R-Butyn

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

[1], [2]

Indications R-Butyn

R-Butin is used as part of complex therapy as an effective antituberculous agent. The international nonproprietary name of the drug is the name "Rifabutin".

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

The goal of treatment with the drug R-Butin is to prevent the likelihood of developing a relapse of tuberculosis and reduce the likelihood of infection of 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 discontinuation of M. Tuberculosis.

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

[3], [4], [5], [6], [7]

Release form

R-Butin is a semisynthetic antibiotic that exerts an effective effect on various types of microbacteria, including mycobacterium tuberculosis.

The form of the preparation - capsules of 150 mg, filled with a red-violet powder that does not dissolve in water, dissolves poorly in ethanol and dissolves in methanol and chloroform.

Many drugs today are available in capsules, like R-Butin. The capsule dosage form has a number of advantages: it ensures a high accuracy of dosing of medicinal substances, the content of the capsules is easier and faster absorbed in the stomach. The capsule shell protects the gastric mucosa and helps prevent the inactivation of the antibiotic by gastric juice enzymes. In addition, the medicine in capsules is protected from adverse factors (light, moisture, air, mechanical influences). In the manufacture of capsules, less auxiliary substances are used than in the manufacture of tableted forms of medicinal substances. The corrective ability of capsules is to eliminate the unpleasant taste and smell of antibiotics. A high aesthetics is achieved by the use of various dyes to obtain shells of capsules.

[8], [9], [10]

Pharmacodynamics

R-Butin (Rifabutin) is a semisynthetic broad-spectrum antibiotic and is used in conjunction with other drugs that have an active effect on a number of infections, including in 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 action and selectively suppresses DNA-dependent RNA polymerase of microscopic bacteria Mycobacterium spp., As well as atypical mycobacteria (Mycobacterium tuberculosis, Mycobacterium avium). In addition, P-Butin is active against Gram-positive microorganisms. Monotherapy with this drug leads to rapid development of resistance.

Clear clinical criteria for evaluating the effectiveness of the drug are absent. However, it has been clinically proven that an antibacterial agent reduces symptom severity, increases the patient's body weight, and also reduces the incidence of relapse. The main purpose of taking an antibiotic is to stop the release of M. Tuberculosis, to prevent possible relapses, to contaminate the surrounding and fatal outcomes in the treatment of patients.

[11], [12], [13],

Pharmacokinetics

R-Butin is rapidly absorbed from the digestive tract into the blood immediately after ingestion. The maximum level of the active substance of the drug is reached approximately 2-4 hours after the use of 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 relative to such intracellular pathogenic microorganisms that are mycobacteria.

Pharmacokinetics R-Butin has a linear character. Rifabutin has the property of rapidly penetrating into cells and being distributed in the tissues of many internal organs, with the exception of the brain. Its greatest concentration is created in the lung tissue. It has been clinically proven that the concentration in the lungs in a day after taking the antibiotic is 5-10 times higher than its concentration in the blood plasma. At the same time there is a poor penetration of the drug through the BBB - blood-brain barrier. The bioavailability index of Rifabutin is 20%, and the binding rate with plasma proteins is 85%. The drug is completely biotransformed in the liver tissues, thus forming inactive metabolites. 53% of P-Butin in the form of metabolites is excreted through the kidneys, 30% - along with bile, 5% - with bile in its original form, and the same - with urine. The elimination half-life of the antibiotic from the body is approximately 35-40 hours.

[14], [15], [16], [17]

Dosing and administration

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

Dosing and Administration: adults are usually prescribed from 150 to 600 mg of P-Butin per day. However, in general, the use of Rifabutin depends on the specific situation:

• In the case of treatment of recurrently diagnosed pulmonary tuberculosis, 150-300 mg of Rifabutin should be taken per day (duration of treatment - 6 months).
• For treatment of patients with chronic multidrug-resistant pulmonary tuberculosis, 300-450 mg of medication per day are prescribed (treatment is 6-9 months).
• When a secondary mycobacterial infection of a non-tuberculous nature occurs, from 450 to 600 mg of the drug per day (the duration of the course of treatment is up to 6 months).
• For the prevention of MAC infections in patients with severe immunodeficiency and AIDS - 300 mg of the drug P-Butin per day.
• In case of serious violations and failures in the work of the kidneys (KK (creatine kinase) - below 30 ml / min), it is necessary to reduce the dosage of P-Butin by 50%.
• In combination with other anti-tuberculosis drugs (Etambutol or Isoniazid, etc.) - 450-600 mg of drug per day.

Elderly patients are given the usual dosing regimen of P-Butin: orally - once a day, regardless of food.

Throughout the period of treatment with P-Butin, it is recommended to periodically check the platelet and leukocyte counts in peripheral blood, as well as the activity of liver enzymes. When taking P-Butin in high doses or in combination with Clarithromycin, the patient has a risk of developing uveitis (an inflammatory process in the choroid of the eye). In this case, the patient needs consultation of an ophthalmologist, and also temporarily stop taking the drug.

