151
2. Davis A, et a!. Multicentre clinical trials of benzimidazolecarbamates in cyst fluid when albendazole was given with cimetidine, Dipo SsiLim. 'bis{!1-[2,3-0ihydroxyt>uta�edi�Hartrato coccosis.1 ' · Breast feeding. The results of a study1 in 33 women given (4-)]diaritimon�e(2-) trihydrate. l. Wen H, et al. Initial observation on albendazole in combination with Csfi,t<,b,jSb,JH,'Q=66/9 ·. . a single oral 400-mg dose of albcndazolc suggested that cimetidine for the treatment of human cystic echinococcosis. Ann Trop albendazole and its active metabolite attained low concen Med Parasitol 1994; 88: 49-52. .• antimony trations in breast milk. The authors considered that CAS - 1107J-15cl ionhydrou.spotassium potassiumtrihydrateJ, t<:frtra te); albendazole was unlikely to be harmful to breast-fed !an timony tartrate Pharmacokinetics ·- . infants. UNIJ DU50Z416V3 tract is Pharmacopoeias. In US. I. Abdel·tawab AM et al. Albendazole and its metabolites in the breast Absorption of albendazole from the gastrointestinal , milk of lactating women following a single oral dose of albendazole. Br J poor but may be enhanced by a fatty meal. Albendazole USP 36: (Antimony Potassium Tartrate). Odourless, Clin Phannacol 2009; 68: 737-42. rapidly undergoes extensive first-pass metabolism. Its colourless, transparent crystals or white powder. The principal metabolite albendazole sulfoxide has anthelmintic crystals effloresce on exposure to air and do not readily Effects on growth. A multiple-dose regimen of albend activity and a plasma half-life of about 8.5 hours. rehydrate even on exposure to high humidity. Soluble 1 in azole in children with asymptomatic trichuriasis has been Albendazole sulfoxide is widely distributed throughout the 12 of water, I in 3 of boiling water, and 1 in 15 of glycerol; reported to be associated with impaired growth in those body including into the bile and the CSF. It is about 70% insoluble in alcohol. Its solutions are acid to litmus. with low levels of infection.1 However it was considered bound to plasma protein. Albendazole sulfoxide is 1 that this should not prevent the use of single doses in eliminated in the bile; only a small amount appears to be Antimony Sodium Tartrate mass treatment programmes. 2 excreted in the urine. 1. Forrester JE, et al. Randomised trial of albendazole and pyrantel in Antim. Sod. !art; s.P ic.o, t�!trato; Sodium References. Anttmor1ico. ? symptomless trichuriasis in children. Lancet 1998; 352: 1103-8. 1. Marriner SE, et a!. Pharmacokinetics of albendazole in man. Bur .l Clin Antirnonylt'di)Jate; Stibium Natrium Tartaric.um; 2. Winstanley P. Albendazole for mass treatment of asymptomatic trichuris Pharmacol 1986; 30: 705-8. Tap.;.pa:t Ha'q)wl!. , AHTMMOHWJ· infections. Lancet 1998; 352: 1080-l. · . • ...... :· 2. Morris DL, et al. Penetration of albendazole sulphoxide into hydatid Disodium blS(!l·[2,3-dihydroxybutanedio.ato(4-)-a'.o'.:d', OjJ cysts. Gut 1987; 28: 75-80. 3. Steiger U, et a!. Albendazole treatment of echinococcosis in humans: diantir;r:tor\ate\2-l; . Dbos:fiurn · bis{l-!·fl3+Hartrato(4-j]jdiantl- Effects on theliver. In a series of 40 patients given albend · azole for echinococcosis, 7 developed abnormalities in effects on microsomal metabolism and drug tolerance. Clin Phannacol rnonatt:(2c)o liver function tests during therapy.' Six had a hepatocellu Ther 1990; 47: 347-53. 4. Jung H, et al. Clinical pharmacokinetics of albendazole in patients with lar type of abnormality attributable to albendazole; the brain cysticercosis. J Clin Pharmacal 1992; 32: 28-31. C"H.