From Wikipedia, the free encyclopedia
Mequitazine (trade name Primalan ) is an H1 antagonist 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
References
Ramírez Chanona, N; del Rio Navarro, BE; Pérez Martín, J (November–December 2005). "Efficacy of Mequitazine (Primalan) on the Relief of Symptoms of Allergic Rhinoconjunctivitis in Children. Documented clinical experience". Revista Alergia Mexico (in Spanish). 52 (6): 221–5. PMID 16568706 .
Theunissen, EL; Vermeeren, A; van Oers, AC; van Maris, I; Ramaekers, JG (February 2004). "A Dose-Ranging Study of the Effects of Mequitazine on Actual Driving, Memory and Psychomotor Performance as Compared to Dexchlorpheniramine, Cetirizine and Placebo". Clinical and Experimental 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 (February 1998). "Oxidation of Histamine H1 Antagonist Mequitazine is Catalyzed by Cytochrome P450 2D6 in Human Liver Microsomes" (PDF) . The Journal of Pharmacology and Experimental Therapeutics . 284 (2): 437–42. PMID 9454781 .
Persi, L; Dupin, O; Arnaud, B; Trinquand, C; Michel, FB; Bousquet, J (April 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 .
H1
Agonists Antagonists
Others: Atypical antipsychotics (e.g., aripiprazole , asenapine , brexpiprazole , brilaroxazine , clozapine , iloperidone , olanzapine , paliperidone , quetiapine , risperidone , ziprasidone , zotepine )
Phenylpiperazine antidepressants (e.g., hydroxynefazodone , nefazodone , trazodone , triazoledione )
Tetracyclic antidepressants (e.g., amoxapine , loxapine , maprotiline , mianserin , mirtazapine , oxaprotiline )
Tricyclic antidepressants (e.g., amitriptyline , butriptyline , clomipramine , desipramine , dosulepin (dothiepin) , doxepin , imipramine , iprindole , lofepramine , nortriptyline , protriptyline , trimipramine )
Typical antipsychotics (e.g., chlorpromazine , flupenthixol , fluphenazine , loxapine , perphenazine , prochlorperazine , thioridazine , thiothixene )
H2
H3
H4
mAChRs Tooltip Muscarinic acetylcholine receptors
Agonists Antagonists
3-Quinuclidinyl benzilate
4-DAMP
Aclidinium bromide (+formoterol )
Abediterol
AF-DX 250
AF-DX 384
Ambutonium bromide
Anisodamine
Anisodine
Antihistamines (first-generation) (e.g., brompheniramine , buclizine , captodiame , chlorphenamine (chlorpheniramine) , cinnarizine , clemastine , cyproheptadine , dimenhydrinate , dimetindene , diphenhydramine , doxylamine , meclizine , mequitazine , perlapine , phenindamine , pheniramine , phenyltoloxamine , promethazine , propiomazine , triprolidine )
AQ-RA 741
Atropine
Atropine methonitrate
Atypical antipsychotics (e.g., clozapine , fluperlapine , olanzapine (+fluoxetine ), rilapine , quetiapine , tenilapine , zotepine )
Benactyzine
Benzatropine (benztropine)
Benzilone
Benzilylcholine mustard
Benzydamine
BIBN 99
Biperiden
Bornaprine
Camylofin
CAR-226,086
CAR-301,060
CAR-302,196
CAR-302,282
CAR-302,368
CAR-302,537
CAR-302,668
Caramiphen
Cimetropium bromide
Clidinium bromide
Cloperastine
CS-27349
Cyclobenzaprine
Cyclopentolate
Darifenacin
DAU-5884
Desfesoterodine
Dexetimide
DIBD
Dicycloverine (dicyclomine)
Dihexyverine
Difemerine
Diphemanil metilsulfate
Ditran
Drofenine
EA-3167
EA-3443
EA-3580
EA-3834
Emepronium bromide
Etanautine
Etybenzatropine (ethybenztropine)
Fenpiverinium
Fentonium bromide
Fesoterodine
Flavoxate
Glycopyrronium bromide (+beclometasone/formoterol , +indacaterol , +neostigmine )
Hexahydrodifenidol
Hexahydrosiladifenidol
Hexbutinol
Hexocyclium
Himbacine
HL-031,120
Homatropine
Imidafenacin
Ipratropium bromide (+salbutamol )
Isopropamide
J-104,129
Hyoscyamine
Mamba toxin 3
Mamba toxin 7
Mazaticol
Mebeverine
Meladrazine
Mepenzolate
Methantheline
Methoctramine
Methylatropine
Methylhomatropine
Methylscopolamine
Metixene
Muscarinic toxin 7
N-Ethyl-3-piperidyl benzilate
N-Methyl-3-piperidyl benzilate
Nefopam
Octatropine methylbromide (anisotropine methylbromide)
Orphenadrine
Otenzepad (AF-DX 116)
Otilonium bromide
Oxapium iodide
Oxitropium bromide
Oxybutynin
Oxyphencyclimine
Oxyphenonium bromide
PBID
PD-102,807
PD-0298029
Penthienate
Pethidine
pFHHSiD
Phenglutarimide
Phenyltoloxamine
Pipenzolate bromide
Piperidolate
Pirenzepine
Piroheptine
Pizotifen
Poldine
Pridinol
Prifinium bromide
Procyclidine
Profenamine (ethopropazine)
Propantheline bromide
Propiverine
Quinidine
3-Quinuclidinyl thiochromane-4-carboxylate
Revefenacin
Rociverine
RU-47,213
SCH-57,790
SCH-72,788
SCH-217,443
Scopolamine (hyoscine)
Scopolamine butylbromide (hyoscine butylbromide)
Silahexacyclium
Sofpironium bromide
Solifenacin
SSRIs Tooltip Selective serotonin reuptake inhibitors (e.g., femoxetine , paroxetine )
Telenzepine
Terodiline
Tetracyclic antidepressants (e.g., amoxapine , maprotiline , mianserin , mirtazapine )
Tiemonium iodide
Timepidium bromide
Tiotropium bromide
Tiquizium bromide
Tofenacin
Tolterodine
Tricyclic antidepressants (e.g., amitriptyline (+perphenazine ), amitriptylinoxide , butriptyline , cidoxepin , clomipramine , desipramine , desmethyldesipramine , dibenzepin , dosulepin (dothiepin) , doxepin , imipramine , lofepramine , nitroxazepine , northiaden (desmethyldosulepin) , nortriptyline , protriptyline , quinupramine , trimipramine )
Tridihexethyl
Trihexyphenidyl
Trimebutine
Tripitamine (tripitramine)
Tropacine
Tropatepine
Tropicamide
Trospium chloride
Typical antipsychotics (e.g., chlorpromazine , chlorprothixene , cyamemazine (cyamepromazine) , loxapine , mesoridazine , thioridazine )
Umeclidinium bromide (+vilanterol )
WIN-2299
Xanomeline
Zamifenacin
Precursors (and prodrugs )