Arthrotec - General Information
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.
Pharmacology of Arthrotec
Arthrotec is a prostaglandin E1 (PGE1) analogue used for the treatment and prevention of stomach ulcers. When administered, misoprostol stimulates increased secretion of the protective mucus that lines the gastrointestinal tract and increases mucosal blood flow, thereby increasing mucosal integrity. It is sometimes co-prescribed with non-steroidal anti-inflammatory drugs (NSAIDs) to prevent the occurrence of gastric ulceration, a common adverse effect of the NSAIDs.
Arthrotec for patients
Read this leaflet before taking Cytotec (misoprostol) and each time your prescription is renewed, because the leaflet may be changed.
Cytotec (misoprostol) is being prescribed by your doctor to decrease the chance of getting stomach ulcers related to the arthritis/ pain medication that you take.
Cytotec can cause miscarriage, often associated with potentially dangerous bleeding. This may result in hospitalization, surgery, infertility, or death. Do not take it if you are pregnant and do not become pregnant while taking this medicine.
If you become pregnant during Cytotec therapy, stop taking Cytotec and contact your physician immediately. Remember that even if you are on a means of birth control it is still possible to become pregnant. Should this occur, stop taking Cytotec and contact your physician immediately.
Cytotec may cause diarrhea, abdominal cramping, and/or nausea in some people. In most cases these problems develop during the first few weeks of therapy and stop after about a week. You can minimize possible diarrhea by making sure you take Cytotec with food.
Because these side effects are usually mild to moderate and usually go away in a matter of days, most patients can continue to take Cytotec. If you have prolonged difficulty (more than 8 days), or if you have severe diarrhea, cramping and/or nausea, call your doctor.
Take Cytotec only according to the directions given by your physician.
Do not give Cytotec to anyone else. It has been prescribed for your specific condition, may not be the correct treatment for another person, and would be dangerous if the other person were pregnant.
This information sheet does not cover all possible side effects of Cytotec. This patient information leaflet does not address the side effects of your arthritis/pain medication. See your doctor if you have questions.
Keep out of reach of children.
Misoprostol has not been shown to interfere with the beneficial effects of aspirin on signs and symptoms of rheumatoid arthritis. Misoprostol does not exert clinically significant effects on the absorption, blood levels, and anti-platelet effects of therapeutic doses of aspirin. Misoprostol has no clinically significant effect on the kinetics of diclofenac or ibuprofen.
Misoprostol should not be taken by anyone with a history of allergy to prostaglandins.
Additional information about Arthrotec
Arthrotec Indication: Indicated for the treatment of ulceration (duodenal, gastric and NSAID induced) and prophylaxis for NSAID induced ulceration.
Mechanism Of Action: Arthrotec 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 Arthrotec 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. 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. Increased thickness of mucus layer, 5. Enhanced mucosal blood flow as a result of direct vasodilatation, 6. Stabilization of tissue lysozymes/vascular endothelium, and 7. Improvement of mucosal regeneration capacity.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Misoprostol
Synonyms: Misoprostolum [Inn-Latin]
Drug Category: Oxytocics; Anti-Ulcer Agents; Abortifacient Agents; Prostaglandins
Drug Type: Small Molecule; Approved
Other Brand Names containing Misoprostol: Arthrotec; Cytotec;
Absorption: Misoprostol is extensively absorbed.
Toxicity (Overdose): Not Available
Protein Binding: 85%
Biotransformation: Rapidly de-esterified to misoprostol acid. The de-esterified metabolite undergoes further metabolism by beta and omega oxidation; oxidation is followed by reduction of the ketone to yield prostaglandin F analogs.
Half Life: 20-40 minutes
Dosage Forms of Arthrotec: Tablet Oral
Chemical IUPAC Name: methyl 7-[(1R,2R,3R)-3-hydroxy-2-[(E)-4-hydroxy-4-methyloct-1-enyl]-5-oxocyclopentyl]heptanoate
Chemical Formula: C22H38O5
Misoprostol on Wikipedia: http://en.wikipedia.org/wiki/Misoprostol
Organisms Affected: Humans and other mammals