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Home , Ulipristal acetate

Acetate/Triptorelin 231 1

Disturbed behaviour. Combined therapy with triptorelin, 5. Keating GM. Triptorelin embonate (6�month formulation). Drugs 2010; 70: 347-53. which suppressed testosterone secretion by inhibiting the pituitary-gonadal axis, and supportive psychotherapy, has Porphyria. Triptorelin has been used successfully to sup­ been tried in the treatment of men with paraphilias (see press premenstrual exacerbations of acute intermittent p. 1030.2): a reduction in abnormal sexual thoughts and porphyria (p. 1556.1), in doses of 3.75mg by intramuscu­ behaviours has been reported, although the study was lar depot injection given monthly.1'2 To reduce the risk of uncontrolled.1 osteoporosis, 'add-back' therapy with topical oestrogen 1. ROsier A, Witztum E. Treatment of men with paraphilia with a long­ and oral calcium was used in one case, 1 and in acting analogue of gonadotropin-releasing hormone. N Engl J Med 1998; 338: 416-22. another.2 I. De Block CEM, et al. Premenstrual attacks of acute intermittent Endometriosis. Gonadorelin analogues are effective in the porphyria: hormonal and metabolic aspects - a case report. Bur J Endocrinol I999; 141: 50--4. management of endometriosis (p. 2264.1), but the need 2. Castelo-Branco C, et al. Use of gonadotropin� releasing hormone analog for long-term therapy to prevent recurrence limits their with tibolone to prevent cyclic attacks of acute intermittent porphyria. value because of the risk of osteoporosis; 'add-back' ther­ 2001; SO: 995-6. apy (hormone replacement) can be used to prevent this. Precocious puberty. The gonadorelin analogues have lar­ References. Uses and Administration I. Lindsay PC, et al. The effect of add-back treatment with tibolone (Livial) gely replaced other treatments in the management of cen­ Triptorelin is an analogue of gonadorelin (p. 2280.3) with on patients treated with the gonadotropin-releasing hormone tral precocious puberty (p. 2254.1). A dose equivalent to triptorelin (Decapeptyl). Fertil Steril 1996; 65: 342-8. similar properties. It is used for the suppression of gonadal triptorelin 50 micrograms/kg, from a 3-mg depot prepara­ 2. Bergqvist A et al. Effects of triptorelin versus placebo on the symptoms tion, may be given intramuscularly every 4 weeks. Alter­ production in the treatment of malignant of endometriosis. Fertil Steri/ 1998; 69: 702-8. neoplasms of the prostate, deviant sexual behaviour in men, 3. Donnez J, et al. Equivalence of the 3-month and 28-day formulations of natively, using a 3.75-mg preparation, doses of 1.875 mg central precocious puberty, and in the management of triptorelin with regard to achievement and maintenance of medical for children weighing less than 20kg, 2.5mg for children castration in women with endometriosis. Fertil Steril 2004; 81: 297-304. endometriosis, female infertility, and uterine fibroids. of 20 to 30kg, or 3.75 mg for children of more than 30kg, 4. Wong AY, Tang L. An open and randomized study comparing the may be given intramuscularly or subcutaneously. The first Triptorelin may be given as the base, acetate, diacetate, or efficacy of standard d.anazol and modified triptorelin regimens for embonate, although for some preparations stated to contain postoperative disease management of moderate to severe endometriosis. 3 doses should be given at 14-day intervals, with further the acetate or diacetate it is not always clear which has Fertil Steril 2004; 81: 1522-7. doses given every 4 weeks; this may be increased to once 5. Loverro G, et al. A randomized study comparing triptorelin or expectant actually been used. Doses are usually given in terms of the every 3 weeks if necessary. A longer acring 11.25-mg management following conservative laparoscopic surgery for sympto­ depot preparation, given intramuscularly once every 3 base, and the following are each equivalent to about 1 mg of matic stage III-IV endometriosis. Bur