Cinnarizine

(sin-nah-rih-zeen)

PCaution when used during lactation : Caution when used during pregnancy

LCaution when used during lactation : Caution when used during lactation

Molecule Info

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Indication(s) & Dosage

Cinnarizine is indicated in -

  • Control of vestibular symptoms of both peripheral and central origin and of labyrinthine disorders including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
  • Prophylaxis of motion sickness.
  • Adjunct therapy for symptoms of peripheral arterial disease.

Oral route

  • Vertigo and vestibular disorders  >12 yrs & adult: 30 mg tid. Child: 5-12 yr: 1/2 of adult dose. 
  • Motion sickness  Adult: 30 mg taken 2 hr before travel and 15 mg every 8 hr during the journey if necessary. Child: 5-12 yr: 1/2 of adult dose.
  • Cerebrovascular disorders  Adult: 75 mg 1-3 times daily.
  • Peripheral vascular disease  Adult: 75 mg bid or tid. 

Administration

Should be taken with food.

Overdose

Symptoms

The signs and symptoms are mainly due to the anticholinergic (atropine-like) activity of cinnarizine.

Acute cinnarizine overdoses have been reported with doses ranging from 90 to 2,250 mg. The most commonly reported signs and symptoms associated with overdose of cinnarizine include: alterations in consciousness ranging from somnolence to stupor and coma, vomiting, extrapyramidal symptoms, and hypotonia. In a small number of young children, seizures developed. Clinical consequences were not severe in most cases, but deaths have been reported after single and polydrug overdoses involving cinnarizine.

Treatment

There is no specific antidote. For any overdose, the treatment is symptomatic and supportive care.

Activated charcoal should only be considered in patients presenting within one hour of taking a potentially toxic overdose (ie more than 15mg/kg).

Contraindications

Proven hypersensitivity to the drug.  Parkinson's disease.  Children and neonates.

Special Precautions

As with other antihistamines, Cinnarizine may cause epigastric discomfort; taking it after meals may diminish the gastric irritation. In patients with Parkinson's Disease, Cinnarizine should only be given if the advantages outweigh the possible risk of aggravating this disease. Because of its antihistamine effect, Cinnarizine may prevent an otherwise positive reaction to dermal reactivity indicators if used within 4 days prior to testing.

Use of cinnarizine should be avoided in porphyria.

There have been no specific studies in hepatic or renal dysfunction. Cinnarizine should be used with care in patients with hepatic or renal insufficiency.

Patients with rare hereditary problems of fructose or galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption or sucrase-isomaltase insufficiency, should not take this medicine because it contains lactose and sucrose.

Adverse Drug Reaction(s)

Extrapyramidal symptoms sometimes associated with severe depression.  Drowsiness, headache, GI upsets, unsteadiness, headache; rarely skin and hypersensitivity reactions, dry mouth, blurred vision, urinary difficulty or retention, constipation and increased gastric reflux, fatigue.  Hypolipidaemic effect.

Drug Interactions

Concurrent use of alcohol, CNS depressants or tricyclic antidepressants may potentiate the sedative effects of either these drugs or of Cinnarizine.

Pregnancy Category (FDA)

Category C: Either studies in animals have revealed adverse effects on the foetus and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Pharmacology

Cinnarizine has been shown to be a non-competitive antagonist of the smooth muscle contractions caused by various vasoactive agents including histamine.

Cinnarizine also acts on vascular smooth muscle by selectively inhibiting the calcium influx into depolarised cells, thereby reducing the availability of free Ca2+ ions for the induction and maintenance of contraction.

Vestibular eye reflexes induced by caloric stimulation of the labyrinth in guinea pigs are markedly depressed by cinnarizine.

Cinnarizine has been shown to inhibit nystagmus.

In animals, cinnarizine is extensively metabolised, N-dealkylation being the major pathway. Approximately two thirds of the metabolites are excreted with the faeces, the rest in the urine, mainly during the first five days after a single dose.

Absorption

In man, after oral administration, absorption is relatively slow, peak serum concentrations occurring after 2.5 to 4 hours.

Distribution

The plasma protein binding of cinnarizine is 91%.

Metabolism

Cinnarizine is extensively metabolised mainly via CYP2D6, but there is considerable interindividual variation in the extent of metabolism.

Elimination

The reported elimination half-life for cinnarizine ranges from 4 to 24 hours.

The elimination of metabolites occurs as follows: one third in the urine (unchanged as metabolites and glucuronide conjugates) and two thirds in the faeces.

ATC Classification

N07CA02 - cinnarizine; Belongs to the class of antivertigo preparations.

 

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Brand/Product Info



Total Products : 10          
Brand Name Manufacturer/Marketer Composition Dosage Form Pack Size & Price
CINARIN Nipa Pharmaceuticals Ltd. Cinnarizine 15mg Tablet 100's: 100.00 MRP
CINARON Square Pharmaceuticals Ltd. Cinnarizine 15mg Tablet 20x10's: 200.00 MRP
CINARYL Opsonin Pharma Limited Cinnarizine 15mg Tablet 100's: 100.00 MRP
CINARZIN IBN SINA Pharmaceutical Industry Ltd. Cinnarizine 15mg Tablet 100's: 100.00 IP
CINAZIN The Acme Laboratories Ltd. Cinnarizine 15mg Tablet 100's: 70.00 MRP
CINNARIZINE Bristol Pharma Limited Cinnarizine 15mg Tablet 200's: 200.00 MRP
CINOMYST Mystic Pharmaceuticals Limited Cinnarizine 15mg Tablet 100's: 70.00 MRP
INARZIN Beximco Pharmaceuticals Ltd Cinnarizine BP 15mg Tablet 100's: 90.00 MRP
SUZARON Rephco Laboratories Ltd. Cinnarizine 15mg Tablet 100's: 50.00 MRP
ZINCIN Aristopharma Ltd. Cinnarizine 15mg Tablet 50's: 250.00 MRP