Abacavir Canon tablets coated.pl.ob. 600 mg 30 pcs. (abacavir)

Release form

Film-coated tablets

Indications

Treatment of HIV infection in adults and children weighing more than 14 kg as part of combination antiretroviral therapy.

Contraindications

- Hypersensitivity to abacavir or any other component of

- Children weighing less than 14 kg (for this dosage form)

- Medium to severe hepatic insufficiency (class B and C on the Child scale - Pugh), due to the lack of clinical data and the recommended dosage regimen

- Mild liver failure (class A on the Child-Pugh scale), due to the inability to ensure dosing regimen

- Breastfeeding period

- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Caution: Patients with a possible risk of coronary heart disease combined use of abacavir and ribavirin (see Interaction section).

Special instructions

The drug should be prescribed by a doctor with experience in treating HIV infection.

Each patient should read the instructions for use.

Hypersensitivity

The use of the drug Abacavir Kanon is associated with a risk of developing RGH, characterized by the appearance of fever and / or rash and other symptoms indicating multiple organ damage. RGH can be life threatening and, in rare cases, when treatment is not prescribed, it can be fatal. The risk of developing RHG with the use of the drug Abacavir Canon is significantly increased in patients with a positive test for the presence of the HLA-B * 5701 allele. However, RGCs on abacavir were noted with less frequency in patients who are not carriers of this allele.

The following rules should be followed.

- A study should be carried out for the presence of the HLA-B * 5701 allele before starting treatment with Abacavir Canon and also before resuming treatment with Abacavir Canon in patients with unknown status with respect to the HLA-B * 5701 allele who had previously tolerated abacavir therapy.

- Abacavir Canon is not recommended for use in patients with the HLA-B * 5701 allele or in patients who have been suspected of having rhG during use of any other drug containing abacavir, regardless of status with respect to HLA-B * 5701.

- Each patient should be reminded that it is necessary to familiarize themselves with the instructions for use included in the package of the drug Abacavir Canon. Also, patients should be reminded that they must always have with them a warning card attached to the drug.

- In all patients receiving therapy with Abacavir Canon, the clinical diagnosis of a suspected RHC should remain the basis for a clinical decision.

- If there is a suspicion of RHC, therapy with Abacavir Canon should be discontinued immediately even if the HLA-B * 5701 allele is absent. Delaying discontinuation of Abacavir Canon therapy after the occurrence of RHC can lead to a life-threatening reaction.

- Patients who have developed hCG should be informed of the need to transfer the remaining tablets of Abacavir Canon to their healthcare provider in order to avoid resuming abacavir.

- Resuming the use of drugs containing abacavir after a suspected RGC on abacavir can lead to a quick return of symptoms within a few hours, which may include life-threatening arterial hypotension and death.

- When considering resuming abacavir therapy after discontinuing treatment with any abacavir-containing drug for any reason, the reason for discontinuing therapy should be established, regardless of the patient's carriage of the HLA-B * 5701 allele. If RHC cannot be ruled out, you can not resume the use of the drug Abacavir Canon or any other medicines containing abacavir.

- If rHG is excluded, it is possible to resume therapy with Abacavir Canon. In rare cases, patients who discontinued use of abacavir for reasons other than symptoms of RGC also showed the development of life-threatening reactions within a few hours after resuming treatment with abacavir (see section Description of individual adverse reactions).

Patients should be informed of the possibility of developing RHF when resuming therapy with Abacavir Canon or other medicines containing abacavir should be administered only if there is quick access to medical care.

The clinical presentation of rhGM on abacavir

the rhg on abacavir has been well studied in clinical trials and during post-registration observation. Symptoms usually appear within the first 6 weeks (the median time to start this reaction is 11 days) after the start of abacavir therapy, however, these reactions can develop at any time during the treatment.

Almost all of the reactions of RGC to abacavir include fever and or a rash as part of the syndrome. Other signs and symptoms that are noted as a manifestation of rhG on abacavir, include symptoms of the respiratory and gastrointestinal tract, which can lead to incorrect diagnosis of RHG as a respiratory disease (pneumonia, bronchitis, pharyngitis) or gastroenteritis (see sections Adverse effects, Description of individual adverse reactions). Patients should be closely monitored and consulted every 2 weeks, especially during the first 2 months of treatment with Abacavir Canon.

