Alpha Normix tablets coated. 200 mg 12 pcs. (Ryfaksymyn)

packaging 12 pcs

Pharmacological action

Rifaximin is a broad-spectrum antibiotic from the rifamycin group. Like other representatives of this group, it irreversibly binds the beta subunit of the bacterial enzyme to 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 susceptible bacteria. The drug has a wide spectrum of antimicrobial activity, including most gram-negative and gram-positive, aerobic and anaerobic bacteria.

A wide antibacterial spectrum of rifaximin helps to reduce the pathogenic intestinal bacterial load, which causes some pathological conditions.

The drug reduces:

- the formation of ammonia and other toxic compounds by bacteria, which in the case of severe liver disease, accompanied by impaired detoxification process, play a role in the pathogenesis and clinical manifestations of hepatic encephalopathy

- increased proliferation of bacteria in the syndrome of excessive

in the intestine growth microorganism the presence in the diverticulum of the colon of bacteria that can cause inflammation in and around the diverticular sac and possibly play a key role in the development of symptoms and complications of diverticular disease

- an antigenic stimulus that, in the presence of genetically determined defects in mucosal immunoregulation and / or in protective function, can initiate or constantly support chronic intestinal inflammation

- the risk of infectious complications during colorectal surgery.

Resistance Mechanism

The development of rifaximin resistance is due to reversible damage to the rpoB gene, which encodes 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 appearance of resistant gram-positive (enterococci) and gram-negative (E. coli) bacteria. When re-using rifaximin in high doses in healthy volunteers and in patients with inflammatory bowel disease, rifaximin-resistant strains appeared, however, they did not colonize the gastrointestinal tract (GIT) and did not displace rifaximin-sensitive strains.

When therapy was discontinued, 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 susceptibility testing cannot be used to determine the sensitivity or resistance of bacteria to rifaximin. Currently, there is insufficient clinical data to establish limits for evaluating sensitivity tests. Rifaximin was evaluated in vitro against pathogens of traveler's diarrhea from four regions of the world: enterotoxigenic and enteroaggregate strains of E. coli, Salmonella spp., Shigella spp., Non-cholera vibrios, Plesiomonas spp., Aeromonas spp. and Campylobacter spp. MPC90 (minimum inhibitory concentration) for the isolated strains was 32 μg / ml, and this level is easily achieved in the intestinal lumen as a result of the high concentration of rifaximin in feces. Since rifaximin in polymorphic alpha has low absorption from the digestive 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 polymorphic form 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 diseases, the plasma concentration 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, not having clinical significance, was noted.

Distribution of

Rifaximin binds moderately to plasma proteins. Communication with proteins in healthy volunteers is 67.5%, and in patients with liver failure 62%.

Excretion

It is excreted unchanged by the intestines (96.9% of the dose taken), as it does not undergo degradation and metabolism when passing through the gastrointestinal tract. Detected by labeled isotopes in urine, rifaximin is not more than 0.025% of the oral dose. Less than 0.01% of the dose is excreted by the kidneys as 25-deacetylrifaximin, the only metabolite of rifaximin identified in humans. Kidney excretion of 14C rifaximin does not exceed 0.4%. The systemic exposure is non-linear, dose-dependent, which is comparable to the absorption of rifaximin, possibly with a limited dissolution rate.

Special patient groups

With renal failure

There are no clinical data on the use of rifaximin in renal failure.

With liver failure

Systemic exposure in patients with liver failure is greater than that in healthy volunteers. An increase in systemic exposure in these patients should be considered in light of the local effect of rifaximin in the intestine and its low systemic bioavailability, as well as the available data on the safety of rifaximin in patients with cirrhosis.

Children

The pharmacokinetics of rifaximin in children has not been studied.

Indications

Treatment of gastrointestinal infections caused by bacteria sensitive to rifaximin, for example, acute gastrointestinal infections, traveler’s diarrhea, intestinal overgrowth syndrome, hepatic encephalopathy, symptomatic inflammatory bowel disease and

Prevention of infectious complications in colorectal surgery.

Contraindications

- Hypersensitivity to rifaximin or other rifamycins or to any of the components that make up the drug.

