Brain distribution and kinetics of desipramine in the rat

1981 ◽  
Vol 59 (2) ◽  
pp. 163-167 ◽  
Author(s):  
P. D. Hrdina ◽  
T. C. Dubas
Keyword(s):  
Single Dose ◽  
Peak Plasma ◽  
Intraperitoneal Administration ◽  
Brain Homogenate ◽  
Repeated Administration ◽  
Pharmacological Action ◽  
Male Rats ◽  
Brain Distribution ◽  
Kinetics Of ◽  
Critical Portion

Pharmacokinetics and regional as well as subcellular brain distribution of desipramine (DMI) were investigated in male rats after single and repeated intraperitoneal administration. After a single dose DMI enters brain rapidly, accumulates with increasing the dose, and attains concentrations about 20 times those seen in plasma. After repeated administration peak plasma and brain levels were 2.7 and 3.7 times, respectively, higher than after a single dose. No significant regional differences were found in brain distribution or disappearance half-lives of the drug. After chronic treatment the drug was preferentially retained in the P2 fraction of brain homogenate; this may reflect the critical portion of drug bound to sites responsible for its pharmacological action.

scholarly journals Inhibition by insulin of the formation of autophagic vacuoles in rat liver. A morphometric approach to the kinetics of intracellular degradation by autophagy.

1978 ◽  
Vol 78 (1) ◽  
pp. 152-167 ◽  
Author(s):  
U Pfeifer
Keyword(s):  
Half Life ◽  
Intraperitoneal Administration ◽  
Male Rats ◽  
Electron Microscopic ◽  
Autophagic Vacuoles ◽  
Intracellular Degradation ◽  
First Order Kinetics ◽  
Different Types ◽  
Electron Microscopic Morphometry ◽  
Kinetics Of

Electron microscopic morphometry has demonstrated a rapid decrease in the fractional volume of autophagic vacuoles (AV) in hepatocytes of adult male rats after the intraperitoneal administration of insulin (5 U/kg of body weight). Except for a significant decrease in glycogen to about one-half its initial value, no major changes in the composition of the remaining cytoplasm, or in the average volume of the single hepatocyte, were seen. The decrease found in the AVs is attributed to an inhibition of the formation of new AVs-probably the morphologic counterpart of the well-known anticatabolic effects of insulin. The decay of the fractional volume of the AVs appeared to follow first-order kinetics. Thus, the termination of the "life" of an AV by destruction of its contents may not depend directly on the "age" of the AV. The average half-life of the AVs amounted to approximately 9 min. Similar values were found for the different types of AVs, except for those containing glycogen. The half-life of these AVs was approximately 18 min. From the half-life values and from the "segregated fractions" at time zero, which were different for the different cytoplasmic components, rates of removal from the cytoplasm by autophagy were calculated. Expressed as "percent per day", the following rates were found: whole cytoplasm, 2.3; mitochondria, 3.9; microbodies, 8.9; and glycogen, 1.1. The results indicate that autophagy, to some extent, is selective and plays an important, but not an exclusive, role in intracellular turnover.

Protective effect of green tea extract against cadmium-induced testicular damage in rats in respect of oxidant/antioxidant equilibrium and androgen production

2020 ◽  
Vol 21 (1) ◽  
pp. 31-35
Author(s):  
Basma El-Desoky ◽  
Shaimaa El-Sayed ◽  
El-Said El-Said
Keyword(s):  
Gene Expression ◽  
Single Dose ◽  
Green Tea ◽  
Serum Testosterone ◽  
Green Tea Extract ◽  
Male Rats ◽  
Controlled Study ◽  
Control Group ◽  
Testicular Damage ◽  
Tea Extract

