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Query: DrugBank:APRD00345 (
ICI
)
5,388
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
1. The beta-adrenergic blocking potencies of practolol,
ICI
66082, tolamolol, acebutolol, H 93/26, H 87/07, pindolol and Ro 3-4787 were compared with that of propranolol, on human and rat adipocytes. 2. A good correlation was found between the potencies on adipocytes of the two species but not between our results and literature data on antagonism of isopernaline tachycardia in the anaesthetized cat. 3. The results indicate that differences between adrenergic beta-receptors in heart and adipose tissue may be detected using cardioselective beta-adrenergic receptor blocking agents.
Br J
Clin
Pharmacol 1975 Aug
PMID:Isoprenaline antagonism of cardioselective beta-adrenergic receptor blocking agents on human and rat adipocytes. 0 50
1. DL-Propranolol, L-propranolol, DL-alprenolol, pindolol (LB46), practolol,
ICI
66082, sotalol and oxprenolol all produced prolonged falls in blood pressure and heart rate after intracerebroventricular administration in conscious normotensive cats. 2. Transient initial pressor responses and tachycardias were observed after intracerebroventricular infusions of all the beta-adrenoceptor antagonists used, except
ICI
66082. 3. D-Propranolol, D-alphrenolol, procaine and lignocaine all produced initial increases in blood pressure and heart rate but did not subsequently cause any reduction in either blood pressure or heart rate. 4. The time of maximum hypotension and bradycardia after intracerebroventricular infusion of beta-adrenoceptor antagonists coincided with the maximum inhibition of the centrally mediated tachycardia observed after intracerebroventricular isoprenaline.
Clin
Sci Mol Med Suppl 1975 Jun
PMID:The brain as a possible site for the cardiovascular effects of beta-adrenoceptor blocking agents in cats. 2 78
1. The effects of propranolol, atenolol (
ICI
66,082), practolol and pindolol on heart rate and maximal left ventricular dp/dt, atrioventricular conduction time, mean aortic flow and diastolic blood pressure during cardiac pacing were investigated over a wide dose range (0.025-4.0 mg/kg, i.v.) in dogs anaesthetized with pentobarbitone.2. Propranolol and atenolol produced similar reductions in haemodynamic parameters. Propranolol had no further effect in dogs pretreated with atenolol. 3. Practolol tended to cause smaller reductions in the haemodynamic parameters than either propranolol or atenolol. Subsequent administration of propranolol still had some depressant activity. 4. Pindolol produced a biphasic response, with depression of cardiac function at the low doses (0.025 and 0.1 mg/kg), but a reversal of effect as the dose was increased. 5. It is therefore concluded that, in anaesthetized dogs, the intrinsic activity of practolol and pindolol limits the fall in heart rate, cardiac conduction, aortic flow and maximal dp/dt observed with beta-adrenoceptor blockade. With pindolol, however, the influence of intrinsic activity is observed only in high doses related to beta-adrenoceptor blockade.
Clin
Exp Pharmacol Physiol
PMID:The influence of the intrinsic sympathomimetic activity of beta-adrenoceptor antagonists on haemodynamic effects in anaesthetized dogs. 3 81
A controlled clinical trial comparing inhalation of disodium cromoglycate (DSCG) and of
ICI
74,917 was carried out using a double-placebo technique in thirty-two patients with extrinsic asthma already shown to be reasonably responsive to DSCG. In view of the fact that
ICI
74,917 is 300 times more potent than DSCG in inhibiting antigenic challenge in animals a better effect was anticipated from the new drug in the human asthmatic subject. Whilst this was not obtained, there appeared to be no lesser effect than that of DSCG.
Clin
Allergy 1979 Jan
PMID:A controlled clinical trial comparing disodium cromoglycate and ICI 74,917 in extrinsic asthma. 10 25
The bronchial effect of intravenous atenolol (
ICI
66.082) has been studied in a double-blind cross over trial in 10 patients with pronounced, labile bronchial asthama. A single i.v. dose of atenolol 3 mg. sufficient to cause a fall in heart rate and systolic blood pressure at rest, induced only a slight and clincially almost negligible impairment of ventilatory function. An ordinary therapeutic dose of salbutamol by inhalation far outweighed the bronchial effect of atenolol. The drug appears promising with regard to its cardio-selective properties.
