Ambroxyl

Ambroxol hydrochloride.

Tablet: Each tablet contains: Ambroxol Hydrochloride 30 mg.
Syrup: Each 5 mL (1 teaspoonful) contains: Ambroxol hydrochloride 15 mg.
Excipients/Inactive Ingredients: Tablet: Lactose starch paste, starch filler, scalum starch glycolate, magnesium stearate, FD&C Red Lake AC # 3 (Erythrosine), deionized water.
Syrup: Sucrose, Sodium Benzoate, Citric Acid, Sodium Citrate, Sorbitol Solution, Pineapple flavor, Strawberry flavor, Polyoxyl 40 Hydrogenated Castor Oil, Sodium Saccharin, Refined Solvent, Deionized Water.

Pharmacology: Ambroxol Hydrochloride is a derivative of the mucolytic, bromhexine which has been found to possess secretolytic and mucokinetic properties. It acts by increasing the production of serum concentrations of the bronchial mucus-secreting glands in the respiratory tract. Through its pulmonary surfactant stimulating activity, Ambroxol Hydrochloride accelerates mucus transport, promoting expulsion of thick, tenacious secretions from the respiratory tract. During treatment with Ambroxol Hydrochloride, chronically inflamed bronchial mucosa tends to return to normal. The patients cough and sputum volumes are reduced; expectoration is facilitated; and breathing is eased considerably.
The good tolerability of Ambroxol Hydrochloride permits its long term use.
Pharmacokinetics: Absorption: Absorption of all immediate release oral forms of Ambroxol hydrochloride is rapid and complete, with dose linearity in the therapeutic range. Maximum plasma levels are reached within 1 to 2.5 hours following oral administration of the immediate-release formulation and after a median of 6.5 hours of the slow-release formulation. The absolute bioavailability after oral administration of 30 mg tablet of Ambroxol was found to be 79%.
Distribution: In the therapeutic range, plasma-protein binding was found to be approximately 90%. Distribution of Ambroxol hydrochloride from blood to tissue is rapid and pronounced, with the highest of the active substance found in the lungs. The volume of distribution following oral administration was estimated to be 552 L.
Metabolism and Elimination: About 30% of an orally administered dose is eliminated via first-pass metabolism. Studies in human liver microsomes have shown that CYP3A4 is responsible for the metabolism of Ambroxol. Ambroxol Hydrochloride is metabolized primarily in the liver by glucuronidation and some cleavage to dibromoanthranilic acid (approximately 10% of dose) aside from some minor metabolites. Ambroxol hydrochloride is eliminated with a terminal half-life of approximately 10 hours. Total clearance is in the range of 660 mL/min, with renal clearance accounting for approximately 83% of the total clearance.
Special Populations: In patients with hepatic dysfunction, elimination of Ambroxol hydrochloride is reduced, resulting in approximately 1.3 to 2-fold higher plasma levels. Due to the high therapeutic range of Ambroxol Hydrochloride, dose adjustments are not necessary.
Others: Age and gender were not found to affect the pharmacokinetics of Ambroxol Hydrochloride to a clinically relevant extent and thus there in no necessity for adjustment of dose regimens. Food was not found to influence the bioavailability of Ambroxol hydrochloride.

Acute and chronic respiratory tract disorders associated with abnormal secretion in bronchitis, bronchial asthma, and bronchiectasis. Ease elimination of phlegm during nasopharyngeal inflammation.

Tablet: Daily dose of 30 mg to 120 mg in 2 to 3 divided doses by mouth or as prescribed by the physician.
Syrup: Adult and children over 10 years: 10 mL (2 teaspoonfuls) three times a day.
Children below 10 years: 6-10 years old: 5 mL (1 teaspoonful) three times a day or as prescribed by the physician.

No specific overdosage symptoms have been reported in man to date. Based on accidental overdose and/or medication error reports, the observed symptoms are consistent with the known side effects of Ambroxol at recommended doses and may need symptomatic treatment.

Ambroxol should not be used in patients known to be hypersensitive to Ambroxol hydrochloride or other components of the formulation. In case of rare hereditary conditions that may be incompatible with an excipient of the product, the use of the product is contraindicated.

Should be used with care in patients with history of peptic ulceration.

Use in Pregnancy: Ambroxol hydrochloride crosses the placental barrier. Nonclinical studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development.
Tablet: Extensive clinical experience after the 28th week of pregnancy has shown no evidence of harmful effects on the fetus. Nonetheless, the usual precautions regarding the use of drugs during pregnancy should be observed. Especially during the first trimester, the use of Ambroxol is not recommended.
Use in Lactation: Ambroxol hydrochloride is excreted in breast milk. Although unfavorable effects on breastfed infants would not be expected, Ambroxol is not recommended for use in nursing mothers.

Gastrointestinal Disorders and Respiratory, Mediastinal and Thoracic Disorders: Dyspepsia, nausea, vomiting, diarrhea and abdominal pain, oral and pharyngeal hypoesthesia, dry mouth and dry throat.
Nervous System Disorders: Dysgeusia (e.g. changed taste).
Immune System Disorders, Skin and Subcutaneous Tissue Disorders: Anaphylactic reactions including anaphylactic shock, angioedema, rash, urticaria, pruritus and other hypersensitivity.

No report of drug interaction. Ambroxol hydrochloride can be administered with other drugs, particularly the standard medication of bronchitis syndrome such as corticosteroids, bronchospasmolytics, diuretics and antibiotics.

Store at temperatures not exceeding 30°C.

Cough & Cold Preparations

R05CB06 - ambroxol ; Belongs to the class of mucolytics. Used in the treatment of wet cough.

Non-Rx