Rifapex

The drug Rifapex contains the active substance known as rifapentine. Rifapentine belongs to the group of antibiotics of the rifampicin class. It is widely used to treat tuberculosis and prevent tuberculosis in some patients.

Rifapentine, like rifampicin, has antibacterial activity and can be effective in the treatment of infections caused by Mycobacterium tuberculosis. It is often used as part of combination therapy for tuberculosis, especially in patients with multidrug resistance.

Like many antibiotics, rifapentine can have side effects, including gastrointestinal disorders, changes in the circulatory system, liver and other organs, and interactions with other medicines. Therefore, it is important to use it only under the supervision of a physician who can evaluate the indication, select the dosage, and monitor the treatment.

Indications Rifapexa

1. Treatment of tuberculosis: Rifapentine is often prescribed as a component of combination antibiotic therapy for the treatment of tuberculosis. It is effective against Mycobacterium tuberculosis, the bacterium that causes tuberculosis, and can be used with other antibiotics to treat active disease.
2. Tuberculosis prophylaxis: Rifapentine is sometimes used to prevent tuberculosis in people at increased risk of developing the disease. For example, in persons with positive mantoux or skin tests for tuberculosis, in patients with HIV infection, or in those who have been in contact with persons infected with tuberculosis.
3. Treatment of infections caused by other types of mycobacteria: In rare cases, rifapentine may be used to treat infections caused by other types of mycobacteria, including Mycobacterium avium complex (MAC).

Release form

1. Oral tablets: This is the most common form of rifapentine. Tablets usually contain 150 mg or 300 mg of the active ingredient. This form is convenient to take daily at home.
2. Oralsuspension powder: Oral suspension powder may be suggested for children or adults who have difficulty swallowing tablets. The suspension allows precise dosing of the medicine and makes it easier to take for those with swallowing problems.

Pharmacodynamics

The mechanism of action of rifapentine is related to its ability to inhibit the activity of bacterial RNA polymerase. This leads to disruption of RNA and protein synthesis in the bacterial cell, resulting in its death. Rifapentine also has good activity against pathogens resistant to other antibiotics.

Like other antibiotics, rifapentine can cause various side effects such as digestive disorders, headaches, allergic reactions, and others. When prescribing and using rifapentine, it is important to follow your doctor's recommendations and be monitored regularly.

Pharmacokinetics

1. Absorption: Rifapentine has good and rapid absorption from the gastrointestinal tract after oral administration. Food may affect the rate and extent of its absorption.
2. Distribution: After absorption, rifapentine is evenly distributed throughout body tissues, including lungs, liver, kidneys, and bones.
3. Metabolism: The main pathway of rifapentine metabolism is associated with its oxidation and demethylation in the liver. It is metabolized with the participation of cytochrome P450 enzyme, which may lead to interactions with other drugs metabolized by this enzyme.
4. Excretion: Rifapentine is excreted mainly with bile and to a lesser extent with urine.
5. Semi-Elimination: The half-life of rifapentine is about 50 hours.

Dosing and administration

For the treatment of active tuberculosis in adults:

• Rifapentine is usually taken in combination with other anti-TB drugs.
• The standard dose is 600 mg once daily for the first two months of treatment, depending on the treatment regimen and combination with other drugs.
• The dosage and duration of treatment can then be adjusted by your doctor.

For the treatment of latent tuberculosis:

• The dosage and treatment regimen for latent tuberculosis may vary. For example, adults and children over 12 years of age may be prescribed a dose of 900 mg of rifapentine in combination with isoniazid once a week for 3 months.
• It is important to strictly follow the doctor's instructions regarding the treatment regimen.

General application guidelines:

• Rifapentine should be taken orally, preferably at the same time each day to maintain a stable concentration of the drug in the blood.
• The drug can be taken independently of meals, but taking it with food may help reduce gastrointestinal side effects.
• During treatment with rifapentine, it is important to see your doctor regularly to monitor the effectiveness of treatment and identify possible side effects.

Use Rifapexa during pregnancy

The use of rifapentine during pregnancy may pose certain risks to the fetus. There is insufficient data on its safety during pregnancy and its use should be performed only if absolutely necessary and under medical supervision.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to rifapentine or any other ingredient of the drug should not use it.
2. Hepaticinsufficiency: The use of rifapentine may be undesirable in patients with severe liver disease such as cirrhosis or hepatitis.
3. Pregnancyand breastfeeding: The use of rifapentine during pregnancy or breastfeeding should be performed only when strictly necessary and under medical supervision.
4. Pediatric age: Data on safety and efficacy of rifapentine in children are limited, therefore its use in children should be supervised by a physician.
5. Interactions with other medicines: Rifapentine may interact with various medicines, including antiretrovirals and antibiotics, which may increase or decrease their effectiveness.
6. Hyperbilirubinemia: The use of rifapentine may cause an increase in blood bilirubin levels and should therefore be used with caution in patients with this condition.
7. Other Conditions: In the presence of other serious conditions such as leukopenia or hypocalcemia, the use of rifapentine may require special caution and monitoring.

Side effects Rifapexa

1. Gastrointestinal disorders: For example, nausea, vomiting, diarrhea, dyspepsia (digestive upset), anorexia (loss of appetite).
2. Hypersensitivity tolight: Some patients may be hypersensitive to sunlight (photosensitization), which may cause sunburns or other skin reactions with prolonged exposure to sunlight.
3. AllergicReactions: Allergic reactions such as skin rash, pruritus, urticaria, angioedema, anapylaxis and even allergic alveolitis may occur.
4. Hepatotoxicity: Liver damage may occur, manifested as increased hepatic enzyme activity, jaundice or hepatitis.
5. Central nervous system: Dizziness, headache, asthenia (general weakness), drowsiness, anorexia may occur.
6. Other Reactions: Hemolytic anemia, leukopenia, tachycardia, vasculitis, arthralgia and myalgia may occur.

Overdose

There is limited information on rifapentine overdose, but serious side effects such as liver toxicity, dyspepsia, headaches, drowsiness, and risk of hepatitis can occur if overused.

In case of suspected rifapentine overdose, medical attention should be sought. Treatment of overdose will be symptomatic, aimed at elimination of possible manifestations of overdose and maintenance of body functions.

Interactions with other drugs

1. Antibiotics: Rifapentine may decrease blood concentrations of antibiotics such as macrolides (erythromycin, clarithromycin) and azoles (ketoconazole, fluconazole).
2. Antituberculosis drugs: Rifapentine may interact with other antibiotics for the treatment of tuberculosis, such as isoniazid and rifampicin, and lead to a decrease in their effectiveness.
3. Antiviral drugs: Rifapentine may decrease the concentration of antiviral drugs such as antiviral protease inhibitors and nucleoside analogs, which may reduce their effectiveness.
4. Anticoagulants: Rifapentine may increase or decrease the effect of anticoagulants (anti-clotting drugs) such as warfarin and may lead to changes in blood clotting.
5. Immunosuppressants: Rifapentine may decrease the concentration of immunosuppressants such as cyclosporine, thus reducing their effectiveness.
6. Drugs used totreat cardiovascular disease: Rifapentine may interact with some drugs used to treat cardiovascular disease, such as antiarrhythmic drugs, and alter their effectiveness.