Beta-clatinol

Beta-Clatinol has an antibacterial effect against Helicobacter pylori and stimulates the manifestation of the anti-Helicobacter properties of other drugs.

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Indications Beta-clatinol

It is used in the treatment of ulcerative lesions developing in the gastrointestinal tract and associated with the activity of the bacterium H. pylori.

Release form

The drug is released in tablets - in the amount of 2 pieces of each of the elements (pantoprazole, clarithromycin, and amoxicillin), which in total is 6 pieces inside the strip. The box contains 7 such strips.

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Pharmacodynamics

Pantoprazole.

The element has an antiulcer effect. It accumulates inside the canals of gastric parietal glandulocytes and is transformed into its active form - cyclic sulfenamide, which selectively interacts (forms a covalent compound) with H ⁺ -K ^- -ATPase.

The substance slows down H ⁺ -K ^- -ATPase of parietal glandulocytes and destroys the movement of hydrogen ions from them into the gastric lumen, and in addition, blocks the final stage of hydrophilic secretion of hydrochloric acid. The severity of inhibition of basal, as well as stimulated (the type of stimulus is not taken into account - this can be histamine, acetylcholine or gastrin) secretion of this element is determined by the size of the pantoprazole dosage.

The average effective dose level during in vivo tests fluctuates between 0.2-2.4 mg/kg. The maximum effect develops exclusively in a highly acidic (pH3) environment (if the pH values are higher, the substance remains almost inactive).

The element has an antibacterial effect on Helicobacter pylori. The minimum inhibitory value of the substance is 128 g/l. The medicinal effect with a single use develops quickly and continues to maintain its activity for 24 hours. The component helps to ensure rapid relief of symptoms of the disease and promotes the regeneration of ulcers in the duodenum. In case of use in a portion of 40 mg, the pH level> 3 is maintained for more than 19 hours.

Clarithromycin.

This element is a macrolide with antibacterial properties against many anaerobes and aerobes, as well as gram-negative and -positive microbes, including Helicobacter pylori.

The antibacterial effect of clarithromycin is provided by suppression of protein synthesis – by means of connection with the ribosomal membrane (its subunit of type 50S) inside bacterial cells. The minimally effective inhibitory indices of clarithromycin, as well as its active metabolic product (element 14-hydroxyclarithromycin) in relation to Helicobacter pylori are equal to 0.06 mcg/ml.

Amoxicillin.

The substance has bactericidal properties. It slows down the activity of transpeptidases, destroys the processes of binding peptide glycan (a supporting protein of cell membranes) at the stage of growth and division, and at the same time promotes the lysis of bacteria.

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Pharmacokinetics

Pantoprazole.

Pantoprazole is able to dissolve in the intestine, so its absorption begins after the tablet leaves the stomach. Absorption is rapid and complete. The bioavailability level is 70-80% (on average - about 77%). Peak values in plasma are noted after 2-4 hours (average values are about 2.7 hours). Plasma protein synthesis is 98%. The half-life is approximately 0.9-1.9 hours, the distribution volume is 0.15 l / kg, and the clearance rate is 0.1 l / h / kg.

The substance penetrates the BBB rather weakly and is also excreted in breast milk. Food or antacids do not affect the AUC, bioavailability, or Cmax values. Pharmacokinetic parameters are linear within the dosage range of 10-80 mg (Cmax and AUC increase proportionally with increasing dosage). Clearance rate and half-life depend on the portion size.

Metabolic processes occur in the liver (such as dealkylation, oxidation, and conjugation). It has a weak affinity for the hemoprotein P450 system; the exchange processes mainly involve isoenzymes CYP3A4, and also 2C19. The main metabolic products are demethylpantoprazole (half-life time is 1.5 hours) and 2 sulfated conjugates.

Excretion is mostly carried out with urine (82%), the substance is in the form of decay products. A small part of the drug is also noted in feces. The drug does not accumulate.

The half-life in individuals with liver cirrhosis increases to 9 hours, and in liver failure it increases slightly, although the half-life of the main metabolic product reaches 3 hours.

Clarithromycin.

After oral administration, it is absorbed quickly and almost completely. Food slows down absorption, but only slightly affects bioavailability. With a single use, 2 peaks of serum values of the substance are noted. The second peak occurs due to the ability of clarithromycin to concentrate in the gallbladder with its subsequent rapid or gradual release.

Plasma synthesis with whey protein is over 90%. Approximately 20% of the consumed portion undergoes liver oxidation, after which the main metabolic product is formed - the element 14-hydroxyclarithromycin. Metabolic processes are catalyzed by enzymes of the hemoprotein complex P450. The substance passes well into tissues and fluids, forming concentrations that exceed plasma values by 10 times.

The half-life of the substance after using a dosage of 0.5 g reaches 7-9 hours. Excretion of the unchanged component occurs with urine - up to 30%, and the remainder - in the form of metabolic products.

Amoxicillin.

