Cinnarizine

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[edit] BRAND NAMES

[edit] COMBINATION FORMULATIONS

CINNARIZINE/DIMENHYDRINATE:

[edit] STRUCTURE

Cinnarizine.jpg

[edit] MECHANISM OF ACTION

Cinnarizine is an histamine H1 antagonist, a calcium channel blocker that inhibits contractions of vascular smooth muscle cells by blocking T-type voltage gated calcium channels and a muscarinic acetycholine receptors antagonist.

Cinnarizine increases erythrocyte flexibility and decreases whole blood viscosity. Therefore, it improves deficient microcirculation and increases cellular resistance to hypoxia. Cinnarizine also reduces the vestibular sensitivity, preventing acute episodes of vertigo.

[edit] INDICATIONS

  • Prophylaxis and treatment of motion sickness
  • Prophylaxis of migraine
  • Therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting
  • Symptomatic treatment of vertigo due to Meniere's disease
  • Adjunct therapy for symptoms of peripheral arterial disease including Reynaud’s phenomenon, acrocyanosis, intermittent claudication, trophic disturbances, trophic and varicose ulcers, paraesthesia, nocturnal cramps, cold extremities.
  • Loss of memory and lack of concentration (Because of its vasorelaxating abilities due to calcium channel blockage in brain, it can be considered a nootropic drug)

[edit] DOSAGE

Cinnarizine should preferably be taken after meals to minimize gastric irritation symptoms

  • Motion Sickness:
    • Adults: 25 mg may be taken 2 hours before departure and 12,5-25 mg may be repeated every 6-8 hours.
    • Children 8 to 12 years: 12,5 mg three times daily when necessary.
    • Children 5 to 7 years: 6,25 mg three times daily when necessary.
  • Disorders of balance:
    • Adults and children over the age of 12 years: 25 mg three times daily. Max: 225mg/day (The effect is dose dependent)
  • Peripheral circulatory disorders and Cerebral circulatory disorders:
    • Adults and children over the age of 12 years: 25 mg three times daily.
  • Prophylaxis of migraine: 25-75 mg at bedtime

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to cinnarizine
  • Parkinson's disease

[edit] WARNINGS AND PRECAUTIONS

  • Cinnarizine may lead to drowsiness and impaired concentration. Caution should be taken during driving or operating dangerous machinery
  • Alcoholic drinks should be avoided

[edit] INTERACTIONS

  • Cinnarizine may enhance the sedative effect of central nervous system depressants including alcohol, barbiturates, hypnotics, narcotic analgesics, tricyclic antidepressants, sedatives and tranquillisers.

[edit] PREGNANCY AND LACTATION

  • Cinnarizine should be used during pregnancy only if the therapeutic benefits justify the potential risks for the fetus.
  • Nursing should be discouraged in women using Cinnarizine

[edit] SIDE EFFECTS

Cinnarizine can cause drowsiness (may diminish after a few days), blurred vision, dry mouth, increased appetite, epigastric pain, skin rashes and, especially in the elderly who have been taking the drug for some time, extrapyramidal effect. very rare cases of lichen planus and lupus-like symptoms have been reported.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antiemetics
5-HT3 receptor antagonists Dolasetron   Granisetron   Ondansetron   Palonosetron   Tropisetron
Dopamine antagonists Alizapride   Bromopride   Clebopride   Domperidone   Metoclopramide   Prochlorperazine   Thiethylperazine
H1 antagonists Dimenhydrinate   Meclizine
NK1 receptor antagonists‎ Aprepitant   Fosaprepitant   Maropitant
Motion sickness‎ Cinnarizine   Dimenhydrinate   Meclizine   Meclizine/Pyridoxine   Scopolamine (Patch)
Pregnancy Meclizine/Pyridoxine   Ondansetron
Veterinary Maropitant
Vertigo
Betahistine   Cinnarizine   Dimenhydrinate/Cinnarizine   Flunarizine   Piracetam   Prochlorperazine
Antimigraine preparations
5 HT1 agonists (Triptans) Almotriptan (Almogran, Axert)   Eletriptan (Relpax)   Frovatriptan (Frova, Migard, Menatriptan)   Rizatriptan (Maxalt)   Sumatriptan (Imigran)   Zolmitriptan (Zomig)
Ergot alkaloids Dihydroergotamine   Ergotamine
NSAIDs/ Analgesics Indometacin   Acetylsalicylic acid (Aspirin)   Diclofenac (Voltaren)   Ibuprofen (Advil, Brufen, Dolgit, Nurofen)   Ketorolac (Toradol)   Naproxen (Naprosyn, Aleve)   Nimesulide   Paracetamol (Efferalgan, Panadol...)
Prophylaxis Cinnarizine (Stugeron, Stugeron forte)   Flunarizine (Sibelium)   Nifedipine (Adalat)   Pizotifen   Propranolol (Inderal)   Topiramate (Topamax)