THE USE OF MISOPROSTOL IN PREGNANT WOMEN MAY CAUSE BIRTH DEFECTS, Abortion, PREMATURE BIRTH OR RUPTURE OF THE UTERUS.
IT HAS BEEN REPORTED WHEN MISOPROSTOL IS ADMINISTERED TO PREGNANT WOMEN TO INDUCE LABOR OR Abortion. THE RISK OF TERMINAL BREACH INCREASES WITH INCREASE AGE OF PREGNANCY AND WITH PREVIOUS TERMINAL SURGERY, INCLUDING DELIVERY WITH AN EMPEROR (see alsoPRECAUTIONARY MEASURESiRAD IK PROD).
MISOPROSTOL SHOULD NOT BE USED BY PREGNANT WOMEN TO REDUCE THE RISK OF UNSAID SOLARS (seeCONTRAINDICATIONS,WARNINGS, iPRECAUTIONARY MEASURES).
PATIENTS SHOULD BE WARNED ABOUT THE ABORTIONAL PROPERTIES AND BE WARNED NOT TO GIVE THE MEDICINE TO OTHERS.
Misoprostol should not be used to reduce the risk of NSAID-induced ulcers in women of childbearing age unless the patient is at high risk for NSAID-related ulcer complications or is at high risk of developing an ulcer. In such patients, misoprostol can be prescribed as the patient
- had a negative serum pregnancy test within 2 weeks prior to starting therapy.
- is able to adhere to effective contraceptive measures.
- she received both oral and written warnings about the dangers of misoprostol, the risk of possible contraceptive failure, and the danger to other women of childbearing age if the drug is accidentally taken.
- she will not start misoprostol until the second or third day of her next normal period.
Misoprostol oral tablets contain 100 mcg or 200 mcg of misoprostol, a synthetic prostaglandin E1analogue.
Misoprostol contains approximately equal amounts of the two diastereomers shown below with their enantiomers marked (±):
Misoprostol is a viscous, water-soluble liquid.
The inactive ingredients of the tablets are hydrogenated vegetable oil, hypromellose, microcrystalline cellulose, and sodium starch glycolate.
Pharmacokinetics
Misoprostol is extensively absorbed and undergoes rapid deesterification to its free acid, which is responsible for its clinical activity and, unlike the parent compound, is detectable in plasma. The alpha side chain undergoes beta oxidation and the beta side chain undergoes omega oxidation followed by ketone reduction to yield prostaglandin F analogs.
In normal volunteers, misoprostol is rapidly absorbed after oral administration with Tmaxof misoprostol acid of 12 ± 3 minutes and a terminal half-life of 20-40 minutes.
There is wide variability in plasma levels of misoprostol acid between and within studies, but mean values after individual doses show a linear relationship with dose over the range of 200-400 mcg. No accumulation of misoprostol acid was observed in multiple dose studies; plasma steady state was reached within two days.
Peak plasma concentrations of misoprostol acid are reduced when the dose is taken with food, and the total availability of misoprostol acid is reduced by concomitant administration of antacids. However, clinical studies have been conducted with concomitant use of antacids, so this effect does not appear to be clinically important.
| Mean ± SD | Cmax(pg/mL) | AUC(0-4) (pghr/mL) | Tmax(minutes) |
| Already | 811 ± 317 | 417 ± 135 | 14 ± 8 |
| S antacidom | 689 ± 315 | 349 ± 108* | 20 ± 14 |
| With a high-fat breakfast | 303 ± 176* | 373 ± 111 | 64 ± 79* |
*Comparisons with fasting results are statistically significant, p<0.05.
After oral administration of radiolabeled misoprostol, approximately 80% of the detected radioactivity is excreted in the urine. Pharmacokinetic studies in patients with varying degrees of renal impairment showed an approximate doubling of T1/2, Cmax, and AUC compared to normal values, but there is no clear correlation between the degree of damage and AUC. In subjects over 64 years of age, the AUC for misoprostol acid is increased. Routine dose adjustment is not recommended in elderly patients or patients with renal impairment, but dose reduction may be necessary if they cannot tolerate the usual dose.
Interaction studies between misoprostol and various non-steroidal anti-inflammatory drugs showed no effect on the kinetics of ibuprofen or diclofenac and a 20% decrease in aspirin AUC, which is not considered clinically significant.
Pharmacokinetic studies also showed a lack of drug interaction with antipyrine and propranolol when these drugs were co-administered with misoprostol. Misoprostol administered for 1 week had no effect on the steady-state pharmacokinetics of diazepam when the two drugs were administered 2 hours apart.
The binding of misoprostol acid to serum proteins is less than 90% and is not concentration dependent in the therapeutic range.
After a single oral dose of misoprostol in a nursing mother, misoprostol acid was excreted in breast milk. The maximum concentration of misoprostol acid in expressed breast milk was reached within 1 hour after administration and was 7.6 pg/ml (CV 37%) and 20.9 pg/ml (CV 62%) after a single administration of 200 mcg and 600 mcg misoprostol respectively. Misoprostol acid concentrations in breast milk decreased to < 1 pg/ml 5 hours after dosing.
