Kontrac
Kontrac Uses, Dosage, Side Effects, Food Interaction and all others data.
Kontrac is a synthetic prostaglandin E1 analogue. It protects the GI mucosa by inhibiting basal, stimulated and nocturnal acid secretion and by reducing the volume of gastric secretions and increasing bicarbonate and mucus secretion. It also induces contractions of smooth muscle fibres of the myometrium and relaxation of the cervix uteri.
Kontrac is a prostaglandin E1 analog used to reduce the risk of NSAID induced gastric ulcers by reducing secretion of gastric acid from parietal cells. Kontrac is also used to manage miscarriages and used alone or in combination with mifepristone for first trimester abortions. An oral dose of misoprostol has an 8 minute onset of action and a duration of action of approximately 2 hours, a sublingual dose has an 11 minute onset of action and a duration of action of approximately 3 hours, a vaginal dose has a 20 minute onset of action and a duration of action of approximately 4 hours, and a rectal dose has a 100 minute onset of action and a duration of action of approximately 4 hours.
| Trade Name | Kontrac |
| Availability | Prescription only |
| Generic | Misoprostol |
| Misoprostol Other Names | Misoprostol, Misoprostolum |
| Related Drugs | omeprazole, famotidine, pantoprazole, Pepcid, Protonix, sucralfate, lansoprazole, Prevacid, oxytocin, Cytotec |
| Type | Tablet |
| Formula | C22H38O5 |
| Weight | Average: 382.5341 Monoisotopic: 382.271924326 |
| Protein binding | Misoprostol is 13,14 Its active metabolite, misoprostol acid, is 81-89% protein bound in serum. |
| Groups | Approved |
| Therapeutic Class | Drugs acting on the Uterus, Prostaglandin analogues |
| Manufacturer | Fourrts India Laboratories Pvt Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Antiulcerant Indication: Kontrac is used for reducing the risk of NSAID (nonsteroidal anti-inflammatory drugs, including aspirin) induced gastric ulcers in patients at high risk of complications from gastric ulcer, eg, the elderly and patients with concomitant debilitating disease, as well as patients at high risk of developing gastric ulceration, such as patients with a history of ulcer. Kontrac has not been shown to reduce the risk of duodenal ulcers in patients taking NSAIDs. Kontrac should be taken for the duration of NSAID therapy. It had no effect, compared to placebo, on gastrointestinal pain or discomfort associated with NSAID use.
Gynecological Indication: Labor induction (in unfavorable cervical conditions) In the prevention & treatment of Postpartum Hemorrhage (PPH)
Kontrac is also used to associated treatment for these conditions: Gastric Ulcer, Incomplete Abortion, Missed Abortion, Postpartum Haemorrhage (PPH), Induction of cervix ripening therapy, Medically induced abortion
How Kontrac works
Kontrac 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.
Kontrac 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.
Dosage
Kontrac dosage
Anti-ulcerant dosage & administration:
- The recommended adult oral dose for reducing the risk of NSAID-induced gastric ulcers:200 mcg Kontracfour times daily with food. If this dose cannot be tolerated, a dose of 100 mcg can be used. Kontracshould be taken for the duration of NSAID therapy as prescribed by the physician. Kontrac should be taken with a meal, and the last dose of the day should be at bedtime.
- Renal impairment: Adjustment of the dosing schedule in renally impaired patients is not routinely needed, but dosage can be reduced if the 200 mcg dose is not tolerated.
Gynecological dosage & administration-
- Induction of Labor: 25 mcg vaginally 6 hourly or, 50 mcg orally 4 hourly.
- Postpartum Hemorrhage (PPH) prophylaxis: 400 mcg to 600 mcg orally or rectally immediately following delivery of the child.
- Postpartum Hemorrhage (PPH) treatment: 1,000 mcg rectally or, 200 mcg orally with 400 mcg sublingually.
Side Effects
Gastrointestinal: GI disorders had the highest reported incidence of adverse events for patients receiving Kontrac. It can cause more abdominal pain, diarrhea and other GI symptoms. The incidence of diarrhea can be minimized by administering it with food and by avoiding co administration with magnesium-containing antacids.
