R-CIN

R-CIN (International name – Rifampicin) is a broad-spectrum antibacterial drug that belongs to the group of ansamycins – antibiotics produced by the ray fungus Streptomyces mediterranei.

Indications R-CIN

R-CIN (Rifampicin) is used in modern medicine as a semi-synthetic anti-tuberculosis antibiotic with a pronounced bactericidal effect. It has a suppressive effect on the synthesis of bacterial RNA, inhibiting their DNA-dependent RNA polymerase.

Indications for use of R-CIN:

• various forms of tuberculosis (Rifampicin is part of complex therapy);
• brucellosis (other: zoonotic infection, undulating fever, Bang's disease) - the drug is used in combination with doxycycline (an antibacterial agent of the tetracycline group);
• leprosy (ancient: chronic granulomatous infection, Hansen's disease, obsolete "leprosy");
• prevention of meningococcal meningitis (in particular, in individuals who have been in close contact with patients, as well as carriers of Neisseria meningitidis bacilli);
• infectious diseases caused by sensitive microorganisms (Rifampicin is used as part of complex antimicrobial therapy).

R-CIN is an anti-tuberculosis drug of the first (main) line. The drug acts both intracellularly and extracellularly, causing rapid selection of bacteria resistant to Rifampicin. Low concentrations of the drug have a bactericidal effect on a number of bacteria: Mycobacterium tuberculosis, Brucella spp., Chlamydia trachomatis, Legionella pneumophila, Rickettsia typhi, Mycobacterium leprae, etc. In high doses, the drug actively affects certain gram-negative microorganisms and gram-positive bacteria: Bacillus anthracis, Staphylococcus spp., Clostridium spp., etc. R-CIN is also active against gonococci and meningococci.

Release form

R-CIN is available in various dosage forms, which allows this drug to be used depending on the specific situation and taking into account the patient’s condition.

Form of release of the drug:

• capsules of 150, 300, 450 and 600 mg, packed in 10 pieces;
• Rifampicin lyophilisate, created for the purpose of preparing a medicinal solution for injections and infusions;
• tablets in a special coating.

One capsule of R-CIN contains 150 mg of the active substance called Rifampicin, as well as auxiliary components: talc, lactose monohydrate, magnesium stearate, sodium lauryl sulfate, as well as corn starch, aerosil, liquid paraffin.

The contents of R-CIN capsules are a powder with a reddish-brown tint. The capsule shell contains substances such as gelatin, water, methylparaben, E110 (sunset yellow), E171 (titanium dioxide) and other ingredients.

It should be remembered that R-CIN, like any other antibiotic, should be prescribed exclusively by a specialist. Only an experienced doctor will be able to select the optimal drug, taking into account the characteristics of the disease and the patient's condition. Conducting a test will reduce the risk of a possible allergic reaction to the antibiotic and protect the patient from complications of treatment.

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Pharmacodynamics

R-CIN belongs to the group of semi-synthetic antibiotics of the Rifampicin group and is widely used in the treatment of various forms of tuberculosis, as well as infections caused by pathogenic bacteria and microorganisms. The activity of the drug depends on its concentration and the method of administration.

Pharmacodynamics of R-CIN:

• is a first-line (main) anti-tuberculosis drug;
• has an effective bactericidal effect;
• has an inhibitory effect on the RNA synthesis of pathogenic bacteria by inhibiting the DNA-dependent RNA polymerase of the pathogen;
• has a sterilizing effect on Mycobacterium tuberculosis at the intra- and extracellular level;
• exhibits pronounced activity against gram-negative bacteria and gram-positive microorganisms such as Staphylococcus spp., Clostridium spp., Bacillus anthracis, etc.;
• has a detrimental effect on pathogens: Mycobacterium leprae, Salmonella typhi, Brucella spp., as well as Chlamydia trachomatis, etc.

Resistance to the drug R-CIN develops quite quickly. At the same time, cross-resistance to other anti-tuberculosis drugs, except for other rifampicins, has not been noted in medicine.

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Pharmacokinetics

R-CIN is a modern broad-spectrum antibiotic that has a pronounced bactericidal effect and has an active effect on a number of pathogenic bacteria and microorganisms.

Pharmacokinetics of R-CIN: immediately after administration, the antibiotic is absorbed into the blood from the gastrointestinal tract and distributed in almost all fluids and tissues of the body: liver, lungs, cerebrospinal fluid, etc. However, it should be taken into account that food to some extent delays the absorption of Rifampicin. The drug has the ability to penetrate the placental barrier during pregnancy. It is characterized by a high level of protein binding, the indicator of which is 89%. The process of R-CIN metabolism occurs in the liver, where microsomal enzymes are stimulated. R-CIN is excreted in urine, bile and feces within 24 hours. The half-life is from 3 to 5 hours. Part of the oral dose of the drug (30%) is excreted by the kidneys.

Patients taking Rifampicin should take into account that the antibiotic has the property of coloring biological fluids and mucous membranes of the body (urine, saliva, sweat, eye mucous membrane) in orange. Soft contact lenses of people who use them may also be colored orange.

