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[Phentolamine in treatment of acute left ventricular insufficiancies].

Phentolamine (Regitine) at the dose of 0.3 mg/mn behaves as an arterial and, above all venous, vasodilatator agent, resulting in a marked and early lowering of the pulmonary pressures in acute oedema of the lung and in cardiac asthma. It was used alone in 47 attacks of acute severe left ventricular failure with very favourable results in 43 cases, as proved by the rapid improvement of the haemodynamic status and of the aicd-base balance. Under strict observation, tolerance has been excellent. This therapeutic method seems of great interest in the cases of acute pulmonary oedema with a maintained blood pressure level, and in the forms with severe arterial hypertension which might tolerate larger doses.

Acid-Base Equilibrium↗

Relation of age to effects of phentolamine and phenylephrine on heart.

In the present study, the responses of neonatal and adult dog hearts to phenylephrine (PE) and phentolamine (PA) were investigated in order to determine the influence of age factors. PA resulted in the slowing of the heart rate, the prolongation of corrected sinus node recovery time, atrial refractory period (ARP), ventricular effective refractory period (VERP), and ventricular functional refractory period (VFRP), and a significant inhibition of conducting tissues in neonatal dogs. In contrast, no such effects were seen in adult dogs. PE had a positive chronotropic effect in neonatal dogs but no such effect in adult dogs. In conclusion, alpha-adrenoceptors played an important excitatory role in the neonatal dog heart.

Age Factors↗

A pilot study of the role of intracavernous injection of vasoactive intestinal peptide (VIP) and phentolamine mesylate in the treatment of erectile dysfunction.

Twenty men with chronic impotence with a mean age of 46 years (range 26-63 y) were treated with self administration of 0.35 ml of Vasopotin 1 and 2, a combination of 30 mg Vasoactive Intestinal Peptide (VIP) and either 1.0 or 2.0 mg Phentolamine Mesylate. All patient were assessed using a standard protocol which included history and examination, vibratory penile biothesiometry, colour flow duplex Doppler ultrasonography and where indicated, Rigiscan nocturnal penile tumescence testing, dynamic infusion cavernosometry and cavernosography (DICC) and angiography. Impotence was classified as psychogenic in six patients, arteriogenic in nine patients, neurogenic in two patients and cavernosal venous leakage in three patients. A total of 60 injections was given. After sexual stimulation, an erection of sufficient rigidity for intercourse occurred in six patients with psychogenic impotence, seven of the nine patients with arteriogenic impotence, two patients with neurogenic impotence and one of three patients with cavernosal venous leakage. No patients experienced priapism, two patients complained of postinjection penile pain and three patients experienced transient facial flushing. Intracavernous self injection of Vasopotin appears to be a useful treatment for erectile dysfunction.

Adult↗

Comparative cardiovascular effects of SNP, ATP and phentolamine during norepinephrine-induced hypertension in dogs.

There has been no study comparing the advantage and disadvantage of various antihypertensive agents during surgery for pheochromocytomas because the study is difficult in clinical setting. In the present experiments using dogs, after increasing the arterial blood pressure with norepinephrine, we decreased it to the baseline with sodium nitroprusside (SNP), adenosine triphosphate (ATP), or phentolamine (PE) and compared the hemodynamic changes. A hyperdynamic state was found with ATP and with PE, but not with SNP. The norepinephrine-induced pulmonary hypertension could be successfully treated with SNP, but not with ATP or PE. The reason for these differences are thought to be the different vasodilative properties on peripheral arteries and veins. We conclude that agents that dilates the arteries and veins should be used to regulate the arterial pressure during surgical removal of a pheochromocytoma.

Journal Article↗

Vasa nervorum constriction from substance P and calcitonin gene-related peptide antagonists: sensitivity to phentolamine and nimodipine.

