Definition
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.
Description
A dideoxynucleoside compound in which the 3'-hydroxyl group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of 5' to 3' phosphodiester linkages, which are needed for the elongation of DNA chains, thus resulting in the termination of viral DNA growth. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Route of Elimination: Renal excretion of unchanged drug appears to be the primary route of elimination, accounting for approximately 80% of an intravenous dose and 60% of an orally administered dose within 24 hours after dosing (n=19). Renal clearance exceeds glomerular filtration rate suggesting renal tubular secretion contributes to the elimination of zalcitabine by the kidneys. Half Life: 2 hours
- Uses/Sources: For the treatment of Human immunovirus (HIV) infections in conjunction with other antivirals.
- Route of Exposure: Bioavailability is over 80% following oral administration.
Toxicity
- Carcinogenicity: 2B, possibly carcinogenic to humans. (L135)
- Toxicity: Acute overdose: Inadvertent pediatric overdoses have occurred with doses up to 1.5 mg/kg zalcitabine. Chronic overdose: in an initial dose-finding study in which zalcitabine was administered at doses 25 times (0.25 mg/kg every 8 hours) the currently recommended dose, one patient discontinued zalcitabine after 1.5 weeks of treatment subsequent to the development of a rash and fever.
Zalcitabine Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
HIV Infections | 9.62 |
|
Schizophrenia | 7.71 |
|
Glomerulonephritis | 7.68 |
|
Astrocytoma | 7.46 |
|
Epilepsy, Temporal Lobe | 7.28 |
|
Heart Valve Diseases | 6.71 |
|
Diabetes Mellitus, Type 1 | 6.68 |
|
Epilepsy | 6.51 |
|
Histiocytosis, Sinus | 6.49 |
|
Histiocytosis with joint contractures and sensorineural deafness | 6.49 |
|
Spastic paraplegia 10, autosomal dominant | 6.49 |
|
Brain Injuries | 6.42 |
|
Alcohol dependence | 6.38 |
|
Vesicoureteral Reflux 2 | 6.38 |
|
Calcinosis | 6.35 |
|
Chronic obstructive pulmonary disease | 6.35 |
|
Influenza, Human | 6.33 |
|
Angiokeratoma | 6.29 |
|
Neuroblastoma | 6.29 |
|
Crohn's disease | 6.27 |
|