The metabolism of desogestrel (13-ethyl-11-methylene-18, 19-dinor-17alpha-pregn-4-en-20-yn-17-ol), an orally active progestogen, was studied in vivo after administration of single oral doses to rats and dogs and in vitro using rat, rabbit, dog, and human liver microsomes. Metabolites were isolated and identified by NMR and MS analysis. After oral administration of [3H]desogestrel to rats and do...

Congenital central hypoventilation syndrome (CCHS) is a neurorespiratory disease characterized by life-threatening sleep-related hypoventilation involving an alteration of CO2/H(+) chemosensitivity. Incidental findings have suggested that desogestrel may allow recovery of the ventilatory response to CO2. The effects of desogestrel on resting ventilation have not been reported. This study was de...

BACKGROUND Suppression of spermatogenesis to azoospermia is required for effective hormonal male contraception, but the degree of suppression varies between ethnic groups. We here report the first study of hormonal suppression of spermatogenesis in two African centres using a regimen of oral progestogen with depot testosterone. METHODS A total of 31 healthy men (21 black) were recruited in Cape...

The newer progestogens desogestrel, norgestimate, gestodene, dienogest and nomegestrol share the common property of having weak or no androgenic effects, but there is great variation between agents in their pharmacokinetic properties and hormonal activities. Both desogestrel (acting as 3-keto-desogestrel) and norgestimate (acting mainly through levonorgestrel) are prodrugs. While nomegestrol is...

Desogestrel is a 3-deoxo progestogenic steroid that requires bioactivation to 3-ketodesogestrel. In these studies we have attempted to define the pathway of 3-ketodesogestrel formation and characterise the enzymes responsible for this biotransformation in vitro. Initial studies using deuterated desogestrel confirmed that desogestrel is metabolised by human liver microsomes via 3alpha-hydroxy an...

OBJECTIVE To assess the risk of venous thromboembolism from use of combined oral contraceptives according to progestogen type and oestrogen dose. DESIGN National historical registry based cohort study. SETTING Four registries in Denmark. PARTICIPANTS Non-pregnant Danish women aged 15-49 with no history of thrombotic disease and followed from January 2001 to December 2009. MAIN OUTCOME M...

OBJECTIVE To assess the effects of the combined contraceptive vaginal ring NuvaRing on ovarian function. DESIGN Randomized, open-label, crossover study. SETTING Clinical pharmacology unit. PARTICIPANT(S) Sixteen healthy female volunteers. INTERVENTION(S) Group 1: one cycle of combined oral contraceptive containing desogestrel (150 microg) and ethinyl estradiol (30 microg) (desogestrel/E...

A plausible mechanism to explain thrombotic risk differences associated with the use of secondand third-generation oral contraceptives (OCs), particularly in carriers of factor VLeiden, is still lacking. In a double-blind trial, 51 women without and 35 women with factor VLeiden were randomized to either a second(30 g ethinylestradiol/150 g levonorgestrel) or third(30 g ethinylestradiol/150 g de...

CONTEXT Previous studies have reported that users of the "third-generation" oral contraceptives (OCs) containing the progestins gestodene and desogestrel have about twice the risk for venous thromboembolism (VTE) compared to users of older OCs containing levonorgestrel. Estimates of the risk for VTE among users of norgestimate-containing OCs compared to other OCs, however, are lacking. OBJECT...

NEW DRUGS Generic Desogestrel/Ethinyl Estradiol Contraceptives Watson Pharmaceuticals, Inc., has announced the final approval from the U.S. Food and Drug Administration (FDA) of its Abbreviated New Drug Application (ANDA) for desogestrel and ethinyl estradiol tablets USP, 0.15 mg/ 0.03 mg, a generic version of OrthoMcNeil’s Ortho-Cept® and Organon’s Desogen®. These products are indicated for th...