J Obstet Gyneccl Reprod Biol 2008; triptorelin: 136: 194-8. months, is another alternative. triptorelin acetate, 1.05 mg References to the use of triptorelin. • triptorelin diacetate, 1.09 mg Fibroids. Gonadorelin analogues have been used as an 1. Oostdijk W, et al. Final height in central precocious puberty after long • term treatment with a slow release GnRH agonist. Arch Dis Child I996; triptorelin embonate, 1.30mg alternative to surgery in the treatment of uterine fibroids • 75: 292-7. Triptorelin is given as a daily subcutaneous injection, or as (see p. 2281.2), despite some concern that this may com­ 2. Cassia A, et al. Randomised trial of IliRH analogue treatment on final an intramuscular or subcutaneous depot preparation lasting plicate the diagnosis of malignancy. height in girls with onset of puberty aged 7.5-8.5 years. Arch Dis Child a month or longer. References to the use of triptorelin. I999; 81: 329-32. 3. Heger S, et al. Long-term outcome after depot gonadotropin-releasing 1. van Leusden HA Symptom-free interval after triptorelin treatment of In the palliative treatment of advanced prostate cancer, . hormone agonist treatment of central precocious puberty: final height, uterine fibroids: long-term results. Gyneccl Bndocrino/ 1992; 6: 189-98. a dose equivalent to triptorelin 3 or 3.75 mg is given body proportions, body composition, bone mineral density, and 2. Golan A, et al. Pre-operative gonadotrophin-releasing hormone agonist intramuscularly as a depot preparation every 4 weeks; the reproductive function. J Clin Bndocrinol Metab I999; 4583-90. treatment in surgery for uterine leiomyomata. Hum Reprod 1993; 8: 450-- 84: 4. Carel J-C, et al. Final height after long-term treatment with triptorelin first dose may be preceded by 100micrograms daily for 7 2. slow release for central precocious pubeny: importance of statural 3. Broekmans FJ, etal. Two-step gonadotropin-releasing hormone agonist days by subcutaneous injection. In some countries, depot growth after interruption of treatment. J Clin Endocrinol Metab I999; treatment of uterine leiomyomas: standard-dose therapy followed by 84: preparations containing 3.75 mg may be given subcuta­ I973-8. reduced-dose therapy. Am J Obstet Gynecol 1996; 175: I208-I6. neously instead. A longer-acting depot preparation that 5. Mul D, et al. Effect of gonadotropin-releasing hormone agonist 4. Vercellini P, et al. Treatment with a gonadotrophin releasing hormone treatment in boys with central precocious puberty: final height results. contains the equivalent of triptorelin 11.25 mg is given once agonist before hysterectomy for leiomyomas: results of a multicentre, Horm Res 2002; 58: I-7. randomised controlled trial. Br J Obstet Gynaeco/ 1998; 105: II48-54. every 12 to 13 weeks; a depot supplying the equivalent of 6. Carel JC, et al. Triptorelin 3-month CPP Study Group. Three-month 5. Seracchioli R, et al. GnRH agonist treatment before total laparoscopic 22.5 mg every 24 weeks is also available in some countries. sustained-release triptorelin (I1.25 mg) in the treatment of central hysterectomy for large uteri. JAm Assoc Gynecol Laparosc 2003; 10: 3I6- Some countries also allow use of depot doses of 3 mg once precocious puberty. Bur J Bndocrino/ 2006; 154: II9-24. 19. every 4 weeks or 11.2 5 mg once every 12 to 13 weeks for medical therapy in locally advanced disease. An Growth retardation. As discussed on p. 1918.3 gonado­ Adverse Effects and Precautions anti -androgen such as acetate may be given relin analogues have been given with growth hormone to for several days before beginning therapy with triptorelin As for Gonadorelin, p. 2282.1. short girls without growth hormone deficiency, in an and continued for about 3 weeks to avoid the risk of a attempt to delay puberty and bone maturation and thus For reference to local reactions occurring disease flare. Locol reactions. maximise the final height achieved. Use in growth horm­ following injection of gonadorelin analogues, including