Pharmacodynamics
Misoprostol has both antisecretory (inhibition of gastric acid secretion) and (in animals) mucosal protective properties. NSAIDs inhibit the synthesis of prostaglandins and a lack of prostaglandins in the gastric mucosa may lead to decreased secretion of bicarbonate and mucus and may contribute to mucosal damage caused by these agents. Misoprostol may increase bicarbonate and mucus production, but has been shown to have an antisecretory effect in humans at doses of 200 mcg and above. Therefore, it is not possible to say whether the ability of misoprostol to reduce the risk of peptic ulcer disease is due to its antisecretory effect, its protective effect on the mucosa, or both.
In vitrostudies in canine parietal cells using tritium misoprostol acid as a ligand led to the identification and characterization of specific prostaglandin receptors. Binding to the receptor is saturable, reversible and stereospecific. The sites have a high affinity for misoprostol, its acidic metabolite and other E-type prostaglandins, but not for prostaglandins F or I and other unrelated compounds, such as histamine or cimetidine. The affinity of the misoprostol receptor site correlates well with an indirect index of antisecretory activity. It is likely that these specific receptors allow the local action of misoprostol taken with food, despite the lower serum concentrations achieved.
Misoprostol causes a moderate decrease in pepsin concentration during basal conditions, but not during histamine stimulation. It has no significant effect on fasting or postprandial gastrin or intrinsic factor secretion.
Effects on gastric acid secretion
Misoprostol, in the range of 50-200 mcg, inhibits basal and nocturnal gastric acid secretion and acid secretion in response to various stimuli, including meals, histamine, pentagastrin, and coffee. The effect is visible 30 minutes after oral administration and lasts for at least 3 hours. In general, the effects of 50 mcg were modest and short-lived, and only the 200 mcg dose had significant effects on nocturnal secretion or on histamine and meal-stimulated secretion.
Effects on the uterus
Misoprostol has been shown to cause uterine contractions that can jeopardize pregnancy. (See boxWARNINGS.)
Other pharmacological effects
Misoprostol has no clinically significant effects on serum levels of prolactin, gonadotropin, thyroid stimulating hormone, growth hormone, thyroxine, cortisol, gastrointestinal hormones (somatostatin, gastrin, vasoactive intestinal polypeptide and motilin), creatinine or uric acid. Gastric emptying, immune function, platelet aggregation, lung function or cardiovascular system are not altered by the recommended doses of misoprostol.
clinical studies
A series of small short-term (approximately 1 week) placebo-controlled studies in healthy human volunteers evaluated the ability of doses of misoprostol to reduce the risk of NSAID-induced mucosal damage. Studies of 200 mcg q.i.d. misoprostol with tolmetin and naproxen, and 100 and 200 mcg q.i.d. with ibuprofen all showed a reduction in the number of significant endoscopic injuries from approximately 70-75% on placebo to 10-30% on misoprostol. Doses of 25-200 mcg q.i.d. reduced mucosal damage and bleeding caused by aspirin.
Reducing the risk of stomach ulcers caused by non-steroidal anti-inflammatory drugs (NSAIDs)
Two 12-week, randomized, double-blind studies in patients with osteoarthritis who had gastrointestinal symptoms but no ulcers on endoscopy while taking NSAIDs compared the ability of misoprostol 200 mcg, misoprostol 100 mcg, and placebo to reduce the risk of gastric ulcer ( GU formation. Patients were approximately evenly distributed between ibuprofen, piroxicam and naproxen and continued on this treatment for 12 weeks. The dose of 200 mcg produced a significant, statistically significant reduction in gastric ulcers in both studies. The lower dose was slightly less effective, with a significant result in only one study.
Reducing the risk of stomach ulcers caused by ibuprofen, piroxicam or naproxen
[Not. of patients with ulcer(s) (%)]
| Therapy | Duration of therapy | | ||
| 4 weeks | 8 weeks | 12 weeks | ||
| Study no. 1 | ||||
| Mizoprostol 200 mcg q.i.d. (n=74) | 1 (1,4) | 0 | 0 | 1 (1,4)* |
| Mizoprostol 100 mcg q.i.d. (n=77) | 3 (3,9) | 1 (1,3) | 1 (1,3) | 5 (6,5)* |
| Placebo (n=76) | 11 (14,5) | 4 (5,3) | 4 (5,3) | 19 (25,0) |
| Study no. 2 | ||||
| Mizoprostol 200 mcg q.i.d. (n=65) | 1 (1,5) | 1 (1,5) | 0 | 2 (3.1)* |
| Mizoprostol 100 mcg q.i.d. (n=66) | 2 (3,0) | 2 (3,0) | 1 (1,5) | 5 (7,6) |
| Placebo (n=62) | 6 (9,7) | 2 (3,2) | 3 (4,8) | 11 (17,7) |
| Studies No. 1 and No. 2** | ||||
| Mizoprostol 200 mcg q.i.d. (n=139) | 2 (1,4) | 1 (0,7) | 0 | 3 (2,2)* |
| Mizoprostol 100 mcg q.i.d. (n=143) | 5 (3,5) | 3 (2,1) | 2 (1,4) | 10 (7,0)* |
| Placebo (n=138) | 17 (12,3) | 6 (4,3) | 7 (5,1) | 30 (21,7) |
* Statistically significantly different from placebo at the 5% level.
