Kaletra - Instructions For Use, Price, Reviews, Tablets, Solution

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Kaletra

Kaletra: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Kaletra

ATX code: J05AE06

Active ingredient: lopinavir + ritonavir (lopinavir + ritonavir)

Manufacturer: ABBOTT (USA)

Description and photo update: 2019-16-08

Prices in pharmacies: from 8440 rubles.

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Kaletra is an antiviral agent that is active against human immunodeficiency virus infection.

Release form and composition

Dosage forms:

• Solution for oral administration: transparent liquid of yellow or light yellow color (60 ml each in amber bottles made of polyethylene terephthalate, complete with a dispenser, in a cardboard box of 5 bottles and dispensers);
• Film-coated tablets: oval with the Abbott logo engraved on one side and the letters “AL” on the red tablets or “AC” on the pale pink (120 tablets with “AL” engraving), "AC" 60 pcs in bottles made of high-density polyethylene, in a cardboard box 1 bottle).

The active ingredients of Kaletra are lopinavir and ritonavir, their content (respectively):

• 1 ml of solution - 80 mg and 20 mg;
• 1 red tablet with "AL" engraving - 200 mg and 50 mg;
• 1 pale pink tablet with "AC" engraving - 100 mg and 25 mg.

Auxiliary components:

• Solution: sodium chloride, macrogol glyceryl hydroxystearate, sodium citrate, potassium acesulfame, sodium saccharinate, citric acid anhydrous, propylene glycol, ethanol, levomenthol, glycerol, povidone K-30, corn syrup with high fructose content, menthol oil, flavoring agent (110, synthesized flavoring additive, vanilla flavoring, purified water;
• Tablets: copovidone K28, sorbitan laurate, colloidal silicon dioxide, sodium stearyl fumarate.

Additionally, as part of the film coating of tablets:

• Red tablets with “AL” engraving: opadry red dye - titanium dioxide, polysorbate 80, hypromellose 6 mPa, macrogol 400, hypromellose 15 mPa, hyprolose, talc, macrogol 3350, colloidal silicon dioxide, iron oxide dye (E172);
• Pale pink tablets with "AC" engraving: opadry II pink 85F14399 - macrogol 3350, polyvinyl alcohol, talc, titanium dioxide, iron oxide red (E172).

Pharmacological properties

Pharmacodynamics

Mechanism of action

Kaletra is a combination drug that contains ritonavir and lopinavir.

Lopinavir is a protease inhibitor of HIV-1 and HIV-2 of the human immunodeficiency virus (HIV). Provides antiviral effect. Due to the mechanism of HIV protease inhibition, Kaletra inhibits the synthesis of viral proteins and prevents the cleavage of the gag-pol polypeptide. This is the reason for the formation of an immature virus that is incapable of infection.

Ritonavir is an inhibitor of the CYP3A isoenzyme mediated metabolism of lopinavir in the liver (the concentration of the latter in the blood plasma increases). In addition, ritonavir inhibits HIV protease.

Resistance

In vitro isolates of HIV-1 were isolated with reduced sensitivity to lopinavir. In vitro, the presence of ritonavir did not alter the release of lopinavir-resistant viruses.

In a clinical trial involving antiretroviral (ARV) therapy in 37 previously untreated patients, viral isolates with plasma HIV RNA levels exceeding 400 copies / ml were analyzed at 24, 32, 40 and / or 48 weeks. All evaluated patients treated with ritonavir / lopinavir showed no signs of phenotypic or genotypic resistance to ritonavir / lopinavir. Ritonavir / lopinavir resistance has also not been identified in children who have not previously received ARV treatment.

At the second stage, clinical trials of the drug were carried out with the involvement of 227 HIV-infected patients who had previously received or not received antiretroviral treatment. In 4 out of 23 patients with virological ineffectiveness of therapy (more than 400 copies of HIV RNA / ml), sensitivity to lopinavir decreased after 12–100 weeks of Kaletra use. At the same time, 3 out of 4 patients had previously taken any HIV protease inhibitor (saquinavir, indinavir, or nelfinavir), 1 out of 4 patients underwent combination therapy with indinavir, ritonavir and saquinavir. All 4 patients had at least 4 mutations associated with resistance to HIV protease inhibitors prior to Kaletra use. A further increase in viral load is due to the appearance of additional mutations,which are associated with resistance to HIV protease inhibitors. This information is insufficient to identify the mutations responsible for the emergence of lopinavir resistance.

