Buy Generic Retrovir (Zidovudine) 100, 300 mg online

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Most popular brand: Retrovir
Active ingredient: Zidovudine
Available dosage forms: 100, 300 mg

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Active – active substance / start: zidovudine

AZT; Viro – Z; Vudazidin; Zaydovin; Zido – HSBC; Zidovirin; Zidovudine; Zidovudine – Verein; Retrovir (Retrovir Azita); Timazid.

Zidovudine – antiviral (anti-retroviral) agent; agent for the treatment of HIV – infection. Blocks reverse transcription – key replication of retroviruses, including human immunodeficiency virus (HIV). It is both an inhibitor and substrate for the action of viral reverse transcriptase. It is used to treat HIV – infection in children and adults in combination with other antiretroviral drugs; to reduce transplacental transmission in pregnant HIV – positive women and in children born to HIV – positive mothers; It can be used for the prevention of occupational exposure to persons who have received injections and cuts while work with HIV – contaminated material. The solution for the on / in infusions used to treat serious manifestations of HIV – infection in patients with AIDS or AIDS-related complex, which can not take the medication inside. Efficacy of zidovudine has been demonstrated in patients with AIDS who had undergone during the last 4 months of the first pneumonia episode caused by Pneumocystis carinii, and patients with complex associated with AIDS and multiple signs of HIV – infection, including candidiasis of the skin and mucous membranes, weight loss, lymphadenopathy, and fever of unknown origin.

Active – active substance:
AZT / Zidovudine.

Dosage Forms:
The capsules.
Oral solution.
The solution for infusion.

Zidovudine

Properties / Action:
Zidovudine – antiviral (anti-retroviral) agent; agent for the treatment of HIV – infection.
Zidovudine is a thymidine analogue and competing with him, blocks reverse transcription – the key retroviral replication process. After penetration into the affected and unaffected virus Zidovudine cells sequentially metabolized (phosphorylated) by cellular thymidine kinase and non-specific kinases to zidovudine triphosphate (monophosphate – diphosphate – triphosphate), which competes with the natural substrate thymidine for insertion into the chain of viral RNA – dependent DNA – polymerase ( reverse transcriptase), thus inhibiting the growth and replication of viral DNA. Zidovudine – triphosphate is both an inhibitor and substrate for the action of viral reverse transcriptase. The ability of AZT to inhibit HIV reverse transcriptase in 100 – 300 times higher than the ability to inhibit DNA – polymerase human.
Zidovudine inhibits the replication of retroviruses, including human immunodeficiency virus (HIV) and other mammalian viruses. It noted the antiviral activity of zidovudine against hepatitis B virus, and anti-bacterial activity against shigel, Salmonella, Klebsiella, enterobacteria Escherichia coli. Zidovudine prolongs the life of HIV – infected patients reduces the incidence and severity of infectious diseases caused by opportunistic microorganisms.
In patients receiving prolonged courses of treatment zidovudine, HIV strains have been isolated with reduced susceptibility to zidovudine. Currently, work is continuing to study the relationship between HIV sensitivity to zidovudine in vitro and its clinical effect. According to reports, in the early stages of HIV – infection rate and the degree of sensitivity in vitro to reduce zidovudine significantly lower than the long-term course of the disease.
development of resistance to thymidine analogues (including zidovudine) results from a gradual emergence of specific mutations in codon 6 of HIV reverse transcriptase. Viruses acquire phenotypic resistance to thymidine analogues resulting combined mutations in codons 41 and 215 or accumulation of at least four of the six mutations. Mutations do not cause cross-resistance to other nucleosides that allows for the treatment of HIV – infection other reverse transcriptase inhibitors. By the development of multi-drug resistance mutations result in 2 types. In one case, the mutations occur in 62, 75, 77, 116 and 151 of HIV reverse transcriptase codons, in the second case it is a T69S mutation with an insert in the 6 – th base pair corresponding to this position, which is accompanied by the emergence of phenotypic resistance to zidovudine and to other nucleoside reverse transcriptase inhibitors. Both of these mutations severely limits therapeutic options for HIV – infection. Zidovudine
used in combination antiretroviral therapy with other nucleoside reverse transcriptase inhibitors, and other groups of drugs (protease inhibitors, nucleoside reverse transcriptase inhibitors). There synergy or enhancement of action of zidovudine in combination with lamivudine his om, om didanosine, alpha interferon th. However, in vitro studies suggest that combination therapy with three drugs (nucleoside analogues or two nucleoside analogues and a protease inhibitor) is more effective than treatment with one or two drugs in suppressing HIV – 1. The use of zidovudine in combination with lamivudine delays the emergence of zidovudine-resistant strains of the virus in the event that the patients had not previously carried out antiretroviral therapy.

