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Gestonorone caproate

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Trade names
  
Depostat, Primostat

CAS Number
  
1253-28-7

Routes of administration
  
Intramuscular

Molar mass
  
414.5775 g/mol

Gestonorone caproate

ATC code
  
G03DA01 (WHO) L02AB03 (WHO)

Legal status
  
In general: ℞ (Prescription only)

Synonyms
  
SH-582, SH-80582, NSC-84054; Gestonorone hexanoate, Gestronol hexanoate, Gestronol caproate, Norhydroxyprogesterone caproate; 17α-Hydroxy-19-norpregn-4-ene-3,20-dione hexanoate; 17α-hydroxy-19-norprogesterone hexanoate

Medical vocabulary what does gestonorone caproate mean


Gestonorone caproate (INN, USAN, JAN) (brand names Depostat, Primostat), also known as gestronol hexanoate (BANM), as well as 17α-hydroxy-19-norprogesterone hexanoate or norhydroxyprogesterone caproate, is a synthetic, steroidal progestin of the 19-norprogesterone and 17α-hydroxyprogesterone groups. It is used in the treatment of sex hormone-dependent conditions such as benign prostatic hypertrophy and endometrial cancer. The drug was developed by Schering and has been marketed since at least 1973, and is available widely throughout Europe, including the United Kingdom, and is also marketed in Japan, China, Mexico, and other countries.

Gestonorone caproate is a strong, long-acting, and pure progestogen, possessing no androgenic, anabolic, antiandrogenic, estrogenic, antiestrogenic, corticosteroid, or teratogenic effects. In animals, it is approximately 25 times more potent than progesterone or hydroxyprogesterone caproate. In humans, 100 or 200 mg intramuscular gestonorone caproate is said to be equivalent to 1000 mg intramuscular hydroxyprogesterone caproate. Like other potent progestins, gestonorone caproate possesses potent antigonadotropic activity and is capable of markedly suppressing the gonadal production and circulating levels of sex hormones such as testosterone and estradiol. A clinical study found that 400 mg/week intramuscular gestonorone caproate suppressed testosterone levels by 75% in men. The drug is administered once weekly by intramuscular injection, via which it acts as a depot. Like the closely related progestins hydroxyprogesterone caproate and 19-norprogesterone, gestonorone caproate shows poor activity orally.

SH-834 was a combination of 90 mg estradiol valerate and 300 mg gestonorone caproate for weekly intramuscular injection that was developed by Schering in the 1970s. It was investigated clinically as a treatment for breast cancer and was found to be effective, but does not seem to have been marketed.

References

Gestonorone caproate Wikipedia