Zalcitabine is an antiretroviral. Antiretrovirals are medications which suppress the activity or replication of retroviruses like HIV. It is a member of some type of medications known as reverse transcriptase inhibitors.
This particular antiviral is categorized as a nucleoside reverse transcriptase inhibitor, which means it blocks the enzyme that’s important for the retrovirus to multiply.
It is suggested in combination with antiretroviral agents for treating HIV disease. It’s utilized as part of a combination program with antiretroviral agents. Nevertheless, it was stopped by Roche Pharmaceuticals on December 31, 2006 because of the availability of newer HIV drugs.
Zalcitabine was approved by the FDA in June 1992.
Mechanism
zalcitabine is converted to its active metabolite, dideoxycytidine 5′-triphosphate (ddCTP), by the sequential action of cellular enzymes.
DdCTP interferes with viral RNA-directed DNA polymerase (reverse transcriptase) by competing for use of the organic substrate deoxycytidine 5′-triphosphate (dCTP), in addition to incorpating into viral DNA. Because of it’s absence of a 3′-OH group, the creation of a 5′ to 3′ phosphodiester linkage that’s crucial for DNA chain elongation is inhibited, thus resulting in the blocking of viral DNA development.
The triphosphate form of this drug inhibits HIV reverse transcriptase by competing for incorporation into viral DNA in addition to chain conclusion of this viral DNA as a result of deficiency of a 3′-OH group.
Don’t Use if:
- You’ve lactic acidosis (a metabolic disease ) or particular liver problems (eg, enlarged liver, liver steatosis, abnormal liver function tests)
- You’re allergic to any component in zalcitabine
- You’re taking lamivudine or didanosine
- Speak to your health care provider or healthcare provider straight away if any of them apply to you.
Zalcitabine warnings
- It may rarely cause severe side effects, which might be fatal.
- It can cause acute neurological problems (peripheral neuropathy), and must be used with extreme care in those who suffer from this disease.
- Tell your doctor promptly if nausea, stomach/abdominal pain, or persistent nausea happen, as zalcitabine might want to be ceased until you may be checked.
- Paradoxically, deadly liver failure has happened in people with hepatitis B disease whilst using zalcitabine.
- Zalcitabine ought to be used with care when you’ve got a hepatitis B disease.
- Tell your doctor immediately if tingling/numbness of their feet and hands, dark urine, yellowing of eyes/skin, quick breathing, muscular aches, or abnormal drowsiness occurs.
zalcitabine Side effects
Frequent side effects include
- Gastrointestinal problems,
- Allergic reactions,
- Anemia and
- Neutropenia.
Some dose limiting toxicities are
- Painful sensorimotor peripheral neuropathy, mainly at the lower extremities.
Other side effects include
- Unusual cases of hepatitis,
- Heart failure,
- Sugar abnormalities and
- pancreatitis.
Pregnancy And Breast feeding
- It is a Category C drug. Human studies insufficient. While Zalcitabine has been demonstrated to be teratogenic in rats at concentrations 1365 and 2730 days over the maximum recommended human dose.
- HIV-infected mothers shouldn’t breastfeed due to the possible danger of transmitting HIV to an infant that’s not infected.
Zalcitabine Dose
The suggested dose for adults is 0.75 mg daily.