Ambroxol - instructions for use, dose, side effects, contraindications

Excipients: sorbitol liquid (non-crystallisable) - 1750.0 mg; glycerol (glycerol) - 637.5 mg; flavoring "Forest berries R3712-1" 11.0 mg; Hyethellosis (hydroxyethylcellulose) - 10.0 mg; benzoic acid 8.5 mg; acesulfame potassium - 5.0 mg; aroma "Vanilla with natural extract RX15460 "- 3.0 mg, purified water - up to 5.0 ml.

Description:

Transparent colorless or with a yellowish brown tint slightly viscous liquid with a characteristic odor.

Pharmacotherapeutic group:Expectorant mucolytic agent

ATX: & nbsp

R.05.C.B.06 Ambroxol

Pharmacodynamics:Ambroxol has secretory, secretory and expectorant action: it stimulates serous cells of the glands of the mucous membrane of the bronchi, increases the content of mucous secretion and the release of surfactant in the alveoli and bronchi; normalizes the disturbed ratio of serous and mucous components of sputum. Activates hydrolyzing enzymes and enhances the release of lysosomes from Clara cells, reducing the viscosity of phlegm. Increases the motor activity of the cilia of the ciliated epithelium. Strengthens the current and transport of mucus (mucociliary clearance). Strengthening mucociliary clearance improves sputum discharge and facilitates coughing.

Pharmacokinetics:

Suction

Ambroxol is characterized by rapid and almost complete absorption from the gastrointestinal tract with a linear dose dependence in the therapeutic concentration range. The maximum concentration in the blood plasma (C_m_Oh) with oral administration is achieved after 1-2.5 hours.

Distribution

The volume of distribution is 552 liters. In the therapeutic concentration range, binding to plasma proteins is about 90%. Bioavailability is 70-80%.Penetrates through the blood-brain barrier, placental barrier, excreted in breast milk. Ambroxol transfer from blood to tissue when taken orally occurs quickly. The highest concentrations of the active component of the drug are observed in the lungs.

Metabolism

Approximately 30% of the dose is exposed to the effect of "primary transmission" through the liver. Studies on microsomes of the human liver showed that the isoenzyme CYP3A4 is the predominant isoenzyme responsible for the metabolism of ambroxol to dibromoanthranilic acid. The rest of the ambroxol is metabolized in the liver, mainly with the formation of glucuronic conjugates and by partial cleavage to dibromantranilic acid (approximately 10% of the administered dose), as well as a small number of additional metabolites.

Excretion

The terminal half-life of ambroxol is 10 hours. The total half-life of ambroxol and its metabolites is about 22 hours. The total clearance is within 660 ml / min. It is excreted by the kidneys: 90% in the form of metabolites, about 10% - in unchanged form.

Pharmacokinetics in specific patient groups

Patients with impaired renal function

If violations of the function of the kidneys are severe (creatinine clearance less than 30 ml / min), accumulation of metabolites of ambroxol is possible.

Due to the high degree of binding to blood plasma proteins and a significant volume of distribution, as well as a slow redistribution from tissues to the blood, effective elimination of ambroxol by dialysis or forced diuresis is unlikely.

Patients with hepatic impairment

With severe hepatic failure, ambroxol clearance is reduced by 20-40%.

Age, sex

There is no clinically significant effect of age and sex on the pharmacokinetics of ambroxol, so there is no reason for choosing a dose for these symptoms.

Indications:

Acute and chronic diseases of the respiratory tract with the release of viscous sputum:

- acute and chronic bronchitis;

- pneumonia;

- chronic obstructive pulmonary disease;

- bronchial asthma with difficulty in sputum discharge;

- bronchiectatic disease.

Contraindications:

- Hypersensitivity to ambroxol or other components of the drug;

- pregnancy (I trimester);

- the period of breastfeeding;

- intolerance to fructose (the drug contains sorbitol).

Carefully:

- Disturbance of motor function of bronchi and increased sputum formation (with the syndrome of immobile cilia);

- decreased cough reflex or sputum retention;

- peptic ulcer of stomach and duodenum during exacerbation;

- pregnancy (II and III trimesters);

- kidney failure;

- hepatic failure of a severe degree.

Patients with impaired renal function or severe liver disease should take the drug Ambroxol with extreme caution, observing large intervals between doses of the drug or taking the drug at a lower dose (half the recommended dose for adults).

Pregnancy and lactation:

Pregnancy

Ambroxol penetrates the placental barrier.

Preclinical studies showed no direct or indirect adverse effects on pregnancy, fetal / fetal, postnatal development, and on generic activities.

The extensive clinical experience of the use of ambroxol after 28 weeks of pregnancy did not reveal evidence of a negative effect on the fetus.

Nevertheless, it is necessary to observe the usual precautions when using medicines during pregnancy.Application of the drug Ambroxol in the first trimester of pregnancy is contraindicated. In the II and III trimesters of pregnancy, the drug can be used only if the potential benefit to the mother exceeds the potential risk to the fetus.

