Page 960 - Basic _ Clinical Pharmacology ( PDFDrive )
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946     SECTION VIII  Chemotherapeutic Drugs


                 Adverse Reactions, Contraindications,               PREP AR A TIONS
                 & Cautions                                          A V AIL ABLE
                 Pyrantel’s adverse effects are infrequent, mild, and transient.
                 They may include nausea, vomiting, diarrhea, abdominal cramps,   GENERIC NAME       AVAILABLE AS
                 dizziness, drowsiness, headache, insomnia, rash, fever, and weak-  Albendazole  Albenza
                 ness. Pyrantel should be used with caution in patients with liver   Bithionol  Bitin
                 dysfunction, as transient aminotransferase elevations have been   Diethylcarbamazine  Hetrazan
                 noted. Experience with the drug in pregnant women and children   Ivermectin  Mectizan, Stromectol
                 younger than 2 years is limited.                     Mebendazole             Generic, Vermox
                                                                      Metrifonate             Trichlorfon, Bilarcil
                                                                      Niclosamide             Niclocide
                 THIABENDAZOLE                                        Oxamniquine             Vansil, Mansil
                                                                      Oxantel pamoate         Quantrel
                 Thiabendazole is an alternative to ivermectin or albendazole for   Oxantel/pyrantel pamoate  Telopar
                 the treatment of strongyloidiasis and cutaneous larva migrans.  Piperazine   Generic, Vermizine
                                                                      Praziquantel            Biltricide; others outside the USA
                 Basic Pharmacology                                   Pyrantel pamoate        Ascarel, Pamix, Pin Rid, Pin-X
                                                                      Thiabendazole           Mintezol
                 Thiabendazole is a benzimidazole compound. Although it is a
                 chelating agent that forms stable complexes with a number of
                 metals, including iron, it does not bind calcium. Thiabendazole
                 is rapidly absorbed after ingestion. With a standard dose, drug   REFERENCES
                 concentrations in plasma peak within 1–2 hours; the half-life is   Ashrafi K et al: Fascioliasis: A worldwide parasitic disease of importance in travel
                 1.2 hours. The drug is almost completely metabolized in the liver   medicine. Travel Med Infect Dis 2014;12:636.
                 to the 5-hydroxy form; 90% is excreted in the urine in 48 hours,   Bagheri H et al: Adverse drug reactions to anthelmintics. Ann Pharmacother
                                                                         2004;38:383.
                 largely as the glucuronide or sulfonate conjugate. Thiabendazole   Brunetti E, White AC Jr: Cestode infestations: Hydatid disease and cysticercosis.
                 can also be absorbed from the skin. The mechanism of action of   Infect Dis Clin North Am 2012;26:421.
                 thiabendazole is probably the same as that of other benzimidazoles   Colley DG et al: Human schistosomiasis. Lancet 2014;383:2253.
                 (inhibition of microtubule synthesis). The drug has ovicidal effects   Danso-Appiah A et al: Drugs for treating Schistosoma mansoni infection. Cochrane
                 against some parasites.                                 Database Syst Rev 2013;2:CD000528.
                                                                     Debrah AY et al: Doxycycline leads to sterility and enhanced killing of female
                                                                         Onchocerca volvulus worms in an area with persistent microfilaridermia after
                 Clinical Uses                                           repeated ivermectin treatment: A randomized, placebo-controlled, double-
                                                                         blind trial. Clin Infect Dis 2015;61:517.
                 The  standard  dosage,  25  mg/kg  (maximum  1.5  g)  twice  daily,   Del Brutto OH: Clinical management of neurocysticercosis. Expert Rev Neurother
                 should  be  given  after  meals.  Tablets  should  be  chewed.  For   2014;14:389.
                 Strongyloides infection, treatment is for 2 days. Cure rates are   Fox LM: Ivermectin: Uses and impact 20 years on. Curr Opin Infect Dis 2006;
                                                                         19:588.
                 reportedly 93%. A course can be repeated in 1 week if indicated.   Fürst T et al: Manifestation, diagnosis, and management of foodborne trematodiasis.
                 In patients with hyperinfection syndrome, the standard dose is   BMJ 2012;344:e4093.
                 continued twice daily for 5–7 days. For cutaneous larva migrans,   Garcia HH et al: Efficacy of combined antiparasitic therapy with praziquantel and
                 thiabendazole cream can be applied topically, or the oral drug can   albendazole for neurocysticercosis: A double-blind, randomised controlled
                                                                         trial. Lancet Infect Dis 2014;14:687.
                 be given for 2 days (although albendazole is less toxic and there-  Henriquez-Camacho C et al: Ivermectin versus albendazole or thiabenda-
                 fore preferred).                                        zole for  Strongyloides stercoralis infection. Cochrane Database Syst Rev
                                                                         2016:CD007745.
                 Adverse Reactions, Contraindications,               Kappagoda S, Singh U, Blackburn BG: Antiparasitic therapy. Mayo Clin Proc
                                                                         2011;86:561.
                 & Cautions                                          Keiser J, Utzinger J: Efficacy of current drugs against soil-transmitted helminth
                                                                         infections: Systematic review and meta-analysis. JAMA 2008;299:1937.
                 Thiabendazole is much more toxic than other benzimidazoles and   Kincaid L et al: Management of imported cutaneous larva migrans: A case series
                 more toxic than ivermectin, so other agents are now preferred   and mini-review. Travel Med Infect Dis 2015;13:382.
                 for most indications. Common adverse effects include dizziness,   Knopp S et al: Albendazole and mebendazole administered alone or in combina-
                 anorexia, nausea, and vomiting. Less common problems are   tion with ivermectin against Trichuris trichiura: A randomized controlled
                                                                         trial. Clin Infect Dis 2010;51:1420.
                 epigastric pain, abdominal cramps, diarrhea, pruritus, headache,   Knopp S et al: Nematode infections: Filariases. Infect Dis Clin North Am
                 drowsiness, and neuropsychiatric symptoms. Irreversible liver   2012;26:359.
                 failure and fatal Stevens-Johnson syndrome have been reported.   Knopp S et al: Nematode infections: Soil-transmitted helminths and trichinella.
                 Experience with thiabendazole is limited in children weighing less   Infect Dis Clin North Am 2012;26:341.
                 than 15 kg. The drug should not be used in pregnancy or in the   Levecke B et al: Assessment of anthelmintic efficacy of mebendazole in school chil-
                                                                         dren in six countries where soil-transmitted helminths are endemic. PLoS
                 presence of hepatic or renal disease.                   Negl Trop Dis 2014;8:e3204.
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