MISOPROSTOL MODE OF ACTION
Misoprostol, a prostaglandin analogue, binds to myometrial cells to cause strong myometrial contractions leading to expulsion of tissue. This agent also causes cervical ripening with softening and dilation of the cervix. Misoprostol binds to and stimulates prostaglandin EP2 receptors, prostaglandin EP3 receptor and prostaglandin EP4 receptor but not Prostaglandin EP1 receptor and therefore is expected to have a more restricted range of physiological and potentially toxic actions than prostaglandin E2 or other analogs which activate all four prostaglandin receptors
Misoprostol in Kenya
Brands of Misoprostol in Kenya:
Cytotec®, Pfizer Laboratories Limited
Isovent®, Square Pharmaceuticals Ltd.
Kontrac® , Fourrts (India) Laboratories Private Limited
Miso-Kare®, Naari PTE Limited
Misoprost®, Cipla Limited
Vagiprost® , ADWIA
- 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, e.g., 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. Misoprostol has not been shown to reduce the risk of duodenal ulcers in patients taking NSAIDs. Misoprostol should be taken for the duration of NSAID therapy. Misoprostol has been shown to reduce the risk of gastric ulcers in controlled studies of 3 months’ duration. It had no effect, compared to placebo, on gastrointestinal pain or discomfort associated with NSAID use.
- Labour induction:
Misoprostol is commonly used for labor induction. It causes uterine contractions and the ripening (effacement or thinning) of the cervix.
Oxytocin has long been used as the standard agent for labor induction, but does not work well when the cervix is not yet ripe. Misoprostol also may be used in conjunction with oxytocin
- Medical Abortion
Misoprostol is used either alone or in conjunction with another medication (mifepristone or methotrexate) for medical abortions as an alternative to surgical abortion. Medical abortion has the advantage of being less invasive.
Misoprostol is most effective when it is used with methotrexate or mifepristone (RU-486).
- Failed miscarriage
Misoprostol may be used to treat the mother in the case of fetal death which did not result in miscarriage.
- Postpartum bleeding
Misoprostol is also used to prevent and treat post-partum bleeding. Orally administered misoprostol was marginally less effective than oxytocin.The use of rectally administered misoprostol is optimal in cases of bleeding; it was shown to be associated with lower rates of side effects compared to other routes.
MISOPROSTOL ADMINISTRATION TO WOMEN WHO ARE PREGNANT CAN CAUSE BIRTH DEFECTS, ABORTION, OR PREMATURE BIRTH. UTERINE RUPTURE HAS BEEN REPORTED WHEN MISOPROSTOL TABLETS WERE ADMINISTERED IN PREGNANT WOMEN TO INDUCE LABOR OR TO INDUCE ABORTION BEYOND THE EIGHTH WEEK OF PREGNANCY (see also PRECAUTIONS and LABOR AND DELIVERY). MISOPROSTOL TABLETS SHOULD NOT BE TAKEN BY PREGNANT WOMEN TO REDUCE THE RISK OF ULCERS INDUCED BY NONSTEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDs) (see CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS).
PATIENTS MUST BE ADVISED OF THE ABORTIFACIENT PROPERTY AND WARNED NOT TO GIVE THE DRUG TO OTHERS.
Misoprostol should not be used for reducing the risk of NSAID-induced ulcers in women of childbearing potential unless the patient is at high risk of complications from gastric ulcers associated with use of the NSAID, or is at high risk of developing gastric ulceration. In such patients, Misoprostol may be prescribed if the patient has had a negative serum pregnancy test within 2 weeks prior to beginning therapy.
is capable of complying with effective contraceptive measures. has received both oral and written warnings of the hazards of Misoprostol , the risk of possible contraception failure, and the danger to other women of childbearing potential should the drug be taken by mistake.
will begin Misoprostol only on the second or third day of the next normal menstrual period.
ADVERSE DRUG REACTION
Body as a whole: aches/pains, asthenia, fatigue, fever, chills, rigors, weight changes.
Skin: rash, dermatitis, alopecia, pallor, breast pain.
Special senses: abnormal taste, abnormal vision, conjunctivitis, deafness, tinnitus, earache.
Respiratory: upper respiratory tract infection, bronchitis, bronchospasm, dyspnea, pneumonia, epistaxis.
Cardiovascular: chest pain, edema, diaphoresis, hypotension, hypertension, arrhythmia, phlebitis, increased cardiac enzymes, syncope, myocardial infarction (some fatal), thromboembolic events (e.g., pulmonary embolism, arterial thrombosis, and CVA).
Gastrointestinal: GI bleeding, GI inflammation/infection, rectal disorder, abnormal hepatobiliary function, gingivitis, reflux, dysphagia, amylase increase.
Hypersensitivity: anaphylactic reaction
Metabolic: glycosuria, gout, increased nitrogen, increased alkaline phosphatase.
Genitourinary: polyuria, dysuria, hematuria, urinary tract infection.
Nervous system/Psychiatric: anxiety, change in appetite, depression, drowsiness, dizziness, thirst, impotence, loss of libido, sweating increase, neuropathy, neurosis, confusion.
Musculoskeletal: arthralgia, myalgia, muscle cramps, stiffness, back pain.
anemia, abnormal differential, thrombocytopenia, purpura, ESR increased.
MISOPROSTOL DRUG INTERACTIONS:
- Misoprostol is predominantly metabolised via fatty acid oxidising systems and has shown no adverse effect on the hepatic microsomal mixed function oxidase (P450) enzyme system.
- A decrease of the efficacy of misoprostol can theoretically occur due to the antiprostaglandin properties of non-steroidal anti-inflammatory drugs (NSAIDs) including aspirin (acetyl salicylic acid). Limited evidence suggests that co-administration of NSAIDs on the day of misoprostol administration does not adversely influence the effects of mifepristone or misoprostol on cervical ripening or uterine contractility and does not reduce the clinical efficacy of medical termination of pregnancy.
- Antacids may decrease the bioavailability of misoprostol.
- Antacids containing magnesium may aggravate diarrhoea caused by misoprostol.
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Clinical | Pharmacokinetic data
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