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Uses and Administration 1894 Gastrointestinal i ..P.r.......epa....................rat ons . Uses and Administration Interactions (details are given Volume B) ProprietaryPreparations in Tropisetron is a 5-HT3 antagonist with an antiemetic action Drugs that induce or inhibit hepatic enzymes may affect similar to that of ondansetron (p. 1872.2). It is used in the plasma concentrations of tropisetron. Licensed product Single-ingredient Preparations. Fr. : Visceralgine; Indon.: Viscer­ algine. prevention of nausea and vomiting induced by cytotoxic information considers that any changes are usually unlikely therapy and in the treatment and prevention of postoper­ to be clinically relevant with the recommended doses. Multi-ingredient Preparations. Belg.: Asodalt: Fr. : Colchimax. ative nausea and vomiting (p. 1811.3). Tropisetron should be used with caution with antiar­ Tropisetron is given as the hydrochloride by slow rhythmics, beta blockers, or drugs likely to prolong the QT intravenous injection or infusion, or orally. Doses are interval, including those likely to cause electrolyte expressed in terms of tropisetron base; 5.64mg of disturbances (see Ondansetron, p. 1874.2). tropisetron hydrochloride is equivalent to about 5 mg of tropisetron base. For the prophylaxis of acute nausea and vomiting Pharmacokinetics associated with cytotoxic chemotherapy a single dose of Tropisetron is well absorbed after oral doses. Peak plasma 5 mg may be given by slow intravenous injection or infusion concentrations occur within 3 hours. Absolute bioavail­ on the day of treatment, shortly before chemotherapy. The ability depends on the dose since first-pass metabolism is injection is given over not less than l minute; it may be saturable. It is 71% bound to plasma proteins. Tropisetron is given into a running infusion. For infusion, it is diluted into metabolised by hydroxylation and conjugation, and IOOmL of a suitable infusion fluid (such as sodium chloride metabolites are excreted mainly in the urine with a small 0.9% or glucose 5%), and given over 15 minutes. amount in the faeces. The cytochrome P450 isoenzyme Subsequent doses of 5 mg daily are given orally, in the CYP2D6 is involved in tropisetron metabolism, and shows morning at least one hour before food, for a further 5 days. genetic polymorphism. The elimination half-life is about 8 Pharmacopoeias. In Jpn. For the treatment of postoperative nausea and vomiting hours in extensive metabolisers and up to 45 hours in poor 2 mg may be given by slow intravenous injection (over not metabolisers. Clearance is also reduced in patients with Profile less than 30 seconds), or by infusion (over 15 minutes), renal impairment. within 2 hours of the end of anaesthesia. For prophylaxis, the Timepidium bromide is a quaternary ammonium same dose may be given shortly before induction of Preparations antirnuscarinic with peripheral actions similar to those of anaesthesia. ..................... ................... (details are given in Volume B) atropine (p. 1312.1). It has been given for the symptomatic For doses in children, see below. ProprietaryPreparations treatment of visceral spasms in usual oral doses of 30 mg Arg.: Austral.: three times daily. It has also been given by subcutaneous, References. Single-ingredient Preparations. Navoban; Navo­ I. Lee CR, et al. Tropisetron: a review of its pharmacodynamic and ban; Austria: Navoban; Belg. : Novaban; Chile: Navobant; intramuscular, and intravenous injection in a dose of pharmacokinetic properties, and therapeutic potential as an antiemetic. China: Di Ou Ping (li1!i!k"F'); Gai Ge En (iili*it.l'!!.); Guang Di (t· 7.5 mg. 46: Drugs 1993; 925-43. Ji!!); He Tai (lU\A); Luo Ting (!l'l'l'); Navoban (Ji.l:Jl,'l'); NiTai­ Urinary metabolites of timepidium may cause a reddish 2. Simpson K, et a!. Tropisetron: an update of its use in the prevention of (til"'-�); 59: Mei Pu Luo Lin ('il!fiiHt); Qi Qiong (:iff/:); Que Zhi coloration of the urine. chemotherapy-induced nausea and vomiting. Drugs 2000; 1297- 1315. Du (lif!z>li); Rui Qi Tai (l'iiilff""-1; Sai Ge En (!fil'll\.\!1); Shu Ji 3. Kranke P, et a!. Tropisetron zur Prophylaxe von Ubeikeit und Erbrechen (�Tl'i);Tuo Li Shi Ning ('li:J'L±'T); Wei Rui Te (iJUiM!I\f); Xin in der postoperativen Phase: eine quantitative systematische Ubersicht. Bei (IV:IJ1);Xin Shun Er (liJ:IIW!!J;); YanDi ('<!JJfi);De nm.: Navo­ Anaesthesist 2002; 51: 805-14. ban; Fr.: Navobant; Ger.: Navobant; Gr. : Navoban; Hong ProprietaryPreparations (details are given in Volume B) Kong: Navoban; Hung.: Navoban; Indon.: Navoban; Setrovel; AdminisiTation in children. Tropisetron hydrochloride is !tal.: Jpn: Malaysia: Mex.: Single-ingredient Preparations. Indon.: Sesden; Jp n: Sesden; Navoban; Navoban; Navoban; Navo­ Singapore: Sesdent. used in children to prevent nausea and vomiting induced ban; Neth.: Novaban; Norw. : Navoban; NZ: Navoban; Philipp. : by cytotoxic chemotherapy; doses are expressed in terms Hensetron; Navoban; Pol. : Navobant; Port.: Navoban; Rus.: of tropisetron base. Children over 2 years of age have Navoban (HaBo6m); Tropindol (TporrHHJ(orr); S.Afr. : Navobant; Spain: Navobant; Saronilt; Swed.: Navoban; Switz. : Navoban; Tiquizium Bromide (p!NNJ been given tropisetron 200 micrograms/kg (maximum dose 5 mg) before chemotherapy, by intravenous injection Thai.: Navobant; Turk. : Navoban; Ukr. : Navoban (HaBo6aH); Venez. : Navoban. Sromurp,·de · tfquiz!