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|Other Name::||DL-MISOPROSTOL; Misoprostol; MISOPROSTOL ACID; Misogon; CYTOTEC;||Appearance::||Light Yellow Viscous Liquid|
|Application::||Prostaglandin E1 Antiulcer/Termination Of Pregnancy||Purity::||>99%|
|Grade Standard:||Medicine Grade|
Prostaglandin E1 Antiulcer/Termination Of Pregnancy ,Misoprostol CAS 59122-46-2
|Synonyms:||Misoprostol (Mixture of Diastereomers);Misoprostol-d5;SC-29333;MISOPROSTOL;MISOPROSTOL ACID;MISOPROSTOL FREE ACID;Misoprostol API;Misogon|
|Product Categories:||Active Pharmaceutical Ingredients;Prostaglandins;Prostaglandin;Fatty Acid Derivatives & Lipids;Glycerols;Intermediates & Fine Chemicals;Prostanoid receptor and related;API;Inhibitors;Pharmaceuticals|
|Misoprostol Chemical Properties|
|Boiling point||429.67°C (rough estimate)|
|density||1.0323 (rough estimate)|
|refractive index||1.6120 (estimate)|
|solubility||Practically insoluble in water, soluble in ethanol (96 per cent), sparingly soluble in acetonitrile.|
|CAS DataBase Reference||59122-46-2(CAS DataBase Reference)|
|EPA Substance Registry System||Prost-13-en-1-oic acid, 11,16-dihydroxy-16-methyl- 9-oxo-, methyl ester, (11.alpha.,13E)-(59122-46-2)|
|RIDADR||UN 2810 6.1/PG 3|
|Hazardous Substances Data||59122-46-2(Hazardous Substances Data)|
|Toxicity||LD50 in rats, mice (mg/kg): 40-62, 70-160 i.p.; 81-100, 27-138 orally (Kotsonis)|
|(11alpha,13E)-(+)-11alpha,16-Dihydroxy-16-methyl-9-oxoprost-13E-en-1-oic acid methyl ester||English|
|Misoprostol Usage And Synthesis|
|Description||Misoprostol is a synthetic prostaglandin E1 analog that is commonly used for medical abortion, management of miscarriage, cervical priming, management of postpartum hemorrhage, and induction of labor. Because of misoprostol’s wide use in reproductive health, the drug is in the World Health Organization (WHO) Model List of Essential Medicines.|
|Pharmacokinetics||Routes for administering misoprostol include orally, sublingually, vaginally, rectally, or buccally. Pharmacokinetics studies carried out to compare vagina and oral administration have revealed that vaginal misoprostol is linked to slower clearance, lower peak plasma levels, and slower absorption, similar to an extended release preparation. Conversely, vaginal misoprostol is associated with more significant effects on the uterus and cervix due to the higher overall exposure to the drug.
Administration through the rectum revealed a similar pattern to vaginal administration; however, it has lower AUC and lower maximum peak concentration. The sublingual route has higher peak levels and more rapid absorption as compared to oral or vaginal administration.
Misoprostol is an effective and safe way of inducing labor although the Food and Drug Administration (FDA) has not yet approved it for use in pregnancy. However, the European Union (EU) approved its use after a study that was done between 2002 and 2012. It acts by causing uterine ripening and constrictions of the cervix.
Misoprostol is normally used in combination with other drugs, such as methotrexate or mifepristone for medical abortion. It works by softening the cervix, causing it to open. Also, it makes the uterine muscles contract, thus inducing labor to expel the fetus. Misoprostol is a similar to prostaglandin which as a hormone that can cause a stronger reaction from the uterus. Most of the time, the drug is given in a clinic or hospital birthing centers.
Misoprostol can be best administered when one has passed 12 or more weeks of pregnancy to avoid possible severe complications. It can also be administered if there is a possibility of ectopic pregnancy or if one has an intrauterine device (IUD).
Misoprostol can be used either vaginally or orally if the pregnancy is still in the first trimester. The pregnant woman is advised to use 12 tablets of 200 grams and should put four tablets into the vagina or under the tongue and let it dissolve for 30 minutes. The woman is further advised to wait for 3 hours and repeat with four more pills in the vagina or under the tongue for 30 minutes.
The drug is more effective when inserted into the vagina; however, doctors usually administer it orally due to the possibility of infection when used vaginally. When used together with mifepristone, misoprostol is effective in approximately 95% of early pregnancies.
Misoprostol is normally used both as treatment and prevention of postpartum hemorrhage secondary to its uterotonic properties. Studies have revealed that orally administered misoprostol is less effective as compared to oxytocin, but it still plays a vital role in treating postpartum hemorrhage when other agents fail or are not available.
Prevention of Ulcer
Misoprostol is commonly used for the treatment and prevention of NSAID-induced gastric and duodenal ulcers due to its analgesic and anti-inflammatory properties. It acts by inhibiting gastric acid inhibition of adenylate cyclase by G-protein coupled receptor that leads to decreased proton pump activity and decreased intracellular cyclic AMP levels at the apical surface of the parietal cell.
Misoprostol is used in treating a mother in case of fetal death that can result in miscarriage. It is also used in the termination of pregnancy for fetal anomalies. Initially, a low dose is administered and doubled for the extra doses until delivery.
|Adverse Drug Reactions||The general adverse reactions experienced include contractions, abdominal pain, and GI intolerance and diarrhea. Many clinical studies revealed that about 13% of patients experienced diarrhea in the initial stages of therapy.
The most often reported side effects of orally taking the drug for the prevention and treatment of gastric ulcers include nausea, abdominal pain, headache, flatulence, dyspepsia, constipation, nausea, and constipation. Many patients experience fever when given multiple doses every 4 to 6 hours.
Women with wanted pregnancies are not supposed to take misoprostol to reduce the risk of increased uterine contractions and tone due to NSAID-induced gastric ulcers. This may cause complete or partial abortions or may lead to pregnancies with linked to congenital disabilities.
The drug may cause uterine hyperstimulation, which can affect the blood supply to the uterus negatively, thus increasing the chances of developing complications such as rupture of the womb.
|Controversy||There have been numerous controversies regarding the use of misoprostol for induction of labor due to various reasons. The use of misoprostol and mifepristone for medical abortion has the potential of improving access to abortion services; therefore, political opponents of abortion may view the drugs as a target and a threat. It is noteworthy that in 2000, the FDA approved the use of mifepristone and misoprostol in conjunction with misoprostol for the termination of early pregnancy, yet misoprostol was not approved for the same purpose.|