Misoprostol; Uses, Side Effects, Drug Interactions, Pregnancy Misoprostol is a synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties. Misoprostol is only found in individuals that have used or taken this drug. It is a synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties. [PubChem]Misoprostol seems to inhibit gastric acid secretion by a direct action on the parietal cells through binding to the prostaglandin receptor. The activity of this receptor is mediated by G proteins which normally activate adenylate cyclase. The indirect inhibition of adenylate cyclase by Misoprostol may be dependent on guanosine-5& rsquo; -triphosphate (GTP). The significant cytoprotective actions of misoprostol are related to several mechanisms. These include 1. Increased secretion of bicarbonate, 2. The considerable decrease in the volume and pepsin content of the gastric secretions, 3. Misoprostol 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 in the cheek, under the tongue, or placed in the vagina. A synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties. Mechanism of Action of Misoprostol Misoprostol seems to inhibit gastric acid secretion by a direct action on the parietal cells through binding to the prostaglandin receptor. The activity of this receptor is mediated by G proteins which normally activate adenylate cyclase. The indirect inhibition of adenylate cyclase by Misoprostol may be dependent on guanosine-5’-triphosphate (GTP). The significant cytoprotective actions of misoprostol are related to several mechanisms. These include 1. Increased secretion of bicarbonate, 2. The considerable decrease in the volume and pepsin content of the gastric secretions, 3. It prevents harmful agents from disrupting the tight junctions between the epithelial cells which stops the subsequent back diffusion of H+ ions into the gastric mucosa, 4. The increased thickness of the mucus layer, 5. Enhanced mucosal blood flow as a result of direct vasodilatation, 6. Stabilization of tissue lysozymes/vascular endothelium, 7. Improvement of mucosal regeneration capacity, and 8. Replacement of prostaglandins that have been depleted as a result of various insults to the area. Misoprostol has also been shown to increase the amplitude and frequency of uterine contractions during pregnancy via selective binding to the EP-2/EP-3 prostanoid receptors. You Might Also Read Lansoprazole; Uses, ,Dosage, Side Effects, Drug InteractionsIndications of Misoprostol Abortion Cervical ripening Gynecological conditions Duodenal ulcer Labor induction NSAID-induced ulcer prophylaxis Postpartum bleeding Stomach ulcer Gastric ulcer Incomplete abortion Missed abortion Postpartum hemorrhage Indicated for the treatment of ulceration (duodenal, gastric and NSAID induced) and prophylaxis for NSAID induced ulceration. Misoprostol is also indicated for other uses that are not approved in Canada, including the medical termination of an intrauterine pregnancy used alone or in combination with methotrexate, as well as the induction of labor in a selected population of pregnant women with unfavorable cervices. This indication is avoided in women with prior uterine surgery or cesarean surgery due to an increased risk of possible uterine rupture. Misoprostol is also used for the prevention or treatment of serious postpartum hemorrhage. Contra-Indications of Misoprostol Extreme Loss of body water Inflammatory bowel disease Tearing of the uterus while pregnant Operation of the uterus or the cervix Pregnancy Previous C Section Dosage of Misoprostol Strengths: 100 mcg; 200 mcg; 600mcg Duodenal Ulcer 200 mcg orally 4 times a day after meals and at bedtime Maintenance dose: 100 to 200 mcg orally 4 times a day Gastric Ulcer 200 mcg orally 4 times a day after meals and at bedtime Maintenance dose: 100 to 200 mcg orally 4 times a day NSAID-Induced Ulcer Prophylaxis 200 mcg orally 4 times a day after meals and at bedtime Maintenance dose: 100 to 200 mcg orally 4 times a day Labor Induction American College of Obstetricians and Gynecologists (ACOG) Recommendations 25 mcg vaginally every 3 to 6 hours Some patients may require doses of 50 mcg every 6 hours Postpartum Bleeding ACOG Recommendations 800 to 1000 mcg rectally once International Federation of Gynecology Obstetrics (FIGO) Recommendations 600 mcg orally OR 800 mcg sublingually once immediately after delivery Abortion ACOG Recommendations>First Trimester of Pregnancy Early Pregnancy Loss: 800 mcg intravaginally once; a second dose may be given if there is no response to the first dose no sooner than 3 hours after the first dose, and usually within 7 days Incomplete Abortion: 600 mcg orally once Missed Abortion: 800 mcg intravaginally OR 600 mcg sublingually once; the dose may be repeated every 3 hours for 2 additional doses You Might Also Read Contraindications of Terbinafine, Warning, Pregnancy CategorySide Effects of Misoprostol The most common Constipation dizziness drowsiness dry mouth chest pain headache joint painPain dizziness nausea and vomiting Severe stomach ache diarrhoea, anorexia, flatulence, headache, fainting, fast or pounding heartbeats. More common Seizures Syndrome of inappropriate secretion of antidiuretic hormone Fast or irregular heartbeat fever Back pain dizziness headache increased cough Acid or sour stomach decreased appetite Agitation chest congestion chest