Ambroxol
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Clinical Pharmacology
Lasolvan - secretomotor, secretolytic, expectorant.
Pharmacodynamics
Stimulates the serous cells of the glands of the mucous membrane of the bronchi, increases the content of mucous secretions and the release of surfactants (surfactant) in the alveoli and bronchi; normalizes the disturbed ratio of serous and mucous components of sputum. Activating hydrolytic enzymes and enhancing the release of lysosomes from Clara cells, reduces the viscosity of sputum. Increases the motor activity of cilia of the ciliated epithelium, increases mucociliary transport of sputum.
After ingestion, the action occurs after 30 minutes and lasts for 6–12 hours.
Pharmacokinetics
Absorption - high, Cmax achieved in 2 hours (for pills, syrup), for solution for ingestion and inhalation - 0.5–3 hours; binding to plasma proteins - 80% (for pills, syrup), for oral solution and inhalation - 90%. Passes through the BBB, placental barrier, excreted in breast milk. The solution for ingestion and inhalation is rapidly distributed in the tissues, the highest concentration is achieved in the lungs.
Metabolized in the liver, forms dibromantranilic acid and glucuronic conjugates. Excreted by the kidneys - 90% in the form of water-soluble metabolites, 5% - unchanged. About 30% of the dose after oral administration is eliminated by means of the primary metabolism. T1/2 - 1.3 hours, for a solution for ingestion and inhalation - 7–12 hours. There is no cumulative effect. The elimination half-life increases with severe chronic renal failure, but does not change with abnormal liver function.
Indications
Acute and chronic diseases of the respiratory tract, accompanied by the release of viscous sputum:
- acute and chronic bronchitis;
- pneumonia;
- COPD;
- bronchial asthma with sputum obstruction;
- bronchiectasis.
Composition
2 ml of solution contains:
Active substance: ambroxol hydrochloride 15 mg;
Excipients: citric acid; disodium hydrogen phosphate dihydrate; sodium chloride; benzalkonium chloride; purified water.
Ambroxol is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Lasolvan | Boehringer Ingelheim | Austria | solution |
Ambroxol | Obnovlenie PFK | Russia | pills |
Ambroxol | solution | ||
Ambroxol | Canonpharma | Russia | pills |
Orvis Broncho | solution | ||
Flavamed | Berlin-Chemie AG | Germany | solution |
Flavamed | Berlin-Chemie AG | Germany | effervescent pills |
Lasolvan | Boehringer Ingelheim | Austria | capsules |
Lasolvan | Boehringer Ingelheim | Austria | syrup |
Lasolvan | Boehringer Ingelheim | Austria | pills |
Ambrohexal | Sandoz | Switzerland | syrup |
Ambrobene | Teva | Israel | solution |
Ambrobene | Teva | Israel | pills |
Ambrobene | Teva | Israel | syrup |
Ambrohexal | Sandoz | Switzerland | pills |
Ambroxol | Ecolab | Russia | syrup |
Ambrosan | PRO.MED.CS Praha a.s | Czech | pills |
Halixol | Egis | Hungary | pills |
Halixol | Egis | Hungary | syrup |
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Dosage and Administration
Inside and inhalation.
For oral use. in the form of drops (1 ml = 25 drops), while eating, adding to tea, fruit juice, milk or water. Adults at the beginning of treatment - 4 ml 3 times a day, children over 6 years old - 2 ml (50 drops) 2-3 times a day, children from 2 to 6 years old - 1 ml (25 drops) 3 times a day , children under 2 years old - 1 ml (25 drops) 2 times a day.
InhalationAdults and children over 6 years old - 1-2 inhalations of 2-3 ml of solution daily, children under 6 years of age - 1-2 inhalations of 2 ml of solution daily.
Inhalation solution can be applied using any modern equipment for inhalation (except steam inhalers). The drug is mixed with saline, it can be diluted in a 1: 1 ratio to achieve optimal air moistening in the respirator. Since inhalation therapy, a deep breath can provoke cough tremors, inhalation should be carried out in normal breathing mode. Before inhalation, it is usually recommended to warm the inhalation solution to body temperature. Patients with bronchial asthma are advised to inhale after taking bronchodilators.
