Kaletra

An innovative drug produced by the British company Abbott Laboratories - Kaletra - is an antiretroviral substance for the treatment of HIV infection (human immunodeficiency virus).

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Indications Kaletra

The only indication for the use of the drug Kaletra is the treatment of HIV infection by inhibiting the replication of the human immunodeficiency virus.

Release form

The release form of Kaletra is tablets, covered on top with a special protective shell, allowing the drug to be “delivered” directly to the area of their most effective work.

Kaletra contains two active substances, each with its own dosage: lopinavir (0.2 mg) and ritonavir (0.05 mg).

Kaletra in tablet form is available in a bottle made of dense polyethylene. One bottle contains 120 units of the drug. The bottle with instructions for use of the drug is packed in a cardboard package.

Additional chemical compounds present in the drug are sorbitan laurate, sodium stearyl fumarate, copovidone K28, colloidal silicon dioxide.

The film coating of the tablet has its own composition.

Pharmacodynamics

This medicine has a narrow specialization. The therapeutic features of Kaletra are determined by the pharmacodynamics of the two main active substances.

Lopinavir is an inhibitor of HIV-1 and HIV-2 protease, which provides the antiviral pharmacodynamics of Kaletra. Inhibition of these proteases ensures disruption of viral protein production, leading to the formation and development of an underdeveloped retrovirus.

Ritonavir is a peptidomimetic and an inhibitor of HIV-1 and HIV-2 aspartyl proteases.

Metabolized in the liver.

Complete information regarding cross-resistance between lopinavir and ritonavir is currently not available, which requires additional research.

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Pharmacokinetics

The pharmacokinetics of Kaletra are determined by the corresponding parameters of lopinavir and ritonavir. As clinical studies have shown, under the influence of CYP3A, lopinavir is almost 100% transformed into its metabolites. The presence of ritonavir slows down the metabolism of lopinavir and leads to an increase in its concentration in the blood plasma, increasing the pharmacological efficacy of Kaletra.

When the recommended dose of lopinavir/ritonavir (0.4/0.1 g) is administered twice daily, the maximum concentration (C _max ) of lopinavir in the blood of 6.1 to 13.5 mcg/mL is achieved four hours after administration.

A single dose of the drug with lean food and on an empty stomach does not show a significant change in the absorption level. When eating moderately fatty food, the absorption results of the drug are improved.

The bioavailability of Kaletra is quite high and amounts to 99%. Lopinavir mainly binds to such plasma protein structures as albumins and alpha-1-acid glycoproteins.

The drug is excreted from the body quite slowly. After eight days, the concentration of lopinavir decreases by 10%, it is excreted mainly in the form of metabolites with urine and more than 80% with feces. About 2.2% of lopinavir is excreted in urine unchanged and 19.8% of them - with feces.

The clearance of lopinavir after oral administration of the drug shows a level from 0.23 to 11.73 L/h.

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Dosing and administration

Kaletra tablets are taken orally. The method of administration and dosage of the drug are prescribed by the attending physician individually, based on the patient's condition and the clinical picture of the disease. The effectiveness of Kaletra does not depend on the time and amount of food taken. Tablets should not be chewed. It is recommended to swallow them whole.

In the ratio of lopinavir/ritonavir, the starting recommended dosage is taking two tablet forms, which in dosage corresponds to 0.4/0.1 g (the concentration of active ingredients lopinavir/ritonavir of one tablet is 0.2/0.05 g) twice during the day. A second schedule of administration is also possible - four tablets once.

For children who are already three years old, the drug in question is prescribed in slightly different dosages.

Schedule of administration and dosage Kaletra in standard adult dosages is approved for use in children whose weight has exceeded 35 kg and whose body surface area (BSA) is at least 1.4 ^m2.

If the child has a lower weight and his BSA falls within the range from 0.6 m2 ^to 1.4 m2 ^, the recommended dosage of the drug is 0.1 g + 0.025 g.

For children whose body surface area is less than 0.6 ^m2, or whose age has not reached three years, Kaletra is used not in tablet form, but in the form of syrup. In this situation, the dose of the drug corresponds to the figure of 0.080 g + 0.020 g/ml.

It is quite easy to calculate the body surface area yourself. To do this, multiply the patient's height in centimeters by his body weight in kilograms and divide the result by 3600.

PSA (m ² ) = (Height (cm) × Body weight (kg)/3600)

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Use Kaletra during pregnancy

The use of the antiviral drug Kaletra during pregnancy is not recommended by doctors and pharmacists.

If the question of the need for antiretroviral therapy arises during the period when a young mother is breastfeeding her baby, then the woman should stop breastfeeding.

Contraindications

Doctors have identified the following contraindications for the use of Kaletra:

1. Individual hypersensitivity of the patient's body to lopinavir and/or ritonavir, as well as to one or more additional substances of the drug.
2. Severe degree of liver dysfunction.
3. The age of the little patient is up to three years.

Particular care should be taken when introducing Kaletra into the treatment protocol for those patients who have the following diseases in their medical history:

1. Cirrhosis.
2. Mild to moderate liver dysfunction.
3. Hemophilia is a blood disorder.
4. Pancreatitis is an inflammation of the pancreas.
5. Viral hepatitis B and C.
6. Exceeded liver enzyme levels.
7. Hypercholesterolemia.
8. Hypertriglyceridemia is an elevated level of triglycerides in the blood.
9. Venerable. The patient's advanced age, exceeding 65 years.
10. Patients with heart problems.

