Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antiviral agent, nucleoside reverse transcriptase inhibitor, thymidine analog. Active in relation to HIV. After entering the cell, zidovudine is sequentially metabolized to zidovudine triphosphate, which competes with the natural substrate thymidine triphosphate for the incorporation of a viral RNA-dependent DNA polymerase (reverse transcriptase) into the strand, thereby inhibiting the replication and growth of viral DNA. The ability of zidovudine to inhibit HIV reverse transcriptase is 100-300 times higher than the ability to suppress human DNA polymerase.
PHARMACOKINETICS
After oral administration, it is quickly and almost completely absorbed from the digestive tract. Penetrates through the BBB, placental barrier. Binding to plasma proteins - 30-38%. Metabolised in the liver.
T 1/2 after oral administration and / in administration - 1 hour. It is excreted in the urine: 14-18% - unchanged, 60-74% - in the form of metabolites.
INDICATIONS
HIV infection (in adults and children older than 3 months): primary manifestations (stage 2B, 2B according to VI Pokrovsky's classification) with a decrease in CD4 lymphocyte count below 400-500 / mm3, stage of incubation (stage 1), stage of secondary diseases (3A, 3B, 3B), stage of acute infection (2A), children without symptoms of the disease, having a significant decrease in immune status. Prevention of occupational infection of persons who received injections and cuts when working with contaminated HIV material, and transplacental HIV infection of the fetus.
DOSING MODE
It is established individually and depends on the stage of the disease, the degree of preservation of the reserves of the bone marrow, the body weight of the patient, the response to treatment.
For admission to adults - 500-600 mg / day, the frequency of admission - 2-5 times / day; Children aged 3 months to 12 years - 360-720 mg / m 2 / day in 4 divided doses.
In / in adults - 1-2 mg / kg every 4 hours; children - 120 mg / m 2 every 6 hours.
SIDE EFFECT
On the part of the hemopoietic system: myelosuppression, anemia, neutropenia, leukopenia, lymphadenopathy, thrombocytopenia, pancytopenia with bone marrow hypoplasia, aplastic or hemolytic anemia.
From the digestive system: nausea, vomiting, dyspepsia, dysphagia, anorexia, taste distortion, abdominal pain, diarrhea, flatulence, bloating, pigmentation or ulceration of the oral mucosa, hepatitis, hepatomegaly with steatosis, jaundice, hyperbilirubinemia, increased hepatic activity enzymes, pancreatitis, increased serum amylase activity.
From the side of the nervous system: headache, dizziness, paresthesia, insomnia, drowsiness, weakness, lethargy, decreased mental performance, tremor, convulsions;anxiety, depression, confusion, mania.
From the sense organs: macular edema, amblyopia, photophobia, vertigo, hearing loss.
From the respiratory system: shortness of breath, cough, rhinitis, sinusitis.
From the cardiovascular system: cardiomyopathy, fainting.
From the urinary system: rapid or difficult urination, hypercreatininaemia.
On the part of the endocrine system and metabolism: lactic acidosis, gynecomastia.
From the musculoskeletal system: myalgia, myopathy, muscle spasm, myositis, rhabdomyolysis, increased activity of CK, LDH.
Dermatological reactions: pigmentation of nails and skin, increased sweating, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Allergic reactions: skin rash, itching, hives, angioedema, vasculitis, anaphylactic reactions.
Other: malaise, back and chest pain, fever, flu-like syndrome, pain syndrome of various localizations, chills, development of secondary infection, redistribution of adipose tissue.
CONTRAINDICATIONS
Neutropenia (the number of neutrophils is less than 750 / Ојl), hemoglobin level is below 7.5 g / dL, increased sensitivity to zidovudine, simultaneous reception with stavudine, doxorubicin, other drugs that reduce the antiviral activity of zidovudine.
PREGNANCY AND LACTATION
It was found that zidovudine penetrates the placental barrier.
It is not known whether zidovudine is excreted in breast milk, therefore, if it is necessary to use during lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
With special care apply in renal failure - it is recommended to correct the dosage regimen depending on the dynamics of zidovudine concentration in the blood.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With special care apply for liver failure - it is recommended to correct the dosage regimen depending on the dynamics of zidovudine concentration in the blood.
APPLICATION IN ELDERLY PATIENTS
With special care are used in elderly patients - correction of the dosing regimen is recommended depending on the dynamics of zidovudine concentration in the blood.
SPECIAL INSTRUCTIONS
With special care apply in renal and hepatic insufficiency, as well as in elderly patients, in these cases correction of the dosage regimen is recommended depending on the dynamics of zidovudine concentration in the blood.
During the treatment period, it is necessary to systematically perform liver and peripheral blood function tests (in the first 3 months of treatment - every 2 weeks, then at least 1 time per month). Treatment should be discontinued if the hemoglobin level is less than 7.5 g / dl and / or the neutrophil count is less than 750 / ОјL. After the recovery of these indicators (usually after a 2-week break), treatment can be resumed.
It should be interrupted treatment with increasing hepatomegaly, a rapid increase in liver transaminases and the development of lactic acidosis.
DRUG INTERACTION
Drugs metabolized in the liver by conjugation with glucuronic acid (paracetamol, acetylsalicylic acid, indomethacin, ketoprofen, codeine, morphine, oxazepam, lorazepam, cimetidine, sulfonamides) can theoretically compete with zidovudine for metabolism and reduce its clearance. Therefore, with simultaneous use, the risk of developing toxic effects of zidovudine or interacting drugs increases.
When used simultaneously with dapsone, pentamidine, amphotericin, flucytosine, ganciclovir, interferon, vincristine, vinblastine, doxorubicin, the risk of toxic development increases
With simultaneous use with ribavirin antagonism is established with respect to antiviral action.
