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Utergin

Name: Utergin drug & pharmaceuticals. Utergin available forms, doses, prices
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Published: 2021-11-11T10:10:10+00:00

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Utergin uses

Description
Clinical pharmacology
Indications and usage
Contraindications
Warnings
Precautions
Adverse reactions
Drug abuse and dependence
Overdosage
Dosage and administration
How supplied
Utergin reviews

Utergin ^®

(methylergonovine maleate)

Tablets, USP

(methylergonovine maleate)

Injection, USP

Rx only

DESCRIPTION

Utergin^® (methylergonovine maleate) is a semi-synthetic ergot alkaloid used for the prevention and control of postpartum hemorrhage.

Utergin is available in sterile ampuls of 1 mL, containing 0.2 mg Utergin for intramuscular or intravenous injection and in tablets for oral ingestion containing 0.2 mg Utergin.

Tablets

Active Ingredient: Utergin, USP, 0.2 mg.

Inactive Ingredients: acacia, carnauba wax, D&C Red #7, FD&C Blue #1, gelatin special, lactose, maleic acid, mixed parabens, povidone, sodium benzoate, sodium hydroxide, starch, stearic acid, sucrose, talc, and titanium dioxide.

Ampuls, 1 mL, clear, colorless solution.

Active Ingredient: Utergin, USP, 0.2 mg.

Inactive Ingredients: maleic acid, 0.10 mg; sodium chloride, 7.0 mg; water for injection, qs to 1 mL.

Chemically, Utergin is designated as ergoline-8-carboxamide, 9,10-didehydro-N-[1-(hydroxymethyl)propyl]-6-methyl-, [8β(S)]-, (Z)-2-butenedioate (1:1) (salt).

Its structural formula is

CLINICAL PHARMACOLOGY

Utergin (methylergonovine 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. The onset of action after I.V. administration is immediate; after I.M. administration, 2-5 minutes, and after oral administration, 5-10 minutes.

Pharmacokinetic studies following an I.V. injection have shown that methylergonovine is rapidly distributed from plasma to peripheral tissues within 2-3 minutes or less. The bioavailability after oral administration was reported to be about 60% with no accumulation after repeated doses. During delivery, with intramuscular injection, bioavailability increased to 78%. Ergot alkaloids are mostly eliminated by hepatic metabolism and excretion, and the decrease in bioavailability following oral administration is probably a result of first-pass metabolism in the liver.

Bioavailability studies conducted in fasting healthy female volunteers have shown that oral absorption of a 0.2 mg methylergonovine tablet was fairly rapid with a mean peak plasma concentration of 3243 ± 1308 pg/mL observed at 1.12 ± 0.82 hours. For a 0.2 mg intramuscular injection, a mean peak plasma concentration of 5918 ± 1952 pg/mL was observed at 0.41 ± 0.21 hours. The extent of absorption of the tablet, based upon methylergonovine plasma concentrations, was found to be equivalent to that of the I.M. solution given orally, and the extent of oral absorption of the I.M. solution was proportional to the dose following administration of 0.1, 0.2, and 0.4 mg. When given intramuscularly, the extent of absorption of Utergin solution was about 25% greater than the tablet. The volume of distribution (Vd_ss/F) of methylergonovine was calculated to be 56.1 ± 17.0 liters, and the plasma clearance (CLp/F) was calculated to be 14.4 ± 4.5 liters per hour. The plasma level decline was biphasic with a mean elimination half-life of 3.39 hours (range 1.5 to 12.7 hours). A delayed gastrointestinal absorption (T_max about 3 hours) of Utergin tablet might be observed in postpartum women during continuous treatment with this oxytocic agent.

INDICATIONS AND USAGE

Following delivery of the placenta, for routine management of uterine atony, hemorrhage and subinvolution of the uterus. For control of uterine hemorrhage in the second stage of labor following delivery of the anterior shoulder.

CONTRAINDICATIONS

Hypertension; toxemia; pregnancy; and hypersensitivity.

