Rifampicin

Rifampicin is an antibiotic that is widely used to treat infections caused by bacteria such as tuberculosis (TB) and some other bacterial infections. It belongs to the class of rifampicins, which act by inhibiting the synthesis of bacterial DNA, resulting in the destruction of bacteria.

Rifampicin is usually taken orally in tablet or capsule form, but can also be used as an injection. In some cases, such as in the treatment of tuberculosis, rifampicin may be used in combination with other antibiotics to enhance the effectiveness of treatment and prevent the development of resistance to the drug.

Like any medicine, rifampicin can cause side effects, including stomach upset, allergic reactions, changes in the blood such as decreased white blood cell counts, and effects on liver function. When using rifampicin, it is important to follow your doctor's advice and monitor any changes in your health.

Indications Rifampicin

1. Tuberculosis (also known as pulmonary and other organ tuberculosis): Rifampicin is a key component of tuberculosis treatment and is usually included in treatment regimens as part of combination antibiotic therapy.
2. Infections caused by other types of mycobacteria: In addition to tuberculosis, rifampicin may also be effective in treating infections caused by other types of mycobacteria such as Mycobacterium leprae (the pathogen that causes leprosy or leprosy) and others.
3. Skin and soft tissue infections: Rifampicin may be used to treat some bacterial infections of the skin and soft tissues, although this is a less common use.
4. Post-exposure prophylaxis: Rifampicin may be prescribed to prevent tuberculosis after exposure to an infected person.
5. Prophylaxis before surgery: Sometimes rifampicin may be used as a prophylactic antibiotic before surgery to prevent infection.

Release form

1. Capsules

Rifampicin capsules usually contain 150 mg or 300 mg of the active substance. This is the most common form of release for adults and children over a certain age who are able to swallow capsules.

2. Pills

Rifampicin tablets may be available in some regions and also contain 150 mg or 300 mg of rifampicin. Tablets offer an alternative to capsules for those who prefer this form.

3. Solution for intravenous injection

Rifampicin can also be administered intravenously, especially when oral administration is not possible or is ineffective. This form is usually used in hospital settings.

4. Powder for preparation of suspension

Rifampicin oral suspension powder is for children or adults who have difficulty taking solid dosage forms. The suspension allows you to dose the medicine accurately and makes it easier to take.

5. Pediatric forms

Specialized pediatric forms of rifampicin, such as suspensions or dissolvable tablets, may be available for children to facilitate dosing and administration.

Pharmacodynamics

1. RNA polymerase inhibitory effect: Rifampicin forms a complex with bacterial RNA polymerase, which interferes with its activity. This slows down RNA synthesis and interferes with bacterial replication.
2. Activity against mycobacteria: Rifampicin is widely used to treat infections caused by Mycobacterium tuberculosis and other types of mycobacteria.
3. Enzyme induction: Rifampicin can induce cytochrome P450 enzymes in the liver, which can lead to accelerated metabolism of many other drugs.
4. Resistance: Due to widespread use, resistance to rifampicin develops over time, which may require combination with other antibiotics to treat infections.
5. Pharmacokinetics: Rifampicin has good absorption from the GI tract and wide distribution in tissues. It is excreted mainly through the liver and biliary tract.

Pharmacokinetics

1. Absorption: Rifampicin is well absorbed from the gastrointestinal tract after oral administration. However, absorption may be reduced by concomitant administration with food, therefore rifampicin is recommended to be taken on an empty stomach or 1-2 hours before meals.
2. Distribution: Rifampicin is widely distributed throughout tissues and organs of the body, including lungs, liver, kidneys, spleen and others. It penetrates the blood-brain barrier and may form therapeutic concentrations in the CNS.
3. Metabolism: Rifampicin is metabolized in liver with formation of active metabolites. The main metabolite is 25-deacetylrifampicin.
4. Excretion: Excretion of rifampicin and its metabolites occurs mainly through bile and intestine. Part of the drug is also excreted through the kidneys.
5. Half-life: The half-life of rifampicin is about 3-4 hours, but may be prolonged in elderly patients or in the presence of hepatic or renal impairment.
6. Effect on metabolism of other drugs: Rifampicin is an inducer of cytochrome P450 enzymes, which may lead to accelerated metabolism of many other drugs, which reduces their concentration in the blood and may reduce their effectiveness. This is important to consider when rifampicin is combined with other drugs.

Dosing and administration

Adults

• Tuberculosis: The usual dose is 600 mg once daily, usually in combination with other anti-TB drugs. The course of treatment may last from 6 to 9 months or longer, depending on the doctor's advice and response to treatment.
• Lepra: Dosage and duration of treatment depend on the form of leprosy, but rifampicin is usually used at a dose of 600 mg once a month in combination with other drugs.
• Other bacterial infections: Dosage may vary depending on the type of infection and its severity.

Children

• Tuberculosis: The dosage for children is usually 10-20 mg/kg body weight per day (maximum daily dose is 600 mg). Rifampicin is taken once daily, usually in combination with other TB drugs.
• Thedosage and route of administration may vary depending on the child's age, weight, and specific condition.

