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Pharmacokinetics and bioavailability...

Mahmood, Iftekhar.

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Pharmacokinetics and bioavailability of selegiline in the dog using an enzymatic assay.

Record Type:	Electronic resources : Monograph/item
Title/Author:	Pharmacokinetics and bioavailability of selegiline in the dog using an enzymatic assay./
Author:	Mahmood, Iftekhar.
Description:	162 p.
Notes:	Source: Dissertation Abstracts International, Volume: 54-11, Section: B, page: 5615.
Contained By:	Dissertation Abstracts International54-11B.
Subject:	Health Sciences, Pharmacy. -
Online resource:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=9409423

Pharmacokinetics and bioavailability of selegiline in the dog using an enzymatic assay.
Mahmood, Iftekhar.

Pharmacokinetics and bioavailability of selegiline in the dog using an enzymatic assay. - 162 p.

Source: Dissertation Abstracts International, Volume: 54-11, Section: B, page: 5615.

Thesis (Ph.D.)--University of Missouri - Kansas City, 1993.

The clinical features of Parkinsonism result from a depletion of dopamine transmission in the corpus striatum; the dopamine deficiency is caused by a loss of melanin-containing nerve cells within the substantia nigra. Though the mainstay of the therapy is levodopa, selegiline is beneficial to parkinsonian patients as an adjuvant to levodopa therapy. Selegiline acts by inhibiting Monoamine oxidase-B (MAO-B), thus elevating the dopamine concentration in the brain. Selegiline is also being evaluated in veterinary medicine for treatment of Cushing's syndrome and reduce the symptoms of cognitive dysfunction in the dog. A dose of 2 mg/kg orally to dogs has assisted in reducing memory loss. Currently no pharmacokinetics data is available for selegiline in the literature, mainly due to lack of analytical methods which can measure concentrations less than 10 ng/ml in plasma.Subjects--Topical Terms:

1017737
Health Sciences, Pharmacy.

Pharmacokinetics and bioavailability of selegiline in the dog using an enzymatic assay.
LDR:03093nmm 2200277 4500 001 1839459
005 20050624104406.5
008 130614s1993 eng d
035 $a (UnM)AAI9409423
035 $a AAI9409423
040 $a UnM $c UnM
100 1 $a Mahmood, Iftekhar. $3 1927849
245 1 0 $a Pharmacokinetics and bioavailability of selegiline in the dog using an enzymatic assay.
300 $a 162 p.
500 $a Source: Dissertation Abstracts International, Volume: 54-11, Section: B, page: 5615.
502 $a Thesis (Ph.D.)--University of Missouri - Kansas City, 1993.
520 $a The clinical features of Parkinsonism result from a depletion of dopamine transmission in the corpus striatum; the dopamine deficiency is caused by a loss of melanin-containing nerve cells within the substantia nigra. Though the mainstay of the therapy is levodopa, selegiline is beneficial to parkinsonian patients as an adjuvant to levodopa therapy. Selegiline acts by inhibiting Monoamine oxidase-B (MAO-B), thus elevating the dopamine concentration in the brain. Selegiline is also being evaluated in veterinary medicine for treatment of Cushing's syndrome and reduce the symptoms of cognitive dysfunction in the dog. A dose of 2 mg/kg orally to dogs has assisted in reducing memory loss. Currently no pharmacokinetics data is available for selegiline in the literature, mainly due to lack of analytical methods which can measure concentrations less than 10 ng/ml in plasma.
520 $a A sensitive fluorometric assay based on inhibition of rat brain Monoamine oxidase-B (MAO-B) in vitro has been described. The procedure measures the inhibition of MAO-B activity produced by the addition of selegiline extracted from plasma. Selegiline concentrations as low as 0.25 ng/ml can be detected. The standard curve was linear from 125 picogram (0.25 ng/ml) to 4000 picogram (8.0 ng/ml) in the incubation tube.
520 $a The pharmacokinetics of selegiline were investigated following intravenous and oral administration to four female mongrel dogs. Each dog received 1 mg/kg selegiline in solution via gavage or by intravenous administration in cross-over studies separated by one week. Plasma samples were analyzed by the enzymatic method. The mean terminal half-life, the volume of distribution of central compartment and systemic clearance of selegiline were 56.04 $\ pm $ 16.59 minutes, 6299 $\ pm $ 438 ml/kg and 160.19 $\ pm $ 19.81 ml/min/kg respectively. After oral administration, selegiline appeared to be absorbed rapidly from the gastrointestinal tract. Absorption appears to follow zero order kinetics with a T $\ sb{\rm max} $ and C $\ sb{\rm max} $ of 25 $\ pm $ 5.8 min and 4.91 $\ pm $ 1.36 ng/ml, respectively. The bioavailability of selegiline in the dog was 7.52 $\ pm $ 2.08%, which is consistent with extensive presystemic metabolism. (Abstract shortened by UMI.)
590 $a School code: 0134.
650 4 $a Health Sciences, Pharmacy. $3 1017737
650 4 $a Biology, Veterinary Science. $3 1021733
650 4 $a Health Sciences, Pharmacology. $3 1017717
690 $a 0572
690 $a 0778
690 $a 0419
710 2 0 $a University of Missouri - Kansas City. $3 1021712
773 0 $t Dissertation Abstracts International $g 54-11B.
790 $a 0134
791 $a Ph.D.
792 $a 1993
856 4 0 $u http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=9409423