[27], [28], [29], [30], [31]

Use R-Butyn during pregnancy

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

The use of P-Butin during pregnancy is fraught with negative consequences for the health of the future mother and her child. If it is necessary to use Rifabutin during breastfeeding, it is necessary to solve the problem of the urgent cessation of lactation. As for the clinical results, strictly controlled studies that related to the use of R-Butin during pregnancy were not conducted.

In practical medicine, only those antibiotics that do not negatively influence the development of the fetus are used. Usually, treatment with antibiotics during pregnancy makes sense only if the therapeutic effect on infectious pathology in a future mother is higher than the harm (likely or potential) for the fetus. Pregnant women need to consider that almost all antibiotics are prescribed by prescription, so a visit to a doctor in case of illness is mandatory. The medical control of therapy allows to avoid negative consequences that can be caused by improper treatment, in particular, an independent uncontrolled intake of antibacterial agents.

Contraindications

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

Contraindications for use R-Butin:

• pregnancy,
• lactation period (breastfeeding),
• hypersensitivity to the drug,
• age to 18 years,
• individual intolerance to rifabutin and other ansamycins,
• severe violations in the work of the liver and kidneys.

When taking P-Butin, it is necessary to strictly adhere to the treatment regimen established by the attending physician. It should be noted that during the treatment can be observed the dyeing of the skin, urine, saliva in a reddish-orange hue.

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

[18], [19], [20], [21], [22], [23], [24]

Side effects R-Butyn

R-Butin must be taken in strict accordance with the prescriptions of the doctor. In case of deterioration or observation of any adverse symptoms, the patient should consult with the attending physician regarding the further administration of the drug. It may be necessary to reduce the dose of the drug, or to find alternative ways of treating the infection.

Side-effects of P-Butin can be manifested as:

• nausea and vomiting,
• changes in taste (dysgeusia),
• diarrhea and abdominal pain,
• jaundice,
• increased activity of liver transaminases,
• anemia (reduction of hemoglobin in erythrocytes),
• thrombocytopenia (decrease in the number of platelets),
• leukopenia (a decrease in the content of leukocytes in the blood),
• arthralgia (soreness of the joints),
• Myalgia (pain in the muscles).

In addition, adverse reactions of the body to the preparation of R-Butin may be allergy (rash, fever), rarely - uveitis (inflammation of the choroid), bronchospasm (sudden contraction of the walls of the bronchi), anaphylactic shock.

In case of an overdose of antibiotic, there may be an increase in side effects. In this case, the patient needs to rinse the stomach. Symptomatic therapy and diuretics are also prescribed.

[25], [26]

Overdose

R-Butin should be used according to the treatment scheme developed by the 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.), and unconsciousness. It is strictly forbidden to carry out treatment with R-Butin.

An overdose of a medicine 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, it is necessary to urgently call an ambulance. Before the doctor comes to the patient, it is necessary to rinse the stomach, causing vomiting. To this end, you can drink 3 cups of salted water (2 teaspoons of salt for 200 mg). After washing the stomach should take a few crushed tablets of activated charcoal.

In serious cases of an overdose of P-Butin, the patient needs medical assistance in a stationary mode. Treatment is carried out taking into account the symptoms. In this case, drugs of the reverse action are usually prescribed, or directed to maintain the liver.

It is very important to determine which preparation the person has poisoned. This will help to develop the right treatment tactics and make a forecast of possible side effects.

Usually Appointed as well as drugs aimed at, for example, with an overdose of a pressure-lowering medicine prescribe a means that stimulate the work of the heart.

Interactions with other drugs

R-Butin has a different effect on certain drugs and can cause organic changes in the body. In particular, it helps to accelerate the metabolism of drugs in the liver.

Interactions of P-Butin with other drugs:

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

The development of clinically significant interactions of the preparation of P-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 should strictly observe the prescribed treatment regimen and take P-Butin in a strictly specified dosage. The drug can be drunk as an empty stomach, either during or after a meal. Rifabutin activity manifests itself in staining urine, tears, skin, saliva and even contact lenses in a reddish-orange color.

If you are taking any medications, before starting treatment with Rifabutin, you need to tell your doctor about it to prevent possible negative consequences.

[32], [33], [34],

Storage conditions

R-Butin must be stored in accordance with the rules prescribed by the Ministry of Health for Schedule B medicines, which contain potent medicines, which must be stored with special precautions and necessarily separately from other medications.

Storage conditions P-Butin:

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

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

In addition, the 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 intake, the capsule vial should be closed tightly to prevent the drug from reacting with oxygen in the air.

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

[35], [36], [37], [38], [39]

Shelf life

R-Butin, like any other medicinal product, has a clearly limited period of application, which must be taken into account for each patient.

Shelf life of this medicine is 2 years, starting from the date of manufacture, indicated on the package. It must be remembered that in no case can you take overdue medications, as they can have unpredictable effects on the human body. After the expiry of the storage period, the medicine should be disposed of immediately.

It is not recommended to pour the capsules in another container, store the R-Butin in the original packaging and preferably with the instructions inside to, if necessary, clarify the information on the drug. It is necessary to comply with all the storage conditions of the medicinal product, which are prescribed in the instructions. Particular attention should be paid to precautions, contraindications, side effects, as well as drug interaction with other medicines.

[40], [41], [42]