Abamat

"Abamat" will not change the human attitude towards the disease, but it is an excellent antiviral agent, specially developed by medical scientists for children and adults with HIV infection.

Indications Abamat

"Abamat", the international name of which is "Abacavir", is intended for the treatment of the virus - HIV of adults and children.

Treatment with the drug requires extreme caution, since HIV infection exerts its influence on the entire human body, which means that the drug should be administered under the strict supervision of a doctor who has the necessary experience in the treatment of AIDS patients and HIV. During the treatment, the patient's viral load and the number of CD4-lymphocytes should be assessed. Patients should be informed that the use of Abamat does not prevent the transmission of the immunodeficiency virus through blood or intimate communication.

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Release form

"Abamat" is presented in the form of peach-colored tablets, which are covered with a shell, round biconvex form, with the inscription "M20" on one side, on the other side there is a "strip" for the fracture into two parts, each part of which is 60 mg.

"Abamat" "M110" is almost identical to "Abamat" "M20", but the form of release "M110" - capsules is also peach color, it is logical, it has the inscription "M110" on one side, the other side is smooth, the dose of which is 300 mg.

The difference between the first and second types of the drug is a dose, which is agreed, first of all, with the attending physician.

Pharmacodynamics

"Abamat" is quickly absorbed from the digestive tract. Bioavailability in adults is 83%. The maximum concentration in the blood serum is 1.5 hours after taking the drug in tablets. When taking the drug in therapeutic doses (600 mg), the maximum concentration is about 3 μg / ml, and the AUC is taken at a frequency of 12 hours - 6 μg / h / ml.

The use of the drug during a meal slows the time of peak occurrence of its concentration in the serum, but does not affect the total concentration in the blood plasma. In the course of which, "Abamat" can be taken, despite the intake of food.

Abacavir - another name for "Abamata", freely penetrates into various tissues of the body, including CSF. The average ratio of abacavir levels in cerebrospinal fluid and serum is approximately 30-44%. When used in therapeutic doses, the level of binding to proteins is approximately 49%.

Concerning metabolism, abacavir undergoes primary metabolism in the liver, 2% of the applied dose is released unchanged in kidneys.

The main metabolites are 5 '- carboxylic acid and 5' - glucuronide, which are converted by alcohol dehydrogenase or by glucuronization.

The half-life of abacavir is 1.5 hours. A significant accumulation after repeated administration of the drug at a dose of 300 mg twice a day does not occur. Metabolites and abacavir in unchanged form in the amount of approximately 83% of the dose are given by the kidneys, the rest - with feces.

As for carcinogenesis, mutagenesis, there are data on the appearance of malignant and benign tumors. In most cases, these tumors occurred with the use of high doses of "Abamat" - 330 mg / kg / day and 600 mg / kg / day. These doses are equivalent to the level, which is 24-32 times higher than the level of systemic distribution of the drug in humans. Although the carcinogenic potential of the drug in humans is unknown, these data provide an opportunity to believe that the potential benefit of using the drug is predominantly carcinogenic in humans.

Hepatic lesions

The process of metabolism "Abamata" is, first of all, in the liver. The pharmacokinetics of Abamat was studied in patients with moderate hepatic lesions (Child-Pugh index-5-6), who took once 600 mg per day. The result revealed an average increase of 1.89 times [1.32; 2.70] AUC of abacavir and 1.58 [1.22; 2.04] times half-life.

Renal damage

Basically, the process of metabolism of "Abamata" takes place in the liver, approximately 2% of the taken dose goes through the kidneys as unchanged compounds. The pharmacokinetics of abacavir in patients with end-stage renal disease is similar to that of patients with normal kidney function. Therefore, dose adjustment for patients with renal lesions is necessary.

Proceeding from the information received by short-term experience, it is necessary to cancel the reception of "Abamat" to patients with the final stages of kidney diseases.

Pharmacokinetics in children

Children "Abamat" quickly and easily absorbed from oral solutions. The general pharmacokinetic parameters of children are similar to adults, with greater variability in plasma concentrations.

If we talk about babies up to 3 months, then there is no necessary information for safe use.

Pharmacokinetics

Active ingredient: 1 tablet coated film contains: abacavir in the form of sulfate 60 mg or 300 mg.

The auxiliary substances include:

• silicon dioxide colloidal,
• microcrystalline cellulose,
• sodium starch (type A),
• magnesium stearate,
• film coating "Opadray Yellow" 03V82849 (titanium dioxide - E171, hypromellose),
• iron oxide red - E172,
• iron oxide yellow - E172,
• polyethylene glycol.

