McCox

Makoks is an antibiotic with anti-tuberculosis properties.

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Indications McCox

Indication for the use of the drug is the complex treatment of such diseases:

• tuberculosis of any site, atypical forms of mycobacteriosis, as well as tuberculosis meningitis;
• inflammations and infections that have a non-tubercular origin are provoked by drug-susceptible pathogens (among them severe forms of leprosy, legionella infection, as well as staphylococcal infection and Bang's disease);
• ongoing asymptomatic carriage of meningococcus - to eliminate it from the nasopharynx, and as a preventive against meningococcal meningitis.

Release form

Available in the form of capsules with a volume of 150 or 300 mg. One blister contains 10 capsules. One packet contains 10 blister plates.

Pharmacodynamics

Rifampicin is a semisynthetic antibiotic that is part of the rifamycin group. This is an anti-tuberculosis drug of the first series. Has bactericidal properties - it slows down the active activity of RNA polymerase, which depends on DNA. This is due to the creation of complexes with it - as a result, the process of synthesis of RNA microbes is reduced.

The medicine actively influences atypical fungi of different species (except M. Fortuitum), Gram-positive cocci (it is strepto- and also staphylococcus), clostridia, and besides it, anthrax wand, etc. Kokki from the gram-negative group (these are meningococci and gonococci (among them β-lactamase)) are exposed to the drug, but at the same time quickly acquire immunity to it.

Actively affects hemophilic rods (among them ampicillin with chloramphenicol), Ducrea sticks, Pertussis sticks, Anthrax bacilli, listeria monocytogenes, F. Tularensis, Legionella pneumophilus, Rickettsia Provachek, and Hansen bacillus. With respect to the rabies virus, rifampicin has a virucidal effect, and in addition it interferes with the development of rabies encephalitis.

Microorganisms from the genus Enterobacteriaceae, and besides this, gram-negative microorganisms of non-fermenting type (such as pseudomonas, acinetobactyr, and in addition Stenothrophomonas spp., Etc.) to the drug are not sensitive. It also has no effect on anaerobes.

Pharmacokinetics

Rifampicin is rapidly absorbed from the digestive tract, and its bioavailability is 95% (in case of fasting). This indicator decreases in case of consumption with food. Effective drug concentrations are formed in saliva, sputum, and in addition to this lung, eosinophils, peritoneal and pleural exudates of the liver with kidneys. In addition, the active substance passes well into the cells, as well as through the blood-brain barrier, breast milk and the placenta. During the treatment of tuberculous meningitis penetrates into the fluid of the spinal cord.

Binding to plasma proteins - 60-90%, dissolution occurs in lipids. The peak concentration in the blood reaches 2 hours after eating on an empty stomach, or 4 hours after eating. The therapeutic concentration of the substance in the body remains approximately 8-12 hours (if the microbes have a hypersensitivity to it - then 24 hours). The active component can concentrate in the tissues of the lungs and accumulate in caverns for a long time.

Metabolism occurs in the liver, as a result of this process, active decomposition products are formed. Half-life is about 3-5 hours. Excretion occurs mainly along with urine and bile. A small part is excreted along with the feces.

Dosing and administration

Rifampicin is taken orally for half an hour before meals or 2 hours after eating. It is necessary to wash down with water.

With tuberculosis: for adults, the daily dosage is 8-12 mg / kg. Patients weighing less than 50 kg - 450 mg; with a weight of 50+ kg, 600 mg each. For children 6-12 years of age, the dosage is 10-20 mg / kg, while the maximum allowable daily limit should not be above 600 mg.

Duration of treatment of tuberculosis is determined individually, depending on the effectiveness (may last 1+ years). In order that the resistance of pathogenic microbes to rifampicin does not develop, the drug should be drunk along with other anti-tuberculosis drugs of I or II series (in a standard dosage).

Pathologies of an infectious-inflammatory nature (non-tuberculosis origin), provoked by drug-sensitive microorganisms such as brucellosis or legionellosis, and in addition to staphylococcal infections in severe form (in combination with another antibiotic to prevent the development of resistant strains): a daily dosage of 900- 1200 mg for 2-3 doses (maximum per day - 1200 mg). Eliminating the signs of the disease, you should take the medicine for another 2-3 days.