Eur J
Clin
Pharmacol 1977
PMID:Effect in bronchial asthma of a new beta-adrenergic blocking drug atenolol (ICI 66, 082). 31 6
Twenty-four patients with seasonal allergic rhinitis were treated in a randomized double-blind trial of 6 weeks' duration, using either
ICI
74,917 (0.5 mg in each nostril four times a day) or an identical placebo aerosol. Four patients receiving placebo were withdrawn from the trial because of the deteriorationin their rhinitis. The twelve patients using
ICI
74,917 were protected as assessed by a combined total symptom score, which was statistically significant (P less than 0.05), from weeks 1 to 4 when the pollen counts were highest.
Clin
Allergy 1977 Jul
PMID:A trial of ICI 74,917 in seasonal allergic rhinitis. 33 97
A study was made of the protective action of the anti-allergic drug
ICI
74,917, a phenanthroline derivative, in specific allergen provocation tests and in combating clinical symptoms in thirteen asthmatic out-patients. It was found that
ICI
74,917 was able to diminish allergen-induced bronchoconstriction significantly (P less than 0.01) during both the placebo period and during chronic treatment with
ICI
74,917 for 4 weeks. The results obtained during these two periods did not differ significantly. There was not, however, any statistically significant difference in the symptom scores or PEF rates during the treatment with
ICI
74,917 or placebo for 1 month. This may indicate that although
ICI
74,197 is able to prevent bronchoconstriction in an allergen provocation test, it failed to improve asthma clinically. No signs of the phenomenon of tachyphylaxis were observed in the present study. The Student's t-test was used in the statistical analysis.
Clin
Allergy 1978 May
PMID:The effect of ICI 74,917 on asthma and bronchial provocation tests. 66 2
Propranolol was given to 30 patients with essential hypertension following randomised, double-blind administration of either placebo or a new cardioselective beta-adrenergic receptor antagonist, atenolol (Tenormin,
ICI
66 082). Both atenolol and propranolol caused statistically significant reduction of recumbent and erect blood pressure and heart rate. There were no important differences between these variables on comparison of atenolol and propranolol.
Eur J
Clin
Pharmacol 1976 Mar 22
PMID:A comparison of the antihypertensive effect of atenolol (ICI 66 082) and propranolol. 78 62
1. Atenolol (
ICI
66.082, Tenormin) is a new beta-adrenoreceptor-blocking agent, devoid of intrinsic sympathomimetic and membrane-stabilizing properties. It does not cross the blood-brain barrier. 2. Atenolol given to hypertensive patients in initial open trials reduced arterial blood pressure significantly. 3. A double-blind comparison between atenolol and placebo in forty-five patients with essential hypertension demonstrated that atenolol gave a statistically significant reduction of blood pressure (delta 28/15 mmHg, P less than 0-005). 4. The optimum anti-hypertensive dose of atenolol in patients with mild to moderately severe essential hypertension was 200 mg daily. 5. Atenolol was compared with propranolol in thirty patients with essential hypertension. No statistically significant differences of anti-hypertensive effect were observed between the two drugs. 6. Long-term results (up to 2 years) in 117 hypertensive patients indicate that drug tolerance is good. No serious toxic effects were observed. 7. In four of twelve hypertensive patients with obstructive airways disease atenolol had to be withdrawn owing to deterioration of ventilatory function.
Clin
Sci Mol Med Suppl 1976 Dec
PMID:Clinical evaluation of atenolol in hypertension. 79 59
1 The pharmacokinetics of
ICI
74,917 were studied in both asthmatic patients and normal volunteers. 2 The tritiated compound was administered to the lungs by inhalation from an aerosol and a bronchoscope, and by intravenous, oral and buccal routes. Radioactivity was measured in plasma, urine, faeces, sputum and exhaled air. 3 After bronchoscopic administration 63% of the available dose was absorbed; after aerosol administration 8% was absorbed from the lung and more than 50% swallowed. 5 Intravenous studies indicated that the drug is excreted in the bile and urine in the ratio 2:1. 5 Minimal oral and no buccal absorption occurred. 6 There was no evidence of tritium exchange or drug metabolism. 7 The mean terminal half-life following administration by all route was 16.1 hours. However, the majority of the dose was rapidly excreted. 8 Aerosol administration is the method of choice for the clinical use of
ICI
74,917.
Br J
Clin
Pharmacol 1977 Jun
PMID:The absorption and elimination of ICI 74,917 in man. 90 4
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