pain confusion diarrhea or loose stools heartburn sleepiness or unusual drowsiness stomach or abdominal cramps, gas, or pain trouble sleeping Less common Abnormal dreams change in sense of taste congestion discouragement, feeling sad, or empty Suicide attempts Acting on dangerous impulses Aggressive or violent behavior Thoughts about suicide or dying New or worse depression New or worse anxiety or panic attacks Agitation, restlessness, anger, or irritability Trouble sleeping An increase in activity or talking more than normal Drug Interactions of Misoprostol Misoprostol may interact with following drugs, supplements & may decrease the efficacy of drugs crofelemer eluxadoline Aceclofenac The therapeutic efficacy of Misoprostol can be decreased when used in combination with Aceclofenac. Approved, Investigational Acemetacin The therapeutic efficacy of Misoprostol can be decreased when used in combination with Acemetacin. Approved, Experimental, Investigational Acetylsalicylic acid The therapeutic efficacy of Misoprostol can be decreased when used in combination with an Acetylsalicylic acid. Approved, Vet Approved Adapalene The therapeutic efficacy of Misoprostol can be decreased when used in combination with Adapalene. Approved Alclofenac The therapeutic efficacy of Misoprostol can be decreased when used in combination with Alclofenac. Approved, Withdrawn Almasilate The risk or severity of adverse effects can be increased when Almasilate is combined with Misoprostol. Approved, Experimental Alminoprofen The therapeutic efficacy of Misoprostol can be decreased when used in combination with Alminoprofen. Experimental Aloglutamol The risk or severity of adverse effects can be increased when Aloglutamol is combined with Misoprostol. Experimental Aluminium The risk or severity of adverse effects can be increased when Aluminium is combined with Misoprostol. Calcium Carbonate The risk or severity of adverse effects can be increased when Calcium Carbonate is combined with Misoprostol. Approved, Investigational Calcium silicate The risk or severity of adverse effects can be increased when Calcium silicate is combined with Misoprostol. Experimental Carbaspirin calcium The therapeutic efficacy of Misoprostol can be decreased when used in combination with Carbaspirin calcium. Chloroquine The therapeutic efficacy of Misoprostol can be decreased when used in combination with Chloroquine. Approved, Investigational, Vet Approved Choline magnesium trisalicylate The therapeutic efficacy of Misoprostol can be decreased when used in combination with Choline magnesium trisalicylate. Approved Clonixin The therapeutic efficacy of Misoprostol can be decreased when used in combination with Clonixin. Approved Curcumin The therapeutic efficacy of Misoprostol can be decreased when used in combination with Curcumin. Approved, Investigational Diclofenac The therapeutic efficacy of Misoprostol can be decreased when used in combination with Diclofenac. Etanercept The therapeutic efficacy of Misoprostol can be decreased when used in combination with Etanercept. Approved, Investigational Ethenzamide The therapeutic efficacy of Misoprostol can be decreased when used in combination with Ethenzamide. Experimental Etodolac The therapeutic efficacy of Misoprostol can be decreased when used in combination with Etodolac. Approved, Investigational, Vet Approved Etofenamate The therapeutic efficacy of Misoprostol can be decreased when used in combination with Etofenamate. Approved, Investigational Etoricoxib The therapeutic efficacy of Misoprostol can be decreased when used in combination with Etoricoxib. You Might Also Read CBC (Complete Blood Count), Defination, Types, Normal Range,ResultsPregnancy & Lactation FDA PregnancyCategory X Pregnancy Women who may become pregnant should use adequate birth control (e.g., birth control pills, condoms, or intrauterine devices) while taking misoprostol. Since misoprostol increases the risk of miscarriage, a woman who may be pregnant should not start taking misoprostol until she is sure that she is not pregnant. If you suspect you are pregnant, stop the medication and contact your doctor. Lactation Breast-feeding mothers should not take misoprostol, as it may cause significant diarrhea for breast-feeding infants. The safety and effectiveness of this medication have not been established for children and adolescents under 18 years of age. References DrugBank http://www.drugbank.ca/drugs/DB00929 http://www.drugbank.ca/drugs/DB00929#targets EPA DSStox https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID7020897 Human Metabolome Database (HMDB) http://www.hmdb.ca/metabolites/HMDB0015064 ClinicalTrials.gov https://clinicaltrials.gov/ DailyMed https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=ARTHROTEC https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=MISOPROSTOL HSDB https://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+59122-46-2 European Chemicals Agency (ECHA) https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/195444 European Chemicals Agency – ECHA https://www.echa.europa.eu/web/guest/information-on-chemicals/cl-inventory-database/-/discli/details/195444 FDA Orange Book https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm PubMed Health http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0011244/ Springer Nature Read more … Show More