When leprosy: oral intake (together with drugs that stimulate immunity) in a daily dosage of 600 mg for 1-2 doses for 3-6 months (you can repeat courses, making intervals of 1 month). In a different scheme (together with combined anti-leprosy treatment), the dosage per day is 450 mg in 3 doses over 2-3 weeks. The treatment course lasts 1-2 years with intervals of 2-3 months.

When meningococci: appointed for 4 days. For adults, the daily dosage is 600 mg, and for children 10-12 mg / kg.

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Use McCox during pregnancy

Use of the drug during pregnancy is permitted only if there are life indications, and when the potential benefit for a woman exceeds the development of possible negative consequences for the fetus.

With the use of rifampicin on the last stages of pregnancy, the risk of bleeding in the postpartum period - in mom and baby - increases.

Contraindications

Among the contraindications:

• intolerance to rifampicin and other components of the drug;
• disorders in the work of the kidneys or liver in severe form;
• jaundice (also mechanical);
• transferred less than 1 year ago, infectious hepatitis;
• pulmonary heart failure in severe form;
• combination with substances such as ritonavir or saquinavir.

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Side effects McCox

Among the side reactions:

• Gastrointestinal organs: vomiting with nausea, diarrhea, deterioration of appetite, abdominal pain, uncomfortable sensations, anorexia, erosive form of gastritis, and in addition pseudomembranous colitis;
• organs of the digestive system: the development of hepatitis or hyperbilirubinemia, and in addition to this discomforting sensations in the right upper quadrant and increased activity of liver transaminases;
• skin: rashes and itching, development of urticaria, exfoliative form of dermatitis, exanthema. In addition, also vasculitis, bladder reaction, malignant exudative, as well as erythema multiforme, and toxic epidermal necrolysis;
• immune reactions: hypersensitivity (including Quincke edema), anaphylaxis and bronchospasm;
• Other: fever, joint pain, severe lacrimation and herpes;
• hemopoietic system: leuko-, as well as neutropenia and thrombocytopenia (without purpura or with it, often develops as a result of intermittent treatment) hemolytic form of anemia and eosinophilia. In rare situations, the development of DIC syndrome or agranulocytosis is possible. In case of the first manifestations of purpura, it is necessary to immediately cancel the medicine. This is necessary, because there is evidence of cerebral hemorrhage and death resulting from the continuation of treatment or its resumption of the appearance of these symptoms;
• organs of the National Assembly: dizziness with headaches, impaired vision, disorientation, development of ataxia or psychosis;
• organs of the endocrine system: adrenal insufficiency (patients with functional impairment), as well as disorders of the menstrual cycle;
• organs of the urinary system: renal necrosis or interstitial nephritis, and in addition an acute degree of renal failure (in circulating form) and hyperuricemia;
• Other: urine / faeces / mucus / sweating / salivary / sputum stained in orange-red hue. In addition, muscle weakness, induction of porphyria, and also myopathy, exacerbated gout, dyspnoea with wheezing, lowering of blood pressure and cerebral hemorrhages.

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Overdose

Manifestations of an overdose: vomiting with nausea, diarrhea and abdominal pain. In addition, the development of jaundice, a feeling of drowsiness, increased fatigue. In addition, the blood plasma elevates the level of liver transaminases, as well as bilirubin. Skin (and along with this mucous in the mouth, saliva, sweat, urine, mucus, feces and sclera) becomes orange or brownish-red (in relation to the dose of medicine used). In addition, there is an allergy, fever, dyspnea, acute hemolytic anemia, thrombocytopenia and leukopenia, edema of the face, lungs and eyes, kidney failure, and convulsions, confusion and itchy skin.

As a treatment - you need to stop taking medication and eliminate the symptoms of an overdose. If the case is severe, a forced diuresis is required. Specific antidote for this medicine is absent.

Interactions with other drugs

When rifampicin is combined with drugs metabolized by the same enzyme system, the metabolic rate of these drugs may increase, and their activity may decrease. Therefore, it is necessary to maintain the correct drug concentration of these drugs in the blood - change their dose at the beginning of the use of rifampicin, and after stopping treatment with it.