WARNINGS

General

This drug should not be administered I.V. routinely because of the possibility of inducing sudden hypertensive and cerebrovascular accidents. If I.V. administration is considered essential as a lifesaving measure, Utergin (methylergonovine maleate) should be given slowly over a period of no less than 60 seconds with careful monitoring of blood pressure. Intra-arterial or periarterial injection should be strictly avoided.

Caution should be exercised in the presence of impaired hepatic or renal function.

Breast-feeding

Mothers should not breast-feed during treatment with Utergin. Milk secreted during this period should be discarded. Utergin may produce adverse effects in the breast-feeding infant. Utergin may also reduce the yield of breast milk. Mothers should wait at least 12 hours after administration of the last dose of Utergin before initiating or resuming breast feeding.

Coronary artery disease

Patients with coronary artery disease or risk factors for coronary artery disease (e.g., smoking, obesity, diabetes, high cholesterol) may be more susceptible to developing myocardial ischemia and infarction associated with methylergonovine-induced vasospasm.

Medication errors

Inadvertent administration of Utergin to newborn infants has been reported. In these cases of inadvertent neonatal exposure, symptoms such as respiratory depression, convulsions, cyanosis and oliguria have been reported. Usual treatment is symptomatic. However, in severe cases, respiratory and cardiovascular support is required.

Utergin has been administered instead of vitamin K and Hepatitis B vaccine, medications which are routinely administered to the newborn. Due to the potential for accidental neonatal exposure, Utergin injection should be stored separately from medications intended for neonatal administration.

PRECAUTIONS

General

Caution should be exercised in the presence of sepsis, obliterative vascular disease. Also use with caution during the second stage of labor. The necessity for manual removal of a retained placenta should occur only rarely with proper technique and adequate allowance of time for its spontaneous separation.

Drug Interactions

CYP 3A4 Inhibitors

There have been rare reports of serious adverse events in connection with the coadministration of certain ergot alkaloid drugs (e.g., dihydroergotamine and ergotamine) and potent CYP 3A4 inhibitors, resulting in vasospasm leading to cerebral ischemia and/or ischemia of the extremities. Although there have been no reports of such interactions with methylergonovine alone, potent CYP 3A4 inhibitors should not be coadministered with methylergonovine. Examples of some of the more potent CYP 3A4 inhibitors include macrolide antibiotics (e.g., erythromycin, troleandomycin, clarithromycin), HIV protease or reverse transcriptase inhibitors (e.g., ritonavir, indinavir, nelfinavir, delavirdine) or azole antifungals (e.g., ketoconazole, itraconazole, voriconazole). Less potent CYP 3A4 inhibitors should be administered with caution. Less potent inhibitors include saquinavir, nefazodone, fluconazole, grapefruit juice, fluoxetine, fluvoxamine, zileuton, and clotrimazole. These lists are not exhaustive, and the prescriber should consider the effects on CYP 3A4 of other agents being considered for concomitant use with methylergonovine.

CYP3A4 inducers

Drugs (e.g. nevirapine, rifampicin) that are strong inducers of CYP3A4 are likely to decrease the pharmacological action of Utergin.

Beta-blockers

Caution should be exercised when Utergin is used concurrently with beta-blockers. Concomitant administration with beta-blockers may enhance the vasoconstrictive action of ergot alkaloids.

Anesthetics

Anesthetics like halothan and methoxyfluran may reduce the oxytocic potency of Utergin.

Glyceryl trinitrate and other antianginal drugs

Utergin produces vasoconstriction and can be expected to reduce the effect of glyceryl trinitrate and other antianginal drugs.

No pharmacokinetic interactions involving other cytochrome P450 isoenzymes are known.

Caution should be exercised when Utergin (methylergonovine maleate) is used concurrently with other vasoconstrictors, ergot alkaloids, or prostaglandins.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term studies have been performed in animals to evaluate carcinogenic potential. The effect of the drug on mutagenesis or fertility has not been determined.

Pregnancy

Category C. Animal reproductive studies have not been conducted with Utergin. It is also not known whether Utergin can cause fetal harm or can affect reproductive capacity. Use of Utergin is contraindicated during pregnancy because of its uterotonic effects.

Labor and Delivery

The uterotonic effect of Methergine is utilized after delivery to assist involution and decrease hemorrhage, shortening the third stage of labor.