An 11.25-mg intramuscular depot preparation, given one-deficient clrildren has also been investigated. How­ every 12 weeks, may be used in the management of triptorelin, see Leuprorelin Acetate, p. 2286.3. ever, there is some doubt about the extent of benefit, and deviant sexual behaviour in men. The addition of an in any case the concept of such treatment in children who Porphyria. The Drug Database for Acute Porphyria, com­ anti-androgen should be considered when starting therapy, are not clinically deficient in growth hormone is contro­ piled by the Norwegian Porphyria Centre (NAPOS) and to counteract the initial rise in serum-testosterone versial, and some authorities do not consider it appropri­ the Porphyria Centre Sweden, classifies triptorelin as por­ concentrations. Similarly, the addition of an ate. phyrinogenic; it should be prescribed only for compelling anti -androgen should be considered before stopping References to the use of triptorelin. reasons and precautions should be taken in all patients.1 triptorelin because of a risk of increased sensitivity to I. Saggese G, et al. Combination treatment with growth hormone and For the use of triptorelin in the prevention of premen­ restored testosterone. gonadotropin-releasing hormone analogs in short normal girls. J Pediatr strual exacerbations of acute porphyria, see above. Similar doses of the 3- or 3.75-mg depot preparations I995; 126: 468-73. may be given for up to 6 months in the management of 2. Saggese G, et al. The effect of administering gonadotropin-releasing I. The Drug Database for Acute Porphyria. Available at: http:/lwww. drugs-porphyria.org (accessed 07 I 0/II) endometriosis or uterine fibroids, with treatment begun hormone agonist with recombinant-human growth hormone (GH) on I the final height of girls with isolated GH deficiency: results from a during the first 5 days of the menstrual cycle. The 11.25-mg controlled study. J Clin Endocrinol Metab 200I; 86: I900-4. Sepsis. A report of 2 patients in whom triptorelin therapy depot may be used as an alternative for endometriosis. In 3. Kamp GA, et al. A randomized controlled trial of three years growth led to sepsis caused by expulsion of necrotic fibroids hormone and gonadotropin-releasing hormone agonist treatment in the management of female infertility doses of 100 micr­ through the cervix. ograms subcutaneously daily, with gonadotrophins, have children with idiopathic short stature and intrauterine growth I retardation. J Clin Bndocrinol Metab 200I; 86: 2969-75. 1. Ellenbogen A, et al. Complication of triptorelin treatment for uterine been recommended from the second day of the menstrual 4. Tauber M. et al. Can some growth hormone (GH)-deficient children myomas. Lancet I989; ii: 167-8. cycle for about 10 to 12 days. benefit from combined therapy with gonadotropin-releasing hormone analogs and GH? Results of a retrospective study. J Clin Endoainol Metab 2003; 88: II79-83. Interactions Administration in children. Triptorelin may be used in As for Gonadorelin, p. 2282.2. the management of central precocious puberty and has Infertility. Gonadorelin analogues are used in the manage­ been used in the diagnosis of delayed puberty. It has also ment of infertility related to hypogonadotrophic hypo­ been tried in the treatment of growth retardation (see gonadism in both men and women. For a discussion of below). infertility and its management, including the role of Triptorelin is rapidly absorbed after subcutaneous injection gonadorelin analogues, see p. 22 53 .I. and peak plasma concentrations occur about 40 minutes Diagnosis hypothalamic ond pituitary dysfunction. after a dose. The biological half-life is about 7.5 hours, of Malignant neoplasms. Triptorelin, like other gonadorelin Gonadorelin analogues have been used in the diagnosis of although longer half-lives have been reported in patients analogues, may be used in the production of androgen delayed puberty (p. 2252.1). Triptorelin has been used in with