Misoprostol is a medication that is used for various medical purposes, primarily related to the gastrointestinal tract and reproductive health. It is a synthetic prostaglandin E1 (PGE1) analog.

Misoprostol (Cytotec) belongs to the class of drugs called prostaglandin analogs. It is used in the treatment and prevention of NSAID-induced gastric ulcers and post-partum hemorrhage. It is also used in the induction of labor and termination of early pregnancy in combination with mifepristone.

Misoprostol (Cytotec) Uses:

• NSAID-induced gastric ulcers, prevention:
  • It is to reduce the risk of NSAID-induced gastric ulcers in patients at high risk of complications.
• Termination of intrauterine pregnancy:
  • Medical termination of intrauterine pregnancy through 70 days' gestation in combination with mifepristone (Mifeprex prescribing information March 2016)
• Off Label Use of Misoprostol in Adults:
  • Cervical ripening and labor induction
  • Early pregnancy loss
  • Treatment of incomplete or missed abortion
  • Prevention and treatment of Postpartum hemorrhage.

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Misoprostol Dose in Adults:

Misoprostol (Cytotec) Dose in the prevention of NSAID-induced gastric ulcers:

• The recommended dose when taken by mouth is 200 micrograms (mcg) four times a day.
• If this higher dose is not well tolerated (causes discomfort or side effects), the doctor may reduce it to 100 mcg four times a day.
• This helps keep your stomach safe from these ulcers.

Misoprostol (Cytotec) Dose in the treatment of Termination of intrauterine pregnancy:

• Refer to the Mifepristone monograph.

Misoprostol (Cytotec) Dose in the treatment of early pregnancy loss (off-label):

• When given through the vaginal route, the initial dose is 800 micrograms (mcg).
• If necessary, this dose can be repeated with a single dose, but it should be done at least three hours after the first dose.
• If there is no response to the initial dose within seven days, another dose can be considered.

Misoprostol (Cytotec) Dose in the treatment of Incomplete abortion (off-label):

• The recommended dose when taken by mouth is 600 micrograms (mcg) given one time.

Misoprostol (Cytotec) Dose in the treatment of Labor induction or cervical ripening (off-label):

Intravaginal (putting the medicine inside the vagina):

• Dose: 25 micrograms (mcg), which is one-fourth of a 100 mcg tablet.
• This dose can be repeated, but not more often than every 3 to 6 hours.
• In some cases, a dose of 50 mcg every 6 hours might be used.

Oral (taken by mouth):

• Dose: 25 mcg (one-fourth of a 100 mcg tablet) given every 2 hours.
• Some studies have also looked at doses of 20 mcg given every 2 hours.

Some things to note:

• Using misoprostol in the vagina might work better for this purpose, but taking it orally might have fewer side effects.
• Misoprostol should not be used under the tongue (sublingual) or in the cheek (buccal) for inducing labor or preparing the cervix.
• The best dose and way to give misoprostol for this use might still need more research.

 

Misoprostol (Cytotec) Dose in the treatment of Missed abortion (off-label):

Intravaginal (putting the medicine inside the vagina):

• Dose: 800 micrograms (mcg).
• If necessary, this dose can be repeated every 3 hours, but only for 2 more doses.

Sublingual (placing the medicine under the tongue):

• Dose: 600 micrograms (mcg).
• Similarly, if needed, this dose can be repeated every 3 hours, but only for 2 additional doses.

Misoprostol (Cytotec) Dose in the prevention of Postpartum hemorrhage (off-label):

Oral (taken by mouth):

• Dose: 600 micrograms (mcg) given as a one-time dose right after delivery.

It's important to note:

• There can be side effects when using misoprostol, and these might depend on the dose and how the medicine is given.
• More research may be needed to find the best dose and way to give misoprostol for this use.

Misoprostol (Cytotec) Dose in the treatment of Postpartum hemorrhage (off-label):

Oral (taken by mouth):

• Dose: Between 600 and 1,000 micrograms (mcg) given as a one-time dose.

Rectal (putting the medicine into the rectum):

• Dose: Between 600 and 1,000 mcg given as a single dose.

Sublingual (placing the medicine under the tongue):

• Dose: 800 mcg given once. If a preventive dose was given earlier, especially if there were side effects, you should be careful with this method.
• Some guidelines mention doses ranging from 600 to 1,000 mcg given once. Yet, a smaller dose of 400 mcg has also been recommended by some experts.

