Rifapentine

Rifapentine is an antibiotic that is widely used to treat infections caused by bacteria of the genus Mycobacterium, including Mycobacterium tuberculosis (the bacterium that causes tuberculosis). It belongs to the group of antibiotics in the rifampicin class, which also includes rifampicin.

Rifapentine has antimycobacterial properties and is commonly used in combination with other antibiotics to treat tuberculosis, especially in multidrug-resistant patients. It can also be used to prevent tuberculosis in persons in contact with infected persons or at high risk of developing the disease.

Rifapentine-based medicines are usually taken orally in tablet or capsule form. Like all antibiotics, rifapentine should only be used when prescribed by a doctor, following the recommended dosage and duration of treatment. It may have side effects and may interact with other medications, so it is important to discuss its use with a medical professional.

Indications Rifapentina

1. Treatment of tuberculosis: Rifapentine can be used together with other antibiotics to treat tuberculosis. This is especially important when multidrug-resistant TB occurs or the patient is noncompliant with previous treatment.
2. Tuberculosis prophylaxis: Rifapentine may be used as a prophylactic agent in some patients, especially those who are in contact with infected persons or have an increased risk of tuberculosis (e.g., patients with HIV infection).
3. Prevention of secondary infections in patients with Mycobacterium avium complex (MAC): In rare cases, rifapentine may be used to prevent secondary infections caused by Mycobacterium avium complex (MAC), especially in immunocompromised patients, such as those with HIV infection.

Release form

Rifapentine is usually available in the form of tablets for oral administration. Rifapentine tablets may contain different amounts of the active substance, but are most commonly found in dosages of 150 mg and 300 mg. This form allows precise dosing of the drug and is convenient for patients to take.

In addition to tablets, other dosage forms such as capsules or powder for suspension may be available in some countries, but tablets are the most common and widely used form.

Pharmacodynamics

Its pharmacodynamics is related to its ability to inhibit bacterial RNA polymerase, which leads to disruption of RNA and protein synthesis in susceptible bacteria. This leads to the death of the bacteria and controls the spread of infection.

Rifapentine has a broad spectrum of activity against many bacteria, including the tuberculosis microorganism Mycobacterium tuberculosis, as well as other Gram-positive and Gram-negative bacteria. It is often used in combination with other antituberculosis drugs to treat tuberculosis and its resistant forms.

Pharmacokinetics

1. Absorption: Rifapentine is usually rapidly and completely absorbed from the gastrointestinal tract after oral administration. Food may slow its absorption but does not affect its completeness.
2. Metabolism: Rifapentine undergoes extensive metabolism in the liver via the cytochrome P450 system. The major metabolite is 25-deaza-riboflavin, which also has activity against microbes.
3. Elimination: Rifapentine and its metabolites are mainly excreted via the kidneys. Its half life is approximately 15-20 hours.
4. Interactions with food:Food intake affects the rate of rifapentine absorption, but does not affect its completeness. Therefore, it is usually taken independently of food intake.
5. Protein binding: Rifapentine binds to blood plasma proteins at a level of about 80-85%.
6. Systemic Exposure: Blood levels of rifapentine may vary depending on many factors including dose, food, liver and kidney status of the patient.
7. Pharmacodynamics: Rifapentine is an antibacterial drug active against many types of bacteria, including tubercle bacillus (Mycobacterium tuberculosis).

Dosing and administration

For the treatment of active tuberculosis in adults:

• Rifapentine is usually prescribed at a dose of 600 mg once daily in combination with other anti-TB drugs.
• The course of treatment and combination of drugs depend on the sensitivity of mycobacteria and can be adjusted depending on clinical response and laboratory test results.

For the treatment of latent tuberculosis:

• For adults and children over 12 years of age, rifapentine may be prescribed at a dose of 900 mg once weekly in combination with isoniazid for 3 months.

Method of Application:

• Rifapentine should be taken orally, regardless of food intake. However, taking it with food may help to reduce gastrointestinal side effects.
• It is important to take rifapentine regularly, at the same time each day, to ensure the best therapeutic effect.
• Do not stop taking rifapentine without consulting your doctor, even if you feel an improvement. A full course of treatment is necessary to completely cure the infection and prevent bacteria from developing resistance to antibiotics.

Use Rifapentina during pregnancy

The use of rifapentine during pregnancy may be associated with certain risks to the fetus. There is insufficient data on its safety during pregnancy and therefore its use should only be used for strict medical indications and under medical supervision.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to rifapentine or other components of the drug should not take it.
2. Hepatic insufficiency: The use of rifapentine may be undesirable in patients with severe hepatic dysfunction.
3. Pregnancy and lactation: Rifapentine use during pregnancy or lactation should be performed only under strict indications and under medical supervision.
4. Pediatric: Data on the use of rifapentine in children are limited, therefore use in children should be under the supervision of a physician.
5. Hyperbilirubinemia: Use of rifapentine may result in increased blood bilirubin levels and should therefore be used with caution in patients with hyperbilirubinemia.
6. Interactions with other medicines: Rifapentine may interact with other medicines, which may impair their effectiveness or cause undesirable side effects.
7. Other conditions: If you have other serious medicalconditions, such as heart, vascular, or kidney disease, the use of rifapentine may require special caution and supervision by your doctor.

Side effects Rifapentina

1. Gastrointestinal disorders: This may include nausea, vomiting, diarrhea, dyspepsia (digestive upset), anorexia (loss of appetite), and abdominal discomfort.
2. Neurologic symptoms: Dizziness, headache, drowsiness, asthenia (general weakness), or increased irritability may occur.
3. Allergic reactions: Include skin rash, pruritus, urticaria, angioedema, allergic dermatitis and rarely anaphylaxis.
4. Changes in blood count: There may be an increase or decrease in the number of white blood cells, platelets, or red blood cells.
5. Increased sensitivity to light: Rifapentine may cause photosensitization, which increases the risk of sunburn with prolonged exposure to sunlight.
6. Liver dysfunction: Increased blood levels of liver enzymes, jaundice and hepatitis may occur.
7. Other side effects: Other rare side effects such as skin hyperpigmentation, myalgia (muscle pain), arthralgia (joint pain), and tachycardia 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 the effectiveness of antibiotics such as azithromycin, clarithromycin, and tetracyclines.
2. Antifungal agents: Rifapentine may affect the metabolism of antifungal drugs such as fluconazole, ketoconazole and itraconazole, which may lead to changes in their concentrations in the blood.
3. Antiepileptic drugs: Interaction between rifapentine and antiepileptic drugs, such as carbamazepine and phenytoin, may reduce the concentration of the latter in the blood, which may lead to worsening of epilepsy control.
4. Antiviral drugs: Rifapentine may affect the metabolism of antiviral drugs such as lopinavir/ritonavir, which may lead to changes in their blood concentrations and an increased risk of side effects.
5. Cardiovascular drugs: Rifapentine may increase the effect of anticoagulants such as warfarin, which may lead to increased clotting time and risk of bleeding.