** Combined data from study #1 and study #2.
In these studies, there were no significant differences between misoprostol and placebo in the relief of daytime or nighttime abdominal pain. Misoprostol has not been shown to reduce the risk of duodenal ulcers, but relatively few duodenal abnormalities have been observed.
In another clinical trial, 239 patients received aspirin 650-1300 mg q.i.d. for rheumatoid arthritis with endoscopic evidence of duodenal and/or gastric inflammation were randomized to misoprostol 200 mcg q.i.d. or placebo for 8 weeks while continuing to take aspirin. The study evaluated the potential interference of misoprostol on aspirin efficacy in these patients with rheumatoid arthritis by analyzing joint tenderness, joint swelling, clinician clinical assessment, patient assessment, changes in ARA classification, changes in hand grip strength, changes in duration of the morning. stiffness, patient assessment pain at rest, movement, interference with daily activities and ESR. Misoprostol did not affect the efficacy of aspirin in these patients with rheumatoid arthritis.
Misoprostol is indicated to reduce the risk of NSAIDs (Non-Steroidal Anti-Inflammatory Drugs, including Aspirin) induced gastric ulcers in patients at high risk of ulcer-related complications, e.g. the elderly and those with concomitant debilitating disease, as well as patients at high risk of developing stomach ulcers, such as patients with a history of ulcers. Misoprostol has not been shown to reduce the risk of duodenal ulcers in patients taking NSAIDs. Misoprostol should be taken during NSAID therapy. Misoprostol has been shown to reduce the risk of stomach ulcers in 3-month controlled studies. Compared to placebo, it had no effect on gastrointestinal pain or discomfort associated with NSAID use.
See framedWARNINGS.
Pregnant women should not take misoprostol to reduce the risk of ulcers caused by nonsteroidal anti-inflammatory drugs (NSAIDs).
Misoprostol should not be taken by anyone with a history of prostaglandin allergy.
See framedWARNINGS.
For hospital use only if misoprostol is used for cervical ripening, induction of labour, or for the treatment of severe postpartum bleeding, which is outside the approved indication.
Misoprostol should be used with caution in patients with pre-existing cardiovascular disease.
Information for patients
Women of childbearing age taking misoprostol to reduce the risk of NSAID-induced ulcers should be advised not to be pregnant when misoprostol treatment is started and to use an effective method of contraception while taking misoprostol.
See framedWARNINGS.
Misoprostol is for use in combination with non-steroidal anti-inflammatory drugs (NSAIDs), including aspirin, to reduce the chance of developing an NSAID-induced peptic ulcer.
Misoprostol should only be taken as prescribed by your doctor.
If the patient has questions or problems with misoprostol, the doctor should be contacted immediately.
THE PATIENT SHOULD NOT GIVE MISOPROSTOL TO OTHERS.Misoprostol is prescribed for a patient's specific condition, it may not be the right treatment for another person, and it could be dangerous for another person if they become pregnant.
A patient information leaflet is included on the misoprostol packaging that the patient receives from the pharmacist. The patient should read the package insert before taking misoprostol and each time the prescription is renewed, as the package insert may have been revised.
Keep misoprostol out of the reach of children.
SPECIAL NOTE FOR WOMEN
Misoprostol can cause birth defects, miscarriage (sometimes incomplete), premature birth, or uterine rupture if given to pregnant women.
Misoprostol is only available as a single-dose container with a patient information leaflet. To seePatient informationat the end of this mark.
Drug Interactions
To seeClinical Pharmacology.Misoprostol has not been shown to interfere with the beneficial effects of aspirin on the signs and symptoms of rheumatoid arthritis. Misoprostol has no clinically significant effects on the absorption, blood levels and antiplatelet effects of therapeutic doses of aspirin. Misoprostol has no clinically significant effect on the kinetics of diclofenac or ibuprofen.
Prostaglandins such as misoprostol may potentiate the activity of oxytocin, especially if given less than 4 hours before starting oxytocin treatment. Concomitant use is not recommended.
Animal Toxicology
A reversible increase in the number of normal gastric surface epithelial cells occurred in the dog, rat and mouse. No such increase was seen in people who received misoprostol for up to 1 year.
The apparent response of female mice to misoprostol in long-term studies at a dose 100 to 1000 times the human dose was hyperostosis, predominantly of the medulla sternebrae. Hyperostosis did not occur in long-term studies in dogs and rats and was not observed in humans treated with misoprostol.