Important things to consider:

• Misoprostol can have side effects, and the type and severity might vary depending on the dose and how it's given.
• More studies may be needed to know the best dose and method for using misoprostol in this situation.

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Use in Children:

Not indicated.

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Misoprostol (Cytotec) Pregnancy Risk Category: X

• Pregnant women shouldn't take misoprostol to prevent ulcers caused by pain relievers because it can lead to birth defects, miscarriage, early birth, or severe womb damage, especially during labor or if trying to end a pregnancy.
• The risk is even higher for women who had previous surgeries on their womb, like a C-section.
• Misoprostol can also cause strong womb contractions which might harm the baby, result in a miscarriage, or damage the womb.
• Doctors do use it with another drug to safely end pregnancies up to 70 days.
• It's also used in certain cases like when there's an incomplete miscarriage, early pregnancy loss, or severe bleeding after childbirth.
• However, for heavy bleeding after childbirth, it's often used when a more common drug isn't available.
• How the drug is given - by mouth, under the tongue, in the vagina, or rectum - can affect how it works and its side effects, like intense womb contractions or fever.
• Women who can still have children should be very cautious with misoprostol; they must ensure they're not pregnant and follow strict birth control measures.
• Sharing this drug is a big no because of its serious effects.

Use during breastfeeding:

• Misoprostol turns into misoprostol acid in the body, and this is what gets into breast milk.
• When a mother takes the drug orally, the highest amount in her milk is usually seen within an hour and then drops over the next 5 hours.
• To reduce the amount the baby gets, some experts suggest mothers take misoprostol right after feeding their baby, so by the next feeding, much of the drug has left the milk.
• No harmful effects have been noted in babies who breastfeed from mothers taking misoprostol.
• Still, the company that makes the drug advises being cautious when giving it to breastfeeding women.

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Cytotec Dose in Kidney Disease:

• If someone has kidney problems, they usually don't need to change the dose of misoprostol.
• But, if they experience side effects, the dose might be decreased.
• It's unclear if dialysis can remove misoprostol from the body.

Cytotec Dose in Liver disease:

• If someone has liver problems, the manufacturer doesn't provide any specific changes to the misoprostol dose in their guidelines.

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Common Side Effects of Misoprostol (Cytotec):

• Gastrointestinal:
  • Diarrhea
  • Abdominal pain

Less Common Side Effects of Misoprostol (Cytotec):

• Central nervous system:
  • Headache
• Gastrointestinal:
  • Constipation
  • Dyspepsia
  • Flatulence
  • Nausea
  • Vomiting

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Contraindications to Misoprostol (Cytotec):

• People shouldn't take misoprostol if they are allergic to it, other similar drugs called prostaglandins, or any ingredient in the medication.
• It should not be taken during pregnancy.
• If misoprostol is being used to end a pregnancy, there are additional reasons someone shouldn't take it, and these can be found in the guidelines for a drug called mifepristone.

Warnings and precautions

Abortifacient: [US Boxed Warning]:

• [US Warning]: Misoprostol can cause miscarriages.
• Because of this, patients need to be clearly warned not to share this medicine with others.

Cardiovascular disease

• Be careful when giving misoprostol to people with heart problems.

Renal impairment

• Be careful when giving misoprostol to people with kidney problems; they might need a different dose.

Misoprostol: Drug Interaction

Risk Factor C (Monitor therapy)
Phenylbutazone	May enhance the neurotoxic effect of MiSOPROStol. Specifically, the combination may result in headaches, dizziness, and transient diplopia.
Risk Factor D (Consider therapy modification)
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 the effects of oxytocin, particularly when given within 4 hours of oxytocin initiation.
Risk Factor X (Avoid combination)
Antacids	May enhance the adverse/toxic effect of MiSOPROStol. More specifically, concomitant use of 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). Exceptions: Aluminum Hydroxide; Calcium Carbonate; Potassium Bicarbonate; Sodium Bicarbonate.
Carbetocin	MiSOPROStol may enhance the adverse/toxic effect of Carbetocin. Specifically, Carbetocin oxytocic effects may be enhanced.

Monitoring parameters:

Preventing Stomach Ulcers from Pain Relievers:

• Check if women can become pregnant with a pregnancy test before starting therapy.
• If there's unexplained vaginal bleeding, figure out its cause.

