Levonorgestrel
Levonorgestrel is a sex hormone with actions, uses similar to progesterone.. its (-) isomer is used clinically. Chemically Levonorgestrel is identified as 13-ethyl-17-hydroxy-18, 19-dinorpregn-4-en-20-yn-3-one. Levonorgestrel is pricipally used in combination with synthetic estrogen etinyl estadiol for contraception. It can also be used topically through an intrauterine contraceptive device.
Primary Characteristics
It is of Synthetic origin and belongs to Hormone.
It belongs to Progesterone agonist pharmacological group on the basis of mechanism of action and also classified in Contraceptive Oral pharmacological group. It is also classified under Sex Hormones .
Molecular Weight: 312.4 · Solubility in Water: insoluble · Solubility in Alcohol: 1 in 120 · Non-proprietary name: Levonorgestrel.
Pharmacokinetics
Absorption: Levonorgestrel has an oral bioavailability is 50% (±50%).
Distribution: Levonorgestrel has a volume of distribution is 1.9 l/kg. plasma protein binding is 93-95%.
Elimination: it is metabolised via Hepatic, plasma half-life is 8-30 hr.
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Indications
Levonorgestrel is primarily indicated in conditions like Contraception, Hormone replacement therapy, Menstruation disorders, Nausea and vomiting (chemotherapy induced), prevention.
Contraindications
Levonorgestrel is contraindicated in conditions like Migraine, Breast cancer, Hepatic disease, Circulatory system disease, Genital tract bleeding, Endometrial cancer, Lipid metabolism disorder.
Dosage
Levonorgestrel's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 0.75 mg | 0.75 mg | Every 24h | PO | |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Levonorgestrel in overdosage may give rise to further complications which include Malignant hypertension.
Levonorgestrel produces potentially life-threatening effects which include Venous thromboembolism, Ischemic heart disease, Cerebrovascular disease, Venous thromboembolism, Cerebrovascular disease. Careful monitoring is needed with proper medical management.
Levonorgestrel is known to cause more or less tolerable side effects which are usually transient. These include Abdominal discomfort, Anxiety, Breast tension, Changes in libido , Depressive moods, Dizziness, Fatigue, Headache, Menstrual irregularity, Nausea, Uterine bleeding, Vomiting , Weight gain.
Warnings / Precautions
Interference in Pathology
Levonorgestrel may interfere in the diagnosis of Serum Tests for Adrenal Corticosteroids , Urine Tests for 17-Ketosteroids and 17-OH Corticosteroids and Aldosterone , Thyopac Method for Measurement of T3 .
Available Brands
Storage Conditions
Drug Classification
- 1.18.3.1 — Hormonal contraceptives