If treatment with abacavir continues when symptoms of rHG occur, they become more pronounced and may become life-threatening. In most cases, these symptoms disappear when you stop taking abacavir.

Lactic acidosis and severe hepatomegaly with steatosis

There are reports of the development of lactic acidosis and severe hepatomegaly with steatosis, including death, due to antiretroviral therapy with nucleoside analogues, including abacavir, taken either individually or in combination. In most cases, these complications occur in women.

Symptoms that may indicate the development of lactic acidosis include general weakness, loss of appetite, rapid weight loss of unclear etiology, disorders of the gastrointestinal tract (nausea, vomiting, and abdominal pain), disorders of the respiratory system (shortness of breath and tachypnea) or neurological symptoms (including motor).

Lactic acidosis has high mortality in the absence of emergency treatment and may be associated with pancreatitis, liver or kidney failure. Lactic acidosis, as a rule, manifested itself after several months of therapy. It is necessary to discontinue therapy with nucleoside analogues in case of symptomatic manifestations of hyperlactatemia and metabolic or lactic acidosis, the progression of hepatomegaly or a rapid increase in the activity of aminotransferases.

The use of the drug Abacavir Canon and other abacavir-containing drugs requires caution for any patient (especially overweight women) with hepatomegaly, hepatitis, or other known risk factors for liver damage and liver steatosis (including the use of certain drugs and alcohol). Patients with concomitant hepatitis C who receive interferon alfa and ribavirin therapy may be at particular risk. High-risk patients require close monitoring.

If there are clinical or laboratory signs of lactic acidosis with or without hepatitis (it can manifest as hepatomegaly and steatosis even in the absence of a marked increase in the activity of aminotransferases), treatment with Abacavir Canon should be stopped.

Mitochondrial dysfunction

In vitro and in vivo studies have shown that nucleoside and nucleotide analogues can cause varying degrees of mitochondrial damage. Cases of itochondrial dysfunction were recorded in HIV-negative children who received intrauterine and / or postnatal nucleoside analogues. The main adverse reactions were hematologic disorders (anemia, neutropenia), metabolic disorders (hyperlactatemia, hyperlipasemia). These adverse reactions are often transient. Some late-onset neurological disorders (increased muscle tone, cramps, behavior disorders) have been reported. Whether these neurological disorders are transient or persistent is currently unknown. Any child, even an HIV-negative one, who has been exposed in utero to nucleoside and nucleotide analogs, must undergo clinical and laboratory examination to rule out mitochondrial dysfunction if signs or symptoms are identified. These data do not affect current national guidelines for the use of antiretroviral therapy in pregnant women for the prevention of vertical transmission of HIV infection.

Redistribution of subcutaneous fat

In some patients receiving combination antiretroviral therapy, redistribution and / or accumulation of subcutaneous fat, including central obesity, dorsocervical fat deposition (buffalo hump), a decrease in the subcutaneous fat layer on the face and limbs, an increase in the mammary glands, an increase in serum lipids and blood glucose concentration may be observed .

Although one or more of the above adverse reactions associated with the common syndrome, which is often referred to as lipodystrophy, can cause all drugs of the HIV and NRTI classes. The data indicate the existence of differences between the individual representatives of these classes of drugs in the ability to cause these adverse reactions.

It should also be noted that lipodystrophy syndrome has a multifactorial etiology, for example, the stage of HIV infection, advanced age and duration of antiretroviral therapy play an important, possibly synergistic, role.

The long-term effects of these adverse reactions are currently unknown.

Clinical examination of patients requires attention to the redistribution of subcutaneous fat. Laboratory testing should include determination of serum lipid concentration and blood glucose concentration. If lipid metabolism is impaired, appropriate treatment is prescribed.

Pancreatitis

Cases of pancreatitis have been reported, although a causal relationship with abacavir has not been established.

