R-Butin

R-Butin is an antibacterial agent with a pronounced bactericidal effect. It belongs to the group of modern semi-synthetic broad-spectrum antibiotics and is characterized by high activity in the fight against mycobacteria harmful to the body. In medicine, the drug is used to treat and prevent various infections, in particular, tuberculosis.

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Indications R-Butin

R-Butin is used as part of complex therapy as an effective anti-tuberculosis drug. The international non-proprietary name of the drug is "Rifabutin".

Indications for use of R-Butin: treatment of chronic pulmonary tuberculosis caused by rifampicin-resistant strains of Mycobacterium tuberculosis. The antibiotic is active against infections caused by Mycobacterium tuberculosis and Mycobacterium xenopi bacteria, M. tuberculosis, M. xenopi and M. avium intracellulare complex (MAIC) microbacteria, and can be used in patients with severe immunodeficiency (HIV-infected and AIDS patients), both for treatment and for prevention.

The purpose of treatment with R-Butin is to prevent the likelihood of tuberculosis relapse and reduce the likelihood of infecting others. The drug helps to avoid the development of drug resistance in patients and also prevents the death of the patient. The laboratory criterion for the effectiveness of the drug is the reduction and cessation of the release of M. tuberculosis.

As a result of taking the drug, patients experience a decrease in the severity of symptoms, a decrease in the frequency of relapses, and an increase in body weight.

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Release form

R-Butin is a semi-synthetic antibiotic that is effective against various types of mycobacteria, including Mycobacterium tuberculosis.

The drug is available in capsules of 150 mg each, filled with a red-violet powder that does not dissolve in water, dissolves poorly in ethanol and dissolves in methanol and chloroform.

Many drugs are currently available in capsules, like R-Butin. The capsule dosage form has a number of advantages: it ensures high accuracy of dosing of drugs, the contents of the capsules are absorbed in the stomach more easily and quickly. The capsule shell protects the gastric mucosa and helps prevent the inactivation of the antibiotic by enzymes of the gastric juice. In addition, the drug in capsules is protected from adverse factors (light, moisture, air, mechanical impacts). In the manufacture of capsules, fewer excipients are used than in the production of tablet forms of drugs. The corrective ability of capsules is the elimination of the unpleasant taste and smell of antibiotics. High aesthetics is achieved by using various dyes to obtain capsule shells.

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Pharmacodynamics

R-Butin (Rifabutin) is a semi-synthetic broad-spectrum antibiotic and is used in combination with other drugs that have an active effect on a number of infections, including the treatment and prevention of tuberculosis.

Pharmacodynamics R-Butin: the drug has an active effect on microorganisms located both extracellularly and intracellularly. It has a pronounced bactericidal effect and selectively suppresses DNA-dependent RNA polymerase of microscopic bacteria Mycobacterium spp., as well as atypical mycobacteria (Mycobacterium tuberculosis, Mycobacterium avium). In addition, R-Butin is active against gram-positive microorganisms. Monotherapy with this drug leads to rapid development of resistance.

There are no clear clinical criteria for assessing the effectiveness of the drug. However, it has been clinically proven that the antibacterial agent reduces the severity of symptoms, promotes weight gain in the patient, and reduces the frequency of relapses. The main purpose of taking the antibiotic is to stop the release of M. tuberculosis, prevent possible relapses, infection of others, and death in the treatment of patients.

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Pharmacokinetics

R-Butin is rapidly absorbed from the gastrointestinal tract into the blood immediately after oral administration. The maximum level of the active substance of the drug is reached approximately 2-4 hours after taking the antibiotic. The drug has a depressing effect on the synthesis of pathogenic bacteria by inhibiting their DNA-dependent RNA polymerase. Perhaps, it is the high level of intracellular concentration of Rifabutin that plays a key role in ensuring the activity of the drug with respect to such intracellular pathogenic microorganisms as mycobacteria.

The pharmacokinetics of R-Butin is linear. Rifabutin has the property of quickly penetrating into cells and distributing in the tissues of many internal organs, with the exception of the brain. Its highest concentration is created in the lung tissue. It has been clinically proven that the concentration in the lungs 24 hours after taking the antibiotic is 5-10 times higher than its concentration in the blood plasma. At the same time, poor penetration of the drug through the BBB - the blood-brain barrier is noted. The bioavailability of Rifabutin is 20%, and the binding index to plasma proteins is 85%. The drug is completely biotransformed in the liver tissue, forming inactive metabolites. 53% of R-Butin in the form of metabolites is excreted through the kidneys, 30% - with bile, 5% - with bile in its original form, and the same amount - with urine. The half-life of the antibiotic in the body is approximately 35-40 hours.

