Kaletra is a combined antiviral drug intended for the treatment of human immunodeficiency virus (HIV).
Release form and composition
Kaletra Dosage Forms:
- Coated tablets (100/25 mg - 60 pcs. In vials of high density polyethylene, 200/50 mg - 120 pcs. In vials of high density polyethylene, 1 bottle per pack);
- Solution for oral administration (in bottles of 60 ml amber colored polyethylene terephthalate complete with a dispenser, 5 sets per carton box).
Active ingredients of the drug:
- Lopinavir: in 1 tablet - 100 or 200 mg, in 1 ml of solution - 80 mg;
- Ritonavir: in 1 tablet - 25 or 50 mg, in 1 ml of solution - 20 mg.
Auxiliary components of tablets: Copovidone K28, sorbitan laurate, colloidal silicon dioxide; the second layer is colloidal silicon dioxide, sodium fumarate.
The composition of the film shell:
- Tablets 100/25 mg: Opadry II pink 85F14399 (titanium dioxide, polyvinyl alcohol, macrogol 3350, talc, iron dye red oxide E172);
- Tablets 200/50 mg: opadry red dye (titanium dioxide, talc, hypromellose 6 mPa, macrogol 3350, hyprolosis, macrogol 400, colloidal silicon dioxide, polysorbate 80, hypromellose 15 mPa, iron dye oxide E172).
Auxiliary components of the solution: sodium saccharinate, levomenthol, sodium citrate, macrogol glycerylhydroxystearate, potassium acesulfame, propylene glycol, sodium chloride, povidone K-30, anhydrous citric acid, glycerol, ethanol, corn syrup with high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with a high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with high fructose, purified water, purified anhydrous, glycerol, ethanol, corn syrup with high fructose, purified water, glycerol, ethanol, purified citrus acid, high fructose citric acid flavoring, flavoring magnasvit 110 (2X), flavor additive synthesized.
Indications for use
Kaletra is used in combination therapy for HIV infection in adults and children over 6 months of age.
- Children age up to 6 months - for solution, up to 3 years - for tablets;
- Severe liver failure;
- The need for simultaneous use astemizole, terfenadine, midazolam, triazolam, cisapride, pimozide, ergot alkaloid (e.g., ergotamine and dihydroergotamine, ergometrine and metilergometrina), lovastatin, simvastatin, Hypericum perforatum drugs, rifampicin, voriconazole;
- Hypersensitivity to any component of the drug.
During the treatment period, the elderly and patients diagnosed with mild and moderate liver failure, viral hepatitis B and C, cirrhosis of the liver, increased liver enzymes, dyslipidemia, hemophilia A and B should be under special observation.
Dosing and Administration
Both dosage forms are for oral administration. Tablets can be taken without reference to meals, solution - during meals.
The recommended dose for adults and children over 12 years old (or weighing more than 40 kg) is 400/100 mg (2 tablets of 200/50 or 5 ml of solution) twice a day. Patients who have not previously received antiretroviral therapy, the daily dose can be taken at once.
Children weighing less than 40 kg Kaletra recommended in the form of a solution. Reception frequency - 2 times a day. A single dose depends on the weight of the child:
- 7-10 kg - 1.25 ml;
- 10-15 kg - 1.75 ml;
- 15-20 kg - 2.25 ml;
- 20-25 kg - 2.75 ml;
- 25-30 kg - 3.5 ml;
- 30-35 kg - 4 ml;
- 35-40 kg - 4.75 ml;
- More than 40 kg - 5 ml.
If necessary, Kaletra is prescribed in combination with nelfinavir, nevirapine, amprenavir or efavirenzem. The doses of both drugs in this case are determined by the doctor depending on the choice of remedies.
