Pentacox® (Pentakoks®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceRifapentinRifapentin
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  • Pentacox®
    pills inwards 
    FARMASINTEZ, JSC (Irkutsk)     Russia
  • Ripafex
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    Lupine Co., Ltd.     India
    • Dosage form: & nbsp
    film-coated tablets

    Composition:

    Active substance:

    Rifapentin 150 mg

    Excipients:

    Each film-coated tablet contains:

    Core: cellulose microcrystalline 4144.4 mg, pregelatinized starch (LM-1500) -25.0 mg, giprolose-20.0 mg, edetic acid-0.3 mg, carboxymethyl starch sodium (sodium starch glycolate) - 15.0 mg, sodium lauryl sulfate - 10.0, ascorbic acid acid -0.3 mg, silicon colloidal dioxide (aerosil grade A-200) - 5.0 mg, macrogol 6000 (PEG-6000) - 5.0 mg, croscarmellose sodium (impellosis) - 10.0 mg, calcium stearate -5.0 mg.

    Shell: The ready-mixed instacoate 3370 is 10.0 mg (hypromellose 5.4 mg, diethyl phthalate -1.2 mg, ethyl cellulose 0.5 mg, talc 0.4 mg, titanium dioxide 1,751 mg, iron oxide red oxide 0.507 mg, iron oxide yellow oxide 0.224 mg).

    Description:
    Tablets are red-brown, color, round biconvex, covered with a film membrane, with an embossed "150" on one side. On a cross-section the tablet of red-brown color with white impregnations.
    Pharmacotherapeutic group:Anti-tuberculosis drug.
    ATX: & nbsp

    J.04.A.B   Antibiotics

    J.04.A.B.05   Rifapentin

    Pharmacodynamics:Rifapentin - Antituberculosis antibiotic, is a derivative of rifamycin. Inhibits DNA-dependent RNA polymerase in sensitive strains of Mycobacterium tuberculosis, but not in mammalian cells. Within the limits of therapeutic concentrations rifapentin exhibits bactericidal action against both extracellular and intracellular Mycobacterium tuberculosis. Rifapentin and its active metabolite (25-deacetyltriphapentin) accumulate in human monocyte macrophages, intracellular concentrations are higher than extracellular ones.

    There is a cross-resistance of strains of Mycobacterium tuberculosis between rifapentin and rifamycin. Cross-resistance between rifapentin and anti-tuberculosis drugs of the non-fefmicin series was not observed.
    Pharmacokinetics:
    Rifapentin is well absorbed from the gastrointestinal tract. After a single dose of 600 mg, the maximum concentration (C max) in the blood plasma is determined after 5-6 hours. Stable concentrations are achieved after 10 days of daily intake of the drug /

    Eating a meal increases the absorption of the drug. Compared to fasting, the area under the pharmacokinetic curve (AUC) and Cmax increased by 43% and 44%, respectively, when taking rifapentin with fatty foods.

    Rifapentin and its active metabolite 25-deacetyltriphapentin bind to blood plasma proteins by 98% and 93%, respectively.

    The half-life (T1 / 2) is approximately 13 hours. Rifapentin is excreted from the body with feces (70%) and urine (17%).
    Indications:The newly diagnosed drug-sensitive tuberculosis (all forms) in both the intensive phase and the continuation phase of treatment. Rifapentin is prescribed in complex therapy in combination with other antituberculous drugs.
    Contraindications:
    - Hypersensitivity to rifamycins.

    - Diseases of the liver and gastrointestinal tract in the stage of exacerbation.

    - Pregnancy, lactation.

    - Thrombophlebitis.

    - Children under 12 years.
    Carefully:
    - In patients with severe atherosclerosis.

    - With the carrier of hepatitis B and C.
    Pregnancy and lactation:
    The drug is contraindicated during pregnancy and lactation.
    Dosing and Administration:
    Inside, 1 time per day, regardless of food intake. The daily dose of rifapentin 10 mg / kg body weight (up to 600 mg) - 2-3 times a week. Simultaneously with rfapentin in an intensive phase of treatment appoint
    first-line antituberculosis drugs: isoniazid, ethambutol, pyrazinamide in doses corresponding to the instructions for the use of these drugs.
    If necessary rifapentin can be combined with a protionamide, cycloserine or levofloxacin.
    Side effects:

    Allergic reactions: fever, dermatitis; eosinophilia, anaphylactic shock.

    From the gastrointestinal tract: nausea, vomiting, diarrhea. Increased activity of "liver" transaminases, drug-induced hepatitis, jaundice.

    On the part of the blood system: thrombocytopenia; leukopenia; anemia.

    Overdose:
    Symptoms: nausea, vomiting, diarrhea, increased activity of "liver" transaminases, hepatitis, jaundice, thrombocytopenia, leukopenia, anemia.

    Treatment: gastric lavage; symptomatic therapy; prescription of choleretic preparations, diuretics.
    Interaction:

    Rifapentin is an inducer of cytochrome P450 isoenzymes. The simultaneous use of rifapentin with drugs metabolized by this enzyme system, such as protease inhibitors, reverse transcriptase inhibitors, can lead to a significant decrease in the concentration of these drugs in blood plasma and the loss of their therapeutic effect.


