Klabaks - instructions for use, doses, side effects, contraindications

Excipients: microcrystalline cellulose, hypromellose 5 cps, giprolase L, croscarmellose sodium, alginic acid, purified water * * Isopropanol, colloidal silicon dioxide, sucrose, aspartame, xanthan gum, sodium citrate, sodium benzoate, titanium dioxide, flavor, peppermint 517, Tutti Frutti flavor 051880 ARC 551, sodium chloride;

enteric coating: a copolymer of methacrylic acid-ethyl acrylate (1: 1) 30% dispersion, macrogol 1500, talc, Carbomer (Carbopol 974 P), purified water *.

* is lost in the production process

Description:

The granulated powder white to almost white color, forming a white suspension to almost white color upon the addition of water. The resulting suspension has a fruity flavor.

Pharmacotherapeutic group:Antibiotic-macrolide

ATX: & nbsp

J.01.F.A.09 Clarithromycin

Pharmacodynamics:

Bacteriostatic macrolide antibiotic is a second-generation macrolide wide spectrum of action. Disrupts the synthesis of the protein of microorganisms (binds to 50S subunit of the ribosome membrane of a microbial cell). Active in relation to: Streptococcus agalactiae (Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi, Neisseria gonorrhoeae, Neisseria meningitides, Listeria monocytogenes, Legionella pneumophila, Mycoplasma pneumoniae, Helicobacter (Campylobacter) pylori, Campylobacter jejuni, Chlamydia pneumoniae (trachomatis), Moraxella (Branhamella) catarrhalis, Bordetella pertussis, Propionibacterium acnes, Mycobacterium avium, Mycobacterium leprae, Staphylococcus aureus, Ureaplasma urealyticum, Toxoplasma gondii, Corynebacterium spp., Borrelia burgdorferi, Pasteurella multocida, some anaerobes (Eubacterium spp., Peptococcus spp., Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus) and all mycobacteria, except Mycobacterium tuberculosis.

Pharmacokinetics:

Absorption is fast. Food slows down absorption, without significantly affecting bioavailability. The bioavailability of clarithromycin in the form of a suspension is equivalent to or slightly higher than when taken in the form of tablets. The connection with plasma proteins is more than 90%. After a single dose, 2 peaks of maximum concentration are recorded. The second peak is due to the ability of the drug to concentrate in the gallbladder, followed by a gradual or rapid release. Time to reach the maximum concentration with oral intake of 250 mg - 1-3 hours.

After oral intake of 20% of the dose is rapidly hydroxylated in the liver by cytochrome P450 enzymes to form the main metabolite - hydroxyclorithromycin, which has a pronounced antimicrobial activity against Haemophilus influenzae.

With a regular intake of 250 mg / day, the equilibrium concentrations of the unchanged drug and its main metabolite are 1 and 0.6 μg / ml, respectively; the half-life is 3-4 hours and 5-6 hours. When the dose is increased to 500 mg / day, the equilibrium concentration of the unchanged drug and its metabolite in plasma is 2.7-2.9 and 0.83-0.88 μg / ml, respectively; the half-life is 4.8-5 hours and 6.9-8.7 hours, respectively. In therapeutic concentrations, it accumulates in the lungs, skin and soft tissues (concentrations 10 times higher than serum levels).

It is allocated by the kidneys and with the fecal masses (20-30% - in unchanged form, the rest - in the form of metabolites). With a single admission of 250 mg and 1.2 g of kidneys, 37.9 and 46% are allocated, with a caloric mass of 40.2 and 29.1%, respectively.

Indications:

Klabaks® suspension is used to treat infectious diseases caused by sensitive microorganisms. These diseases include:

- infections of the lower respiratory tract (bronchitis, pneumonia);

- infections of the upper respiratory tract (pharyngitis, sinusitis), otitis media;

- infections of the skin and soft tissues (folliculitis, erysipelas);

- clarithromycin is indicated for elimination H.pylori and a decrease in the frequency of recurrences of duodenal ulcers.

