Universal reference book for medicines
Product name: PENTAKOKS

Active substance: rifapentine

Type: Antibiotic of the rifamycin group.
Anti-TB drug
Manufacturer: FARMASINTEZ (Russia) manufactured by PLETHICO PHARMACEUTICALS (India) packing and (or) secondary packaging and issuing quality control FARMASINTEZ (Russia)
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
The anti-tuberculosis antibiotic of the rifamycin group is cyclopentyl rifamycin.
Inhibits the DNA-dependent RNA polymerase of sensitive strains of Mycobacterium tuberculosis, but not in mammalian cells. In therapeutic doses, rifapentin exhibits bactericidal activity against intracellular and extracellular forms of Mycobacterium tuberculosis. Rifapentin and its active metabolite (25-deacetyltriphapentin) accumulate in human monocyte macrophages with an intra / extracellular ratio of approximately 24: 1 and 7: 1, respectively.
There is a cross-resistance of strains of Mycobacterium tuberculosis between rifapentin and rifamycin.
Cross-resistance between rifapentin and other anti-tuberculosis drugs was not observed.
PHARMACOKINETICS
After ingestion at a dose of 600 mg C max, rifapentin in blood plasma is reached after 4-6 hours. When taking rifapentin with fatty foods, AUC and C max increased by 43% and 44%, respectively.

The binding of rifapentin to plasma proteins (mainly with albumins) is 97.7%.

Under the influence of esterases, it is metabolized with the formation of an active metabolite of 25-deacetyltriphapentin.

T 1/2 is 13.19 ± 1.38 hours. It is excreted with feces (70%) and with urine (17%).
Within 7 days, 80% of the active substance is excreted from the body.
INDICATIONS
Treatment of pulmonary tuberculosis caused by Mycobacterium tuberculosis in combination with one or more anti-tuberculosis drugs.

DOSING MODE
Applied only with the sensitivity of the pathogen to this antibiotic.

Rifapentin is intended for oral administration at a dose of 600 mg 1-2 times a week at intervals of at least 3 consecutive days (72 hours) in combination with other anti-tuberculosis drugs (ethambuol, pyrazinamide, isoniazid, streptomycin).

Treatment is carried out according to a special scheme consisting of an initial phase of therapy, lasting 2 months and a subsequent phase, lasting 4 months.
The choice of an antituberculous agent for a combination is based on the sensitivity of the pathogen. The effectiveness of rifapentin in combination with ethambutol, pyrazinamide, isoniazid or streptomycin is shown.
The treatment is carried out under strict clinical control.

SIDE EFFECT
These reactions were observed with rifapentin as part of a combination therapy.

From the urinary system: pyuria, proteinuria, hematuria, urinary tract infections, incontinence episodes, cystitis, urethral diseases, pyelonephritis.

From the side of metabolism: hyperuricemia, hyperkalemia, hypoglycemia, increase in the content of non-protein nitrogen, hyperglycemia, increased LDH, hyperphosphatemia, weight loss, increased residual urea nitrogen, diabetes mellitus, increased activity of AP, hypophosphatemia, hypercalcemia, hypovolemia, , porphyria.

On the part of the hematopoiesis system: anemia, lymphopenia, neutropenia, leukocytosis, neutrophilia, thrombocytosis, thrombocytopenia, polycythemia, lymphadenopathy, lymphocytosis, hematoma, hematoma, purpura, thrombosis.

On the part of the body as a whole: back pain, pain in the whole body, chest pains, injuries, abdominal pain, fever, weakness, propensity for puffiness, asthenia, abscesses.

Dermatological reactions: rash, increased sweating, itching, acne, skin diseases, maculopapular rash, eczema, ulcerative skin lesions, hives, dry skin, furunculosis, skin pigmentation disorder, fungal dermatitis, nail diseases, erythematous rash, alopecia.

On the part of the respiratory system: hemoptysis, cough, upper respiratory tract infections, bronchitis, pharyngitis, dyspnea, pleurisy, loud breathing, pneumothorax, pneumonia, rhinitis, dyspnoea, pleural effusion, pneumonitis, sinusitis, increased sputum, pulmonary fibrosis, pathways, asthma, bronchospasm, laryngeal edema.

From the digestive system: anorexia, dyspepsia, vomiting, nausea, constipation, diarrhea, hemorrhoids, increased ALT and AST activity, gastroenteritis, gastritis, esophagitis, cheilitis, deterioration of the teeth, pancreatitis, proctitis, increased salivary glands volume, tenesmus, nonspecific gastric - intestinal disorders, bilirubinemia, hepatomegaly, jaundice, hepatotoxicity, hyperbilirubinemia, porphyria, diarrhea due to Clostridium difficile.

Infections: influenza, tuberculosis infection, other infections, shingles, infection with parasites and protozoa.