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Dosing and administration

R-CIN must be used strictly as prescribed by the doctor, in the dosage prescribed by him. Self-medication is unacceptable, since uncontrolled or incorrectly selected regimen of taking Rifampicin can cause dangerous complications in the patient.

Method of administration and dosage: the drug is administered orally (in the form of capsules and tablets) and also administered intravenously (drip).

Tablets or capsules are taken on an empty stomach half an hour to an hour before meals or 2 hours after meals. When treating tuberculosis patients, the daily dosage of Rifampicin is 450 to 600 mg for adults (taking into account the patient's body weight), for newborns and small children - from 10 to 20 mg / kg. If meningococcal carriage is detected, the dose for adults is a maximum of 600 mg of the drug per day (duration of administration is 4 days).

In the process of treating tuberculosis, R-CIN is usually combined with some anti-tuberculosis drug: in particular, Ethambutol, Pyrazinamide, Isoniazid, etc.

In case of pulmonary tuberculosis, the treatment period is usually 6 months; in case of disseminated tuberculosis or tuberculous meningitis, as well as in case of tuberculosis complications with HIV infection, the treatment period with Rifampicin is 9 months. In each specific case, the doctor prescribes a separate treatment regimen for the patient. In case of exacerbations of the disease and ineffectiveness of therapeutic treatment, anti-tuberculosis drugs should be taken in a hospital strictly under the supervision of medical personnel.

In the treatment of leprosy:

• multibacillary types: for adults - 600 mg of the drug once a month (together with Dapsone and Clofazimine); for children - 10 mg/kg (plus Dapsone); therapy period - 2 years;
• pausibacillary types: for adults - 600 mg of the drug once a day (together with Dapsone); for children - 10 mg/kg once a month (together with Dapsone); treatment period - 6 months.

When treating infectious diseases with R-CIN, the development of which is provoked by sensitive microorganisms, the antibiotic is administered together with other antimicrobial drugs. In this case, the daily dose of Rifampicin is: from 0.6 to 1.2 g - for adults; from 10 to 20 mg/kg - for children and newborns. The drug is taken twice a day.

For the treatment of brucellosis in adults, 900 mg/day of R-CIN is prescribed once, preferably in the morning on an empty stomach; the drug is combined with Doxycycline. The duration of the therapy period is 45 days.

For the prevention of meningococcal meningitis, R-CIN is prescribed twice a day every 12 hours: 600 mg for adults; 10 mg/kg for children; 5 mg/kg for newborns per dose.

Intravenously (via a drip), Rifampicin is prescribed in certain cases: in the presence of destructive tuberculosis, the development of serious purulent-septic processes, as well as to create a high concentration of antibiotic in the blood in order to quickly suppress the source of infection; if taking the drug is difficult or poorly tolerated by the patient.

The duration of intravenous treatment with R-CIN depends on the overall tolerability of the drug and is approximately a month or more, with a subsequent transition to the use of the drug in tablet form.

When treating various non-tuberculous infections, the antibiotic dose is 0.3-0.9 g, maximum – 1.2 g per day. The duration of therapy is determined by the doctor on an individual basis, taking into account the effectiveness of the drug, and is approximately 7 to 10 days.

Patients taking R-CIN should take into account the possibility of the skin, urine, tears, sputum, and soft contact lenses becoming orange-red in color under the influence of the drug.

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Use R-CIN during pregnancy

R-CIN is not recommended for use during pregnancy, as are most antibiotics and other medications that may harm the unborn child. A pregnant woman is strictly prohibited from self-medicating. This can cause very dangerous consequences, including termination of pregnancy and premature birth.

The use of R-CIN during pregnancy is permissible only in exceptional cases, when the expected benefit to the pregnant woman outweighs the potential threat to the fetus. In any case, the question of using Rifampicin during pregnancy is decided only by the attending physician. In the first trimester, Rifampicin therapy is possible only for vital indications.

It should be taken into account that taking R-CIN in the last weeks before delivery increases the risk of bleeding in the postpartum period, both in the mother and the newborn. In such cases, vitamin K is prescribed.

Rifampicin is concentrated in tissues and body fluids, including breast milk. Therefore, during lactation, if it is necessary to use R-CIN, the mother is advised to stop breastfeeding.

Contraindications

R-CIN, like any other antibiotic, has its own contraindications, which must be taken into account during treatment to avoid adverse effects.

Contraindications for the use of R-CIN:

• hypersensitivity to the active substance of the drug - Rifampicin, as well as its components;
• hepatitis in remission (less than 1 year);
• jaundice;
• serious liver and kidney dysfunction (in particular, CRF – chronic renal failure);
• cardiopulmonary failure;
• pregnancy and lactation period;
• infancy.

Rifampicin is prescribed to newborns (including premature babies) and infants only in cases of extreme necessity. The drug is used with great caution in cases of exhaustion and various liver diseases. If necessary, taking the drug should be combined with constant monitoring of kidney function, especially after a break in taking the drug.

