Zidovudine action

Zidovudine action

Drug 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

Zidovudine action
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 interactions

Zidovudine 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 toxicity

Zidovudine 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.

Zidovudine azt

Zidovudine action
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[42] 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.

Zidovudine anemia

With an accout for my. It is an analog of thymidine. It was originally intended to treat cancer, but failed to show efficacy and had an unacceptably high side effect profile. After showing that this drug was an effective agent against HIV in vitrothe team conducted the initial clinical trial that provided evidence that it could increase CD4 counts in AIDS patients. Burroughs Wellcome Co. It was initially administered in much higher dosages than today, typically mg every four hours even at night. One of AZT's side effects includes anemia, a common complaint in early trials. Modern treatment regimens typically use lower dosages e. AZT may be used in combination with other antiretroviral medications to substantially reduce the risk of HIV infection following a significant exposure to the virus such as a needle-stick injury involving blood or body fluids from an individual known to be infected with HIV. AZT is also recommended as part of a regimen to prevent mother-to-child transmission of HIV during pregnancy, labor and delivery. Common side effects of AZT include nausea, headache, changes in body fat, and discoloration of fingernails and toenails. More severe side effects include anemia and bone marrow suppression, which can be overcome using erythropoietin or darbepoetin treatments. AZT has been shown to work additively or synergistically with many anti-HIV agents; however, acyclovir and ribavirin decrease the antiviral effect of AZT. Drugs that inhibit hepatic glucuronidation, such as indomethacinacetylsalicylic acid Aspirin and trimethoprimdecrease the elimination rate and increase the toxicity. AZT does not destroy the HIV infection, but only delays the progression of the disease and the replication of virus, even at very high doses. A study showed that AZT could not impede the resumption of virus production, and eventually cells treated with AZT produced viruses as much as the untreated cells. So as to slow the development of resistance, it is generally recommended that AZT be given in combination with another reverse transcriptase inhibitor and an antiretroviral from another group, such as a protease inhibitor or a non-nucleoside reverse transcriptase inhibitor. The azido group increases the lipophilic nature of AZT, allowing it to cross cell membranes easily by diffusion and thereby also to cross the blood-brain barrier. Cellular enzymes convert AZT into the effective 5'-triphosphate form. Studies have shown that the termination of the formed DNA chains is the specific factor in the inhibitory effect. The triphosphate form also has some ability to inhibit cellular DNA polymerasewhich is used by normal cells as part of cell division. AZT has been the target of some controversy due to the nature of the patent process. However, the patent expired in placing AZT in the public domainallowing other drug companies to manufacture and market generic AZT without having to pay GlaxoSmithKline any royalties. The U. Katzung, Bertram G. Basic and Clinical Pharmacology10th edition. Read what you need to know about our industry portal chemeurope. My watch list my. My watch list My saved searches My saved topics My newsletter Register free of charge. Keep logged in. Cookies deactivated. To use all functions of this page, please activate cookies in your browser. Login Register.

Zidovudine dose

You are viewing BNF. By mouth, or by intravenous infusion. Abnormally low haemoglobin concentration consult product literature ; abnormally low neutrophil counts consult product literature. Elderly ; lactic acidosis ; risk of haematological toxicity particularly with high dose and advanced disease ; vitamin B 12 deficiency increased risk of neutropenia. Lactic acidosis associated with hepatomegaly and hepatic steatosis has been reported with zidovudine. Use with caution in patients with hepatomegaly, hepatitis, or other risk factors for liver disease and hepatic steatosis including obesity and alcohol abuse. Manufacturer advises discontinue treatment if symptoms of hyperlactataemia, lactic acidosis, progressive hepatomegaly or rapid deterioration of liver function become apparent. Leucopenia ; malaise ; myalgia. Bone marrow disorders ; dyspnoea ; generalised pain ; myopathy ; thrombocytopenia. Alertness decreased ; anxiety ; appetite decreased ; cardiomyopathy ; chest pain ; chills ; cough ; depression ; drowsiness ; dyspepsia ; gynaecomastia ; hepatic disorders ; hyperhidrosis ; influenza like illness ; nail discolouration ; oral discolouration ; paraesthesia ; pure red cell aplasia ; seizure ; taste altered ; urinary frequency increased. If anaemia or myelosuppression occur, reduce dose or interrupt treatment according to product literature, or consider other treatment. Metabolic effects may occur with zidovudine; plasma lipids and blood glucose concentrations should be measured routinely. Manufacturer advises consider dose reduction in moderate to severe impairment—consult product literature. With intravenous use. CapsuleOral solutionSolution for infusion. Other drugs classified as nucleoside reverse transcriptase inhibitors. By mouth, or by intravenous infusion For Adult Seek specialist advice combination therapy preferred consult local protocol. By intravenous infusion For Adult 0. Elderly ; lactic acidosis ; risk of haematological toxicity particularly with high dose and advanced disease ; vitamin B 12 deficiency increased risk of neutropenia Cautions, further information Lactic acidosis Lactic acidosis associated with hepatomegaly and hepatic steatosis has been reported with zidovudine. Individual interactants: Zidovudine. Common or very common Leucopenia ; malaise ; myalgia. Uncommon Bone marrow disorders ; dyspnoea ; generalised pain ; myopathy ; thrombocytopenia. Rare or very rare Alertness decreased ; anxiety ; appetite decreased ; cardiomyopathy ; chest pain ; chills ; cough ; depression ; drowsiness ; dyspepsia ; gynaecomastia ; hepatic disorders ; hyperhidrosis ; influenza like illness ; nail discolouration ; oral discolouration ; paraesthesia ; pure red cell aplasia ; seizure ; taste altered ; urinary frequency increased. Frequency not known Lipoatrophy. Lipodystrophy syndrome Metabolic effects may occur with zidovudine; plasma lipids and blood glucose concentrations should be measured routinely. Manufacturer advises caution in moderate to severe impairment increased risk of accumulation. Monitoring of patient parameters Monitor full blood count after 4 weeks of treatment, then every 3 months. The abbreviation AZT which is sometimes used for zidovudine has also been used for another drug. Back to top. Related Treatment Summaries Herpesvirus infections HIV infection Other drugs classified as nucleoside reverse transcriptase inhibitors.

