Alpha Normix Coated Tablets 200mg N36
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Active ingredients
Rifaximin
Release form
Pills
Composition
1 tablet contains: Active ingredient: rifaximin (with alpha polymorphic structure) - 200 mg. Excipients: sodium carboxymethyl starch - 15 mg, glyceryl palmitostearate - 18 mg, colloidal silicon dioxide - 1 mg, talc - 1 mg, microcrystalline cellulose - 115 mg. The composition of the film shell: hypromellose - 5.15 mg, titanium dioxide (E171) - 1.5 mg, disodium edetate - 0.02 mg, propylene glycol - 0.5 mg, iron red oxide (E172) - 0.15 mg.
Pharmacological effect
Rifaximin is a broad-spectrum antibiotic from the rifamycin group. Like other members of this group, it irreversibly binds the beta subunits of the bacterial enzyme DNA-dependent RNA polymerase and, therefore, inhibits the synthesis of RNA and bacterial proteins. As a result of irreversible binding to the enzyme, rifaximin exhibits bactericidal properties against sensitive bacteria. The drug has a broad spectrum of antimicrobial activity, including the majority of gram-negative and gram-positive, aerobic and anaerobic bacteria. The wide antibacterial spectrum of rifaximin contributes to the reduction of pathogenic intestinal bacterial load, which causes some pathological conditions. The drug reduces: - the formation of ammonia by bacteria and other toxic compounds, which in the case of severe liver disease, accompanied by a violation of the detoxification process, play a role in the pathogenesis and clinical manifestations of hepatic encephalopathy; - increased proliferation of bacteria in the syndrome of excessive growth of microorganisms in the intestine; - the presence of bacteria in the colon diverticulum, which may be involved in inflammation in and around the diverticular sac and possibly play a key role in the development of symptoms and complications of diverticular disease; - the intensity of the antigenic stimulus, which, in the presence of genetically determined defects in the immunoregulation of the mucous membrane and / or in the protective function, can initiate or constantly maintain chronic inflammation of the intestine; - the risk of infectious complications in colorectal surgery. Mechanism of resistance: The development of rifaximin resistance is due to reversible damage to the GroB gene, which encodes a bacterial RNA polymerase.The incidence of resistant subpopulations among bacteria isolated from patients with traveler's diarrhea was low. According to clinical studies, a three-day course of rifaximin therapy in patients with traveler's diarrhea was not accompanied by the emergence of resistant gram-positive (enterococci) and gram-negative (E. coli) bacteria. When high doses of rifaximin were used repeatedly in healthy volunteers and in patients with inflammatory bowel disease, rifaximin-resistant strains appeared, however, they did not colonize the gastrointestinal tract and did not displace rifaximin-sensitive strains. When discontinuing therapy, resistant strains quickly disappeared. Experimental and clinical data suggest that the use of rifaximin in patients with traveler's diarrhea and latent infection of Mycobacterium tuberculosis and Neisseria meningitidis will not be accompanied by the selection of rifampicin-resistant strains. Sensitivity: In vitro sensitivity testing cannot be used to determine the sensitivity or resistance of bacteria to rifaximin. Currently, clinical data are insufficient to establish limit values for evaluating sensitivity tests. Rifaximin was assessed in vitro against traveler diarrhea pathogens from four regions of the world: enterotoxigenic and enteroaggregative strains of Escherichia coli, Salmonella spp., Shigella spp., Non-cholera vibrioes, Plesiomonas spp., Aeromonas spp., And Campylo-sympo. MPK90 for the isolated strains was 32 μg / ml, and this level is easily achievable in the intestinal lumen as a result of a high concentration of rifaximin in the feces. Since rifaximin in the polymorphic form of alpha has a low absorbability from the gastrointestinal tract and acts locally in the intestinal lumen, it may be clinically ineffective against invasive bacteria, even if these bacteria are sensitive to it in vitro. Pharmacokinetics Absorption: Rifaximin in the polymorphic form of alpha is practically not absorbed when taken orally (less than 1%). With repeated use in healthy volunteers and in patients with damaged intestinal mucosa, with inflammatory bowel disease, the concentration in plasma is very low (less than 10 ng / ml). When using the drug 30 minutes after ingestion of fatty foods, an increase in the systemic absorption of rifaximin, which has no clinical significance, was noted. Distribution: Rifaximin is moderately bound to plasma proteins. Communication with proteins in healthy volunteers is 67.5%, and in patients with liver failure, 62%.Excretion: Excreted from the body unchanged by the intestine (96.9% of the dose taken), since it does not undergo degradation and metabolism when passing through the gastrointestinal tract. Detected using labeled isotopes in the urine, rifaximin is no more than 0.025% of the ingested dose. Less than 0.01% of the dose is excreted by the kidneys as 25-deacetylrifaximin, the only rifaximin metabolite identified in humans. The excretion of rifaximin by the 14C kidneys does not exceed 0.4%. Systemic exposure is non-linear, dose-dependent, which is comparable to the absorption of rifaximin, possibly a limited dissolution rate. Pharmacokinetics in special groups of patients: There is no clinical data on the use of rifaximin in renal failure. Systemic exposure in patients with hepatic insufficiency is greater than that in healthy volunteers. Increased systemic exposure in these patients should be considered in the light of the local action of rifaximin in the intestine and its low systemic bioavailability, as well as available data on the safety of rifaximin in patients with liver cirrhosis.