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Dosing and administration

R-Butin is usually prescribed to the patient once a day. The capsule is taken orally, before or after meals. The duration of taking the antibiotic depends on the treatment regimen.

Method of administration and dosage: adults are usually prescribed from 150 to 600 mg of R-Butin per day. However, in general, taking Rifabutin depends on the specific situation:

• In case of treatment of re-diagnosed pulmonary tuberculosis, 150-300 mg of Rifabutin should be taken per day (duration of treatment is 6 months).
• For the treatment of patients with chronic multidrug-resistant pulmonary tuberculosis, 300-450 mg of the drug per day is prescribed (treatment lasts 6-9 months).
• In case of secondary mycobacterial infection of non-tuberculous nature – from 450 to 600 mg of the drug per day (duration of treatment – up to 6 months).
• For the prevention of MAC infections in patients with severe immunodeficiency and AIDS - 300 mg of the drug R-Butin per day.
• In case of serious disorders and failures in kidney function (the CC (creatine kinase) indicator is below 30 ml/min), it is necessary to reduce the dosage of R-Butin by 50%.
• In combination with other anti-tuberculosis drugs (Ethambutol or Isoniazid, etc.) - 450-600 mg of the drug per day.

Elderly patients are prescribed the usual dosage regimen of R-Butin: orally - once a day, regardless of food.

During the entire period of treatment with R-Butin, it is recommended to periodically monitor platelet and leukocyte counts in the peripheral blood, as well as liver enzyme activity. When taking R-Butin in high doses or in combination with Clarithromycin, the patient has an increased risk of developing uveitis (an inflammatory process in the vascular membrane of the eye). In this case, the patient needs to consult an ophthalmologist and also temporarily stop taking the drug.

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Use R-Butin during pregnancy

R-Butin is contraindicated during pregnancy and lactation, this is clearly stated in the instructions for the drug. Therefore, pregnant women are not recommended to take this antibiotic, like many others.

The use of R-Butin during pregnancy is fraught with negative consequences for the health of the expectant mother and her child. If it is necessary to use Rifabutin during breastfeeding, it is necessary to decide on the urgent termination of lactation. As for clinical results, strictly controlled studies that would concern the use of R-Butin during pregnancy have not been conducted.

In practical medicine, only those antibiotics are used whose action does not negatively affect the development of the fetus. Usually, antibiotic treatment during pregnancy makes sense only when the therapeutic effect regarding the infectious pathology of the expectant mother is higher than the harm (probable or potential) to the fetus. Pregnant women should take into account that almost all antibiotics are dispensed by prescription, so a visit to the doctor in case of illness is mandatory. Medical supervision of therapy allows you to avoid negative consequences that can be caused by improper treatment, in particular, independent uncontrolled intake of antibacterial agents.

Contraindications

R-Butin is used in medicine to treat infections caused by bacteria, including tuberculosis. Despite its effectiveness and sustained action, the drug has a number of contraindications that must be taken into account before starting treatment.

Contraindications for the use of R-Butin:

• pregnancy,
• lactation period (breastfeeding),
• hypersensitivity to the drug,
• age under 18,
• individual intolerance to Rifabutin and other ansamycins,
• severe disturbances in the functioning of the liver and kidneys.

When taking R-Butin, it is necessary to strictly adhere to the treatment regimen established by the attending physician. It should be taken into account that during treatment, skin, urine, and saliva may become reddish-orange.

If the patient's condition worsens while taking the antibiotic, it is necessary to consult a doctor. It should also be taken into account that the safety of R-Butin in children's age groups has not been studied. Therefore, children are contraindicated to take this drug. This is due to the possibility of increased hepatotoxicity of Rifabutin due to age-related changes in the liver.

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Side effects R-Butin

R-Butin should be taken strictly as prescribed by the doctor. If the condition worsens or any unfavorable symptoms are observed, the patient should consult with the attending physician regarding further use of the drug. It may be necessary to reduce the dose of the drug or find alternative ways to treat the infection.

Side effects of R-Butin may include:

• nausea and vomiting,
• changes in taste (dysgeusia),
• diarrhea and abdominal pain,
• jaundice,
• increased activity of liver transaminases,
• anemia (decreased hemoglobin content in red blood cells),
• thrombocytopenia (decreased platelet count),
• leukopenia (decrease in the content of leukocytes in the blood),
• arthralgia (joint pain),
• myalgia (muscle pain).