Therapy with three nucleoside reverse transcriptase inhibitors (NRTIs)

In patients with a high level of viral load (> 100,000 copies / ml), the appointment of a triple combination, containing abacavir, lamivudine and zidovudine, requires special consideration.

Cases of a high frequency of virologic failure and the emergence of resistance in the early stages were recorded when a combination of abacavir with tenofovir desoproxil fumarate and lamivudine was used 1 time per day.

Liver disease

The efficacy and safety of abacavir have not been established in patients with severe concomitant liver disease. The drug Abacavir Canon is contraindicated in patients with impaired liver function of moderate and severe degree.

Patients with pre-existing liver dysfunction, including active chronic hepatitis, have an increased incidence of liver dysfunction during combination antiretroviral therapy, and should be monitored in accordance with accepted practice. It is necessary to consider the possibility of suspension or termination of treatment in case of manifestations of worsening of the disease in such patients.

Concomitant hepatitis B or C

Patients with concomitant chronic hepatitis B or C who receive combination antiretroviral therapy have an increased risk of severe and potentially fatal adverse reactions from the liver. In the case of concomitant antiviral therapy for hepatitis B or C, you should also familiarize yourself with the relevant instructions for the use of these drugs.

Caution should be exercised while administering abacavir and ribavirin.

Kidney disease

The drug Abacavir Canon should not be prescribed to patients with end-stage chronic renal failure.

Immunity restoration syndrome

If HIV-infected patients with severe immunodeficiency have asymptomatic opportunistic infections or residual symptoms at the time antiretroviral therapy is started, such therapy may increase the symptoms of opportunistic infections or other serious consequences. Typically, these reactions occur during the first weeks or months after initiation of antiretroviral therapy. Typical examples are cytomegalovirus retinitis, generalized and / or focal infection caused by mycobacteria, and pneumonia caused by Pneumocystis jiroveci (formerly P. carinii). The appearance of any symptoms of inflammation requires immediate examination and, if necessary, treatment.

Autoimmune diseases (such as Graves disease, polymyositis and Guillain-BarrГ© syndrome) were observed against the background of restoration of immunity, however, the time of primary manifestations varied, and the disease could occur many months after the start of therapy and have an atypical course.

Osteonecrosis

Although the etiology of this disease is multifactorial (including glucocorticosteroids, alcohol use, severe immunosuppression, high body mass index), cases of osteonecrosis were most common in patients with advanced HIV infection and / or those taking long-term combined antiretroviral therapy. Patients should consult a doctor if they experience pain and stiffness in the joints or difficulty moving.

Opportunistic infections

The use of Abacavir Canon or other antiretroviral drugs does not preclude the development of opportunistic infections or other complications of HIV infection, so patients should be monitored by a doctor with experience in treating HIV-related diseases.

HIV transmission

Antiretroviral therapy, including Abacavir Canon, does not preclude the possibility of HIV transmission through sexual contact or through contact with infected blood, and therefore does not eliminate the need for appropriate precautions.

Myocardial infarction

As a result of a prospective observational epidemiological study to study the incidence of myocardial infarction in patients receiving combination antiretroviral therapy, there was a connection between a previous intake of abacavir for 6 months and an increased risk of developing myocardial infarction. According to a generalized analysis of clinical studies, there was no increase in the risk of developing myocardial infarction associated with taking abacavir. The biological mechanisms explaining the potentially increased risk are unknown. In general, the available data obtained from cohort observations and controlled clinical trials do not allow us to unambiguously determine the relationship between abacavir therapy and the risk of myocardial infarction.

However, antiretroviral therapy, including drugs containing abacavir, should be prescribed with caution to patients with a possible risk of coronary heart disease. All measures must be taken to minimize all modifiable risk factors (such as arterial hypertension, dyslipidemia, diabetes and smoking).

Impact on the ability to drive transp. Wed and fur.: There is no evidence to support the effects of abacavir on the ability to engage in potentially hazardous activities requiring increased attention. However, patients should be informed of the possible development of adverse reactions such as increased fatigue during treatment with abacavir. They should be advised to exercise caution when driving and operating machinery.

