Mequitazine

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Mequitazine
Mequitazine structure.svg
Clinical data
Trade namesPrimalan
AHFS/Drugs.comInternational Drug Names
ATC code
Legal status
Legal status
  • EU: Rx-only [1]
Identifiers
  • 10-(1-Azabicyclo[2.2.2]octan-3-ylmethyl)phenothiazine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.045.005 Edit this at Wikidata
Chemical and physical data
FormulaC20H22N2S
Molar mass322.47 g·mol−1
3D model (JSmol)
  • c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2
  • InChI=1S/C20H22N2S/c1-3-7-19-17(5-1)22(18-6-2-4-8-20(18)23-19)14-16-13-21-11-9-15(16)10-12-21/h1-8,15-16H,9-14H2
  • Key:HOKDBMAJZXIPGC-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

Mequitazine (trade name Primalan) is an H1 antagonist and anticholinergic of the phenothiazine chemical class. It is used to treat allergies and rhinitis.

It was patented in 1969 and came into medical use in 1976.[2]

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 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.

References

  1. ^ https://www.ema.europa.eu/documents/psusa/mequitazine-list-nationally-authorised-medicinal-products-psusa/00001986/202001_en.pdf[bare URL PDF]
  2. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 548. ISBN 9783527607495.

Further reading

External links

  • "Mequitazine". Drug Information Portal. U.S. National Library of Medicine.