Gynecological: Gynecological disorders such as spotting, cramps, hypermenorrhea, menstrual disorder and dysmenorrhea have been reported. Postmenopausal vaginal bleeding may be related to Kontrac administration.
Elderly: Overall, there were no significant differences in the safety profile in patients 65 years of age or older compared with younger patients.
Toxicity
The oral LD50 in rats is 81mg/kg and in mice is 27mg/kg. The intraperitoneal LD50 in rats is 40mg/kg and in mice is 70mg/kg.
Patients experiencing an overdose may present with sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea, fever, palpitations, hypotension, and bradycardia. Hemodialysis is not expected to be useful in the treatment of misoprostol overdose but oral activated charcoal may help reduce absorption. In the event of an overdose, treat symptoms with supportive therapy. This may include removal of undissolved tablets from the vagina or buccal cavity, intravenous fluid replacement, acetaminophen, diazepam, haloperidol, or intramuscular diclofenac depending on the symptoms that present.
Precaution
Precaution should be taken in conditions where hypertension might precipitate severe complications (e.g. cerebrovascular and cardiovascular disease).
Interaction
There is no evidence of clinically significant interaction between Kontrac and cardiac, pulmonary and CNS drugs and NSAIDs. Bioavailability of Kontrac is decreased with high doses of antacid.
Food Interaction
- Take with food. Food decreases incidence of diarrhea.
Kontrac Disease Interaction
Volume of Distribution
Data regarding the volume of distribution of misoprostol is scarce.
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.
Elimination Route
For an 800µg oral dose of misoprostol, the AUC was 2.0192±0.8032h*ng/mL, the Cmax was 2.6830±1.2161ng/mL, and a tmax of 0.345±0.186h. For a 800µg sublingual dose of misoprostol, the AUC was 3.2094±1.0417h*ng/mL, the Cmax was 2.4391±1.1567ng/mL, and a tmax of 0.712±0.415h. For a 800µg buccal dose of misoprostol, the AUC was 2.0726±0.3578h*ng/mL, the Cmax was 1.3611±0.3436ng/mL, and a tmax of 1.308±0.624h.
Half Life
The half life of an 800µg oral dose is 1.0401±0.5090h, for a sublingual dose is 0.8542±0.1170h, and for a buccal dose is 0.8365±0.1346h.
Clearance
Because of the rapid de-esterification of misoprostol before or during absorption, it is usually undetectable in plasma. Kontrac's active metabolite, misoprostol acid, has a total body clearance of 0.286L/kg/min. Subjects with mild renal impairment had a total body clearance of 0.226±0.073L/kg/min, subjects with moderate renal impairment had a total body clearance of 0.270±0.103L/kg/min, and subjects with end stage renal disease had a total body clearance of 0.105±0.052L/kg/min.
Elimination Route
As much as 73.2±4.6% of a radiolabelled oral dose of misoprostol is recovered in the urine.
Pregnancy & Breastfeeding use
Pregnancy: Kontrac is contraindicated to pregnant women.
Lactation: It is not known whether Kontrac's active metabolite- misoprostol acid is excreted in human milk. Kontrac should not be administered to nursing mothers because the excretion of misoprostol acid could cause diarrhea in nursing infants.
Contraindication
Kontrac is contraindicated to anyone with a history of allergy to prostaglandins and it is also contraindicated in pregnancy.
Acute Overdose
The toxic dose of Kontrac in human has not been determined. Clinical signs that may indicate an overdose are sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea and fever. Symptoms should be treated with supportive therapy.
Storage Condition
Store in a cool and dry place, protected from light and moisture. Keep out of the reach of the children
Innovators Monograph
You find simplified version here Kontrac
Kontrac contains Misoprostol see full prescribing information from innovator Kontrac Monograph, Kontrac MSDS, Kontrac FDA label
FAQ
What is Kontrac used for?
Kontrac is used to prevent and treat stomach and duodenal ulcers, induce labor, cause an abortion, and treat postpartum bleeding due to poor contraction of the uterus. Kontrac is taken by mouth when used to prevent gastric ulcers in persons taking NSAIDs.
How safe is Kontrac?
Kontrac is a safe method for people seeking to end their pregnancy. The medication softens and dilates the cervix, causes uterine contractions, and pushes pregnancy tissue out.
