Disease relevance of Losulazine

• The efficacy of losulazine was determined in 32 patients with hypertension [1].
• One subject receiving losulazine dropped out for personal reasons during the first week of the study, and the other subject (also taking losulazine) dropped out when a drug-related pruritus (itchy eyes) developed [1].
• Acute oral administration of doses of losulazine ranging from 0.1 to 30 mg/kg did not cause orthostatic hypotension [2].
• These results suggest that hyperprolactinemia mediated through hypothalamic dopamine depletion is the mechanism of anestrus in rats treated with losulazine [3].
• In the F1 mating portion of the postnatal and pre- and postnatal sections, F1 offspring from losulazine-treated dams had reduced body weights over the entire study [4].

High impact information on Losulazine

• Losulazine in the dosage range of 10 to 30 mg b.i.d. effectively lowered the blood pressure [1].
• A comparison of the profiles of effect of losulazine, guanethidine, guanadrel and reserpine on blood pressure, heart rate, blood pressure responses to norepinephrine and tyramine and blood pressure after desipramine pretreatment indicated that losulazine and reserpine had similar mechanisms of action [2].
• The data presented in this report are consistent with the conclusion that losulazine reduced arterial blood pressure in nonhuman primates via depletion of norepinephrine from postganglionic adrenergic neurons [2].
• Although variable, the acute hypotensive effects of losulazine were associated with both reductions of peripheral vascular resistance and reductions in cardiac output [2].
• These results suggest that regional differences in the response of aminergic neurons to acute administration of losulazine and reserpine reflect differences in the ability of these drugs to penetrate the blood-brain barrier [5].

Biological context of Losulazine

• Acute oral administration of losulazine at 0.1, 1, 10 and 30 mg/kg evoked dose-related hypotensive responses in the absence of significant alterations of heart rate [2].
• The mechanism of anestrus in rats treated with losulazine, a peripheral sympatholytic antihypertensive agent, was investigated by determining its effect on hypothalamic catecholamines and serum sex hormones and by evaluating the influence of bromocriptine on the reproductive functions of rats treated with losulazine [3].
• Rats treated with losulazine only were depleted of hypothalamic catecholamines, were hyperprolactinemic, and had interrupted estrous cycles and attenuated vaginal mucosa [3].
• Losulazine was administered orally to 21 bred Sprague-Dawley rats per group at 0, 4, and 8 mg/kg/day by three dosing schedules: gestation day 15 until term (prenatal section); postnatal days 1 to 21 (postnatal section); and gestation day 15 until postnatal day 21 (pre- and postnatal section) [4].
• Thus, although prenatal exposure only did not result in adverse effects, postnatal exposure to losulazine via lactation affected offspring growth, development, and reproductive capacity [4].

Anatomical context of Losulazine

• Quantitative evaluation of the different varieties of germ cells at stage VII of the seminiferous epithelium cycle and epididymal sperm count in all losulazine-treated rats revealed a persistant prominent detrimental change in spermatogenesis [6].

Associations of Losulazine with other chemical compounds

• Both animal pharmacology and clinical experience suggest that losulazine hydrochloride may be free of the clinically limiting side effects that often plague compounds that decrease blood pressure by interfering with autonomic neurogenic function [7].

Gene context of Losulazine

• Study on the activities of testes and accessory sex glands after losulazine treatment in rats [6].
• Blood pressure, heart rate, plasma renin activity, and plasma catecholamines were monitored before and after the oral administration of losulazine at a dose which caused a submaximal hypotension in sodium-replete monkeys [8].

Analytical, diagnostic and therapeutic context of Losulazine

• Mean body weights were statistically significantly greater and mean gestation periods were statistically significantly longer in losulazine-treated females than in females of the vehicle control group [9].

References