Pharmacokinetics
The pharmacokinetics of rifaximin have not been studied in children.
Indications
Treatment of gastrointestinal infections caused by rifaximin-sensitive bacteria, including: Acute gastrointestinal infections. Traveler diarrhea. Syndrome of overgrowth of microorganisms in the intestine. In hepatic encephalopathy. In symptomatic uncomplicated diverticular disease of the intestinal tract. Prevention of infectious complications in colorectal surgery.
Contraindications
Diarrhea with fever and loose stools of blood. Intestinal obstruction (including partial). Severe ulcerative bowel disease. Children under 12 years old (efficacy and safety have not been established). Hereditary intolerance to fructose, impaired glucose-galactose absorption, deficiency of sucrase-isomaltase (for the dosage form of granules for the preparation of a suspension for oral administration). Hypersensitivity to rifaximin or other rifamycins or to any of the components that make up the drug. With care: a renal failure, simultaneous use with oral contraceptives.
Use during pregnancy and lactation
Data on the use of the drug Alpha Normix during pregnancy is very limited. Animal studies have shown the transient effect of rifaximin on ossification and the structure of the skeleton in the fetus. The clinical significance of these results is unknown. The use of the drug Alpha Normix during pregnancy is not recommended. It is not known whether rifaximin penetrates breast milk. The risk to a breastfed infant cannot be excluded. In order to decide whether to continue receiving rifaximin during breastfeeding, it is necessary to evaluate the ratio of the risk to the child and the benefit to the mother.
Dosage and administration
The drug is taken inside with a glass of water, regardless of the meal. In the treatment of diarrhea, adults and children over 12 years old are prescribed 200 mg each (1 tab. Or 10 ml of suspension) every 6 hours. Treatment for traveler's diarrhea should not exceed 3 days. In hepatic encephalopathy, adults and children over 12 years old are prescribed 400 mg (2 pills or 20 ml of suspension) every 8 hours. To prevent postoperative complications of colorectal surgery, adults and children over 12 years old are prescribed 400 mg (2 pills or 20 ml of suspension) every 12 hours. Prevention is carried out 3 days before surgery. In the syndrome of excessive bacterial growth, adults and children over 12 years old are prescribed 400 mg (2 pills) every 8-12 hours. For symptomatic uncomplicated diverticulosis, 200-400 mg are prescribed to adults and children over 12 years old (1-2 pills or 10 to 20 ml of suspension) every 8-12 hours. In chronic inflammatory bowel diseases, adults and children over 12 years old are prescribed 200-400 mg each (1-2 pills or from 10 to 20 ml of suspension) every 8-12 hours.
Side effects
Side effects are classified by frequency as follows very often (≥1 / 10), often (≥1 / 100-less than 1/10), infrequently (≥1 / 1000-less than 1/100), rarely (≥1 / 10000-less 1 / 1000), very rarely (less than 1/100000), is unknown (frequency cannot be set based on the available data). On the cardiovascular system it is not often - a feeling of heartbeat, blood flushes to the skin of the face, an increase in blood pressure. On the side of the hematopoietic system it is rare. lymphocytosis, monocytosis, neutropenia. unknown - thrombocytopenia. On the part of the immune system it is unknown - anaphylactic reactions, hypersensitivity, anaphylactic shock, laryngeal edema. Metabolic disturbances infrequently - loss of appetite, dehydration. On the psyche side, it is not often - pathological dreams, depressive mood, insomnia, nervousness. dizziness, headache.infrequently - hypesthesia, migraine, paresthesia, drowsiness, pain in the sinuses. unknown - pre-unconscious, agitation. On the part of the organ of vision infrequently - diplopia. On the side of the inner ear infrequently - earache, systemic dizziness. On the side of the respiratory system infrequently - shortness of breath, dry throat, nasal congestion, sore throat, cough, rhinorrhea . On the part of the digestive system, often - bloating, abdominal pain, constipation, diarrhea, flatulence, nausea, tenesmus, vomiting, urge to stool. infrequently - pain in the upper abdomen, ascites, dyspepsia, gastrointestinal motility disturbance, discharge of mucus and blood with a stool, dry lips, hard stools, increased AST activity, agevziya. unknown - changes in liver function tests, heartburn. From the urinary system infrequently - glucosuria, polyuria, pollakiuria, hematuria, proteinuria. From the side of the skin and subcutaneous fatty tissue infrequently - rash, sunburn. unknown - angioedema, allergic dermatitis, exfoliative dermatitis, eczema, erythema, pruritus, purpura, urticaria, erythematous rash, erythema of the palms, pruritus of the genitals. ., pain in the neck. Infections infrequently - candidiasis, herpes simplex, nasopharyngitis, pharyngitis, infections of the upper respiratory tract. unknown - clostridial infection. On the part of the reproductive system, infrequently - polymenorrhea. Common reactions are often - fever. infrequently - asthenia, pain and discomfort of indefinite localization, chills, cold sweat, flu-like symptoms, peripheral edema, hyperhidrosis, swelling of the face, fatigue. On the part of laboratory indicators, a change in INR.
