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Trihexyphenidyl Hydrochloride/Tropatepine Hydrochloride 821

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Trihexyphenidyl Hydrochloride/Tropatepine Hydrochloride 821 Trihexyphenidyl Hydrochloride/Tropatepine Hydrochloride 821 (p.1220). It also has a direct antispasmodic action on levodopa, but the dose of each drug may need to be Tropatepine Hydrochloride (rINNM) smooth muscle. reduced. Trihexyphenidyl hydrochloride 3 to 6 mg dai- Hidrocloruro de tropatepina; SD-1248-17; Tropatépine, Chlo- Trihexyphenidyl hydrochloride is given orally in the ly is usually adequate. rhydrate de; Tropatepini Hydrochloridum. 3-(Dibenzo[b,e]thie- symptomatic treatment of parkinsonism (p.791), in- pin-11(6H)-ylidene)tropane hydrochloride. cluding the alleviation of the extrapyramidal syndrome Extrapyramidal disorders. Antimuscarinics such as trihexy- Тропатепина Гидрохлорид induced by drugs such as phenothiazines, but, like oth- phenidyl are used in the management of dystonias (p.809) al- C22H23NS,HCl = 370.0. though only about half of all children and adolescents, and fewer CAS — 27574-24-9 (tropatepine); 27574-25-0 er antimuscarinics, is of no value against tardive dysk- adults (who tolerate antimuscarinics less well) show any re- (tropatepine hydrochloride). inesias. It has been used in the treatment of dystonias, sponse. Adverse effects may be limited by starting with a low ATC — N04AA12. ATC Vet — QN04AA12. but see Extrapyramidal Disorders, below. Trihexyphe- dose: one suggested regimen1 starts with trihexyphenidyl 1 mg nidyl hydrochloride is given in 3 or 4 divided doses daily and rises up to 12 mg daily over the next 4 to 6 weeks; some patients may require up to 60 to 100 mg daily. The BNFC sug- daily before or with food. CH3 gests that children aged 1 month to 18 years may be given oral N In Parkinson’s disease the usual initial dose of 1 mg doses of 1 to 2 mg daily in 1 or 2 divided doses, adjusted accord- daily is gradually increased at intervals of 3 to 5 days ing to response. by increments of 2 mg to 6 to 10 mg daily according to response; for advanced cases, 12 to 15 mg daily or 1. Jankovic J. Dystonia: medical therapy and botulinum toxin. Adv even more (up to 20 mg daily) may be needed. As a Neurol 2004; 94: 275–86. rule, postencephalitic patients tolerate and require the Preparations larger doses. Usual doses for drug-induced extrapyramidal BP 2008: Trihexyphenidyl Tablets; USP 31: Trihexyphenidyl Hydrochloride Elixir; Trihexyphenidyl Hydrochlo- S symptoms lie within the range of 5 to 15 mg daily, al- ride Extended-release Capsules; Trihexyphenidyl Hydrochloride Tablets. though as little as 1 mg daily may be sufficient in some (tropatepine) cases. Proprietary Preparations (details are given in Part 3) Since the elderly and arteriosclerotic patients are more Arg.: Artane; Austral.: Artane; Austria: Artane; Belg.: Artane; Braz.: Ar- Profile susceptible to the adverse effects of antimuscarinics a tane; Triexidyl; Canad.: Apo-Trihex; Chile: Artane†; Tenvatil; Tonaril; Tropatepine hydrochloride is an antimuscarinic with actions and dose at the lower end of the range is usually recom- Denm.: Peragit; Fr.: Artane; Parkinane; Ger.: Artane; Parkopan; Gr.: Ar- uses similar to those of trihexyphenidyl (p.820). It is used in the tane; Hong Kong: Apo-Trihex; Artandyl; Artane; India: Pacitane; Parnon; management of parkinsonism (p.791), including the alleviation mended. Indon.: Arkine; Artane; Hexymer; Irl.: Artane†; Israel: Artane†; Partane; Rodenal; Ital.: Artane; Malaysia: Aca; Apo-Trihex; Uphazhexol†; Mex.: of the extrapyramidal syndrome induced by drugs such as phe- Antimuscarinic treatment of parkinsonism should Artane†; Hipokinon; Kexidil; Neth.: Artane; Pol.: Parkopan; Port.: Artane; nothiazines, but, like other antimuscarinics, is of no value in tar- never be terminated suddenly and it is usual when S.Afr.: Artane; Singapore: Apo-Trihex; Beahexol; Spain: Artane; Swed.: dive dyskinesias. Tropatepine hydrochloride is given orally in Pargitan; Thai.: Aca; Acamed; Artane†; Pozhexol; Tridyl; UK: Broflex; USA: usual doses of 10 to 30 mg daily; it is also given intramuscularly changing from one drug to another to withdraw one in Trihexy. or by slow intravenous injection in doses of 10 to 20 mg daily. small amounts while gradually increasing the dose of Preparations the other. Multi-ingredient: Ger.: Spasman†; India: Sycot; Trinicalm Forte; Trini- calm Plus; Spain: Largatrex†. Proprietary Preparations (details are given in Part 3) Trihexyphenidyl hydrochloride may be given with oth- Fr.: Lepticur. er drugs used for the relief of parkinsonism, such as The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii) 828 Antiprotozoals 4. Viotti R, et al. Treatment of chronic Chagas’ disease with benz- Pentavalent Antimony patients with leishmaniasis.1 ECG abnormalities developed dur- nidazole: clinical and serologic evolution of patients with long- ing 35 treatment courses. They were qualitatively similar to those term follow-up. Am Heart J 1994; 127: 151–62. Compounds previously described during treatment with trivalent antimonial 5. Bern C, et al. Evaluation and treatment of Chagas disease in the