Adverse reactions
Allergic reactions: skin rash, urticaria, angioedema, in some cases - allergic contact dermatitis. Cases of acute severe reactions of the anaphylactic type (anaphylactic shock) have been extremely rarely reported.
Contraindications
With long-term use in high doses.- heartburn, gastralgia, nausea, vomiting.
Hypersensitivity; pregnancy (I term).
Carefully:
- II – III trimester of pregnancy;
- lactation period;
- renal and / or liver failure.
Drug interactions
Compatible with drugs that inhibit generic activity.
Combined use with antitussive drugs leads to difficulty in sputum discharge on the background of cough reduction.
Increases bronchial secretion in amoxicillin, cefuroxime, erythromycin and doxycycline.
Pregnancy and Lactation
Preclinical trials and extensive clinical experience have not revealed undesirable effects of drug treatment during pregnancy. Nevertheless, it is necessary to follow the general rules of prescribing drugs, especially in the first trimester. Lasolvan® penetrates into breast milk, but in therapeutic doses does not adversely affect the child.
If necessary, use Lasolvana® in the II – III trimesters of pregnancy, the potential therapy for the mother and the possible risk to the fetus should be evaluated
Special instructions
It should not be combined with antitussive agents that impede the excretion of sputum.
The solution for oral administration and inhalation contains benzalkonium chloride. In patients with hyperactivity of the respiratory tract, this preservative may cause bronchospasm during inhalation.
Overdosage
Symptoms: possible - nausea, vomiting, diarrhea, dyspepsia, gastralgia.
Treatment: induction of vomiting, gastric lavage in the first 1-2 hours after taking the drug; reception of fat-containing products, symptomatic therapy.
- Brand name: Lasolvan
- Active ingredient: Ambroxol
- Dosage form: Solution for oral administration and inhalation
- Manufacturer: Boehringer Ingelheim
- Country of Origin: Austria
Studies and clinical trials of Ambroxol (Click to expand)
- Changes in pulmonary function in preterm infants recovering from RDS following early treatment with ambroxol: Results of a randomized trial
- Evaluation of the effects of ambroxol on the ofloxacin concentrations in bronchial tissues in COPD patients with infectious exacerbation
- Rapid and sensitive liquid chromatography tandem mass spectrometry method for the quantification of ambroxol in human plasma
- ChemInform Abstract: Synthesis of Chiral and Achiral Analogues of Ambroxol via Palladium-Catalyzed Reactions.
- Voltammetric Oxidation of Ambroxol and Application to Its Determination in Pharmaceuticals and in Drug Dissolution Studies
- Selective quantification of ambroxol in human plasma by HPLC
- Synthesis of labeled ambroxol and its major metabolites
- Solid-state chemistry of ambroxol theophylline-7-acetate
- Pulmonary selectivity and local pharmacokinetics of ambroxol hydrochloride dry powder inhalation in rat
- Rapid and sensitive determination of ambroxol in human plasma and urine by high-performance liquid chromatography
- High-performance liquid chromatographic determination of ambroxol in human plasma
- Oral sustained delivery of ambroxol from in situ-gelling pectin formulations
- The effect of taste masking agents on in situ gelling pectin formulations for oral sustained delivery of paracetamol and ambroxol
- High-performance liquid chromatographic determination of ambroxol in pharmaceuticals
- Characterization of bromhexine and ambroxol in equine urine: Effect of furosemide on identification and confirmation
- Quantitative determination of ambroxol hydrochloride in tablets
- Lung injury induced by paraquat, hyperoxia and cobalt chloride: Effects of ambroxol
- Determination of ambroxol in human plasma by high performance liquid chromatography–electrospray ionization mass spectrometry (HPLC–MS/ESI)
- Simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation by liquid chromatography
- Nondestructive determination of the ambroxol content in tablets by Raman spectroscopy
- Determination of ambroxol hydrochloride, methylparaben and benzoic acid in pharmaceutical preparations based on sequential injection technique coupled with monolithic column
- Development and validation of a reversed-phase HPLC method for simultaneous estimation of ambroxol hydrochloride and azithromycin in tablet dosage form
- FT-Raman quantitative determination of ambroxol in tablets
- HPLC and chemometrics-assisted UV-spectroscopy methods for the simultaneous determination of ambroxol and doxycycline in capsule