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Side effects Kaletra

The highly effective antiretroviral drug Kaletra, when taken orally, can cause quite a few side effects:

1. Reaction of the digestive organs:

• The appearance of symptoms of diarrhea.
• Nausea that can cause vomiting reflex.
• Pain in the abdominal area.
• Flatulence.
• Exacerbation of various diseases associated with the digestive tract: colitis, enterocolitis, hemorrhoids, hepatitis, gastroenteritis, liver steatosis, gastroesophageal reflux, hepatomegaly and a number of others that occur less frequently.

1. The reaction of the body's protective function is an allergic reaction of the body, caused by its symptoms:

• Hyperemia of the skin.
• Angioedema.
• Hives.
• Rash.
• Itching.
• Burning.

1. Cardiovascular response:

• Increased blood pressure.
• Less common are manifestations of atherosclerosis, deep vein thrombosis, myocardial infarction and a number of other disorders.

1. Neuralgic reaction:

• Headaches.
• Sleep disturbance.
• The appearance of noise in the ears.
• Neuropathy, neuralgia.
• Dizziness.
• The emergence of a feeling of anxiety.
• Visual impairment.

1. Reaction of the musculoskeletal system:

• Pain syndrome affecting the back area.
• Myalgia.

1. Reaction of the dermis and subcutaneous layers:

• Manifestation of various pathological changes of a dermatological nature.

1. Endocrine system reaction:

• Decreased appetite.
• Weight loss.
• Diabetes mellitus.
• Hypertriglyceridemia.
• Hypercholesterolemia (high levels of cholesterol in the blood).

1. Reaction of the excretory system:

• Renal dysfunction.

1. Reaction of the human reproductive system:

• Absence of menstruation for several menstrual cycles.
• Heavy blood loss during menstruation.
• Erectile dysfunction.

1. Reaction of the body's hematopoietic elements:

• Anemia is a condition caused by a deficiency of red blood cells.
• Lymphadenopathy is a reaction of the lymph nodes, expressed by their proliferation.

1. Deterioration of the general condition of a person:

• Frequent infections affecting the lower and upper respiratory tract.
• Infection of the dermis and subcutaneous fat.
• Furunculosis.
• Asthenia.
• Decreased overall tone of the body.
• Deterioration of laboratory test results.

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Overdose

Overdose of lopinavir and/or ritonavir, the active ingredients of the antiviral drug for HIV infection Kaletra, is unknown due to the paucity of facts and observations.

There is no effective antidote, and if adverse side effects occur, symptomatic treatment is carried out.

If necessary, detoxification measures can be carried out: gastric lavage (allows to remove the remains of the drug), as well as the use of a sorbent (this can be regular activated carbon).

Due to the fact that the active ingredients of Kaletra show a high percentage of binding to blood plasma proteins, its use in the treatment of overdose with dialysis is inappropriate.

A number of warnings regarding admission:

1. Lopinavir and ritonavir are primarily converted to their metabolites in the liver, so if liver function is impaired, the standard dosage may need to be adjusted.
2. During treatment with Kaletra, you should cancel your trips behind the wheel of a vehicle. If your work requires maintaining a high level of attention for a long time, you should raise the issue of temporarily transferring to another type of work.

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Interactions with other drugs

Most often, the drug Kaletra is used in the complex treatment of HIV infection. Therefore, interactions with other drugs Kaletra is a prerequisite for the effectiveness of the entire treatment complex.

Concomitant use with zidovudine and abacavir leads to a decrease in their concentration in the blood, which may lead to a deterioration in the effectiveness of the drug.

The opposite effect is observed when used together with tenofovir. The quantitative component in the blood plasma of the latter pharmacological agent increases, causing overdose symptoms.

Simultaneous work with non-narcotic analgesics requires medical personnel to constantly monitor the patient's health and the appearance of side effects, as a deterioration in the condition, including respiratory depression, is possible.

With the parallel use of HIV protease inhibitors, an increase in creatine phosphokinase activity is observed.

When Kaletra is used with nevirapine, a decrease in the quantitative indicator of lopinavir in the patient's blood is observed, which weakens the effect of the antiviral drug in question.

The combined use of lopinavir and ritonavir with efavirenzin and nevirapine is strictly prohibited, as the effect of Kaletra on retroviral structures is inhibited.

Delavirdine shows activation of lopinavir and an increase in its quantitative presence in the patient's blood plasma.

Concomitant use of Kaletra and anticoagulant drugs (eg, warfarin) increases the risk of bleeding.

Lopinavir and ritonavir, when used together in one treatment protocol, with amprenavir increase C _min (numerical presence in plasma) of the latter. Their combined administration once a day is contraindicated.

A similar clinical picture is observed in the case of parallel administration of Kaletra and nelfinavir. Doctors should not allow their combined use.

Doses of drugs that inhibit the chemokine receptor CCR5 (eg, maraviroc) should be reduced when co-administered with lopinavir and ritonavir.

As clinical observations have shown, the quantitative component of saquinavir in the complex treatment protocol should be reduced.

When Kaletra and boceprevir are used together, doctors observe a decrease in the quantitative component of lopinavir and the second antiviral drug, which makes their combined use impossible.

It is necessary to be very careful when administering and adjusting the doses of the drug in one therapeutic protocol of the antiviral drug in question and drugs of the antidepressant group. There is a high risk of developing side effects.

Treatment in combination with antifungal drugs is also not recommended.

During treatment with Kaletra, oral contraceptives should not be used, as their effective protection may be impaired, requiring their replacement with other forms of contraceptive protection.

Storage conditions

Storage conditions for Kaletra require compliance with the following points:

1. The storage location for lopinavir and ritonavir should be protected from direct sunlight.
2. The storage temperature range is allowed within the range from + 15 to + 30 degrees above zero.
3. The antiretroviral drug should be kept in places that are inaccessible to teenagers and small children.

Shelf life

In this case, the shelf life of the drug in question, Kaletra, is four years.