2267
of monophasic combined oral contraceptive preparations. ette; Gr. : Cerazette; Hong Kong: Cerazette; Hung. : Azalia; Cer Doses of 50 to 150 micrograms daily may be used in triphasic azette; India: Cerazette; Indon.: Cerazette; Irl. : Cerazette; combined preparations. A dose of 75 micrograms daily is Israel: Cerazette; Ital.: Cerazet; Cerazette; Mex.: Cerazette; used as an oral progestogen -only contraceptive; unlike Neth.: Cerazette; Norw.: Cerazette; NZ: Cerazette; Philipp.: traditional progestogen-only contraceptives, desogestrel is Cerazette; Pol.: Azalia; Cerazette; Port.: Cerazette; Rus.: Ceraz ('lap03erra); (JlaKTHHer); Spain: said to reliably inhibit ovulation. Progestogen-only ette Lactinette Azalia; Cerazet; Swed.: Cerazette; Switz. : Cerazette; Thai.: Cerazette; UK: contraceptive efficacy is reduced if a dose of desogestrel is Aizea; Cerazette; Cerelle; Zelleta; Ukr.: Cerazette (qapo3erra); Dienogest is a nonethinylated progestogen (see Progester delayed by more than 12 hours. Lactinette (JlaK.TnHer); Venez.: Arlette; Cerazette. one, p. 2300.2) structurally related to nortestosterone. It is reported to have anti-androgenic properties. Dienogest is The effects of a progestogen-only Arg.: Aus Contraception. Multi-ingredient Preparations. Marvelon; Mercilon; used as the progestogen component of some combined oral contraceptive containing desogestrel have been tral. : Marvelon; Austria: Gracial; Liberel; Marvelon; Mercilon; contraceptives (see p. 2231.3). A dose of 2mg daily is reported.1·3 Oral desogestrel has also been investigated as Belg.: Desorellet; Gracial; Marvelon; Mercilon; Ovidol; Braz.: typically used in monophasic preparations, and doses of 2 or a male contraceptive, combined with testosterone given Femina; Gestradiol; Gracia]; Malu; Mercilon Conti; Merdlon; 3 mg daily may be found in multiphasic sequential by intramuscular injection,4 subcutaneous implant,5•6 or Microdiol; Minian; Novial; Primera; Primeravintet; Canad. : preparations. It is also used as the progestogen component transdermal patch.7 Apri; Linessa; Marvelon; Ortho-Cept; Chile: Ciclidon; Conti Marvelon; Dal; Desoren; Gracial; Gynostat; Marvelon; Midalet; in menopausal HRT (see p. 2244. 1) in a daily dose of 2 mg. l. Collaborative study group on the desogestrel-containing progestogen (�JlXJk); In the management of endometriosis (p. 2264.1) an oral only pill. A double-blind study comparing the contraceptive efficacy, Miniestrel; Neolette; China: Mercilon Cz.: Adele; Gra acceptability and safety of two progestogen-only pills containing cial; Laurina; Marvelon; Mercilon; Natalya; Novynette; Regu dose of dienogest 2 mg daily is used; it is given in a desogestrel 75 micrograms/day or levonorgestrel 30 micrograms/day. lon; Tricia; Denm.: Daisynelle; Desorelle; Femelle; Femigen; continuous regimen regardless of menstrual bleeding. Bur J Contracept Reprod Health Care 1998; 3: 169-78. Femistad; Gracial; Marvelon; Mercilon; Novynette; Fin.: Gra Reviews. 2. Rice CF, et al. A comparison of the inhibition of ovulation achieved by cial; Laurina; Marvelon; Mercilon; Fr.: Cycleanet; Desobel; l. Foster RH, Wilde Dienogest. Drugs 1998; 56: 825-33. desogestrel 75 micrograms and levonorgestrel 30 micrograms daily. Hum MI. Mercilon; Varnoline; Ger.: Biviol; Cyclosat; Desmin; Lamunat; 2. Wellington Perry CM. Estradiol valerate/dienogest. Drugs 2002; 62: Reprod 1999; 14: 982-5. K 491-504. 