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Br J Clin Pharmacol. Jan 1988; 25(1): 27–32.
PMCID: PMC1386611

Evaluation of the antimuscarinic activity of atropine, terfenadine and mequitazine in healthy volunteers.


1 The anticholinergic effects of atropine and two antihistamines (terfenadine and mequitazine) were investigated vs placebo in a double-blind study. 2 Salivary secretion, basal pupil diameter, pilocarpine (0.25%) induced miosis and heart rate were determined in eight healthy volunteers, seven male and one female, aged between 23 and 35 years. Each volunteer received all four separate courses of treatment: i.e. terfenadine 60 mg or mequitazine 5 mg twice daily for 3 days, and one single dose on the day of the trial; for the placebo or atropine courses they received the placebo twice daily during 3 days and, on the morning of test day, either the placebo again or atropine 1 mg. Pupillary diameter was measured under standardized conditions using a pupil gauge (Smith and Nephew Pharmaceuticals Ltd). 3 Atropine significantly reduced salivary output (-2.25 +/- 0.36 ml from control values of 4.17 +/- 0.42 ml, P less than 0.001) and heart rate (-9.7 +/- 3.7 beats min-1 from 77.5 +/- 2.7, P less than 0.05). These maximal effects were observed 3 h after atropine dosing for salivary secretion and 1 h for heart rate. Atropine did not affect basal pupil diameter or pilocarpine-induced miosis. 4 Mequitazine and terfenadine did not affect salivary flow, heart rate or pilocarpine-induced miosis. 5 Terfenadine and mequitazine had no anticholinergic effect in these tests involving a limited number of subjects.

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Selected References

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  • Brion N, Culig J, Turner P. Etude de l'action de l'indalpine sur le diamètre pupillaire chez de volontaire sain. Therapie. 1985 Jan-Feb;40(1):9–11. [PubMed]
  • Demaubeuge J, Tennstedt D, Broux R. Does mast cell protection plus mediator antagonism surpass the effect of a classic antihistaminic in the treatment of chronic urticaria? A double-blind comparison of oxatomide and mequitazine. Dermatologica. 1982 Jun;164(6):386–394. [PubMed]
  • Dry J, Pradalier A, Di Palma H, Lanoue R. Essai clinique en double aveugle contre placebo de la méquitazine chez des patients non hospitalisés. Therapie. 1980 Mar-Apr;35(2):189–195. [PubMed]
  • File RR, Patton TF. Topically applied pilocarpine. Human pupillary response as a function of drop size. Arch Ophthalmol. 1980 Jan;98(1):112–115. [PubMed]
  • Garteiz DA, Hook RH, Walker BJ, Okerholm RA. Pharmacokinetics and biotransformation studies of terfenadine in man. Arzneimittelforschung. 1982;32(9A):1185–1190. [PubMed]
  • Girard JP, Sommacal-Schopf D, Bigliardi P, Henauer SA. Double-blind comparison of astemizole, terfenadine and placebo in hay fever with special regard to onset of action. J Int Med Res. 1985;13(2):102–108. [PubMed]
  • Hayes AH, Jr, Copelan HW, Ketchum JS. Effects of large intramuscular doses of atropine on cardiac rhythm. Clin Pharmacol Ther. 1971 May-Jun;12(3):482–486. [PubMed]
  • Kerr FA, Szabadi E. Comparison of the effects of chronic administration of ciclazindol and desipramine on pupillary responses to tyramine, methoxamine and pilocarpine in healthy volunteers. Br J Clin Pharmacol. 1985 May;19(5):639–647. [PMC free article] [PubMed]
  • Kingsley PJ, Turner P. Class experiment in clinical pharmacology with benzilonium bromide, an anticholinergic drug. Eur J Clin Pharmacol. 1974;7(2):141–143. [PubMed]
  • Kottmeier CA, Gravenstein JS. The parasympathomimetic activity of atropine and atropine methylbromide. Anesthesiology. 1968 Nov-Dec;29(6):1125–1133. [PubMed]
  • Kulshrestha VK, Gupta PP, Turner P, Wadsworth J. Some clinical pharmacological studies with terfenadine, a new antihistamine drug. Br J Clin Pharmacol. 1978 Jul;6(1):25–29. [PMC free article] [PubMed]
  • Lazenby GW, Reed JW, Grant WM. Short-term tests of anticholinergic medication in open-angle glaucoma. Arch Ophthalmol. 1968 Oct;80(4):443–448. [PubMed]
  • Longmore J, Bradshaw CM, Szabadi E. Effects of locally and systemically administered cholinoceptor antagonists on the secretory response of human eccrine sweat glands to carbachol. Br J Clin Pharmacol. 1985 Jul;20(1):1–7. [PMC free article] [PubMed]
  • Patel KR. Effect of terfenadine on methacholine-induced bronchoconstriction in asthma. J Allergy Clin Immunol. 1987 Feb;79(2):355–358. [PubMed]
  • Richards DM, Brogden RN, Heel RC, Speight TM, Avery GS. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38–61. [PubMed]
  • Shur E, Checkley S. Pupil studies in depressed patients: an investigation of the mechanism of action of desipramine. Br J Psychiatry. 1982 Feb;140:181–184. [PubMed]
  • Szabadi E, Gaszner P, Bradshaw CM. The peripheral anticholinergic activity of tricyclic antidepressants: comparison of amitriptyline and desipramine in human volunteers. Br J Psychiatry. 1980 Nov;137:433–439. [PubMed]

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