Амбровикс (tablets)

General characteristics. Structure:

Active ingredient: 30 mg of Ambroxol of a hydrochloride.

Excipients: starch corn, sodium lactose monohydrate, cellulose microcrystallic krakhmalglikolit (type A), magnesium stearate, silicon dioxide colloid anhydrous.

The medicine liquefying a bronchial secret, facilitating process of expectoration and not stimulating a tussive reflex.

Pharmacological properties:

Pharmacodynamics. In researches it is shown that Ambroxol possesses sekretomotorny, sekretolitichesky and expectorant action, stimulates serous cells of glands of a mucous membrane of bronchial tubes, increases the maintenance of a mucous secret and release of surfactant (surfactant) in alveoluses and bronchial tubes. Normalizes the broken ratio of serous and mucous components of a phlegm. Activating the hydrolyzing enzymes and strengthening release of lysosomes from cells Klara, reduces viscosity of a phlegm. Increases physical activity of cilia of a ciliary epithelium, increases mukotsiliarny transport of a phlegm. Has anesthetic effect that is explained by property of Ambroxol to block natrium channels. This process is reversible and depends on concentration. At the research in vitro it was established also that release of cytokines from fabric mononuclear and polymorphonuclear blood cells considerably decreases. Effect of Ambroxol begins in 30 min. and continues 6-12 h. The maximum therapeutic effect is shown for the 3rd days of treatment.

Pharmacokinetics. Absorption and distribution: Bystry and almost full absorption with linear dependence on a dose in a therapeutic interval of concentration is characteristic of Ambroxol. Cmax in plasma is reached in 0.5-3 h. In a therapeutic interval of concentration linkng with proteins of plasma makes about 90%. Transition of Ambroxol in fabric at oral administration comes from blood quickly. The highest concentration of active component of drug are observed in lungs. Gets through hematoencephalic and placental barriers, it is allocated with breast milk.
Metabolism and removal:
About 30% of the accepted dose are exposed to effect of "the first passing" through a liver. Researches on microsomes of a liver of the person showed that CYP3A4 is the prevailing isoform responsible for Ambroxol metabolism. The rest of Ambroxol is metabolized in a liver, mainly, by conjugation with formation pharmacological of inactive metabolites (dibromantranilovy acid and glucuronic conjugates).
T1/2 of Ambroxol makes 10 hours and can increase at a heavy renal failure, but does not change at an abnormal liver function. Also the GIT in the form of metabolites, 5% in not changed look is removed preferential by kidneys (90%). The general clearance is in limits of 660 ml/min., about 8% of the general clearance are the share of renal clearance.

Clinically significant influence of age and floor on Ambroxol pharmacokinetics therefore there are no bases for selection of a dosage for these signs is not revealed.

Indications to use:

The acute and chronic bronchopulmonary diseases which are followed by allocation of a viscous phlegm:
— acute and chronic bronchitis;
— pneumonia;
— chronic obstructive pulmonary disease;
— bronchial asthma with difficulty of an otkhozhdeniye of a phlegm;
— bronchoectatic disease.

Route of administration and doses:

Inside, after meal to wash down with liquid. To adults and children 12 years are more senior appoint on 1 tablet (30 mg) 3 times a day in the first 2-3 days, then on 1 tablet 2 times, if necessary for increase in therapeutic effect it is possible to appoint on the 2nd tablet 2 times a day (120 mg/days); children are 6-12 years old – 1/2 tablets (15 mg) 2-3 times a day. During treatment it is necessary to use a lot of liquid (juice, tea, water) for strengthening of mucolytic effect of drug. Duration of treatment is defined by the doctor individually and depends on disease severity. In need of drug use more than 4-5 days consultation and control of the doctor is required.

Features of use:

Extremely weakened patients sick with anatomic narrowing of bronchial tubes and the increased secretion of slime at use of Ambroxol can have difficulties of evacuation of a bronchial secret. In these cases it is necessary to take measures for suction of a secret.

At the admission of reception of medicine it is not necessary to double a dose.

It is necessary to appoint medicine with care at a peptic ulcer of a stomach and duodenum. At a heavy renal failure and a liver it is necessary to use lower doses of reception or to increase an interval between receptions.

Very exceptional cases of crushing skin defeats, for example, Stephens-Johnson's syndrome and a Lyell's disease are registered; however, communication of their emergence with administration of drugs of Ambroxol is not proved. Mostly these cases can be explained with sharpness of a basic disease or the accompanying treatment. At development of above-mentioned syndromes it is recommended to stop as a precautionary measure treatment by Ambroxol and to ask immediately for medical care.

Management of transport and mechanisms. Special researches concerning influence of Ambroxol on ability to manage motor transport and mechanisms were not conducted.

Pregnancy and lactation. Ambroxol gets through a placental barrier. In pilot studies on animals direct or indirect adverse impact on pregnancy, embryonic, prenatal and post-natal development and on childbirth is not revealed. Clinical trials within 28 weeks of pregnancy did not find the evidence of negative influence of drug on a fruit. Nevertheless, it is necessary to observe usual precautionary measures when using drug at pregnancy. With care it is necessary to use drug during breastfeeding as Ambroxol is emitted with breast milk. Use of drug in II and III trimesters of pregnancy and at the nursing mothers perhaps only in that case when the estimated advantage for mother surpasses potential risk for a fruit.

Side effects:

Medicine is transferred usually well. In rare instances (<0,1%) from the alimentary system abdominal pains, nausea, vomiting, locks or diarrhea, and also development of allergic reactions in the form of skin rash, a small tortoiseshell, a Quincke's disease, suffocation, fervescence with a fever are possible.

Very seldom (<0,01%) increase in department of slime in a nasal cavity, the increased salivation, and also dryness mucous an oral cavity and airways is observed. In isolated cases – an acute anaphylaxis.

Interaction with other medicines:

Ambroxol increases penetration into a bronchial secret of amoxicillin, a tsefuroksim, erythromycin, doxycycline.

Drug is compatible to the drugs which are slowing down patrimonial activity.

It is not necessary to apply in a combination with antibechics (for example, containing codeine) as it complicates an otkhozhdeniye of the liquefied phlegm from bronchial tubes and its accumulation in them against the background of suppression of a tussive reflex.

Contraindications:

- I trimester of pregnancy;
- hypersensitivity to Ambroxol or other components of drug;
-  stomach ulcer and 12-perstny gut;
- age of children up to 6 years (because of the high content of active ingredient in a tablet of 30 mg). To children up to 6 years appoint Ambroxol drugs in a liquid form.

With care it is necessary to appoint drug in II and III trimesters of pregnancy, in the period of a lactation (breastfeeding), to patients with a renal and/or liver failure.

Overdose:

The expressed overdose symptoms at the person are not described. It was reported about the arising short-term nervous irritability and diarrhea. Ambroxol was well transferred at its reception inside to 25 mg/kg/days. Possible symptoms (judging by preclinical trials): the increased salivation, nausea, vomiting, diarrhea, dyspepsia and hypotension.

Treatment: Symptomatic therapy. Calling of artificial vomiting and a gastric lavage after reception are carried out to the first 1-2 h only in cases of extreme overdose.

Storage conditions:

To store in the place protected from light at a temperature not above +25 °C. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

Without recipe

Packaging:

Tablets of 30 mg in a blister strip packaging No. 10х2, No. 10х5 and in banks No. 20, No. 50. Together with a leaf insert two or five blister strip packagings or bank are located in a pack from a cardboard.