Zidovudine contraindications

Medically reviewed by Drugs. Last updated on Sep 1, Zidovudine capsules have been associated with hematologic toxicity including neutropenia and severe anemia, particularly in patients with advanced HIV-1 disease [see Warnings and Precautions 5. Prolonged use of Zidovudine has been associated with symptomatic myopathy [see Warnings and Precautions 5. Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues alone or in combination, including Zidovudine and other antiretrovirals. Suspend treatment if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur [see Warnings and Precautions 5. Zidovudine capsules, a nucleoside reverse transcriptase inhibitor, are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. Zidovudine capsules are indicated for the prevention of maternal-fetal HIV-1 transmission [see Dosage and Administration 2. The indication is based on a dosing regimen that included 3 components:. Points to consider prior to initiating Zidovudine capsules in pregnant women for the prevention of maternal-fetal HIV-1 transmission include:. Oral Dosing The recommended oral dose of Zidovudine capsules is mg twice daily in combination with other antiretroviral agents. Healthcare professionals should pay special attention to accurate calculation of the dose of Zidovudine capsules, transcription of the medication order, dispensing information, and dosing instructions to minimize risk for medication dosing errors. Prescribers should calculate the appropriate dose of Zidovudine capsules for each child based on body weight kg and should not exceed the recommended adult dose. Before prescribing Zidovudine capsules, children should be assessed for the ability to swallow capsules. If a child is unable to reliably swallow a Zidovudine capsule, the Zidovudine syrup formulation should be prescribed. The recommended oral dosage in pediatric patients aged 4 weeks to less than 18 years and weighing greater than or equal to 4 kg is provided in Table 1. Alternatively, dosing for Zidovudine capsules can be based on body surface area BSA for each child. The recommended oral dose of Zidovudine capsules is mg per m 2 per day in divided doses mg per m 2 twice daily or mg per m 2 three times daily. In some cases the dose calculated by mg per kg will not be the same as that calculated by BSA. The recommended dosage regimen for administration to pregnant women greater than 14 weeks of pregnancy and their neonates is:. During labor and delivery, intravenous Zidovudine should be administered at 2 mg per kg total body weight over 1 hour followed by a continuous intravenous infusion of 1 mg per kg per hour total body weight until clamping of the umbilical cord. Start neonatal dosing within 12 hours after birth and continue through 6 weeks of age. Neonates unable to receive oral dosing may be administered Zidovudine intravenously. See Table 2 for dosing recommendations. Significant anemia hemoglobin less than 7. In patients who develop significant anemia, dose interruption does not necessarily eliminate the need for transfusion. If marrow recovery occurs following dose interruption, resumption in dose may be appropriate using adjunctive measures such as epoetin alfa at recommended doses, depending on hematologic indices such as serum erythropoietin level and patient tolerance. In patients maintained on hemodialysis or peritoneal dialysis or with creatinine clearance CrCl by Cockcroft-Gault less than 15 mL per min, the recommended oral dosage is mg every 6 to 8 hours. There are insufficient data to recommend dose adjustment of Zidovudine capsules in patients with impaired hepatic function or liver cirrhosis. Frequent monitoring of hematologic toxicities is advised [see Use in Specific Populations 8. Zidovudine capsules are contraindicated in patients who have had a potentially life-threatening hypersensitivity reaction e. Zidovudine should be used with caution in patients who have bone marrow compromise evidenced by granulocyte count less than 1, cells per mm 3 or hemoglobin less than 9. Hematologic toxicities appear to be related to pretreatment bone marrow reserve and to dose and duration of therapy. Treating HIV: Antiretroviral drugs - Infectious diseases - NCLEX-RN - Khan Academy

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