Desogestrel

Uses and Administration

Desogestrel is a progestogen (see Progesterone, Refer to ) structurally related to levonorgestrel that is used as a hormonal contraceptive (see Refer to ). A typical daily dose of 150 micrograms is used as the progestogenic component of monophasic combined oral contraceptive preparations. Doses of 50 to 150 micrograms daily may be used in triphasic combined preparations. A dose of 75 micrograms daily is used as an oral progestogen-only contraceptive; unlike traditional progestogen-only contraceptives, desogestrel is said to reliably inhibit ovulation. Progestogen-only contraceptive efficacy is reduced if a dose of desogestrel is delayed by more than 12 hours.

(last reviewed 2010-06-30; last modified 2008-06-25)

Contraception

The effects of a progestogen-only contraceptive containing desogestrel have been reported.1-3Oral desogestrel has also been investigated as a male contraceptive, combined with testosterone given by intramuscular injection,4 subcutaneous implant,5,6or transdermal patch.7

(last reviewed 2010-06-30; last modified 2008-08-29)

References

1. Collaborative study group on the desogestrel-containing progestogen-only pill. A double-blind study comparing the contraceptive efficacy, acceptability and safety of two progestogen-only pills containing desogestrel 75 micrograms/day or levonorgestrel 30 micrograms/day.Eur J Contracept Reprod Health Care. 1998; 3: 169–78. PubMed

2. Rice CF, et al.. A comparison of the inhibition of ovulation achieved by desogestrel 75 micrograms and levonorgestrel 30 micrograms daily.Hum Reprod. 1999; 14: 982–5. PubMed

3. Korver T, et al.. Maintenance of ovulation inhibition with the 75-microgram desogestrel-only contraceptive pill (Cerazette®) after scheduled 12-h delays in tablet intake.Contraception. 2005; 71: 8–13. PubMed

4. Wu FCW, et al.. Oral progestogen combined with testosterone as a potential male contraceptive: additive effects between desogestrel and testosterone enanthate in suppression of spermatogenesis, pituitary-testicular axis, and lipid metabolism.J Clin Endocrinol Metab. 1999; 84: 112–22. PubMed

5. Kinniburgh D, et al.. Oral desogestrel with testosterone pellets induces consistent suppression of spermatogenesis to azoospermia in both Caucasian and Chinese men.Hum Reprod. 2002; 17: 1490–1501. PubMed

6. Anderson RA, et al.. Investigation of hormonal male contraception in African men: suppression of spermatogenesis by oral desogestrel with depot testosterone.Hum Reprod. 2002; 17: 2869–77. PubMed

7. Hair WM, et al.. A novel male contraceptive pill-patch combination: oral desogestrel and transdermal testosterone in the suppression of spermatogenesis in normal men.J Clin Endocrinol Metab. 2001; 86: 5201–9. PubMed

Adverse Effects, Treatment and Precautions

Adverse Effects and Precautions

As for progestogens in general (see Progesterone, Refer to and Refer to ). See also under Hormonal Contraceptives, Refer to and Refer to . When used as a progestogen-only contraceptive, irregular bleeding is more common with desogestrel than with other progestogen-only preparations. Desogestrel is reported to have few androgenic effects, and to have less adverse effect on the serum lipid profile than older 19-nortestosterone derivatives. However, there is some evidence that desogestrel-containing combined oral contraceptives are associated with a small increased risk of venous thromboembolism (see Refer to , and for precautions, see Refer to ).

(last reviewed 2010-06-30; last modified 2008-06-25)

Porphyria

The Drug Database for Acute Porphyria, compiled by the Norwegian Porphyria Centre (NAPOS) and the Porphyria Centre Sweden, classifies desogestrel in combined hormonal contraceptives as probably porphyrinogenic; it should be prescribed only for compelling reasons and precautions should be considered in all patients.1

(last reviewed 2010-06-30; last modified 2011-11-15)

References

1. The Drug Database for Acute Porphyria. Available at: Link (accessed 04/10/11)

Interactions

As for progestogens in general (see Progesterone, Refer to ). See also under Hormonal Contraceptives, Refer to .

(last reviewed 2010-06-30; last modified 1998-10-23)

Pharmacokinetics

After oral doses, desogestrel undergoes oxidative transformation in the intestinal mucosa and liver to its active metabolite 3-keto-desogestrel (etonogestrel—see Refer to ).

(last reviewed 2010-06-30; last modified 2008-06-20)

References.

