Rhinological agents (chemically defined), α-sympathomimetic. The active ingredient of Iliadin 0.05% Decongestant Nasal Drops has a sympathomimetic, vasoconstrictive, and thus a decongestant effect on the mucous membranes.
Adult nasal drops: The effect of Iliadin 0.05% Decongestant Nasal Drops sets in within few seconds. In a clinical study, the median onset was found to be 25 seconds. The effect persists for up to 12 hours.
Children nasal drops: The effect of Iliadin 0.025% Decongestant Nasal Drops sets in within a few minutes. The effect persists for up to 12 hours.
Infant nasal drops: Pharmacology: Pharmacodynamics: Substance or indication group Rhinological agents (chemically defined), a-sympathomimetic.
Oxymetazoline has a sympathomimetic, vasoconstrictive and therefore a decongestant effect on mucous membranes. The application of Iliadin 0.01% Decongestant Nasal Drops into the nostrils decongests the inflamed nasal mucosa and causes excessive secretion to stop. The patient is able to breathe freely through the nose again. Also, decongestion of the nasal mucosa opens and dilates the efferent ducts of the paranasal sinuses and clears the auditory tube. This facilitates the discharge of secretion and combats bacterial invasion.
Pharmacokinetics: Investigations with radiolabelled oxymetazoline in healthy volunteers revealed that this intranasally applied rhinological agent has no systemic effect. Oral administration (double-blind studies) showed first unspecific ECG changes only after administration of 1.8mg oxymetazoline - this is equivalent to 3.6ml of a 0.05% solution. Neither blood pressure nor pulse rate were affected by the intake of this quantity of active substance. After intranasal application of doses higher than recommended the absorbed quantity can suffice to trigger systemic effects in the cardiovascular system. In rare cases the quantity absorbed after intranasal application can suffice to produce systemic effects in the central nervous system (cf. adverse reactions).
The half-life of terminal elimination after nasal application is 35 hours in humans. 2.1% is excreted via the kidneys and about 1.1% via the faeces. No information is available on the distribution of oxymetazoline in humans.
Iliadin 0.01% Decongestant Nasal Drops sets in within a few minutes. The effect persists for up to 12 hours.
Toxicology: Preclinical safety data: Acute toxicity: The LD50 of oxymetazoline hydrochloride was established as 0.9mg/kg (i.v.) and 1.3mg/kg (oral) in rats. Mice showed an LD50 of 9.2mg/kg (i.v.) and 26mg/kg (oral). Symptoms of acute intoxication included piloerection, exophthalmos, mydriasis and nosebleeds. At higher doses pallor, mild cyanosis and reduced motility were observed. In terminal conditions asphyctic convulsions occurred.
Subacute toxicity: 0.6ml of an 0.05% solution (0.3mg oxymetazoline hydrochloride) - instilled into each nostril 3 times daily for 13 weeks - was well tolerated by dogs. No toxic effects, systemically or in the nasal mucosa, occurred. No significant changes in the ECG or in the eyes were observed. The doses investigated amounted to up to 60 times the dosage recommended for humans.
Chronic toxicity: Dogs received nasal doses of 0.06ml and 0.24ml of 0.05% oxymetazoline hydrochloride solution twice daily for 1 year. No toxic effects developed. The doses investigated amounted to up to three times the dosage recommended for humans.
Reproduction toxicology: Reproduction in rats: Subcutaneous administration of 0.08mg/kg and 0.24mg/kg oxymetazoline from the 6th and 15th postcoital day did not cause any somatic abnormalities in the offspring. A slight difference in the number of resorptions was not statistically significant. The doses investigated amounted to up to 25 times and 75 times, respectively, the dosage recommended for humans.
Mutagenic and tumorigenic potential: No data are available on mutagenesis and carcinogenesis.