Cross-resistance

There is insufficient data on the occurrence of cross-resistance with ritonavir / lopinavir treatment.

The virological response to ritonavir / lopinavir was altered in the presence of three or more of the following amino acid substitutions in the HIV protease gene: K20M / N / R, L10F / I / R / V, L33F, L24I, I47V, M36I, I54L / T / V, G48V, I84V, V82A / C / F / S / T. In an in vitro clinical study, the value of lopinavir sensitivity reduction based on the virological response to ritonavir / lopinavir treatment was investigated in relation to the parental genotype and phenotype of the virus. The study (М98-957) was conducted with the involvement of 56 patients with HIV RNA more than 1000 copies / ml, who were previously prescribed therapy with indinavir, nelfinavir, ritonavir and saquinavir. These patients were taking one of the recommended doses of ritonavir / lopinavir in combination with nucleoside reverse transcriptase inhibitors and efavirenz. Before starting treatment, EC concentration₅₀ lopinavir (drug concentration that suppresses replication of 50% of viruses) for 56 different virus strains was 0.5–96 times higher than the EC ₅₀ concentration effective against wild-type virus. At the same time, 31 out of 56 strains (55%) of the virus showed a decrease in sensitivity to lopinavir by 4 times or more. On average, for 31 strains, the sensitivity decreased by 27.9 times.

48 weeks after the first dose of ritonavir / lopinavir, nucleoside reverse transcriptase inhibitors and efavirenz, HIV RNA concentration less than 400 copies / ml was recorded in 25% (2 out of 8), 73% (11 out of 15) and 93% (in 25 out of 15 27) patients with a decrease in the initial sensitivity to lopinavir, respectively, ≥ 40 times, 10–40 times and ≤ 10 times. The concentration of HIV RNA less than 50 copies / ml in these groups was 25% (2/8), 60% (9/15) and 81% (22/27) of patients, respectively.

There is insufficient evidence to identify mutations that cause lopinavir resistance.

Pharmacokinetics

Absorption

The pharmacokinetics of lopinavir in combination with ritonavir has been studied in HIV-infected patients and healthy volunteers. No significant differences were found between these two groups. Lopinavir is almost completely metabolized by the CYP3A isoenzyme, and the use of ritonavir inhibits the metabolism of lopinavir, causing an increase in its plasma concentration. When a combination of lopinavir / ritonavir was used at a dose of 400/100 mg 2 times a day, the mean equilibrium plasma concentration of lopinavir in HIV-infected patients exceeded the mean equilibrium concentration of ritonavir by 15–20 times. At the same time, the plasma content of ritonavir was less than 7% of its concentration when ritonavir was taken at a dose of 600 mg 2 times a day. In vitro EC _{50 of} lopinavir is approximately 10 times less than EC₅₀ ritonavir. Therefore, lopinavir determines the antiviral activity when ritonavir and lopinavir are taken together.

In a pharmacokinetic study in which HIV-positive patients (n = 19) took part, a combination of 400/100 mg lopinavir / ritonavir was administered with food for 3 weeks 2 times a day. The average maximum concentration of lopinavir in blood plasma (C _max) was 9.8 ± 3.7 μg / ml, and the time to reach C _max was about 4 hours. Before the morning dose, the mean equilibrium concentration was 7.1 ± 2.9 μg / ml. Within the dosing interval, the minimum concentration was 5.5 ± 2.7 μg / ml. For lopinavir, the area under the concentration-time pharmacokinetic curve (AUC) for 0.5 days after taking Kaletra averaged 92.6 ± 36.7 μg · h / ml. In combination with ritonavir, the absolute bioavailability of lopinavir has not been established.

Effect of food on absorption

With oral administration of lopinavir / ritonavir solution and fatty foods (872 kcal, 56% of calories are provided due to fat) C _max and AUC of lopinavir increased by 56% and 130%, respectively, compared with similar characteristics when taken on an empty stomach. To increase bioavailability and minimize the variability of pharmacokinetics, the solution is recommended to be used during meals.

