Ambroxol hydrochloride

General characteristics. Structure:

International and chemical names: ambroxol; trans-4-[(2-amino-3,5-dibrombenzil) amines] cyclohexanol hydrochloride;
main physical and chemical properties: tablets of color, white or white with a yellowish shade, a round form, with a flat surface and with a facet;
structure: 1 tablet contains 30 mg of Ambroxol of a hydrochloride;
excipients: lactose, коповидон, aerosil, calcium stearate, кросповидон.

Pharmacological properties:

Pharmacodynamics. Ambroxol a hydrochloride – synthetic sekretolitichesky and sekretomotorny means of group of benzylamines. Drug has a promoting effect of rather serous cells of glands of a mucous membrane of bronchial tubes that leads to increase in secretion of slime and change of a ratio of serous and mucous components of a phlegm. Simultaneous activation of hydrolytic enzymes and increase in a physical activity of a ciliary epithelium of bronchial tubes causes department of a pathological secret from walls of bronchial tubes and improves its removal from respiratory tracts, recovering drainage function of small bronchial tubes and bronchioles. Drug increases the content of surfactant in lungs, and also prevents its destruction in pnevmotsita. It leads to normalization of rheological indicators of a phlegm, reduces its viscosity and adhesive properties. Ambroxol the hydrochloride directly stimulates activity of a ciliary epithelium of bronchial tubes, prevents its adhesion and improves mukotsiliarny evacuation of a phlegm. Drug reduces hyperreactivity of muscles of bronchial tubes of patients with bronchial asthma. Has poorly expressed antibechic action. Ambroxol has antiinflammatory effect, shows antioxidant properties, stimulates local immunity.

Pharmacokinetics. At oral administration of Ambroxol the hydrochloride is quickly and completely soaked up in digestive tract. Well gets into tissues of lungs. The maximum concentration of Ambroxol in a blood plasma is observed in 1/2–3 hours after oral administration. Therapeutic action develops in 30 minutes and lasts from 6 to 12 hours (depending on the accepted dose). An elimination half-life – 10–12 hours. Cumulation of drug is not observed. Extent of linkng with proteins of a blood plasma – about 90%. After intake quickly gets into all bodies and fabrics, but the greatest concentration of drug is noted in tissues of lungs. Well gets through GEB, a placental barrier, cosecretes with breast milk. Metabolism of Ambroxol happens in a liver by conjugation to formation of inactive metabolites (glucuronides and dibromoantranilovy acid). 90% of drug are removed with urine.

Indications to use:

The acute and chronic respiratory diseases which are followed by the complicated elimination of a viscous secret (acute and chronic bronchitis, a bronchoectatic disease, tracheitis, laryngitis, pharyngitis). Bronchial asthma with a slow otkhozhdeniye of a phlegm; pneumonia, mucoviscidosis of lungs; prevention and treatment of complications after extensive lung operations. It is applied by preparation for a bronkhoskopiya and after the conducted research.

Route of administration and doses:

Adults and children from 12 years accept Ambroxol a hydrochloride on 1 tablet 2 times a day, if necessary – 3 times a day. At an exacerbation of chronic diseases the single dose can be raised to 60 mg 2 times a day. To children from 5 to 12 years usually appoint 15 mg (½ tablets) 2–3 in days, from 2 to 5 years of-7,5 mg (¼ tablets) 3 times a day. Drug is accepted in time or after food, washing down with a small amount of water. The therapeutic dose for children makes 1,2–1,6 mg/kg a day in 2–3 receptions.  The course of treatment makes 4-14 days.

Features of use:

Drug cosecretes with breast milk, but hydrochloride Ambroxol use in therapeutic doses does not make collateral impact on babies.

Side effects:

Ambroxol is well transferred, but at prolonged use and in high doses drug can cause heartburn, dyspepsia, nausea, vomiting; seldom – allergic reactions in the form of skin rashes, a small tortoiseshell, a Quincke's disease. Hypersalivation, increase in secretion mucous a nose, a hyperthermia, a dysuria are possible.

Interaction with other medicines:

It is not recommended to appoint Ambroxol a hydrochloride along with antibechic drugs which oppress removal of a phlegm. Drug raises a therapeutic effectiveness of doxycycline, a tsefuroksim and amoxicillin. Ambroxol the hydrochloride increases concentration of rifampicin in lungs. Use of drug with cardiac glycosides, diuretics is possible, the hydrochloride Ambroxol combination with theophylline therapeutic is reasonable.

Contraindications:

The first trimester of pregnancy, peptic ulcer of a stomach and 12-perstny gut, hypersensitivity to Ambroxol and other components of drug.

Overdose:

Cases of overdose are not described, but digestion disturbances, discomfort or pains in epigastric area, feeling of overflow of a stomach, nausea, vomiting can appear. In other cases of overdose it is necessary to cancel drug and to carry out symptomatic therapy.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. A period of validity - 2 years.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in blister strip packagings, on 2 planimetric packagings in a pack.