(last reviewed 2010-06-30; last modified 2008-06-20)

References

1. Madden S, et al.. Metabolism of the contraceptive steroid desogestrel by the intestinal mucosa.Br J Clin Pharmacol. 1989; 27: 295–9. PubMed

2. Madden S, et al.. Metabolism of the contraceptive steroid desogestrel by human liver in vitro.J Steroid Biochem. 1990; 35: 281–8. PubMed

3. Kuhnz W, et al.. Protein binding of the contraceptive steroids gestodene, 3-keto-desogestrel and ethinyloestradiol in human serum.J Steroid Biochem. 1990; 35: 313–18. PubMed

4. Kuhnz W, et al.. Pharmacokinetics and serum protein binding of 3-keto-desogestrel in women during three cycles of treatment with a low-dose combination oral contraceptive.Arzneimittelforschung. 1992; 42: 1142–6. PubMed

5. Timmer CJ, et al.. Bioavailability and bioequivalence of etonogestrel from two oral formulations of desogestrel: Cerazette and Liseta.Eur J Drug Metab Pharmacokinet. 1999; 24: 335–43. PubMed

6. Verhoeven CH, et al.. Excretion and metabolism of desogestrel in healthy postmenopausal women.J Steroid Biochem Mol Biol. 2001; 78: 471–80. PubMed

7. Korhonen T, et al.. The role of CYP2C and CYP3A in the disposition of 3-keto-desogestrel after administration of desogestrel.Br J Clin Pharmacol. 2005; 60: 69–75. PubMed

Preparations: Single-Ingredient

The following preparations list represents a compilation of all available salt forms or related substances for this drug product.

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

ARGENTINA: Camelia; Carmin; Cerazette; Lumilac; Pink;AUSTRIA: Cerazette; Cycle; Cyprella¤; Desirett; Desofemono; Moniq; Tangolita;BELGIUM: Celea¤; Cerazette; Desoceane; Desopop; Lueva; Nacrez; Saphirena;BRAZIL: Araceli; Cerazette; Juliet; Kelly; Nactali; Perola;CHILE: Arlette; Cerazette; Lactafem; Nogesta; Vanish;CZECH REPUBLIC: Azalia; Cerazette; Daisenette; Evellien; Fleur¤; Florette; Lamya; Seculact; Torri; Velavel¤; Xynia; Zarelle¤;DENMARK: Azalia; Cerazet¤; Cerazette; Delamonie; Diamilla¤; Lueva¤; Nacrez¤; Vinelle; Zarelle;FINLAND: Azalia; Cerazette; Delamonie; Gestrina¤; Vinelle; Zarelle;FRANCE: Antigone; Cerazette; Clareal; Desopop; Diamilla; Optimizette;GERMANY: Cerazette; Damara; Desirett; Desofemono; Desofenance; Evakadin; Feanolla; Jubrele; Onefra; Solgest;GREECE: Cerazette;HONG KONG: Cerazette;HUNGARY: Azalia; Cerazette; Diamilla; Femelle; Nacrez;INDIA: Cerazette;INDONESIA: Cerazette; Desirett;IRELAND: Azalia; Cerazette;ISRAEL: Cerazette; Diamilla; Fominic;ITALY: Cerazet; Cerazette; Myrline;MALAYSIA: Cerazette;MEXICO: Cerazette;NETHERLANDS: Cerazette; Delamonie; Solgest; Zarelle;NORWAY: Cerazette; Vinelle;NEW ZEALAND: Cerazette;PHILIPPINES: Cerazette;POLAND: Azalia; Cerazette; Desandrelle; Desirett; Dessette mono; Diamilla; Lemena; Limetic; Ovulan; Seculact; Symonette;PORTUGAL: Azalia; Cerazette; Desostada¤; Diamilla; Fanaka¤; Lueva¤; Myrline;RUSSIAN FEDERATION: Cerazette (Чарозетта); Lactinette (Лактинет); Modell Mam (Модэлль Мам);SPAIN: Azalia; Cerazet; Desopop; Famylette¤; Kerizet; Nacrez;SWEDEN: Azalia; Cerazette; Gestrina; Vinelle; Zarelle;SWITZERLAND: Anouk; Azalia; Cerazette; Cevanel¤; Desofemono; Desonur; Diamilla; Yolienne; Zenzi;THAILAND: Cerazette;TURKEY: Cerazette;UNITED KINGDOM: Aizea; Cerazette; Cerelle; Zelleta;UKRAINE: Cerazette (Чарозетта)¤; Lactinette (Лактинет);VENEZUELA: Arlette; Cerazette; Valma;

Preparations: Multi-Ingredient

The following preparations list represents a compilation of all available salt forms or related substances for this drug product.

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Preparations: Pharmacopoeial

The following preparations list represents a compilation of all available salt forms or related substances for this drug product.

BP 2019: Desogestrel Tablets;USP 42: Desogestrel and Ethinyl Estradiol Tablets;

Therapeutic Use

Sex Hormones and their Modulators

Last Updated 1/21/20

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