"Abamat" is an antiviral agent for systemic use.

Abamat is a nucleoside reverse transcriptase inhibitor, and it is also potent with the HIV-1-HIV-2 inhibitor, including HIV-1 isolates with an underestimated sensitivity to zidovudine, lamivudine, zalcitabine, nevirapine, or didanosine. In a cell, this drug is converted into an active metabolite, carbovir triphosphate, which acts by inhibiting HIV reverse transcriptase, resulting in a disruption of the necessary binding in the viral DNA system and stopping its replication.

Dosing and administration

Treatment should be performed by a doctor who has experience in treating patients with HIV infection.

"Abamat" is taken orally, regardless of food intake.

Adults and children over 12 years of age (who weigh at least 30 kg): 300 mg twice a day or 600 mg once a day.

When switching from the regime twice a day to the schedule of a one-time daily intake, in the morning, the first dose of 600 mg should be taken in the morning. If the evening regimen is preferable, then on the day of transition in the morning take 300 mg, and in the evening - 600 mg.

When switching from a mode once a day to a regime twice a day, the first 300 mg should be taken in the morning.

Children from 3 years (whose weight is not less than 14 kg) to 12 years, the recommended dose is 8 mg / kg 2 times a day; the maximum daily allowance is up to 600 mg per day. "Abamat" should be prescribed only to those children who can swallow the pill. For patients who can not swallow a pill, "Abacavir" can be offered in the form of a solution for oral administration.

Recommendations for the use of tablets are 60 mg for children weighing between 14 and 30 kg.

Dose adjustment for renal failure is not required, since the metabolism of Abamata occurs predominantly in the liver, patients with mild liver failure (Child-Pugh index-5-6) are recommended to take 200 mg of "Abamat" twice daily . For this dosing should be used "Abamat" in the form of a solution for oral administration.

Dose adjustment for elderly patients. When the drug is prescribed for elderly patients, it is necessary to take into account a higher incidence of heart, liver and kidney function disorders, the presence of concomitant diseases and the use of medications.

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Use Abamat during pregnancy

"Abamat" has a whole complex of contraindications and side effects. But the safety of the use of "Abamat" during pregnancy is not established, hence, and there are no recommendations for pregnant women. But the doctor can prescribe the reception of this remedy only if the expected benefit to the mother during this period exceeds the risk for the fetus.

"Abamat" for breastfeeding HIV-infected mothers, as well as during pregnancy, is not advised to take as well as its effect on the child is unknown. Studies have not established the penetration of the drug into the mother's milk, therefore, during the reception should stop breastfeeding.

But in any case, a pregnant woman or a woman who has already given birth must follow the clear instructions of the doctor, especially since the given medicine is dispensed in pharmacies only when the prescription is given.

Contraindications

"Abamat" has several contraindications, which include:

• Hypersensitivity to the components that make up the drug.
• Moderate or severe hepatic impairment.
• Terminal stage of kidney disease.
• Positive test for the presence of the HLA-B * 5701 allele.

In addition to contraindications, "Abamat" also has side effects, which are also indicated in the instructions, and which are necessarily taken into account by the attending physician during the therapy. Establish a predisposition to contraindications can be through the diagnosis: laboratory tests and ultrasound.

Side effects Abamat

There is evidence that approximately 5% of patients receiving Abamat developed hypersensitivity reactions that were characterized by the appearance of multiple organ symptoms with or without fever and or the appearance of rashes (maculopapular or in the form of urticaria), rarely ended lethal.

Symptoms can occur at any time during treatment, however, they usually appear within the first six weeks after the start of treatment (mean time of onset is 11 days).

Symptoms and signs of allergic reactions are given below. Those that occurred with a frequency of more than 10% are highlighted in bold.

From the skin: a rash (maculopapular or in the form of urticaria).

On the part of the digestive system: abdominal pain, diarrhea, nausea, vomiting, gastroenteritis, ulcers on the mucous membrane of the oral cavity.

On the part of the respiratory system: cough, shortness of breath, respiratory depression syndrome, sore throat, respiratory failure, changes in the chest radiograph (mainly infiltrates that may be localized): fever, fatigue, poor health, lymphadenopathy, swelling , conjunctivitis, arterial hypotension, anaphylaxis.

From the nervous system: headaches, paresthesia.

On the part of the hematopoiesis system: lymphopenia.

On the part of the digestive system: increasing the level of functional hepatic tests, hepatitis, liver failure.

Musculoskeletal system: muscle pain, single cases of myolysis, arthralgia, increased level of CK.

