Emtritab, 200 mg 30 pcs

.

Indications

Active ingredient

Composition

Active ingredient:

Emtricitabine 200 mg

Excipients:

The core: pregelatinized starch – 12.0 mg, colloidal silica (aerosil grade A-300) – 2.0 mg, croscarmellose sodium – 12.0 mg, lactose – 118.0 mg, magnesium stearate – 4.0 mg, microcrystalline cellulose – 40.0 mg.

The film coating: hydroxypropyl methylcellulose (hypromellose) – 8.7 mg, copovidone 0.3 mg, macrogol 6000 – 1.74 mg, talc – 0.3 mg, titanium dioxide – 0.96 mg.

How to take, the dosage

Orally as part of combination therapy, regardless of meals.

In children under 18 years of age and weighing more than 33 kg: 200 mg once daily.

If there is a delay in taking the drug for less than 12 hours, the missed dose should be taken as soon as possible and the normal dosing regimen resumed. If the medication is more than 12 hours late, the missed dose should not be taken; the next dose of emtricitabine should be taken at the usual time.

If a patient vomits within 1 hour of taking the drug, another dose of emtricitabine must be taken. If the patient vomits more than 1 hour after taking the drug, there is no need to take another dose of emtricitabine until the next scheduled dose of the drug is received.

Patients with impaired renal function

In children with impaired renal function it is recommended the same scheme of adjustment of the drug dosage regimen depending on creatinine clearance value as in adults. Patients with impaired liver function

In patients with impaired liver function the use of emtricitabine has not been studied. The drug should be used with caution in this category of patients.

Elderly patients

The use of emtricitabine has not been studied in patients older than 65 years. The drug should be used with caution in this category of patients because of possible reduction of renal excretory function.

Special Instructions

Patients should be warned that treatment with antiretrovirals, including emtricitabine, does not prevent the risk of HIV transmission to other people through sexual contact or blood transfusion. Patients must therefore take appropriate precautions.

Opportunistic infections

Renal dysfunction

In patients with renal insufficiency (with creatinine clearance < 50 ml/min) or terminal chronic renal failure requiring dialysis, correction of emtricitabine dosing regimen is recommended (see section “Dosage and administration”).

Hepatic impairment

The pharmacokinetics of emtricitabine in patients with hepatic impairment has not been studied. But since emtricitabine is slightly metabolized in the liver, no significant effect of hepatic impairment on the pharmacokinetics of the drug is expected.

Lactoacidosis/extensive hepatomegaly with fatty liver dystrophy In HIV-infected patients (predominantly women) taking nucleoside analogues as monotherapy or in combination with other antiretroviral drugs, cases of lactoacidosis, usually accompanied by marked hepatomegaly and fatty liver dystrophy, including a fatal outcome, have been described. Symptoms that may indicate the development of lactoacidosis include: general weakness, loss of appetite, sudden unexplained weight loss, disorders of the gastrointestinal tract and respiratory system (shortness of breath), the appearance of neurological symptoms (including motor disorders). Lactoacidosis leads to high mortality in the absence of emergency treatment and may be associated with pancreatitis, hepatic or renal failure. Lactoacidosis usually appears after several months of therapy. Patients with co-infected hepatitis C who receive interferon alfa and ribavirin therapy may represent a special risk group. These patients require close monitoring.

Treatment with emtricitabine always requires caution, especially if patients have risk factors for liver disease. In case of appearance of clinical or laboratory signs of lactoacidosis or liver dysfunction (including heiatomegaly and fatty liver dystrophy even in absence of expressed increase in liver transaminases level) emtricitabine should be stopped. Redistribution/accumulation of subcutaneous fat

In some patients, combination antiretroviral therapy may be accompanied by redistribution/accumulation of subcutaneous fat, including decreased peripheral fat and increased visceral fat, weight loss in the extremities and face, increased mammary glands and fat deposition on the back of the neck and back (“buffalo hump”), and increased serum lipid and blood glucose concentrations. Although all drugs in the protease inhibitor and nucleoside reverse transcriptase inhibitor classes can cause one or more of the above adverse reactions associated with the common syndrome often referred to as lipodystrophy, accumulating evidence suggests that there are differences between individual members of these drug classes in their 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, older age, and duration of antiretroviral therapy play an important, perhaps synergistic, role in the development of this complication. The long-term effects of these adverse reactions are currently unknown. The clinical evaluation of patients should include assessment of physical signs of adipose tissue redistribution. Serum lipid and blood glucose concentrations should also be measured. Lipid metabolism disorders should be corrected, guided by their clinical manifestations.

Immune recovery syndrome

In patients who have received combination antiretroviral therapy, including emtricitabine, immune recovery syndrome has been observed. Asymptomatic or residual opportunistic infections (including those caused by Mycobacterium avium, Mycobacterium tuberculosis, Pneumocystis carinii, Cytomegalovirus) may worsen during immune recovery, which may require additional examination and treatment. Autoimmune diseases (such as Graves’ disease, polymyositis and Guillain-Barré syndrome) were observed against the background of immune recovery, but the time of the 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 osteonecrosis is considered to be multifactorial (including glucocorticosteroid use, alcohol consumption, severe immunosuppression, high body mass index), cases of osteonecrosis have been reported particularly in patients with advanced HIV infection and/or with long-term combination antiretroviral therapy. Patients should be advised to consult a physician if they experience joint pain, stiffness in the joints, or difficulty in movement.

