Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1     Pharmacodynamic properties
Pharmacotherapeutic group: Gonadotropins
ATC code: G03GA02
The target organs of the hormonal effect of HMG are the ovaries and testes. HMG has a gametotrophic and steroidogenic effect.

By use of the FSH component, HMG induces an increase of the growing follicles in the ovaries and stimulates their development. FSH increases the production of estradiol in the granulosa cells by aromatising androgens that emerge from the theca cells under influence of the LH component.

In the testicles, FSH induces the transformation from immature to mature Sertoli cells. It mainly has an effect on the maturation of the sperm channels and the development of the spermatozoa. However, a high intratesticular androgen concentration is necessary, which requires previous treatment with HCG.

Pharmacokinetic Properties

5.2     Pharmacokinetic properties

HMG is orally ineffective and requires intramuscular or subcutaneous injection. The pharmacokinetics of HMG following intramuscular and subcutaneous application has been examined specifically for each preparation. The maximum serum level of FSH is reached 6 – 48 hours after intramuscular injection and 6 – 36 hours after subcutaneous injection.
Subsequently, the serum level decreases with a 56-hour (intramuscular) resp. 51-hour (subcutaneous) half-life.
HMG is mainly excreted renally.

Bioavailability
The bioavailability of Menogon is higher after subcutaneous application than after intramuscular application. The FSH values after intramuscular and subcutaneous application (dosage: 300 IU) were:
 intramuscular: AUC 0 - = 320.1 mlE/ml x h;
cmax = 4.15 mlE/ml;
tmax = 18 h
subcutaneous: AUC 0 - = 385.2 mlE/ml x h;
cmax = 5.62 mlE/ml;
tmax = 12 h