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Cinnarizine

Cinnarizine
Cinnarizine.svg
Clinical data
Trade names Stugeron, Stunarone, Arlevert, Diznil-25
AHFS/Drugs.com International Drug Names
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Biological half-life 3–4 h
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.005.514
Chemical and physical data
Formula C26H28N2
Molar mass 368.514 g/mol
3D model (Jmol)
  

Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker, it is also known to promote cerebral blood flow, and so is used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis. However, it is more commonly prescribed for nausea and vomiting due to motion sickness or other sources such as chemotherapy,vertigo, or Ménière's disease. Cinnarizine was first synthesized by Janssen Pharmaceutica in 1955. The nonproprietary name is derived from the cinnamyl substituent on one of the nitrogen atoms, combined with the generic ending "-rizine" for "antihistaminics/cerebral (or peripheral) vasodilators". It is not available in the United States or Canada. It has also been cited as one of the most used drugs for seasickness within the British Royal Navy.

Cinnarizine is predominantly used to treat nausea and vomiting associated with motion sickness,vertigo,Ménière's disease, or Cogan's syndrome. In fact, it is one of only a select few drugs that has shown a beneficial effect in the chronic treatment of the vertigo and tinnitus, associated with Meniere's disease. However, due to increased levels of drowsiness caused by the medication, it is generally of limited use in pilots and aircrew who must be dependably alert. In a clinical study (n=181), treatment with cinnarizine reduced the occurrence of moderate vertigo experience by 65.8% and extreme vertigo by 89.8%.

It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus by limiting the activity of the vestibular hair cells which send signals about movement. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness could be a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception, but the true evolutionary reason for this malady is currently unknown.


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