Breastfeeding period

Ambroxol can be excreted in breast milk. Despite the fact that undesirable effects in children receiving breastfeeding were not observed, if it is necessary to use the drug, breastfeeding should be stopped. Fertility

Preclinical studies of ambroxol showed no adverse effects on fertility.

Dosing and Administration:

Inside. A drug Ambroxol can be used regardless of food intake. The mucolytic effect of the drug is manifested when taking a large amount of fluid, so during treatment is recommended a plentiful drink. The drug should not be taken immediately before bedtime.

In 5 ml of syrup contains 15 mg of ambroxol.

Adults and children over 12 years of age: during the first 2-3 days take 10 ml of syrup 3 times a day, then the dose should be reduced to 10 ml of syrup 2 times a day.

Children from 6 to 12 years old: 5 ml of syrup 2-3 times a day.

Children from 2 to 6 years old: 2.5 ml of syrup 3 times a day.

Children under 2 years: 2.5 ml of syrup 2 times a day.

The maximum daily intake for adults is 120 mg ambroxol; the maximum daily dose for children from 6 to 12 years is 45 mg ambroxol, for children from 2 to 6 years - 22.5 mg ambroxol, for children under 2 years - 15 mg ambroxol.

The duration of treatment is selected individually, depending on the course of the disease. If the symptoms persist for 4-5 days after the start of the drug is recommended to consult a doctor.

Side effects:

Classification of the incidence of adverse events according to

World Health Organization (WHO):

very often ≥ 1/10;

often from ≥ 1/100 to <1/10;

infrequently from ≥ 1/1000 to <1/100;

rarely from ≥ 1/10000 to <1/1000;

very rarely <1/10000, including individual messages;

the frequency is unknown - it is not possible to establish the frequency of occurrence from the available data.

Gastrointestinal disorders: often - nausea; infrequently - dyspepsia, pain in the upper abdomen, vomiting, diarrhea, heartburn; frequency unknown - decreased sensitivity in the oral cavity and pharynx, dryness the mucous membrane of the mouth and pharynx.

Immune system disorders: rarely - skin rash, hives; frequency unknown - anaphylactic reactions (including anaphylactic shock), Stevens-Johnson syndrome, Lyell syndrome, hypersensitivity reactions, skin itching, angioedema, acute generalized exanthematous pustulosis.

Impaired nervous system: frequency is unknown - dysgeusia (a violation of taste sensations).

Other: rarely - adynamia, fever.

Overdose:

Symptoms

Specific symptoms of an overdose of ambroxol in humans are not described.

There are reports of accidental overdose and / or medical error, which resulted in symptoms of known side effects of ambroxol: nausea, dyspepsia, vomiting, diarrhea, abdominal pain. In this case, the need for symptomatic therapy.

Measures to help with overdose

Artificial vomiting, gastric lavage in the first 1-2 hours after taking the drug, symptomatic therapy.

Interaction:

When used with antitussive drugs, it may be difficult for sputum to escape as a result of suppressing the cough reflex.

With simultaneous use with amoxicillin, cefuroxime, erythromycin, doxycycline ambroxol increases their absorption into the bronchial secret.

No clinically relevant adverse interactions with other drugs have been reported.

Special instructions:

A drug Ambroxol should not be used in conjunction with antitussive drugs, which can inhibit cough reflex.

A drug Ambroxol should be used with caution in patients with a weakened cough reflex or disturbed mucociliary transport because of the possibility of sputum congestion.

Patients taking the drug Ambroxol, do not recommend performing respiratory gymnastics; In seriously ill patients, aspiration of diluted sputum should be performed.

In patients with bronchial asthma ambroxol can strengthen cough.

Do not take the drug immediately before going to bed.

There are isolated reports of severe skin lesions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis, coinciding with the appointment of expectorants such as ambroxol. In most cases, they can be explained by the severity of the underlying disease and / or concomitant therapy.In patients with Stevens-Johnson syndrome or toxic epidermal necrolysis in the early phase may appear temperature, pain in the body, rhinitis, cough and sore throat. With symptomatic treatment, it is possible to erroneously designate mucolytic agents, such as ambroxol. When new lesions of the skin and mucous membranes appear, it is recommended to stop the drug treatment Ambroxol and seek medical help immediately.

For violations of kidney function, the drug Ambroxol should be used only on the advice of a doctor.

In 5 ml of the drug Ambroxol contains 1750.0 mg of sorbitol. Patients with a rare hereditary intolerance to fructose should not take the drug.

Effect on the ability to drive transp. cf. and fur:

There is no information about the adverse effects on the ability to drive vehicles and service mechanisms that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Syrup 15 mg / 5 ml.

Packaging:

100 ml or 200 ml in bottles made of polyethylene terephthalate or dark glass with a screw cap, with the first opening control of high-density polyethylene or polypropylene.

Each bottle together with a measuring cup of polypropylene and instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004496

Date of registration:19.10.2017

Expiration Date:19.10.2022

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp21.11.2017

Illustrated instructions

Instructions

Ambroxol (Ambroxol)