Pergoveris

Pergoveris Mechanism of Action

Manufacturer:

Merck

Distributor:

Zuellig Pharma
Full Prescribing Info
Action
Pharmacotherapeutic group: Gonadotrophins. ATC code: G03GA05/G03GA07.
Pharmacology: Pharmacodynamics: Pergoveris is a preparation of follicle stimulating hormone and luteinising hormone produced by genetically engineered Chinese Hamster Ovary (CHO) cells.
In clinical trials the efficacy of the combination of follitropin alfa and lutropin alfa has been demonstrated in women with hypogonadotropic hypogonadism.
In the stimulation of follicular development in anovulatory women deficient in LH and FSH, the primary effect resulting from administration of lutropin alfa is an increase in oestradiol secretion by the follicles, the growth of which is stimulated by FSH.
In one clinical study of women with hypogonadotrophic hypogonadism and an endogenous serum LH concentration below 1.2 IU/L the appropriate dose of r-hLH (lutropin alfa) was investigated. A dose of 75 IU r-hLH daily (in combination with 150 IU follitropin alfa (r-hFSH)) resulted in adequate follicular development and oestrogen production. A dose of 25 IU r-hLH daily (in combination with 150 IU follitropin alfa) resulted in insufficient follicular development. Therefore, administration of less than one vial of Pergoveris daily may provide too little LH-activity to ensure adequate follicular development.
Pharmacokinetics: Follitropin alfa and lutropin alfa have shown the same pharmacokinetic profile as follitropin alfa and lutropin alfa separately.
Follitropin alfa: Following intravenous administration, follitropin alfa is distributed to the extracellular fluid space with an initial half-life of around 2 hours and eliminated from the body with a terminal half-life of about one day. The steady state volume of distribution and total clearance are 10 l and 0.6 l/h, respectively. One-eighth of the follitropin alfa dose is excreted in the urine.
Following subcutaneous administration, the absolute bioavailability is about 70%. Following repeated administration, follitropin alfa accumulates 3-fold achieving a steady-state within 3-4 days. In women whose endogenous gonadotrophin secretion is suppressed, follitropin alfa has nevertheless been shown to effectively stimulate follicular development and steroidogenesis, despite unmeasurable LH levels.
Lutropin alfa: Following intravenous administration, lutropin alfa is rapidly distributed with an initial half-life of approximately one hour and eliminated from the body with a terminal half-life of about 10-12 hours. The steady state volume of distribution is around 10-14 l. Lutropin alfa shows linear pharmacokinetics, as assessed by AUC which is directly proportional to the dose administered. Total clearance is about 2 l/h, and less than 5% of the dose is excreted in the urine. The mean residence time is approximately 5 hours.
Following subcutaneous administration, the absolute bioavailability is approximately 60%; the terminal half-life is slightly prolonged. The lutropin alfa pharmacokinetics following single and repeated administration of lutropin alfa are comparable and the accumulation ratio of lutropin alfa is minimal. There is no pharmacokinetic interaction with follitropin alfa when administered simultaneously.
Toxicology: Preclinical safety data: Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity and genotoxicity.
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in