General recommendations for intake

• Rifampicin should be taken on an empty stomach, 30 minutes before a meal or 2 hours after a meal to improve its absorption.
• It is important to take rifampicin regularly and as prescribed by your doctor, even if symptoms have improved.
• Do not stop taking rifampicin without consulting your doctor, as this may lead to a recurrence of the infection or the development of bacterial resistance to the antibiotic.

Use Rifampicin during pregnancy

The use of rifampicin during pregnancy is usually recommended only when the benefits of treatment outweigh the potential risks to the fetus. Rifampicin is an antibiotic that is widely used to treat tuberculosis and other bacterial infections. However, it can affect the metabolism of many other medicines, including oral contraceptives, which can reduce their effectiveness.

The use of rifampicin during pregnancy may be justified when a woman suffers from a serious infectious disease that cannot be treated with other antibiotics. In such cases, a careful assessment of the benefits and risks is important and the decision to use should be made in conjunction with a physician.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to rifampicin or any other ingredient of the drug should not use it.
2. Liver disease: In patients with hepatic insufficiency or other serious liver disease, the use of rifampicin may be undesirable due to its potential hepatotoxicity.
3. Interactions with other medicines: Rifampicin may interact with various medicines, including anticoagulants, oral contraceptives, antiretrovirals and other antibiotics. This may result in decreased drug effectiveness or increased risk of side effects.
4. Porphyria: Rifampicin may exacerbate the symptoms of porphyrin disease, so its use should be avoided in patients with this condition.
5. Pregnancy and lactation: Use of rifampicin during pregnancy or lactation should be performed only when strictly necessary and under medical supervision.
6. Pediatric age: The use of rifampicin in children under a certain age should only be administered and supervised by a physician.
7. Leukopenia: Rifampicin may cause leukopenia (decreased white blood cell count), so it should be used with caution in patients with this condition.

Side effects Rifampicin

1. Gastric disorders: Including nausea, vomiting, diarrhea, dyspepsia (digestive upset), appetite disorders, and intestinal dysbiosis.
2. Allergic reactions: May include urticaria, pruritus, skin rash, and angioedema (swelling of the face, lips, tongue, and/or larynx).
3. Blood changes: Rifampicin may cause anemia, agranulocytosis (decreased number of granulocytes in the blood), and thrombocytopenia (decreased number of platelets in the blood).
4. Increase in liver enzymes: In some people, rifampicin may cause an increase in liver enzyme levels in the blood.
5. Senses: Including changes in the color of urine, sweat and tears to orange, and changes in taste.
6. Changes in liver function: Including hepatitis and jaundice (jaundice of the skin and sclerae).
7. Hypersensitivity to sunlight: Increased skin sensitivity to sunlight and possible development of sunburn.
8. Changes in urine: Including red or brown staining of the urine, which is a normal reaction to rifampicin.

Overdose

Rifampicin overdose can lead to various symptoms and complications. However, accurate data on rifampicin overdose are limited.

The following symptoms may occur if rifampicin is taken in large amounts:

1. Gastrointestinal disorders: Nausea, vomiting, diarrhea, abdominal pain may occur as a result of rifampicin overdose.
2. Livertoxicity: Rifampicin may cause liver damage. In case of overdose, this effect may be aggravated, which may lead to jaundice, increased levels of liver enzymes in the blood and other signs of liver failure.
3. Neurological symptoms: In some cases, rifampicin overdose can cause headache, dizziness, drowsiness, agitation, seizures, and even coma.
4. Respiratory problems: A severe overdose of rifampicin can cause difficulty breathing, respiratory arrest, or hypoxia.
5. Other symptoms: Symptoms of allergic reactions such as skin rash, itching, swelling, and anaphylactic shock may also occur.

Interactions with other drugs

1. Oral contraceptives: Rifampicin may decrease the effectiveness of oral contraceptives and increase the risk of unintended pregnancy in women taking them together with rifampicin. For women taking oral contraceptives, an alternative method of contraception or additional contraceptive measures may be required while taking rifampicin.
2. Anticoagulants: Rifampicin may decrease blood concentrations of anticoagulants, such as warfarin, which may lead to a decrease in their anticoagulation effect and increase the risk of thromboembolic events. Monitoring of anticoagulant levels and their dose adjustment may be required in concomitant use with rifampicin.
3. Antiepileptic drugs: Rifampicin may decrease blood concentrations of antiepileptic drugs such as carbamazepine, phenytoin and valproate, which may lead to a decrease in their effectiveness. Monitoring of antiepileptic drug levels and dose adjustment may be required when concomitant use with rifampicin.
4. Antitubercular drugs: When combined treatment with rifampicin and other antitubercular drugs may require regular monitoring of the patient and dose adjustment depending on the therapeutic effect and side effects.

Storage conditions

Rifampicin is usually stored in a dry place at room temperature, i.e. 15°C to 25°C, in the original package, protected from light and moisture. The instructions on the label or your doctor's instructions should be followed. Special storage conditions may also apply if necessary, so it is important to read the instructions on the package or consult your doctor or pharmacist.