prostate cancer, and shorter half-lives in some groups blockade in patients with prostate cancer (p. 712.3). boys to differentiate gonadotrophin deficiency from consti­ of healthy subjects. tutional delayed puberty, 1•2 although one study' found it References. References. to be less accurate than a test using human chorionic 1. Klippel KF, et al. Wirksamkeit und Vertraglichkeit von 2 Applikations­ I. MUller PO, et al. Pharmacokinetics of triptorelin after intravenous bolus formen (s.c. und i.m.) von Decapeptyl Depot bei Patienten mit administration in healthy males and in males with renal or hepatic gonadotrophin. fortgeschrittenem Prostatakarzinom. Urologe I999; 38: 270--5. insufficiency. Br J Clin Pharmaool 1997; 44: 335-41. 1. zamboni G, et al. Use of the gonadotropin-releasing hormone agonist 2. Heyns CF, et al. Comparative efficacy of triptorelin pamoate and triptorelin in the diagnosis of delayed puberty in boys. J Pediatr 1995; leuprolide acetate in men with advanced prostate cancer. BJU lnt 2003; 126: 756-8. 92: 226-31. Preparations 2. Kauschansky A, et al. Use of GnRH agonist and human chorionic 3. Botto H, et al. Etude randomisee multicentrique comparant Ia castration p�ri;;i;;;y·�;:;;-��·(d�;�ii�·��;·;���·;�·:v�i-;;;;;�·ii;············· gonadotrophin tests for differentiating constitutional delayed puberty medicale par triptoreline a Ia castration chirurgicale dans le traitement from gonadotrophin deficiency in boys. Clin Endocrinol (Oxj) 2002; 56: du cancer de la prostate localement avanc€ ou metastatique. Pros Urol Arg.: Decapeptyl; Gonapeptyl; 603-7. 2007; 17: 235-9. Single-ingredient Preparations. Austral.: Diphereline; Austria: Decapeptyl; Pamorelin; Belg.: 3. Degros V, et al. The human chorionic gonadotropin test is more powerful 4. LundstrOm EA, et al. Triptorelin 6�month formulation in the than the gonadotropin-releasing hormone agonist test to discriminate management of patients with locally advanced and metastatic prostate Decapeptyl; Gonapeptyl; Salvacyl; Braz.: Gonapeptyl; Neo Dec­ male isolated hypogonadotropic hypogonadism from constitutional cancer: an open-labeL non-comparative, multicentre, phase III study. apeptyl; Canad. : Trelstar; Chile: Decapeptyl; China: Decapeptyl delayed puberty. Bur J Endocrinol 2003; 149: 23-9. Clin Drug Investig 2009; 29: 757-65. (i.!i&Ht); Diphereline (i.!i$M<); Cz.: Decapeptyl; Diphereline;

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) 231 2 Sex Hormones and their Modulators

Denm.: Decapeptyl; Gonapeptyl; Pamorelin; Salvacyl; Fin.: Dec­ The elimination of is expected to be 1' Uses and Administration apeptyl; Gonapeptyl; Pamorelin; Salvacyl; Fr. : Decapeptyl; reduced in patients with hepatic impairment and its use in Gonapeptyl; Salvacyl; Ger.: Decapeptyl; Pamorelin; Salvacyl; moderate or severe impairment is not recommended Urofollitropin is a gonadotrophin, obtained from the urine Gr.: Arvekap; Gonapeptyl; Hong Kong: Decapeptyl; Diphere­ without close monitoring. Ulipristal acetate has a high of postmenopausal women, possessing follicle-stimulating line; Hung.: Decapeptyl; Diphereline; India: Decapeptyl; Irl. : affinity for receptors, and hormone (FSH) activity but virtually no luteinising activity. Israel: Ital. : Decapcptyl; Gonapcptyl; Decapeptyl; Diphereline; effects have been seen in animal studies. The use of ulipristal For details of the actions of FSH, see p. 2278.2. Decapeptyl; Gonapeptyl; Malaysia: Decapeptyl; Mex. : Pam ore­ acetate is not recommended in patients who have asthma Urofollitropin is used similarly to human menopausal lin; Neth.: Decapeptyl; Gonapeptyl; Pamorelin; Salvacyl; Tripto­ that is inadequately controlled by oral gonadotrophins (p. 2284.2) in the treatment of female fem; Norw. : Pamorelin; Salvapar; Philipp.: Decapeptyl; Pol. : infertility with the exception that, being without Decapeptyl; Diphereline; Port. : Decapeptyl; Fertipeptil; Gona­ therapy. luteinising hormone activity, it can be used in patients peptyl; Rus.: Decapeptyl (,[l;eKanenrilll); Diphereline where any increase in luteinising hormone activity is not ().1mj>epemm); S.Afr. : Decapeptylt; Gonapeptyl; Singapore: Dec­ apeptyl; Spain: Decapeptyl; Gonapeptyl; Swed.: Decapeptylt; Interactions required, as in polycystic ovarian disease. Urofollitropin is given subcutaneously or intramuscularly in a dosage Gonapeptyl; Moapart; Pamorelin; Switz. : Decapeptyl; Pamore­ Drugs that increase gastric pH (such as antacids, Hrreceptor adjusted according to the patient's response. Usually a dose lin; Salvacyl; Thai.: Decapeptyl; Diphereline; Turk. : Decapep­ antagonists, and proton pump inhibitors) may reduce the providing 75 to !50 units of FSH daily is given initially. tyl; UK: Decapeptyl; Gonapeptyl; Salvacyl; Ukr. : Decapeptyl absorption of ulipristal acetate. This may reduce its efficacy eKanerrnm); Diphereline (LI,m}Jepemrn); USA: Trelstar; Venez. : When an adequate response is achieved, as determined by CU for and concmnitant use is Decapeptyl. oestrogen monitoring or ultrasonic visualisation of follicles, therefore not recommended. However, during continuous treatment is stopped and after I or 2 days a single dose of use the systemic exposure to ulipristal increases (with a chorionic gonadotrophin 5000 to lO 000 units is given to delayed and decreased peak plasma concentration) and the induce . Treatment with urofollitropin should be effect is not expected to be clinically significant for patients stopped if there is no response after 4 weeks although being treated for uterine fibroids. Drugs that alter the treatment may be attempted again in future cycles. US activity of the cytochrome P450 isoenzyme CYP3A4 have product information has recommended that a maximum the potential to affect the plasma concentrations of ulipristal daily dose of 450 units should not be exceeded, and that acetate. CYP3A4 inducers may decrease its efficacy as an courses of treatment should be no longer than 12 days. emergency contraceptive, and an interaction should be Urofollitropin is also used with other drugs as part of IVF considered possible for at least 2 to 3 weeks after such procedures. It is typically given in a dose providing 150 to inducers have been stopped. Concomitant use with potent 225 units of FSH daily, usually beginning from day 2 or 3 of inducers is not recommended with ulipristal acetate given the menstrual cycle. Alternatively, therapy has been begun continuously for fibroid treatment. Moderate and potent with clomifene citrate and continued with urofollitropin, or inhibitors of CYP3A4 are also not recommended with urofollitropin may be given after suppression of gonadotro­ continuous therapy. phin release with a gonadorelin analogue. Treatment is Ulipristal acetate may interfere with the action of continued until an adequate response is obtained and the , such as those found in combined and final injection of urofollitropin is followed I to 2 days later Uses and Administration -only hormonal contraceptives. Regular hor­ by 5000 to l 0 000 units of chorionic gonadotrophin. Oocyte Ulipristal is a with monal contraception may be continued when ulipristal retrieval is performed 34 to 3 5 hours later. antagonist and effects. It inhibits or delays acetate is used for emergency contraception, but a reliable Urofollitropin is also used with chorionic gonadotrophin ovulation, alters the endometrial epithelium, and can barrier method of contraception should also be used until to stimulate spermatogenesis in the treatment of male reduce fibroid size. the next menstrual period starts. The concomitant use of , infertility, although a preparation with combined lutein­ A single oral dose of ulipristal acetate 30 mg may be given ulipristal acetate and for emergency : ising activity, such as human menopausal gonadotrophins, for emergency contraception (p. 2233.2). 