Beta-Clatinol

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

[1], [2]

Indications of the beta-Clathinol

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

Release form

Release of the medication is carried out in tablets - in the amount of 2 pieces of each of the elements (pantoprazole, clarithromycin, and also amoxicillin), which in general is 6 pieces inside the strip. The box contains 7 such strips.

[3]

Pharmacodynamics

Pantoprazole.

Element has antiulcer effect. It accumulates inside the tubular gastric parietal glandulotsitov and converted to its active form - sulfenamide cyclic nature, which selectively reacts (forms a covalent linkage) with an H ⁺ -K ^- -ATPase.

The substance slows the H ⁺ -K ^- -ATPase of parietal glandulocytes and disrupts the movement of hydrogen ions from them into the gastric lumen, and besides it blocks the final stage of hydrophilic release of hydrochloric acid. The severity of basal and inhibitory depression (the type of stimulus is not taken into account - it can be histamine, acetylcholine or gastrin), the release of this element is determined by the size of the dosage of pantoprazole.

The level of the average effective portion during the in vivo tests ranges between 0.2-2.4 mg / kg. The maximum exposure develops exclusively in a strongly acidic (such as pH3) medium (if the pH is higher - the substance remains almost inactive).

The element has an antibacterial effect on Helicobacter pylori. Minimally slowing down the index of the substance is 128 g / l. The drug effect with a one-time application develops rapidly and continues to be active for 24 hours. The component helps to provide rapid relaxation of the symptoms of the disease and promotes the regeneration of ulcers in the area of the duodenum intestines. If used in a dose of 40 mg, the pH> 3 is maintained for more than 19 hours.

Clarithromycin.

This element is a macrolide with antibacterial properties against a lot of anaerobes and aerobes, as well as gram-negative and-positive microbes, among which Helicobacter pylori.

The antibacterial effect of clarithromycin is provided by the suppression of protein synthesis - by linkage to the ribosomal membrane (its subunit type 50S) inside the bacterial cells. Minimally effective retarding indices of clarithromycin, as well as its active metabolic product (element 14-hydroxyclarithromycin) against Helicobacter pylori are equal to 0.06 μg / ml.

Amoxicillin.

The substance has bactericidal properties. It slows the activity of transpeptidases, destroys peptidoglycan binding (it is the supporting protein of cell membranes) at the stage of growth and division, and at the same time promotes the lysis of bacteria.

[4], [5]

Pharmacokinetics

Pantoprazole.

Pantoprazole is able to dissolve inside the intestine, so its absorption begins after the tablet leaves the stomach. Absorption is fast and complete. The level of bioavailability is 70-80% (on average - about 77%). Peak values inside the plasma are noted after 2-4 hours (mean values - about 2.7 hours). Plasma synthesis of proteins 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 weakly penetrates the BBB, and also excretes with the mother's milk. The consumption of food or antacids does not affect the values of AUC, bioavailability, and Cmax. Pharmacokinetic parameters are linear within the limits of dosages of 10-80 mg (in proportion to the increase in dosage, the parameters Cmax and AUC increase). The level of clearance and half-life depends on the size of the portion.

Metabolic processes occur in the liver (such as dealkylation, oxidation, and conjugation). Has a weak affinity for the hemoprotein P450 system, in the exchange processes involved mainly isoenzymes CYP3A4, and in addition 2S19. The main products of metabolism are demethylpantoprazole (half-life - 1.5 hours) and 2 conjugates of sulfated character.

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

The half-life of patients with hepatic cirrhosis increases to 9 hours, and if liver insufficiency increases slightly, although the half-life of the main product of metabolism reaches 3 hours.

Clarithromycin.

After oral administration, it absorbs quickly and almost completely. Food inhibits absorption, but only slightly affects the bioavailability. With a one-time application, there are 2 peaks of serum values of the substance. The second peak is due to the ability of clarithromycin to concentrate inside the gallbladder with its further rapid or gradual release.

Plasma synthesis with whey protein is over 90%. Approximately 20% of the consumed portion undergoes hepatic oxidation, after which the main product of metabolism, the element 14-hydroxyclarithromycin, is formed. The metabolic processes catalyze the enzymes of the hemoprotein complex P450. The substance passes well inside tissues and liquids, forming concentrations exceeding the plasma values by a factor of 10.

The half-life of the substance after applying 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 absorbed almost completely and very quickly, forming a peak concentration after 1-2 hours. Demonstrates stability within the acidic environment, and eating does not affect its absorption. Plasma synthesis with protein is approximately 17%.

