14 research outputs found
Experimental Goettingen minipig and beagle dog as two species used in bioequivalence studies for clinical pharmacology (5-aminosalicylic acid and atenolol as model drugs). Gen Physiol Biophys 18: 80–85
Abstract. Due to proven similarities in biotransformation between man and mini pig, minipig seems to be the experimental animal of choice for preclinical phar macokinetic studies when an experiment with a drug exhibiting a great first pass bioelimination (like 5-aminosalicylic acid) is to be realised. On the other hand, both minipig and dog may be suitable species for a pharmacokinetic study with a drug characterized by a small extent of first pass biotransformation (like atenolol)
Axolotl as a Model to Study Scarless Wound Healing in Vertebrates: Role of the Transforming Growth Factor Beta Signaling Pathway
The influence of streptococcal peptidoglycane on neonate pharmacokinetics of trimethoprim
Miotic action of tramadol is determined by CYP2D6 genotype
Polymorphic CYP2D6 is the enzyme that activates the opioid analgesic tramadol by O-demethylation to M1. Our objective was to determine the opioid effects measured by pupillary response to tramadol of CYP2D6 genotyped volunteers in relation to the disposition of tramadol and M1 in plasma. Tramadol displayed phenotypic pharmacokinetics and it was possible to identify PM subjects with >99% confidence from the metabolic ratio (MR) in a single blood sample taken between 2.5 and 24 h post-dose. Homozygous extensive metabolizers (EM) differed from poor metabolizers (PM), with an almost three-fold greater (P=0.0014) mean maximal pupillary constriction (Emax). Significant correlations between the AUC and Cmax values of M1 versus pupillary constriction were found. The corresponding correlations of pharmacokinetic parameters for tramadol itself were weaker and negative. The strongest correlations were for the single-point metabolic ratios at all sampling intervals versus the effects, with rs ranging from 0.85 to 0.89 (p0.01). It is concluded that the concept of dual opioid/non-opioid action of the drug, though considerably stronger in EMs, is valid for both EM and PM subjects. This is the theoretical basis for the frequent use and satisfactory efficacy of tramadol in clinical practice when given to genetically non-selected population
Hepatotoxicity of Diazepam Structural and Trace Metal Studies in Rat
Studies of effects of diazepam on liver parenchyma are very
scanty. In this study, adult albino rats were treated with diazepam in
two different doses (0.25 mg and 0.30 mg/kg body wt) daily for 30
and 60 d. Through light microscopy and electron microscopy,
prenecrotic and necrotic changes were noted in the high-dose group.
Trace metal analysis indicated that zinc (Zn) was reduced by 30 and
60 day under both the doses, whereas iron (Fe) and copper (Cu) were
reduced significantly in these groups only after 60 d of treatment.
This reduction in metal contents may have some correlations with
necrotic changes in liver parenchyma