Among other things, the increase in the level of creatinine, renal failure, rash and adverse reactions from the gastrointestinal tract are more likely to occur in children than in adults. A frequent isolated symptom of a hypersensitivity reaction was rashes on the skin. Some patients with hypersensitivity reactions are initially perceived as having respiratory system diseases (pneumonia, pharyngitis, bronchitis), flu-like illnesses, gastroenteritis or reactions to other medications.

The delay in the diagnosis of hypersensitivity leads to the fact that patients continue to use abacavir, which can cause severe aggravation of allergic reactions and even death. Therefore, you should always keep in mind the likelihood of a hypersensitivity reaction, if the patients have the above symptoms. If the risk of such a reaction is impossible to exclude, the use of Abamat or other drugs that contain abacavir is not revoked. When continuing treatment, symptoms of hypersensitivity reactions worsen, and after the drug is usually withdrawn. Patients who developed a hypersensitivity reaction should prioritize the treatment and never renew it with any medication containing "Abamat".

There are some reports of hypersensitivity reactions that occurred after repeated use of the drug, when this was preceded by the appearance of one of the main signs of hypersensitivity (skin rash, fever, fatigue, malaise, gastrointestinal or respiratory symptoms).

In rare cases, hypersensitivity reactions occurred in patients who resumed treatment, but this was not preceded by hypersensitivity symptoms. For many other adverse reactions, it remains unclear whether they are associated with the use of "Abamat" or other drugs used to treat HIV infection, is the result of the disease as such.

Many of the above symptoms (nausea, vomiting, diarrhea, fever, fatigue, rash) appear as part of the hypersensitivity reaction. Therefore, patients with any of these symptoms should be carefully examined for allergic reactions. In the event of termination of treatment due to the presence of at least one of these symptoms, the resumption of treatment is possible only under the direct supervision of a physician.

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Overdose

In case of an overdose, it is first of all necessary to make sure that the patient does not have an allergic reaction to "Abamat" or its components, and if necessary, conduct a standard maintenance therapy. In other cases, treatment is symptomatic. It is not known whether this drug is excreted by peritoneal dialysis or hemodialysis.

In order to avoid an overdose, follow strictly the recommendations of a doctor. In case of any unforeseen symptoms, it is necessary to inform the attending physician. It is possible that the symptomatology may be associated with an allergic reaction.

Interactions with other drugs

The probability of P450 mediated interaction of "Abamat" with other medical devices is low. "Abamat" suppresses the enzymes CYP3A4, CYP2C9 and CYP2D6 at clinically appropriate concentrations.

The interaction of protease inhibitors and other medications that are metabolized by basic P450 enzymes is unlikely.

The interaction between "Abamat", "Zidovudin" and "Lamivudin" is absent.

Admission of the drug with "Ethanol" leads to the development of a scale under the pharmacokinetic curve "concentration / time" (AUC) of "Abamat" by almost 41%. "Abamat" does not affect the metabolism of "Ethanol".

Simultaneous application of 600 mg of "Abamat" twice a day and "Methadone" helps to reduce the maximum concentration (Cmax) of "Abamat" by 35% and for one hour delays the period of reaching the maximum concentration (tmax), however AUC remains unchanged. This antiviral agent increases the average systemic scale of Methadone by 22%. Adult patients taking "Methadone" and "Abamat" should be checked for signs of withdrawal syndrome, indicating a low dosage, since a dose adjustment of "Methadone" may be required.

The components of retinoids are eliminated with alcohol dehydrogenase. Interaction with Abamat is possible, but it has not been studied.

[4], [5], [6], [7], [8]

Storage conditions

"Abamat" has standard storage rules, that is, in a dark, dry place inaccessible to children, the temperature of which should not exceed 30 ° C. And to store it is necessary in the original packing together with the loose leaf - the instruction.

It should be remembered that non-observance of the norms during storage can significantly shorten the shelf life of the drug as most substances that are active or additional components lose their therapeutic properties at too high a temperature or when interacting with the sun's rays.

It is for these reasons that Abamat, in whose insert there is all the information on this matter, should be kept, observing all instructions.

Shelf life

"Abamat", if you keep it, following the instructions, is suitable for 2 years from the date of issue. But, otherwise, the exact date of the end of its expiration date can not be called.

Buying "Abamat", do not hesitate, look at the date of manufacture and the name of the manufacturer. Why check the date - it is understandable. As for the manufacturer, the only one who can produce it is Matrix Laboratories Limited India. Counterfeits among drugstores were not observed. And, here, if to speak about "virtual" ways of delivery, then everything is possible, even the delivery of an overdue product.