Contraindications:

- Clarithromycin is contraindicated in patients with increased sensitivity to antibiotics from the macrolide group;

- when treating clarithromycin, do not prescribe ergot derivatives;

- when treating clarithromycin it is forbidden to take cisapride, pimozide, astemizole and terfenadine (see also section Interaction with other medicinal products). In patients taking these drugs concomitantly with clarithromycin, there is an increase in their concentration in the blood. It is possible to extend the interval QT and the development of cardiac arrhythmias, including ventricular paroxysmal tachycardia, ventricular fibrillation and flutter or ventricular fibrillation;

- severe dysfunction of the liver and / or kidney;

- porphyria;

- pregnancy (I trimester);

- lactation period.

Carefully:

Renal and / or hepatic insufficiency (mild to moderate).

Dosing and Administration:

Inside. Suspension of Klabaks® can be taken regardless of food intake. Before each use, it is recommended to shake the suspension well, after use, it should be stored in a vial with a tightly closed lid.

Children up to 12 years old the drug is prescribed in a dose of 7.5 mg / kg of body weight 2 times a day. The maximum daily dose is 500 mg. The duration of the course of treatment is 7-10 days.

In patients with renal insufficiency with creatinine clearance less than 30 ml / min, the doso of the drug should be reduced 2 times. The maximum duration of a course in patients of this group should be no more than 14 days.

Doses of KLABAK® suspension depending on weight and age, recommended for children

Body weight * (kg)	Age (years)	Dosage 2 times a day
		mg	ml
		mg	125 mg / 5ml	250 mg / 5ml
8-11	1-2	62,5	2,5	1,25
12-19	3-6	125	5	2,5
20-29	7-9	187,5	7,5	3,75
30-40	10-12	250	10	5,0

* Children weighing <8 kg should receive a dose of approximately 7.5 mg / kg 2 times a day or 0.3 ml / kg of a suspension of 125 mg / 5 ml 2 times a day.

Adults and children from 12 years old: recommended taking the drug in tablets of 250 mg or 500 mg.

Instructions for preparing a suspension

For getting 60 ml of suspension To dry powder, add 2 ml of 34 ml of water. After each addition of water, it is necessary to shake the bottle well.

For getting 100 ml of suspension To dry powder, 55 ml of water should be added in 2 divided doses. After each addition of water, it is necessary to shake the bottle well.

Side effects:

The most common symptoms are from the gastrointestinal tract (nausea, dyspepsia, abdominal pain, vomiting and diarrhea).There are reports of the development of pseudomembranous colitis from moderately expressed to life threatening. Other adverse reactions include headaches, taste disorders and transient increases in liver enzyme activity.

There are reports of rare cases of development of paresthesia.

Sometimes hepatitis cases were observed with an increase in the level of liver enzymes in the serum and the development of cholestasis and jaundice. These liver damage in some cases were severe and, as a rule, reversible. In exceptional cases, hepatic insufficiency developed with a lethal outcome.

Rarely reported increases in serum creatinine, the development of interstitial nephritis, the development of renal failure.

When taking clarithromycin orally, allergic reactions were observed, the intensity of which varied from hives and skin rashes, to anaphylaxis and Stevens-Johnson syndrome.

There are reports of hearing loss during the treatment with clarithromycin, which in most cases was restored after the drug was discontinued. Also, changes in the perception of taste, as a rule, appearing together with a taste disorder, the development of glossitis,stomatitis, candidiasis of the oral mucosa and changes in the color of the tongue during the treatment with clarithromycin, changes in the color of teeth in those receiving clarithromycin patients. Changing the color of the teeth in most cases was reversible.

In rare cases, hypoglycemia was noted, and in some of them, those who received hypoglycemic agents for oral ingestion or insulin during the treatment with clarithromycin.

It is known about individual cases of thrombocytopenia and leukopenia.

When taking clarithromycin, transient side effects on the central nervous system were observed: dizziness, anxiety, fear, fear, insomnia, nightmares, tinnitus, confusion, disorientation, hallucinations, psychoses and depersonalization.

In the treatment with clarithromycin, as with other macrolides, the lengthening of the interval QT, ventricular arrhythmia, including ventricular paroxysmal tachycardia and flutter or fibrillation of the ventricles.

With prolonged use of clarithromycin, the development of resistance of microorganisms is possible.

Overdose:

Probably the development of symptoms from the gastrointestinal tract (nausea, vomiting, diarrhea); headache, confusion.