Distribution

In the equilibrium state, 98–99% of lopinavir binds to blood plasma proteins. Lopinavir binds to albumin and alpha 1-acid glycoprotein (a higher affinity is observed for the latter). Plasma protein binding at steady state remains constant in the range of concentrations recorded after taking lopinavir / ritonavir at a dose of 400/100 mg 2 times a day. This indicator is comparable in HIV-positive patients and healthy volunteers.

Metabolism

In vitro, lopinavir is metabolized mainly by exposure to the CYP3A isoenzyme of the liver cytochrome P ₄₅₀ system. Since ritonavir is a potent inhibitor of the CYP3A isoenzyme that inhibits the metabolism of lopinavir, taking a combination of ritonavir and lopinavir increases the plasma concentration of the latter. After a single administration of ¹⁴ C-labeled lopinavir / ritonavir at a dose of 400/100 mg, 89% of the radioactivity is provided by the parent drug. In the human body, 13 metabolites of lopinavir have been identified. Induction of cytochrome P ₄₅₀ isoenzymesritonavir provides the induction of its own metabolism. With long-term use, the concentration of lopinavir before taking the next dose decreased over time, stabilizing after about 10-16 days.

Withdrawal

8 days after the application of 400/100 mg of ¹⁴ C-labeled lopinavir / ritonavir, approximately 82.6 ± 2.5% and 10.4 ± 2.3% of the taken ¹⁴ C-lopinavir are detected, respectively, in feces and urine. The share of unchanged lopinavir is 19.8% and 2.2%, respectively. After prolonged use, less than 3% of the dose of lopinavir taken unchanged is excreted through the kidneys. When taken orally, the clearance of lopinavir (CL / F) is 5.98 ± 5.75 L / h.

Taking Kaletra 1 time per day

The once-daily pharmacokinetics of lopinavir / ritonavir was evaluated in HIV-infected patients who had not previously taken antiretroviral drugs. In the case of long-term (over 4 weeks) daily use of 800/200 mg of lopinavir / ritonavir in combination with 200 mg of emtricitabine and 300 mg of tenofovir once a day in combination with a meal, the mean maximum plasma concentration of lopinavir was 11.8 ± 3, 7 μg / ml, and the time to reach C _max is about 6 hours. Before applying the morning dose, the mean equilibrium concentration of lopinavir was 3.2 ± 2.1 μg / ml, the value of the minimum concentration of lopinavir within the 24-hour dosing interval was 1.7 ± 1.6 μg / ml. When taken once a day, the AUC of lopinavir averaged 154.1 ± 61.4 μg h / ml.

Special patient groups

In elderly patients, the pharmacokinetics of lopinavir have not been studied. There were no significant pharmacokinetic differences depending on the sex or race of adult patients.

During the study of the use of Kaletra in children with the involvement of 53 patients aged 0.5–12 years, the pharmacokinetics of lopinavir / ritonavir was studied when taken twice a day at 300/75 or 230 / 57.5 mg / m ². When double application 230 / 57.5 mg / m ² of lopinavir / ritonavir 300/75 or without nevirapine mg / m ² of lopinavir / ritonavir with nevirapine lopinavir plasma fixed concentration similar to those in adult patients twice daily was prescribed 400 / 100 mg lopinavir / ritonavir without nevirapine. Single daily use of lopinavir / ritonavir in children has not been studied.

The average equilibrium C _max, C _min and AUC of lopinavir after taking 230 / 57.5 mg / m ² lopinavir / ritonavir 2 times a day without nevirapine (n = 12) were 8.2 ± 2.9 μg / ml, respectively. 3.4 ± 2.1 μg / ml and 72.6 ± 31.1 μg h / ml. In the case of a double dose of 300/75 mg / m2 ^of lopinavir / ritonavir and nevirapine (n = 12), these indicators were, respectively, 10 ± 3.3 μg / ml, 3.6 ± 3.5 μg / ml and 85.8 ± 36.9 μg h / ml. The following regimens for taking nevirapine were observed: 2 times a day, 4 mg / kg (for patients over 8 years old) and 7 mg / kg (for patients 0.5–8 years old).