Composition

1 tablet, film-coated 600 mg, contains: Active ingredient: abacavir sulfate 702.8 mg, in terms of abacavir 600 mg.

Excipients: sodium carboxymethyl starch 58 mg, colloidal silicon dioxide 11 mg, magnesium stearate 11 mg, povidone K-30 46 mg, microcrystalline cellulose 391.2 mg.

Film composition: Opadry II yellow 38 mg, including: hypromellose (hydroxypropyl methylcellulose) 12.92 mg, lactose monohydrate 10.64 mg, macrogol (polyethylene glycol) 4.56 mg, titanium dioxide 7.98 mg, iron dye oxide yellow 1.9 mg.

Dosage and Administration

The drug Abacavir Canon is taken orally, regardless of food intake. The drug should be prescribed by a doctor with experience in treating

HIV infection. To ensure accurate dosage of the drug, it is recommended to swallow the tablet completely without division, however, as an alternative, the division and grinding of tablets with the addition of a small amount of semi-solid food or liquid is allowed. The entire amount of the mixture must be taken orally immediately.

Adults and children weighing at least 25 kg

The recommended dose of the drug Abacavir Canon is 600 mg / day. The drug is prescribed in a dose of 300 mg (1 tablet 300 mg or Tablets 600 mg, break exactly at risk) 2 times a day or 600 mg (2 tablets 300 mg or 1 tablet 600 mg) 1 time per day.

Special patient groups

Children

Children with a body weight of 14 to 25 kg

-Children with a body weight of 14 to 20 kg: the recommended dose of the drug Abacavir Canon is 150 mg (1/2 tablet 300 mg, break exactly at risk) 2 times a day or 300 mg (1 tablet 300 mg) 1 time per day

-Children weighing more than 20 kg but less than 25 kg: the recommended dose of Abacavir Canon is 150 mg ( 300 mg tablets , break exactly at risk) in the morning and 300 mg (1 tablet 300 mg) in the evening or 450 mg (1 tablets 300 mg) once a day

For children weighing less than 14 kg or patients unable to swallow tablets, it is recommended to use the drug as a solution for oral administration.

Patients with impaired renal function

In patients with impaired renal function, dose adjustment of the drug Abacavir Canon is not required.

Patients with impaired liver function

Abacavir is metabolized primarily in the liver. The recommended dose of abacavir for patients with mild hepatic impairment (5-6 points on the Child-Pugh scale) is 200 mg 2 times a day. Given the need for lower doses of abacavir in patients with mild hepatic impairment, for the correct dosage of the drug, it is prescribed in an alternative dosage form - oral solution. There are no data on the pharmacokinetics and safety of the use of abacavir in patients with impaired liver function of moderate to severe degree. Thus, the use of abacavir in patients with impaired liver function of moderate and severe degree is contraindicated.

Side effects

The nature of other adverse reactions other than RGH, but observed in patients taking Abacavir Canon, is not fully understood. Whether these adverse reactions are a consequence of the use of the drug Abacavir Canon or a wide range of other drugs that are simultaneously prescribed for the treatment of HIV infections, or they are caused by the disease itself, has not yet been established.

Many of the following adverse reactions associated with taking the drug Abacavir Canon (nausea, vomiting, diarrhea, fever, fatigue, rash) are usually observed with the development of rhG to abacavir. therefore, if any of these symptoms occurs, a thorough examination of the patient is indicated to confirm the development of hrg. If the drug Abacavir Canon was canceled due to the appearance of the above symptoms and it was decided to resume therapy with the drug Abacavir Canon, then this can only be done under direct medical supervision.

Very rare cases of polymorphic exudative erythema, Stevens-Johnson syndrome, or toxic epidermal necrolysis have been reported, in which it was not possible to exclude rhG to abacavir. In such cases, you must permanently stop taking medications containing abacavir.

