Zidovudine

Zidovudine is a synthetic dideoxynucleoside antiviral agent. It was first synthesized as an antineoplastic drug in the 1960s. In 1985, it was found to inhibit the in vitro infectivity of human immunodeficiency virus type-1 (HIV-1), although it was known to possess antiviral activity as early as 1974. Zidovudine is active against other retroviruses and some bacteria, but its sole indication is for the treatment and prevention of HIV infection in adults and children. On a weight basis, Zidovudine is more active than didanosine, but less active than zalcitabine, against HIV-1. It was approved by the FDA in March 1987.


Adult Dose
Dose: 2.857 mg/kg
Single Dose: 2.9 (2.857)
Frequency: 8 hourly
Route: PO
Instructions: Initial
Neonatal
Dose: 7.5 to 9 mg/kg
Single Dose: 8.2 (8.25)
Frequency: 6 hourly
Route: Oral
Instructions:
Paedriatic
Dose: 7.05 to 8.46 mg/kg
Single Dose: 7.8 (7.755)
Frequency: 6 hourly
Route: Oral
Instructions: -
Characteristics
Zidovudine also known as AZT. . It is of Synthetic origin and belongs to Thymidine. It belongs to Reverse transcriptase inhibitor pharmacological group on the basis of mechanism of action and also classified in Antiviral Agents pharmacological group.The Molecular Weight of Zidovudine is 267.20. Its pKa is 9.68.
Contraindications
Zidovudine is contraindicated in conditions like Anaemia,Neutropenia.
Effects
The severe or irreversible adverse effects of Zidovudine, which give rise to further complications include Polymyositis, Encephalitis.Zidovudine produces potentially life-threatening effects which include Anemia, Neutropenia, Leucopenia. which are responsible for the discontinuation of Zidovudine therapy.The symptomatic adverse reactions produced by Zidovudine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Nausea, Insomnia.
Indications
Zidovudine is primarily indicated in conditions like AIDS, HIV infection.
Interactions
Zidovudine is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAcyclovirAspirinAtovaquoneAtovaquone possibly inhibits metabolism of Zidovudine.AzapropazoneCimetidine (HCl)Cimetidine in competition for active tubular secretion decreases the renal clearance of zidovudine upto 56%.MinorPatients with renal impairment must avoid this combination.ClarithromycinClarithromycin alter the rate of absorption of zidovudine by changing gastric emptying time.MinorCo-TrimoxazoleDidanosineEtodolacFenbufenFenoprofenFloctafenineFluconazoleFluconazole decreases the clearence of zidovudine and enhances its elimination half life by inhibiting hepatic metabolism.ModerateClosely monitor for zidovudine toxicity. Reduce the dose of zidovudine or discontinue fluconazole if necessary.FlurbiprofenFosphenytoinGanciclovir (Na)HydroxyureaIndinavir (Sulphate)Indinavir enhances AUC of zidovudine upto 36%. During concomitant administration plasma concentration of indinavir is increased upto 13% by acting on its hepatic enzyme.MinorAdjust dose if necessary. Closely monitor the patient for toxicity of zidovudine.IndomethacinInterferon AlphaKetoconazoleLamivudineMeclofenamic AcidMeloxicamOxaprozinParacetamolCombined use of these agents may potentiate the risk of bone marrow suppression and hepatotoxicity.MinorClosely monitor the patient for the development hepatotoxicity and bone marrow toxicity.ProbenecidPyrazinamideRibavirinRibavirin may antagonize the cell culture antiviral activity of Zidovudine against HIV. RifabutinRifampicinStavudineStrontium-89 ChlorideThe concomitant use of bone marrow depressants and strontium-89 chloride may have additive myelosuppressive effects. ModeratePatients should be monitored for excessive bone marrow suppression during treatment with strontium-89 chloride. Dose reductions of the other bone marrow depressants may be necessary.TenoxicamTrimethoprim These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Pregnant Mothers, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Inj (reconstituted soln) Store at room temperature or refrigerator. Use within 24 hrs if refrigerated and within 8 hrs if kept at room temperature. Oral Syrup Store Between 15°C-25°C. Protect from Sunlight. Tab, Caps Store at room temperature, Below 30°C. Refrigeration and Freezing is not recommended. Protect from Sunlight and Moisture.
Warnings
Zidovudine should be used with caution in patients with history of anemia, bleeding or other blood problems, liver or kidney disease or any allergy. This medication should be used only when clearly needed during pregnancy. Avoid zidovudine during lactation to prevent transmission of HIV to child that may not be infected.
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