In addition, side effects of the body on taking the drug R-Butin may include allergies (rash, fever), rarely uveitis (inflammation of the vascular membrane of the eye), bronchospasm (sudden contraction of the muscles of the bronchial walls), and anaphylactic shock.

In case of an antibiotic overdose, side effects may increase. In this case, the patient needs to have his stomach washed. Symptomatic therapy and diuretics are also prescribed.

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Overdose

R-Butin should be used according to the treatment regimen developed by a medical specialist, strictly following the dosage established by him. Otherwise, the following symptoms of drug overdose are possible: dizziness, nausea, vomiting, increased side effects (in particular, abdominal pain, diarrhea, jaundice, changes in blood composition, etc.), as well as unconsciousness. It is strictly forbidden to carry out treatment with R-Butin on your own.

Overdose of a drug is a very dangerous condition that can lead to negative consequences and cause irreversible reactions of the body. At the first signs of an overdose, you must immediately call an ambulance. Before the doctor arrives, the patient must wash out the stomach by inducing vomiting. For this purpose, you can drink 3 glasses of salted water (2 teaspoons of salt per 200 mg). After washing the stomach, you should take several crushed tablets of activated charcoal.

In serious cases of R-Butin overdose, the patient needs inpatient medical care. Treatment is carried out taking into account the symptoms. In this case, drugs with a reverse effect or aimed at supporting the liver are usually prescribed.

It is very important to determine what drug the person was poisoned with. This will help to develop the correct treatment tactics and predict possible side effects.

Usually, drugs aimed at For example, in case of an overdose of a drug that lowers blood pressure, drugs that stimulate the heart are prescribed.

Interactions with other drugs

R-Butin has different effects on some medications and can cause organic changes in the body. In particular, it promotes the acceleration of drug metabolism in the liver.

Interactions of R-Butin with other drugs:

• zidovudine - Rifabutin reduces its concentration in plasma;
• clarithromycin, fluconazole - increase the concentration of P-Butin in blood plasma;
• Oral contraceptives - Rifabutin reduces their effectiveness.

The development of clinically significant interactions of the drug R-Butin with such drugs as ethambutol, sulfonamides, sulfonamides, theophylline, zalcitabine, pyrazinamide is unlikely. In addition, Rifabutin affects the pharmacokinetics of drugs metabolized by the cytochrome P450 IIIA system.

The patient must strictly adhere to the treatment regimen prescribed by the doctor and take R-Butin in the strictly specified dosage. The drug can be taken on an empty stomach, during or after meals. Rifabutin's activity is manifested in the coloring of urine, tears, skin, saliva and even contact lenses in a reddish-orange color.

If you are taking any medications, you should tell your doctor before starting treatment with Rifabutin to avoid possible negative consequences.

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Storage conditions

R-Butin must be stored in accordance with the rules prescribed by the Ministry of Health for List B drugs, which include potent drugs that must be stored with special care and always separately from other drugs.

Storage conditions for R-Butin:

• at a temperature not exceeding 25°C;
• in a dry place, well protected from light;
• in sealed factory packaging.

Under the influence of direct sunlight, chemical reactions may occur in the capsules, which often lead to the loss of the therapeutic effect and rapid deterioration of the drug. For this reason, R-Butin should be stored in a dark place, preferably on a separate shelf in a cabinet with opaque doors.

In addition, capsules are able to actively absorb moisture, easily get wet and spoil. Therefore, the drug should be stored away from places with high humidity, such as a bathroom. After each use, the bottle with capsules should be tightly closed to prevent the drug from reacting with oxygen in the air.

All medications should be stored in a separate place, for example, on the top shelf of a cabinet, away from small children and elderly family members with poor vision.

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Shelf life

R-Butin, like any other medication, has a clearly limited period of use, which must be taken into account by each patient.

The shelf life of this medicine is 2 years, starting from the date of manufacture indicated on the package. It is important to remember that under no circumstances should you take expired medications, as they can have an unpredictable effect on the human body. Upon expiration of the shelf life, the medicine must be immediately disposed of.

It is not recommended to pour the capsules into another container, R-Butin should be stored in the original packaging and preferably with the instructions inside, so that if necessary, you can clarify the information about the drug. It is imperative to comply with all storage conditions for the drug, which are prescribed in the instructions. Particular attention should be paid to precautions, contraindications, side effects, as well as the interaction of the drug with other drugs.

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