Zalcitabine Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R40:Verdacht auf krebserzeugende Wirkung.
R36/37:Reizt die Augen und die Atmungsorgane.
R34:Verursacht Verätzungen.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S27:Beschmutzte, getränkte Kleidung sofort ausziehen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
Zalcitabine is an orally active dideoxynucleoside andog for combination use with
zidovudine in advanced HIV infection and also as monotherapy for AIDS patients who
cannot tolerate or have not responded to zidovudine. It has a similar mechanism of
action (inhibition of reverse transcriptase) to didanosine. Like didanosine, its side effect profile includes peripheral neuropathy. Unlike
zidovudine, zalcitabine does not cause bone marrow suppression.
Chemische Eigenschaften
White to Off-White Cyrstalline Powder
Definition
ChEBI: A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.
Indications
Zalcitabine (ddC, Hivid) is a cytidine analogue active
against HIV-1, HIV-2, and hepatitis B virus. It is used
for the treatment of HIV infection in adults and asymptomatic
children as part of a multidrug regimen. It may
be less effective than the other nucleoside inhibitors
and is used less frequently.
Allgemeine Beschreibung
Zalcitabine, 2',3'-dideoxycytidine or ddCyd, is an analog ofcytosine that demonstrates activity against HIV-1 and HIV-2,including strains resistant to AZT. The potency (in peripheralblood mononuclear cells) is similar to that of AZT, but thedrug is more active in populations of monocytes andmacrophages as well as in resting cells.
The oral bioavailability of zalcitabine is over 80% in adultsand less in children.The major dose-limiting side effect isperipheral neuropathy, characterized by pain, paresthesias,and hypesthesia, beginning in the distal lower extremities.These side effects are typically evident after several months oftherapy with zalcitabine. A potentially fatal pancreatitis is anothertoxic effect of treatment with ddC. The drug has beenapproved for the treatment of HIV infection in adults with advanceddisease who are intolerant to AZT or who have diseaseprogression while receiving AZT. ddC is combined with AZTfor the treatment of advanced HIV infection.
Air & Water Reaktionen
Water soluble.
Reaktivität anzeigen
Zalcitabine may be sensitive to prolonged exposure to light.
Brandgefahr
Flash point data for Zalcitabine are not available; however, Zalcitabine is probably combustible.
Pharmakologie
Peripheral neuropathy occurs in up to 50% of patients
taking zalcitabine. Stomatitis, esophageal ulceration,
hepatotoxicity, rash, and pancreatitis may occur.
Zalcitabine should be used with caution in individuals
with a history of pancreatitis, liver disease, or alcohol
abuse. Dosage adjustment is necessary for individuals
with renal impairment. Zalcitabine should not be used in
combination with didanosine, lamivudine, or stavudine.
Pharmakokinetik
Zalcitabine (ddC) is a useful alternate drug to ZDV and is given in combination with ZDV when CD4 cell counts fall to less than 300 cells/mm3 . Monotherapy with ddC is more active than ZDV. Its oral bioavailability is 87%, and its plasma half-life is approximately 1 hour.
In low doses (0.005 mg/kg every 4 hours), ddC produces sustained decrease in p24 antigen level and increase in CD4 cell counts. The CSF fluid/plasma ratio of ddC is 0.2. Following oral administration, bioavailability of ddC is less than 80%, which is further reduced when taken with food. The mean maximum plasma concentration of the drug also is reduced from 25.2 to 15.5 ng/mL when the drug was taken with food.
Nebenwirkungen
It has side effects, such as stomatitis, rash, fever, malaise, arthritis, and arthralgia.
Stoffwechsel
Dideoxyuridine is the major metabolite in urine and feces. The drug penetrates the blood-brain barrier. The major toxicity of ddC is peripheral neuropathy, in which case it should be discontinued. In some cases, pancreatitis occurs when given alone or in combination with ZDV."
Zalcitabine Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