What does Kontrac do in the body?
Kontrac helps to decrease your risk of serious ulcer complications such as bleeding. It ends a pregnancy by blocking the action of the hormone (progesterone) that supports the pregnancy.
What are the common side effects of Kontrac?
The most common side effects of Kontrac include:
- diarrhea,
- stomach pain,
- nausea,
- upset stomach,
- gas,
- vaginal bleeding or spotting,
- heavy menstrual flow, and.
- menstrual cramps.
Is Kontrac safe during pregnancy?
Kontrac is a safe method for people seeking to end their pregnancy.
Is Kontrac safe during breastfeeding?
No interruption of breastfeeding is necessary when Kontrac is given by any route. As a precaution, infants exposed to Kontrac via breastmilk should be monitored for nausea, vomiting and poor feeding.
Can I drink alcohol with Kontrac?
Daily use of alcohol and tobacco may increase your risk for stomach bleeding.
Can I drive after talking Kontrac?
You can drive yourself after taking your Kontrac.
How do I take Kontrac?
Take the 4 Kontrac pills. Put 2 pills on one side of your mouth, and the other 2 on the other side of your mouth. Wait 3 minutes for the pill to dissolve. After 30 minutes, swallow what is left of the pills.
How many time can I take Kontrac daily?
Kontrac is usually taken 4 times a day.
Can I take Kontrac on an empty stomach?
Kontrac is best taken with or after meals and at bedtime, unless otherwise directed by your doctor.
How long is Kontrac active?
Kontrac by mouth is the least effective treatment for producing complete abortion in a period of 24 hours due to the liver's first-pass effect which reduces the bioavailability of the Kontrac.
How long does Kontrac stay in my system?
Kontrac has an elimination half life of 20-40 minutes. This means that after 20-40 minutes the substance has lost half of its pharmacologic activity.
How many days we can take Kontrac?
Vaginal Kontrac, 800 µg, can be used between 1 and 3 days after Kontrac, 200 mg, for abortion at up to 56 days' gestation, increasing the flexibility of the regimen.
How many doses of Kontrac is safe?
The recommended adult oral dose of Kontrac 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.
What happens if I take too much Kontrac?
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.
Can Kontrac affect future pregnancy?
Kontrac treatment, for women with first trimester missed abortion and favorable reproductive history, is an acceptable treatment with no detrimental effect on future fertility.
Who should not take Kontrac?
You should not use Kontrac if you are allergic to Kontrac or other prostaglandins, or if you are pregnant. To make sure Kontrac is safe for you, tell your doctor if you have: inflammatory bowel disease (IBD), irritable bowel syndrome (IBS), or other intestinal problems; heart disease;
What happens if I miss a dose?
Take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose of this medication.
Can I stop taking Kontrac?
Kontrac must be taken regularly to be effective. Women should not take their first dose until the second or third day of their menstrual period (to be sure that they are not pregnant). Do not stop taking Kontrac without talking to your doctor.
Can Kontrac cause damage to the womb?
Kontrac can cause birth defects, premature birth, uterine rupture, miscarriage, or incomplete miscarriage and dangerous uterine bleeding.
When should Kontrac be repeated?
Women of more than 9 weeks pregnancy according to last menstrual period will be given a choice of vacuum aspiration or further medical treatment with 2 additional doses of Kontrac given after 7 and 9 hours after the initial vaginal treatment.
Can Kontrac cause heart problems?
This Kontrac may raise the risk of heart and blood vessel problems like heart attack and stroke. These effects can be deadly. The risk may be greater if you have heart disease or risks for heart disease.
Can Kontrac affects my liver?
Mifepristone with Kontrac have not been associated with serum enzyme elevations or with clinically apparent liver injury.
Can Kontrac cause stroke?
Higher doses of Kontrac used for termination of pregnancy (800 μg or higher) can rarely lead to profound hypotension, carry a theoretical risk of coronary vasospasm and a low risk of arrhythmias and stroke.
Can Kontrac affect my kidneys?
Overall, the results indicate that low-dose Kontrac is vasodilatory, natriuretic, and diuretic whereas high-dose Kontrac increases renal vascular tone and inhibits sodium and water excretion.