After oral administration, it is almost completely and very quickly absorbed, forming a peak concentration after 1-2 hours. It demonstrates stability in an acidic environment, and food intake does not affect its absorption. Plasma synthesis with protein is approximately 17%.

Easily penetrates histohematic barriers (excluding unchanged BBB), and also inside tissues with organs. The medicinal properties of the element accumulate inside urine, lungs, peritoneal fluid, intestinal mucosa, contents of hydrothorax or blisters forming on the skin, and also inside middle ear fluid, female genitals, fetal tissues and bile with the gall bladder (with healthy liver function).

The half-life is 1-1.5 hours. If the patient has problems with kidney function, this period is extended to 12.6 hours, taking into account the values of CC. Part of the substance is metabolized with the subsequent formation of inactive metabolic products. About 50-70% of the unchanged component is excreted through the kidneys by tubular excretion (80%), as well as glomerular filtration (20%), and another 10-20% through the liver. Small amounts of amoxicillin pass into breast milk.

Dosing and administration

Beta-Clatinol should be taken daily, twice a day (morning and evening) before meals, in the amount of 3 tablets (1 from each category). To facilitate use, the drug is released in blisters, each of which contains the required daily dose of the drug - 1 tablet of each component. Therapy usually lasts for 1-2 weeks.

Use Beta-clatinol during pregnancy

Beta-Clatinol should not be prescribed during pregnancy.

Contraindications

Main contraindications:

• hypersensitivity to amoxicillin and pantoprazole with clarithromycin;
• severe liver diseases;
• a history of pathologies affecting the gastrointestinal tract (this especially applies to colitis caused by taking antibiotics);
• renal dysfunction;
• porphyria;
• allergic diathesis;
• bronchial asthma;
• infectious mononucleosis;
• hay fever;
• lymphocytic leukemia;
• breast-feeding;
• children under 18 years of age.

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Side effects Beta-clatinol

The use of the medication may cause the appearance of certain side effects.

Pantoprazole:

• digestive disorders: dry mouth, belching, diarrhea, bloating, vomiting, increased appetite, abdominal pain, nausea, constipation, as well as increased activity of transaminases and the appearance of GIST;
• signs of dysfunction of the nervous system and sensory organs: dizziness, insomnia, headaches, development of a feeling of nervousness and drowsiness, as well as asthenia, tremor, tinnitus, depression and paresthesia. Photophobia, hallucinations, visual disturbances, a feeling of confusion and disorientation (especially in people prone to such behavior) may also occur, as well as a worsening of these symptoms if they were present before taking the drug;
• problems with the functioning of the lymph and hematopoietic system: development of thrombocytopenia or leukopenia;
• liver disorders: increased liver enzyme levels (such as transaminases and γ-GT) and triglycerides. In addition, hepatocellular disorders develop, resulting in liver failure or jaundice;
• lesions affecting the urinary system and kidneys: the appearance of tubulointerstitial nephritis;
• signs from the urogenital system: the appearance of swelling, the development of hematuria or impotence;
• immune symptoms: anaphylactic signs, including anaphylaxis;
• reactions affecting the structure of bones and muscles, as well as the skin: the appearance of acne, arthralgia, alopecia, erythema multiforme, exfoliative dermatitis, photosensitivity, Stevens-Johnson syndrome and TEN;
• signs of allergy: urticaria, rash, Quincke's edema and itching;
• Others: development of myalgia, hyperglycemia, hypercholesterolemia, fever or hyperlipoproteinemia.

Clarithromycin:

• digestive and hepatobiliary dysfunction: dryness of the oral mucosa, epigastric pain, vomiting, bloating, development of stomatitis, glossitis, constipation, and nausea. There is also discoloration of the tongue, taste buds disorder, development of diarrhea, pseudomembranous colitis, dyspeptic symptoms, oral candidiasis, and also candidal stomatitis and the appearance of spots on the tongue. The shade of the teeth may change, jaundice, hepatitis, pancreatitis and cholestasis may occur, and in addition, fatal liver failure;
• manifestations affecting the functioning of the nervous system: a feeling of confusion, disorientation or anxiety, as well as the appearance of vertigo and dizziness, insomnia, headaches, disturbing dreams, hallucinations, as well as tinnitus and noise. In addition, paresthesia, psychosis with depersonalization, dyspnea, seizures and uveitis occur. Olfactory dysfunction and hearing loss are observed (this disorder is restored after stopping treatment);
• disorders of the cardiovascular system: ventricular flutter or fibrillation, prolongation of the QT interval, ventricular tachycardia and pirouette-type arrhythmia;
• immune disorders: anaphylactic symptoms;
• mental disorders: feelings of anxiety and depression;
• laboratory test results: transient increase in liver transaminase activity, leukopenia and thrombocytopenia, hypoglycemia, and in addition, an increase in blood urea levels and serum creatinine values;
• problems with the function of the musculoskeletal system: development of myalgia or arthralgia;
• disorders affecting urinary function: renal failure or tubulointerstitial nephritis;
• Allergy symptoms: Quincke's edema, rashes and urticaria. Rarely, anaphylaxis, Stevens-Johnson syndrome or TEN occur.