From the side of the central nervous system: insomnia, drowsiness, nonspecific convulsions, dysphonia, hypoesthesia, torticollis, hyporeflexia, meningitis, stupor, migraine, anxiety, impaired consciousness, stupor.

From the musculoskeletal system: arthralgia, arthritis, arthrosis, gout, myalgia, myositis, fracture of bones, muscle weakness, muscle spasm.

From the cardiovascular system: arterial hypertension, syncope, tachycardia, palpitation, orthostatic hypotension, pericarditis, deep vein thrombophlebitis, vascular disorders, vasodilation.

On the part of the reproductive system: penile disease, vaginitis, vaginal bleeding, leukorrhea, mastitis in men, prostate disease.

From the sense organs: conjunctivitis, nonspecific hearing disorders, otitis media, ear pains, external otitis media, perforation of the tympanic membrane, eye pain, eye disorders, loss of taste sensations.

Malignant neoplasms: pulmonary carcinoma, nonspecific neoplasm, carcinoma, lipoma.

Other: a change in the color of body fluids.

CONTRAINDICATIONS
Hypersensitivity to rifapentin and other antibiotics of the rifamycin group.

PREGNANCY AND LACTATION
Adequate and strictly controlled studies of the safety of rifapentin during pregnancy and lactation (breastfeeding) have not been conducted.

It is not known whether rifapentin is excreted in human milk.
It should be borne in mind that, when the drug is used, breast milk can acquire a reddish-orange color. If rifapentin is needed during lactation, the question of stopping breastfeeding should be addressed.
In experimental studies , rifapentin has been shown to have an embryothetotoxic effect in animals.

APPLICATION FOR FUNCTIONS OF THE LIVER
In patients with diseases or conditions predisposing to the development of neuropathy (including renal failure), pyridoxine (vitamin B 6 ) should be used simultaneously to avoid the development of peripheral neuropathy.

APPLICATION FOR CHILDREN
The safety and efficacy of rifapentin in patients younger than 12 years of age have not been studied.

APPLICATION IN ELDERLY PATIENTS
Use with caution in elderly patients, taking into account the possible deterioration in the function of the liver, kidneys, cardiovascular system, the presence of concomitant diseases and simultaneous use of other drugs.

SPECIAL INSTRUCTIONS
It 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 higher rate of treatment failure and / or tuberculosis recurrence in the presence of rifampin-resistant strains.

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

Do not use rifapentin as a monotherapy.

Caution should be used rifapentin in patients with cavernous pulmonary tuberculosis 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, in addition to lung lesions, of extrapulmonary 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 way of excretion between rifapentin and bilirubin.
between rifampin and bilirubin this competition is observed. During the treatment period, the level of bilirubin in the blood should be monitored.
Patients with diseases or conditions predisposing to the development of neuropathy (including malnutrition, HIV infection, renal failure, alcoholism, as well as pregnancy and the period of breastfeeding) should be simultaneously used to prevent the development of peripheral neuropathy pyridoxine (vitamin B 6 ).

Against the background of rifapentin application, red-orange staining of tissues and / or body fluids (eg, skin, teeth, tongue, urine, feces, saliva, sputum, tears, sweat, cerebrospinal fluid) is possible.

Do not use rifapentin in patients with porphyria, given that rifampin causes an exacerbation of the disease.

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

Use with caution in elderly patients, taking into account the possible deterioration in the function of the liver, kidneys, cardiovascular system, the presence of concomitant diseases and simultaneous use of other drugs.

The safety and efficacy of rifapentin in patients younger than 12 years of age have not been studied.

DRUG INTERACTION
Rifapentin is the inducer of cytochrome P450 isoenzymes, so when used concomitantly with drugs metabolized by this enzyme system, such as protease inhibitors, reverse transcriptase inhibitors, can cause a significant decrease in the concentration of these drugs in the 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 metabolized by these isoenzymes, it is possible to increase their metabolism.
Induction of isoenzymes caused by rifapentin is observed for 4 days after the first dose and returns to the baseline level 14 days after rifapentin withdrawal. In addition, the degree of induction of enzymes rifapentin depends on its dose and frequency of use: less pronounced activity is observed at an oral dose of 600 mg at an interval of 72 hours, compared with daily intake.
When used simultaneously with rifapentin, a dose adjustment of the following drugs metabolized with the participation of CYP3A4 and CYP2C8 / 9 isoenzymes may be required: warfarin, phenytoin, quinidine, fluconazole, itraconazole, ketoconazole, haloperidol, phenobarbital, diazepam, propranolol, diltiazem, nifedipine, verapamil, digoxin , prednisone, clofibrate, hypoglycemic agents derivatives of sulfonylureas, ethinyl estradiol, levonorgestrel, cyclosporine, tacrolimus, theophylline, methadone, sildenafil, levothyroxine, amitriptyline, nortriptyls
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The information is provided for your information, do not self-medicate, it is dangerous for your health.

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