An assessment of beta‐adrenoceptor blockade in man by SK &amp; F 92657, a new drug with combined vasodilator and beta‐adrenoceptor blocking actions, and comparison with propranolol [proceedings]

Pitcher, DW; Curry, PV; Trounce, J R

doi:10.1111/j.1365-2125.1980.tb04858.x

Cited by 6 publications

(3 citation statements)

References 4 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…When these results are compared to those obtained previously in this laboratory, using a similar technique, propranolol appears to be approximately ten times more potent on a weight for weight basis than SK & F 92657 in blocking the effects of isoprenaline on forearm blood flow. This difference in f8-adrenoceptor blocking potency cannot be accounted for solely in terms of molecular weight, but is of the same order as that seen after oral administration of the two drugs (Pitcher, Curry & Trounce, 1980).…”

Section: Discussonmentioning

confidence: 81%

Investigation of a combined arteriolar dilator and beta‐adrenoceptor antagonist (SK & F 92657) in the peripheral vessels of man.

Collier¹,

Pitcher²

1980

Brit J Clinical Pharma

Self Cite

View full text Add to dashboard Cite

1 SK & F 92657 is a new compound which in animals has both precapillary vasodilator and beta‐adrenoceptor blocking activity. The effects of the drug on forearm blood flow and dorsal hand vein distensibility have been studied in healthy volunteers. 2 Forearm blood flow was measured by venous occlusion plethysmography. The drug was infused directly into a brachial artery. The effects of SK & F 92657 on resting flow and on the dose‐response relationship for intra‐arterial isoprenaline were studied. 3 Venous distensibility was measured in the large veins on the back of the hand. The drug was infused directly into a selected vein and its effects on resting tone and on the responses to noradrenaline and to isoprenaline were investigated. 4 Intra‐arterial infusion of SK & F 92657 over 2 min caused a dose‐dependent increase in forearm blood flow which developed gradually to reach a maximum after approximately 40 min. Infusion into dorsal hand veins at 100 ng/min and 500 ng/min had no dilator effect in veins preconstricted with noradrenaline. At higher doses SK & F 92657 potentiated the constrictor effect of noradrenaline. 5 In both veins and arteries SK & F 92657 attenuated the dilator effects of isoprenaline. The drug had no effect on the venodilator effects of bradykinin, histamine or sodium nitroprusside. 6 The pattern of response of these vessels to locally infused SK & F 92657 is exactly that expected of a drug combining the properties of hydralazine‐like vasodilatation and beta‐adrenoceptor blockade. Furthermore, in the arterioles, both properties were manifest at the same dose.

show abstract

Section: Discussonmentioning

confidence: 81%

Investigation of a combined arteriolar dilator and beta‐adrenoceptor antagonist (SK & F 92657) in the peripheral vessels of man.

Collier¹,

Pitcher²

1980

Brit J Clinical Pharma

Self Cite

View full text Add to dashboard Cite

show abstract

“…In healthy normotensive subjects, prizidilol hydrochloride lowers blood pressure (Bell et al, 1979), and the ,3-adrenoceptor antagonist activity of single oral doses of 200 mg prizidilol hydrochloride assessed by inhibition of isoprenaline-induced tachycardia was found to be 52% of that seen with propranolol 40 mg (Pitcher, Curry & Trounce, 1979).…”

Section: Introductionmentioning

confidence: 97%

“…For this reason, a study was designed to test the effects of 400 mg of SK & F 92657 and either 25 mg or 50 mg of hydralazine combined with 40 mg of propranolol. The dose of propranolol was chosen in an attempt to produce equivalent ,3adrenoceptor antagonism to that of 400 mg prizidilol hydrochloride (Pitcher et al, 1979).…”

Section: Introductionmentioning

confidence: 99%

Comparison of prizidilol hydrochloride (SK & F 92657), a new antihypertensive agent with beta‐adrenoceptor antagonist and vasodilator activity with propranolol and hydralazine in normal volunteers.

Steiner¹,

Clancy²,

Manghani³

et al. 1981

Brit J Clinical Pharma

View full text Add to dashboard Cite

1 Some cardiovascular pharmacology of prizidilol hydrochloride, a new antihypertensive compound with precapillary vasodilator and ,3-adrenoceptor antagonist activity, in man is described.2 To investigate further the pharmacological profile of this drug the effects of a single oral dose of 400 mg prizidilol hydrochloride were compared with propranolol 40 mg in combination with either 25 mg or 50 mg of hydralazine for up to 6 h after dosing, in a placebo controlled study in eight healthy subjects. 3 Prizidolol hydrochloride significantly reduced supine and standing diastolic blood pressure and was more effective than propranolol combined with either dose of hydralazine in this respect. 4 Supine heart rate was significantly increasd after prizidilol hydrochloride, but was not significantly changed after propranolol combined with either dose of hydralazine. The reasons for the increase in supine heart rate after prizidolol are discussed. 5 /8-adrenoceptor antagonism was assessed in terms of inhibition of exercise induced increases in heart rate and systolic blood pressure. At the doses used, prizidolol hydrochloride was less effective than propranolol and hydralazine combined, particularly during the first 3 h after dosing.

show abstract

Prizidilol (SK & F 92657), a new vasodilator with beta-blocking properties in the treatment of essential hypertension

Lüscher

Havelka

Greminger

et al. 1982

Eur J Clin Pharmacol

View full text Add to dashboard Cite

The antihypertensive effect of a new vasodilator with betablocking properties (SK & F 92657) was investigated in 10 patients with mild to moderate essential hypertension. After a mean treatment period of 26,5 weeks (6,5-49 weeks) blood pressure was significantly reduced, from 168 +/- 22/106 +/- 6 mmHg to 144 +/- 19/94 +/- 12 mmHg (p less than 0.05 and 0.025). The mean dose was 410 mg (100-700 mg). Heart rate decreased slightly from 77 +/- 12 to 70 +/- 8 beats/min. Plasma renin activity and plasma aldosterone showed only minor changes. Nausea, heavy dreams, facial and hand flushing and mild depression were reported as side effects. In most patients the symptoms disappeared without reduction in the dose. In one patient anaemia developed after 7 weeks and treatment with prizidilol was stopped. A slight but statistically significant decrease in haemoglobin concentration of 1.1 +/- 0.6 g/dl was observed in 5 of the 10 patients (p less than 0.02). Thus, a mean dose of prizidilol of 410 +/- 242 mg/day had a mean blood pressure lowering effect of 24/12 mmHg. In 7 of the 10 patients (70%) diastolic blood pressure could be reduced to 95 mmHg or less. However, the observed haematological side-effects should be carefully monitored in further studies and may limit the clinical use of prizidilol.

show abstract

An assessment of beta‐adrenoceptor blockade in man by SK & F 92657, a new drug with combined vasodilator and beta‐adrenoceptor blocking actions, and comparison with propranolol [proceedings]

Cited by 6 publications

References 4 publications

Investigation of a combined arteriolar dilator and beta‐adrenoceptor antagonist (SK & F 92657) in the peripheral vessels of man.

Investigation of a combined arteriolar dilator and beta‐adrenoceptor antagonist (SK & F 92657) in the peripheral vessels of man.

Comparison of prizidilol hydrochloride (SK & F 92657), a new antihypertensive agent with beta‐adrenoceptor antagonist and vasodilator activity with propranolol and hydralazine in normal volunteers.

Prizidilol (SK & F 92657), a new vasodilator with beta-blocking properties in the treatment of essential hypertension

Contact Info

Product

Resources

About