Carcinogenesis, mutagenesis, impaired fertility
There was no evidence of an effect of misoprostol on the occurrence or incidence of tumors in rats given daily doses up to 150 times the human dose for 24 months. Similarly, there was no effect of misoprostol on the appearance or prevention of tumors in mice given daily doses up to 1000 times the human dose for 21 months. The mutagenic potential of misoprostol has been tested in several casesin vitrotests, all of which were negative.
When misoprostol was administered to male and female breeding rats at doses ranging from 6.25 times to 625 times the maximum recommended human therapeutic dose, it caused dose-related pre- and post-implantation losses and a significant reduction in the number of live pups born at the highest dose. These findings point to the possibility of a general adverse effect on male and female fertility.
Pregnancy
Teratogenic effects
See framedWARNINGS.Congenital anomalies sometimes associated with fetal death have been reported following unsuccessful use of misoprostol as an abortifacient, but the drug's teratogenic mechanism has not been proven. Several reports in the literature have associated the use of misoprostol during the first trimester of pregnancy with cranial abnormalities, cranial nerve palsies, facial deformities and limb abnormalities.
Misoprostol is not fetotoxic or teratogenic in rats and rabbits at doses 625 and 63 times higher than the human dose.
Non-teratogenic effects
See framedWARNINGS. Misoprostol can endanger pregnancy (may cause miscarriage) and thus harm the fetus when given to a pregnant woman. Misoprostol can cause uterine contractions, uterine bleeding and expulsion of the products of conception. Abortions caused by misoprostol may be incomplete. If a woman becomes pregnant or becomes pregnant while taking this drug, the drug should be discontinued and the patient should be advised of the potential hazard to the fetus in order to reduce the risk of NSAID-induced ulcers.
Rad and porod
Misoprostol can cause or increase uterine contractions. Vaginal administration of misoprostol, off-label, is used as a cervical ripening agent, for labor induction, and for the treatment of severe postpartum bleeding in the presence of uterine atony. The major adverse effect of the use of misoprostol in obstetrics is uterine tachysystole, which may progress to uterine tetany with marked impairment of uteroplacental blood flow, uterine rupture (requiring surgical repair, hysterectomy and/or salpingo-oophorectomy) or amniotic fluid embolism and lead. to adverse cardiac changes in the fetus. Uterine activity and fetal status should be monitored by trained obstetric personnel in a hospital setting.
The risk of uterine rupture associated with the use of misoprostol during pregnancy increases with advancing gestational age and with previous uterine surgery, including cesarean delivery. High multiparity also appears to be a risk factor for uterine rupture.
Off-label misoprostol use may also be associated with meconium passage, meconium-colored amniotic fluid, and caesarean section. Maternal shock, maternal death, fetal bradycardia and fetal death have also been reported with the use of misoprostol.
Misoprostol should not be used in the third trimester in women with a history of cesarean section or major uterine surgery due to the increased risk of uterine rupture. Misoprostol should not be used in cases where uterotony is generally contraindicated or where uterine hyperstimulation is considered inappropriate, such as pelvic disproportion, large multiparity, hypertonic or hyperactive uterine patterns, or fetal distress when delivery is not on hands or when a surgical procedure is more appropriate.
The effect of misoprostol on the subsequent growth, development and functional maturation of the infant when misoprostol is used for cervical ripening or labor induction has not been established. Data on the effect of misoprostol on the need for forceps or other intervention are not known.
The use of misoprostol to treat postpartum bleeding has been associated with reports of high temperatures (over 40 degrees Celsius or 104 degrees Fahrenheit) accompanied by effects on the autonomic and central nervous system, such as tachycardia, disorientation, agitation and convulsions. These fevers were transient. Supportive therapy should be determined by the patient's clinical picture.
Breastfeeding mothers
Misoprostol is rapidly metabolised in the mother to misoprostol acid, which is biologically active and is excreted in breast milk. There are no published reports of misoprostol side effects in breastfed infants of mothers taking misoprostol. Caution should be exercised when misoprostol is given to nursing mothers.
Use in children
The safety and efficacy of misoprostol in pediatric patients have not been established.
The following have been reported as side effects in subjects receiving misoprostol:
Gastrointestinal
In subjects who received 400 or 800 mcg of misoprostol daily during clinical studies, the most common gastrointestinal adverse reactions were diarrhea and abdominal pain. The frequency of diarrhea at a dose of 800 mcg in controlled studies in patients taking NSAIDs ranged from 14-40%, and in all studies (more than 5000 patients) it averaged 13%. Abdominal pain occurred in 13-20% of patients in NSAID studies and approximately 7% in all studies, but there was no consistent difference compared to placebo.