In patients with renal insufficiency, the pharmacokinetics of lopinavir has not been studied, however, due to the insignificant renal clearance, the probability of a decrease in the total clearance for this category is low.

The metabolism and excretion of lopinavir is mainly carried out by the liver. Long-term use of 400/100 mg lopinavir / ritonavir 2 times a day in patients with mild and moderate hepatic insufficiency, simultaneously infected with hepatitis C virus and HIV, provided an increase in lopinavir AUC by 30% and C _max - by 20% (in comparison with therapy in HIV-infected patients with normal liver function). In patients with hepatic impairment, binding to blood plasma proteins is lower (99.09%) than in the control groups (99.31%). The pharmacokinetics of lopinavir / ritonavir in patients with severe hepatic impairment have not been studied.

In the course of pharmacokinetic studies, a slight decrease in C _max and AUC of lopinavir in pregnant patients in the III trimester compared with the II trimester was revealed.

In the second trimester, in HIV-infected pregnant patients who were prescribed 400/100 mg of lopinavir / ritonavir in film-coated tablets 2 times a day, the following pharmacokinetic parameters were recorded:

• AUC _0–12 - 68.7 μg · h / ml (variation coefficient 20.6%);
• C _max - 7.9 μg / ml (variation coefficient 21.1%);
• the concentration of the drug in the blood before taking the next dose (Cpredose) - 4.7 μg / ml (variation coefficient 25.2%).

In the third trimester, in HIV-infected pregnant patients who were prescribed 400/100 mg of lopinavir / ritonavir in film-coated tablets 2 times a day, the following pharmacokinetic parameters were recorded:

• AUC _0–12 - 61.3 μg · h / ml (variation coefficient 22.7%);
• C _max - 7.5 μg / ml (variation coefficient 18.7%);
• Cpredose - 4.3 μg / ml (variation coefficient 39%).

In the postpartum period, in HIV-infected pregnant patients who were prescribed 400/100 mg of lopinavir / ritonavir in film-coated tablets 2 times a day, the following pharmacokinetic parameters were recorded:

• AUC _0–12 - 94.3 μg · h / ml (variation coefficient 30.3%);
• C _max - 9.8 μg / ml (variation coefficient 24.3%);
• Cpredose - 6.5 μg / ml (variation coefficient 40.4%).

Drug interactions

In vitro, lopinavir / ritonavir is an inhibitor of the CYP3A isoenzyme. In the case of the simultaneous use of lopinavir / ritonavir and drugs metabolized by this isoenzyme, the concentration of such drugs in the blood plasma may increase, and their side or therapeutic effects may be enhanced or prolonged.

Lopinavir / ritonavir at therapeutic concentrations does not inhibit the isoenzymes CYP2C9, CYP2D6, CYP2E1, CYP2C19, CYP1A2, or CYP2B6.

In vivo, lopinavir / ritonavir induces its own metabolism, enhancing the biotransformation of some drugs that are metabolized by enzymes of the cytochrome P _{450 system} and by glucuronidation.

Since the CYP3A isoenzyme is involved in the metabolism of lopinavir / ritonavir, taking drugs that induce the activity of this isoenzyme can lead to an increase in lopinavir clearance, which in turn helps to reduce the plasma concentration of lopinavir. Concomitant use of lopinavir / ritonavir with other inhibitors of the isoenzyme CYP3A may be accompanied by an increase in plasma concentrations of lopinavir.

Indications for use

According to the instructions, Kaletra is indicated as part of a combination therapy for acquired human immunodeficiency syndrome (HIV infection) in adults and children.

Contraindications

• Breastfeeding period;
• Severe liver failure;
• Concomitant use with voriconazole, terfenadine, astemizole, triazolam, midazolam, cisapride, ergot alkaloids (for example, ergometrine and methylergometrine, ergotamine and dihydroergotamine), pimozide, lovastatin, preparations of St. John's wort, ryfovastatin
• Hypersensitivity to drug components.

It is recommended to prescribe Kaletra with caution to patients with cirrhosis of the liver, viral hepatitis B and C, mild to moderate liver failure, increased liver enzyme activity, hemophilia A and B, dyslipidemia (including hypercholesterolemia, hypertriglyceridemia), as well as patients over 65 years of age.

