Ambroxol Reneval, tablets 30 mg 50 pcs

Pharmacotherapeutic group: expectorant, mucolytic.

The ATC code: R05CB06

Pharmacological properties

Pharmacodynamics

Ambroxol is the active N-demethylated metabolite of bromhexine.

It has secretomotor, secretolytic and expectorant effects.

Stimulates bronchial glands, increases motor activity of the atomizing epithelium by influencing type 2 pneumocytes in the alveoli and Clara cells in the bronchioles, increases formation of endogenous surfactant – a surfactant that ensures gliding of bronchial secretion in the airway lumen. Ambroxol increases the proportion of the serous component in the bronchial secretion, improving its structure and contributing to reduction of viscosity and liquefaction of sputum; as a result, mucociliary transport is improved and expulsion of sputum from the bronchial tree is facilitated.

On average when taken orally, the action of the drug starts within 30 minutes; its duration of action is 6-12 hours, depending on the dose taken.

Pharmacokinetics

Absorption.After oral administration, ambroxol is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum concentration (C_max) in blood plasma is reached after 1-3 hours. Volume of distribution is 552 l. Absolute bioavailability of ambroxol in oral administration as a result of “primary passage” through the liver is reduced by approximately 1/3.

Distribution.The binding to plasma proteins is 80-90%. Ambroxol penetrates through the placental and blood-brain barrier, is excreted with breast milk.

Metabolism. Ambroxol is metabolized in the liver by conjugation to form pharmacologically inactive metabolites.

Elimation. The terminal blood plasma elimination half-life (T_1/2) is 7-12 hours. The total half-life of ambroxol and its metabolites is about 22 hours. Total clearance is within 660 ml/min. Excreted by the kidneys: 90% as metabolites (such as dibromoanthranilic acid, glucuronides), about 10% – unchanged. In severe renal impairment (creatinine clearance less than 30 ml/min) accumulation of ambroxol metabolites is possible; in severe hepatic failure ambroxol clearance is reduced by 20-40 %.

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

Indications

Disorders of sputum secretion and transport in acute and chronic respiratory diseases: acute and chronic bronchitis, pneumonia, chronic obstructive pulmonary disease, bronchial asthma, bronchiectatic disease.

Active ingredient

Ambroxol

Composition

Active substance: ambroxol hydrochloride – 30.0 mg; excipients: lactose monohydrate, corn starch, colloidal silicon dioxide (aerosil), magnesium stearate

How to take, the dosage

Orally, after meals, with enough fluids. Adults and children over 12 years of age: 30 mg (1 tablet) 3 times a day during the first 2-3 days, then the drug dose should be reduced to 1 tablet 2 times a day. Children of 6 to 12 years of age: 15 mg (1/2 tablet) 2 to 3 times a day. If symptoms of the disease persist for 4-5 days from the beginning of therapy, it is recommended to consult a physician.

Interaction

When concomitant use of ambroxol with anti-cough drugs, sputum may be difficult to excrete as a result of cough reflex suppression. When concomitant use with amoxicillin, cefuroxime, erythromycin, doxycycline, ambroxol increases their concentration in bronchial secretion.

Special Instructions

During treatment it is necessary to drink a lot of liquid (juices, tea, water), because this enhances the mucolytic effect of the drug.

Ambroxol should not be taken at the same time with anti-cough drugs that make it difficult to expectorate sputum.

Ambroxol should be taken with caution in patients with impaired cough reflex or impaired mucociliary transport because of the possibility of sputum accumulation.

Patients taking ambroxol should not be advised to perform breathing exercises; aspiration of dilute sputum should be performed in patients with severe disease.

In patients with bronchial asthma, ambroxol may increase coughing.

In patients with severe skin lesions – Stevens-Johnson syndrome or Lyell syndrome – fever, body pain, rhinitis, cough and sore throat may appear in the early phase. Mucolytic agents such as ambroxol may be mistakenly prescribed for symptomatic treatment. There have been isolated reports of Stevens-Johnson syndrome and Lyell’s syndrome coinciding with the administration of the drug; however, there is no causal link to the drug administration. If the above syndromes develop, it is recommended to discontinue treatment and seek medical attention immediately.

In case of impaired renal function, the drug should be used only on the recommendation of a physician.

Prevention for patients with diabetes mellitus: 1 tablet contains less than 0.01 bread units.

Influence on driving and operating ability

There have been no cases of the drug affecting driving and operating ability. There have been no studies on the effect of the drug on the ability to drive vehicles and to engage in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

Round flat cylindrical tablets, white or white with a yellowish tint, with a bevel and a rib.

Contraindications

Hypersensitivity to the components of the drug, hereditary galactose intolerance, lactase deficiency or glucose and galactose malabsorption syndrome, first trimester of pregnancy and breastfeeding period, children under 6 years of age.

With caution

Bronchial motility disorder and increased mucus secretion (e.g., in rare primary ciliary dyskinesia syndrome); renal failure and/or severe liver failure); gastric and duodenal ulcer, including history; II-III trimesters of pregnancy.

Side effects

Classification of the frequency of side effects according to the recommendations of the World Health Organization (WHO):

Very common > 1/10; common > 1/100 to < 1/10; infrequent > 1/1000 to < 1/100; rare > 1/10000 to < 1/1000; very rare < 1/10000, including individual reports; frequency unknown – the incidence cannot be determined from available data.

Allergic reactions:

frequency unknown – hypersensitivity reactions, anaphylactic reactions (including anaphylactic shock), angioedema.

In the digestive system:

often – nausea, decreased sensitivity in the mouth or pharynx; infrequent – dyspepsia, vomiting, diarrhea, abdominal pain; rarely – heartburn, dryness of the mucosa of the mouth and throat, constipation.

In the respiratory system:

rarely – dry mucous membrane of the respiratory tract, rhinorrhea (mucus discharge from the nose).

Side of the skin:

Rarely – skin rash, urticaria; frequency unknown – skin itching, Stevens-Johnson syndrome (erythema multiforme exudative), Lyell syndrome (toxic epidermal necrolysis), acute generalized exanthematous pustulosis.

Sense organs:

frequent – dysgeusia (taste disturbances).

Others:

Rarely – weakness, headache, dysuria (disorders of urination), hyperthermia, fever.

Overdose

Symptoms: nausea, vomiting, diarrhea, upper abdominal pain, heartburn, dyspepsia (indigestion). There are reports of the occurrence of transient anxiety. Significant decrease in blood pressure is possible in severe overdose. Treatment: artificial vomiting, gastric lavage during the first 1-2 hours after drug intake, intake of fat-containing products, symptomatic therapy. Due to the high degree of binding of ambroxol to plasma proteins and large volume of distribution, hemodialysis or forced diuresis is inexpedient.

Pregnancy use

Use of the drug in the first trimester of pregnancy and during breast-feeding is contraindicated. Administration of the drug in II-III trimesters of pregnancy is possible only after careful evaluation of the ratio of benefits from treatment and possible risks.

Similarities

Ambrohexal, Lazolvan, Halixol, Ambroxol, Ambrobene, Orvis Broncho, ORVIS, Lazolvan Max, Zvezdochka, Zvezdochka for colds