Rifampicin increases the rate of metabolism of such drugs: antiarrhythmic drugs (eg, mexiletine, disopyramide, and in addition propafenone, quinidine and toxainide), beta-blockers (such as bisoprolol or propranolol), Ca2 + channel blockers (such as verapamil, diltiazem, nimodipine , and in addition nifedipine, nicardipine, isradipine and nisolpidin) and SG (digoxin and digitoxin). In addition, anticonvulsants (carbamazepine and phenytoin), psychotropic drugs (such as aripiprazole or haloperidol), tricyclics (nortriptyline and amitriptyline), hypnotics, anxiolytics (benzodiazepine, zolipidem, and diazepam and zopiclone) and barbiturates.

In addition, it also affects thrombolytics (antagonists of the vitamin K group) and anticoagulants of the indirect type. It is required to monitor prothrombin time every day or at a periodicity sufficient to determine the optimal dosage of anticoagulant.

A similar effect is on antimycotics (fluconazole, ketoconazole, and in addition terbinafine, voriconazole and itraconazole), antiviral (among them indinavir, amprenavir, saquinavir and nelfinavir, and in addition efavirenz, lopinavir, atazanavir and nevirapine) and antibacterial drugs (such as dapsone, telimycin, doxycycline, as well as chloramphenicol, fluoroquinolones and clarithromycin), as well as SCS (systemic use).

In this way, anti-estrogens (toremifene, tamoxifen and gestrinone), estrogens, hormonal contraceptives and gestagens are also affected. Women who use the OC are advised to use non-hormonal contraceptives in rifampicin treatment. In addition, also to thyroid hormones (such as levothyroxine), clofibrate, oral antidiabetics (for example, tolbutamide, chloropamide and thiazolinediones).

The effect is also on immunosuppressants (sirolimus and cyclosporine with tacrolimus), cytostatic drugs (erlotinib and imatinib with irinotecan), losartan, opioid analgesics, and in addition to methadone, quinine, praziquantel, riluzole.

The same activity is observed for selective antagonists of serotonin receptors (ondansetron), theophylline, diuretics (eplerenone), and besides statins, the metabolism of which occurs through CYP 3A4 (this may be simvastatin).

Due to the combination of atovaquone and rifampicin, the concentration in the blood serum of the first decreases, while the second one increases on the contrary. In the case of combination with ketoconazole, the concentration of both drugs decreases.

The combination with enalapril lowers the concentration of its active degradation product (enalaprilat) in the blood. Therefore, depending on the patient's condition, it may be necessary to adjust the dosage of the medication.

The connection with antacid drugs can cause a slowdown in the absorption of rifampicin, so it is recommended to take it at least 1 hour before using antacids.

In combination with Biseptolum and probenecid, the concentration of rifampicin in the blood rises.

Due to the combination with saquinavir or ritonavir, the risk of developing hepatotoxicity increases, so it is forbidden to combine them with rifampicin. In addition, hepatotoxicity can develop when combined with isoniazid and halothane. Combine rifampicin with the latter is not recommended, and when used concomitantly with isoniazid, liver function should be carefully monitored.

When combined with sulfasalazine, the concentration of sulfapyridine in the plasma decreases. This is usually due to the fact that the balance of the intestinal microflora is disturbed, where the conversion of sulfasalazine to sulfapyridine and mesalamine takes place.

Due to the combination with pyrazinamide (daily intake for 2 months) severe abnormalities in liver function can occur (there is evidence of a fatal outcome). Such a compound is allowed only if the condition is carefully monitored and if the possible use is higher than the risk of developing hepatotoxicity and death.

Simultaneous reception with clozapine or flecainide increases the toxic effect on the bone marrow.

When combined with LS paraaminosalicylic acid, which contains bentonite - to get the necessary concentration of drugs in the blood, you need to observe the gap between their use (at least 4 hours).

As a result of a compound with ciprofloxacin or clarithromycin, the concentration of rifampicin may increase.

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Storage conditions

Keep in a place that is closed from sunlight and moisture, and access to children. Temperature conditions - no more than 25 ° С.

Shelf life

Macox is allowed to be used for 3 years from the date of manufacture of the medicine.