Most of the adverse reactions listed below are not limiting. The frequency of occurrence is determined as follows: very often -> 1/10,

often - from> 1/100 to <1/10,

infrequently - from> 1/1000 to <1/100,

rarely - from> 1/10000 up to <1/1000,

is very rare - <1/10000.

Clinical trial data

Metabolism and nutritional disorders

Often: loss of appetite.

Disorders of the nervous system

Often: headache.

Disorders from the groaning of the gastrointestinal tract

Often: nausea, vomiting, diarrhea.

General disorders and disorders at the injection site

Often: fever, drowsiness, fatigue.

In controlled clinical trials, it was shown that changes in laboratory parameters during treatment with abacavir are observed infrequently, as in the control group of patients not receiving abacavir.

Children

Safety data confirming a single dose of abacavir in children was obtained in the ARROW study (COL 105677), in which 669 children infected with HIV-1, received abacavir and lamivudine - 1 or 2 times a day. No additional safety signals were detected in children taking abacavir 1 or 2 times a day compared with adults.

Post-registration observation data

Metabolic and nutritional disorders

Often: hyperlactatemia.

Rarely: lactic acidosis, accumulation and / or redistribution of adipose tissue. The frequency of these adverse reactions depends on many factors, including the antiretroviral drugs used in combination with abacavir.

Gastrointestinal disturbances

Rarely: pancreatitis (a causal relationship with abacavir has not been established).

Disorders of the skin and subcutaneous tissue

Often: rash (in the absence of systemic manifestations).

Very rare: polymorphic exudative erythema, including Stevens-Johnson syndrome and toxic epidermal necrolysis.

Cases of lactic acidosis have been reported, sometimes fatal, usually associated with severe hepatomegaly and fatty liver, using nucleoside analogues.

The use of combination antiretroviral therapy has been associated with redistribution of adipose tissue (lipodystrophy) in HIV patients, including a decrease in the subcutaneous fat layer on the face and limbs, an increase in intra-abdominal and visceral fat, an increase in mammary glands, and dorsocervical fat deposition (buffalo hump).

The use of combination antiretroviral therapy has been associated with metabolic disorders such as hypertriglyceridemia, hypercholesterolemia, insulin resistance, hyperglycemia and hyperlactatemia.

In HIV-infected patients with severe immunodeficiency, inflammatory reactions to asymptomatic or residual opportunistic infections may occur during initiation of combination antiretroviral therapy. Cases of autoimmune diseases (for example, Graves disease) that occur under conditions of immune reactivation have also been reported, but the timing of the manifestation of the disease is more diverse and these phenomena can occur many months after the start of therapy.

Cases of osteonecrosis have been reported, especially in patients with well-known risk factors, advanced HIV infection, or long-term use of combination antiretroviral therapy. The frequency of this phenomenon is unknown.

Description of the individual adverse reactions

Hypersensitivity

The hypersensitivity reaction (hCG) to abacavir has been defined as a common adverse reaction in the treatment of drugs containing abacavir. Signs and symptoms of HRM are given below. These signs and symptoms were identified during clinical trials or during post-registration observation. Symptoms and signs that occur in at least 10% of patients with RHC are shown in bold. In almost all patients with RGH, a fever and / or rash (usually maculopapular or urticaria) develops as part of the syndrome, but reactions can occur without a rash or fever. Other major symptoms include symptoms of the gastrointestinal tract, respiratory system, or constitutional symptoms, such as drowsiness or malaise.

Disorders of the skin and subcutaneous tissue

Rash (usually maculopapular or urticaria).

Disorders of the gastrointestinal tract

Nausea, vomiting, diarrhea, abdominal pain, ulceration of the oral mucosa.

Disorders of the respiratory system, chest and mediastinal organs

Shortness of breath, cough, sore throat, adult respiratory distress syndrome, respiratory failure.

Disorders of the nervous system

Headache, paresthesia.

Disorders of the blood and lymphatic system

Lymphopenia.

Disorders of the liver and biliary tract

Increased biochemical parameters of liver function, hepatitis, liver failure.

Violations of the musculoskeletal and connective tissue

myalgia, myolysis, arthralgia, increased activity of creatine phosphokinase.