Objective: Investigating the effect of green tea extract (GTE) on the testicular damage induced by cadmium chloride CdCl2 in male rats. Design: Randomized controlled study. Animals: 40 male Wistar rats. Procedures: Rats were randomly divided into four groups: A) control group (each rat daily received pellet diet); B) GTE group each rat daily received pellet diet as well as 3 ml of 1.5 % w/v GTE, C) CdCl2 group each rat was I/P injected a single dose of 1 mg/kg CdCl2, then daily received pellet diet, and D) CdCl2+GTE group each rat was I/P injected a single dose of 1 mg/kg CdCl2 then daily received pellet diet as well as 3 ml of 1.5 % w/v GTE. After 30 days, blood samples were collected for hormonal assays (testosterone, FSH, and LH). In addition, both testes were collected; one of them was used for quantification of 17-beta hydroxysteroid dehydrogenase III (17β-HSDIII) gene expression using a real-time PCR. The other testis was used for determination of catalase and reduced glutathione; GSH, Nitric oxide (NO) and malondialdehyde (MDA) levels. Results: CdCl2 decreased serum testosterone levels and its synthesis pathway (17β-HSDIII testicular gene expression). While antioxidants catalase and GSH were reduced, oxidants MDA were enriched in the testes of CdCl2-poisoned rats. This CdCl2-promoted testicular dysfunction was corrected via the administration of GTE to male rats. Conclusion and clinical relevance: GTE could be used as a remedy for protecting against CdCl2-induced testicular damage in male rats.

Potential anti-toxic effect of d-ribose-l-cysteine supplement on the reproductive functions of male rats administered cyclophosphamide

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Gabriel O. Oludare ◽  
Gbenga O. Afolayan ◽  
Ganbotei G. Semidara
Keyword(s):  
Body Weight ◽  
Single Dose ◽  
Sperm Motility ◽  
Sperm Count ◽  
Male Rats ◽  
Oxidative Enzymes ◽  
Protective Effects ◽  
Testosterone Levels ◽  
Group I ◽  
Antioxidant Defence System

Abstract Objectives This study aimed to access the protective effects of d-ribose-l-cysteine (DRLC) on cyclophosphamide (CPA) induced gonadal toxicity in male rats. Methods Forty-eight male Sprague-Dawley rats were divided into six groups of eight rats each. Group I the control, received distilled water (10 ml/kg), Group II received a single dose of CPA 100 mg/kg body weight intraperitoneally (i.p), Groups III and IV received a single dose of CPA at 100 mg/kg (i.p) and then were treated with DRLC at 200 mg/kg bodyweight (b.w) and 400 mg/kg b.w for 10 days, respectively. Rats in Groups V and VI received DRLC at 200 and 400 mg/kg b.w for 10 days, respectively. DRLC was administered orally. Results Results showed that CPA increased percentage of abnormal sperm cells and reduced body weight, sperm count, sperm motility, follicle-stimulating hormone (FSH), luteinizing hormone (LH) and testosterone levels (p<0.05). CPA also induced oxidative stress as indicated by the increased malondialdehyde (MDA) content and reduced activities of the oxidative enzymes measured (p<0.05). Liver enzymes were elevated while the blood cells production was decreased in the rats administered CPA. DRLC supplementation enhanced the antioxidant defence system as indicated in the reduced MDA levels and increased activities of the antioxidant enzymes when compared with CPA (p<0.05). Bodyweight, sperm count, sperm motility, FSH, and testosterone levels were increased in the CPA + DRLC II group compared with CPA (p<0.05). Conclusions The results of this present study showed that DRLC has a potential protective effect on CPA-induced gonadotoxicity.

Chronopharmacology of β-Adrenoceptor-Blocking Drugs: Pharmacokinetic and Pharmacodynamic Studies in Rats

1983 ◽  
Vol 2 (6) ◽  
pp. 347-358 ◽  
Author(s):  
B. Lemmer ◽  
K. Bathe ◽  
P. H. Lang ◽  
G. Neumann ◽  
H. Winkler
Keyword(s):  
Treatment Time ◽  
Human Subjects ◽  
Temporal Variations ◽  
Male Rats ◽  
Pharmacokinetic Parameters ◽  
Nonspecific Effects ◽  
Elimination Half ◽  
Receptor Blockers ◽  
Β Receptor ◽  
Kinetics Of

Specific and nonspecific effects and the pharmacokinetic behavior of β-adrenoceptor-blocking drugs of different Iipophilicity (atenolol, bupranolol, carazolol, metoprolol, ox-prenolol, practolol, propranolol, sotalol) were investigated in L-D-synchronized male rats as a function of treatment time. The studies revealed that pharmacodynamic effects on heart rate, cardiac noradrenaline turnover, and motor activity as well as pharmacokinetic parameters of racemic mixtures of β-receptor blockers display temporal variations with more pronounced pharmacological effects and shorter elimination half-lives in the dark span. Studies with the isomers of bupranolol and practolol indicate no stereospecificity in the central depressant effect; the kinetic behavior of, for example, propranolol, however, exhibits stereospecificity. The results demonstrate the importance of circadian rhythms in modifying the effects and kinetics of drugs. These findings may have therapeutic implication in human subjects.