More than 2% of adult patients have the following side effects:
- The digestive system: diarrhea, flatulence, dyspepsia, abdominal pain, nausea, dysphagia, vomiting;
- Cardiovascular system: arterial hypertension, vascular disorders;
- Musculoskeletal system: myalgia;
- Nervous system: headache, paresthesia, insomnia;
- Skin and subcutaneous tissue: lipodystrophy and rash;
- Endocrine system: amenorrhea, hypogonadism in men;
- Infections: bronchitis;
- Mental disorders: depression, decreased libido;
- Metabolism and nutritional disorders: weight loss, anorexia;
- General disorders: fever, chills, asthenia.
The following side effects are noted in less than 2% of adult patients whose relationship with Kaletra has not been reliably established:
- Immune system: allergic reactions;
- Endocrine system: Cushing's syndrome, hypothyroidism;
- Blood and lymphatic system: anemia, leukopenia, lymphadenopathy;
- Nervous system: dizziness, facial nerve palsy, migraine, ataxia, dyskinesia, cerebral infarction, drowsiness, peripheral neuritis, muscle hypertonia, tremor, taste perversion, neuropathy, convulsions, amnesia, encephalopathy, extrapyramidal syndrome;
- Organs of vision, hearing and vestibular apparatus: visual impairment, dizziness, tinnitus;
- Cardiovascular system: deep vein thrombosis, varicose veins, vasculitis, thrombophlebitis, heart palpitations, orthostatic hypotension, atrial fibrillation, myocardial infarction;
- Digestive system: belching, dry mouth, enterocolitis, esophagitis, enteritis, fecal incontinence, periodontitis, gastritis, stomatitis (including ulcerative), constipation, hemorrhagic colitis, pancreatitis;
- Liver and biliary tract: hepatomegaly, hepatitis, fatty deposits in the liver, cholecystitis, cholangitis, liver pain, jaundice;
- Respiratory system: rhinitis, shortness of breath, increased cough, pulmonary edema, asthma;
- Skin and hypoderm: dryness and discoloration of the skin, alopecia, eczema, swelling of the face, maculopapular rash, acne, changes in the structure of nails, itching, sweating, striae, skin ulcers, seborrhea, exfoliative dermatitis;
- Musculoskeletal system: back pain, muscle weakness, arthrosis, arthralgia, osteonecrosis, changes in the joints;
- Kidneys and urinary tract: nephritis, kidney stones;
- Mental disorders: nervousness, sleep disturbance, anxiety, agitation, apathy, emotional lability, confusion, thinking disorder;
- Metabolism and nutrition disorders: dehydration, vitamin deficiency, lactic acidosis, increased appetite, weight gain, obesity, diabetes;
- Infections: furunculosis, flu-like syndrome, pharyngitis, sinusitis, otitis media, gastroenteritis, sialadenitis, bacterial and viral infections;
- Reproductive system: gynecomastia, breast enlargement, impaired ejaculation, impotence;
- Tumors: cysts and benign skin tumors;
- Common symptoms: malaise, pain in the chest and behind the sternum, general edema, peripheral edema;
- Changes in laboratory parameters: neutropenia, increased activity of ALT, AST, GGT, a decrease in the content of inorganic phosphorus, an increase in the content of total cholesterol, glucose, bilirubin, triglycerides, amylase, uric acid.
The profile of adverse events during the use of Kaletra in children under 12 years of age was similar to that in adults. But rash, diarrhea, vomiting and taste perversion were most common. There are isolated cases of bradyarrhythmias, erythema multiforme, hepatitis and Stevens-Johnson syndrome. From the laboratory indicators, the following changes were observed: thrombocytopenia, neutropenia, a decrease or increase in the concentration of sodium, an increase in the content of total bilirubin, total cholesterol amylase, ACT and ALT.
The experience of acute overdose of Kaletra in humans is absent. There is no specific antidote. Dialysis is ineffective. If necessary, make a gastric lavage and prescribe activated carbon. In the future, the necessary control over vital systems, monitoring the clinical condition of the patient. If necessary, conduct activities aimed at maintaining the life support of the body.
During the period of treatment, it is recommended to refrain from driving vehicles and performing potentially hazardous types of work that require high concentration of attention and speed of reactions.