    Rifapentin can reduce the effectiveness of hormonal contraceptives (during treatment, patients should use reliable non-hormonal contraception).


    Rifapentin is an inducer of the isoenzymes CYP3A4 and CYP2C8 / 9, so when used simultaneously with drugs that are substrates for these isoenzymes, it is possible to increase their metabolism. Induction of isoenzymes caused by rifapentin; is observed within 4 days after taking the first dose and returns to the baseline level 14 days after the discontinuation of rifapentin. In addition, the degree of induction of enzymes with rifapentin depends on its dose and frequency of use: less pronounced activity is observed when taken at a dose of 600 mg at an interval of 72 hours compared with daily intake. When used simultaneously with rifapentin, a dose adjustment of medicinal products that are metabolized with the participation of isoenzymes CYP3A4 and CYP2C8 / 9: warfarin, phenytoin, quinidine, fluconazole, itraconazole, ketoconazole, haloperidol, phenobarbital, diazepam, propranolol, diltiazem, nifedipine, verapamil, digoxin, prednisone, clofibrate, hypoglycemic agents, derivatives of sulfonylureas, hormonal contraceptives (ethinyl estradiol, levonorgestrel), ciclosporin, tacrolimus, theophylline, methadone, sildenafil, levothyroxine, amitriptyline, nortriptyline.


    Pyrazinamide slows the excretion of rifapentin.


    Isoniazid and protionamide are synergists of rifapentin; when combined, antimicrobial activity increases.


    It is not recommended simultaneous administration of rifapentin with PASK, t. PASK disrupts the absorption of rifapentin.


    Patients receiving antacids are recommended to take rifapentin at least 1 hour before taking antacids or 2 hours afterwards.


    Simultaneous intake of alcohol can increase the risk of liver damage.

    Special instructions:
    Should not be used as a weekly long-term therapy (for 4 months) in combination with isoniazid in HIV-seropositive patients with pulmonary tuberculosis due to a high risk of treatment failure and / or relapse of tuberculosis.

    Rifapentin has not been studied as part of the initial therapy (within 2 months) in HIV-seropositive patients with pulmonary tuberculosis. .

    It is not recommended to apply rifapentin as a monotherapy.

    Rifapentin should be used with caution in patients with cavernous pulmonary tuberculosis - the lungs and / or presence of a causative agent in sputum after the initial phase of therapy or in the presence of bilateral lung injury due to a higher risk of recurrence.

    In HIV seropositive patients receiving rifapentin therapy in the long-term phase of treatment (within 4 months), there is a higher incidence of tuberculosis recurrence. The risk of recurrence is the presence, along with lung lesions, of extra-pulmonary tuberculosis, low CD4 cell count, the use of antifungal agents for azole derivatives, and the younger age of the patient.

    It is impossible to exclude the appearance of hyperbilirubinemia due to competition for the ways of excretion between rifapentin and bilirubin. During the treatment period, the level of bilirubin in the blood should be monitored.

    In patients with diseases or conditions predisposing to the development of neuropathy (including nutritional deficiencies, HIV infection, renal failure, alcoholism), in order to avoid the development of peripheral neuropathy, one should simultaneously apply pyridoxine.

    Against the background of rifapentin application, red-orange staining of tissues and / or body fluids (for example, skin, teeth, tongue, urine, feces, saliva, sputum, tear fluid, sweat, cerebrospinal fluid) is possible. Patients receiving rifapentin, do not wear contact lenses.

    Do not use rifapentin in patients with porphyria (we can not exclude the possibility of exacerbation of this disease).

    In case of development against the background of treatment of diarrhea caused by Clostridium difficile, appropriate therapy should be started immediately.

    Rifapentin should be used with caution in elderly patients, given the possible worsening of the liver, kidney, cardiovascular system, the presence of concomitant diseases and the simultaneous use of other medicines.

    The safety and efficacy of rifapentin in patients younger than 12 years of age have not been studied. During treatment with rifapentin, a monthly blood test, urine test; determination of the activity of "liver" transaminases; bilirubin direct and indirect.

    The microbiological examination should be carried out before the start of treatment, and also during the treatment to monitor the therapeutic response.Oral contraceptives in combination with rifapentin are not effective. Other contraceptives should be used.
    Effect on the ability to drive transp. cf. and fur:During treatment with rifapentin, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:Tablets, film-coated, 150 mg.
    Packaging:For 30, 50 or 100 tablets, coated with a film shell, placed in a can of polymer with a lid pulled with the control of the first opening. For 1 can, along with the instruction for use, is placed in a pack of cardboard.
    Storage conditions:In a dry, the dark place at a temperature of no higher than 25 C. Keep out of reach of children.
    Shelf life:2 years. Do not use after the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001055
    Date of registration:27.10.2011
    Date of cancellation:2016-10-27
    The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia
    Manufacturer: & nbsp
    Representation: & nbspPharmasynthesis, JSCPharmasynthesis, JSC
    Information update date: & nbsp20.05.2016
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