- Zidovudine action
- Zidovudine side effects
- Zidovudine interactions
- Zidovudine toxicity
- Zidovudine azt
- Zidovudine anemia
- Zidovudine dose
- Zidovudine contraindications
Zidovudine actionDrug information provided by: IBM Micromedex. It is very important that your doctor check your or your child's progress at regular visits to make sure that this medicine is working properly. Blood tests may be needed to check for unwanted effects. Zidovudine may cause blood problems. These problems may result in a greater chance of certain infections and slow healing. Therefore, you should be careful when using regular toothbrushes, dental floss, and toothpicks not to damage your or your child's gums. Check with your or your child's medical doctor or dentist if you have any questions about proper oral hygiene mouth care during treatment with this medicine. Check with your doctor if you or your child has muscle pain, tenderness, wasting, or unusual tiredness or weakness while you are using this medicine. Zidovudine may cause blood and bone marrow problems. Symptoms of bone marrow problems include fever, chills, sore throat pale skin, or unusual tiredness or weakness. These problems may require blood transfusions or temporarily stopping treatment with zidovudine. Check with your or your child's doctor if any new health problems or symptoms occur while you or your child are taking zidovudine. Two rare but serious reactions to this medicine are lactic acidosis too much acid in the blood and liver toxicity, which includes an enlarged liver. These are more common if you are female, very overweight obeseor have been taking anti-HIV medicines for a long time. Call your doctor right away if you or your child have more than one of these symptoms: abdominal discomfort or cramping, dark urine, decreased appetite, diarrhea, general feeling of discomfort, light-colored stools, muscle cramping or pain, nausea, unusual tiredness or weakness, trouble breathing, vomiting, or yellow eyes or skin. Your immune system may get stronger when you start taking HIV medicines. Tell your doctor right away if you or your child notices any changes in your health. Sometimes the immune system will start to fight infections that were hidden in your body, such as pneumonia or tuberculosis. This medicine may decrease or lose body fat, especially in your face, arms, legs, or buttocks, when this medicine is used for a long time. Talk to your doctor if you have concerns. Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription over-the-counter [OTC] medicines and herbal or vitamin supplements. All rights reserved.
Zidovudine side effects
After conversion to its active metabolite, inhibits activity of HIV reverse transcriptase and terminates viral DNA growth. Adults and children older than age mg P. Children ages 4 weeks to younger than 18 years weighing 30 kg 66 lb or more: mg P. Don't exceed recommended adult dosage. Pregnant women more than 14 weeks of pregnancy : mg P. For neonates unable to receive oral dosing, 1. Infuse over 1 hour. Avoid rapid infusion or bolus injection. Don't give by I. CNS: headache, paresthesia, malaise, insomnia, dizziness, drowsiness, asthenia, seizures. GI: nausea, vomiting, constipation, abdominal pain, dyspepsia, anorexia, pancreatitis. Hematologic: severe anemia necessitating transfusionsagranulocytopenia, severe bone marrow depression. Acetaminophen, aspirin, indomethacin: increased risk of zidovudine toxicity. Amphotericin B, dapsone, flucytosine, pentamidine: increased risk of nephrotoxicity and bone marrow depression. Cytotoxic drugs, myelosuppressants, nephrotoxic drugs such as ganciclovir, interferon alfa : increased risk of hematologic toxicity. Fluconazole, methadone, probenecid, valproic acid: increased zidovudine blood level, greater risk of toxicity. Be aware that drug can cause hepatotoxicity. Related to zidovudine: stavudinedidanosine. It was the first agent approved for such use. Pharmacologic class: Nucleoside reverse transcriptase inhibitor Therapeutic class: Antiretroviral Pregnancy risk category C.
