Disease relevance of amezinium

• We examined the short-term effects of amezinium in five patients with severe neurogenic orthostatic hypotension [1].
• Repeated administration of amezinium (10 to 40 mg/d) produced an increase in sitting blood pressure in three patients and improvement of the orthostatic symptoms in all patients without remarkable recumbent hypertension [1].
• Leg ulceration during amezinium methylsulfate therapy for hypotension in a hemodialyzed patient with generalized vascular calcification [2].
• 6. The acute toxicity of amezinium in mice and rats was low [3].
• 1. The most conspicuous action of amezinium was in modifying reserpine-induced ptosis and reserpine-induced hypothermia [3].

High impact information on amezinium

• The results show that amezinium, at least at low concentrations, is selectively taken up released by action potentials [4].
• The results also confirmed previous reports that amezinium is highly selective for MAO-A [5].
• In the present study, the effects of amezinium on the deamination of noradrenaline were investigated in intact lungs of rats, since the pulmonary endothelial cells are a site where the catecholamine transporter is non-neuronal uptake1 [5].
• No decrease in [123I]MIBG accumulation was resulted from drug therapy (droxidopa, amezinium and thyrotropin-releasing hormone) [6].
• On the mechanism of action of amezinium methylsulphate on the dog saphenous vein [7].

Chemical compound and disease context of amezinium

• Etilefrine and Amezinium are used during pregnancy to prevent hypotension and fetal growth retardation [8].

Biological context of amezinium

• The effect of amezinium on the pre-ejection period corrected for heart rate (PEPc) and mean velocity of fiber shortening (VCFmean) indicated positive inotropic properties [9].
• Change in stroke volume in 6 healthy volunteers was induced by passive head-up tilting (80 degrees) and by oral administration of the sympathomimetic drug amezinium [10].
• Before and 2 h after oral administration of amezinium 30 mg or placebo the cardiovascular responses to orthostatic stress, induced by 80 degrees passive head-up tilt, were assessed by recording blood pressure, systolic time intervals, and echocardiogram [9].
• Pharmacokinetics of amezinium in man [11].
• These properties and the characteristics of amezinium with respect to absorption, bioavailability and elimination are considered favourable for safe and effective handling of the drug [12].

Anatomical context of amezinium

• Pharmacological effect of amezinium on urethra and bladder of rabbits [13].
• Determination of amezinium in body fluids [14].
• In rat blood amezinium distributes between erythrocytes and plasma with a ratio of 2.7:1; the proportion bound to plasma proteins is about 20% [15].
• In feces, MIII and the unchanged amezinium were found [16].
• 2. Amezinium itself is taken up into synaptosomes [17].

Associations of amezinium with other chemical compounds

• Etilefrine and amezinium reduce uterine blood flow of pregnant guinea pigs [8].
• Direct effect of amezinium on rabbit urethra: effect of estrogen and progesterone treatment [18].
• The pharmacokinetics of the antihypotensive drug 4-amino-6-methoxy-1-phenyl-pyridazinium methyl sulfate (ameziniummetilsulfate, LU 1631, Regulton), in the following briefly called amezinium, has been investigated in 8 healthy volunteers [12].
• Resting heart rate decreased after injection of PCB, AMZ, DHE, and MDD [19].
• The results show amezinium to have potent, long-lasting blood pressure increasing and positive inotropic actions in man after oral as well as parenteral administration [20].

Gene context of amezinium

• 4. Amezinium inhibits MAO-A in rat heart homogenate with a Ki of 3 x 10(-6) mol/l and MAO-B in liver homogenate with a Ki of 3 x 10(-4) mol/l; the inhibition is reversible [17].
• 5. Renal clearance of amezinium is not constant [11].

Analytical, diagnostic and therapeutic context of amezinium

• Together with findings from animal experiments the results are used to describe the pharmacokinetic behaviour of amezinium in man at the present state of knowledge: 1 [11].
• Absolute bioavailability of amezinium. A cross-over study after i.v. and p.o. application [21].
• Determination of amezinium in plasma by RP HPLC and its application to bioequivalence studies [22].
• Although amezinium enhances muscle contractile responses to electrical stimulation, this effect is strong when amezinium is used alone; concurrent estrogen treatment improves the effects of amezinium [18].

References