Product Information
Registration Status: ActiveDIPHERELINE P.R. POWDER AND SOLVENT FOR SUSPENSION FOR INJECTION 11.25MG/VIAL is approved to be sold in Singapore with effective from 2014-09-25. It is marketed by ZUELLIG PHARMA PTE LTD, with the registration number of SIN14635P.
This product contains Triptorelin 11.25mg/vial in the form of INJECTION, POWDER, FOR SUSPENSION, EXTENDED-RELEASE. It is approved for INTRAMUSCULAR use.
This product is manufactured by IPSEN PHARMA BIOTECH (Lyophilisate manufacturer) in FRANCE, andCENEXI (Solvent manufacturer) in ITALY.
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
Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men.
Indication
Triptorelin is indicated for the palliative treatment of advanced prostate cancer.
Mechanism of Action
Triptorelin is a synthetic agonist analog of gonadotropin releasing hormone (GnRH). Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone.
Pharmacokinetics
- Absorption
- Following IV administration of triptorelin, triptorelin is completely absorbed.
- Distribution
- After a single IV dose of 0.5mg, the volume of distribution of triptorelin peptide in healthy males was 30 - 33L.
- Metabolism
- The metabolism of triptorelin in humans is not well understood; however, metabolism likely does not involve hepatic enzymes such as cytochrome P450. Whether or not triptorelin affects, or how it affects other metabolizing enzymes is also poorly understood. Triptorelin has no identified metabolites.
- Elimination
Clearance
In healthy male volunteers, total clearance of triptorelin was 211.9 mL/min.
Toxicity
Some of the most commonly reported adverse effects of triptorelin are hot flushes reported in 58.6% of patients, skeletal pain in 12.1%, impotence in 7.1%, and headache in 5.0%. Other reported adverse effects include injection site pain, general body pain, leg pain, fatigue, hypertension, dizziness, diarrhea, vomiting, insomnia, emotional lability, anemia, pruritus, urinary tract infections, and urinary retention. Triptorelin is classified as Pregnancy Category X and contraindicated in pregnant women or in women who may become pregnant. Hormonal changes caused by triptorelin increase the risk for pregnancy loss. Studies done on pregnant rats demonstrated maternal toxicity and embryo-fetal toxicities.
Active Ingredient/Synonyms
(6-D-Tryptophan)luteinizing hormone-releasing hormone | (D-Trp6)-GnRH | Luteinizing hormone-releasing factor (pig), 6-D-tryptophan | pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 | triptorelina | triptoreline | triptorelinum | Triptorelin |
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.