Zidovudine interactionsZidovudine can cause serious, life-threatening side effects. These include hypersensitivity reaction or rash, a buildup of lactic acid in the blood lactic acidosisliver problems, muscle weakness myopathyand blood disorders, such as extremely reduced numbers of red blood cells severe anemia or reduced numbers of white blood cells neutropenia. Worsening of liver disease sometimes resulting in death has occurred in people with both HIV and hepatitis C virus infection HCV who were taking HIV medicines and also being treated for HCV infection with interferon with or without ribavirin. If you are taking zidovudine as well as interferon with or without ribavirin and you experience side effects, tell your health care provider. While taking zidovudine, it is important to keep all of your appointments with your health care provider. Zidovudine is a prescription medicine approved by the U. To prevent mother-to-child transmission perinatal transmission of HIV. If you are taking HIV medicines, don't cut down on, skip, or stop taking them unless your health care provider tells you to. Vials of zidovudine for IV injection contain mg of zidovudine in a 20 mL solution. The diluted medicine is injected slowly infused over a specified period of time through a needle or catheter into a vein. If you take too much zidovudine, contact your health care provider or local poison control center right away, or go to the nearest hospital emergency room. For more information on how to take zidovudine, see the FDA drug labels for zidovudine tablets and zidovudine capsules, syrup, and solution for IV injection. For more information on how to take zidovudine for IV injection, see the drug summary from MedlinePlus. If you miss a dose of zidovudine, take the missed dose as soon as you remember it. But if it is almost time for your next dose, skip the missed dose and just take your next dose at the regular time. Do not take two doses at the same time to make up for a missed dose. Zidovudine may cause side effects. Many side effects from HIV medicines, such as nausea or occasional dizziness, are manageable. Some side effects of zidovudine can be serious. Serious side effects of zidovudine include lactic acidosis, liver problems, myopathy, and blood disorders such as severe anemia or neutropenia. See section above: What are the most important things to know about zidovudine? Tell your health care provider if you have any side effect that bothers you or that does not go away. These are not all the possible side effects of zidovudine. To learn more about possible side effects of zidovudine, read the drug label or package insert or talk to your health care provider or pharmacist.
Zidovudine toxicityZidovudine is more active against acutely infected cells as compared to chronically infected cells. Zidovudine is well absorbed and undergoes first-pass hepatic glucuronidation to zidovudine glucuronide. Peak plasma concentrations occur at 0. Both zidovudine glucuronide and zidovudine are eliminated through renal excretion with tubular secretion contributing to the elimination. This dose has been shown to have antiviral activity. However, it is less marked and more slowly achieved than mg twice a day. Hemodialysis or continuous ambulatory peritoneal dialysis CAPD - mg once daily. Zidovudine should be used with caution in patients who have bone marrow compromise i. Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of NRTIs. The use of zidovudine and stavudine d4T concomitantly is contraindicated due to antagonism that occurs between these two thymidine analogues. Ganciclovir, interferon-alpha and other cytotoxic or bone marrow suppressive agents trimethoprim-sulfamethoxazole, dapsone, pyrimethamine, flucytosine, adriamycin, vinblastine, sulfadiazine, hydroxyurea, vincristine and amphotericin B may increase the risk of hematologic toxicity associated with zidovudine. Both doxorubicin and ribavirin have demonstrated in vitro inhibition of zidovudine phosphorylation and antagonize its antiviral activity. Frequent blood counts in patients with advanced HIV disease, periodic blood counts in patients with asymptomatic or early HIV disease.
