ZIDOVUDINE

Orlistat

Interfere the drug absorption of HIV medication

HIV medication become less effective

Probenecid

Ibuprofen , Naproxen

Drug interaction may
affect the kidney

Ganciclovir, Dapsone, Trimethoprim

May suppress bone marrow function

Easily available 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

IUPAC NAME

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

Other Names

ADZ ,ZDV , Azidothymidine

Brand Name

Retrovir

Antiretroviral medication

Nucleotide/Nucleoside Reverse Transcriptase Inhibitors

Subtopic

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

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

Always use in combination with other HIV Infection

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

Reduce the risk of HIV transmission

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

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.

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

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

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].

300-mg tablets

100-mg capsules

10-mg/ml syrup

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

Hypersensitivity reaction or rash

Build up of lactic acid in blood

Hepatotoxicity

Muscle weakness (Myopathy)

Blood disorder

Anemia (reduced numbers of red blood cells )

Neutropenia (reduced numbers of white blood cells )

1964 : Azidothymidine first developed

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

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

Solution

Capsule

Syrup

Tablet (Film-coated)

Oral

Parenteral Route :
Intravenous Injection

Absorption

Rapid and complete absorption from
gastrointestinat tract

undergo first-pass metabolism

systemic bioavailability of capsules and solutions
is approximately 65%

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

Distribution

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

Metabolism

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

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.