Albendazole Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R61:Kann das Kind im Mutterleib schädigen.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Chemische Eigenschaften
Albendazole occurs as a white to faintly yellowish powder. It is practically insoluble in water and alcohol, very slightly soluble in ether and dichloromethane, but freely soluble in anhydrous formic acid.
Verwenden
Albendazole is a derivative of benzimidazole, is a drug with a broad antihelmintic spectrum. It exhibits an antihelmintic effect against sensitive cestodes and nematodes by blocking the process of glucose uptake by the parasites, which is expressed in the depletion of glycogen reserves and subsequent reduction in the level of adenosintriphophate. As a result, the parasite stops moving and dies. It is used upon infection of Acaris lumbricoides, Ancylostoma duodenale, Necator americanus, Enterobius vermicularis, and Trichuris trichiura. Synonyms of this drug are SKF 62979 and others.
Indications
Albendazole appears to cause cytoplasmic microtubular
degeneration, which in turn impairs vital cellular
processes and leads to parasite death.There is some evidence
that the drug also inhibits helminth-specific ATP
generation by fumarate reductase.
Antimicrobial activity
Albendazole is active against trichostrongyles
and exhibits useful activity against tissue-dwelling larvae
of Trichinella spiralis, larvae of animal hookworms (causing
cutaneous larva migrans) and microfilariae of various filarial
species. It also exhibits some activity against cysticercosis and
hydatid stages of Echinococcus granulosus and Echinococcus
multilocularis. It has been successfully used in infections with
the protozoon Giardia lamblia and for microsporidiosis.
Allgemeine Beschreibung
Albendazole occurs as a white crystalline powder that isvirtually insoluble in water. The oral absorption of albendazoleis enhanced by a fatty meal. The drug undergoes rapidand extensive first-pass metabolism to the sulfoxide, whichis the active form in plasma. The elimination half-life ofthe sulfoxide ranges from 10 to 15 hours. Considerable biliaryexcretion and enterohepatic recycling of albendazolesulfoxide occurs. Albendazole is generally well toleratedin single-dose therapy for intestinal nematodes. The highdose,prolonged therapy required for clonorchiasis orechinococcal disease therapy can result in adverse effectssuch as bone marrow depression, elevation of hepatic enzymes,and alopecia.
Mechanism of action
Albendazole is given orally and is poorly and variably
absorbed (5%) because of its poor water solubility.
Oral bioavailability is increased as much as five
times when the drug is given with a fatty meal instead of
on an empty stomach. Concurrent treatment with corticosteroids
increases plasma concentrations of albendazole.
The drug is rapidly metabolized in the liver to an
active sulfoxide metabolite.The half life of the metabolites
is 8 to 12 hours.
Pharmakokinetik
Albendazole is better absorbed after oral absorption than
other benzimidazole carbamates. It is extensively metabolized
to the anthelmintically active albendazole sulfoxide,
producing plasma concentrations of the metabolite
of about 1.3 mg/L 2–5 h after a 400 mg oral dose. The
half-life is about 8 h and the major route of excretion is
via the bile. Plasma protein binding of the sulfoxide is
around 70%.
Clinical Use
Albendazole has a broad spectrum of activity against intestinal nematodes and cestodes, as well as the liver flukes Opisthorchis sinensis, Opisthorchis viverrini, and Clonorchis sinensis. It also has been used successfully against Giardia lamblia. It is widely used throughout the world for the treatment of intestinalnematode infection. It is effective as a single-dose treatmentfor ascariasis, New and Old World hookworm infections,and trichuriasis. Multiple-dose therapy with albendazole caneradicate pinworm, threadworm, capillariasis, clonorchiasis,and hydatid disease. The effectiveness of albendazole againsttapeworms (cestodes) is generally more variable and lessimpressive. It also is effective in treating cerebral and spinal neurocysticercosis, particularly when given with dexamethasone.Albendazole is recommended for treatment of gnathostomiasis.
Nebenwirkungen
Various mild intestinal and other upsets usually resolve
without treatment. With extended use, as for larval tapeworm
infections, hepatic abnormalities or leukopenia may
require discontinuation of treatment. In rare cases granulocytopenia,
pancytopenia, agranulocytosis or thrombocytopenia
may occur. It should not be given during pregnancy
since it may cause fetal harm; women should be cautioned
against becoming pregnant within a month of completing
treatment.
Albendazole Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