Overdose
According to clinical studies in patients with traveler's diarrhea, rifaximin doses up to 1800 mg / day were well tolerated. Even in patients with normal intestinal bacterial flora, rifaximin at a dose of up to 2400 mg / day for 7 days did not cause adverse symptoms. In case of accidental overdose, symptomatic and supportive therapy is indicated.
Interaction with other drugs
In vitro studies show that rifaximin does not inhibit cytochrome P450 system isoenzymes (CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4) and does not induce CYP1A2 and CYP2B6, but is a weak inducer of CYP3A4.Clinical studies of drug interactions suggest that in healthy volunteers, rifaximin does not significantly affect the pharmacokinetics of drugs metabolized with CYP3A4. In patients with impaired liver function, it cannot be ruled out that rifaximin can reduce the drug exposure of CYP3A4 substrates (for example, warfarin, antiarrhythmic, anticonvulsant, etc.) while being used with them, as in liver failure it has a higher systemic exposure compared with healthy volunteers. In vitro studies suggest that rifaximin is a moderate substrate of P-glycoprotein and is metabolized by the isoenzyme CYP3A4. It is not known whether rifaximin has a systemic exposure to drugs that inhibit P glycoprotein and / or CYP3A4 while being used with it. Potential interactions of rifaximin with other drugs that are removed from the cell by P-glycoprotein or other transport proteins (MDR1, MRP2, MRP4, BCRP, BSEP) are unlikely.
special instructions
Clinical evidence suggests that Alpha Normix is not effective in treating intestinal infections caused by Campylobacter jejuni, Salmonella spp., Shigella spp., Which cause frequent diarrhea, fever, and blood with a stool. The drug Alpha Normix is not recommended for use if patients have fever and loose stools with blood. Alpha Normix should be discontinued if the symptoms of diarrhea worsen or persist for more than 48 hours. Another antibiotic therapy should be prescribed. Treatment for traveler's diarrhea should not exceed 3 days. It is known that Clostridium difficile-associated diarrhea can develop with the use of almost all antibacterial agents, including the drug Alpha Normiks. The potential relationship of Alpha Normix with the development of Clostridium difficile-associated diarrhea and pseudomembranous colitis cannot be ruled out. Experience with rifaximin in combination with other rifamycins is absent. Patients should be warned that, despite the slight absorption of rifaximin (less than 1%), it can cause the urine to stain reddish: this is due to the active substance rifaximin, which, like most antibiotics of this series (rifamycins), has a reddish-orange color.With the development of superinfection microorganisms that are insensitive to rifaximin, the administration of the drug Alpha Normix should be stopped and appropriate therapy should be prescribed. Due to the effect of the drug Alpha Normix on the intestinal flora, the effectiveness of oral contraceptives containing estrogens may decrease after taking it. It is recommended to use additional contraceptive measures when taking the drug Alpha Normiks, especially if the estrogen content in oral contraceptives is less than 50 μg. Taking the drug Alpha Normix possible no earlier than 2 hours after ingestion of activated carbon. Granules for the preparation of oral suspension contain sucrose, so the drug Alpha Normiks in this dosage form can not be used with hereditary fructose intolerance, impaired glucose-galactose absorption, sucrase-isomaltase deficiency. Influence on the ability to drive vehicles and control mechanisms Although dizziness and drowsiness are observed when using the drug Alpha Normiks, however, it does not significantly affect the ability to drive vehicles and engage in activities requiring increased attention and psychomotor speed. In the case of dizziness and drowsiness when using the drug, you should refrain from performing these types of activities.