R-CIN

R-CIN (International name - Rifampicin) is an antibacterial agent of a wide spectrum, which belongs to the group of ansamycins - antibiotics, in the formation of which the radiant fungus Streptomyces mediterranei participates.

[1], [2]

Indications R-CIN

R-CIN (Rifampicin) is used in modern medicine as a semisynthetic antituberculous antibiotic with a pronounced bactericidal effect. It suppresses the synthesis of bacterial RNA, inhibiting their DNA-dependent RNA polymerase.

Indications for use 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);
• lepra (dr: chronic granulomatous infection, Hansen's disease, obsolete leprosy);
• prevention of meningococcal meningitis (in particular, in persons who were in close contact with patients, as well as carriers of bacilli of Neisseria meningitidis);
• infectious diseases that are caused by sensitive microorganisms (Rifampicin is used as part of complex antimicrobial therapy).

R-CIN is an anti-tuberculosis drug I (main) series. 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 the use of this drug depending on the specific situation and taking into account the patient's condition.

Form of preparation:

• capsules of 150, 300, 450 and 600 mg, packed in an amount of 10 pcs .;
• lyophilizate Rifampicin, created to prepare a medicinal solution for injections and infusions;
• tablets in a special shell.

One capsule of R-CIN contains 150 mg of 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 hue. The capsule shell includes substances such as gelatin, water, methylparaben, E110 (yellow sunset), 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 choose the optimal drug, taking into account the features of the disease and the patient's condition. Conducting the sample will reduce the risk of possible allergic reaction to the antibiotic and protect the patient from complications of treatment.

[3], [4], [5]

Pharmacodynamics

R-CIN belongs to the group of semisynthetic 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 preparation depends on its concentration and mode of administration.

Pharmacodynamics R-CIN:

• is the antituberculous agent of the first (main) series;
• has an effective bactericidal action;
• has a depressing effect on the synthesis of RNA of pathogenic bacteria by inhibiting the DNA-dependent RNA polymerase of the pathogen;
• has a sterilizing effect on mycobacterium Mycobacterium tuberculosis at the intra- and extracellular level;
• shows a pronounced activity against Gram-negative bacteria and Gram-positive microorganisms, such as Staphylococcus spp., Clostridium spp., Bacillus anthracis, etc .;
• has a harmful effect on the pathogens: Mycobacterium leprae, Salmonella typhi, Brucella spp., as well as Chlamydia trachomatis, etc.

Resistance to the drug R-CIN develops quickly enough. However, in medicine, there was no cross-resistance to other anti-tuberculosis drugs, except for other rifampicins.

[6], [7], [8], [9], [10], [11], [12]

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 virtually all body fluids and tissues: liver, lungs, cerebrospinal fluid, and the like. However, it must be borne in mind that food to some extent delays the absorption of Rifampicin. The drug has the property of penetrating the placental barrier during pregnancy. It is characterized by a high level of binding with proteins, 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 for 24 hours. The elimination half-life is between 3 and 5 hours. Part of the oral dose of the drug (30%) is excreted by the kidneys.

Patients who take Rifampicin need to take into account that the antibiotic has the ability to stain biological fluids and mucous membranes (urine, saliva, sweat, eye mucosa) in orange. In the orange color, soft contact lenses can also be colored in people who use them. 

[13], [14], [15], [16], [17], [18], [19], [20]

Dosing and administration

R-CIN should be used strictly according to the doctor's prescription, in the dosage prescribed by him. Self-medication is unacceptable, since an uncontrolled or improperly selected regimen of Rifampicin may cause dangerous complications in the patient.

Dosage and administration: the drug is administered inside (in the form of capsules and tablets), and also administered intravenously (drip).

Tablets or capsules are taken on an empty stomach half an hour before meals or 2 hours after meals. In the treatment of tuberculosis patients, the daily dosage of Rifampicin ranges from 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. When detecting the carriage of meningococci, the dose for adults is a maximum of 600 mg per day (duration of admission is 4 days).

In the process of treatment of tuberculosis, R-CIN is usually combined with some anti-tuberculosis drug: in particular, Etambutol, Pyrazinamide Isoniazid, and others.

With pulmonary tuberculosis, the therapy period is usually 6 months; in the treatment of disseminated tuberculosis or tuberculosis meningitis, as well as the complication of tuberculosis with HIV infection, the duration of treatment with Rifampicin is 9 months. In each case, the doctor appoints the patient a separate treatment regimen. In case of exacerbation of the disease and ineffectiveness of therapeutic treatment, antituberculous drugs should be taken in a hospital strictly under the supervision of medical personnel.

When treating leprosy:

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

When treating R-CIN infectious diseases, 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 to adults; from 10 to 20 mg / kg - for children and newborns. The drug is taken twice a day.

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

In order to prevent the disease with meningococcal meningitis, R-CIN is prescribed twice a day every 12 hours: 600 mg to adults; 10 mg / kg for children; 5 mg / kg - to the newborn for 1 reception.

Intravenous (with the aid of a dropper) Rifampicin is prescribed in some cases: in the presence of destructive tuberculosis, the development of serious purulent-septic processes, and to create a high concentration of antibiotic in the blood in order to quickly suppress the focus of infection; if the medication is difficult or difficult to tolerate.

The duration of intravenous treatment with P-CIN depends on the total tolerability of the drug and is approximately one month or more with a further transition to the use of the drug in tablet form.

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

Patients taking R-CIN should consider the possibility of dyeing the skin, urine, tear fluid, sputum, and soft contact lenses in an orange-red hue under the influence of the drug.