During pregnancy, the appointment of Kaletra is possible if the intended benefit outweighs the possible risk to the fetus and mother.

Cannot be applied:

• Solution: in infants up to 6 months;
• Tablets: for children under 3 years of age.

Patients with severe renal insufficiency should take Kaletra tablets with caution.

Instructions for the use of Kaletra: method and dosage

• Tablets: taken orally, swallowing only whole (cannot be broken or chewed), regardless of food intake. Recommended dosage for adults: 400/100 mg 2 times a day or 800/200 mg 1 time a day for patients who have not previously received antiretroviral therapy; patients who previously received antiretroviral therapy - 400/100 mg 2 times a day, it is not recommended to prescribe a single daily dose. If a patient suspects a decrease in sensitivity to lopinavir, confirmed by laboratory or clinically, it is necessary to increase the dose of Kaletra to 500/125 mg (2 pcs. 200/50 mg and 1 pc. 100/25 mg or 5 pcs. 100/25 mg) when combined with nevirapine, efavirenz, nelfinavir, or amprenavir. Children weighing more than 35 kg or with a body surface area of more than 1.4 sq.m.the recommended dosage is 400/100 mg 2 times daily without concomitant use of nevirapine, efavirenz, amprenavir, or nelfinavir. Children weighing less than 35 kg and a body surface area of up to 0.6 square meters. the doctor calculates the dose according to a special scheme individually. Children with a body surface area of less than 0.6 sq. M. it is recommended to take Kaletra solution;
• Solution: taken orally with meals. Recommended dosage for adults: 5 ml of solution 2 times a day or 10 ml 1 time a day for patients who have not previously taken antiretroviral drugs; for patients receiving antiretroviral therapy - 5 ml of solution 2 times a day, this category of patients is not recommended to prescribe a single daily dose. In the case of a suspected decrease in sensitivity to lopinavir, it is recommended to increase the dose of Kaletra to 6.5 ml 2 times a day when combined with nevirapine or efavirenz. Dosage for children is determined by the doctor according to a special scheme by calculation, it depends on the drug combination, sensitivity to lopinavir, weight and age of the child. A single dose of the solution for children weighing up to 15 kg is determined at the rate of 12/3 mg per 1 kg of the child's weight, and 10/2,5 mg per 1 kg - for children from 15 to 40 kg. Reception of the calculated volume of the solution is prescribed 2 times a day. The daily dose for children weighing more than 40 kg should not exceed 5 ml of solution 2 times a day.

Dose adjustment of Kaletra is not required with the simultaneous use of ranitidine and omeprazole.

When combined therapy of adults with nevirapine, efavirenz, nelfinavir, amprenavir, Kaletra cannot be prescribed once a day, and for a dose of 400/100 mg twice a day, no correction is required.

The use of the drug in children 1 time per day has not been studied.

Side effects

In more than 2% of adult patients, the use of Kaletra causes serious and moderate side effects:

• General disorders: fever, asthenia, chills;
• From the digestive system: diarrhea, abdominal pain, dyspepsia, nausea, flatulence, vomiting, dysphagia;
• From the nervous system: insomnia, headache, paresthesia;
• From the side of the cardiovascular system: arterial hypertension, vascular disorders;
• Mental disorders: depression, decreased libido;
• On the part of the skin and subcutaneous tissue: rash, lipodystrophy;
• From the side of metabolism and nutritional disorders: weight loss, anorexia;
• From the musculoskeletal system: myalgia;
• Infections: bronchitis;
• From the endocrine system: amenorrhea, hypogonadism in men.

During the period of Kaletra use, some (less than 2%) adult patients experienced the following side effects, but their relationship with the drug intake has not been established:

• General symptoms: malaise, chest and chest pain, general and peripheral edema;
• Nutrition and metabolic disorders: dehydration, vitamin deficiency, diabetes mellitus, lactic acidosis, increased appetite, weight gain, obesity;
• From the lymphatic system and blood: leukopenia, anemia, lymphadenopathy;
• From the side of the cardiovascular system: varicose veins, palpitations, atrial fibrillation, deep vein thrombosis, myocardial infarction, orthostatic hypotension, vasculitis, thrombophlebitis;
• From the liver and biliary tract: cholecystitis, cholangitis, hepatitis, fatty deposits in the liver, hepatomegaly, jaundice, liver functional disorders;
• Infections: furunculosis, flu-like syndrome, gastroenteritis, otitis media, bacterial infections, pharyngitis, sinusitis, sialadenitis, viral infections;
• From the immune system: allergic reactions;
• From the endocrine system: hypothyroidism, Cushing's syndrome;
• From the nervous system: dizziness, drowsiness, neuropathy, amnesia, cerebral infarction, ataxia, convulsions, encephalopathy, dyskinesia, extrapyramidal syndrome, muscle hypertonicity, tremor, paralysis of the facial nerve, peripheral neuritis, migraine, perversion or loss of taste;
• Mental disorders: anxiety, sleep disturbance, apathy, agitation, confusion, nervousness, emotional lability, impaired thinking;
• From the side of the organ of vision: visual impairment;
• From the vestibular apparatus and the organ of hearing: dizziness, tinnitus;
• From the respiratory system: shortness of breath, asthma, rhinitis, increased cough, pulmonary edema;
• From the digestive system: dry mouth, belching, constipation, enterocolitis, enteritis, esophagitis, gastritis, fecal incontinence, hemorrhagic colitis, stomatitis and ulcerative stomatitis, periodontitis, pancreatitis;
• Skin and subcutaneous tissue disorders: dry skin, itching, alopecia, acne, eczema, facial edema, exfoliative dermatitis, maculopapular rash, seborrhea, skin discoloration, stretch marks, skin ulcers, sweating, changes in the structure of nails;
• From the kidneys and urinary tract: nephritis, kidney stones;
• Malignant, benign and unspecified tumors: benign skin tumors, cysts;
• Reproductive system disorders: impotence, gynecomastia, breast enlargement, ejaculation disorder;
• From the musculoskeletal system: back pain, muscle weakness, arthralgia, osteonecrosis, arthrosis, changes in the joints;
• Changes in laboratory parameters: an increase in total cholesterol and bilirubin, glucose, triglycerides, amylase, uric acid, an increase in the activity of alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyl transpeptidase (GGT), neutropenia, a decrease in the level of inorganic phosphorus.

Adverse events in children from 6 months to 12 years old were similar to those in adults, most often there were perversions of taste, rash, vomiting, diarrhea.

There were also isolated cases of Stevens-Johnson syndrome, hepatitis, bradyarrhythmia, erythema multiforme.

Overdose

There are data on cases of overdose of Kaletra solution for oral administration. In case of accidental overdose in premature infants, the following side effects were observed: cardiomyopathy, complete atrioventricular block, acute renal failure, lactic acidosis. The solution contains propylene glycol 15.3% (w / v) and ethanol (42.4% v / v), therefore, to prevent overdose of lopinavir / ritonavir, the exact calculation of the dose of the drug should be done very carefully (especially when it is prescribed to infants and young children).

Clinical data on acute overdose of lopinavir / ritonavir are limited. There is no specific antidote. Therapy involves carrying out measures to maintain the life support of the body, including monitoring the vital functions of the body and the clinical condition of the patient. If necessary, gastric lavage and the use of activated carbon are prescribed.

Since the plasma protein binding of lopinavir / ritonavir is high, dialysis is impractical. In this case, in case of an overdose of Kaletra solution, dialysis can be prescribed to remove propylene glycol and ethanol.

special instructions

With extreme caution, it is recommended to prescribe the simultaneous use of any intranasal and inhaled glucocorticosteroids (GCS), since there is a high risk of developing systemic side effects. If it is necessary to use GCS for a long time, it is advisable to prescribe their other form.

When combined with tadalafil, sildenafil or vardenafil, their concentration in the blood plasma increases, this can lead to arterial hypotension and prolonged erection.

Kaletra must be taken in a standard dose within 10 days prior to the appointment of rifampicin, since their simultaneous administration causes a dose-dependent decrease in the concentration of lopinavir in the blood plasma. Then, under close control of liver function, titration of the dose of Kaletra upwards is possible.

In patients with functional disorders of the liver, the concentration of active substances in the plasma increases, therefore, their treatment must be carried out under regular careful monitoring of laboratory parameters, including the activity of AST, ALT.