Using in Pregnancy-related Situations:

• Monitoring during use: Keep an eye on womb activity and the baby's health.
• For incomplete or missed abortion:
  • Check the situation 1 to 2 weeks after giving the medicine.
• Ending a Pregnancy:
  • Before the procedure: Confirm if the woman is pregnant, know her Rh blood status, and if she might be anemic, check her blood levels.
  • After the procedure: Make sure the pregnancy has fully ended using an exam, a hormone test (hCG), or ultrasound. If there's heavy bleeding, check blood levels. If a woman feels sick, throws up, or has diarrhea and feels weak (but doesn't have a fever or other signs of infection) more than a day after taking misoprostol, check her full blood count.
• Managing Early Pregnancy Loss:
  • Check the Rh blood status.
  • 7 days after the first dose, see how the treatment is working.

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How to administer Misoprostol (Cytotec)?

• Take it with food.
• Don't take it with antacids that have magnesium (this can help prevent diarrhea).
• The last dose each day should be taken before going to sleep.
• Continue taking misoprostol as long as you're on the pain relievers that can cause stomach ulcers.

Ending a Pregnancy:

• Look at the guidelines for the drug Mifepristone.

Starting Labor or Preparing for Labor (Off-label uses):

• Since the suggested doses often mean breaking up tablets, it's a good idea to weigh the pieces or make a solution to make sure the right dose is given.

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Mechanism of action of Misoprostol (Cytotec):

• It's a man-made version of a natural body substance called prostaglandin E.
• It's used to replace the protective substances in our stomach that get used up when taking certain medicines like NSAIDs.
• It can also cause the uterus (womb) to contract, which is why it's used in some pregnancy-related situations.

How quickly it works:

• Starts to inhibit stomach acid in about 30 minutes.

How long it lasts:

• Keeps inhibiting stomach acid for 3 hours.

Absorption:

• Gets into the body quickly and in large amounts.
• Food can slow down how much of its active form, misoprostol acid, gets absorbed.

Binding with proteins in the body:

• Misoprostol acid binds with less than 90% of proteins.

Processing in the body (Metabolism):

• Processed in the liver.
• Quickly turns into misoprostol acid, which is active and does the job.

How long it stays in the body (Half-life):

• Misoprostol acid: 20 to 40 minutes.

When it reaches its highest level in the blood:

• Misoprostol acid: Around 12 ± 3 minutes when fasting.

How it leaves the body:

• Mainly through urine (80%).

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International Brand Names of Misoprostol:

• Cytotec
• NOVO-Misoprostol
• PMS-Misoprostol
• Aboprost
• Alsoben
• Asotec
• Chromalux
• Cyprostil
• Cyprostol
• Cyrux
• Cytil
• Cytolog
• Cytotec
• Dazitum
• Gastrul
• Gymiso
• Herwont
• Isovent
• Mipros
• Mirolut
• Misel
• Miso-Fem
• Misoclear
• Misodel
• Misodex
• Misofar
• MisoOne
• Misoone
• Misopa
• Misoprost
• Misoprost-200
• Misotac
• Misotrol
• Mispregnol
• Misprolen
• Misprosmek
• Mysodelle
• Myspess
• Mystol
• Noprostol
• Prosomed
• Taneciprol
• Topogyne
• U-Miso
• Vagiprost

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Misoprostol Brand Names in Pakistan:

Misoprostol Tablets 25 mcg
Mite	Genix Pharma (Pvt) Ltd
S.T Mom	Zafa Pharmaceutical Laboratories (Pvt) Ltd.
Stmom	Zafa Pharmaceutical Laboratories (Pvt) Ltd.

Misoprostol Tablets 50 mcg
Mite	Genix Pharma (Pvt) Ltd

Misoprostol Tablets 100 mcg
Mitek	Genix Pharma (Pvt) Ltd
Prosotec	Atco Laboratories Limited
Tector	Macter International (Pvt) Ltd.
Zivus	Wilshire Laboratories (Pvt) Ltd.

Misoprostol Tablets 200 mcg
Breeky	Sami Pharmaceuticals (Pvt) Ltd.
Cyotec	Biogen Pharma
Cytotol	Saffron Pharmaceutical Company
Miso	Global Pharmaceuticals
Misoclear	Zafa Pharmaceutical Laboratories (Pvt) Ltd.
Mite	Genix Pharma (Pvt) Ltd
Prosotec	Atco Laboratories Limited
Stmom	Zafa Pharmaceutical Laboratories (Pvt) Ltd.
Tector	Macter International (Pvt) Ltd.
Zivus	Wilshire Laboratories (Pvt) Ltd.