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

Use R-CIN during pregnancy

R-CIN is not recommended during pregnancy, like most antibiotics, as well as other medications that can harm an unborn child. A pregnant woman is strictly forbidden to engage in self-medication. This can cause very dangerous consequences, including abortion and premature birth.

The use of P-CIN during pregnancy is permissible only in exceptional cases, when the estimated benefit for a pregnant woman exceeds the potential threat to the fetus. In any case, the question of the use of Rifampicin during pregnancy is decided only by the attending physician. In the first trimester, Rifampicin therapy is possible only for life indications.

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

Rifampicin is concentrated in tissues and body fluids, including breast milk. Therefore, during lactation, when there is a need to use R-CIN the mother is recommended to stop breastfeeding.

Contraindications

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

Contraindications to 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 violations of the liver and kidneys (in particular, chronic renal failure - chronic renal failure);
• cardiopulmonary insufficiency;
• pregnancy and lactation;
• thoracic age.

Rifampicin is given to newborns (including premature infants) and infants only if absolutely necessary. With great care, the drug is used for exhaustion, various liver diseases. Admission of the drug, if necessary, must 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 a general picture of blood is shown. In the course of treatment with Rifampicin non-tuberculosis infections, a rapid development of resistance of microorganisms can be observed. It can be prevented by combining the drug with other chemotherapeutic agents.

[21], [22], [23]

Side effects R-CIN

R-CIN, like any other drug, has a number of side effects that must be considered in the treatment of this drug. In case of any side effects, the patient should be told about it to his or her treating doctor. It may be necessary to reduce the dosage of the antibiotic, or to find alternative therapies.

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

• digestive system: worsening of appetite, nausea and vomiting, diarrhea, development of erosive gastritis, hyperbilirubinemia, hepatitis. It is also possible the occurrence of allergic reactions in the form of fever, hives, angioedema (Quincke's edema), bronchospasm, arthralgia;
• endocrine system: malfunctions in the menstrual cycle in women;
• nervous system: attacks of headache, disorientation, ataxia (coordination disorder), deterioration of visual acuity;
• urinary system: development of interstitial nephritis, nephronecrosis;
• other organs and systems: leukopenia, dysmenorrhea, myasthenia gravis, and exacerbation of gout.

Repeated reception of Rifampicin after a certain break may cause the patient to have a flu-like syndrome, expressed by chills, headache, fever, dizziness. Possible manifestations of anemia, skin reactions, renal failure.

[24], [25], [26]

Overdose

R-CIN should be taken with caution, strictly following the treatment regimen and not exceeding the dosage prescribed by the attending physician. When an antibiotic is overdosed, symptoms may manifest, which can develop as side effects: headache, nausea and vomiting, allergic reactions, abnormalities in liver function, etc.

Overdose Rifampicin may also cause the following symptoms in the patient:

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

When observing one of the above signs, the patient should take measures as soon as possible to hospitalize him. An overdose of a medication requires immediate intervention: you need to call an ambulance immediately, and before the doctor comes, the patient needs to rinse the stomach and provoke vomiting. To do this, you can use salted water or a solution of potassium permanganate.

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

[31], [32]

Interactions with other drugs

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

Interactions of R-CIN with other drugs:

• helps to reduce the effectiveness of estrogen in the composition of hormonal contraceptives, speeding up metabolism;
• reduces the activity of antiarrhythmic drugs (Dizopiramid, Mexiletin, Quinidine, Pyrmenol, etc.), Ketoconazole, Cyclosporine A, Heckobarbital, oral hypoglycemic agents, beta-blockers and many other drugs (details - in the instructions to R-CIN);
• alcohol, as well as drugs Acetaminophen and isoniazid increase the hepatotoxicity of rifampicin;
• with simultaneous administration of the drug with ketoconazole, antacids, opiates and anticholinergic drugs, there is a decrease in the bioavailability of Rifampicin;
• in the combination of the drug with Isoniazid or Pyrazinamide, there is an increase in the frequency and severity of liver function disorders.

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

[33], [34], [35]

Storage conditions

R-CIN should be stored, like other antibiotics, in a dry, well-protected from light and sun rays. At the same time, the room temperature should not exceed 30 ° C.

The storage conditions of P-CIN should be taken into account in order to prevent damage to the medicinal product. In the course of storage there is a gradual destruction of antibiotics, which leads to a decrease in the chemotherapeutic and stimulating activity of the drug, but its toxicity does not increase.

It should be remembered that antibiotics are potent drugs (group B), so they should be kept away from children to prevent adverse effects. It is advisable for this purpose to use the upper shelf lockable on the key cabinet, where you can put the entire medicine cabinet.

Do not use the medicine if its quality is doubtful. It happens that the shelf life of the drug has not expired, but the capsules or tablets have turned yellow or crumbled into powder, and a sediment has appeared in the injection solution. The instructions may indicate the deviation of the physical properties of medicinal products, which does not affect their therapeutic effect. But if there are no such instructions in the manual, it is better not to use medicine.

Shelf life

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

The expiration date of R-CIN should be taken into account without fail, since overdue antibiotics can be dangerous for the organism and cause its intoxication. In any case, if the medicinal product has not been used before the time specified in the instructions, it must be discarded.

It is necessary to take into account that the end date of use of almost any medicinal product implies its correct storage - in a place protected from moisture and light. This nuance in general determines the duration of the drug: if all storage conditions are accurately observed, the antibiotic will last longer and will not lose its properties.

[36], [37], [38]