The development of pathogenic microorganisms in the intestines often leads to diarrhea, digestive disorders, and inflammatory processes. For treatment in these cases, the antibiotic “Alpha Normix” is used. This is a universal-purpose product, the components of which destroy pathogenic bacteria. The effect is noticeable after the first use.
Pharmacological properties of the drug Alpha Normix
Pharmacodynamics. Rifaximin is a broad-spectrum antibiotic and is a semi-synthetic derivative of rifamycin SV. Irreversibly binds the β-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 wide spectrum of antibacterial activity, including most gram-negative and gram-positive, aerobic and anaerobic bacteria that cause gastrointestinal infections, including traveler's diarrhea. Gram-negative Aerobes: Salmonella spp., Shigella spp., Escherichia coli, including enteropathogenic strains, Proteus spp., Campylobacter spp., Pseudomonas spp., Yersinia spp., Enterobacter spp., Klebsiella spp., Helicobacter pylori ; anaerobes: Bacteroides spp., including Bacteroides fragilis, Fusobacterium nucleatum ; Gram-positive aerobes: Streptococcus spp., Enterococcus spp. , including Enterococcus fecalis, Staphylococcus spp. ; anaerobes: Clostridium spp. , including Clostridium difficile and Clostridium perfrigens, Peptostreptococcus spp. . Absorption of rifaximin in the α polymorphic form in the gastrointestinal tract when taken orally is insignificant (≤1%). The antibiotic acts locally in the intestine, where its high concentration is achieved, significantly higher than the minimum inhibitory concentration for the tested enteropathogenic microbes (after 3 days of therapy, a fecal level of 4000–8000 mcg/g is achieved when taking a daily dose of 800 mg). Due to this, rifaximin has a pronounced antibacterial effect. The use of the drug helps to reduce pathogenic intestinal bacterial flora, which causes some pathological conditions or is involved in their pathogenesis. The drug reduces:
- the formation by bacteria of ammonia and other toxic compounds, which in the case of severe liver disease, accompanied by a violation of the detoxification process, are involved in the pathogenesis of hepatic encephalopathy;
- increased proliferation of bacteria in intestinal microbial overgrowth syndrome;
- the presence of bacteria in the intestinal diverticulum, which may be involved in inflammation in and around the diverticulum and may play a key role in the development of symptoms and complications of diverticulosis;
- antigenic stimuli that, in the presence of genetically determined defects in mucosal immunoregulation and/or protective function, can induce or permanently maintain chronic intestinal inflammation;
- risk of infectious complications during colorectal surgery.
Due to the virtually absent absorption of rifaximin in the gastrointestinal tract, there is no risk of systemic side effects. In numerous clinical studies, rifaximin was always well tolerated by patients. Pharmacokinetics Rifaximin oral absorption is ≤1% based on pharmacokinetic studies in rats, dogs and humans.
The drug is not detected in blood plasma after administration in therapeutic doses (detection limit ≤0.5–2 ng/ml) or is detected in very low concentrations (less than 10 ng/ml in almost all cases) both in healthy volunteers and in patients with damaged intestinal mucosa (as a result of ulcerative colitis or Crohn's disease). Rifaximin found in urine is no more than 0.5% of the dose taken orally. Almost all rifaximin taken orally is found in the gastrointestinal tract, where very high concentrations of the drug are achieved (concentrations in feces of 4000-8000 mcg/g are achieved after 3 days of taking the drug at a daily dose of 800 mg). Comparative pharmacokinetic studies have demonstrated that polymorphic forms of rifaximin are absorbed from the intestine in greater quantities than polymorphic form α.
Pharmacodynamics and pharmacokinetics
"Alpha Normix" belongs to the refampicin group of antibiotics. The active component binds parts of bacterial enzymes, inhibits RNA synthesis, which inevitably leads to mass death of pathogenic microorganisms of different groups. The drug allows you to successfully fight gram-positive and gram-negative bacteria.
The active substance of the antibiotic is not absorbed into the intestines and does not enter the blood. The components act only on the pathogenic intestinal microflora, which minimizes the likelihood of side effects. As a result of taking the drug, it is possible to reduce:
- the level of ammonia and other compounds that are products of the vital activity of microorganisms;
- the concentration of bacteria that are present and multiply in colonic diverticula;
- intensity of inflammatory processes with all accompanying symptoms;
- proliferation of pathogenic bacteria, if it is associated with the syndrome of rapid proliferation of intestinal microflora;
- an antigenic stimulus that can cause chronic inflammatory processes in the intestines;
- risk of infection complications during or after colorectal surgery.
The antibiotic acts primarily on the intestinal microflora. No more than 1% is absorbed through the intestinal mucosa. The active substance of the drug is present in the blood in small quantities after administration. The maximum concentration is reached 3 hours after administration. Reaction products are excreted in feces by 99% and in small quantities (up to 1%) in urine.
