Meclozine

Oral
Vertigo

Oral
Motion sickness

Pharmacogenomics

In an in-vitro metabolic study, CYP2D6 was noted to be the dominant enzyme for the metabolism of meclozine. FDA drug label states that large inter-individual variability in meclozine exposure may occur in patients with CYP2D6 phenotypes, thus resulting to poor, intermediate, extensive or ultra-rapid metabolism. Monitoring for adverse reactions and clinical effects is recommended in these patients.

May be taken with or without food.

Patients with asthma, narrow-angle glaucoma, prostatic hyperplasia, bladder neck obstruction, urinary stricture, pyloric or duodenal obstruction. Patients with CYP2D6 polymorphism. Renal and hepatic impairment. Children and elderly. Pregnancy and lactation.

Significant: Drowsiness.
Eye disorders: Rarely, blurred vision.
Gastrointestinal disorders: Dry mouth, vomiting.
General disorders and administration site conditions: Fatigue.
Immune system disorders: Anaphylactic reaction.
Nervous system disorders: Headache.

PO: B

This drug may cause drowsiness, if affected, do not drive or operate machinery.

May increase CNS depression with tranquilizers and sedatives.

May enhance CNS depressant effect with alcohol.

Description: Meclozine blocks vasodepressor response to histamine and has a slight blocking action against acetylcholine. It decreases excitability of the middle ear labyrinth and blocks conduction in the middle ear vestibular-cerebellar pathways.
Synonym: Meclizine
Onset: Approx 1 hour.
Duration: Approx 24 hours.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 3 hours.
Distribution: Volume of distribution: 7 L/kg.
Metabolism: Metabolised in the liver to norchlorcyclizine.
Excretion: Via urine and faeces as unchanged drug and metabolites. Elimination half-life: Approx 5-6 hours.

Source: National Center for Biotechnology Information. PubChem Database. Meclizine, CID=4034, https://pubchem.ncbi.nlm.nih.gov/compound/Meclizine (accessed on Jan. 22, 2020)

Store between 20-25°C. Protect from light.

Antiemetics / Antivertigo Drugs

R06AE05 - meclozine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.

Annotation of FDA Label for Meclizine and CYP2D6. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 18/10/2019.

Anon. Meclozine Hydrochloride. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/10/2019.

Antivert (Casper Pharma LLC). U.S. FDA. https://www.fda.gov/. Accessed 18/10/2019.

Bonamine Chewable Tablet (Interphil Laboratories Inc.). MIMS Philippines. http://www.mims.com/philippines. Accessed 18/10/2019.

Buckingham R (ed). Meclizine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/10/2019.

McEvoy GK, Snow EK, Miller J et al (eds). Meclizine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 23/11/2015.

Meclizine Hydrochloride Tablet (Amneal Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 18/10/2019.

Meclizine Hydrochloride Tablet (Epic Pharma, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/11/2015.

Rugby Travel Sickness Tablet, Chewable (Rugby Laboratories). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/11/2015.

Sea-Legs Tablet (Seton Products Limited). MHRA. https://products.mhra.gov.uk/. Accessed 23/11/2015.

Sea-Legs Tablets (G R Lane Health Products Ltd.). MHRA. https://products.mhra.gov.uk/. Accessed 22/10/2019.