Gonadotropin releasing Hormone
Synonyms :
GnRH, Leuprolide, Leuprolide Acetate, Leuprorelin Acetate
Mechanism :
GNRH stimulates the release of the pituitary gonadotropins, LH and FSH, resulting in a temporary increase of gonadal steroidogenesis. Repeated dosing abolishes the stimulatory effect on the pituitary gland.
Indication :
- Central precocious puberty in children
Contraindications :
Contraindicated in children <1 year of age as diluent contains benzyl alcohol.
Also contraindicated in hypersensitivity to GnRH, GnRH agonist analogs, undiagnosed abnormal vaginal bleeding, pregnancy or women who may become pregnant while receiving the drug, women who are breast-feeding.
Dosing :
Not to be given to children under two years of age.
Leuprolide acetate:
Start: 50 mcg/kg/day subcutaneously, may increase by 10 mcg/kg/day until total downregulation; Discontinue with onset of puberty.
Depot preparation monthly:
<25 kg: 7.5 mg IM every month.
>25 kg to 37.5 kg: 11.25 mg IM every month.
>37.5 kg: 15 mg IM every month.
Assess response 1-2 months after first injection; increase next monthly dose to the next higher level, if adequate hormonal and clinical suppression not achieved with starting doses.
Depot preparation every 3 month:
11.25 mg or 30 mg as single IM injection every 3 months. Assess response 2-3 months and 6 months after injection.
Adverse Effect :
Common Reactions: Hot flashes/diaphoresis, tumor flare, transient headache, generalized pain, joint disorder, dyspepsia, edema, weight changes, dizziness, breast tenderness/gynecomastia, injection site reaction, insomnia, urogenital disorders, paraesthesia, neuromuscular disorder, asthenia.
Serious Reactions: Anaphylaxis, bone density loss, depression, suicidal tendency, pituitary apoplexy, seizures, hepatotoxicity, QT prolongation (long-term use).
Interaction :
Phenothiazines, Metoclopramide and Digoxin: Response may be blunted by medicines causing a rise in prolactin.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function Monitor closely |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in normal renal function |
| HD | Unlikely to be dialysed. Dose as in normal renal function |
| HDF/High flux | Unknown dialysability. Dose as in normal renal function |
| CAV/VVHD | Unlikely to be dialysed. Dose as in normal renal function |
Hepatic Dose :
No dosage adjustments are recommended.