Nursing Mothers

Mothers should not breast-feed during treatment with Utergin and at least 12 hours after administration of the last dose. Milk secreted during this period should be discarded.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Clinical studies of Utergin did not include sufficient number of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in response between the elderly and younger patients. In general dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

ADVERSE REACTIONS

The most common adverse reaction is hypertension associated in several cases with seizure and/or headache. Hypotension has also been reported. Abdominal pain (caused by uterine contractions), nausea and vomiting have occurred occasionally. Rarely observed reactions have included: acute myocardial infarction, transient chest pains, vasoconstriction, vasospasm, coronary arterial spasm, 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.

Postmarketing Experience

The following adverse drug reactions have been derived from post-marketing experience with Utergin via spontaneous case reports. Because these reactions are reported voluntarily from a population of uncertain size, it is not possible to reliably estimate their frequency which is therefore categorized as not known.

Nervous system disorders

Cerebrovascular accident, paraesthesia

Cardiac disorders

Ventricular fibrillation, ventricular tachycardia, angina pectoris, atrioventricular block

DRUG ABUSE AND DEPENDENCE

Utergin (methylergonovine maleate) has not been associated with drug abuse or dependence of either a physical or psychological nature.

OVERDOSAGE

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.

Because reports of overdosage with Utergin (methylergonovine maleate) are infrequent, the lethal dose in humans has not been established. The oral LD₅₀ (in mg/kg) for the mouse is 187, the rat 93, and the rabbit 4.5. Several cases of accidental Utergin injection in newborn infants have been reported, and in such cases 0.2 mg represents an overdose of great magnitude. However, recovery occurred in all but one case following a period of respiratory depression, hypothermia, hypertonicity with jerking movements, and convulsions.

Also, several children 1-3 years of age have accidentally ingested up to 10 tablets (2 mg) with no apparent ill effects. A postpartum patient took 4 tablets at one time in error and reported paresthesias and clamminess as her only symptoms.

Treatment of acute overdosage is symptomatic and includes the usual procedures of:

removal of offending drug by inducing emesis, gastric lavage, catharsis, 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.

DOSAGE AND ADMINISTRATION

Parenteral 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

1 mL, 0.2 mg, administered slowly over a period of no less than 60 seconds

Orally

One tablet, 0.2 mg, 3 or 4 times daily in the puerperium for a maximum of 1 week.

HOW SUPPLIED

Tablets

0.2 mg round, coated, orchid, branded “78-54” one side, “SANDOZ” other side.

Bottles of 100…………………………………………………………..NDC 0078-0054-05

Ampuls

1 mL size

Boxes of 20…………………………………………………………….NDC 0078-0053-03

Store and Dispense

Tablets: Store below 25°C (77°F); in tight, light-resistant container.

Ampuls: Store in refrigerator, 2ºC-8°C (36°F-46°F). Protect from light. Administer only if solution is clear and colorless.

Distributed by:

Novartis Pharmaceuticals Corporation

East Hanover, New Jersey 07936

T2012-125

June 2012

Utergin structural formula.

Utergin pharmaceutical active ingredients containing related brand and generic drugs:

Methylergonovine Maleate

Utergin available forms, composition, doses:

Injectable; Injection; Methylergonovine Maleate 0.2 mg / ml
Tablets, Film-Coated; Oral; Methylergonovine Maleate 0.125 mg
Tablets; Oral; Methylergonovine Maleate 0.125 mg

Utergin destination | category:

Human:
Drugs acting on the uterus

Utergin Anatomical Therapeutic Chemical codes:

G02AB01 - Methylergometrine

Utergin pharmaceutical companies:

References

Dailymed."METHERGINE (METHYLERGONOVINE MALEATE) TABLET, COATED [BRYANT RANCH PREPACK]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
"methylergonovine". https://pubchem.ncbi.nlm.nih.gov/co... (accessed August 28, 2018).
"methylergonovine". http://www.drugbank.ca/drugs/DB0035... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Utergin?

Depending on the reaction of the Utergin after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Utergin not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is Utergin addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

Review

sdrugs.com conducted a study on Utergin, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Utergin consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.