Citations for: Grandi, G.; Cagnacci, A.; Volpe, A. Pharmacokinetic Evaluation of Desogestrel as a Female Contraceptive. Expert Opin. Drug Metab. Toxicol. 2014, 10 (1), 1–10.

Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
  • Oral: 70-75%
  • Subdermal implant: 100%
Etonogestrel (API)
Pharmacology Data Field
12-24 h, 30 h, 38 +/- 20 h
Etonogestrel (API)
Pharmacology Data Field
95.5-99% bound. 66% to albumin, 32% to SHBG.
Etonogestrel (API)
Toxicology Data Field
Vaginal inflammation, headache, breast pain, URI, haemorrhage, abdominal pain, pharyngitis, Leukorrhea, weight gain, flu-like symptoms, acne, dizziness, dysmenorrhoea, back pain, nausea
Etonogestrel (API)
Pharmacology Data Field
Excreted free or as conjugates, primarily via urine (60%) and feces (35%). Small amounts excreted in the breast milk; as a result, 0.01-0.05 ug per kg body weight per day may be ingested by the child.
Etonogestrel (API)
Metabolites
N/A
Metabolites
N/A
Metabolites
N/A
Toxicology Data Field
General progestin side effects: Abnormal uterine bleeding; breast enlargement, pain, or tenderness; unexpected or increased flow of breast milk; hot flashes; loss of sexual desires; dry mouth; unusual thirst; frequent urination; abdominal pain; cramping; nausea; loss of appetite; dizziness; headache; mood changes; insomnia; unusual tiredness or weakness; swelling in ankles or feet; unusual or rapid weight gain; skin rash; acne; loss or gain of hair; brown spots on skin; sudden changes in vision.
Desogestrel (API)
Toxicology Data Field
No treatment-related tumorigenic effects seen from administration of desogestrel only. Increase in mammary adenocarcinoma in female rats in the high-dose group compared to controls.
Desogestrel (API)
Toxicology Data Field
Not associated with point mutations in the in vitro Ames test and to chromosomal aberrations in a micronucleus test in female rats.
Desogestrel (API)
Pharmacology Data Field
76% as etonogestrel.
Desogestrel (API)
Pharmacology Data Field
30 h (single or multiple doses)
Desogestrel (API)
Pharmacology Data Field
As etonogestrel: 58% to serum albumin, 38% to SHBG, 3.5% unbound. (Grandi)
32% to SHBG, 66% to albumin, 2% free. (Schindler)
Desogestrel (API)
Toxicology Data Field
No treatment-related tumorigenic effects seen from administration of desogestrel only.
Etonogestrel (API)
Pharmacology Data Field
60% excreted via urine, 35% excreted via feces.
Desogestrel (API)
Pharmacology Data Field
  • 640 pg/mL from oral administration of 75 μg desogestrel
  • 4273 +/- 830 ng/L from 30 μg ethinyl estradiol/150 μg desogestrel oral pill
Desogestrel (API)
Pharmacology Data Field
< 2 h from multiple oral administration of 75 μg desogestrel (Grandi)
1.15 h (Schindler)
Desogestrel (API)
Pharmacology Data Field
  • 640 pg/mL from oral administration of 75 μg desogestrel
  • 4273 +/- 830 ng/L from 30 μg ethinyl estradiol/150 μg desogestrel oral pill
  • 1716 +/- 445 ng/L from etonogestrel vaginal ring
  • 813 pg/mL from subdermal implant
Etonogestrel (API)
Toxicology Data Field
Not associated with point mutations in the in vitro Ames test and to chromosomal aberrations in a micronucleus test in female rats.
Etonogestrel (API)
Pharmacology Data Field
  • Oral: 1.5 h; 2-3 h
  • Subdermal implant: 4 days
Etonogestrel (API)
Pharmacology Data Field
Subdermal implant: 7.5 L/h
Etonogestrel (API)
Pharmacology Data Field
Possibly > 90 pg/mL
Etonogestrel (API)