With prolonged use of R-CIN, regular monitoring of liver function and the overall blood picture is indicated. During treatment of non-tuberculous infections with Rifampicin, rapid development of microorganism resistance may be observed. It can be prevented by combining the drug with other chemotherapeutic agents.

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Side effects R-CIN

R-CIN, like any other medicine, has a number of side effects that must be taken into account during treatment with this drug. If any side effects occur, the patient should tell their doctor about it. Perhaps the dosage of the antibiotic should be reduced or alternative treatment methods should be found.

Side effects of R-CIN can be observed in the form of various disorders and malfunctions:

• digestive system: loss of appetite, nausea and vomiting, diarrhea, development of erosive gastritis, hyperbilirubinemia, hepatitis. Allergic reactions in the form of fever, urticaria, angioedema (Quincke's edema), bronchospasm, arthralgia may also occur;
• endocrine system: menstrual cycle disorders in women;
• nervous system: headache attacks, disorientation, ataxia (coordination disorder), deterioration of visual acuity;
• urinary system: development of interstitial nephritis, nephronecrosis;
• other organs and systems: leukopenia, dysmenorrhea, myasthenia, as well as exacerbation of gout.

Repeated administration of Rifampicin after a certain break may cause a flu-like syndrome in the patient, expressed by chills, headache, fever, dizziness. Manifestations of anemia, skin reactions, renal failure are also possible.

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Overdose

R-CIN should be taken with caution, strictly following the treatment regimen and not exceeding the dosage prescribed by the attending physician. In case of an antibiotic overdose, symptoms may appear that may develop in the form of side effects: headache, nausea and vomiting, allergic reactions, liver dysfunction, etc.

An overdose of Rifampicin may also cause the following symptoms in the patient:

• pulmonary edema,
• increase in temperature,
• dyspnea,
• hemolytic anemia,
• convulsions,
• lethargy,
• confusion.

If you observe one of the above symptoms in a patient, you should take measures to hospitalize him/her as soon as possible. An overdose of a drug requires immediate intervention: you need to immediately call an ambulance, and before the doctor arrives, the patient needs to have his/her stomach washed and vomit induced. For this, you can use salted water or a solution of potassium permanganate.

Treatment of overdose symptoms involves the use of symptomatic and efferent therapy methods: administration of sorbents (in particular, activated carbon), forced diuresis. Often, the doctor prescribes drugs that stabilize liver function.

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Interactions with other drugs

R-CIN has a certain effect on various groups of drugs, and is also susceptible to the effect of other drugs that disrupt its therapeutic effect. This nuance must be taken into account during the treatment process.

Interactions of R-CIN with other drugs:

• helps reduce the effectiveness of estrogen in hormonal contraceptives by accelerating metabolism;
• reduces the activity of antiarrhythmic drugs (Disopyramide, Mexiletine, Quinidine, Pirmenol, etc.), Ketoconazole, Cyclosporine A, Hexobarbital, oral hypoglycemic agents, beta-blockers and many other drugs (details in the instructions for R-CIN);
• Alcohol, as well as the drugs Acetaminophen and Isoniazid, increase the hepatotoxicity of Rifampicin;
• when taken simultaneously with Ketoconazole, antacids, opiates and anticholinergic drugs, a decrease in the bioavailability of Rifampicin is observed;
• in combination with Isoniazid or Pyrazinamide, an increase in the frequency and severity of liver dysfunction is noted.

Before using R-CIN, the patient must consult a doctor to prevent the possibility of adverse symptoms, including those caused by interactions with other drugs.

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Storage conditions

R-CIN should be stored, like other antibiotics, in a dry place, securely protected from light and sunlight. The air temperature in the room should not exceed 30 °C.

The storage conditions of R-CIN must be taken into account to prevent the drug from deteriorating. During storage, antibiotics gradually deteriorate, which leads to a decrease in the chemotherapeutic and stimulating activity of the drug, but its toxicity does not increase.

It is important to remember that antibiotics are potent drugs (group B), so they should be kept out of reach of children to prevent adverse effects. It is advisable to use the top shelf of a lockable cabinet for this purpose, where you can place the entire first aid kit.

You cannot use a medicine if its quality is questionable. It happens that the expiration date of the drug has not yet expired, but the capsules or tablets have turned yellow or crumbled into dust, and sediment has appeared in the injection solution. The instructions may indicate deviations in the physical properties of drugs, which does not affect their therapeutic effect. But if there are no such instructions in the instructions, it is better not to use the medicine.

Shelf life

R-CIN has its own validity period, indicated in the instructions for the drug - 3 years. With the expiration of this period, the activity of the antibiotic gradually decreases.

The expiration date of R-CIN must be taken into account without fail, since expired antibiotics can be dangerous for the body and cause intoxication. In any case, if the drug has not been used before the expiration date specified in the instructions, it must be thrown away.

It is necessary to take into account that the expiration date of almost any drug implies its proper storage - in a place protected from moisture and light. This nuance generally determines the validity period of the drug: if all storage conditions are strictly observed, the antibiotic will last longer and will not lose its properties.

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