Active ingredient Raltegravir is rapidly absorbed after taking the drug on an empty stomach, Cmax in the blood plasma is reached after about 3 hours. AUC and Cmax increase in proportion to the dose in the dose range from 100 to 1600 mg. The absolute bioavailability of raltegravir is not established. Raltegravir can be taken regardless of the mode of food intake.
With the introduction of 2 times/day, the equilibrium state is reached quickly, approximately 2 days after the start of treatment. The values of AUC and Cmax indicate a minimal cumulation of raltegravir, plasma concentrations in 12 hours indicate a slight cumulation.
In the concentration range from 2 to 10 μmol, the binding of raltegravir to plasma proteins is 83%. Raltegravir easily penetrates the placental barrier. Does not penetrate the BBB.
After ingestion of raltegravir, approximately 51% and 32% are excreted through the intestine and kidneys, respectively. In the stool, only raltegravir is found – the product of the hydrolysis of raltegravir-glucuronide, secreted into bile. In the urine, raltegravir and raltegravir-glucuronide are determined in proportions of approximately 9% and 23% of the administered dose, while in the blood plasma, 70% is raltegravir, and 30% is raltegravir-glucuronide. The main way of metabolism of raltegravir is represented by the process of glucuronidation mediated by the enzyme uridine-diphosphate-glucuronosyltransferase.
Treatment of HIV-1 infection (even if other antiretroviral drugs are ineffective) in combination with other antiretroviral drugs.
Is taken internally. The recommended dose is 400 mg 2 times a day. The maximum dose is 1600 mg/day.
Treatment is performed in combination with other antiretroviral drugs under the supervision of a doctor.
• On the part of the digestive system: diarrhea, nausea, abdominal pain; rarely vomiting, discomfort and pain in the upper abdomen, constipation, dyspepsia, flatulence, gastritis, glossitis, gastroesophageal reflux, hepatitis, hepatomegaly, hyperbilirubinemia, increased activity of AST, ALT, and AP in the serum.
• From the central nervous system and peripheral nervous system: a headache, dizziness, asthenia, weakness; rarely – irritability, peripheral neuropathy, paresthesia, polyneuropathy, drowsiness, depression, insomnia, unusual dreams, feelings of anxiety.
• On the part of the hematopoiesis system: rarely – anemia, incl. macrocytic anemia, neutropenia.
• From the cardiovascular system: rarely – myocardial infarction, palpitations, ventricular extrasystole.
• From the senses: rarely – blurred vision.
• On the part of metabolism: rarely – increased appetite, decrease or increase in body weight, lipomatosis, fat metabolism disorder, diabetes mellitus, hyperglycemia, hyperlactatemia, hyperlipidemia, hypertriglyceridemia.
• From the musculoskeletal system: rarely – arthralgia, myalgia, pain in the extremities, back pain, muscle spasms, myositis, muscle atrophy, increased activity of CK.
• From the urinary system: rarely – toxic nephropathy, nephrotic syndrome, nocturia, pollakiuria, renal failure, tubular necrosis.
• On the part of the reproductive system: rarely – erectile dysfunction, gynecomastia.
• Allergic reactions: hypersensitivity reactions.
• Dermatological reactions: rarely – acquired lipodystrophy, hyperhidrosis, erythema, rash, incl. macular and maculopapular rash, xeroderma, pruritus.
• Other: rarely – a feeling of discomfort in the chest, chills, fever, phlegmon, infections caused by the Herpes simplex virus, nosebleeds.
Child and adolescence under 16; pregnancy, lactation (breastfeeding); increased sensitivity to raltegravir.
Pregnancy and lactation
Contraindicated in pregnancy, lactation (breastfeeding).
Use with caution in patients at risk of developing myopathy, rhabdomyolysis, and increasing the concentration of CK in the blood serum.
At the initial stages of combination therapy with antiretrovirals, HIV-infected patients may develop an inflammatory response to asymptomatic or residual opportunistic infections (cytomegalovirus or pneumocystis pneumonia caused by Pneumocystis jiroveci, tuberculosis or paratuberculosis caused by Mycobacterium avium), which can manifest as a worsening of the clinical condition and strengthening of existing symptoms. Usually, such reactions are observed in the first weeks or months after the initiation of therapy. In such cases, additional diagnostic and therapeutic measures may be required.
Since it is not known whether raltegravir is withdrawn during dialysis, it is not recommended to take a reception on the eve of a dialysis session.
Impact on the ability to drive vehicles and manage mechanisms
Studies on the impact on the ability to drive vehicles and the use of mechanisms have not been conducted. Given the possibility of developing dizziness, weakness, drowsiness and blurred vision in the background of therapy, patients should exercise special care when engaging in potentially hazardous activities.
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