Cinnarizine

ATC CodeN06DX12, N07CA02
CAS number298-57-7
PUB number1547484
Drugbank IDDB00568
Empirical formulaC26H28N2
Molar mass (g·mol−1)368.524
Physical statesolid

Basics

Cinnarizine is an antihistamine and calcium channel blocker from the diphenylmethylpiperazine group. It is prescribed for nausea and vomiting due to motion sickness or other causes such as chemotherapy, dizziness, or Ménière's disease. Cinnarizine is taken by mouth.

Pharmacology

Pharmacodynamics

Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities including contraction of airway and gastrointestinal smooth muscle, vasodilation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release, and chemotaxis of eosinophils and mast cells. Cinnarizine also blocks muscarinic acetylcholine receptors. Cinnarizine also inhibits calcium channels through its action resulting in a relaxing effect on vascular smooth muscle.

Pharmacokinetics

Cinnarizine is most commonly taken orally in tablet form. After ingestion, the substance is absorbed quite rapidly and reaches maximum plasma concentration within 1-3 hours after administration. Cinnarizine is CNS-responsive due to its high lipophilicity, which is why it can have a sedative effect on patients. Cinnarizine is metabolized in the liver, after which one-third is excreted in the urine and two-thirds in the stool. The elimination half-life varies between 3.4-60 hours depending on the age of the patient.

Toxicity

Side effects

Possible side effects are

  • drowsiness
  • Sweating
  • Dry mouth
  • headache
  • Skin problems
  • Lethargy
  • Gastrointestinal irritation
  • Hypersensitivity reactions
  • Movement problems/muscle stiffness
  • Tremors

Because cinnarizine can cause drowsiness and blurred vision, it is important not to operate heavy machinery while using it if side effects become apparent.

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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