Product Information
Registration Status: ActiveELIGARD POWDER AND SOLVENT FOR SOLUTION FOR INJECTION 22.5MG is approved to be sold in Singapore with effective from 2014-02-25. It is marketed by ASTELLAS PHARMA SINGAPORE PTE LTD, with the registration number of SIN14512P.
This product contains Leuprorelin 22.5mg in the form of INJECTION, POWDER, LYOPHILIZED, FOR SUSPENSION,EXTENDED-RELEASE. It is approved for SUBCUTANEOUS use.
This product is manufactured by Tolmar Inc. (Powder in UNITED STATES.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Leuprolide belongs to the general class of drugs known as hormones or hormone antagonists. It is a synthetic 9 residue peptide analog of gonadotropin releasing hormone. Leuprolide is used to treat advanced prostate cancer. It is also used to treat uterine fibroids and endometriosis. Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease.
Indication
For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
Mechanism of Action
Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
Pharmacokinetics
- Absorption
- Bioavailability by subcutaneous administration is comparable to that by intravenous administration.
- Distribution
- * 27 L [intravenous bolus administration to healthy male volunteers]
- Metabolism
- Primarily degraded by peptidase and not by cytochrome P450 enzymes.
- Elimination
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.
Active Ingredient/Synonyms
(D-Leu(6),des-gly-NH2(10),pro-ethylamide(9))-gonadotropin-releasing hormone | L-Pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-L-proline ethylamide | Leuprorelin | Leuprorelina | Leuproreline | Leuprorelinum | PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-NHC2H5 | PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-nhet | Leuprolide |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.