ZIDOVUDINE

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ZIDOVUDINE

5) PHARMACOKINETICS

Elimination

Elimination will occur in the form of GZDV.For intravenous dosing, about 29% of the dose was excreted in the urine unchanged and about 45% of the dose was excreted as GZDV.

Metabolism

It metabolized by glucuronide conjugation to inactive metabolite, 3′-azido-3′-deoxy-5′- O-beta-D-glucopyranuronosylthymidine (GZDV).

Distribution

Volume of distribution via Intravenous Administration is 1.6± 0.6 L/kg

Absorption

Administration of high fat meal - decrease the rate and extent of absorption

systemic bioavailability of capsules and solutions is approximately 65%

undergo first-pass metabolism

Rapid and complete absorption from gastrointestinat tract

6) ROUTES OF DRUG ADMINISTRATION

Parenteral Route : Intravenous Injection

Oral

7) DOSAGE FORM

Tablet (Film-coated)

Syrup

Capsule

Solution

8) HISTORY

March 1987 : Approval of zidovudine by the US Food and Drug Administration

1983 : Burroughs Wellcome began a screening program and do further test that contracted with US National Cancer Institute (NCI)

1964 : Azidothymidine first developed

9) ADVERSE EFFECT

Blood disorder

Neutropenia (reduced numbers of white blood cells )

Anemia (reduced numbers of red blood cells )

Muscle weakness (Myopathy)

Hepatotoxicity

Build up of lactic acid in blood

Hypersensitivity reaction or rash

10) STRENGTH OF DOSAGE

20-ml/200-mg single-use vials for intravenous injection

10-mg/ml syrup

100-mg capsules

300-mg tablets

References

Webmd.com. n.d. Zidovudine.(July 2020) Available at: https://www.webmd.com/drugs/2/drug-4386/zidovudine-oral/details#:~:text=Some%20products%20that%20may%20interact,NSAIDs%20such%20as%20ibuprofen%20or [Accessed 5 July 2020].

Drugbank.ca. 2020. Zidovudine - Drugbank. [online] Available at: https://www.drugbank.ca/drugs/DB00495#BE0004136l

Niaid.nih.gov. 2018. Antiretroviral Drug Discovery And Development. [online] Available at: https://www.niaid.nih.gov/diseases-conditions/antiretroviral-drug-development

Zidovudine Dosage, Side Effects. (2020, January 20). AIDSinfo. Derived from https://aidsinfo.nih.gov/drugs/4/zidovudine/0/patient#:%7E:text=Some%20side%20effects%20of%20zidovudine,as%20severe%20anemia%20or%20neutropenia.

4) USAGE

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Although HIV cannot be cure, it can help people with HIV to live longer and obtain healthy lives.

Reduce the risk of HIV transmission

To prevent mother -to-child transmission (perinatal transmission)

Always use in combination with other HIV Infection

To treat HIV Infection in adults and children 4 weeks of age and older

3) MECHANISM OF ACTION (PHARMACODYNAMIC)

Zidovudine is phosphorylated to active metabolites (Zidovudine-triphosphate)

Bind to HIV reverse transcriptase enzyme competitively and inhibit it

Incorporate into viral DNA

Chain termination of DNA synthesis occur

2) CLASSIFICATION

Subtopic

Nucleotide/Nucleoside Reverse Transcriptase Inhibitors

Antiretroviral medication

1 ) NOMENCLATURE

Brand Name

Retrovir

Other Names

ADZ ,ZDV , Azidothymidine

IUPAC NAME

1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione

12)DRUG AVAILABILITY IN MALAYSIA

Combination of zidovudine with new drugs such as Lamivudine and Saquinavir have been shown to be more effective in maintaining good quality of life in AIDS patients

Easily available in Malaysia

11) DRUG-DRUG INTERACTION (Drug that may interact with Zidovudine)

Ganciclovir, Dapsone, Trimethoprim

May suppress bone marrow function

Ibuprofen , Naproxen

Drug interaction may affect the kidney

Probenecid

Orlistat

HIV medication become less effective

Interfere the drug absorption of HIV medication