Diarrhea was dose dependent and usually started early during treatment (after 13 days), usually resolved spontaneously (often resolved after 8 days), but sometimes required discontinuation of misoprostol (2% of patients). Rare cases of severe diarrhea leading to severe dehydration have been reported. Patients with an underlying condition such as inflammatory bowel disease or those in whom dehydration, should it occur, would be dangerous should be carefully monitored if misoprostol is prescribed. The frequency of diarrhea can be reduced by taking it after meals and at bedtime and by avoiding the concomitant use of misoprostol with magnesium-containing antacids.
Gynecological
Women receiving misoprostol during clinical trials reported the following gynecological disorders: bleeding (0.7%), cramps (0.6%), hypermenorrhea (0.5%), menstrual disorder (0.3%), and dysmenorrhea (0. 1%). Postmenopausal vaginal bleeding may be associated with the use of misoprostol. If it appears, diagnostic examination should be performed to exclude gynecological pathology. (See boxWARNINGS.)
elderly
There were no significant differences in the safety profile of misoprostol in approximately 500 patients with ulcers aged 65 years or older compared to younger patients.
Additional side effects that have been reported are categorized as follows:
Frequency greater than 1%
In clinical trials, the following adverse reactions were reported by more than 1% of subjects receiving misoprostol and may be causally related to the drug: nausea (3.2%), flatulence (2.9%), headache (2.4 %), dyspepsia (2.0%), vomiting (1.3%) and constipation (1.1%). However, there were no significant differences between the incidence of these events for misoprostol and placebo.
Causal relationship unknown
The following side effects have been reported rarely. Causal relationships between misoprostol and these events have not been established, but cannot be excluded:
The body as a whole:pain, asthenia, fatigue, fever, chills, stiffness, weight changes.
Skin:rash, dermatitis, alopecia, pallor, breast pain.
Special senses:abnormal taste, abnormal vision, conjunctivitis, deafness, tinnitus, ear pain.
Breathing:upper respiratory tract infection, bronchitis, bronchospasm, shortness of breath, pneumonia, epistaxis.
Cardiovascular:chest pain, edema, diaphoresis, hypotension, hypertension, arrhythmia, phlebitis, increased cardiac enzymes, syncope, myocardial infarction (some fatal), thromboembolic events (e.g. pulmonary embolism, arterial thrombosis and stroke).
Gastrointestinal:GI bleeding, GI inflammation/infection, rectal disorder, hepatobiliary function abnormal, gingivitis, reflux, dysphagia, amylase increased.
Hypersensitivity:anaphylactic reaction
Metabolic:glycosuria, gout, increased nitrogen, increased alkaline phosphatase.
Genito-urinary:polyuria, dysuria, haematuria, urinary tract infection.
Nervous System/Psychiatric:anxiety, change in appetite, depression, drowsiness, dizziness, thirst, impotence, loss of libido, increased sweating, neuropathy, neurosis, confusion.
Musculoskeletal System:arthralgia, myalgia, muscle spasms, stiffness, back pain.
Blood clotting:anemia, abnormal differential, thrombocytopenia, purpura, increased ESR.
The toxic dose of misoprostol in humans has not been established. Cumulative total daily doses of 1600 mcg were tolerated and only symptoms of gastrointestinal discomfort were reported. In animals, acute toxic effects include diarrhoea, gastrointestinal lesions, focal cardiac necrosis, hepatic necrosis, renal tubular necrosis, testicular atrophy, respiratory distress and central nervous system depression. Clinical signs that may indicate overdose are sedation, tremors, convulsions, dyspnoea, abdominal pain, diarrhoea, fever, palpitations, hypotension or bradycardia. Symptoms should be treated with supportive therapy.
It is not known whether misoprostol acid is dialysable. However, since misoprostol is metabolized as a fatty acid, dialysis is probably not an appropriate treatment for overdose.
The recommended oral dose of misoprostol for adults to reduce the risk of stomach ulcers caused by NSAIDs is 200 mcg four times a day with food. If this dose is not tolerated, a 100 mcg dose may be used. (To seeClinical Pharmacology: Clinical Studies.) Misoprostol should be taken during treatment with NSAIDs as recommended by the doctor. Misoprostol should be taken with a meal and the last dose of the day should be taken at bedtime.
Kidney damage
Dosage schedule adjustment in patients with renal impairment is not routinely required, but the dose may be reduced if the 200 mcg dose is not tolerated. (To seeClinical Pharmacology.)
Misoprostol Tablets, 200 mcg are available as white, round, scored, flat, bevelled edge tablets, marked "N" above the score and "444" below the score and plain on the reverse.
NDC numberMaat
68071-2904-4 disposable vial of 4 vials
Pharmacist:Dispense into this child-resistant container as defined in the USP.
Include a patient information leaflet with each dispensing.
Store at 20° to 25°C (68° to 77°F); excursions permitted at 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Store in a dry place.
All trademarks are the property of their respective owners.
Distributed by:
ANI Pharmaceuticals, Inc.
