Xylometazoline

2 - ( (4 - ( 1,1-dimethylethyl ) -2,6- dimethylphenyl ) methyl) -4,5- dihydro -1H-imidazole

  • 526-36-3
  • 1218-35-5 ( xylometazoline · monohydrochloride )
  • R01AA07
  • R01AB06
  • S01GA03

Sympathomimetic

α1 -adrenoceptor agonist

Monohydrochloride

Risk

230 mg · kg -1 ( LD50, Rat, oral, hydrochloride)

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Xylometazoline is a chemical compound from the group of imidazole derivatives. It is used as a drug for decongestion of the nasal mucosa. As α -sympathomimetic it is an α1 -adrenoceptor agonist and causes contraction of smooth muscle. Thus, the locally situated blood vessels in the nose narrows ( vasoconstriction ) and the reduced blood flow can decongest mucous membranes. Xylometazoline therefore found in nasal sprays, nasal ointments and nasal drop application. It was first synthesized by CIBA AG Albrecht Hüni from Basel at the pharmaceutical company and patented in 1959. Patenting in Switzerland took place in 1961. Meanwhile, various xylometazolinhaltige runny nose sprays and drops each as a generic available.

Xylometazoline is pharmaceutic, but not a prescription in Germany. It has a similar mode of action, such as adrenaline and binds to the same receptors. After absorption through the nasal mucosa it unfolds first local effect on the α - receptors in the blood vessels of the nasal mucosa ( this causes the ebb ) and then also systemic effect. For this reason, it should not be used by patients with high blood pressure or other heart problems. In infants and young children, respiratory depression and coma are possible. A use in pregnancy is contraindicated.

Side effects

It can cause the following side effects:

  • Respiratory system - common ( 1-10 %): xylometazoline may cause ( burning, or dryness of the nasal mucosa ) that sensitive patient temporarily slight irritation symptoms. The drug may lead to increased mucosal swelling (reactive hyperemia) after the decay of its effect. Prolonged or frequent use and higher doses of xylometazoline lead to the development of tolerance and can result in the nose burning, or dryness of the mucous membrane as well as a reactive congestion rhinitis medicamentosa with ( drug sniffing ). This effect can occur even after 5 days of treatment and cause permanent mucosal damage with crust formation (rhinitis sicca) after continued use.
  • Nervous system - Rare ( 0.01-0.1 % ): headache, insomnia - even fatigue.
  • Heart and circulation: Local use in the nose it occasionally ( 0.1-1 %) to systemic side effects such as palpitations, pulse rate and blood pressure increase.
  • Effects on ability to drive and use machines: are systemic effects affecting the cardiovascular system and central nervous system side effects can not be excluded With prolonged use or high doses of xylometazoline. In these cases, may be impaired ability to drive a motor vehicle and to operate machinery.
  • Drug dependence: xylometazoline is highly addictive. According to the German Centre for Addiction Issues, there are more than 100, 000 addicts in Germany.

Trade names

Balkis (D), GeloNasal (D), imidine (D), Nasben (CH), Nasobol (CH), Olynthus (D, A), Otriven (D), Otrivin (A, CH), Rapako xylo (D), ratio soft ( A), Stop Rhino (CH), Rinosedin (CH), sniffles Endrine (D), SNUP (D ), numerous generics (D, A, CH), Xylometazoline ( NL)

Nasic for children (D), nasic (A, CH, D), OtriDuo (A), Triofan (CH), XyloDex (A)

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Dangerous Substances Directive (67/548/EEC) Active ingredient Mucous membrane of nose Smooth muscle tissue Ciba Specialty Chemicals Epinephrine Hypoventilation
626780
de