Pharmacokinetics:
Zidovudine is well absorbed from the gastro – intestinal tract. Bioavailability is 60-70%. According to calculations in the form of a solution Zidovudine oral zidovudine bioequivalent in capsule form. Absorbance AZT in the form of solution for oral administration is much more intense than that after administration of the capsules from reaching Cmax plasma in 0.5 h and 0.8 h, respectively. It penetrates into most tissues and body fluids through the placenta and the blood-brain barrier. Determined in amniotic fluid and fetal blood; Zidovudine concentrations in the plasma of children at birth is the same as that of mothers during childbirth. Found in cerebrospinal fluid at a concentration of 15 – 64%, depending on the dose. Found in the seminal fluid, and breast milk. Plasma protein binding – 30 – 38%. It is metabolized in the liver. The major metabolite is 5 ‘- glucuronide; with a / in the introduction is found another metabolite – 3’amino – 3 ‘- deoxythymidine. Zidovudine has a short half-life – T1 / 2 of plasma – 1.1 h, the active form in the cell – to 3 hours. Approximately 20% of zidovudine excreted unchanged by the kidneys, about 75% – metabolized to form glucuronide and subsequent excretion through the kidneys. After the on / in the introduction of 29% of the dose Zidovudine vydelyaetya unchanged in the urine and 45% of the dose – in the form of glucuronide. Renal clearance of AZT far exceeds creatinine clearance, which indicates the excretion of large parts of the drug via tubular secretion.
Children under the age of 14 days, the degree of binding of zidovudine with glucuronic acid reduced, and therefore the increased bioavailability, reduced clearance, half-life is prolonged. However, starting with 3 weeks of life in children pharmacokinetic parameters are similar to those in adults.
In pregnant women, no signs of accumulation of zidovudine and its pharmacokinetics is similar to that in non-pregnant.
In patients with severe renal impairment Cmax of zidovudine in plasma increased by 50%. In renal insufficiency, there is a significant accumulation of the main metabolite glucuronide, but signs of toxic effects are not observed.
When liver failure can occur as a result of reducing accumulation of zidovudine glucuronidation (requires dose adjustments).
Special data on pharmacokinetics in elderly patients are missing.
Hemo – and peritoneal dialysis have no effect on elimination of zidovudine, while elimination of glucuronide enhanced.

Indications:
For intake:

Treatment of HIV – infection in children and adults in combination with other antiretroviral drugs; use in patients with HIV – infection in the incubation step (step 1), an acute infection (step 2A) and primary manifestations (step 2B and 2C), a secondary stage diseases (stages IN, ST, 3B classification VP Pokrovsky );

to reduce transplacental transmission in pregnant HIV – positive women (more than 14 weeks), and in children born to HIV – positive mothers;

can be used for the prevention of occupational exposure to persons who have received injections and cuts while work with HIV – contaminated material.
For intravenously infusion:

short-term treatment of serious manifestations of HIV – infection in patients with AIDS or AIDS-related complex, who can not take Zidovudine inside.
Efficacy has been demonstrated in patients with AIDS who had undergone during the last 4 months the first episode of pneumonia caused by Pneumocystis carinii, and patients with complex associated with AIDS and multiple signs of HIV – infection, including candidiasis skin and mucous membranes, reduced weight (more than 10%, or more than 6 kg), lymphadenopathy and fever of unknown origin.