Baudette, MN 56623
Issued:09/2022
LB4429-02
PATIENT INFORMATION
Read these instructions before taking misoprostol and each time your prescription is renewed, as the instructions may change.
Your doctor prescribes misoprostol to reduce the chance of getting an ulcer due to the arthritis/pain medication you are taking.
To reduce the risk of NSAID-induced ulcers, do not use misoprostol if you are pregnant. (See boxWARNINGS.) Misoprostol can cause miscarriage (sometimes incomplete which can lead to dangerous bleeding and require hospitalization and surgery), premature birth, or birth defects. It is also important to avoid pregnancy while taking this medicine and for at least one month or one menstrual cycle after you stop taking it. Misoprostol can cause the uterus to rupture (uterine rupture) during pregnancy. The risk of uterine rupture increases as your pregnancy progresses and if you have had surgery on your uterus, such as a caesarean section. The rupture (tearing) of the uterus can lead to severe bleeding, hysterectomy, and/or maternal or fetal death.
If you become pregnant during treatment with misoprostol, stop taking misoprostol and contact your doctor immediately. Keep in mind that it is possible to get pregnant even if you are using birth control. If this happens, stop taking misoprostol and contact your doctor immediately.
Misoprostol can cause diarrhoea, abdominal cramps and/or nausea in some people. In most cases, these problems arise during the first few weeks of treatment and disappear after about a week. You can minimize possible diarrhea by taking misoprostol with food.
Because these side effects are usually mild to moderate and usually disappear within a few days, most patients can continue to take misoprostol. If you have long-term problems (longer than 8 days), or if you have severe diarrhoea, cramps and/or nausea, please contact your doctor.
Take misoprostol only as directed by your doctor.
Do not give misoprostol to anyone else. It is prescribed for your specific condition, may not be the right treatment for another person, and would be dangerous if the other person is pregnant.
This information sheet does not cover all possible side effects of misoprostol. This Patient Information Leaflet does not discuss the side effects of your arthritis/pain medicines. Consult your doctor if you have any questions.
Keep out of reach of children.
All trademarks are the property of their respective owners.
Distributed by:
ANI Pharmaceuticals, Inc.
Baudette, MN 56623
Issued:09/2022
LB4429-02
NuCare Pharmaceuticals, Inc.
FAQs
How much misoprostol is needed oral? ›
Adults—200 micrograms (mcg) four times a day with food. Other patients may need 100 mcg four times a day with food. Take the last dose of the day at bedtime. Children—Use and dose must be determined by your doctor.
What is the maximum misoprostol? ›When used for cervical ripening, misoprostol can be administered orally, sublingually, or vaginally, although there is more evidence for vaginal regimens. A commonly used dose is 25 µg administered vaginally every 4 hours as needed, with a maximum dose of 150 µg.
What is the failure rate of misoprostol? ›A misoprostol-only regimen has lower success rates of about 80-85%, with continuing pregnancy rates of 3-10% and complication rates of 1-4% up to 13 weeks gestation.
How many doses of misoprostol for miscarriage? ›Missed abortion: Misoprostol 600mcg sublingually or, in the absence of vaginal bleeding, 800mcg vaginally every three hours until pregnancy expulsion (generally 1-3 doses). Where available, add pretreatment with mifepristone 200mg orally 1-2 days before misoprostol.
Can I take 800 mg misoprostol orally? ›Up to 13 weeks since the last menstrual period: 800 micrograms single dose sublingually or vaginally. If expulsion has not occurred within 24 hours administer a 2nd dose of 800 micrograms.
Should I take misoprostol orally or insert? ›Misoprostol tablets can be used either in the vagina, or under the tongue (sublingual). You and your doctor will discuss the best option for you. Misoprostol tablets should be placed deep into the vagina two hours before your planned admission time.
What happens if I take misoprostol orally? ›This medicine may cause diarrhea, stomach cramps, or nausea in some people. These effects will usually disappear within a few days as your body adjusts to the medicine. However, check with your doctor if the diarrhea, cramps, or nausea is severe and/or does not stop after a week.
How long does it take for misoprostol to soften cervix? ›Misoprostol comes in tablets that can be given by mouth or placed directly against the cervix. The medicine will be absorbed and will start softening your cervix over time. After several hours and several doses, you might end up 2 or 3 cm dilated, and, if you're lucky, perhaps in early labor.
Is 600 micrograms of misoprostol more effective than 400 micrograms? ›In this review, 400 µg of misoprostol were found to be safer than ³ 600 µg and just as effective.
Is misoprostol high risk? ›It may cause a pregnancy to end, premature birth, or birth defects. In rare cases, serious complications (such as uterine rupture) have occurred when misoprostol was used to start labor or end a pregnancy. These complications have resulted in harm to the unborn baby and mother.
Which of the misoprostol is more effective? ›
Administration of misoprostol by the sublingual route is better than the oral and vaginal routes for cervical ripening.