Colchicine toxicity (also fatal) has been reported with the use of clarithromycin and colchicine, especially in the elderly and in patients with renal failure.

Amoxicillin:

• digestive disorders: development of glossitis, oral candidiasis, stomatitis, dysbacteriosis, as well as vomiting, diarrhea, nausea and pain in the anal area. Hemorrhagic or pseudomembranous colitis and intestinal candidiasis may also develop, as well as superficial discoloration of tooth enamel;
• problems affecting the senses and nervous system: a feeling of anxiety, confusion or agitation, the development of headaches, seizures, insomnia or dizziness, as well as changes in behavior. Seizures are usually observed in people with kidney failure or when taking large doses of drugs;
• disorders in the cardiovascular system: development of tachycardia;
• problems with hemostasis, lymph and hematopoietic system: moderate increase in transaminase values in the blood, transient anemia, leuko-, thrombocyto- and neutropenia, eosinophilia, agranulocytosis, Werlhof's disease, hemolytic anemia, and in addition, prolongation of PT and bleeding indicators;
• liver and biliary tract dysfunction: moderate and temporary increase in transaminase activity;
• problems with renal function and urination: the appearance of crystalluria;
• symptoms of respiratory dysfunction: problems with respiratory activity;
• disorders of the urogenital system: vaginal candidiasis or tubulointerstitial nephritis;
• disorders of muscle and bone function: pain in the joints, as well as convulsive manifestations;
• lesions affecting the subcutaneous layer and skin: erythema multiforme, exfoliative dermatitis, maculopapular rashes, Stevens-Johnson syndrome, skin rashes and acute stage of generalized exanthematous pustulosis;
• immune signs: development of anaphylaxis;
• the appearance of infections or invasions: cutaneous candidiasis;
• symptoms of hypersensitivity: itching with rashes and urticaria (if urticaria occurs immediately after using the drug, this indicates the presence of an allergy, which is why the drug should be discontinued). Bullous dermatitis, serum sickness, and allergic vasculitis are occasionally observed. TEN and angioedema are noted sporadically;
• systemic disorders: there are isolated reports of drug-induced fever. With repeated or prolonged use of Beta-Clatinol, superinfection may occur, as well as colonization with resistant yeasts or microbes that cause vaginal/vaginal candidiasis.

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Overdose

Intoxication may cause potentiation of side effects.

If a patient is suspected of having developed an overdose, symptomatic and supportive measures should be taken.

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Interactions with other drugs

Pantoprazole.

The substance may reduce the extent of pH-dependent absorption of ketoconazole and other medications.

It is compatible with drugs that are metabolized by the P450 hemoprotein enzyme system (such as digoxin with phenazepam, carbazepine and diazepam, as well as diclofenac and theophylline, piroxicam with naproxen, warfarin and metoprolol with phenytoin, ethyl alcohol and nifedipine).

Does not affect the properties of hormonal contraceptives.

Clarithromycin.

The combination of clarithromycin with theophylline may cause an increase in plasma levels of the latter.

Combined administration with terfenadine increases its values in plasma, which can cause prolongation of the QT interval, and in addition, heart rhythm disorders.

Concomitant use of the substance with oral anticoagulants (eg, warfarin) may enhance their activity.

Combinations of the element with cyclosporine, disopyramide, carbazepine, and in addition lovastatin, phenytoin, cisapride, valproate, astemizole and pimozide with digoxin can increase the plasma values of these drugs.

The substance increases the blood levels of drugs whose metabolism occurs in the liver with the help of enzymes of the hemoprotein P450 complex: such as warfarin and other indirect coagulants, theophylline, digoxin, midazolam with carbamazepine, cisapride, cyclosporine with astemizole and triazolam, carob alkaloids, etc.

Clarithromycin reduces the absorption of zidovudine.

Amoxicillin.

The substance weakens the properties of oral contraception containing estrogen, and in addition, reduces the clearance level and increases the toxic effects of methotrexate.

Amoxicillin potentiates the absorption of digoxin.

The excretion process is slowed down when combined with indomethacin, probenecid, aspirin, as well as sulfinpyrazone, phenylbutazone and oxyphenbutazone, as well as other drugs that inhibit tubular secretion.

The antibacterial properties of the component are reduced when combined with antacids, as well as bacteriostatic drugs of the chemotherapeutic type; potentiation of properties occurs when combined with metronidazole or aminoglycosides.

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Storage conditions

Beta-Klatinol can be kept in a dark place, out of reach of small children. Temperature indicators - no more than +25°C.

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Shelf life

Beta-Clatinol can be used for 2 years from the date of release of the drug.

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Reviews

Beta-clatinol is effective in the treatment of ulcers. Reviews show that the drug is able to completely eliminate the disorder even in quite severe forms of ulcers.