Benemycin

Benemicin is an antibiotic with a wide range of medicinal effects. It is used as an anti-tuberculosis, antibacterial, and anti-leprosy drug.

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Indications Benemycin

The medicine is indicated for the elimination of the following pathologies:

• tuberculosis of any form;
• leprosy (in combination with dapsone);
• infectious processes caused by the action of bacteria sensitive to drugs;
• brucellosis (in combination with tetracyclines).

It is also used to prevent the development of meningococcal meningitis in the carriers themselves, as well as in people who come into contact with them.

Release form

It is produced in the form of capsules. One case contains 100 capsules, one package contains 1 such case.

Pharmacodynamics

The active component of the drug is rifampicin. Benemicin is used to eliminate diseases caused by the following bacteria: Koch's bacillus, Legionella pneumophila, Chlamydia trachomatis, Hansen's bacillus, Brucella spp., and Rickettsia typhi. High concentrations of the drug allow it to act on individual gram-negative microorganisms. The drug is especially active against anthrax bacilli, streptococci and staphylococci, as well as clostridia. Benemicin is also active against gram-negative cocci (such as gonococci and meningococci).

The active component inhibits bacterial DNA-dependent RNA polyerase.

Rifampicin is prohibited to be used in monotherapy, since in this case bacteria resistant to this component quickly develop.

Pharmacokinetics

After oral administration, rifampicin is rapidly absorbed from the gastrointestinal tract (almost 100%). It should be taken into account that if there is food in the stomach, the absorption of the drug slows down significantly.

The peak concentration in the blood serum (after oral administration of the average daily medicinal dose (600 mg)) of the substance is reached after 1.5-2 hours and is equal to 6-7 mcg/ml. Suppression of growth and reproduction of most strains of Koch's bacillus begins already in the case of reaching a concentration of 0.5 mcg/ml. The medicinal concentration in the blood lasts for about 8-12 hours.

With protein inside the plasma is synthesized by about 75%, and the half-life is 2-5 hours. The active substance passes well into bone tissue, lymph nodes, caverns, tuberculosis foci, and biological fluids. It can also penetrate the placenta and into breast milk. The drug concentration in the cerebrospinal fluid occurs in case of inflammation of the meninges.

After rifampicin is absorbed into the blood, the substance enters the liver through the portal vein, after which it is again excreted into the digestive tract along with bile, and then reabsorbed into the blood.

Part of the active substance undergoes metabolism in the liver, during which diacetylrifampicin is formed, which retains anti-tuberculosis properties, but is less well absorbed in the intestine. Excretion occurs through the digestive tract, with bile, unchanged. This is why during the first 3 weeks of therapy (while the body adapts to such a metabolic cycle), an increase in transaminases is detected in the blood plasma, which disappears over time.

About 60% of the substance taken orally is excreted with feces, and another 30% with urine (unchanged and as decay products). A small amount of the drug is excreted with tears and then other biological fluids, giving them an orange color.

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Dosing and administration

The medicine should be taken orally half an hour before meals.

In the treatment of tuberculosis, the drug is used in combination with other anti-tuberculosis drugs (for example, pyrazinamil, ethambutol, streptomycin, and isoniazid). For adults weighing up to 50 kg, the daily dose is 450 mg. If the patient's weight is over 50 kg, 600 mg is prescribed per day. Infants and children are allowed to be given 10 mg/kg per day. No more than 600 mg of the drug can be taken per day.

The treatment course for tuberculous meningitis, disseminated tuberculosis, tuberculosis against the background of HIV, as well as for spinal lesions of a neurological nature lasts at least 9 months with daily use of the drug. At the same time, at the initial stage (during the first 2 months), the drug should be taken in combination with isoniazid and pyrazinamide, and with them etabuthol or streptomycin, and the remaining 7 months - in combination with isoniazid.

The treatment course for pulmonary tuberculosis lasts six months and is carried out according to one of the schemes described below:

• During the first 2 months, standard treatment is administered - a combination of Benemycin with the four anti-tuberculosis drugs listed above. The next 4 months, the drug is taken together with isoniazid;
• according to the above scheme, take during the first 2 months, and then 2-3 times a week in combination with isoniazid;
• taking the drug 3 times a week for 6 months (together with pyrazinamide, as well as isoniazid and streptomycin (or etabuthol instead)).