Easily penetrates through the histohematological barriers (excluding the unchanged BBB), and besides it inside the tissues with organs. The medicinal characteristics of the element are cumulated inside the urine, lungs, peritoneal fluid, intestinal mucosa, contents of hydrothorax or blisters forming on the skin, and also inside the middle ear, female genitalia, fetal tissues and bile with gallbladder (with healthy liver function).

The elimination half-life is 1-1.5 hours. If the patient has problems with kidney function, this period is prolonged to 12.6 hours, taking into account the QC values. 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%), and glomerular filtration (20%), and 10-20% through the liver. Small amounts of amoxicillin pass into the mother's milk.

Dosing and administration

Beta-Clatinol should be consumed daily, twice a day (in the morning and in the evening) before meals, in the amount of 3 tablets (1 in each category). To facilitate the use, the medicine is produced in blisters, each of which contains the necessary daily portion of the drug - according to the first tablet of each of the components. Therapy usually lasts for 1-2 weeks.

Use of the beta-Clathinol during pregnancy

In pregnancy, Beta-Clatinol is not allowed.

Contraindications

The main contraindications:

• hypersensitivity to amoxicillin and pantoprazole with clarithromycin;
• hepatic diseases of a serious nature;
• presence in the anamnesis of the pathologies touching the area of the digestive tract (in particular, this refers to the colitis caused by the intake of antibiotics);
• disorders of renal activity;
• porphyria;
• diathesis of an allergic nature;
• bronchial asthma;
• mononucleosis of infectious origin;
• Pollinosis;
• lymphocytic leukemia;
• breast-feeding;
• children under the age of 18 years.

[6]

Side effects of the beta-Clathinol

The use of medication can cause the emergence of certain side-effects.

Pantoprazole:

• disorders of digestive activity: dry mouth mucous, eructation, diarrhea, bloating, vomiting, increased appetite, abdominal pain, nausea, constipation, and in addition an increase in transaminase activity and the appearance of GISO;
• signs of disruption in the work of the National Assembly and senses: the occurrence of dizziness, insomnia, headaches, the development of a feeling of nervousness and drowsiness, and in addition asthenia, tremor, ear noise, depression and paresthesia. There may also be photophobia, hallucinations, visual disturbances, a sense of entanglement and disorientation (especially in people with a penchant for such behavior), and in addition, worsening of these manifestations when they are present before taking drugs;
• problems with the lymphatic and hematopoietic system: development of thrombocyto- or leukopenia;
• hepatic disorders: an increase in the values of liver enzymes (such as transaminases and γ-HT), as well as triglycerides. In addition, hepatocellular disorders develop, against which there is liver failure or jaundice;
• lesions affecting the system of urination and kidneys: the appearance of tubulointerstitial nephritis;
• signs of the urogenital system: the appearance of edemas, the development of hematuria or impotence;
• immune symptoms: anaphylactic signs, among which 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 allergies: urticaria, rashes, Quincke edema and itching;
• Other: the development of myalgia, hyperglycemia, hypercholesterolemia, fever or hyperlipoproteinemia.

Clarithromycin:

• disorders of the digestive and hepatobiliary function: the appearance of dryness in the oral mucosa, epigastric pain, vomiting, bloating, the development of stomatitis, glossitis, constipation, and nausea. There is also a discoloration of the tongue, a disorder of taste buds, the development of diarrhea, pseudomembranous colitis, dyspeptic symptoms, oral candidiasis, and also the candidal form of stomatitis and the appearance of spots in the tongue. There may be a change in the shade of the teeth, jaundice, hepatitis, pancreatitis and cholestasis, and in addition liver failure is of a lethal nature;
• manifestations affecting the work of the National Assembly: a sense of confusion, disorientation or anxiety, and in addition the appearance of vertigo and dizziness, insomnia, headaches, anxious dreams, hallucinations, as well as ear ringing and noise. In addition, there are paresthesia, psychosis with depersonalization, dyspnea, seizures and uveitis. There are violations of the olfactory function and hearing loss (this disorder is restored after discontinuation of treatment);
• disorders of CCC function: fluttering or ventricular fibrillation, prolongation of QT-interval, ventricular tachycardia and piruette-type arrhythmia;
• immune disorders: anaphylactic signs;
• mental disorders: feelings of anxiety and depression;
• indications of laboratory tests: transient increase in the activity of the effects of transaminases of the liver, leuko- and thrombocytopenia, hypoglycemia, and in addition an increase in the level of urea inside the blood and serum creatinine values;
• problems with the function of ODA: the development of myalgia or arthralgia;
• disorders affecting the urinary function: kidney failure or tubulointerstitial nephritis;
• allergy symptoms: Quincke edema, rashes and hives. Occasionally there is anaphylaxis, Stevens-Johnson syndrome or TEN.