{J; f:lS�- oz; qu i<J; over at least 1 minute, or by infusion (at a concentration _ 'J 1lqulzit·. 8�bn\ldum:1i ii bromuro de; Tiquizlpfl). Br�:> riwr" de; T�Xi:\3 MR fipoMwt{. of 50 micrograms/rnL in a suitable infusion fluid, over rran sc3·(DI·2·tbienylm.pthyieneloct�hydro-Scmettlyi-2H-r.ju\, about 15 minutes). In children weighing less than 25 kg · nolizinium brornide. the same dose may be given intravenously once daily for C,"H14BrNS;,"410.4 up to a further 4 days as required. In those weighing more CA S.- 7173i''S.il-'3. than 25 kg, a dose of 5 mg may be given orally once daily for up to a further 5 days; if oral dosage is not possible, UN!/ .,_ 659K6049SF. 5 mg may be given intravenously. Profile Fatigue. Tropisetron has been reported to be of benefit in patients with chronic fatigue, see under Uses and Admin­ Tiquizium bromide is an antimuscarinic with actions similar istration of Ondansetron, p. 1873.1. to those of atropine (p. 1312.1). It is used as an antispasmodic (p. 1803.3) in the treatment of gastro- ' Pain. For reference to the use of tropisetron in various intestinal spasm, biliary tract disease, and urolithiasis; a painful syndromes, see under Uses and Administration of suggested oral dose is 5 to lOmg three times daily. Ondansetron, p. 1873.1. Troxipide is used for its cytoprotective properties in the treatment of gastritis and peptic ulcer disease (p. 1813.2) in Pruritus. Tropisetron and other 5-HT3 antagonists have a usual oral dose of l 00 mg three times daily, after food. Proprietary Preparations (details are given in Volume B) been investigated for the management of pruritus (see under Ondansetron, p. 1873.1). P epo a ic:>ns Single-ingredient Preparations. Jpn: Thiaton. r r _t ........................ Adverse Effects and Precautions ProprietaryPreparations (details are given in Volume B) China: Ke Fen Qi As for Ondansetron, p. 1873.2. Fatigue, abdominal pain, Single-ingredient Preparations. (H:lf�); Shuqi Jpn: Aplace. and diarrhoea may also occur. Visual hallucinations, and an ('iii<�); increase in blood pressure in patients with pre-existing hypertension, have been noted at high repeated doses. ECG changes such as prolongation of QT interval have been noted with high-dose intravenous tropisetron. The drug should therefore be used with caution in patients with cardiac rhythm or conduction disturbances. Care should be taken when driving or operating machinery. No dosage reduction is considered necessary in renal or hepatic impairment despite possible reductions in clearance. Pharmacopoeias. Chin. includes monographs for recombi­ nant human epidermal growth factor suitable for external Tropisetron Hydrochloride (BANM. r!NNMJ Carcinogenicity. The manufacturer (Novartis, UK) has reported an increased incidence of hepatic neoplasms in Hidrocloruro ICS-20 rropisetron; 1 .: de. �ropisetr6n;. 5-930; male mice given high doses of tropisetron but it is sug­ Chlorhydrate de; Tropisetr6Q. hklrocloturo Trppls�?tron­ de; gested that these effects are both species and sex specific. hydrochlorid; Tropisetroni hydrochlorldurn; Tpor. u.JceTpoHa Urogastrone is a polypeptide first isolated from human \V.APOY J10j)Y1/\. Effects on the cardiovascular system. For a discussion of urine. Two forms have been identified, p and y urogastrone. The p form consists of 53 amino acids and is distinguishable C .,H7,,N20,,HCI.i320.8 the effects of 5-HT3 antagonists on the cardiovascular sys­ CA S ..,..- 105826 J;I2 ·4. tem, see under Ondansetron, p. 1873.3. from the y form by an additional terminal arginine residue. ATC -� A04AAD3. The p form is reported to be identical to human epidermal AtC \let ..:., QAQ411AD3. Porphyria. The Drug Database for Acute Porphyria, com­ growth factor and this tenm is widely used in the literature. piled by the Norwegian Porphyria Centre (NAPOS) and Urogastrone inhibits gastric acid secretion and has been UN!! �- A 7 93 38();?YO. the Porphyria Centre Sweden, classifies tropisetron as tried in the treatment of peptic ulcer disease and other In Bur. (see p. vii). Pharmacopoeias. probably not porphyrinogenic; it may be used as a drug of gastrointestinal disorders but its rapid destruction in the Ph. Bur. 8: (Tropisetron Hydrochloride). A white or almost first choice and no precautions are needed.' stomach has limited its clinical use. white powder. Freely soluble or soluble in water; sparingly l. The Drug Database for Acute Porphyria. Available at: http://www. It is a potent stimulator of cellular proliferation and has soluble in alcohol; very slightly soluble in dichloromethane. drugs-porphyria.org (accessed 07110111) also been used as an aid to wound healing. All cross-references refer to entries in Volume A .
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