The Pharmacologic Effects of ST-155 (Catapres) and Related Imidazolines in the Rat

Hm, Maling; Ak, Cho; Horakova, Z; Ma, Williams

doi:10.1159/000136038

Cited by 18 publications

(3 citation statements)

References 16 publications

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“…Naphazoline systemic effects in otolaryngology may be due to direct adsorption into the nasal mucosa, and partial absorption of the drug when swallowed into the stomach [17]. Naphazoline hypotensive activity was established experimentally in the early stages of its study in dogs [7], cats [49] and rats [20]. In experimental conditions of naphazoline concentrations ranging from 0.5 mM to 10 mM in a normal MacEwen solution, cardiac contractures were induced in rats and guinea pigs.…”

Section: Current Issues In Pharmacy and Medical Sciencesmentioning

confidence: 99%

Rationale for naphazoline effects in-depth study

Kuzminov

Turkina

Кuzminov

2018

Current Issues in Pharmacy and Medical Sciences

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This article presents a retrospective review of data on side effects of drugs containing naphazoline and data on toxicity of the agent when entered the body via different pathways. Most publications on clinical signs of possible naphazoline-associated side effects are lacking thorough analysis of possible causes. Limited data on the pharmacokinetics and pharmacodynamics of the drug led to various complications after its administration. Therefore, further studies on naphazoline content dynamics or products of its biotransformation in biological substrates and determination of half-life of the agent must be conducted. This will allow establishingsafe levels for different exposure pathways and harmful levels of the naphazoline with respect to its material accumulation. It should be noted that scientific publications contain controversial data regarding allergenic potential of the agent. Possible side effects of the drug on the reproductionand development are not revealed. Determination of effects the products containing naphazoline may have on immune and reproductive system is an important part of the research.

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Section: Current Issues In Pharmacy and Medical Sciencesmentioning

confidence: 99%

Rationale for naphazoline effects in-depth study

Kuzminov

Turkina

Кuzminov

2018

Current Issues in Pharmacy and Medical Sciences

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“…The discrepancy could be dose-related since clonidine has been shown to possess a dual effect upon the alpha-adrenergic receptors. In small amounts it acts as an alpha-adrenergic receptor agonist (15), while in larger doses as an antagonist (8,12). These properties of clonidine could explain its different effect upon the blood pressure in the two groups of animals.…”

Section: Bmentioning

confidence: 99%

Water Diuresis from Clonidine (Catapres)

Chrysanthakopoulos¹,

Lavender²

1975

Experimental Biology and Medicine

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Available clinical and experimental evidence indicates that clonidine 2-2(2,6-di-ch1orophenylamino)-2 imidazoline hydrochloride, has potent hypotensive, bradycardic and bradypneic properties (1-6). It also produces sedation and local anesthesia, inhibits gastric acid secretion, and raises blood sugar (7). Its effect on blood pressure in the anesthetized dog is a bimodal one. An initial short rise is followed by a prolonged decrease. Similar observations have been reported in the rabbit, rat, and cat (8,9). Concerning the actions of clonidine upon renal hemodynamic and excretory functions, it was shown by Onesti et al. (6) that when the drug was given either orally or intravenously to dogs and man, it had no effect on the effective renal plasma flow, glomerular filtration rate, and potassium excretion, while it decreased the excretion of sodium and chloride. The pathophysiologic mechanism by which clonidine exerts its renal effects has not as yet been elucidated. The purpose of this study, therefore, was to attempt to clarify if clonidine has any direct renal effect by infusing the drug in small amounts into the renal artery of one kidney of the anesthetized dog and comparing its effects against the other kidney without disturbing systemic hemodynamics. In a second group of animals the drug was given intravenously in order to study the systemic effects and significance of a different route of administration.Materials and methods. Sixteen well-conditioned dogs of both sexes weighing 22-25 kg were used in this study. The animals were anesthetized with sodium pentobarbital (30 mg/kg) and kept lightly anesthetized for the whole length of the experiments. All the animals were intubated and ventilated with room air. The jugular vein and the external carotid artery were exposed and catheterized with polyethylene tubing for con-tinuous infusion and monitoring of the blood pressure, respectively. The dogs were primed with a solution containing inulin and paraaminohippuric acid (PAH) in isosmotic saline. Thereafter the dogs were maintained with a sustaining solution of similar composition but different concentration administered at a rate of 6.0 ml/min, in order to maintain the dog's blood levels of inulin and PAH at 25-30 mg% and 2-4 mg%, respectively.A mercury manometer was connected to the external carotid artery for continuous monitoring of the blood pressure and blood sampling from a manifold. Both ureters were exposed through a midline incision and catheterized with polyethylene tubing for continuous urine collection into graduated cylinders. In 10 dogs (Group 1) the right renal artery was exposed through a left flank incision and cannulated through the abdominal aorta with an 18-gauge Rochester needle for infusion of the drug. In six dogs (Group 2) the drug was given intravenously. The experiments in both groups were divided into a control and experimental period. The control period consisted of four urine collections 20 min each and the experimental period of six collections 20 min each also. Blood for clearances of...

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“…Intravenous administration of clonidine (Catapres) produces initial sympathomimetic effects by stimulating ai-adrenoceptors (Maling, Cho, Horakova & Williams, 1969) followed by hypotension and bradycardia which have been ascribed to a central action (Sherman, Greca, Woods & Buckley, 1968;Shaw, Hunyor & Korner, 1971). Hukuhara, Otsuka, Tadeka & Sakai (1968) and Schmitt & Schmitt (1969) reported an inhibition of the action potentials in the splanchnic and cardiac nerves following central administration of clonidine.…”

Section: Introductionmentioning

confidence: 99%

Effect of Clonidine on the Excitability of Vasomotor Loci in the Cat

Johri

Singh

et al. 1975

British J Pharmacology

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1The effect of clonidine on the direct excitability of hypothalamic, medullary and spinal vasomotor loci has been investigated in cats anaesthetized with chloralose. 2 Clonidine inhibited the excitability of these loci when it was localized to the central sites by intracerebroventricular, intravertebral arterial or intrathecal injection in very low doses (1-2 jg). 3 Topical application of clonidine (0.01% and 1.0%) to the floor of the fourth ventricle inhibited pressor responses evoked either by stimulation of medullary or hypothalamic vasomotor areas. Inhibition of the pressor responses was accompanied by hypotension and bradycardia in many experiments. 4 It appears that effects of clonidine on the vasomotor loci of the medulla oblongata and the spinal cord contribute to its hypotensive action.

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The Pharmacologic Effects of ST-155 (Catapres) and Related Imidazolines in the Rat

Cited by 18 publications

References 16 publications

Rationale for naphazoline effects in-depth study

Rationale for naphazoline effects in-depth study

Water Diuresis from Clonidine (Catapres)

Effect of Clonidine on the Excitability of Vasomotor Loci in the Cat

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