Leuprolide Pharmacology

Leuprolide

About Leuprolide
GnRH analog, LH-RH Agonist, Antineoplastic.
Mechanism of Action of Leuprolide
This GnRH analogue is a potent inhibitor of gonadotropin secretion. By continuous administration of this drug cause down regulation of LHRH receptors and an uncoupling of LHRH signal transduction mechanism. This results a desensitization of gonadotropins and marked reduction in the secretion of bioactive LH &FSH. This reduction in circulating LH&FSH together with down regulation of GnRH receptors produces a complete inhibition of testicular and ovarian function and a fall in sex steroid level. This drug also have direct inhibitory effect on LHRH receptors present in extra pituitary tissues like tumors .Reducing level of estrogen in women reduce the size of the endometrial implants and decrease dysmenorrhea and pelvic pain associated with endometriasis.
Pharmacokinets of Leuprolide
Absorption- Rapidly and completely absorbed after subcutaneous administration.
Distribution-Highly distributed to kidney, liver, pineal and pituitary tissues.
Metabolism- It is metabolized into its metabolites in hypothalamus and anterior pituitary gland.
Onset of Action for Leuprolide
< 2 - 4 weeks
Duration of Action for Leuprolide
60 - 90 days
Half Life of Leuprolide
N/A
Side Effects of Leuprolide
1. ECG changes
2. Edema
3. High blood pressure
4. Insomnia
5. Headache
6. Dizziness
7. Light headness
8. Nervousness
9. Constipation
10. Diarrhea
11. Anorexia
12. Appetite increase
13. Alopecia
14. Increased sweating
15. Impotence
16. Gyenecomastia
17. Nausea
18. Vomiting
19. Joint disorder
20. Myalgia
21. Bone pain
22. Urinary frequency
23. Hematurea
24. Dyspnoea
25. Anemia
26. Dermatitis
27. Acne
28. Seborrhea
29. Asthenia
Contra-indications of Leuprolide
1. Contraindicated in patients with hypersensitivity to the drug or other GnRH analogues
Special Precautions while taking Leuprolide
1. Uterine leiomyomata
2. Hypo estrogen state

Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Leuprolide
1. Breast cancer
2. Prostate cancer
3. Central precocious puberty
4. Endometriasis pain
5. Anaemia due to bleeding of uterine leiomyomas
6. Uterine fibroids
Interactions for Leuprolide
N/A
Typical Dosage for Leuprolide
Subcutaneous-
Adult-
Prostate cancer: 1mg/day as a single dose
Endometriasis and uterine fibroids: 3.75 mg every month as a single dose
Uterine surgery preparation:3.75 mg as a single depot given 5-6 weeks before the procedure
Children-
Precocious puberty:50mcg/kg/day
Intramuscular-
Adult-
Endometriosis and fibroids in uterus: 3.75mg every month as a single depot
Children-
Precocious puberty:0.3mg/kg every 4 weeks
Schedule of Leuprolide
N/A
Storage Requirements for Leuprolide
Stored at controlled room temperature. Protect from direct light and heat. Keep out of reach of children.
Effects of Missed Dosage of Leuprolide
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. Do not double the dose.
Effects of Overdose of Leuprolide
Give symptomatic and supportive treatment.

Home Delivery for Leuprolide in Your City

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

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 leuprolide and other medicines and health products. Home delivery services for leuprolide 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 leuprolide 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 leuprolide before they complete the sale. You can get this information while placing the order for leuprolide with the pharmacy.

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