Previous work has suggested that vasa nervorum are 'tonically' vasodilated by substance P (SP) and calcitonin gene-related peptide (CGRP) arising from perivascular afferent nerve fibers. Local application of specific receptor antagonists of SP or CGRP results in constriction of vasa nervorum. In this work, we examined the responsiveness of vasa nervorum to epineurial spantide and spantide II (SP antagonists) and hCGRP (8-37) (CGRP antagonist) using serial hydrogen clearance curves in the rat sciatic nerve. Vasoconstriction from spantide and hCGRP (8-37) was dose-dependent, and was slightly greater with spantide than hCGRP (8-37). Spantide II induced vasoconstriction comparable to that of spantide. The vasoconstrictive effects of both spantide and hCGRP (8-37) were eliminated by concurrent systemic treatment with with either phentolamine or nimodipine. The findings support the hypothesis that SP or CGRP blockade interrupts 'tonic' peptide vasodilatation and permits vasoconstriction, perhaps by unopposed adrenergic action mediated through calcium channels. The findings however do not exclude a unique direct vasoconstrictive action of the peptide antagonists.

Animals↗

Simultaneous identification/determination system for phentolamine and sildenafil as adulterants in soft drinks advertising roborant nutrition.

An easily available, simultaneous identification/determination procedure for phentolamine (PHE) and sildenafil (SIL) in adulterated dietary supplements was established by using a combination of three different analytical methods; thin-layer chromatography (TLC), liquid chromatography-mass spectrometry (LC/MS) and a high-performance liquid chromatography (HPLC)/photo-diode-array. The sample solution for TLC was applied to silica gel 60 F(254) plates with chloroform/ammonia solution (28)/methanol (70:5:3, lower layer) and chloroform/diethylamine/methanol (15:3:2) as the developing solvent. Spots were located under UV radiation at 254 nm. Mass spectra of PHE and SIL by LC/MS were investigated with electrospray ionization (ESI) interface, under both positive and negative ion mode. The HPLC analysis was performed on a column of Wakosil 5C18 (4.6 mm x 150 mm, 5 microm) with water/methanol/acetonitrile/triethylamine (580:250:170:1) adjusted with phosphoric acid to pH 3.0 as the mobile phase, and the effluent was monitored with a photo-diode-array detector. Quantitative HPLC analysis of PHE and SIL were detected at 280 nm. When this procedure was applied to commercial soft drinks, PHE and SIL were identified and determined at a concentration of 17 mg PHE and 44 mg SIL per bottle, respectively. The procedure described here is available for the screening of PHE and SIL in adulterated supplements.

Journal Article↗

Hypertension following coronary artery bypass graft surgery: comparison of hemodynamic responses to nitroprusside, phentolamine, and converting enzyme inhibitor.

Sustained systemic hypertension (mean arterial pressure 119 +/- 4 mm Hg) developed in 39 patients undergoing coronary artery bypass graft (CABG) surgery. In groups of patients with comparable mean arterial pressure, left ventricular filling pressure, heart rate, and cardiac output, treatment with sodium nitroprusside (NP) in 20 patients, phentolamine (PH) in 10 patients and nonapeptide converting enzyme inhibitor (CEI) in nine patients uniformly lowered mean arterial pressure by 26, 21, and 20%, respectively. Cardiac output increased during NP (5.7 +/- 0.1 to 6.4 +/- 0.3 L/min, P < 0.0005) and after CEI (5.7 +/- 0.4 to 7.4 +/- 0.5 L/min, P < 0.0005) but not after PH (5.7 +/- 0.3 to 5.9 +/- 0.3 L/min, P > 0.05). Left ventricular filling pressure decreased in all groups (P < 0.005), but heart rate increased during NP (91.3 +/- 2.4 to 98.4 +/- 2.2 beats/min, P < 0.0005 and after PH (95.5 +/- 2.1 to 99.2 +/- 3.0, P < 0.005), while it was unchanged after CEI P > 0.05). Of the nine patients with CABG hypertension who received CEI, seven exhibited a mean decrease in arterial pressure of 18.5 +/- 3.4%, while in the remaining two patients, mean arterial pressure was decreased only 3.4%. In the former, the pretreatment mean plasma renin activity (PRA) was 7.5 +/- 2.4 ng/ml/hr, while in the latter, mean PRA was 1.3 ng/ml/hr.

Adult↗