DESOGEN desogestrel and ethinyl estradiol

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

desogestrel (UNII: 81K9V7M3A3) (desogestrel - UNII:81K9V7M3A3)

Available from:

Organon USA Inc.

INN (International Name):

desogestrel

Composition:

desogestrel 0.15 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

DESOGEN- DESOGESTREL AND ETHINYL ESTRADIOL
ORGANON USA INC.
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DESOGEN TABLETS
(DESOGESTREL AND ETHINYL ESTRADIOL TABLETS USP)
PATIENTS SHOULD BE COUNSELED THAT THIS PRODUCT DOES NOT PROTECT
AGAINST HIV INFECTION (AIDS) AND
OTHER SEXUALLY TRANSMITTED DISEASES.
DESCRIPTION
DESOGEN Tablets (desogestrel and ethinyl estradiol tablets USP)
provides an oral contraceptive
regimen of 21 white round tablets each containing 0.15 mg desogestrel
(13-ethyl-11-methylene-18,19-
dinor-17 alpha-pregn-4-en-20-yn-17-ol) and 0.03 mg ethinyl estradiol
(19-nor-17 alpha-pregna-1,3,5
(10)-trien-20-yne-3,17-diol). Inactive ingredients include vitamin E,
corn starch, povidone, stearic acid,
colloidal silicon dioxide, lactose, hydroxypropyl methylcellulose,
polyethylene glycol, titanium
dioxide, and talc. DESOGEN also contains 7 green round tablets
containing the following inert
ingredients: lactose, corn starch, magnesium stearate, FD&C Blue No. 2
aluminum lake, ferric oxide,
hydroxypropyl methylcellulose, polyethylene glycol, titanium dioxide,
and talc. The molecular weights
for desogestrel and ethinyl estradiol are 310.48 and 296.40,
respectively. The structural formulas are
as follows:
CLINICAL PHARMACOLOGY
Combination oral contraceptives act by suppression of gonadotropins.
Although the primary mechanism
of this action is inhibition of ovulation, other alterations include
changes in the cervical mucus (which
increase the difficulty of sperm entry into the uterus) and the
endometrium (which reduce the likelihood
of implantation).
Receptor-binding studies, as well as studies in animals, have shown
that etonogestrel, the biologically
active metabolite of desogestrel, combines high progestational
activity with minimal intrinsic
androgenicity (91,92). The relevance of this latter finding in humans
is unknown.
PHARMACOKINETICS
Absorption
Desogestrel is rapidly and almost completely absorbed and converted
into etonogestrel, its biologically
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®
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active metabolite. Following oral administration, the relative
bioavailability of des