In case of an overdose, immediate gastric lavage and symptomatic treatment are necessary. Hemodialysis and peritoneal dialysis do not lead to a significant change in the level of clarithromycin in the blood serum.

Interaction:

With simultaneous intake increases the concentration in the blood of drugs metabolized in the liver with the help of cytochrome P450 enzymes - indirect anticoagulants, carbamazepine, theophylline, astemizole, cisapride, terfenadine (2-3 times), triazolam, midazolam, cyclosporine, disopyramide, phenytoin, rifabutin , lovastatin, digoxin, ergot alkaloids, and others.

It is reported that there are rare cases of acute necrosis of skeletal muscles that coincide in time with simultaneous administration of clarithromycin and inhibitors of hydroxymethylglutaryl-CoA reductase, lovastatin and simvastatin.

There are reports of an increase in the concentration of digoxin in the plasma of patients receiving concomitantly digoxin and clarithromycin tablets. In such patients it is necessary to constantly monitor the serum digoxin content in order to avoid digitalis intoxication.

Clarithromycin can reduce the clearance of triazolam and, thus, increase its pharmacological effects with the development of drowsiness and confusion.

The simultaneous use of clarithromycin and ergotamine (ergot derivative) can lead to acute ergotamine intoxication, manifested by severe peripheral vasospasm and perverted sensitivity.

Simultaneous administration of zidovudine orally to HIV-infected adults and clarithromycin tablets may lead to a decrease in equilibrium concentrations of zidovudine. Given the fact that clarithromycinprobably changes the absorption of zidovudine, this interaction is largely avoided when taking clarithromycin and zidovudine at various hours of the day (with an interval of at least 4 hours).

With the simultaneous administration of clarithromycin and ritonavir, the serum concentration of clarithromycin increases. Correction of the dose of clarithromycin in these cases is not required for patients with normal renal function. However, in patients with creatinine clearance from 30 to 60 ml / min, the dose of clarithromycin should be reduced by 50%. When creatinine clearance is less than 30 ml / min, the dose of clarithromycin should be reduced by 75%.With simultaneous treatment with ritonavir should not be prescribed clarithromycin in doses over 1 g / day.

It is possible to develop cross-resistance between clarithromycin, clindamycin and lincomycin.

Special instructions:

In the presence of chronic liver diseases it is necessary to conduct regular monitoring of "hepatic" enzymes serum.

Caution is prescribed against the background of drugs metabolized by the liver (it is recommended to measure their concentration in the blood).

In the case of co-administration with warfarin or other indirect anticoagulants, prothrombin time should be monitored.

With heart disease in the anamnesis, simultaneous administration with terfenadine, cisapride, astemizole is not recommended.

It is necessary to pay attention to the possibility of cross-resistance between clarithromycin and other antibiotics from the macrolide group, as well as lincomycin and clindamycin.

With prolonged or repeated use of the drug, it is possible to develop superinfection (growth of insensitive bacteria and fungi).

Each 5 ml suspension of 125 mg / 5 ml contains 2.9 g of sucrose, and every 5 ml of a suspension of 250 mg / 5 ml - 2.5 g of sucrose,that it is necessary to take into account when prescribing the drug to children with hereditary fructose intolerance, glucose-galactose malabsorption syndrome, sugar isomaltase deficiency and other disorders of carbohydrate metabolism.

Form release / dosage:Granules for the preparation of a suspension for ingestion 125 mg / 5 ml and 250 mg / 5 ml.

Packaging:

In bottles of 60 ml or 100 ml of high-density polyethylene, with a protective membrane, a screw cap and a measuring cap; 1 bottle with instructions for use is placed in a cardboard box.

Storage conditions:

Store in a dry place at a temperature of no higher than 25 ° C.

The ready-made suspension should be stored at a temperature not higher than 25 ° C, do not freeze or cool.

Keep out of the reach of children.

Shelf life:

2 years.

The finished suspension is 14 days.

Do not use after the expiry date stated on the package

Terms of leave from pharmacies:On prescription

Registration number:LS-002312

Date of registration:01.12.2006

Expiration Date:01.12.2011

The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India

Manufacturer: & nbsp

RANBAXY LABORATORIES, Ltd. India

Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED

Information update date: & nbsp11.01.2018

Illustrated instructions

Instructions

Klabaks® (Klabax®)