Kaletra is a combined antiviral drug. Its main components are lopinavir and ritonavir. Lopinavir is a drug belonging to an inhibitor of the HIV-1 and HIV-2 protease. These are the proteases of the human immunodeficiency virus (HIV). It stimulates the antiviral activity of this drug. The outcome of this substance is the formation if inactive virus unable to damage human cells. Ritonavir inhibits CYP3A4 isoenzyme. It leads to an increase in the lopinavir concentration in blood plasma. Ritonavir is also an HIV protease inhibitor.
Kaletra is applied as the HIV infection treatment. It is prescribed in adults and children over 3 years of age. The main route of administration is combination therapy.
Dosage and administration
The dose is defined depending on the individual case. The patient’s condition is taken into account. Your physician will assess your state and prescribe the right dosage.
In what cases this medicine is contraindicated?
Hypersensitivity to lopinavir, ritonavir;
Severe liver failure;
Children’s age up to 3 years (children from 6 months to 3 years old are prescribed a drug in the dosage form for oral administration);
The use of tKaletra 1 time/day in children and adolescents under 18 years of age;
The use of lopinavir/ritonavir 1 time/day in pregnant women.
What side effects may appear after taking this medicine?
The immune system: often – hypersensitivity reactions, incl. urticaria and angioedema; infrequently – a syndrome of restoration of immunity.
The digestive system: very often – diarrhea, nausea; often – vomiting, abdominal pain (in the upper and lower sections), gastroenteritis, colitis, dyspepsia, pancreatitis, gastroesophageal reflux, hemorrhoids, flatulence, bloating, hepatitis, hepatomegaly, cholangitis, liver steatosis; infrequently – constipation, stomatitis, ulcers of the oral mucosa, duodenitis, gastritis, gastrointestinal bleeding (including rectal bleeding), dry mouth, ulcers of the stomach and intestines, fecal incontinence.
The cardiovascular system: often – arterial hypertension; infrequently – atherosclerosis, myocardial infarction, AV block, tricuspid valve insufficiency, deep vein thrombosis; frequency unknown – increased PR interval.
The skin and subcutaneous fat: often – a rash (including maculopapular), dermatitis, eczema, seborrhea, increased sweating at night, itching; infrequently – alopecia, capillary, vasculitis; frequency is unknown – lipodystrophy and redistribution of subcutaneous fat.
The musculoskeletal system: often – musculoskeletal pain (including arthralgia and back pain), myalgia, muscle weakness, muscle spasms; infrequently – rhabdomyolysis, osteonecrosis.
Metabolic disorders and disorders of the endocrine system: often – hypercholesterolemia, hypertriglyceridemia, weight loss, decreased appetite, diabetes mellitus; infrequently – weight gain, lactic acidosis, increased appetite, male hypogonadism; frequency unknown – insulin resistance.
The kidneys and urinary tract: often – renal failure; infrequently – hematuria, nephritis.
The reproductive system: often – erectile dysfunction, amenorrhea, menorrhagia.
The hemopoietic system: often – anemia, leukopenia, neutropenia, lymphadenopathy.
The sensory organs: infrequently – vestibular dizziness, tinnitus, visual impairment.Infections: very often – upper respiratory tract infections; often – infections of the lower respiratory tract, infections of the skin and subcutaneous fat, including cellulitis, folliculitis, furunculosis.
General reactions: often – weakness, asthenia.
It is recommended to follow such requirements as:
the simultaneous use of drugs that clearance is significantly dependent on metabolism through the CYP3A isoenzyme. These are the following drugs astemizole, blonanserin, terfenadine, midazolam (when taken orally), triazolam, cisapride, pimozide, salmeterol, sildenafil, tadalafil, vardenafil, avanafil, voriconazole, ergot alkaloids (eg, ergotamine and dihydroergotamine, ergometrine and methylergometrine), HMG-CoA reductase inhibitors (lovastatin, simvastatin, atorvastatin,) alfuzosin, fusidic acid (in the treatment of skin infections), amiodarone, quetiapine;
the simultaneous use with St. John’s wort, boceprevir, simeprevir;simultaneous use with ketoconazole and itraconazole in high doses (more than 200 mg/day);
the simultaneous use of a daily recommended dose of Kaletra with rifampicin;
the simultaneous use of this drug and tipranavir with a low dose of ritonavir;
the use of generic Kaletra 1 time/day in combination with carbamazepine, phenobarbital or phenytoin;
the use of this generic drug 1 time/day in combination with the drugs efavirenz, nevirapine, amprenavir or nelfinavir.
What are overdose symptoms and treatment options?
The clinical experience of acute overdose of lopinavir/ritonavir (Generic Kalera) in humans is fully explored.
There is no antidote. Treatment should include general supportive care, including monitoring the patient’s vital indicators and clinical status. If necessary, unabsorbed drug is excreted through gastric lavage. Activated charcoal is prescribed. Because lopinavir/ritonavir is highly bound to plasma proteins, the use of dialysis is impractical.