1. Leuprolide Drugbank ID : DB00007
Protein chemical formula : C59H84N16O12
Protein average weight :
Half life : ~3 hours
Chemical name : 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate

2. Description : Indication : Pharmacodynamics :
ELIGARD (leuprolide acetate) ® is a sterile polymeric matrix formulation of leuprolide acetate, a GnRH agonist, for subcutaneous injection. It is designed to deliver leuprolide acetate at a controlled rate over a one-, three-, four- or six-month therapeutic period.
Indication :
For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
Pharmacodynamics :
Used in the palliative treatment of advanced prostate cancer. Leuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.

3. Mechanism of action : Metabolism : Absorption :
Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
Metabolism :
Primarily degraded by peptidase and not by cytochrome P450 enzymes.
Absorption :
Bioavailability by subcutaneous administration is comparable to that by intravenous administration.

4. Volume of distribution :
Route of Elimination :
Excretion in urine.
Volume of distribution :
27 L [intravenous bolus administration to healthy male volunteers]
Clearance :
8.34 L/h [healthy male receiving a 1-mg IV bolus]
Toxicity :
In rats subcutaneous administration of 250 to 500 times the recommended human dose, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a clinical counterpart of this phenomenon. In early clinical trials with leuprolide acetate doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose.

5. Targets : Affected organisms : Categories : Sequence : PHWSYLLR
Gonadotropin-releasing hormone receptor
Affected organisms :
Humans and other mammals
Categories :
Antineoplastic Agents, Hormonal and Fertility Agents, Female and Estrogen Antagonists
Sequence :
PHWSYLLR

6. Brands : Eligard
Company : Atrix Labs/QLT In
Description : ELIGARD (leuprolide acetate) ® is a sterile polymeric matrix formulation of leuprolide acetate, a GnRH agonist, for subcutaneous injection. It is designed to deliver leuprolide acetate at a controlled rate over a one-, three-, four- or six-month therapeutic period.
Used for/Prescribed for : Eligard is used in men to treat the symptoms of prostate cancer. Eligard treats only the symptoms of prostate cancer and does not treat the cancer itself.
Formulation : ELIGARD (leuprolide acetate) ® is prefilled and supplied in two separate, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the ATRIGEL® Delivery System and the other contains leuprolide acetate. ATRIGEL® is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable poly (DL-lactide-co-glycolide) (PLGH or PLG) polymer formulation dissolved in a biocompatible solvent, N-methyl-2-pyrrolidone (NMP)
Form : suspension
Route of administration : subcutaneous injection

7. Dosage : 7. 5mg-1 injection/month, 22
Dosage : 7.5mg-1 injection/month, 22.5mg-1 injection per 3 month, 30mg-1 injection per 4 month, 45 mg- 1 injection every 6 month. Contraindication : Hypersensitivity and pregnancy Side effects : Rare but serious side effects from Eligard may include ; pain or unusual sensations in your back; numbness, weakness, or tingly feeling in your legs or feet; muscle weakness or loss of use; loss of bowel or bladder control; or liver problems - nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes). Common Eligard side effects may include: acne, increased growth of facial hair; breakthrough bleeding in a female child during the first 2 months of leuprolide treatment; dizziness, weakness, tired feeling; hot flashes, night sweats, chills, clammy skin; nausea, diarrhea, constipation, stomach pain; skin redness, itching, or scaling joint or muscle pain; Drug interaction : total of 57 drugs (176 brand and generic names) are known to interact (moderate interactions) with Eligard (leuprolide) A

8. General references :
# Saleh FM, Niel T, Fishman MJ: Treatment of paraphilia in young adults with leuprolide acetate: a preliminary case report series. J Forensic Sci Nov;49(6): "Pubmed":
# Geier MR, Geier DA: The potential importance of steroids in the treatment of autistic spectrum disorders and other disorders involving mercury toxicity. Med Hypotheses. 2005;64(5): "Pubmed":
# Doraiswamy PM, Xiong GL: Pharmacological strategies for the prevention of Alzheimer's disease. Expert Opin Pharmacother Jan;7(1):1-10. "Pubmed":
# Sequence Information "Link": "RxMed":

9. References : http://www. eligard. com/ http://www. rxlist