What is azidothymidine used to treat?

azidothymidine is a drug used to delay the development of AIDS (acquired immunodeficiency syndrome) in patients infected with HIV (human immunodeficiency virus). AZT belongs to a group of drugs known as nucleoside reverse transcriptase inhibitors (NRTIs). In 1987 AZT became the first of these drugs to be approved by the U.S. Food and Drug Administration for the purpose of prolonging the lives of AIDS patients.

About the pharmacological effects of this product

zidovudine is an antiviral drug with high activity against retroviruses including human immunodeficiency virus (HIV) in vitro. It is phosphorylated into zidovudine triphosphate by thymidine kinase in virus-infected cells, which can selectively inhibit HIV reverse enzyme, leading to the termination of HIV chain synthesis, thereby preventing HIV replication.

What about the overuse of this product?

Incidents involving adults and children with doses of more than 50g have been reported, and none of them is fatal. These reported events were spontaneous or induced nausea and vomiting. Blood changes are transient and not serious, and some patients have nonspecific central nervous system symptoms, such as headache, dizziness, sleepiness, fatigue, and unconsciousness. A 35-year-old man took 36g of this product at a time, and he developed seizures 3 hours later. Because no other cause was found, it may be caused by drugs. All patients recovered without sequelae. Hemodialysis or peritoneal dialysis had no effect on the excretion of this product, but the excretion of its metabolite GZDV increased.

About the pharmacokinetics of this product

zidovudine combines with the DNA polymerase of the virus to stop the growth of the DNA chain, thereby inhibiting the replication of the virus. Human α- DNA polymerase has little effect on human cell proliferation.

After using the capsule, it is absorbed rapidly. After the first pass metabolism, the bioavailability is 52% - 75%. After intravenous drip of 2.5mg/kg for 1 hour or oral administration of 5mg/kg, the blood drug concentration can reach 4 ~ 6 μ mol/L（1.1～1.6mg/L）； 4 hours after administration, cerebrospinal fluid concentration can reach 50 ~ 60% of plasma concentration; VD=1.6L/kg； The protein binding rate is about 34 ~ 38%; The product is mainly glucuronide into inactive gaze in the liver; One hour after use. About 14% of drugs are excreted into the urine through glomerular filtration and active infiltration of renal tubules; 74% of metabolites are also excreted by the urine. For the treatment of acquired immunodeficiency syndrome (AIDS). When patients develop complications (Pneumocystis carinii or other infections), they need to be treated with other symptomatic drugs.

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