Disorders of the kidneys and urinary tract

Increased serum creatinine concentration, renal failure.

General disorders and disorders at the injection site

Fever, fatigue, malaise, swelling, lymphadenopathy, arterial hypotension, conjunctivitis, anaphylactic reactions. The resumption of taking Abacavir Canon after RGC to abacavir leads to a quick return of symptoms within a few hours. Repeated RGH is usually more severe than the first, and may include life-threatening, arterial hypotension, and death. In rare cases, reactions also occur when therapy with Abacavir Canon is resumed after its withdrawal, caused by the appearance of only one of the main symptoms of hypersensitivity (see above) and in very rare cases, this reaction occurs when you resume taking the drug Abacavir Canon by patients who did not have any symptoms of rHG before discontinuing the drug (i.e., patients who were previously considered to be tolerating abacavir therapy).

For detailed information on the clinical management of a suspected case of abacavir RHC, see Special instructions.

Drug Interactions

In vitro studies and analysis of the main metabolic pathways of abacavir indicate that its interaction with other drugs cytochrome P450 mediated is unlikely.

Abacavir does not inhibit metabolic reactions involving the cytochrome P450 isoenzyme CYP3A4.

In vitro studies have shown that - abacavir does not interact with drugs that are metabolized by the isoenzymes CYP3A4, CYP2C9 and CYP2D6. Clinical studies have not revealed the induction of hepatic metabolism of exogenous substances under the influence of abacavir. Thus, the interaction of abacavir with HIV protease inhibitors and other drugs metabolized with the main cytochrome P450 isoenzymes is unlikely.

Clinical studies have shown no clinically significant interactions between abacavir, zidovudine, and lamivudine. Powerful enzyme inducers such as rifampicin, phenobarbital and phenytoin, when exposed to UDP-glucuronyl transferase, may slightly decrease the concentration of abacavir in plasma.

Ethanol: Ethanol slows down the metabolism of abacavir, which leads to an increase in AUC by 41%. However, the clinical significance of this change is small. Abacavir does not affect the metabolism of ethanol.

Methadone: According to pharmacokinetic studies, the use of abacavir at a dose of 600 mg 2 times a day in combination with methadone reduces Cmax of abacavir in blood serum by 35%, increases Tmax in serum by 1 hour, but does not change AUC. The clinical significance of these changes is small.

The same study found that abacavir increases systemic clearance of methadone by 22%. In most cases, these changes are also regarded as clinically insignificant, however, in certain situations, a dose change of methadone may be required.

Retinoids: retinoids, for example, isotretinoin, are eliminated with the participation of alcohol dehydrogenase, therefore, they can interact with abacavir, however, to date, no special studies have been conducted.

Ribavirin: due to the fact that abacavir and ribavirin have the same phosphorylation pathways, an interaction between these substances is expected, which may lead to a decrease in the intracellular phosphorylation of ribavirin metabolites and potentially lead to a decrease in the likelihood of achieving a stable virologic response in hepatitis C coinfected HIV-infected patients taking pegylated interferon and ribavirin therapy. Conflicting data on the simultaneous use of abacavir and ribavirin have been published. According to some reports, HIV-infected patients receiving abacavir-containing drugs may be at risk of a low frequency of response to antiviral therapy with pegylated interferon and ribavirin. Caution must be exercised while taking these drugs.

Overdose of

Symptoms of

In clinical studies, no adverse reactions were found with abacavir in single doses up to 1200 mg and daily allowance up to 1800 mg. The effect of the drug in higher doses has not yet been studied.

Treatment

In the event of an overdose, the patient is monitored to detect symptoms of poisoning and timely initiation of treatment. If necessary, carry out symptomatic treatment. The effectiveness of peritoneal dialysis and hemodialysis for abacavir removal is unknown.

Storage conditions

At a temperature not exceeding 25 ° C in the manufacturer's packaging.

Keep out of the reach of children.

Expiration

3 years.

Dosage form

tablet

Appointment

Vzrosl m on purpose doctor, Detyam on purpose doctor

Indications

HIV infection



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