�Na-'- ,Oi,Sb'2;=581,6 seventh had cholestatic jaundice which was probably not 5. Jung H, et a!. Clinical pharmacokinetics of albendazole in children with CAS 3452HJ9cfl. : due to albendazole. See also Incidence of Adverse Effects, neurocysticercosis. Am J Ther 1997; 4: 23-6. UN!/ _;;3KUtO£P4fjL; 6. Dayan AD. Albendazole, mebendazole and praziquantel: review of Pharmacopoeias. In Int. (as C.JI Na0 Sb 308.8) and US. p. 150.3 for reports of raised serun1-transaminase levels. 4 7 = non-clinical toxicity and pharmacokinetics. Acta Trop 2003; 86: 141-59. Albendazole should only be used in the treatment of USP 36: (Antimony Sodium Tartrate). Odourless, colour echinococcosis if there is constant medical supervision with less, transparent crystals or white powder. The crystals regular monitoring of serum-transaminase concentrations effloresce on exposure to air. Freely soluble in water; and of leucocyte and platelet counts. Patients with liver ProprietaryPreparations (details are given in Volume B) insoluble in alcohol. damage should be treated with reduced doses of Single-ingredient Preparations.Arg.: Vastus; Vermizole; Austral.: benzimidazole carbamates, if at all.' Eskazole; Zentel; Austria: Eskazole; Braz. : Alba-3; Albel; Sodium Stibocaptate (BAN. r!NN! l. Morris DL, Smith PG. Albendazole in hydatid disease-hepatocellular Albendrox; Albendy; Albentel; Albenzonil; Albezin; Alin; Ben toxicity. Trans R Soc Trop Med Hyg 1987; 81: 343-4. zol; Imavermilt; Mebenix; Monozol; Neo Bendazol; Parasin; Antimony· Dimer�apt0sw:<::inate; Estibocaprato de 2. Davis A, et al. Multicentre clinical trials of benzimidazolecarbamates in Parazol; Vermiclase; Vermital; Zentel; Zolben; Chile: Ceprazolt; sodio; Natriisodiurn Stlbo;ca • pta$; 1544/6;' Sb-58; Stiboc<:!ptate; human cystic echinococcosis (phase 2). Bull "WHO 1989; 67: 503-8. Vermoil; Zemel; China: Abentel Zentel Cz.: Stiboc'aotate de Sodium; Ro·+ Haipv!)'l. <:;1 kf6ol$mar. Zentelt; Fr.: Eskazole; Zentel; Ger.: Eskazole; Gr.: Albendol; Antimony sodium · tl9eso-2'l'Wiib/6;,3·dimek aptbsucc1nate. The Pregnancy. Albendazole is teratogenic in some animals ('iJJ.lH\c); (ll!ii1ll'/i'); Eskazole; Zemel; India: ABD; Abide; ABZ; Abzole; AH AI; 806.1 and there are no adequate and well controlled studies in for mul�.· './aries hom �··G:,,I:tfil\li>0\'"S."Sl:l1 "' to Albacos; Albamaa; Albasym; Albazole; Albekon; Albendol;-I; C:zH;Na,01 �t\Sb2 human pregnancy. Albendazole is therefore usually Albent; Albenzole; Albesan; Albest; Albestar; Albex; Albezole; contra-Indicated during pregnancy and US licensed pro 0\5 =:(C9>�.0 ,;Hi}lai!iuS� Sth}. Albol; Albosym; Alboven; Albrodo; Alenda; Alia; Alrrtinth; 3 duct information cautions against becoming pregnant Altec; Alworm; Alzad; Alzol; Anthel; Antiworm; Ariban; Asi _;; 064"6 r 'l ' . . while taking albendazole or within one month of complet bend; Atbend; Aviband; Avizole; Band; Bandy; Banthel; Bend ON!! '- lJFV4 iJIJLHiO, • ing treatment. ex; Bendol; Benrod; Benzys; Biwom; C-Band; C-Bend; C-Trop; Stibophen For reference to a study of women given albendazole Cidazole; Combantrin-A; Conthel; Cuwarm; Dazo; Dispel; E with ivermectin during the second trimester of pregnancy, Bend; Ebex; Ejectil; Elbend; Eleben; Elminex; Emanthalt; Estibofeno; Foua(jin;Stlbophenum; see p. 158.2. Enbenol; Foben; Gekare; Getrid; Janbol; Kiraza; Lupibend; alsl4.5-dthydroxybenzel')ec1, 3-cl!sufphonaCilri�H.t6(4-)'0" ,0:)a11ti· Milibend; Morband; N-Bend; NBWorm; Nemaban; Nemofex; monate(5-) pen.t�SQdiut:nheptahxdrleishmaniasis until the advent of sulfoxide were increased by about 260 and 360% respec Adazol; Alzel; Benzol; Zentel; Pol.: Zentel; Port.: Zentel; Rus.: the less toxic pentavalent