Actions of Mukinol in details
Pharmacology: Preclinically, Mukinol hydrochloride, the active ingredient of Mukinol, has been shown to increase respiratory tract secretion. It enhances pulmonary surfactant production and stimulates ciliary activity. These actions result in improved mucus flow and transport (mucociliary clearance). Improvement of mucociliary clearance has been shown in clinical pharmacologic studies. Enhancement of fluid secretion and mucociliary clearance facilitates expectoration, and eases cough.
In patients suffering from COPD, long-term treatment (6 months) with Mukinol (Mukinol Retard Capsule 75 mg) resulted in a significant reduction of exacerbations that became evident after 2 months of treatment. Patients in the Mukinol treatment group lost significantly fewer days through illness and had fewer days when they needed antibiotic therapy. Treatment with Mukinol Retard also induced a statistically significant improvement of symptoms (difficulty of expectoration, cough, dyspnea, auscultatory signs) compared with placebo.
A local anaesthetic effect of Mukinol hydrochloride has been observed in the rabbit eye model which may be explained by the sodium-channel blocking properties. It was shown in vitro that Mukinol hydrochloride blocks cloned neuronal sodium channels; binding was reversible and concentration-dependent.
Cytokine release from blood but also tissue-bound mononuclear and polymorphonuclear cells was found to be significantly reduced by Mukinol hydrochloride in vitro.
In clinical studies in patients with sore throat, pharyngeal pain and redness was significantly reduced.
Following the administration of Mukinol, antibiotic concentrations (amoxicilline, cefuroxime, erythromycin) in bronchopulmonary secretions and in the sputum are increased.
Pharmacokinetics: Absorption: Absorption of all immediate release oral forms of Mukinol 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 a 30 mg tablet was found to be 79%. The slow-release capsule showed a relative availability of 95% (dose-normalized) in comparison to a daily dose of 60 mg (30 mg twice daily) administered as immediate-release tablet.
Distribution: In the therapeutic range, plasma protein-binding was found to be approximately 90%. Distribution of Mukinol hydrochloride from blood to tissue is rapid and pronounced, with the highest concentration 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 Mukinol. Mukinol hydrochloride is metabolized primarily in the liver by glucuronidation and some cleavage to dibromanthranilic acid (approximately 10% of dose) aside from some minor metabolites.
Mukinol hydrochloride is eliminated with a terminal elimination 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 Mukinol hydrochloride is reduced, resulting in approximately 1.3 to 2-fold higher plasma levels.
Due to the high therapeutic range of Mukinol hydrochloride, dose adjustments are not necessary.
Others: Age and gender were not found to affect the pharmacokinetics of Mukinol hydrochloride to a clinically relevant extent and thus there is no necessity for adjustment of dosage regimens.
Food was not found to influence the bioavailability of Mukinol hydrochloride.
Mukinol administration
Should be taken with food.
Mukinol pharmacology
When Max Pidek Pharmaceuticals administered orally amoxicillin rapidly and completely absorbed from the gastrointestinal tract and is not destroyed in the acidic environment of the stomach. Cmax of amoxicillin in the blood plasma is reached after 1-2 h. When increasing doses of 2 times the concentration also increased by 2 times. In the presence of food in the stomach does not reduce the overall removals. Similar concentrations of amoxicillin reached in the blood when administered orally, IV and IM.
The binding of amoxicillin to plasma proteins is about 20%.
Widely distributed in tissues and body fluids. Reported high concentrations of amoxicillin in the liver.
T1/2 from the plasma is 1-1.5 h. About 60% of the dose adopted by mouth, is excreted unchanged in the urine by glomerular filtration and tubular secretion, with a dose of 250 mg of amoxicillin concentration in urine exceeds 300 micrograms / ml. A number of amoxicillin is determined in feces.
T1/2 for Newborns and the elderly can be longer.
In renal insufficiency T1/2 may be 7-20 hours.
In small quantities amoxicillin penetrates through BBB in inflammation of the pia mater.
amoxicillin is removed by hemodialysis.
References
- EPA DSStox. "Ambroxol: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
