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  • Original articleNewer antihistaminics: IV. Some pharmacologic and therapeutic effects of β-(p-bromo-benzhydryloxy)-ethyldimethylamine hydrochloride, a derivative of diphenhydramine hydrochloride
  • Add time:08/26/2019         Source:sciencedirect.com

    1.1. From a study of 34 normal individuals and some 296 patients treated with Ambodryl (β-[4-bromobenzhydryloxy]-ethyldimethylamine hydrochloride), the following pharmacologic actions were demonstrated in human beings: (a) suppression of the “wheal and flare” reaction which normally follows the intracutaneous introduction of histamine; (b) a tendency to pupillary dilatation in larger doses (300 mg. or more daily); and (c) slight lowering of the basal metabolic rate in the largest doses, although the degree of this change may not be statistically significant.2.2. In daily doses varying from 75 to 600 mg. orally ingested for periods of time varying from 1 to 54 weeks, no appreciable changes were produced by Ambodryl in the following: weight; pulse rate; blood pressure; electrocardiogram; icteric index; van den Bergh reaction; cephalin flocculation; serum inorganic phosphorus, cholesterol, cholesterol esters, total protein, albumin, and globulin; blood urea nitrogen, creatinine, and glucose; the blood count; gastric acidity; glucose tolerance; and urinalysis.3.3. Ambodryl has been administered to 296 patients for periods of time ranging from 1 day to 14 months in amounts varying from unit doses of 25 mg. to 300 mg. daily. Maintenance doses of the drug have varied from 50 to 300 mg. daily.4.4. Partial or complete relief has been afforded all cases of urticaria, angioneurotic edema, contact dermatitis, spastic colon, and premenstrual tension. Approximately 90 per cent of all cases of seasonal allergic rhinitis have obtained relief. Between 75 and 80 per cent of the cases of atopic eczema and nonseasonal allergic rhinitis have been improved and 50 per cent of the patients with bronchial asthma and migraine have been helped. Other conditions which have been treated include generalized pruritus of varied etiology, gastrointestinal allergies due to food, essential hypertension, sea and airsickness, and postoperative hiccoughing.5.5. In 321 subjects, the over-all incidence of side effects or toxic symptoms was 8.4 per cent; in a therapeutic range of dosage (from 75 to 300 mg. daily) for the same subjects this incidence was 6.2 per cent. No untoward reactions were observed in daily doses below 100 mg. Qualitatively, the unpleasant symptoms resembled those associated with the administration of diphenhydramine hydrochloride. In descending order of frequency they included drowsiness, dryness of the throat, diarrhea, and anorexia.6.6. The therapeutic activity and toxicity of Ambodryl have been critically compared with those of diphenhydramine hydrochloride and Toladryl. Practical considerations in connection with such comparisons are discussed.

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