Desogestrel, norgestimate, and gestodene: the newer progestins.
OBJECTIVE
To review and compare the newer progestins desogestrel, norgestimate, and gestodene with regard to chemistry, pharmacokinetics, efficacy, and tolerability.


METHODS
Primary literature on desogestrel, norgestimate, and gestodene was identified from a comprehensive MEDLINE English-literature search from 1984 through 1994, with additional studies selected by review of the references. Indexing terms included progestins, desogestrel, gestodene, norgestimate, levonorgestrel, and norgestrel.


METHODS
Only human clinical and pharmacokinetic trials performed in Europe, Canada, and the US were included.


METHODS
All available data from human studies were reviewed; both comparative and noncomparative studies were included because of the paucity of direct comparative information available.


RESULTS
The newer progestins were designed to minimize the adverse effects (e.g., acne, hirsuitism, nausea, carbohydrate and lipid metabolism changes) observed with older oral contraceptives (OCs) while maintaining efficacy and good menstrual cycle control. Desogestrel, norgestimate, and gestodene have minimal amounts of androgenicity and antiestrogenic potential. All of these agents are pharmacokinetically similar to older agents: they are highly bioavailable when administered orally, hepatically metabolized, and obtain steady-state concentrations after 8-10 days of continuous administration. The newer agents have similar Pearl Indexes and slightly better cycle control. Furthermore, the new progestins appear to cause fewer adverse effects, such as acne and hirsuitism, and similar rates of weight gain, blood pressure changes, and lipid and carbohydrate metabolism changes.


CONCLUSIONS
Desogestrel, norgestimate, and gestodene appear to offer clinical advantages because of their decreased androgenicity. Women whose cycles are currently well controlled with other OCs should not be switched to a newer progestin. However, any of the combination OC products that contain these progestins may be prescribed for women intolerant of older agents or to first-time users of OCs. The newer progestins appear to be efficacious and offer similar cycle control, improved safety and tolerability profiles, and comparable price with the older agents.
School of Medicine, West Virginia University, Robert C Byrd Health Sciences Center, Charleston 25304, USA.
B
B
Kaplan
D002986:Clinical Trials as Topic; D003276:Contraceptives, Oral / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D017135:Desogestrel / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004347:Drug Interactions; D005260:Female; D006801:Humans; D009644:Norgestrel / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D009652:Norpregnenes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D045167:Progesterone Congeners / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
D003276:Contraceptives, Oral; D009652:Norpregnenes; D045167:Progesterone Congeners; C033273:Gestodene; D009644:Norgestrel; D017135:Desogestrel; C017576:norgestimate