Lerin
Lerin Uses, Dosage, Side Effects, Food Interaction and all others data.
Lerin is an ergot alkaloid, which directly stimulates contractions of uterine and vascular smooth muscle.
Lerin is a semisynthetic ergot alkaloid and a derivative of ergonovine and is used for the prevention and control of postpartum and post-abortion hemorrhage. In general, the effects of all the ergot alkaloids appear to results from their actions as partial agonists or antagonists at adrenergic, dopaminergic, and tryptaminergic receptors. The spectrum of effects depends on the agent, dosage, species, tissue, and experimental or physiological conditions. All of the alkaloids of ergot significantly increase the motor activity of the uterus. After small doses contractions are increased in force or frequency, or both, but are followed by a normal degree of relaxation. As the dose is increased, contractions become more forceful and prolonged, resting tonus is markedly increased, and sustained contracture can result.
| Trade Name | Lerin |
| Generic | Methylergometrine |
| Methylergometrine Other Names | Ergotyl, Methylergobasin, Methylergometrin, Méthylergométrine, Methylergometrine, Methylergometrinum, Methylergonovine, Metilergometrina, Metilergometrinio |
| Type | Injection, Tablet |
| Formula | C20H25N3O2 |
| Weight | Average: 339.4314 Monoisotopic: 339.194677059 |
| Groups | Approved |
| Therapeutic Class | Drugs acting on the Uterus |
| Manufacturer | Troikaa Pharmaceuticals Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Treatment and prophylaxis of postpartum and postabortal haemorrhage, Treatment and prophylaxis of postpartum and postabortal haemorrhage, Prophylaxis of postpartum haemorrhage
Lerin is also used to associated treatment for these conditions: Postpartum Haemorrhage (PPH), Uterine Atony, Uterine subinvolution
How Lerin works
Lerin acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions through binding and the resultant antagonism of the dopamine D1 receptor. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss.
Dosage
Lerin dosage
Intramuscular (Adult)-
- Treatment and prophylaxis of postpartum and postabortal haemorrhage: 200 mcg. May repeat every 2-4 hr. Max: 5 doses.
Intravenous (Adult)-
- Treatment and prophylaxis of postpartum and postabortal haemorrhage:As an emergency measure: 200 mcg by slow inj over at least 1 minute, may repeat every 2-4 hr, up to a max of 5 doses.
Oral (Adult)-
- Prophylaxis of postpartum haemorrhage:200 mcg 3-4 times daily in the puerperium for 2-7 days.
Side Effects
Headache, dizziness, hallucinations; tinnitus; nausea, vomiting, foul taste, diarrhoea; hypertension, temporary chest pain, palpitations, bradycardia; nasal congestion, dyspnoea; diaphoresis; thrombophlebitis; haematuria; water intoxication; leg cramps; allergic reactions.
Toxicity
Signs and symptoms of overexposure: hypertension, seizures, headache, hypotension, nausea, and vomiting.
Precaution
Captivation of the placenta may occur if given during the 2nd or 3rd stage of labour prior to delivery of the placenta; use in this situation should only be done by a qualified personnel. Avoid prolonged use. Caution in patients with sepsis, hepatic or renal impairment. Lactation.
Interaction
Possible increase in serum levels and risk of severe vasoconstrictive effects with potent CYP3A4 inhibitors (e.g. erythromycin, troleandomycin, clarithromycin, ritonavir, indinavir, nelfinavir, delavirdine, ketoconazole, itraconazole, voriconazole) and less potent CYP3A4 inhibitors (e.g. saquinavir, nefazodone, fluconazole, fluoxetine, fluvoxamine, zileuton, clotrimazole).
Food Interaction
- Avoid grapefruit products. Grapefruit inhibits the metabolism of methylergometrine through the CYP3A4 pathway and, therefore, may increase serum levels of methylergometrine. Use caution if co-administering.
Volume of Distribution
- 56.1 ± 0 L
Elimination Route
Absorption is rapid after oral (60% bioavailability) and intramuscular (78% bioavailability) administration.
Half Life
3.39 hours
Elimination Route
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.
Pregnancy & Breastfeeding use
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Hypertension, eclamptic or previously hypertensive patients, heart disease, venoatrial shunts, mitral valve stenosis, obliterative vascular disease. Do not use in cases of threatened spontaneous abortion. Pregnancy.
Acute Overdose
Symptoms: Prolonged gangrene, numbness in extremities, acute nausea, vomiting, abdominal pain, respiratory depression, changes in BP, seizures.
Management: Symptomatic and supportive.
Storage Condition
Intramuscular: Store under refrigeration at 2-8° C. Protect from light.
Intravenous: Store under refrigeration at 2-8° C. Protect from light.
Oral: Store below 25° C.
Innovators Monograph
You find simplified version here Lerin
FAQ
What is Lerin used for?
This Lerin is used after childbirth to help stop bleeding from the uterus. Lerin belongs to a class of drugs known as ergot alkaloids. Lerin is a medication of the ergoline and lysergamide groups which is used as an oxytocic in obstetrics and in the treatment of migraine.
How safe is Lerin?
A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing. This is not a complete list of possible side effects.
How does Lerin work?
Lerin works by increasing the rate and strength of contractions and the stiffness of the uterus muscles. These effects help to decrease bleeding.
What are the common side effects of Lerin?
The most common side effects 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.
Is Lerin safe during pregnancy?
You should not use Lerin during your pregnancy. This Lerin is to be used only after delivery of your baby.
Is Lerin safe during breastfeeding?
A small amount of Lerin is passed to baby in breast milk. Women can take the drug for up to one week after birth. During this time not enough of the drug passes to the baby in breast milk to cause negative side effects.
Can I drink alcohol with Lerin?
Using Lerin with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use Lerin, or give you special instructions about the use of food, alcohol, or tobacco.
Can I drive after taking Lerin?
Lerin can cause contraction of the uterus and lead to baby birth. So, driving a car may be highly unsafe.
When should be taken of Lerin ?
Take this Lerin by mouth with or without food, usually 3 to 4 times daily for up to 1 week after delivery or as directed by your doctor. Dosage is based on your medical condition and response to treatment. Use this medication regularly to get the most benefit from it.
How many time can I take Lerin daily?
Orally, One tablet, 0.2 mg, 3 or 4 times daily in the puerperium for a maximum of 1 week.
How long does Lerin stay in my system?
The plasma level decline was biphasic with a mean elimination half-life of 3.39 hours (range 1.5 to 12.7 hours).
How long does Lerin take to work?
The onset of action after I.V. administration is immediate; after I.M. administration, 2-5 minutes, and after oral administration, 5-10 minutes.
When should I stop taking Lerin?
If the bleeding hasn't slowed down in one hour after the third pill, call your clinic number or the emergency number and talk with a nurse. o If the bleeding slows down or stops, stop taking Lerin.
What happens if I miss a dose?
If you miss a dose of Lerin, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
What happen if I overdose on Lerin?
Seek emergency medical attention. Overdose symptoms may include vomiting, stomach pain, throbbing headache, numbness or tingling in your fingers or toes, cold feeling, weak or shallow breathing, or seizure (convulsions).
Who should not take Lerin?
You should not use Lerin during your pregnancy. This medication is to be used only after delivery of your baby. Do not breast-feed within 12 hours after taking Lerin. If you use a breast pump during this time, throw out any milk you collect. Do not feed it to your baby.
Can Lerin affects my heart ?
This medicine may cause contraction of the uterus and cause you to give birth early. This medicine may increase your chance of having a heart attack.
How quickly does Lerin work?
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.