Do you get contractions with misoprostol? ›Oral misoprostol is effective at inducing (starting) labour. It is more effective than placebo, as effective as vaginal misoprostol and vaginal dinoprostone, and results in fewer caesarean sections than oxytocin.
Can I take 800 mg misoprostol for miscarriage? ›The recommended dose of misoprostol is 800 mcgs (4 200-mcg tablets) inserted vaginally. Study results have demonstrated that vaginal administration is more effective than oral use of misoprostol. One dose is about 70% effective, and 2 is about 84% effective.
How can I clean my uterus after a miscarriage naturally? ›- Take Rest and Proper Medications. Give yourself an ample amount of rest as it is paramount. ...
- Hot and Cold Compress. Most women feel headaches and body ache after miscarriage. ...
- Nutrient-rich diet. ...
- Manage Stress. ...
- Use of Herbs.
...
Oral Tablet.
| Quantity | Per unit | Price |
|---|---|---|
| 100 | $0.72 | $72.35 |
Following 400 µg oral misoprostol administration, the Serum misoprostol level increases rapidly and peaks at about 30 min.
Can you take misoprostol orally for miscarriage? ›You will be given tablets of misoprostol to place into the vagina, dissolve under your tongue or swallow. Your doctor will instruct you as to which route is best for your type of miscarriage. Vaginal administration of the tablets causes the least amount of side effects. They are easily placed in the back of the vagina.
Can I take too much misoprostol? ›Clinical signs that may indicate an overdose are sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea, fever, palpitations, hypotension, or bradycardia. Symptoms should be treated with supportive therapy.
Is misoprostol used to soften the cervix? ›Misoprostol is extensively used in obstetrics and has proved to be very effective cervical softening agent necessary intermination of pregnancy.
Can I take 400 mg misoprostol? ›In terms of tolerability, vaginal misoprostol of 400 ug was reported with fewer side effects and sublingual misoprostol of 600 ug was reported with more side effects. Misoprostol is a non-invasive, effective medical method for completion of abortion in missed abortion.
Can misoprostol rupture the uterus? ›
Studies has showed an overall uterine rupture rate of 0.05% after misoprostol and 0.11% after surgical abortion among women with an unscarred uterus.
How effective is misoprostol when taken sublingually? ›A pilot study has shown that repeated doses of sublingual misoprostol are useful in the medical management of first trimester miscarriages, with a success rate of 92%. The effects of misoprostol on the uterine cervix and contractility are crucial for successful abortion.
Can you give Cytotec orally? ›If you are taking this drug to prevent stomach ulcers, take it by mouth as directed by your doctor, usually four times a day. Take it after meals and at bedtime to minimize diarrhea. If you are taking this medication to end a pregnancy, take it by mouth exactly as directed by your doctor.
How do you know if your cervix is softening? ›Cervical Softening Symptoms
You may, for example, notice that your vaginal discharge is increasing or notice that you're losing your mucus plug (which can be lost all at once or slowly in small increments). You may also feel some mild pelvic pressure or cramping similar to menstrual pain as your cervix softens.
Getting up and moving around may help speed dilation by increasing blood flow. Walking around the room, doing simple movements in bed or chair, or even changing positions may encourage dilation. This is because the weight of the baby applies pressure to the cervix.
How do you know if your cervix is dilating? ›- Signs of Cervical Dilation. ...
- #1: “Lightening Crotch” or Vaginal Pain. ...
- #2: Backache and Menstrual Like Cramps. ...
- #3: Bloody Show – A Sign of Cervical Dilation. ...
- #4: Less Talking, But Possibly More Noise. ...
- #5: Intuition. ...
- #6: Less 'Politeness' – a Sign of Cervical Dilation.
Conclusion: Transvaginal application of 600 ug misoprostol (3 times every 6 hours) caused a higher rate of complete abortion compared with an application of 400 ug misoprostol. The side effect of both groups showed no statistical difference.
How effective is misoprostol 200 mcg? ›Of the 746 subjects who had no or minimal bleeding before misoprostol, 80% bled within 4 h and 98% within 24 h of using misoprostol. By day 7, 95% of women had a complete abortion. Side effects were aceptable in 85% of subjects, and 94% found the procedure acceptable.
What are the disadvantages of misoprostol? ›This medicine may cause diarrhea, stomach cramps, or nausea in some people. These effects will usually disappear within a few days as your body adjusts to the medicine. However, check with your doctor if the diarrhea, cramps, or nausea is severe and/or does not stop after a week.
What is the duration of action of misoprostol? ›Key facts: Route Onset of action Duration of action Oral 8 min ∼ 2 h∗ Sublingual 11 min ∼ 3 h Vaginal 20 min ∼ 4 h Rectal 100 min ∼ 4 h ∗After oral administration, uterine tonus develops, which is not followed by uterine contractions, unless repeated doses are given.
What is the warning of misoprostol? ›
IMPORTANT WARNING:
Misoprostol may cause miscarriages, premature labor, or birth defects. If you are a woman of childbearing age, you may take misoprostol to prevent ulcers only if you have had a negative pregnancy test in the past 2 weeks and if you use a reliable method of birth control while taking misoprostol.