Common side effects include headaches, fever, and nausea. Zidovudine was first described in AZT is usually dosed twice a day in combination with other antiretroviral therapies. AZT has been used for post-exposure prophylaxis PEP in combination with another antiretroviral drug called lamivudine. Together they work to substantially reduce the risk of HIV infection following the first single exposure to the virus. AZT is now a principal part of the clinical pathway for both pre-exposure prophylaxis and post-exposure treatment of mother-to-child transmission of HIV during pregnancy, labor, and delivery and has been proven to be integral to uninfected siblings' perinatal and neonatal development. A number of studies were initiated in the late s that sought to test the efficacy of a shorter, simpler regimen for use in 'resource-poor' countries. Most common side-effects include nausea, vomiting, acid reflux heartburnheadache, cosmetic reduction in abdominal body fat, light sleeping, and loss of appetite. Less common side effects include faint discoloration of fingernails and toenails, mood elevation, occasional tingling or transient numbness of the hands or feet, and minor skin discoloration. Allergic reactions are rare. Early long-term higher-dose therapy with AZT was initially associated with side effects that sometimes limited therapy, including anemianeutropeniahepatotoxicitycardiomyopathyand myopathy. All of these conditions were generally found to be reversible upon reduction of AZT dosages. Even at the highest doses that can be tolerated in patients, AZT is not potent enough to prevent all HIV replication and may only slow the replication of the virus and progression of the disease. AZT is a thymidine analogue. Reverse transcription is necessary for production of HIV's double-stranded DNAwhich would be subsequently integrated into the genetic material of the infected cell where it is called a provirus. Cellular enzymes convert AZT into the effective 5'-triphosphate form. At very high doses, AZT's triphosphate form may also inhibit DNA polymerase used by human cells to undergo cell divisionbut regardless of dosage AZT has an approximately fold greater affinity for HIV's reverse transcriptase. AZT crystallizes into an asymmetric nucleated monoclinic salt structure, forming an equalized hydrogen-nitrogen-oxygen bonded network of base-paired dimers; its multiscaled crystallized lattice superstructure and surfactant headgroup electrostatic bond polarity was reported in and In the s, the theory that most cancers were caused by environmental retroviruses gained clinical support and funding. It had recently become known, due to the work of Nobel laureates Howard Temin and David Baltimore that nearly all avian cancers were caused by bird retroviruses, but corresponding human retroviruses have not yet been found. In parallel work, other compounds that successfully blocked the synthesis of nucleic acids had been proven to be both antibacterial, antiviral, and anticancer agents, the leading work being done at the laboratory of Nobel laureates George Hitchings and Gertrude Elionleading to the development of the antitumor agent 6-mercaptopurine. This report attracted little interest from other researchers as the Friend leukemia virus is a retrovirus, and at the time, there were no known human diseases caused by retroviruses. In order to expedite the process of discovering a drug, the NCI researchers actively sought collaborations with pharmaceutical companies having access to libraries of compounds with potential antiviral activity. Clair set up a program to discover drugs with the potential to inhibit HIV replication. Clair, Janet RideoutSandra Lehrman and others. Their research efforts were focused in part on the viral enzyme reverse transcriptase. Reverse transcriptase is an enzyme that retroviruses, including HIV, utilize to replicate themselves. Secondary testing was performed in mouse cells infected with the retroviruses Friend virus or Harvey sarcoma virus, as the Wellcome group did not have a viable in-house HIV antiviral assay in place at that time, and these other retroviruses were believed to represent reasonable surrogates. AZT proved to be a remarkably potent inhibitor of both Friend virus and Harvey sarcoma virus, and a search of the company's records showed that it had demonstrated low toxicity when tested for its antibacterial activity in rats many years earlier. This initial trial of AZT proved that the drug could be safely administered to patients with HIV, that it increased their CD4 counts, restored T cell immunity as measured by skin testing, and that it showed strong evidence of clinical effectiveness, such as inducing weight gain in AIDS patients. It also showed that levels of AZT that worked in vitro could be injected into patients in serum and suppository form, and that the drug penetrated deeply only into infected brains. AZT was subsequently approved unanimously for infants and children in Inthe advocacy group Public Citizen filed a lawsuit claiming that the patents were invalid. Subsequently, Barr Laboratories and Novopharm Ltd. In response, Burroughs Wellcome Co. This suit was appealed up to the Supreme Court of the US, but in they declined to formally review it. Barr Laboratorieswas a landmark in US law of inventorship. From Wikipedia, the free encyclopedia.