3. Korver T, et al. Maintenance of ovulation inhibition with the 75- Lavelle; Marvelon; Novial; Oviala; Oviolt; Gr.: Gracial; Lauri 3. Hoy SM, Scott LJ. Estradiol valerate/dienogest: in oral contraception. microgram desogestrel-only contraceptive pill (Cerazette) after na; Marvelon; Mercilon; Hong Kong: Gracial; Marvelon; Drugs 2009; 69: 1635--46. scheduled 12-h delays in tablet intake. Contraception 2005; 71: 8-13. Mercilon; Novynette; Hung.: Gracial; Laurina; Marvelon; 4. Perez-Campos EF. Ethinylestradioltdienogest in oral contraception. 4. Wu FCW, et al. Oral progestogen combined with testosterone as a Mercilon; Novynette; Regulon; Samba; India: Femilon; Locipil; Drugs 2010; 70: 681-9. potential male contraceptive: additive effects between desogestrel and Novelon; Indon.: Marvelon; Mercilon; Irl. : Gracial; Leticia; 5. McCormack PL. Dienogest: a review of its use in the treatment of te<;;tosterone enanthate in suppression of spermatogenesis, pituitary Marviol; Mercilon; Vivides; Israel: Feminet; Mercilon; 1\tticro endometriosis. Drugs 2010; 70: 2073-88. testicular axis, and lipid metabolism. J Clin Endocrinol Metab 1999; 84: 112-22. diol; Ital. : Dueva; Gracial; Lucille; Mercilon; Novynette; Pla 5. Kinniburgh D, et al. Oral desogestrel with testosterone pellets induces num; Practil; Securgin; Malaysia: Marvelon; Merdlon; Novyn Porphyria. The Drug Database for Acute Porphyria, com consistent suppression of spermatogenesis to azoospermia in both ette; Regulon; Mex. : Desmin; Detegen; Marvelon; Mercilon; piled by the Norwegian Porphyria Centre (NAPOS) and Caucasian and Chinese men. Hum Reprod 2002; 17: 1490-1501. Novial; Neth.: Gracial; Juliane; Laurina; Lonicera; Marvelon; the Porphyria Centre Sweden, classifies dienogest and oes 6. Anderson RA, et al. Investigation of hormonal male contraception in Norw.: NZ: Mercilon; Ovidolt; Marvelon; Mercilon; Marvelon; trogen combinations as probably porphyrinogenic; it African men: suppression of spermatogenesis by oral desogestrel with Mercilon; Philipp.: Gracia!; Marvelon; Mercilon; Pol.: depot testosterone. Hum Reprod 2002; 17: 2869-77. should be prescribed only for compelling reasons and pre Marvelon; Mercilon; Novynette; Regulon; Port.: Gracial; Lauri 7. Hair WM, et a!. A novel male contraceptive pill-patch combination: oral cautions should be considered in all patients.' desogestrel and transdermal testosterone in the suppression of na; Marvelon; Mercilon; Novynette; Regulon; Rus.: Marvelon l. The Drug Database for Acute Porphyria. Available at: http:l/www. spermatogenesis in normal men. J Clin Endocrinol Metab 2001; 86: (MapnenoH); Mercilon (MepcHJioH); Novynette (HonHHer); Regu drugs-porphyria.org (accessed 04/lO/ll) '5201-9. lon (PerynoH); Tri-Merci (Tpw-Mepca); S.Afr.: Marvelon; Mercilon; Singapore: Marvelon; Mercilon; Spain: Bemasive; Swed. : Gracial; Microdiol; Regulon; Suavuret; Desolett; P.r.�P.?.r<:lti()n.