There is information about the appearance of colchicine toxicity (also fatal) as a result of the use of clarithromycin together with colchicine, especially in the elderly, as well as with kidney failure.

Amoxicillin:

• disorders in the digestive organs: the development of glossitis, oral candidiasis, stomatitis, dysbiosis, and in addition vomiting, diarrhea, nausea and pain in the anus. Also can develop colitis of hemorrhagic or pseudomembranous nature and intestinal candidiasis, and besides this is a superficial discoloration of tooth enamel;
• problems affecting the senses and the NA: a feeling of anxiety, confusion or arousal, the development of headaches, seizures, insomnia or dizziness, and also the appearance of changes in behavior. Seizures are usually noted in people with kidney failure or when using large portions of drugs;
• violations in the field of CAS: the development of tachycardia;
• problems with hemostasis, lymphoma and hematopoietic system: a moderate increase in the values of transaminases inside the blood, transient anemia, leuko-, thrombocyto- and neutropenia, eosinophilia, agranulocytosis, Verlhof disease, hemolytic anemia, and in addition prolongation of PTV indices and bleeding;
• disorders of the liver and ZHVP: a moderate and temporary increase in the activity of the transaminase;
• problems with renal function and urinary activity: the appearance of crystalluria;
• symptoms of impaired respiratory function: problems with respiratory activity;
• disturbances in the work of the urogenital system: vaginal candidiasis or tubulointerstitial nephritis;
• disorders of the musculature and bones: pain in the joints, and in addition convulsive manifestations;
• lesions affecting the subcutaneous layer and skin: erythema polyforma, exfoliative dermatitis, maculopapular type rashes, Stevens-Johnson syndrome, skin rash and acute stage of exanthematous pustules of generalized nature;
• immune signs: the development of anaphylaxis;
• occurrence of infections or invasions: cutaneous candidiasis;
• symptoms of hypersensitivity: itching with rashes and urticaria (if after using the drug immediately there was a urticaria, it demonstrates the presence of an allergy, because of what the medicine needs to be canceled). Occasionally there is dermatitis bullous character, serum sickness, and besides vasculitis of an allergic type. TEN and angioedema are noted singly;
• systemic disorders: there are isolated information about the development of drug-induced fever. With repeated or prolonged use of Beta-Clatinol, superinfection may occur, as well as colonization of resistant yeasts or microbes that cause the appearance of vaginal / vaginal candidiasis.

[7], [8], [9]

Overdose

Intoxication can cause potentiation of side effects.

If a patient is suspected of developing an overdose, symptomatic and supportive measures are required.

[10], [11], [12], [13]

Interactions with other drugs

Pantoprazole.

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

It is compatible with drugs metabolized by the enzyme system of hemoprotein P450 (such as digoxin with phenazepam, carbazepine and diazepam, and in addition 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 can cause an increase in the plasma parameters of the latter.

Combined therapy with terfenadine increases its values within the plasma, which can cause lengthening of the QT-interval, and in addition to the rhythm disorder of the heartbeat.

The simultaneous use of a substance with an oral anticoagulant (for example, with warfarin) can enhance the activity of their effects.

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 values of drugs metabolized inside 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, ciclosporin with astemizole and triazolam, carob alkaloids and so on.

Clarithromycin decreases the severity of absorption of zidovudine.

Amoxicillin.

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

Amoxicillin potentiates the absorption of digoxin.

The process of excretion slows down when combined with indomethacin, probenecid, aspirin, and in addition, sulfinpyrazone, phenylbutazone and oxyphenbutazone, as well as other drugs that inhibit the tubular secretion.

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

[14], [15], [16]

Storage conditions

Beta-Clatinol is allowed to be kept in a dark place, protected from access by young children. The temperature is not more than 25 ° C.

[17]

Shelf life

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

[18]

Reviews

Beta-clathinol is effective in the treatment of ulcer diseases. The reviews show that the drug is able to completely eliminate the disorder even with quite severe forms of ulcers.