Misoprostol

Misoprostol is a Prostaglandin E1 Analogues belonging to Antiulcer agent.

Misoprostol is a prostaglandin E1 analogue used to reduce the risk of NSAID-induced gastric ulcers.

Misoprostol Rapidly and almost completely absorbed from the GI tract. Time taken to reach peak plasma concentration is Approximately 15-30 min. The apparent volume of distribution of the active metabolite of misoprostol was in subjects with normal renal function was 13.6±8.0L/kg, with mild renal impairment was 17.3±23.0L/kg, with moderate renal impairment was 14.3±6.8L/kg, and with end stage renal disease was 11.0±9.6L/kg. Misoprostol is <90% protein bound in serum. It rapidly metabolised to misoprostol acid (active form) and further metabolised via oxidation in several body organs. Excreted mainly via urine 80%.

Misoprostol shows side effects like Diarrhea, headache, stomach pain, upset stomach, gas, vomiting, constipation, indigestion.

Misoprostol is available in the form of Oral Tablet.

Misoprostol is available in India, US, Canada, Sri Lanka, Malaysia, Philippines, Japan, China, UK, Russia, and Australia.

Misoprostol belongs to the Antiulcer agent acts as a Prostaglandin E1 Analogues.

Misoprostol is a synthetic prostaglandin E1 analog that stimulates prostaglandin E1 receptors on parietal cells in the stomach to reduce gastric acid secretion. Mucus and bicarbonate secretion are also increased along with thickening of the mucosal bilayer so the mucosa can generate new cells. Misoprostol binds to smooth muscle cells in the uterine lining to increase the strength and frequency of contractions as well as degrade collagen and reduce cervical tone.

The effect of this Misoprostol lasts for 3 hours after administration.

The Tmax of Misoprostol was found to be approximately 15-30 minutes.

Misoprostol is available in the form of Oral tablet.

Misoprostol Tablet is taken orally, usually in divided dose.

Misoprostol is an effective antiulcer medication used to prevent the secretion of acid in the stomach. It is primarily used to prevent ulcers caused due to non-steroidal pain medication.

Misoprostol is a Prostaglandin E1 Analogues belonging to Antiulcer agent.

Misoprostol is a synthetic prostaglandin E₁ analog that replaces the protective prostaglandins consumed with prostaglandin-inhibiting therapies (eg, NSAIDs); has been shown to induce uterine contractions.

Misoprostol is approved for use in the following clinical indications

• Cervical ripening and labor induction
• Early pregnancy loss
• Incomplete abortion, treatment
• Nonsteroidal anti-inflammatory drug–induced gastric ulcers, prevention
• Postpartum hemorrhage

• Cervical ripening and labor induction

Intravaginal (off-label route): 25 mcg (one-fourth of 100 mcg tablet); may repeat at intervals no more frequent than every 3 to 6 hours; 50 mcg every 6 hours may be used in some cases.

Oral: 25 mcg (one-fourth of 100 mcg tablet) every 2 hours (Tang 2013); 20 mcg doses every 2 hours have also been evaluated.

• Early pregnancy loss

Intravaginal (off-label route): Initial dose: 800 mcg in patients <13 weeks' gestation. May repeat with one dose if needed, ≥3 hours after the first dose and typically within 7 days if no response to the initial dose is observed.

• Incomplete abortion, treatment

Oral: 600 mcg as a single dose in patients <14 weeks' gestation.

Sublingual (off-label route): 400 mcg as a single dose in patients <14 weeks' gestation.

• Nonsteroidal anti-inflammatory drug–induced gastric ulcers, prevention

Oral: 200 mcg 4 times daily; if not tolerated, may decrease dose to 100 mcg 4 times daily.

• Postpartum hemorrhage

Prevention:

Buccal/sublingual (off-label route): 200 to 400 mcg as a single dose administered immediately after delivery.

Oral: 600 mcg as a single dose administered immediately after delivery.

Treatment:

Oral: 600 to 1,000 mcg as a single dose.

Rectal (off-label route): 600 to 1,000 mcg as a single dose.

Sublingual (off-label route): 800 mcg as a single dose. Use caution if a prophylactic dose was already given, especially if adverse events were observed.

Misoprostol is available in various strengths as 100 mcg; 200 mcg.

Misoprostol is available in the form of Oral tablet.

• Dosage Adjustment in Kidney Patient

Dose adjustment is not routinely needed; however, the dose may be reduced if the recommended dose is not tolerated. It is not known if misoprostol is removed by dialysis.

Misoprostol is contraindicated in patients with

• Should not be taken by anyone with a history of allergy to prostaglandins.
• Misoprostol should not be taken by pregnant women to reduce the risk of ulcers induced by nonsteroidal anti-inflammatory drugs (NSAIDs).

• Bacterial infections

Use of this medicine has been reported to cause bacterial infections in some patients. Any instance of infection after using this medicine should be informed to the doctor.

• Excessive bleeding

Use of this medicine has been associated with excessive bleeding in some patients and hence any such instance should be reported to the doctor.

• Uterine rupture

This medicine has been associated with cases of uterine rupture when used for labor induction in some cases. Caution is advised while using this medicine if the patient is in the late thirties and beyond or the delivery is cesarean.

• Diarrhea

Use of this medicine can cause diarrhea and hence should not be coadministered with other diarrhea causing medications.

• Severe anemia

Use of this medicine is not recommended for women with severe anemia.