With the completion rates using misoprostol falling between 71%–84%, there's still a chance that this strategy won't work, and surgical intervention will be required. That's true on top of the fact that medicated miscarriage is often reported to be more painful than natural miscarriage.
Is Cytotec absorbed quickly? ›In normal volunteers, Cytotec (misoprostol) is rapidly absorbed after oral administration with a Tmax of misoprostol acid of 12 ± 3 minutes and a terminal half-life of 20-40 minutes.
Is misoprostol more effective orally in first trimester? ›Oral administration of misoprostol is an effective alternative to vaginal administration in preinduction cervical ripening prior to first trimester pregnancy termination.
How can I open my cervix naturally? ›- Acupuncture.
- Breast stimulation.
- Castor oil.
- Enemas (injection of water or liquid into the rectum to clear the colon).
- Herbal supplements.
- Hot baths.
- Sexual intercourse.
- Transcutaneous electrical nerve stimulation (TENS).
Misoprostol (Cytotec) is safe and effective for induction of labor, although it is not approved by the Food and Drug Administration (FDA) for use in pregnancy.
Is misoprostol a Pitocin? ›Misoprostol is a synthetic prostaglandin analogue commonly used for labor induction. It causes uterine contractions and ripening of the cervix. Oxytocin sold under the brand name Pitocin among others, is a medication made from the peptide oxytocin and is used to cause contraction of the uterus to start labor.
How do I know if I passed everything after a miscarriage? ›Most of the tissue passes within 2 to 4 hours after the cramping and bleeding start. Cramping usually stops within a day. Light bleeding or spotting can go on for 4 to 6 weeks. Two weeks after the tissue passes, your ob-gyn may do an ultrasound exam or other tests to make sure all the tissue has passed.
Do they scrape your uterus after a miscarriage? ›Often, some of the pregnancy tissue remains in the uterus after a miscarriage. If it is not removed by scraping the uterus with a curette (a spoon-shaped instrument), you may bleed for a long time or develop an infection.
How do you remove a sac after a miscarriage? ›This treatment involves a surgical procedure known as a dilatation and curettage (D&C) which is done under a general anaesthetic. The procedure will remove any pregnancy tissue from your uterus. It is successful in 95 to 100 per cent of cases but there are small surgical risks.
What not to do after miscarriage? ›
No sex, tampons, or douching for 2 weeks.
We recommend waiting until after 2 normal periods to attempt pregnancy again.
Misoprostol is a medication that can prevent stomach ulcers if you also take NSAID medications. It reduces the amount of acid in your stomach, which protects your stomach lining. The brand name of this medication is Cytotec®.
What is 200 mcg of misoprostol? ›DOSAGE AND ADMINISTRATION
The recommended adult oral dose of misoprostol for reducing the risk of NSAID-induced gastric ulcers is 200 mcg four times daily with food. If this dose cannot be tolerated, a dose of 100 mcg can be used.
Misoprostol comes in tablets that can be given by mouth or placed directly against the cervix. The medicine will be absorbed and will start softening your cervix over time. After several hours and several doses, you might end up 2 or 3 cm dilated, and, if you're lucky, perhaps in early labor.
What is misoprostol 800 mg used for? ›Misoprostol is used to prevent ulcers in people who take certain arthritis or pain medicines, including aspirin, that can cause ulcers. It protects the stomach lining and decreases stomach acid secretion.
What is the success rate of oral misoprostol induction? ›In general, 20-30% of all pregnancies undergo IOL (8). A recent meta-analysis showed that oral misoprostol had the lowest caesarean section (CS) rate compared to other IOL medication (9). In this study, 85.5% of our patients had a successful vaginal delivery.
How long does it take for misoprostol to start contractions? ›This medicine causes cramping and bleeding to empty your uterus. For most people, the cramping and bleeding usually starts 1-4 hours after taking the misoprostol.
Which route is best for misoprostol? ›Administration of misoprostol by the sublingual route is better than the oral and vaginal routes for cervical ripening.
Why use misoprostol 200 mcg? ›Misoprostol helps to decrease your risk of serious ulcer complications such as bleeding. This medication protects your stomach lining by lowering the amount of acid that comes in contact with it.This medication is also used in combination with another drug (mifepristone) to end a pregnancy.
What is the use of misoprostol 600 mg? ›A: MISOPROST 600MCG TABLET heals peptic ulcers by reducing excessive stomach acid secretion caused due to prolonged NSAIDs use. It also stimulates the contraction of uterine muscles which helps in initiating labour pain, reducing postpartum bleeding and for inducing abortion during the early stages of pregnancy.
Does sublingual work faster than oral? ›
In general, they produce faster onset of action compared to orally ingested drug formulations. Drug absorption is relatively faster across the sublingual mucosa compared to the buccal mucosa due to the thinner epithelium.