compounds. They continued to be tively, albendazole sulfone by some 190%, and (-)-(R) Nemozole (HeMo3on); Sanoxal (CaHoKcan); S.Afr. : Bendex; Wor used in the treatment of schistosomiasis, but have now been praziquantel by about 65%, when albendazole and prazi madole; Zentel; Singapore: Albendol; Alzental; Zentel; Spain: superseded by less toxic and more easily given drugs such as quantel were given together. Although this raised the pos Eskazole; Switz.: Zentel; Thai.: Abentelt; Albatel; Alben-Hero; praziquantel. sibility of increased efficacy from the combination, the Alben-VC; Alben; Albenda; Albenz; Albezol; Aida; Aldazole; Antimony sodium tartrate was formerly used as an magnitude of the changes suggested that increased adverse Alfuca; Alzol; Anthedat; Benyad; CB-400; Falben; Fate!; Gen emetic. The sodium tartrate and potassium tartrate have effects might be a problem, and dose adjustment might be dazel; Labenda; Leo-400t; Manozide; Mesin; Mycotelt; Proda also been used as expectorants. needed.2 zole; San-San; Vermixide; Vetoben; Zeben; Zela; Zentel; Zen 1. Homeida M, et al. Pharmacokinetic interaction between praziquantel zera; Turk. : Andazol; UAB: Albenda; Ukr.: Aldazole and albendazole in Sudanese men. Ann Trop Med Parasitol 1994; 88: 551- (AJJbJI.a30IJ); Vormil (BopMHJI); Zentel (3eHTen); USA: Albenza; Adverse Effects and Treatment 9. Venez. : Albezol; Albicar; Bevindazol; Helal; Sostril; Taron; Ven 2. Lima RM, et a!. Albendazole-praziquantel interaction in healthy dazol; Zentel. Trivalent antimony compounds are more toxic than volunteers: kinetic disposition, metabolism and enantioselectivity. Br J pentavalent antimonials such as sodium stibogluconate, Clin Pharmacal 2011; 71: 528-35. Multi-ingredientPreparafions. India: Ablaze-1M; ABZ Plus; Alba possibly because they are excreted much more slowly. The cos-IR; Albosym-IR; Alvect; Authel-UP; Ariban Plus; Ascapil A; most serious adverse effects are on the heart and liver. There Antiepileptics. Phenytoin, carbamazepine, and phenobarbital Bandy Plus; Benrod-I; Benzole; D-Worm; Ectin-A; Elect-A; are invariably ECG changes during treatment, but hypo appear to induce the oxidative metabolism of albendazole Elminova; Eradix; Eris Plus; Getrid-I; Hymin Plus; Hymin; tension, bradycardia, and cardiac arrhythmias are more Imectin Forte; Ivecop-AB; Ivercid-A; Iverzole; Ivoral; Kaybend; via the cytochrome P450 isoenzyme CYP3A by roughly serious. Sudden death or cardiovascular collapse may occur Kidi; Machi Plus; Networm; Mex. : C Cobistal; Farmiver; Oxal; the same extent, resulting in significantly reduced concen at any time. Elevated liver enzyme values are common; liver Thai.: Albemed. trations of albendazole sulfoxide. This interaction is likely damage with hepatic failure and death is more likely in to be clinically significant when albendazole is used to Pharmacopoeial Preparafions patients with pre-existing hepatic disease. treat systemic worm infections, and increased doses of USP 36: Albendazole Tablets. Adverse effects immediately after intravenous use of 1 albendazole would be needed The interaction is probably trivalent antirnonials, in particular the tartrates, have not clinically significant when albendazole is used for included coughing, chest pain, pain in the arms, vomiting, intestinal worm infections. Trivalent Antimony Compounds abdominal pain, fainting, and collapse, especially after rapid l. Lanchote VL, et al. Pharmacokinetic interaction between albendazole injection. Extravasation during injection is extremely sulfoxide enantiomers and antiepileptic drugs in patients with Compuestos antimpnio rrivalente; Tpexea(let