Use of the drug Alpha Normix
Suspension Adults and children over 12 years of age: 10 ml oral suspension 3 times daily to 20 ml oral suspension 2–3 times daily (600–1200 mg rifaximin). Children aged 6 to 12 years: 10 ml oral suspension 2–3 times daily to 20 ml oral suspension 2 times daily (400–800 mg rifaximin). Children aged 2 to 6 years: 5 ml oral suspension 2-3 times daily to 10 ml oral suspension 3 times daily (200-600 mg rifaximin). For the treatment of adults and children over 6 years of age, instead of an oral suspension, Alpha Normix can be used in the form of film-coated tablets, 200 mg each. Tablets Adults and children over 12 years of age: from 1 tablet 3 times a day to 2 tablets 2-3 times a day (600-1200 mg rifaximin). Children aged 6 to 12 years: from 1 tablet 2-3 times a day to 2 tablets 2 times a day (400-800 mg of rifaximin). The duration of treatment should not exceed 7 days and depends on the clinical effect in patients. If necessary, repeated courses of treatment can be carried out with a break of 20–40 days. The total duration of therapy depends on the adequacy of the clinical effect in patients. Doses and frequency of administration can be changed on the recommendation of a doctor. Preparation of the suspension The granules for the preparation of the oral suspension are in a hermetically sealed bottle. The bottle must be opened, water added to the mark and shaken well. Add water again until the slurry reaches the specified level. The concentration of rifaximin in the finished suspension is 100 mg per 5 ml. To measure 5, 10 or 15 ml of suspension, add a measuring cup. The suspension remains stable for 7 days at room temperature. Before taking the drug, the bottle must be shaken well.
Compound
1 tablet contains 200 mg of the active ingredient rifaximin + additional substances (sodium carboxymethyl starch, microcrystalline cellulose, glycerol palmitostearate, colloidal silicon dioxide, talc, hypromellose, E172, titanium dioxide, disodium edetate, propylene glycol).
For 5 ml of a pre-prepared suspension of the drug there is 100 mg of rifaximin + additional ingredients (sodium carmellose, kaolin, sodium benzoate, wild cherry flavor, microcrystalline cellulose, pectin, sodium saccharinate, sucrose).
Side effects of the drug Alpha Normix
Analysis of safety data showed that the risk of side effects when using Alpha Normix is very low. These effects are limited primarily to gastrointestinal disturbances (nausea, dyspepsia, vomiting, abdominal pain and cramps), are mild to moderate and usually self-limit without the need for dose changes or interruption of therapy. The drug is practically not absorbed from the gastrointestinal tract, which eliminates the risk of developing systemic side effects. In rare cases, skin reactions such as urticaria may occur, which are likely due to individual intolerance to treatment. The risk of side effects is 0.7–2% of all cases of drug use. Post-marketing surveillance data confirm the above risk assessment and the nature of the observed events.
Side effects
Side effects are rare. Of those observed during the drug study, most were symptoms of concomitant diseases: increased blood pressure , dizziness , palpitations, headache , distortion or loss of taste, shortness of breath rash , cold sweat, fever , diarrhea , heartburn , angioedema .
The most likely reactions to occur are from the gastrointestinal tract: nausea , pain in the epigastric region , vomiting . Most often, reactions of this kind go away on their own some time after the start of use.
Special instructions for the use of Alpha Normix
During prolonged treatment with high doses or when the intestinal mucosa is damaged, a small amount of the drug (≤1%) may be absorbed, which can cause urine to turn reddish. This is due to the active substance, which, like most antibiotics of this series (rifamycins), has a red-orange color. Use during pregnancy and lactation. Rifaximin did not cause teratogenic effects in rats and rabbits. Adequate data and well-controlled studies in pregnant women are lacking. Since reproductive toxicity studies in animals do not allow assessment of the possibility of a toxic effect in humans, during pregnancy the drug should be taken only in cases of urgent need and under the direct supervision of a physician. The penetration of rifaximin into breast milk has not been studied, but is expected to be negligible due to very low absorption into the systemic circulation. Therefore, the use of Alpha Normix by women who are breastfeeding is permitted with appropriate medical supervision. The ability to influence the reaction rate when driving vehicles or other mechanisms. Not installed.
Indications for use
An antibiotic is prescribed to treat infections that are sensitive to its effects, namely:
- intestinal bacterial overgrowth syndrome;
- diverticular disease of the colon;
- traveler's diarrhea;
- acute infections in the gastrointestinal tract ;
- hepatic encephalopathy ;
- inflammation of the intestines (chronicle);
- prevention of complications after surgical operations in the colorectal region .
Directions for use and doses
Inside. Adults and children over 12 years old - from 1 table. every 8 hours up to 2 tablets. every 8–12 hours (corresponding to 600–1200 mg of rifaximin).
The duration of treatment should not exceed 7 days and is determined by the clinical condition of the patients.
If necessary, a second course of treatment should be carried out no earlier than after 20–40 days. The total duration of treatment is determined by the clinical condition of the patients.
On the recommendation of a doctor, the doses and frequency of their administration may be changed.
