LUTREPULSE KIT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LUTREPULSE KIT (LUTREPULSE KIT).
LUTREPULSE (gonadorelin acetate) is a synthetic decapeptide analog of endogenous gonadotropin-releasing hormone (GnRH). It binds to GnRH receptors on the anterior pituitary gonadotroph cells, stimulating synthesis and release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In males, LH stimulates Leydig cells to produce testosterone; in females, LH triggers ovulation and FSH stimulates follicular development.
| Metabolism | Gonadorelin is rapidly cleaved by peptidases in plasma and tissues, primarily at the Gly-Leu bond, producing inactive metabolites. Renal excretion accounts for the majority of elimination, with less than 10% excreted unchanged. |
| Excretion | Renal: 10% unchanged; hepatic metabolism, metabolites primarily excreted in bile (70%) and feces. |
| Half-life | 3 hours (initial phase), terminal elimination half-life 10-12 hours; clinically, steady-state reached within 2 days. |
| Protein binding | 60-70% bound to sex hormone-binding globulin (SHBG) and albumin. |
| Volume of Distribution | 0.3-0.5 L/kg; indicates distribution primarily into extracellular fluid. |
| Bioavailability | Subcutaneous: 100% (relative to IV); Intramuscular: 94%. |
| Onset of Action | Intravenous: 5-10 minutes; Subcutaneous: 30-60 minutes. |
| Duration of Action | Intravenous: 4-6 hours; Subcutaneous: 8-12 hours; effect duration dose-dependent. |
5 mcg subcutaneously every 90 minutes via pulsatile pump.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required based on GFR. |
| Liver impairment | No dose adjustment required for Child-Pugh class A, B, or C. |
| Pediatric use | Not approved for pediatric use. |
| Geriatric use | No specific dose adjustment; use with caution due to limited data. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LUTREPULSE KIT (LUTREPULSE KIT).
| Breastfeeding | Excretion into human milk is unknown. M/P ratio not reported. Use during lactation is not recommended due to potential effects on the nursing infant's hormonal balance. |
| Teratogenic Risk | LUTREPULSE KIT (gonadorelin acetate) is not indicated for use during pregnancy. Fetal risk cannot be excluded; no adequate human data. In animal studies, no teratogenic effects were observed at clinically relevant doses. However, use during pregnancy may disrupt the normal hormonal milieu and theoretically affect fetal development, particularly in the first trimester. |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
["Known hypersensitivity to gonadorelin acetate or any component of the formulation","Pregnancy","Lactation (relative contraindication)","Presence of any condition not amenable to ovulation induction, such as primary ovarian failure, galactorrhea, or uncontrolled thyroid/adrenal dysfunction","Patients with sex hormone-dependent tumors (e.g., prostate cancer, breast cancer) should avoid prolonged use"]
| Precautions | ["Hypersensitivity reactions (anaphylaxis, urticaria, angioedema) have been reported; discontinue if serious reaction occurs.","Ovarian hyperstimulation syndrome (OHSS) may occur in women undergoing ovulation induction; monitor for abdominal pain, distention, nausea, and rapid weight gain.","Multiple gestation pregnancy risk increased (especially with ovulation induction).","Use caution in patients with pituitary adenoma; stimulate LH/FSH release may precipitate infarction.","Not intended for long-term therapy; prolonged use may lead to desensitization of pituitary gonadotrophs."] |
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| Fetal Monitoring |
| If inadvertent exposure occurs during pregnancy, monitor fetal development with ultrasound and assess for potential hormonal disruption. No specific monitoring guidelines exist. |
| Fertility Effects | LUTREPULSE KIT is used to induce ovulation in women with hypothalamic amenorrhea. It can restore fertility. Ovarian hyperstimulation syndrome (OHSS) and multiple gestations are possible risks. Discontinue use upon confirmed pregnancy. |