In vivo assessment of hepatic and extrahepatic first pass effect of salbutamol (SALB) in anesthetized rabbits

Perreault, Sylvie; Dumont, Louis; Ong, Huy; Souich, P. du

doi:10.1016/0014-2999(90)93248-o

Cited by 6 publications

(12 citation statements)

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“…11 This is supported by the fact that sulfo-conjugates represent the major form of salbutamol-conjugates excreted in rabbits 8 and humans. 12 Thus, it is necessary to develop and pharmacologically characterize new drugs that show affinity, selectivity, and potency in their action on  2 AR, and which also have longer duration (half-life) in the organism and fewer side effects than the agonists currently employed.…”

Section: Introductionmentioning

confidence: 94%

“…The methodology described by Perreault et al 8,18 was used for collecting samples. Thus, each of the animals received a 0.1 mg/kg dose of R-salbutamol or BR-AEA via the ear vein.…”

Section: Pharmacokinetics Of Br-aeamentioning

confidence: 99%

“…9,18 Additionally, intravenous and endotracheal administrations have shown similar bioavailability for salbutamol. 8 Accordingly, a cannula was inserted into the contralateral ear marginal vein to sample blood, and rabbits were maintained in restriction boxes. Blood samples (3 mL) were withdrawn via the ear vein at predetermined time intervals up to 24 h after drug administration.…”

Section: Pharmacokinetics Of Br-aeamentioning

confidence: 99%

“…6 Another disadvantage is that this  2 AR agonist has a short half-life, 7 due to its fast metabolism in the intestine, liver, and lung (in order of capacity for the metabolism of salbutamol). 8 Intestinal metabolism is triggered with oral administration but can be avoided with intravascular and inhaled administration.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol derivative) in rabbit

Soriano-Ursúa¹,

Correa‐Basurto²,

Romero-Huerta³

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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Section: Introductionmentioning

confidence: 94%

“…The methodology described by Perreault et al 8,18 was used for collecting samples. Thus, each of the animals received a 0.1 mg/kg dose of R-salbutamol or BR-AEA via the ear vein.…”

Section: Pharmacokinetics Of Br-aeamentioning

confidence: 99%

Section: Pharmacokinetics Of Br-aeamentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol derivative) in rabbit

Soriano-Ursúa¹,

Correa‐Basurto²,

Romero-Huerta³

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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show abstract

“…7 The complex architecture of lungs reflects over 40 different cell types with remarkable diversity in cell functionality and is capable of extracting drugs from the blood circulation because all the cardiac output goes through it. 8,9 7,12-Dimethylbenz(a)anthracene (DMBA) is a class of polycyclic aromatic hydrocarbon (PAH). It is absorbed mainly through the skin, respiratory, intestinal tracts; by ingestion and inhalation.…”

Section: Introductionmentioning

confidence: 99%

Effect of 3β, hydroxy-lup-20(29)-en-28-oic acid on 7,12-Dimethylbenz(a) anthracene impaired cellular homeostasis in extrahepatic organs of Sprague Dawley rats

Kaur

Arora

et al. 2017

J Xenobiotics

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Abstract3β, hydroxy-lup-20(29)-en-28-oic acid (Betulinic acid), a pentacyclic lupane-type triterpene has diverse pharmacological functions both in vitro and in vivo. The present study focuses its protective effect on polycyclic aromatic hydrocarbon (7,12-Dimethylbenz(a)anthracene or DMBA) induced alterations in membrane bound ATPases, detoxification enzymes and antioxidant enzymes in stomach and lungs of female Sprague Dawley rats. Healthy female Sprague Dawley rats were randomly assorted into six groups and the treatments were given orally for 7 weeks on alternate days. It was observed that betulinic acid facilitated the downregulation of elevated membrane bound ATPases (Na + /K + -ATPase, Ca 2+ -ATPase and Mg 2+ -ATPase) in DMBA administered rats. Likewise, the detoxification enzymes as well as antioxidant enzymes were modulated to normalcy in rats. Overall, betulinic acid was seen to be effective modulator of DMBA induced alterations in biochemical parameters.

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Extrahepatic metabolism of frusemide in anaesthetized rabbits

Vergés

Héroux

Maurice

et al. 1995

British J Pharmacology

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Frusemide is removed from the body by biotransformation and renal secretion, but since frusemide metabolism is not altered in patients with hepatic cirrhosis, the role of the liver may be questioned. The aim of the study was to investigate which organs contribute to the first‐pass metabolism and systemic clearance of frusemide. Groups of anaesthetized New Zealand rabbits were administered frusemide proximally (prox) and distally (dist) to different organs, and blood was sampled from the abdominal aorta. The area under frusemide plasma concentrations‐time curve (AUC0‐∞) was calculated and frusemide extraction by an organ was estimated from the ratio (AUCdist‐AUCprox)/AUCdist. The small intestine extracted 83% of the absorbed dose of frusemide but the first‐pass uptake by the liver and lungs was negligible. To assess the contribution of the intestine and the kidneys to the systemic clearance of frusemide, it was injected into the jugular vein and blood was sampled proximal and distal to each organ. The kidneys extracted 24% of frusemide circulating in the renal arteries; on the other hand, the ability of the intestine to extract frusemide from the systemic circulation could not be detected. The lungs did not metabolize frusemide in vitro; the rate of metabolism of frusemide in vitro by kidneys was similar to that estimated in the intestine, and both rates were faster (P<0.05) than that observed in the liver. It is concluded that in rabbits, presystemic metabolism of frusemide is carried out by the intestine, and that systemic clearance of frusemide is mainly performed by the kidneys, although other organs, such as the intestine and the liver, must contribute to it.

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In vivo assessment of hepatic and extrahepatic first pass effect of salbutamol (SALB) in anesthetized rabbits

Cited by 6 publications

References 0 publications

Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol derivative) in rabbit

Pharmacokinetic parameters and a theoretical study about metabolism of BR-AEA (a salbutamol derivative) in rabbit

Effect of 3β, hydroxy-lup-20(29)-en-28-oic acid on 7,12-Dimethylbenz(a) anthracene impaired cellular homeostasis in extrahepatic organs of Sprague Dawley rats

Extrahepatic metabolism of frusemide in anaesthetized rabbits

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