Dosage and administration:
The course zidovudine treatment assigned strictly doctor – specialist and is carried out under laboratory monitoring. Dosage is determined individually and depends on the stage of the disease, the degree of preservation of the bone marrow reserves, patient weight, response to treatment.
Inside (capsule, oral solution)
Adults and children over 12 years
The range of dosage -.. 500 – 1500 mg /day. The recommended dose of 500-800 mg / day in 2-3 divided doses in combination with other antiretrovirals. Efficacy daily dose of less than 1000 mg of zidovudine for the treatment and prevention of HIV – associated complications is not installed. .
Children from 3 months to 12 years
The daily dose – 360-480 mg / m ^ 2 (10 – 15 mg / kg) in 3-4 divided doses in combination with other antiretroviral agents. Efficacy daily dose of less than 720 mg zidovudine / m ^ 2 (20 mg / kg) or 180 mg / m ^ 2 every 6 hours for the treatment and prevention of neurological complications of HIV – infection has not been established. The maximum dose should not exceed 200 mg every 6 hours.
For children under the age of 3 months the existing data are insufficient to make recommendations.
Prevention of HIV transmission – transmission from mother to fetus
It is established by special investigations that the level of infection of the fetus is reduced by 4 times.. Toxicity (teratogenicity), there was, as toxic dose of zidovudine for various bodies in 50 times higher than those used for the treatment. 2 Effective prevention schemes.
1. Pregnant women – 500 mg / day (100 mg 5 times a day), starting at 14 weeks of pregnancy before birth. During birth administered Zidovudine / in a dose of 2 mg / kg over 1 h, then administered by continuous Zidovudine / in infusion at a dose of 1 mg / kg / hour – until the umbilical cord is not pinched. Newborns AZT administered orally in the form of oral solution at a dose of 2 mg / kg body weight every 6 hours. AZT is administered within 12 hours after birth and continue taking it up to 6 weeks. Babies who are unable to take the drug inside prescribe AZT in the form of on / in infusion at a dose of 1.5 mg / kg (for at least 30 min) every 6 hours.
2. Pregnant women – 300 mg 2 times a day to 36 weeks before the onset of labor, and then – every 3 hours until the end of the delivery.
HIV – infection in persons exposed to infected material (occupational exposure, in patients during manipulation, with injury of skin, mucosal, parenteral administration, etc…)
assigned Zidovudine 200 mg 5 times per day for 3 – 5 days. The first dose should be taken zidovudine or for 2 hours before possible infection or within 2 hours after contact. If the drug occurs much later than the specified time, while receiving zidovudine increased to 10 days.
B / (solution for infusion) .
By slow infusion in diluted form for 1 hour. The solution is administered Zidovudine only as long as the patients will not take the drug inside. It is not allowed in the / m introduction.
Rules for the preparation of the solution intravenously infusion .
The solution for the on / in infusion must be diluted prior to administration. The required dose is added to a solution of 5% glucose solution for the on / in and mixed with it, the final concentration was equal to zidovudine 2 mg / ml or 4 mg / ml. These solutions remain stable for 48 hours at 5 ° C and 25 ° C. Cultivation should be under full aseptic immediately before administration; the unused portion of the solution should be destroyed in a vial. At its turbidity of the solution should be discarded.
Adults and children over 12 years .
1-2 mg / kg every 4 hours. This dose with a / in the introduction of zidovudine provides the same exposure of the drug, as well as the dose of zidovudine 1.5 mg / kg or 3 mg / kg every 4 hours (600 or 1200 mg / day in patients of 70 kg body weight) when administered. Efficiency lower doses in the treatment or prevention of HIV – and of associated neurological complications of malignant tumors is unknown. Once the patient is able to take Zidovudine inside, intravenously the introduction should be discontinued.
Children from 3 months to 12 years.
Information about the use of zidovudine for the on / in infusion in children is insufficient. AZT was administered at various doses from 80 to 160 mg / m ^ 2 every 6 hours (320-640 mg / m ^ 2 / day). Doses of between 240-320 mg / m2 per day in 3-4 divided doses comparable to doses of 360 mg / m ^ 2 to 480 mg / m ^ 2 per day 3 – 4 divided doses when administered, but as far as they are effective in the present time is not set.
Prevention of HIV transmission – transmission from mother to fetus
Pregnant women, ranging from 14 weeks gestation until the onset of labor is recommended to prescribe AZT in.. During labor assigned Zidovudine / in a dose of 2 mg / kg as an infusion over 1 hour, and then as a continuous infusion at a dose of 1 mg / kg / h until the umbilical cord is not until the clip is applied.
Newborn ZDV appointed inside, starting with the first 12 hours after birth to 6 weeks. If it is impossible ingestion administered intravenously a dose of 1.5 mg / kg as an infusion over 30 minutes every 6 hours.
In severe renal insufficiency recommended dose of 300-400 mg / day orally or 1 mg / kg 3-4 times per day intravenously. Depending on the response from the peripheral blood and clinical effect may require further adjustment of the dose. Hemodialysis and peritoneal dialysis have little effect on the elimination of zidovudine, but promotes the excretion of glucuronide. For patients in end-stage renal failure on hemodialysis or peritoneal dialysis, the recommended dose is 100 mg every 6 – 8 h.
The change in dosage may be required in patients with haematological adverse reactions patients. It is most common in patients who had initially low bone marrow reserve prior to treatment. If the hemoglobin decreases to 7.5 – 9 g / dL (4.65 – 5.59 mmol / L) or the number of white blood cells is reduced to 0.75 – 1.0 x10 ^ 9 / L, the Zidovudine can be used at a lower daily dose until until recover function bone marrow. Bone marrow recovery may be accelerated by short (2 – 3 weeks) interruption of zidovudine. If the change discussed dose, the daily dose may be, for example, halved and then increased depending on the tolerance of the original. In / in the introduction of zidovudine should be discontinued if hemoglobin levels below 7.5 g / l or the neutrophil count less 0.75h10 ^ 9 / L. bone marrow function is normally restored within two weeks, then it is possible to resume treatment at a lower dose. After a further 2 – 4 weeks, the dose can be gradually increased, depending on the tolerance of the patient to the initial dose (although information on / in a limited application of zidovudine for 2 weeks).
When hepatic dysfunction may require dose adjustment, however, the existing data are insufficient to develop dosing recommendations. Limited experience with zidovudine in patients with cirrhosis of the liver suggests a possible drug accumulation due to decreased formation of glucuronide. If monitoring of plasma levels of zidovudine is impossible, it is recommended to pay attention to signs of intolerance to the preparation, and if necessary to adjust the dose and / or increase the interval between doses doses.
Special studies on the use of zidovudine in patients have not been conducted over 65 years. However, given the possible age-related changes, such as reduction in renal function and alteration of haematological parameters it is recommended to carefully monitor the patient’s condition prior to the appointment and during treatment with zidovudine.

Overdose:
The symptoms: fatigue, headache, nausea, vomiting, haematological disorders. Contraindications:

myopathy;

The expiration date on the package.
Terms of pharmacy holiday – by prescription.