Lopinavir / ritonavir inhibits CYP3A isoenzyme, therefore simultaneous use of Kaletra with drugs that are metabolized by CYP3A isoenzymes (including immunosuppressants, HMG-CoA reductase inhibitors, dihydropyridine calcium antagonists and sildenafil), can lead to an increase in their concentration in the dihydropyridine calcium antagonists and sildenafil, can lead to an increase in their concentration in the dihydropyridine calcium antagonists and sildenafil, can lead to an increase in their concentration in dihydropyridine calcium antagonists and sildenafil, can lead to an increase in their concentration in the blood, calcium dihydropyridine antagonists of calcium and sildenafil, can lead to an increase in their concentration in the blood, is dihydropyridine calcium antagonists and sildenafil, can lead to an increase in their concentration in the blood. therapeutic action and side effects.
With caution and in minimal doses, rosuvastatin and atorvastatin should be used, because there is a significant increase in their average maximum and total concentrations, which increases the risk of serious side effects, such as myopathy and rhabdomyolysis. Not recommended simultaneous use with lovastatin and simvastatin. If necessary, the appointment of HMG-CoA reductase is recommended to use fluvastatin or pravastatin, since they should not interact with lopinavir and ritonavir.
The drug may increase the concentration of indinavir. When prescribed in a dose of 400/100 mg 2 times / day, a dose reduction of indinavir may be required. In the case of the appointment of Kaletra 1 time per day in such a combination, it should not be used.
The drug should also not be used 1 time per day in combination with amprenavir, nevirapine, nelfinavir, saquinavir, phenytoin, phenobarbital, carbamazepine.
With the combined use of Kaletra with fosamprenavir, there is a decrease in the concentration of lopinavir and fosamprenavir. Adequate doses of two drugs in terms of safety and efficacy for combined use have not been established.
Care should be taken to control the concentration of substances in the blood when using the drug in combination with amiodarone, bepridil, lidocaine, quinidine, digoxin, drugs that extend the QT interval, cyclosporine, tacrolimus and sirolimus, methadone, fluticasone, felodipine, nifedipine and nicardipine.
Caution, in low doses and under the control of adverse events, sildenafil, tadalafil and vardenafil should be used.
It is not recommended to prescribe high doses of itraconazole and ketoconazole in combination with Kaletra, since their serum concentration may increase.
The drug can reduce the concentration of warfarin, phenytoin, cortisol. Not recommended for simultaneous use with voriconazole.
Rifampicin in combination with lopinavir / ritonavir can lead to a worsening of the virologic response and the potential development of Kaletra resistance, the whole class of protease inhibitors, and even to other antiretroviral drugs. For this reason, these drugs should not be combined.
With simultaneous use, the concentration and, as a consequence, the frequency of side effects of trazodone and such anticancer drugs as vinblastine and vincristine may increase.
Patients with impaired renal function, if necessary, the appointment of clarithromycin should reduce its dose.
Kaletra can reduce the therapeutic concentration of atovajona, so an increase in its dose may be required.
When combined with rifabutin for 10 days, the average maximum concentration and total concentration of the drug in the blood plasma increase 3.5 and 5.7 times, respectively. Given these data, the dose of rifabutin should be reduced by at least 75%.
Dexamethasone may decrease the concentration of lopinavir.
Kaletra should not be prescribed in combination with preparations containing St. John's wort, as this combination leads to a decrease in its concentration in plasma, a decrease in therapeutic efficacy and / or development of resistance.
Kaletra can reduce the concentration of ethinyl estradiol in plasma, resulting in a decrease in the effectiveness of oral contraceptives and estrogen-containing patches. Other or additional contraceptive measures should be taken.
Terms and conditions of storage
Tablets should be stored at a temperature of 15-30 ºС, a solution - 2-8 ºС (in a refrigerator). Keep out of the reach of children!
Shelf life of tablets - 4 years, solution - 2 years.