HYDROXYPROGESTERONE CAPROATE injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

HYDROXYPROGESTERONE CAPROATE (UNII: 276F2O42F5) (HYDROXYPROGESTERONE - UNII:21807M87J2)

Available from:

ANI Pharmaceuticals, Inc.

INN (International Name):

HYDROXYPROGESTERONE CAPROATE

Composition:

HYDROXYPROGESTERONE CAPROATE 250 mg in 1 mL

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

HYDROXYPROGESTERONE CAPROATE- HYDROXYPROGESTERONE CAPROATE INJECTION
ANI PHARMACEUTICALS, INC.
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HYDROXYPROGESTERONE CAPROATE INJECTION USP
DESCRIPTION
Hydroxyprogesterone Caproate Injection USP is a sterile, long-acting
preparation of the caproate ester
of the naturally-occurring progestational hormone,
hydroxyprogesterone, in an oil solution for
intramuscular use.
The chemical name for hydroxyprogesterone caproate is
pregn-4-ene-3,20-dione, 17[(1-
oxohexyl)oxy]. It has an empirical formula of C
H O and a molecular weight of 428.60.
Hydroxyprogesterone caproate exists as white to creamy white
crystalline powder.
The structural formula is:
Each 5 mL multiple dose vial contains hydroxyprogesterone caproate,
250 mg/mL, in castor oil (28.6%
v/v) and benzyl benzoate (46% v/v) with the preservative benzyl
alcohol (2% v/v).
CLINICAL PHARMACOLOGY
Hydroxyprogesterone is a potent, long-acting, progestational steroid
ester which transforms
proliferative endothelium into secretory endothelium, induces mammary
gland duct development, and
inhibits the production and/or release of gonadotropic hormone; it
also shows slight estrogenic,
androgenic, or corticoid effects as well, but should not be relied
upon for these effects.
In advanced adenocarcinoma of the uterine corpus, Hydroxyprogesterone
Caproate Injection in a dosage
of 1,000 mg or more, one or more times each week, often induces
regressive changes.
_Absorption_: Peak serum levels of hydroxyprogesterone caproate
appeared after 3 to 7 days in non-
pregnant female subjects following a single intramuscular injection of
1,000 mg hydroxyprogesterone
caproate. The pharmacokinetics of the 250 mg dose of
hydroxyprogesterone caproate has not been
evaluated in a study.
_Metabolism_: The conjugated metabolites include sulfated and
glucuronidated products. _In vitro_ data
indicate that the metabolism of hydroxyprogesterone caproate is
predominantly mediated by CYP3A4
and CYP3A5.
_Excretion_: Both conjugated metabolites and free steroids are
excreted in the urine and feces,