Cinnarizine is an antihistamine and calcium channel blocker of the diphenylmethylpiperazine group. It is also known to promote cerebral blood flow, and so is used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis. Cinnarizine could be also viewed as a nootropic drug because of its vasorelaxation abilities (due to calcium channel blockage), which happen mostly in the brain. It is also effectively combined with other nootropics, primarily piracetam; in such combination, each drug potentiate the other in boosting brain oxygen supply.
Mechanism of action of cinnarizine
Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system. Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage-gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors.
Indications of cinnarizine
- Vertigo/Meniere’s disease,
- Nausea and vomiting,
- Motion sickness
- Vestibular symptoms of other origins.
- Motion sickness, vertigo and Meniere’s disease.
- Controlling the dizziness when traveling in vehicles (motion sickness)
- In problems caused by balance disorders such as Meniere’s disease.
- Tinnitus (ear noise)
- Nausea and/or vomiting
- For the treatment of vertigo/Meniere’s disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins.
Contraindications of cinnarizine
Dosages of cinnarizine
- PO Vertigo and vestibular disorders 30 mg tid or 75 mg 1-2 times/day.
- Motion sickness 30 mg 2 hr before travel then 15 mg 8 hrly during the journey if necessary.
- Cerebrovascular disorders 75 mg once daily. Peripheral vascular disease 75 mg bid or tid.
Peripheral vascular disease
- Adult: 75 mg bid or tid.
- Adult: 75 mg once daily.
- Adult: 30 mg 2 hr before travel then 15 mg 8 hrly during the journey if necessary.
- Child: 5-12 yr 15 mg 2 hr before travel then 7.5 mg 8 hrly during the journey as necessary.
- Adult: 30 mg tid or 75 mg 1-2 times daily.
- Child: 5-12 yr 15 mg tid.
Side effects of cinnarizine
- Blurred vision
- slower heart rate
- dry eyes
- hair loss
- weakness or tiredness
- Cough producing mucus
- difficulty with breathing
- tightness in the chest
- Abdominal or stomach pain and tenderness
- blistering, peeling, or loosening of the skin
- dry mouth
- sleepiness or unusual drowsiness
- trouble sleeping
- Decreased appetite
Drug Interaction of cinnarizine
System organ class
Adverse drug reactions
|Nervous system disorders||Somnolence||Lethargy||Dyskinesia, extrapyramidal disorder (sometimes associated with depressive feelings), Parkinsonism, tremor|
|Gastrointestinal disorders||Nausea, dyspepsia||Vomiting, upper abdominal pain|
|Hepatobiliary disorders||Cholestatic jaundice|
|Skin and subcutaneous tissue disorders||Hyperhidrosis, Lichenoid keratosis including lichen planus||Subacute cutaneous lupus erythematosus|
|Musculoskeletal and connective tissue disorders||Muscle rigidity|
|General disorders and administrative site conditions||Fatigue|
Cinnarizine may interact with following drugs
Pregnancy & Lactation of cinnarizine
FDA Pregnancy Category C
The safety of cinnarizine in human pregnancy has not been established although studies in animals have not demonstrated teratogenic effects. As with other drugs, it is not advisable to administer cinnarizine in pregnancy.
There are no data on the excretion of cinnarizine in human breast milk. Taking cinnarizine whilst breastfeeding is not recommended.