When taking anti-tuberculosis drugs 2-3 times a week, the treatment process should be carefully monitored by a doctor.

For the treatment of multibacillary leprosy, the adult dosage is 600 mg once a month (a combined dose with clofazimine (50 mg daily + 300 mg monthly), as well as dapsone (100 mg daily)). The pediatric dosage is 10 mg per month in combination with clofazimine (50 mg every other day + 200 mg once a month), and in addition to it with dapsone (1-2 mg/kg daily). The course duration is 2 years.

For the treatment of pausibacillary leprosy, the adult dosage is 600 mg once a month (in combination with dapsone at 1-2 mg/kg (dose 100 mg) once a day). Children are given the drug at a dosage of 10 mg/kg once a month (in combination with dapsone, 1-2 mg/kg per day). The treatment course lasts six months.

Other antibacterial agents are also used to eliminate infectious pathologies caused by microbes sensitive to the drug. The adult dosage per day is 0.6-1.2 g, and for infants and children - 10-20 mg / kg per day. The drug should be taken twice a day.

When treating brucellosis, the medicine is taken once a day (in the morning), in the amount of 900 mg. Additionally, it is also necessary to drink doxycycline. The duration of the course is selected individually, on average - at least 45 days.

For the prevention of meningococcal meningitis, it is necessary to take the medicine in the amount of 600 mg twice a day with an interval of 12 hours. The course lasts 2 days.

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Use Benemycin during pregnancy

It is contraindicated to take this medicine during pregnancy.

Contraindications

Among the contraindications of the drug:

• diagnosed renal dysfunction;
• jaundice;
• infectious form of hepatitis suffered less than 1 year ago;
• hypersensitivity to rifampicin and other components of the drug;
• lactation period.

The drug should also be prescribed to children with caution.

Side effects Benemycin

Taking the drug can cause the following side effects:

• Gastrointestinal organs: nausea with vomiting, diarrhea, loss of appetite, development of hepatitis, pseudomembranous colitis, erosive gastritis, and hyperbilirubinemia. In addition, the level of liver transaminases may increase;
• CNS organs: the appearance of headaches, a feeling of disorientation, loss of vision, and the development of ataxia;
• urinary system organs: nephronecrosis or tubulointerstitial nephritis is observed;
• allergies: fever, bronchospasm, urticaria, Quincke's edema or eosinophilia, as well as arthralgia;
• Others: muscle weakness, development of leukopenia or dysmenorrhea, also induction of porphyria, and in addition hyperuricemia and gout in the acute stage.

Due to irregular intake of the drug or at an early stage of a repeated course of treatment, it is possible to develop an allergy on the skin, as well as a flu-like syndrome (fever, severe dizziness with headaches, muscle pain and chills), hemolytic anemia, Werlhof's disease and acute renal failure.

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Overdose

In case of drug poisoning due to overdose, the following symptoms may occur:

• the appearance of convulsions;
• falling into lethargy;
• feeling of confusion.

These disorders require symptomatic therapy, gastric lavage, and activated charcoal to treat them. Forced diuresis may also be used.

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Interactions with other drugs

Benemicin is able to weaken the effect of sex hormones, hormonal contraception, oral anticoagulants, antiarrhythmic drugs (such as mexiletine, disopyramide, as well as tocainide, quinidine and pirmenone), antidiabetic drugs, and also dapsone, ketoconazole, phenytoin, hexobarbital and nortriptyline. Along with this, also theophylline, benzodiazepines, GCS, cyclosporine type A, traconazole and β-blockers, as well as chloramphenicol enalapril, cimetidine (acceleration of the metabolism process) and calcium channel blockers.

As a result of combined administration with ketoconazole, antacid and anticholinergic drugs, as well as opiates, the bioavailability of the drug decreases.

In people with liver problems, the combination with pyrazinamide and isonaside may provoke disease progression.

PAS medicines containing the substance bentonite are allowed to be taken at an interval of 4 hours after taking Benemycin, since there is a possibility of disruption of the absorption processes of the active components.

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Storage conditions

Benemicin should be kept in a place protected from moisture and sunlight, inaccessible to small children. Temperature – no more than 25 ^o C.

Shelf life

Benemicin is permitted to be used for 3 years from the date of release of the drug.

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