Treatment of HIV-1 infection in combination antiretroviral therapy in adults.
Drug technology, Russia
Active substances :
Tenofovir disoproxil fumarate 300.0 mg
Tenofovir is contraindicated in patients with hypersensitivity to any component of the drug.
Renal failure with creatinine clearance less than 50 ml / min, including patients on hemodialysis. If creatinine clearance is less than 30 ml / min, use of the drug should be avoided; in the event that other treatment is not available, renal function should be carefully monitored and the interval between drug administration should be adjusted.
The following are adverse reactions with a suspected (possible) connection with the drug, which are listed by systemic organ classes in decreasing order of their severity, with the following frequency: very often (> 1/10) and often (> 1/100, <1/10 ), rarely (> 1/10000, <1/1000), very rare
Metabolic and nutritional disorders : very often – hypophosphatemia.
From the nervous system : very often – dizziness.
From the gastrointestinal tract : very often – diarrhea, vomiting, nausea; often flatulence.
Combination retroviral therapy has been associated with metabolic disorders such as hypertriglyceridemia, hypercholesterolemia, insulin resistance, hyperglycemia, and hyperlactatemia; redistribution of subcutaneous tissue (lipodystrophy).
Cases of osteonecrosis have been reported, especially in patients with risk factors or with long-term combination antiviral therapy. The frequency is unknown.
Metabolic and nutritional disorders : rarely – lactic acidosis, frequency unknown – hypokalemia
Respiratory, thoracic and mediastinal disorders: very rarely – dyspnea.
From the gastrointestinal tract : rarely – pancreatitis.
From the side of the hepatobiliary system : rarely – increased activity of transaminases; very rarely – hepatitis, the frequency is unknown – hepatic steatosis.
Skin and subcutaneous tissue disorders : rarely – rash.
From the side of the musculoskeletal system: the frequency is unknown – rhabdomyolysis, osteomalacia, muscle weakness, myopathy.
From the urinary system : rarely – acute renal failure, proximal renal tubulopathy (including Fanconi syndrome), hypercreatininemia; very rarely – acute tubular necrosis; frequency unknown – nephritis (including acute interstitial), nephrogenic diabetes insipidus.
General disorders and changes at the injection site : very rarely – asthenia.
Didanosine : an increase in the concentration of didanosine when used together; they must be used with caution and monitored for didanosine toxicity (eg, pancreatitis, neuropathy). The combination of tenofovir with didanosine is not recommended; if warranted, dose reduction or discontinuation of didanosine therapy should be considered. Tenofovir is combined with reduced doses of didanosine (for example, patients weighing> 60 kg are prescribed didanosine 250 mg once a day; <60 kg – 200 mg once a day). On the other hand, such a low-dose combination may be characterized by low antiviral activity and insufficient increase in the number of CO4 lymphocytes, as indicated by the high incidence of therapy failure when using this combination with the addition of efavirenz or nevirapine .
Atazanavir: A decrease in the concentration of atazanavir when used together and an increase in the concentration of tenofovir. It is necessary to use tenofovir with atazanavir only with an additional increase in the action of the latter with ritonavir .
Lopinavir / ritonavir: Increases in tenofovir concentrations when used together.
Darunavir: increases the concentration of tenofovir by 20-25%. The drugs should be used in standard doses, and the nephrotoxic effects of tenofovir should be carefully monitored. Tenofovir is mainly excreted from the body through the kidneys, the combined use of tenofovir with drugs that reduce renal function or reduce / stop active tubular secretion may increase serum tenofovir concentration and / or increase the concentration of other drugs excreted through the kidney.
Ganciclovir, valganciclovir, and cidofovir compete with tenofovir for active renal tubular secretion, resulting in increased levels of tenofovir or a concomitant drug; vigilance is required regarding possible side effects. Nephrotoxic drugs can also increase serum tenofovir concentrations.
How to take, course and dosage
Inside, regardless of food intake. Recommended dose for the treatment of HIV-1 infection: 300 mg once a day.
Recommended tenofovir dosing regimen for renal failure: Creatinine clearance 30-49 ml / min: 300 mg every 48 hours Creatinine clearance 10-29 ml / min: 300 mg every 72-96 hours Hemodialysis: 300 mg every 7 days after the end of the session dialysis.
There are no recommendations on the dosage regimen in patients with creatinine clearance less than 10 ml / min (without hemodialysis).
In case of overdose, the patient should be examined for possible signs of intoxication. If necessary, standard supportive therapy is applied.
Tenofovir is effectively removed by hemodialysis with an extraction rate of approximately 54%. After taking 300 mg of tenofovir, a 4-hour hemodialysis treatment removes approximately 10% of the dose of tenofovir taken.