� ...... Adverse Effects and Precautions Switz. : Mercilon; Trimiront; Desoren; Gracia!; Marvelon; (details are given in Volume B) As for progestogens in general (see Progesterone, p. 2301.2 Mercilon; Thai.: Daisy; Marvelon; Mercilon; Minny; Novyn ProprietaryPreparations and p. 2301.3). See also under Hormonal Contraceptives, ette; Oilezz; Turk. : Desolett; Myralon; UK: Cimizt; Gedarel; Single-ingredient Prepara�ons. Austral.: Visanne; Austria: p. 2233.3 and p. 2240.3. When used as a progestogen-only Marvelon; Mercilon; Ukr.: Marvelon (MapnenoH); Mercilon Visanne; Canad.: Visanne; Cz.: Visanne; Denm.: Visanne; Fin.: contraceptive, irregular bleeding is more common with (MepcmiOH); Novynette (HonHHer); Regulon (PerynoH); Tri Visanne; Ger.: Visanne; Gr.: Visannette; Hung.: Visanne; Israel: desogestrel than with other progestogen-only preparations. Merci (TpH-MepcH); USA: Apri; Azurette; Caziant; Cesia; Visabelle; Jpn: Dinagest; Neth.: Visanne; Norw.: Visanne; Port. : Desogestrel is reported to have few androgenic effects, and Cyclessa; Desogen; Kariva; Mircette; Ortho-Cept; Reclipsen; Visanne; Singapore: Visanne; Spain: Visannette; Swed.: to have less adverse effect on the serum lipid profile than Solia; Velivet; Viorele; Venez. : Ciclidon; Marvelon; Mercilon; Visanne; Switz. : Visanne. Mipil; Novial. older 19-nortestosterone derivatives. However, there is Multi-ingredient Prepara�ons. Arg.: Dienopil; Florence; Rubi; some evidence that desogestrel-containing combined oral PharmacopoeialPrepara�ons Austral.: Qlaira; Valette; Austria: Motion; Qlaira; Valette; Belg.: contraceptives are associated with a small increased risk of BP 2014: Desogestrel Tablets; Climodien; Qlaira; Chile: Gianda; Tinelle; Cz. : Dienille; Dienor venous thromboembolism (see p. 2238.1, and for USP 36: Desogestrel and Ethinyl Estradiol Tablets. ette; Jeanine; Klimodien; Qlaira; Denm.: Climodient; Qlaira; precautions, see p. 2241.2). Fin.: Qlaira; Fr.: Climodiene; Qlaira; Ger.: Climodien; Lafarnme; Maxim; Qlaira; Valette; Gr.: Climodien; Qlaira; Porphyria. The Drug Database for Acute Porphyria, com Hung. : Dienille; Qlaira; Irl.: Qlaira; Israel: Qlair; Ital. : Klaira; piled by the Norwegian Porphyria Centre (NAPOS) and Neth.: Climodien; Lafamme; Qlaira; Norw.: Climodient; Qlaira; the Porphyria Centre Sweden, classifies desogestrel in Pol.: Atywia; Jeanine; Qlaira; Port. : Climodien; Lafamme; combined hormonal contraceptives as probably porphyri Qlaira; Valette; Rus.: Climodien (KnHMO.rt:HeH); Jeanine ()KaHHH); nogenic; it should be prescribed only for compelling rea Singapore: Qlaira; Spain: Ailyn; Climodien; Danielle; Donabel; sons and precautions should be considered in all patients.1 Mevaren; Qlaira; Swed. : Climodient; Qlaira; Turk.: Climodien; UK: Qlaira; Ukr.: Jeanine ()KaHHH); Klimodien (KrrHMO,D.JfeH)t; l. The Drug Database for Acute Porphyria. Available at: http:/fwww. Silhouette (CJIJIYeT); USA: Natazia. drugs-porphyria.org (accessed 04/ 10111) Interactions Diethylstilbestrol (BAN, r/NN) As for progestogens in general (see Progesterone, p. 2302.2). See also under Hormonal Contraceptives, p. 2242.3. [)ES: Diethylstilbestrol; D!ethylstilb¢sttiotu•n:· •. oJeth)dliti!boes" trol; . Dietilestii!JE:srtol: • Dietilstlfbest.tolis: .• ()ietil�tiii;Qsztrol; Oi�;.tylstiltl strol; Oi�tyyllstlfbestroH; Es ilb!!strol; NSC -3010: Pharmacokinetics USP 36: (Dienestrol). Colourless, white, or practically white ; .• � Stilb�?'