Kaletra (Lopinavir and Ritonavir)

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Kaletra is a combination drug that contains lopinavir and ritonavir. Lopinavir belongs to an inhibitor of HIV-1 and HIV-2 protease of the human immunodeficiency virus (HIV). It provides antiviral activity of Kaletra. HIV proteases’ suppression inhibits the synthesis of viral proteins. It contributes to the formation the inability of the virus to reproduce.

Ritonavir belongs to a group of an HIV-1 and HIV-2 aspartyl protease inhibitors. It is intended for oral administration. It is an active peptidomimetic. The HIV proteases’ inhibition prevents the cleavage of the bond by a group-specific antigen polymerase (gag-pol) polyprotein. It also contributes to the formation of the virus not deteriorating for the human body. Ritonavir has a selective affinity for HIV protease. This substance shows little activity against human aspartyl protease.

In what cases this medicine is prescribed?

Generic Kalentra is prescribed as treatment of HIV infection in adults and children from 3 years of age. It is used as a part of combination therapy.

How to take this medicine?

Tablets are intended for oral administration, regardless of food intake; swallow as a whole.

Tablets 200mg + 50mg: for patients who have not previously taken antiretroviral therapy, the recommended dose of Kaletra is 400/100 mg (2 tablets) 2 times/day or 800/200 mg (4 tablets) 1 time/day.

For patients who have previously taken antiretroviral therapy, the recommended Kaletra dose is 400/100 mg (2 tablets) 2 times/day. The use of the drug 1 time/day in these patients has not been studied, therefore, it is not recommended.

What should me healthcare professional know before I take this medicine?

Your healthcare professional should know about:

  • severe liver failure;
  • children’s age up to 3 years (children from 6 months to 3 years of age are prescribed a drug in the form of an oral solution);
  • hypersensitivity to lopinavir, ritonavir or to additional components of Kaletra.

Possible side effects caused by Kaletra

  • Immune system: infrequently – hypersensitivity reactions; seldom – a syndrome of restoration of immunity.
  • Digestive system: very often – diarrhea; often – abdominal pain, flatulence, nausea, vomiting, irregular stools; infrequently – dyspepsia, abdominal discomfort, dry mouth, hemorrhagic enterocolitis, fecal incontinence, gastritis, gastroesophageal reflux, pancreatitis, hepatitis; rarely – dysphagia, pain in the lower abdomen, constipation, duodenitis, enterocolitis, enteritis, belching, esophagitis, gastric ulcer, hemorrhoids, mouth ulcers, periodontitis, rectal bleeding, stomatitis, hepatomegaly, cholecystitis, jaundice, liver steatosis and liver pain ; less than 2% – cholangitis.
  • Nervous system: often – headache; infrequently – insomnia, paresthesia, decreased libido, depression, sleep disturbance, anxiety, nervousness, dizziness, peripheral neuropathy, drowsiness, perversion of taste; rarely – excitement, confusion, emotional lability, disorientation, thinking disorders, amnesia, ataxia, dyskinesia, encephalopathy, extrapyramidal syndrome, facial paresis, muscle tone, migraine, neuropathy, loss of taste and tremor; less than 2% – apathy, cerebral infarction and convulsions.
  • Cardiovascular system: infrequently – vascular disorders; rarely – increased blood pressure, angina pectoris, AV block, myocardial infarction, palpitations, tricuspid valve insufficiency, deep vein thrombosis, thrombophlebitis, varicose veins and vasculitis; less than 2% – atrial fibrillation, orthostatic hypotension.
  • Dermatological reactions: often – lipodystrophy; infrequently – rash, acne, alopecia, allergic dermatitis, maculopapular rash, itching and hyperhidrosis; rarely – dry skin, eczema, idiopathic capillaritis, exfoliative dermatitis, facial swelling, impaired nail structure, seborrhea, discoloration of the skin, striae, skin ulcers; less than 2% – skin hypertrophy.
  • Musculoskeletal system: infrequently – myalgia, arthralgia; rarely – osteoarthritis, lower back pain and bone necrosis, joint disease; less than 2% – muscle weakness.
  • The side of metabolism: infrequently – dehydration, obesity, anorexia, decrease or increase in body weight; rarely – a decrease or increase in appetite, hyperamilasemia, hyperlipasemia, hyperuricemia, hypophosphatemia, hypocholesterolemia, hypovitaminosis and hypothyroidism, lactic acidosis, lipomatosis.
  • Endocrine system: infrequently – diabetes mellitus, Itsenko-Cushing’s syndrome; rarely – male hypogonadism.
  • Urinary system: rarely – hematuria, nephrolithiasis, nephritis and deviations of laboratory parameters of urine, changes in the smell of urine.
  • Reproductive system: infrequently – erectile dysfunction; rarely: amenorrhea, ejaculation disorder, breast enlargement, gynecomastia, menorrhagia.
  • Respiratory system: infrequently – bronchitis; rarely – cough, shortness of breath, pulmonary edema; less than 2% – bronchospasm.
  • Hemopoietic system: rarely – anemia, leukopenia and lymphadenopathy.
  • Sensory organs: infrequently – tinnitus; rarely – visual disturbances, hyperacusia, dizziness, imbalance.
  • Infections: rarely – a bacterial infection, bronchopneumonia, inflammation of the subcutaneous fat, folliculitis, furunculosis, gastroenteritis, otitis media, perineal abscess, pharyngitis, rhinitis, sialadenitis, sinusitis and viral infection (including flu).
  • Neoplasms: rarely – neoplasms (including benign skin neoplasms), cysts.
  • General: often – asthenia; infrequently – pain, pain in the sternum, fever, swelling, malaise; rarely – chills, peripheral edema, chest pain.

Interactions

Lopinavir/ritonavir in vitro and in vivo inhibits the CYP3A isoenzyme. The simultaneous use of Kaletra and drugs metabolized by CYP3A isoenzymes can result in an increase in their plasma concentrations and enhance or prolong the therapeutic effect and side effects.

The risk of a significant increase in AUC (≥3 times) during treatment with lopinavir/ritonavir is highest in the case of the simultaneous use of drugs that are actively metabolized by the action of CYP3A isoenzymes and are metabolized during the first passage through the liver:

  • simultaneous use with drugs whose clearance is significantly dependent on CYP3A-mediated metabolism, including astemizole, blonanserin, terfenadine, midazolam, triazolam, cisapride, pimozide, rifampicin, salmeterol, sildenafil (only in the case of treatment of pulmonary hypertension), vardenofenol, alfenofen, (for example, ergotamine and dihydroergotamine, ergometrine and methylergometrine), inhibitors of HmG-CoA reductase (lovastatin, simvastatin), preparations of St. John’s wort perforated, fosamprenavir;
  • 1 time/day use in combination with carbamazepine, phenobarbital or phenytoin.

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

Lopinavir / ritonavir in vivo induces its own metabolism and causes an increase in the biotransformation of some drugs metabolized by isoenzymes under the action of isoenzymes of the P450 cytochrome system and by glucuronidation.

Lopinavir/ritonavir is metabolized by the action of CYP3A isoenzymes. The simultaneous use of lopinavir/ritonavir with the inducers of this isoenzyme can result in a decrease in the concentration of lopinavir in plasma and its therapeutic effect. Other drugs that inhibit CYP3A isoenzymes can cause an increase in plasma lopinavir concentration, although these changes were not found in the case of the simultaneous use of ketoconazole.