Esmart

Esmart Uses, Dosage, Side Effects, Food Interaction and all others data.

Misoprostol 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.

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. 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.

Esmart
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Esmart
Generic	Diclofenac (Na) + Misoprostol
Weight	75mg, 0mg, 50mg
Type	Tablet
Therapeutic Class
Manufacturer	Pharmevo (pvt) Ltd,
Available Country	Pakistan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Antiulcerant Indication: Misoprostol 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. Misoprostol has not been shown to reduce the risk of duodenal ulcers in patients taking NSAIDs. Misoprostol 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)

Esmart 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 Esmart works

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.

Dosage

Esmart dosage

Anti-ulcerant dosage & administration:

The recommended adult oral dose for reducing the risk of NSAID-induced gastric ulcers:200 mcg Misoprostolfour times daily with food. If this dose cannot be tolerated, a dose of 100 mcg can be used. Misoprostolshould be taken for the duration of NSAID therapy as prescribed by the physician. Misoprostol 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 Misoprostol. 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 Misoprostol 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 Misoprostol and cardiac, pulmonary and CNS drugs and NSAIDs. Bioavailability of Misoprostol is decreased with high doses of antacid.

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 C_max was 2.6830±1.2161ng/mL, and a t_max of 0.345±0.186h. For a 800µg sublingual dose of misoprostol, the AUC was 3.2094±1.0417h*ng/mL, the C_max was 2.4391±1.1567ng/mL, and a t_max of 0.712±0.415h. For a 800µg buccal dose of misoprostol, the AUC was 2.0726±0.3578h*ng/mL, the C_max was 1.3611±0.3436ng/mL, and a t_max 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. Misoprostol'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: Misoprostol is contraindicated to pregnant women.

Lactation: It is not known whether Misoprostol's active metabolite- misoprostol acid is excreted in human milk. Misoprostol should not be administered to nursing mothers because the excretion of misoprostol acid could cause diarrhea in nursing infants.

Contraindication

Misoprostol is contraindicated to anyone with a history of allergy to prostaglandins and it is also contraindicated in pregnancy.

Acute Overdose

The toxic dose of Misoprostol 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.