contraception method while taking Cytotec.

Manufacturer-Listed Adverse Reactions

Per the CDC, adverse reactions are an undesirable medical condition that has been demonstrated to be caused by a vaccine. Evidence for the causal relation is usually obtained through randomized clinical trials, controlled epidemiologic studies, isolation of the vaccine strain from the pathogenic site, or recurrence of the condition with repeated vaccination (i.e., rechallenge); synonyms include side effect and adverse effect.

Aches/pains, Asthenia (weakness), Fatigue, Fever, Rigors, Weight changes, Rash, Dermatitis, Alopecia (hair loss), Pallor, Breast/chest pain, Abnormal taste/vision, Conjunctivitis, Syncope (fainting), Deafness, Tinnitus (ringing ears), Earache, Upper respiratory tract infection, Bronchitis, Bronchospasm, Dyspnea (shortness of breath), Pneumonia, Epistaxis (nosebleed), Edema, Diaphoresis, Reflux, Hypotension/hypertension, Arrhythmia, Phlebitis, Increased cardiac enzymes, GI bleeding, GI inflammation/infection, Rectal disorder, Abnormal hepatobiliary function, Gingivitis, Dysphagia (difficulty swallowing), Amylase increase, Anaphylaxis, Glycosuria (sugar in the urine), Gout, Increased nitrogen, Increased alkaline phosphatase, Polyuria (large urine production), Dysuria (painful urination), Hematuria (blood in urine), Urinary tract infection, Abnormal differential, Neuropathy, Neurosis, Confusion, Arthralgia (joint stiffness), Myalgia (muscle pain), Muscle cramps, Stiffness, Back pain, Anemia, Anxiety, Change in appetite, Depression, Drowsiness, Dizziness, Impotence, Loss of libido, Sweating increase, Purpura, ESR increased, and Thrombocytopenia

Specific Populations

Pregnancy

Pregnancy: Pregnancy Category X.
Teratogenic effects: See boxed WARNINGS. Congenital anomalies sometimes associated with fetal death have been reported subsequent to the unsuccessful use of misoprostol as an abortifacient but the drug’s teratogenic mechanism has not been demonstrated. Several reports in the literature associate the use of misoprostol during the first trimester of pregnancy with skull defects, cranial nerve palsies, facial malformations, and limb defects.

Nonteratogenic effects: See boxed WARNINGS. Cytotec may endanger pregnancy (may cause abortion) and thereby cause harm to the fetus when administered to a pregnant woman. Cytotec may produce uterine contractions, uterine bleeding, and expulsion of the products of conception. Abortions caused by Cytotec may be incomplete. If a woman is or becomes pregnant while taking this drug to reduce the risk of NSAID induced ulcers, the drug should be discontinued and the patient apprised of the potential hazard to the fetus.

Cytotec can induce or augment uterine contractions. Vaginal administration of Cytotec, outside of its approved indication, has been used as a cervical ripening agent, for the induction of labor and for treatment of serious postpartum hemorrhage in the presence of uterine atony. A major adverse effect of the obstetrical use of Cytotec is hyperstimulation of the uterus which may progress to uterine tetany with marked impairment of uteroplacental blood flow, uterine rupture (requiring surgical repair, hysterectomy, and/or salpingo-oophorectomy), or amniotic fluid embolism. Pelvic pain, retained placenta, severe genital bleeding, shock, fetal bradycardia, and fetal and maternal death have been reported.

There may be an increased risk of uterine tachysystole, uterine rupture, meconium passage, meconium staining of amniotic fluid, and Cesarean delivery due to uterine hyperstimulation with the use of higher doses of Cytotec; including the manufactured 100 mcg tablet. The risk of uterine rupture increases with advancing gestational ages and with prior uterine surgery, including Cesarean delivery. Grand multiparity also appears to be a risk factor for uterine rupture.

The effect of Cytotec on the later growth, development, and functional maturation of the child when Cytotec is used for cervical ripening or induction of labor have not been established. Information on Cytotec’s effect on the need for forceps delivery or other intervention is unknown.

Breastfeeding

It is unlikely that Cytotec is excreted in human milk since it is rapidly metabolized
throughout the body. However, it is not known if the active metabolite (misoprostol acid) is excreted in human milk. Therefore, Cytotec should not be administered to nursing mothers because the potential excretion of misoprostol acid could cause significant diarrhea in nursing infants.

Fertility

Misoprostol, when administered to breeding male and female rats at doses 6.25 times to 625 times the maximum recommended human therapeutic dose, produced dose-related pre- and post-implantation losses and a significant decrease in the number of live pups born at the highest dose. These findings suggest the possibility of a general adverse effect on fertility in males and females.

Pediatric

Safety and effectiveness of Cytotec in pediatric patients have not been established.

Mechanism of Action

This is the specific biochemical interaction through which a drug or vaccine substance produces its pharmacological effect. This section also includes the minimum protective level designated for a certain disease.

Misoprostol has both antisecretory (inhibiting gastric acid secretion) and (in
animals) mucosal protective properties. NSAIDs inhibit prostaglandin synthesis, and a deficiency of prostaglandins within the gastric mucosa may lead to diminishing bicarbonate and mucus secretion and may contribute to the mucosal damage caused by these agents. Misoprostol can increase bicarbonate and mucus production, but in man this has been shown at doses 200 mcg and above that are also antisecretory. It is therefore not possible to tell whether the ability of misoprostol to reduce the risk of gastric ulcer is the result of its antisecretory effect, its mucosal protective effect, or both.

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