While taking protease inhibitors in patients, cases of hyperglycemia, diabetic ketoacidosis and decompensation of diabetes mellitus were observed, but their relationship and frequency have not been clinically established.

In patients with progressive HIV infection, treatment with Kaletra increases the likelihood of developing pancreatitis and hypertriglyceridemia, or the risk of exacerbation in patients with a history of pancreatitis.

Various degrees of severity of cross-resistance of protease inhibitors are noted, and studies of the effect of Kaletra on the effectiveness of other protease inhibitors during subsequent therapy are continuing.

Therapy with protease inhibitors causes cases of bleeding, spontaneous formation of subcutaneous hematomas, the development of hemarthrosis in patients with hemophilia types A and B.

Against the background of the use of the drug, patients may experience external changes associated with cushingoid and an increase in the mammary glands, redistribution or accumulation of fat deposits in the back and neck with a simultaneous decrease in fat on the face and limbs.

Before starting the use of Kaletra and the entire period of therapy, the level of cholesterol and triglyceride concentrations should be regularly monitored, in the case of lipid disorders, the appointment of appropriate drugs is indicated.

At the beginning of combination antiretroviral therapy with Kaletra, patients may experience exacerbations of residual or asymptomatic opportunistic infections, which necessitate additional examination and treatment.

Patients should be informed about the need to see a doctor if they develop stiffness and pain in the joints, impaired motor function, since these signs may be associated with the development of osteonecrosis.

Given the incidence of concomitant diseases, decreased kidney, liver or heart function and concomitant therapy in patients over 65 years of age, Kaletra should be used with caution in patients of this category.

During the period of therapy, patients are prohibited from driving vehicles and mechanisms and other potentially hazardous activities, the implementation of which requires concentration of attention and a high speed of psychomotor reactions.

Application during pregnancy and lactation

During pregnancy, it is prohibited to use Kaletra once a day.

The effect of lopinavir / ritonavir pill was evaluated in 3366 pregnant women. Research data indicate that taking the drug does not lead to serious congenital malformations in comparison with the initial frequency of their occurrence. If needed, lopinavir / ritonavir tablets can be used during pregnancy.

Kaletra in the form of a solution can be used in pregnant women if the expected benefit to the mother is higher than the potential risk to the fetus.

During lactation, when taking Kaletra, you must stop breastfeeding.

Pediatric use

It is forbidden to use Kaletra tablets for the treatment of patients under the age of 3 years (for children 0.5–3 years old, the drug is prescribed in the form of a solution for oral administration). Also, tablets are not allowed to be used to treat patients under the age of 18 in the 1 time per day regimen.

Kaletra in the form of a solution for oral administration is contraindicated for the treatment of patients under the age of 6 months, and should be used with caution under the age of 18 years.

With impaired renal function

In case of renal failure, Kaletra solution should be used with caution, and tablets - without restrictions.

For violations of liver function

In severe hepatic impairment, Kaletra is contraindicated. With mild to moderate liver failure, as well as with liver cirrhosis, the drug should be used with caution.

Use in the elderly

When treating elderly patients (from 65 years), Kaletra should be used with caution.

Drug interactions

The oncologist prescribes the drugs taken simultaneously, taking into account the high activity of the active substances of Kaletra, their dose and the patient's age.

Analogs

Analogs of Kaletra are: Aluvia, Lopitsip, Emletra, Baraklud, Viktrelis, Virodin, Lamivudin, Viracept, Indivir-400, Lopitsip, Nelvir, Olisio, Reataz, Ritam, Telzir.

Terms and conditions of storage

Store at temperature: solution - 2-8 ° C, tablets - 15-30 ° C. Keep out of the reach of children.

Shelf life: solution - 2 years, tablets - 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Kaletra

Reviews of Kaletra are ambiguous: some patients report good tolerance and high efficacy of the drug, others about the development with prolonged use of negative phenomena (obesity, headaches, destruction of joints, etc.).

Price for Kaletra in pharmacies

The approximate price for Kaletra is 3950–4890 rubles. for 120 tablets of 200/50 mg.

Kaletra: prices in online pharmacies

Drug name Price Pharmacy

Kaletra 200 mg + 50 mg film-coated tablets 120 pcs. RUB 8440 Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!