- Diarrhea accompanied by fever and loose stools with blood.

- Intestinal obstruction (including partial).

- Severe intestinal ulceration.

- Children under 12 years of age (efficacy and safety not established).

- Hereditary fructose intolerance, malabsorption of glucose-galactose, insufficiency of sucrose-isomaltase (for the dosage form granules for the preparation of a suspension for oral administration).

Precautions

Renal failure, concomitant use with oral contraceptives, concomitant use with a P-glycoprotein inhibitor such as cyclosporine.

Use during pregnancy and lactation

During pregnancy, the use of the drug is possible only in case of emergency, with the observance of precautions and under the direct supervision of a doctor.

The use of the drug during breastfeeding is allowed with appropriate medical supervision.

Composition

Each film-coated tablet contains:

Active ingredient:

rifaximin with a polymorphic structure of alpha 200 mg.

Excipients: sodium carboxymethyl starch 15 mg, glyceryl palmitostearate 18 mg, colloidal silicon dioxide 1 mg, talc 1 mg, microcrystalline cellulose 115 mg. Film sheath: hypromellose 5.15 mg, titanium dioxide (E171) 1.5 mg, disodium edetate 0.02 mg, propylene glycol 0.5 mg, red oxide red (E172) 0.15 mg.

Dosage and administration

Take orally with a glass of water, regardless of food intake.

Treatment of diarrhea

Adults and children over 12 years of age: 1 tablet of 200 mg or 10 ml of suspension (equivalent to 200 mg of rifaximin) every 6 hours. Treatment of traveler's diarrhea should not exceed 3 days.

Hepatic encephalopathy:

Adults and children 12 years of age and older: 2 tablets of 200 mg or 20 ml of

suspension (equivalent to 400 mg of rifaximin) every 8 hours. Prevention of postoperative complications in colorectal surgery:

Adults and children over 12 years of age: 2 tablets of 200 mg or 20 ml of suspension (equivalent to 400 mg of rifaximin) every 12 hours.

Prevention is carried out 3 days before surgery.

Overgrowth syndrome:

Adults and children over 12 years of age: 2 tablets of 200 mg every 8-12 hours.

Symptomatic uncomplicated diverticulosis:

Adults and children over 12 years of age: 1-2 tablets of 200 mg or 10 to 20 ml of suspension (equivalent to 200 to 400 mg of rifaximin) every 8-12 hours.

Chronic inflammatory bowel disease:

Adults and children 12 years of age and older: 1-2 tablets of 200 mg or 10 to 20 ml of suspension (equivalent to 200 to 400 mg of rifaximin) every 8-12 hours.

The duration of treatment with Alpha Normix should not exceed 7 days. A second course of treatment should be carried out no earlier than 20 to 40 days later. The total duration of treatment is determined by the clinical condition of the patients. On the recommendation of a doctor, the dose and frequency of their administration can be changed.

Dose adjustment in elderly patients and in patients with hepatic and renal failure is not required.

Preparation of suspension

Granules for preparation of suspension for oral administration are in a hermetically sealed vial. To prepare the suspension,

must open the bottle, add water to the mark and shake the bottle well. Add water repeatedly until the suspension reaches the indicated level of 60 ml.

The concentration of rifaximin in the prepared suspension is 100 mg in 5 ml. Shake the suspension well before use. Measure the finished suspension with the measuring cup available in the package.

Side effects

Side effects are classified by frequency of occurrence as follows: very often ( 1/10), often ( 1/100 - 1/10), infrequently ( 1/1000 - 1/100), rarely ( 1/10000 - 1/1000), very rarely ( 1/10000), unknown (frequency cannot be set based on available data).

From the cardiovascular system:

Infrequently: palpitations, flushing of the face, increased blood pressure.

Blood side:

Infrequently: lymphocytosis, monocytosis, neutropenia.

Unknown: thrombocytopenia.

On the part of the immune system:

Unknown: anaphylactic reactions, hypersensitivity, anaphylactic shock, laryngeal edema.

Metabolic disorders:

Infrequently: loss of appetite, dehydration.

