CAS:59122-46-2 Misoprostol

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Introduction                                            

Misoprostol, sold under the brandname Cytotec among others, is a medication used to start labor, cause an abortion, prevent and treat stomach ulcers, and treat postpartum bleeding due to poor contraction of the uterus.For abortions it is often used with mifepristone or methotrexate.By itself effectiveness for this purpose is between 66% and 90%.It is taken either by mouth, under the tongue, or placed in the vagina.

Common side effects include diarrhea and abdominal pain. It is pregnancy category X meaning that it is known to result in negative outcomes for the baby if taken during pregnancy. Uterine rupture may occur. It is a prostaglandin analogue — specifically, a synthetic prostaglandin E1 (PGE1).
 

Misoprostol was developed in 1973.It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.It is available as a generic medication.The wholesale cost in the developing world is about 0.36 to 2.00 USD a dose.A months supply to treat stomach ulcers in the United States is between 100 and 200 USD.The same costs between 30 and 55 EUR in Europe.

Function                                                  

Misoprostol is used for the prevention of NSAID-induced gastric ulcers. It acts upon gastric parietal cells, inhibiting the secretion of gastric acid by G-protein coupled receptor-mediated inhibition of adenylate cyclase, which leads to decreased intracellular cyclic AMP levels and decreased proton pump activity at the apical surface of the parietal cell. Because other classes of drugs, especially H2-receptor antagonists and proton pump inhibitors, are more effective for the treatment of acute peptic ulcers, misoprostol is only indicated for use by people who are both taking NSAIDs and are at high risk for NSAID-induced ulcers, including the elderly and people with ulcer complications. Misoprostol is sometimes coprescribed with NSAIDs to prevent their common adverse effect of gastric ulceration (e.g. with diclofenac in Arthrotec).

Misoprostol has other protective actions, but is only clinically effective at doses high enough to reduce gastric acid secretion. For instance, at lower doses, misoprostol may stimulate increased secretion of the protective mucus that lines the gastrointestinal tract and increase mucosal blood flow, thereby increasing mucosal integrity. However, these effects are not pronounced enough to warrant prescription of misoprostol at doses lower than those needed to achieve gastric acid suppression.

However, even in the treatment of NSAID-induced ulcers, omeprazole proved to be at least as effective as misoprostol,[10] but was significantly better tolerated, so misoprostol should not be considered a first-line treatment. Misoprostol-induced diarrhea and the need for multiple daily doses (typically four) are the main issues impairing compliance with therapy.

Application                                             

Misoprostol is used for self-induced abortions in Brazil, where black market prices exceed US$100 per dose. Illegal medically unsupervised misoprostol abortions in Brazil are associated with a lower complication rate than other forms of illegal self-induced abortion, but are still associated with a higher complication rate than legal, medically supervised surgical and medical abortions. Failed misoprostol abortions are associated with birth defects in some cases.Poor immigrant populations in New York City have also been observed to use self-administered misoprostol to induce abortions, as this method is much cheaper than a surgical abortion (about $2 per dose).The drug is readily available in Mexico.Use of misoprostol has also increased in Texas in response to increased regulation of abortion providers.

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