Misoprostol is rapidly metabolized in the mother to misoprostol acid, which is biologically active and is excreted in breast milk. Caution should be exercised when misoprostol is administered to a nursing woman.

Misoprostol can cause birth defects, abortions and other serious complications if given to pregnant women. Hence, use of this medicine for treatment or prevention of ulcers is not recommended.

Common

• Abdominal pain, diarrhea (including severe diarrhea), Constipation, dyspepsia, flatulence, nausea, vomiting, Headache, Acute myocardial infarction, arterial thrombosis, cardiac arrhythmia, chest pain, edema, hypertension, hypotension, increased cardiac enzymes in blood specimen, phlebitis, pulmonary embolism, syncope, Alopecia, dermatitis, diaphoresis, pallor, skin rash, Increased thirst, loss of libido, weight changes, Change in appetite, dysgeusia, dysphagia, gastroesophageal reflux disease, gastrointestinal hemorrhage, gastrointestinal infection, gastrointestinal inflammation, gingivitis, increased amylase, rectal disease, Dysuria, glycosuria, gynecological disease (dysmenorrhea, heavy menstrual bleeding, menstrual disease, spotty menstruation, uterine cramps), hematuria, impotence, mastalgia, urinary tract infection, Abnormal white blood cell differential, anemia, increased erythrocyte sedimentation rate, purpuric disease, thrombocytopenia, Abnormal hepatobiliary function, increased serum alkaline phosphatase, Anaphylaxis, Anxiety, asthenia, body pain, cerebrovascular accident, chills, confusion, depression, dizziness, drowsiness, fatigue, neuropathy, neurosis, pain, rigors, Arthralgia, back pain, gout, muscle cramps, myalgia, stiffness, Conjunctivitis, visual disturbance, Deafness, otalgia, tinnitus, Increased blood urea nitrogen, polyuria, Bronchitis, bronchospasm, dyspnea, epistaxis, pneumonia, upper respiratory tract infection.

Rare

• Uterine rupture, Abnormal platelet aggregation, prolonged bleeding time.

• Antacids

May enhance the adverse/toxic effect of misoprostol. More specifically, concomitant use with magnesium-containing antacids may increase the risk of diarrhea. Management: Avoid concomitant use of misoprostol and magnesium-containing antacids. In patients requiring antacid therapy, employ magnesium-free preparations. Monitor for increased adverse effects (e.g., diarrhea, dehydration).

• Carbetocin

Misoprostol may enhance the adverse/toxic effect of Carbetocin. Specifically, Carbetocin oxytocic effects may be enhanced.

• Oxytocin

Misoprostol may enhance the adverse/toxic effect of Oxytocin. Specifically, oxytocic effects may be enhanced. Management: The manufacturer of misoprostol recommends avoiding concomitant use with oxytocin. Misoprostol may augment effects of oxytocin, particularly when given within 4 hours of oxytocin initiation.

• Phenylbutazone

May enhance the neurotoxic effect of misoprostol. Specifically, the combination may result in headache, dizziness, and transient diplopia.

The common side effects of Misoprostol include the following

Common side effects

• Diarrhea, headache, stomach pain, upset stomach, gas, vomiting, constipation, indigestion.

Rare side effects

• Vomiting blood, bloody or black, tarry stools.

• Pregnancy

Misoprostol can cause birth defects, abortions and other serious complications if given to pregnant women. Hence, use of this medicine for treatment or prevention of ulcers is not recommended.

• Nursing Mothers

Misoprostol is rapidly metabolized in the mother to misoprostol acid, which is biologically active and is excreted in breast milk. Caution should be exercised when misoprostol is administered to a nursing woman.

• Pediatric Use

Safety and effectiveness of Misoprostol in pediatric patients have not been established.

Symptoms: Convulsions, sedation, tremor, dyspnoea, diarrhoea, abdominal pain, fever, palpitations, hypotension, bradycardia.

Management: Supportive treatment.

Pharmacodynamic

Misoprostol is a prostaglandin E1 analog used to reduce the risk of NSAID induced gastric ulcers by reducing secretion of gastric acid from parietal cells. Misoprostol is also used to manage miscarriages and used alone or in combination with mifepristone for first trimester abortions.

Pharmacokinetics

• Absorption

Misoprostol rapidly and almost completely absorbed from the GI tract. Time taken to reach peak plasma concentration is Approximately 15-30 min.

• Distribution

The apparent volume of distribution of the active metabolite of misoprostol was in subjects with normal renal function was 13.6±8.0L/kg, with mild renal impairment was 17.3±23.0L/kg, with moderate renal impairment was 14.3±6.8L/kg, and with end stage renal disease was 11.0±9.6L/kg. Misoprostol is <90% protein bound in serum.

• Metabolism and Excretion

Misoprostol rapidly metabolized to misoprostol acid (active form) and further metabolized via oxidation in several body organs. Excreted mainly via urine 80%.

• https://www.mims.com/philippines/drug/info/misoprostol?mtype=generic
• https://www.uptodate.com/contents/misoprostol-drug-information?search=misoprostol&source=panel_search_result&selectedTitle=1~128&usage_type=panel&kp_tab=drug_general&display_rank=1
• https://www.rxlist.com/misoprostol-drug.htm#overdosage
• https://www.practo.com/medicine-info/misoprostol-188-api
• https://medlineplus.gov/druginfo/meds/a689009.html
• https://go.drugbank.com/drugs/DB00929
• https://www.drugs.com/dosage/misoprostol.html