Mergot

Tablet: Each tablet contains: Methylergometrine maleate, USP 125 mcg.
Methylergometrine maleate is a drug that has action on the uterus similar to that of ergometrine maleate and is used similarly in the prevention and treatment of postpartum hemorrhage.
Injection: Clear colorless solution free from extraneous particles.
Each mL contains: Methylergometrine Maleate, USP 200 mcg (Methylergonovine Maleate).

Pharmacology: Injection: Mechanism of Action: Methylergometrine maleate acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss.
Pharmacokinetics: Tablet: Methylergometrine Maleate is reportedly to be rapidly absorbed after administration by mouth and intramuscular injection. Elimination is rapid and appears to be by hepatic and renal routes. The absorption and fate of Methylergometrine Maleate had been studied following oral administration in healthy subjects and in postpartum women. Small amounts of Methylergometrine have been detected in breast milk.
Injection: Methylergometrine maleate is rapidly distributed from plasma to peripheral tissues within 2-3 minutes or less. During delivery, with intramuscular injection, bioavailability increased to 78%.
When given intramuscularly, the extent of absorption of Methylergometrine maleate solution was about 25% greater than the tablet. The volume of distribution Vdss/F of methylergometrine was calculated to be 56.1 ± 17.0 liters. The plasma level decline was biphasic with a mean elimination half-life of 3.39 hours (range 1.5 to 12.7 hours).

Tablet: Methylergometrine Maleate is used for the prevention and treatment of postpartum hemorrhage.
Injection: Used in the active management of the third stage of labour, and in the prevention and treatment of postpartum or postabortal haemorrhage.

Tablet: 4 tablets (500 mcg) three times daily for three days or as prescribed by the physician.
Injection: Parental drug products should be inspected visually for particulate matter and discoloration prior to administration.
Intramuscularly: 1 mL, 0.2 mg, after delivery of the anterior shoulder, after delivery of the placenta, or during the puerperium. May be repeated as required, at intervals of 2-4 hours.
Intravenously: Dosage same as intramuscular. Or as prescribed by the physician.

Injection: Symptoms of acute overdose may include: nausea, vomiting, abdominal pain, numbness, tingling of the extremities, rise in blood pressure, in severe cases followed by hypotension, respiratory depression, hypothermia, convulsions, and coma.
Removal of offending drug by including emesis, gastric lavage, cartharsis and supportive diuresis.
Maintenance of adequate pulmonary ventilation, especially if convulsions or coma develop.
Correction of hypotension with pressor drugs as needed.
Control of convulsions with standard anticonvulsant agents.
Control of peripheral vasospasm with warmth to the extremities if needed.

Injection: Hypertension, toxemia, pregnancy and hypersensitivity.

Tablet: Methylergometrine Maleate should not be used for the induction of labor or during the first stage of labor. Its use should also be avoided in patients with eclampsia.

Injection: Use in Pregnancy & Lactation: See Contraindications for further information.

Tablet: Adverse effects include nausea and vomiting. Hypertension also occurs after intravenous administration.
Injection: The most common adverse reaction is hypertension associated in several cases with seizure and/or headache.
Hypotension has also been reported.
Nausea and vomiting have occurred occasionally.
Rarely observed reactions have included: acite myocardial infarction, transient chest pains, arterial spasm (coronary and peripheral), bradycardia, tachycardia, dyspnea, hematuria, thrombophlebitis, water intoxication, hallucinations, leg cramps, dizziness, tinnitus, nasal congestion, diarrhea, diaphoresis, palpitation, rash, and foul taste.
There have been rare isolated reports of anaphylaxis, without a proven causal relationship to the drug product.

Injection: Some products that may interact with this drug include: Other ergot alkaloids(such as ergotamine, dihydroergotamine), "triptan" migraine medications (such as eletriptan, rizatriptan, sumatriptan).
Other medications can affect the removal of methylergometrine from body.
Examples include: azole antifungals (such as itraconazole, ketoconazole), macrolide antibiotics (such as erythromycin, clarithromycin), HIV protease inhibitors (such as ritonavir), HIV NNRTI's (such as delavirdine, efavirenz), among others. Grapefruit and grapefruit juice may interact with methylergometrine. The interaction could lead to potentially dangerous effects.

Tablet: Store at temperatures not exceeding 30°C.
Injection: Store at 2°C between 8°C.

Drugs Acting on the Uterus

G02AB01 - methylergometrine ; Belongs to the class of ergot alkaloids. Used to induce abortion or augment labour and to minimize blood loss from the placental site.

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