Cinnarizine; Uses, Dosage, Side Effects, Drug Interactions Cinnarizine is an anti-histaminic drug which is mainly used for the control of vomiting due to motion sickness. It acts by interfering with the signal transmission between the vestibular apparatus of the inner ear and the vomiting center of the hypothalamus. 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 is actually a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception. 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. 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. You Might Also Read What Is Evabotulinumtoxina? Indications, ContraindicationsIndications 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 Hypersensitivity to Cinnarizine is a contraindication. In addition, Cinnarizine should not be used if you have the following conditions: Hypersensitivity to this drug Allergy Depression Porphyria Dosages of cinnarizine Adult 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. Cerebrovascular disorders Adult: 75 mg once daily. Motion sickness 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. Vertigo and vestibular disorders Adult: 30 mg tid or 75 mg 1-2 times daily. Child: 5-12 yr 15 mg tid. Side effects of cinnarizine The most common Drowsiness Dry mouth Headache Indigestion Depression Skin rashes Restlessness Weight gain Common Sweating Blurred vision Dizziness. slower heart rate diarrhea dry eyes hair loss nausea weakness or tiredness Common Cough producing mucus difficulty with breathing tightness in the chest Abdominal or stomach pain and tenderness blistering, peeling, or loosening of the skin Anxiety dry mouth irritability sleepiness or unusual drowsiness trouble sleeping Decreased appetite You Might Also Read Darbepoetin alfa - Uses, Dosage, Side Effects, InteractionsSerious Swelling of the hands, arms, feet, ankles, or lower legs Chest pain Difficulty breathing Itching or rash Dizziness Lack of energy Black, tarry, or bloody stools Bloody vomit, or vomit that looks like coffee grounds Pale skin passing out or fainting seizures Drug Interaction of cinnarizine System organ class Adverse drug reactions Frequency category Common Uncommon Not known 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 Investigations Weight increased Cinnarizine may interact with following drugs Amitriptyline Tramadol Chlorpromazine Diazepam Medicines for depression (e.g. tricyclic antidepressants such as amitriptyline) Pregnancy & Lactation of cinnarizine FDA Pregnancy Category C Pregnancy 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. Lactation There are no data on the excretion of cinnarizine in human breast milk. Taking cinnarizine whilst breastfeeding is not recommended. References DrugBank http://www.drugbank.ca/drugs/DB00568 http://www.drugbank.ca/drugs/DB00568#targets http://www.drugbank.ca/drugs/DB00568#enzymes https://www.drugs.com/uk/cinnarizine-15mg-tablets-leaflet.html EPA DSStox https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID3022821 https://www.infomed.ch/100drugs/cincont.html European Chemicals Agency (ECHA) https://echa.europa.eu/substance-information/-/substanceinfo/100.037.030 https://echa.europa.eu/substance-information/-/substanceinfo/100.005.514 https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/12216 https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/27294 ClinicalTrials.gov https://clinicaltrials.gov/ FDA/SPL Indexing Data https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/ https://www.infomed.ch/100drugs/cincont.html NIST http://www.nist.gov/srd/nist1a.cfm SpectraBase https://spectrabase.com/compound/CSJAMSER2Kz#25wuXX9URii https://spectrabase.com/compound/CSJAMSER2Kz#F96QyhzRWVI Springer Nature Read more … WHO ATC https://www.whocc.no/atc/ https://www.whocc.no/atc_ddd_index/ Wikipedia https://en.wikipedia.org/wiki/Cinnarizine https://pubchem.ncbi.nlm.nih.gov MeSH https://www.ncbi.nlm.nih.gov/mesh/68002936 http://www.nlm.nih.gov/mesh/meshhome.html https://www.ncbi.nlm.nih.gov/mesh/68002121 https://www.ncbi.nlm.nih.gov/mesh/68006634 Show More