1t should be taken contraception is not recommended. A non-hormonal may be preferred. The usual dose of urofollitropin provides as soon as possible, and no later than 120 hours (5 days), contraceptive method is recommended during continuous l50units of FSH three times a week. Treatment with after unprotected . If vomiting occurs ulipristal acetate treatment of fibroids. urofollitropin and chorionic gonadotrophin should be within 3 hours, another dose should be taken. Ulipristal is In-vitro studies suggest that ulipristal acetate may be an continued for at least 4 months. For a brief discussion of also under investigation as a continuous form of inhibitor of P-glycoprotein. Co-administration of ulipristal hypogonadism see p. 2252.3. contraception. with substrates of this transporter protein is therefore not Ulipristal acetate may be used for pre-operative recommended, although clinical evidence of an interaction Infertility. For reference to the use of preparations with management in women with symptoms of uterine fibroids is lacking. (p. 2281.2). An oral dose of 5 mg once daily is used, usually follicle-stimulating hormone activity in infertility, see for up to 3 months before surgery. Treatment should be p. 2253.1. started during the first week of a menstrual cycle. A Pharmacokinetics References to the use of urofollitropin including significant reduction in menstrual blood loss or amenor­ contradictory results as to its relative efficacy versus Ulipristal acetate is rapidly absorbed from the gastro­ rhoea is expected within the first l 0 days of treatment; recombinant follicleAstimu1ating hormone. intestinal tract; its absorption is pH-dependent and may be menstrual periods generally return within 4 weeks after I. McFaul PB, et al. Treatment of clomiphene citrate-resistant polycystic reduced when gastric pH is raised. The drug is highly bound ovarian syndrome with pure follicle-stimulating hormone or human stopping treatment. to plasma proteins. It is extensively metabolised to menopausal gonadotropin. Perfil Steri/ 1990; 53: 792-7. References. demethylated and hydroxylated metabolites, mainly by 2. European Metrodin HP Study Group. Efficacy and safety of highly purified urinary follicle-stimulating hormone with human chorionic L Anonymous. Ulipristal - a new emergency contraceptive pill. Drug Ther Bull 2010; 48: 86-8. the cytochrome P450 isoenzyme CYP3A4 and to a small gonadotropin for treating men with isolated hypogonadotropic 2. McKeage K, Croxtall JD. Ulipristal acetate: a review of its usc in extent by CYPlA2 and CYP2D6. The terminal plasma half­ hypogonadism. Fertil Steril 1998; 70: 256-62. emergency contraception. Drugs 2011; 71: 935-45. life of ulipristal acetate is about 32 to 38 hours after a single 3. Crain JL, et a!. Outcome comparison of in vitro fertilization treatment 3. Snow SE, et al. Ulipristal acetate for emergency contraception. Ann dose. with highly purified subcutaneous follicle-stimulating hormone Pharmacother 2011; 45: 780-6. (Fertinex, a urofollitropin) versus intramuscular menotropins. Am 1 4. Donnez J, et al. PEARL I Study Group. Ulipristal acetate versus placebo 1998; 179: 299-307. for fibroid treatment before surgery. N Engl 1 Med 2012; 366: 409-20. 4. Lenton et al. Induction of ovulation in women undergoing assisted 5. Donnez J, et a!. PEARL II Study Group. Ulipristal acetate versus reproductive techniques: recombinant human FSH (follitropin versus highly purified urinary FSH (urofollitropin HP) . Hum leuprolide acetate for uterine fibroids. N Eng! J Med 2012; 366: 421-32. (details are given in Volume B) ProprietaryPreparations 2000; 15: 1021-7. 