!01; tilboestrof; After oral doses, desogestrel undergoes oxidative transfor needle-like crystals, or white or practically white crystalline � )lM�TW!dw11btl"i!fflOfl : (£\·of5-Di�th)if�tilbenEt4-4'..Jtoi. mation in the intestinal mucosa and liver to its active powder. It is odourless. Practically insoluble in water; · metabolite 3-keto-desogestrel (etonogestrel-see soluble in alcohol, in acetone, in ether, in methyl alcohol, in C,aH,2qO�=iZ6�4 · p. 2277.3). propylene glycol, and in solutions of alkali hydroxides; <:)\��S6-_1�- t.· ATC:c References. slightly soluble in chloroform and in fatty oils. GOJC8(12;L02AA0 i, • ...... , . AI(,; Yit'7 ()(j03Cf!(J2; CXi03(C05, 1. Madden S, et al. Metabolism of the contraceptive steroid desogestre] by . OL02Aj,p. l the intestinal mucosa. Br J Clin Phannacol 1989; 27: 295-9. .t;JN/1. -;''73}/JCAJ)B'[, . 2. Madden S, et a!. Metabolism of the contraceptive steroid desogestrel by Pharmaco oeias. In Chin., Bur. (see p. vii), and US. human liver in vitro. J Steroid Biochem 1990; 35: 281-8. Dienestrol is a synthetic nonsteroidal oestrogen structurally p 3. Kuhnz W, et al. Protein binding of the contraceptive steroids gestodene, Ph. Eur. 8: (Diethylstilbestrol). A white or almost white 3-keto·desogestrel and ethinyloestradiol in human serum. J Steroid related to diethylstilbestrol (below). It has been used as a Biochem 1990; 35: 313-18. vaginal cream in the treatment of menopausal atrophic crystalline powder. Practically insoluble in water; freely 4. Kuhnz W, et al. Pharmacokinetics and serum protein binding of 3-keto vaginitis. If used on a long-term basis in women with a soluble in alcohol; dissolves in solutions of alkali desogestrel in women during three cycles of treatment with a low-dose uterus a progestogen is required. hydroxides. Protect from light. combination oral contraceptive. Arzneimittelforschung 1992; 42: 1142-6. 5. Timmer CJ, et al. Bioavailability and bioequivalence of etonogestrel from Dienestrol diacetate has been used as an ingredient of USP 36: (Diethylstilbestrol). A white, odourless, crystalline two oral formulations of desogestrel: Cerazette and liseta. Bur .J Drug topical preparations for skin disorders. powder. Practically insoluble in water; soluble in alcohol, in Metab Phannacokinet 1999; 24: 335-43. chloroform, in ether, in fatty oils, and in dilute alkali 6. Verhoeven CH, et al. Excretion and metabolism of desogestrel in healthy hydroxides. Store in airtight containers. Protect from light. postmenopausal women. J Steroid Biochem Mol Bioi 2001; 78: 471-80. P.r�P.?.r<:lti?.n.� 7. Korhonen T, et a!. The role of CYP2C and CYP3A in the disposition of 3- ProprietaryPreparations (details are given in Volume B) keto-desogestrel after administration of desogestrel. Br J Clin Phannacol Diethylstilbestrol Dipropionate (BANM, riNNM! 2005; 60: 69-75. Single-ingredient Prepara�ons. USA: Ortho-Dienestrolt. Pharmacopoeial Preparations USP 36: Dienestrol Cream. ProprietaryPreparations (details are given in Volume B) Single-ingredient Preparations. Arg.: Camelia; Carmin; Ceraz ette; Lumilac; Austria: Cerazette; Belg.: Cerazette; Lueva; Dienogest (BAN, USAN, r/NN) Braz. : Cerazette; Kelly; Chile: Arlette; Cerazette; Lactafem; Nogesta; Vanish; Cz.: Azalia; Cerazette; Fleur; Denm.: Cerazet; D
The symbol t denotes a preparation no longer actively marketed The symbol ® denotes a substance whose use may be restricted in certain sports (see p. viii)