Mitochondrial dysfunction

The ability of nucleotide and nucleoside analogues to cause varying degrees of mitochondrial damage has been demonstrated under in vitro and in vivo conditions. Mitochondrial abnormalities have been reported in HIV-negative neonates exposed intrauterine and/or postnatally to nucleoside analogues. The main manifestations of mitochondrial dysfunction are hematological disorders (anemia, neutropenia) and metabolic disorders (hyperlactatemia, hyperlipasemia). These changes are often of transient nature. Some remote neurological disorders (hypertension, seizures, behavioral disorders) have been reported. All children exposed intrauterus to nucleosides or nucleoside analogues, even HIV-negative newborns, should be closely monitored clinically and laboratory and screened for possible mitochondrial abnormalities if they show signs or symptoms.

Patients co-infected with HIV and hepatitis B or C virus

The risk of hepatotoxic effects of antiretrovirals in patients co-infected with HIV and hepatitis B or C virus is higher than in those with HIV infection alone. Therefore, patients with chronic hepatitis B or C who take antiretroviral drugs at the same time are at increased risk of adverse effects on the liver, with possible death. These patients must be closely monitored, both clinically and laboratory.

Cancellation of therapy with emtricitabine may provoke a severe exacerbation of hepatitis in patients infected with hepatitis B virus (HBV). Therefore it is recommended to screen patients for viral hepatitis B before initiating antiretroviral therapy. In patients infected with HIV-1 and HBV it is necessary to monitor liver function carefully, but at least for some months after emtricitabine withdrawal. Resumption of therapy for viral hepatitis may be needed in some cases. In patients with severe liver disease (cirrhosis) it is not recommended to stop the treatment as worsening of hepatitis appearing after discontinuation of therapy can lead to decompensation of liver function.

Contraindications

Hypersensitivity to emtricitabine and other drug components.

Children under 3 years of age and weighing less than 33 kg (for this dosage form).

The period of lactation.

Simultaneous use with combined drugs containing emtricitabine and with lamivudine, zalcitabine.

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption. because the drug contains lactose.

Hepatic impairment, advanced age, pregnancy, liver disease, concomitant use with drugs with excretion by active tubular secretion.

Side effects

Blood and hemopoietic system: often – neutropenia; infrequently – anemia.

The immune system: often – allergic reactions.

The digestive system: very common – diarrhea, nausea; common – increased amylase activity, including increased pancreatic amylase activity; increased serum lipase activity, vomiting, abdominal pain, dyspepsia.

Nervous system disorders: very often – headache, often – dizziness. Mental disorders: often – insomnia, pathological dreams.

Hepatobiliary system disorders: often – increase of aspartate aminotransferase (ACT) and/or alanine aminotransferase (ALT) activity in serum, hyperbilirubinemia.

Skin disorders: common – vesiculobulic rash, pustular rash, maculopapular rash, rash, pruritus, urticaria, skin color changes (pigmentation increase); infrequent – angioedema.

Skeletal, muscular and connective tissue disorders: very common – increase of creatine kinase activity.

Others: pain, asthenia.

The combination antiretroviral therapy was associated with metabolic abnormalities such as hypertriglyceridemia, hypercholesterolemia, hyperglycemia and hyperlactatemia; redistribution/accumulation of subcutaneous fat (lipodystrophy).

In HIV-infected patients who have taken nucleoside analogues, cases of lactoacidosis have been described, usually accompanied by marked hepagomegaly and fatty liver dystrophy. The frequency of development depends on many factors, including the specific combination of antiretrovirals.

Osteonecrosis has been reported in patients with risk factors such as late-stage HIV infection or long-term combination antiretroviral therapy.

Patients taking emtricitabine or other antiretrovirals may develop opportunistic infections or other complications of HIV infection.

Children

In clinical trials, the side effects of the drug in pediatric and adult patients were similar. Hyperpigmentation was the most common. Anemia was an additional adverse reaction seen in clinical studies in children.

Overdose

In case of overdose, the patient should be examined for possible signs of intoxication. If necessary, standard supportive therapy is used.

Hemodialysis may be used to eliminate emtricitabine; a 3-hour hemodialysis procedure results in removal of approximately 30% of the drug dose taken. Interaction with other medicinal products

The possibility of pharmacokinetic interaction with the drugs which are metabolized with CYP450 isoenzymes is not high, because emtricitabine is not an inhibitor of these isoenzymes.

Emtricitabine is excreted mainly by the kidneys. Concomitant use of emtricitabine with drugs that impair renal function or compete for active tubular secretion may lead to increased serum concentrations of emtricitabine and/or other drugs that are excreted by the kidneys. When prescribing emtricitabine in combination with zidovudine, indinavir, stavudine, famcyclovir and tenofovir disoproxil fumarate no clinically significant pharmacokinetic interactions of these drugs and emtricitabine were revealed.

Pregnancy use