Levonorgestrel Pharmacology

Levonorgestrel

About Levonorgestrel
A synthetic Progestagen . Hormonal contraception.
Mechanism of Action of Levonorgestrel
It is a progestin derivative exerts it`s action through nuclear progesterone receptors situated in female genital tract, breast, CNS, and pituitary. When the drug binds to progesterone receptors it undergoes dimerisation and attaches to progesterone response element of target genes and regulates transcription through coactivators. It inhibits growth hormone release from pituitary by reinforcement of normal feedback inhibition. It reduces frequency of LH secretary pulses, attenuate LH surge, and suppresses ovulation. It causes thickening of cervical mucous and induces sloughing of the endometrium. It also disrupts fertilization and inhibits implantation.
Pharmacokinets of Levonorgestrel
Absorption: Well absorbed orally and bioavailability is about 100%.Distribution: Distributed in to the target sites in a protein bound form. Metabolism: Undergoes partial metabolism in liver.Excretion: Drug and it`s metabolites are excreted mainly through urine and a small portion is excreted in faeces.
Onset of Action for Levonorgestrel
N/A
Duration of Action for Levonorgestrel
N/A
Half Life of Levonorgestrel
N/A
Side Effects of Levonorgestrel
1. Breast tenderness
2. Nausea
3. Vomiting
4. Abdominal pain
5. Headache
6. Dizziness
7. Fatigue
8. Depression
Implants:
1. Breast tenderness
2. Nausea
3. Vomiting
4. Abdominal pain
5. Headache
6. Dizziness
7. Fatigue
8. Depression
9. Tingling
10. Numbness
11. Amenorrhoea
12. Irregular bleeding
13. Prolonged bleeding
14. Spotting
15. Cervicitis
16. Vaginitis
17. Leucorrhoea
18. Brest discharge
19. Decreased thyroxin levels
20. Weight gain
21. Mastalgia
22. Musculoskeletal pain
23. Dermatitis
24. Acne
25. Hirsutism
26. Alopecia
27. Itching



Contra-indications of Levonorgestrel
Oral:
1. Hypersensitivity to the drug
2. Undiagnosed genital bleeding
Implants:
1. Hypersensitivity to the drug or implant system
2. Undiagnosed genital bleeding
3. Thrombophlebitis
4. Thromboembolic disorders
5. Intracranial hypertension
6. Breast cancer
7. Liver tumors
8. Acute hepatic diseases
Special Precautions while taking Levonorgestrel
1. Emergency contraceptive method should not replace normal contraceptive method
2. Use implants preferably in women who already have one child
3. Avoid use of implants in pelvic inflammatory diseases
4. Hepatic impairment
5. Cardiovascular disorders
6. Diabetes mellitus
7. Seizures
8. Mental depression
9. Migraine
10. High blood pressure
Pregnancy Related Information
Contraindicated
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution
Children Related Information
Contraindicated
Indications for Levonorgestrel
1. Emergency contraception
2. Long term prevention of pregnancy (up to 5years)
Interactions for Levonorgestrel
Simultaneous administration of certain anticonvulsant drugs (phenobarbital, phenytoin, primidone, carbamazepine, certain antibiotics such as rifabutin, rifamycin and griseofulvin) can reduce or suppress the effectiveness of emergency contraception.

Typical Dosage for Levonorgestrel
Oral:
Emergency contraception: 750mcg Levonorgestrel soon after unprotected sex; not later than 72hours. Take a second tablet after 12 hours of taking first dose.
Implant:
Long term prevention of pregnancy (up to 5years):
A total dose of 216mg present in 6 silastic capsules are surgically implanted in the superficial plane beneath the skin of upper arm during first week of onset of menses.
Intrauterine implant:
Long term prevention of pregnancy (up to 5years): The product is inserted in to the uterus by a trained person; once every 5years.
Schedule of Levonorgestrel
H
Storage Requirements for Levonorgestrel
Store at controlled room temperature below 25 degree C.Keep away from excess heat and moisture. Keep out of reach of children.
Effects of Missed Dosage of Levonorgestrel
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule.
Effects of Overdose of Levonorgestrel
Give supportive measures and symptomatic treatment

Home Delivery for Levonorgestrel in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including levonorgestrel.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for levonorgestrel and other medicines and health products. Home delivery services for levonorgestrel may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take levonorgestrel only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for levonorgestrel before they complete the sale. You can get this information while placing the order for levonorgestrel with the pharmacy.

Levonorgestrel is a generic medicine name and there are several brands available for it. Some of the brands for levonorgestrel might be better known than levonorgestrel itself. If the pharmacy that's willing to deliver medicines to your home doesn't have levonorgestrel in stock, you can ask for one of the branded alternatives for levonorgestrel.