Mequitazine

Mequitazine

Clinical data
Trade names	Primalan
AHFS/Drugs.com	International Drug Names
ATC code	R06AD07 (WHO)
Identifiers
IUPAC name 10-(1-azabicyclo[2.2.2]octan-3-ylmethyl)phenothiazine
CAS Number	29216-28-2
PubChem (CID)	4066
DrugBank	DB01071
ChemSpider	3926
UNII	Y463242LY2
KEGG	D01324
ECHA InfoCard	100.045.005
Chemical and physical data
Formula	C20H22N2S
Molar mass	322.468 g/mol
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Mequitazine (trade name Primalan) is an antihistamine and anticholinergic of the phenothiazine chemical class. It is used to treat allergies and rhinitis.

Contraindications

Severe liver disease; premature infants or full-term neonates.

Special precautions

Pregnancy, lactation; severe cardiovascular disorders; asthma; angle-closure glaucoma, urinary retention, prostatic hyperplasia, pyloroduodenal obstruction; renal and hepatic impairment; elderly, children; epilepsy. May impair ability to drive or operate machinery.

Adverse drug reactions

CNS depression including slight drowsiness to deep sleep, lassitude, dizziness, incoordination. Headache, psychomotor impairment and antimuscarinic effects. Rarely, rashes and hypersensitivity reactions, blood disorders, convulsions, sweating, myalgia, paraesthesias, extrapyramidal effects, tremor, confusion, sleep and GI disturbances, tinnitus, hypotension, hair loss. Photosensitivity, jaundice.

Drug interactions

Enhances effects of CNS depressants e.g. alcohol, barbiturates, hypnotics, opioid analgesics, anxiolytics and antipsychotics. Can mask signs of ototoxicity caused by aminoglycosides. QT prolongation (which can lead to torsades de pointes arrhythmia) reported with spiramycin.

See also

• Phenothiazine

References

• Ramírez Chanona N, del Rio Navarro B, Pérez Martín J (2005). "Efficacy of mequitazine (Primalan) on the relief of symptoms of allergic rhinoconjunctivitis in children. Documented clinical experience". Rev Alerg Mex. 52 (6): 221–5. PMID 16568706.
• Theunissen E, Vermeeren A, van Oers A, van Maris I, Ramaekers J (2004). "A dose-ranging study of the effects of mequitazine on actual driving, memory and psychomotor performance as compared to dexchlorpheniramine, cetirizine and placebo.". Clin Exp Allergy. 34 (2): 250–8. doi:10.1111/j.1365-2222.2004.01874.x. PMID 14987305.
• Nakamura K, Yokoi T, Kodama T, Inoue K, Nagashima K, Shimada N, Shimizu T, Kamataki T (1998). "Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes.". J Pharmacol Exp Ther. 284 (2): 437–42. PMID 9454781.
• Persi L, Dupin O, Arnaud B, Trinquand C, Michel F, Bousquet J (1997). "Efficacy of mequitazine in comparison with placebo assessed by ocular challenge with allergen in allergic conjunctivitis.". Allergy. 52 (4): 451–4. doi:10.1111/j.1398-9995.1997.tb01028.x. PMID 9188930.