Mental disorders:

Infrequently: pathological dreams, depressed mood, insomnia, nervousness.

From the central nervous system:

Often: dizziness, headache.

Infrequently: hypesthesia, migraine, paresthesia, drowsiness, headache in the sinus area.

Unknown: fainting state, arousal.

On the part of the organ of vision:

Infrequently: diplopia.

From the inner ear:

Infrequently: earache, systemic dizziness.

Respiratory:

Infrequently: shortness of breath, dry throat, nasal congestion, pain in the oropharynx, cough, rhinorrhea.

From the gastrointestinal tract and liver:

Often: bloating, abdominal pain, constipation, diarrhea, flatulence, nausea, tenesmus, vomiting, urge to defecate.

Infrequently: pain in the upper abdomen, ascites, dyspepsia, impaired gastrointestinal motility, mucus and blood secretion with stools, dry lips, “hard” stools, increased activity of aspartate aminotransferase, agevezia.

Unknown: impaired liver function tests, heartburn.

From the urinary system:

Infrequently: glucosuria, polyuria, pollakiuria, hematuria, proteinuria.

From the skin and subcutaneous fat:

Infrequently: rash, sunburn.

Unknown: angioedema, allergic dermatitis, exfoliative dermatitis, eczema, erythema, pruritus, purpura, urticaria, erythematous rash, erythema of the palms, genital itching.

From the musculoskeletal system:

Infrequently: back pain, muscle spasm, muscle weakness, myalgia, neck pain.

Infections:

Infrequently: candidiasis, herpes simplex, nasopharyngitis, pharyngitis, upper respiratory tract

infections.

Unknown: clostridial infection.

Reproductive system disorders:

Infrequently: polymenorrhea.

Common symptoms:

Often: fever.

Infrequently: asthenia, pain and discomfort of uncertain localization, chills, cold sweat, flu-like symptoms, peripheral edema, hyperhidrosis, facial edema, fatigue.

Laboratory Research: Changing the International Normalized Relationship.

Drug Interaction

In vitro studies show that rifaximin does not inhibit isoenzymes of the cytochrome P-450 system (CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4) and is not inducible CY2 and 1 CYP3A4. Clinical studies of drug interaction suggest careful monitoring of the international normalized relationship should be undertaken at the beginning and end of treatment. In order to maintain the desired level of anticoagulation, dose selection of oral anticoagulants may be required.

In vitro studies suggest that rifaximin is a moderate substrate of P-glycoprotein and is metabolized by the CYP3A4 isoenzyme.

It is unknown whether systemic exposure to rifaximin increases the drugs that inhibit CYP3A4 when co-administered.

In healthy volunteers, co-administration of a single dose of ciclosporin (600 mg), a potent inhibitor of P-glycoprotein, and a single dose of rifaximin (550 mg) resulted in an 83-fold and 124-fold increase in mean Cmax and AUC, respectively rifaximin. that rifaximin is a moderate substrate of β-glycoprotein and is metabolized by the CYP3A4 isoenzyme.

It is unknown whether systemic exposure to rifaximin increases the drugs that inhibit CYP3A4 when co-administered.

In healthy volunteers, co-administration of a single dose of ciclosporin (600 mg), a potent inhibitor of P-glycoprotein, and a single dose of rifaximin (550 mg) resulted in an 83-fold and 124-fold increase in mean Cmax and AUC, respectively rifaximin. The clinical significance of such elevation for systemic exposure is unknown.

Potential interactions of rifaximin with other drugs that are excreted from the cell by P-glycoprotein or other transport proteins (MRP2, MRP4, BCRP, BSEP) are unlikely.

overdose

According to clinical studies, patients with diarrhea of ​​the traveler dose of rifaximin up to 1800 mg / day were well tolerated.

Even in patients with normal intestinal bacterial flora, rifaximin at doses up to 2400 mg / day did not cause any adverse symptoms for 7 days. With an accidental overdose, symptomatic and supportive therapy is shown.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30 ° C.

Shelf suitability

3 Year

Deystvuyuschee substances

Ryfaksymyn

Dosage form

dosage form

tablets

A.f. Italy



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