Antimonio pentavalente, compuestos de. drugs, but occurred less frequently and later during the course of United States: a systematic review. JAMA 2007; 298: 2171–81. treatment. The most common abnormality was inversion and/or 6. Gallerano RH, et al. Therapeutic efficacy of allopurinol in pa- decreased amplitude of T waves. Incidence was related to total tients with chronic Chagas’ disease. Am J Trop Med Hyg 1990; Meglumine Antimonate 43: 159–66. daily dose and duration of treatment. One patient died suddenly 7. Apt W, et al. Treatment of chronic Chagas’ disease with itraco- Antimoniato de meglumina; Antimony Meglumine; Meglumine during the 4th week of treatment with antimony 60 mg/kg daily. nazole and allopurinol. Am J Trop Med Hyg 1998; 59: 133–8. Antimoniate; Protostib; RP-2168. 1-Deoxy-1-methylamino-D- Other deaths probably related to cardiac toxicity have been re- glucitol antimonate. ported in patients receiving 60 mg/kg daily2 and 30 mg/kg daily.3 8. Apt W, et al. Itraconazole or allopurinol in the treatment of 1 chronic American trypanosomiasis: the regression and preven- Меглумина Антимонат It has been recommended that for treatment with sodium sti- tion of electrocardiographic abnormalities during 9 years of fol- bogluconate ECGs should be obtained every 3 to 4 days in pa- low-up. Ann Trop Med Parasitol 2003; 97: 23–9. C7H18NO8Sb = 366.0. CAS — 133-51-7. tients given antimony 20 mg/kg daily for more than 20 days or a ATC — P01CB01. higher dose for more than 10 days. If Stokes-Adams attacks or ATC Vet — QP51AB01. ventricular tachyarrhythmias develop, sodium stibogluconate should be stopped and appropriate treatment given. A retrospec- Acetarsol (BAN, rINN) tive study4 in patients treated with sodium stibogluconate for Sodium Stibogluconate (BAN, rINN) mostly cutaneous leishmaniasis found that the mean QTc interval Acetaminohydroxyphenylarsonsäure; Acétarsol; Acetarsolum; Estibogluconato de sodio; Natrii Stibogluconas; Natriumstiboglu- Acetarsone; Acetphenarsinum; Asetarsoli; Osarsolum. 3-Aceta- steadily increased throughout the period of treatment, reaching a konaatti; Natriumstiboglukonat; Sod. Stibogluc.; Sodium Antimo- potentially toxic threshold by the third week, but cardiotoxicity mido-4-hydroxyphenylarsonic acid. ny Gluconate; Sodyum Stiboglukonat; Stibogluconate de Sodium; was seen only in one elderly patient who had hypokalaemia and Ацетарсол Stibogluconat-Natrium. pre-existing cardiovascular morbidity. Identification before C H AsNO = 275.1. Натрия Стибоглюконат treatment of factors that may increase cardiovascular risk is im- 8 10 5 portant. CAS — 97-44-9. CAS — 16037-91-5. 1. Chulay JD, et al. Electrocardiographic changes during treatment ATC — A07AX02; G01AB01; P01CD02. ATC — P01CB02. ATC Vet — QP51AB02. of leishmaniasis with pentavalent antimony (sodium stibogluco- ATC Vet — QA07AX02; QG01AB01; QP51AD05. nate). Am J Trop Med Hyg 1985; 34: 702–9. Description. A pentavalent antimony compound of indefinite 2. Bryceson ADM, et al. Visceral leishmaniasis unresponsive to an- composition. It has been represented by the formula timonial drugs II: response to high dosage sodium stibogluco- nate or prolonged treatment with pentamidine. Trans R Soc Trop C6H9Na2O9Sb but usually there are less than 2 atoms of Na for OH Med Hyg 1985; 79: 705–14. O each atom of Sb. Solutions may be sterilised by autoclaving. HO 3. Thakur CP. Harmful effect of high stibogluconate treatment of Pharmacopoeias. In Br., Chin., Int., and It. kala-azar in India. Trans R Soc Trop Med Hyg 1986; 80: 672–3. HO BP 2008 (Sodium Stibogluconate). It is mainly the disodium salt 4. Lawn SD, et al. Electrocardiographic and biochemical adverse As N CH3 2 3 4 H of μ-oxy-bis[gluconato(3-)O ,O ,O -hydroxo-antimony]. It con- effects of sodium stibogluconate during treatment of cutaneous tains not less than 30.0% and not more than 34.0% of antimo- and mucosal leishmaniasis among returned travellers. Trans R O ny(V), calculated with reference to the dried and methanol-free Soc Trop Med Hyg 2006; 100: 264–9. substance. It is a colourless, odourless or almost odourless, most- Effects on the kidneys. Sodium stibogluconate given for 10 Profile ly amorphous powder. Very soluble in water; practically insolu- days to 16 young men with cutaneous leishmaniasis had no ap- Acetarsol, a pentavalent organic arsenical derivative, was for- ble in alcohol and in ether. A solution in water containing 10% of parent adverse effect on glomerular or tubular renal function.1 merly given orally in the treatment of intestinal amoebiasis and pentavalent antimony has a pH of 5.0 to 5.6 after autoclaving. However, evidence of renal tubular dysfunction has been report- vaginally in the treatment of trichomoniasis, but the use of pen- ed in patients with mucocutaneous leishmaniasis given meglu- tavalent arsenical compounds has been abandoned in favour of Adverse Effects, Treatment, and Precau- mine antimonate or sodium stibogluconate for 30 days or more2 more effective and less toxic drugs. For the adverse effects of tions and acute renal failure has occurred in patients both with,3 and arsenic and their treatment, see Arsenic Trioxide, p.2260.
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