5. Mohamed MA, et al. Urinary follicle-stimulating hormone (FSH) is more Adverse Effects and Precautions Single-ingredient Preparations, Austria: ellaOne; Belg.: ellaOne; effective than recombinant FSH in older women in a controlled Cz. : Denm.: Fr. : randorrtized study. Fertil Steril 2006; 85: 1398-1403. Adverse effects reported for ulipristal acetate include ellaOne; ellaOne; Esmya; ellaOne; Esmya; Ger.: ellaOne; Gr.: ellaOne; Hung.: ellaOne; Irl.: ellaOne; 6. Revelli A, et al. Recombinant versus highly-purified, urinary follicle­ abdominal pain and gastrointestinal disturbances, such as stimulating hormone (r-FSH vs. HP-uFSH) in ovulation induction: a Israel: ella; Ital. : ellaOne; Neth.: ellaOne; Esmya; Norw. : nausea and vomiting. Other effects include headache, randorrtized study with cost-minimization analysis. Reprod ellaOne; Esmya; Pol. : ellaOne; Port. : ellaOne; Singapore: ella; dizziness, mood disorders, breast tenderness, myalgia, back 4: 38. Spain: ellaOne; Swed. : ellaOne; UK: eHaOne; Esmya; Ukr.: 7. Pacchiarotti A, et al. Efficacy of a combined protocol of urinary and pain, and fatigue. Less commonly reported effects have Dvella ().jBcnna); USA: ella. recombinant follicle-stimulating hormone used for ovarian stimulation included blurred vision, vertigo, and skin reactions such as of patients undergoing ICSI cycle. J Assist Reprod Genet 2007; 24: 400--5. acne, rash, pruritus, and urticaria. Other adverse effects 8. Baker VL, et al. Clinical efficacy of highly purified urinary FSH versus reported with continuous use include hot flushes, recombinant FSH in volunteers undergoing controlled ovarian stimulation for in vitro fertilization: a randomized, multicenter, functional ovarian cysts that usually disappear sponta­ Urofollitropin !BAN, usAN. rtNN! investigator-blind trial. Fertil Steril 2009; 91: 1005-ll. neously within a few weeks, and a few cases of uterine . haemorrhage in women at risk of excessive bleeding Orofolitropin; · \Jrofolttroprn; · Umfoiitropina; Urofoiitropir ras; associated with uterine fibroids. Increases in blood Urofoilitrophin; Urofollitroptini; Umfol!itropine: Urofo!Jitropi· Adverse Effects and Precautions cholesterol and triglycerides have also been recorded. num; Ypo¢ollnvtrpoliv.H. As for Human Menopausal Gonadotrophins, p. 2284.3.

Dysmenorrhoea is common after a dose of ulipristal CA5 � 97048cLJ-0, acetate for emergency contraception. Menstrual distur­ 8 tc .� G03G;104. bances can also occur and the next menstrual period may Pharmacokinetics ATC Vet - QG03GA04 start several days earlier or later than expected after a single UN!! �. W9BB9SU6HP. After multiple intramuscular or subcutaneous dosing of dose. Endometrial changes and thickening may oCcur in urofollitropin, peak plasma concentrations of follicle­ patients being treated for uterine fibroids. However, these Pharmacopoeias. In Bur. (see p. vii). stimulating hormone occur about 10 hours after a dose changes are different from endometrial hyperplasia and Ph. Eur. 8: (Urofollitropin). A dry preparation containing and the elimination half-life is about 15 or 20 hours reversible after stopping treatment. Endometrial thickening menopausal gonadotrophin obtained from the urine of respectively. that persists 3 months after ulipristal is stopped and postmenopausal wmnen. It has follicle-stimulating activity menstruation has returned should be investigated. and no or virtually no luteinising activity. The potency is not Prepa...... rations... should be excluded before the use of ulipristal less than 90 units of follicle-stimulating hormone per mg; ...... (details are given in Volume B) acetate for emergency contraception. In women being the ratio of units of luteinising hormone to units of follicle­ ProprietaryPreparations treated for fibroids, ulipristal acetate should be started in the stimulating hormone is not more than 1:60. An almost Single-ingredient Preparations. Arg.: Follitrin; Fostimon; Aus­ first week of a menstrual cycle. Although_ continuous white or slightly yellow powder. Soluble in water. Store in tral. : Metrodint; Austria: Bravelle; Fostimon; Belg.: Fostimon; treatment causes anovulation in most patients, a airtight containers at a temperature of 2 degrees to 8 Braz.: Bravelle; Fostimon; Metrodint; Canad.: Bravelle; Chile; non-hormonal method of contraception is recommended. degrees. Protect from light. Follitrin; China: Lishenbao (1#] $�); Cz.: Bravelle; Fostimon;

All cross-references refer to entries in Volume A