Single-dose kinetics of deuterium-labelled cannabidiol in man after smoking and intravenous administration

1986 ◽  
Vol 13 (2) ◽  
pp. 77-83 ◽  
Author(s):  
Agneta Ohlsson ◽  
Jan-Erik Lindgren ◽  
Susanne Andersson ◽  
Stig Agurell ◽  
Hampton Gillespie ◽  
...  
Keyword(s):  
Single Dose ◽  
Intravenous Administration ◽  
Kinetics Of

Single-dose pharmacokinetics of orally administered terbinafine in bearded dragons (Pogona vitticeps) and the antifungal susceptibility patterns of Nannizziopsis guarroi

2021 ◽  
pp. 1-8
Author(s):  
Michael S. McEntire ◽  
Jennifer M. Reinhart ◽  
Sherry K. Cox ◽  
Krista A. Keller
Keyword(s):  
Single Dose ◽  
High Performance ◽  
Clinical Decision Making ◽  
Peak Plasma ◽  
Antifungal Susceptibility ◽  
Plasma Concentrations ◽  
Clinical Decision ◽  
Oral Solution ◽  
Susceptibility Data ◽  
Pogona Vitticeps

Abstract OBJECTIVE To identify the antifungal susceptibility of Nanniziopsis guarroi isolates and to evaluate the single-dose pharmacokinetics of orally administered terbinafine in bearded dragons. ANIMALS 8 healthy adult bearded dragons. PROCEDURES 4 isolates of N guarroi were tested for antifungal susceptibility. A compounded oral solution of terbinafine (25 mg/mL [20 mg/kg]) was given before blood (0.2 mL) was drawn from the ventral tail vein at 0, 4, 8, 12, 24, 48, 72, and 96 hours after administration. Plasma terbinafine concentrations were measured with high-performance liquid chromatography. RESULTS The antifungal minimum inhibitory concentrations against N guarroi isolates ranged from 4,000 to > 64,000 ng/mL for fluconazole, 125 to 2,000 ng/mL for itraconazole, 125 to 2,000 ng/mL for ketoconazole, 125 to 1,000 ng/mL for posaconazole, 60 to 250 ng/mL for voriconazole, and 15 to 30 ng/mL for terbinafine. The mean ± SD peak plasma terbinafine concentration in bearded dragons was 435 ± 338 ng/mL at 13 ± 4.66 hours after administration. Plasma concentrations remained > 30 ng/mL for > 24 hours in all bearded dragons and for > 48 hours in 6 of 8 bearded dragons. Mean ± SD terminal half-life following oral administration was 21.2 ± 12.40 hours. CLINICAL RELEVANCE Antifungal susceptibility data are available for use in clinical decision making. Results indicated that administration of terbinafine (20 mg/kg, PO, q 24 to 48 h) in bearded dragons may be appropriate for the treatment of dermatomycoses caused by N guarroi. Clinical studies are needed to determine the efficacy of such treatment.

scholarly journals Effects of holothuria extract on pain behaviour and Fos like immunoreactivity (FLI) in formalin pain

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Che Badariah AA ◽  
Asma HA ◽  
Mohd Nizam H ◽  
Siti FA
Keyword(s):  
Phase 1 ◽  
Intraperitoneal Administration ◽  
Male Rats ◽  
Repeated Measure ◽  
Saline Control ◽  
Control Group ◽  
Formalin Injection ◽  
Intraplantar Injection ◽  
Pain Behaviour ◽  
Behaviour Score

Introduction: The aim of this study was to determine the effects of gamat extract on pain behaviour and Fos like immunoreactivity (FLI) expression in the ventral posterolateral thalamus using the acute pain model. Materials & Methods: Fourteen Sprague-Dawley male rats (220-300 gram) were given intraplantar injection of 0.05ml formalin (1%) followed by intraperitoneal administration of either 4 mg/kg gamat extracts (Holothuria spp.) or saline (control). Behavioural changes were observed and rats were sacrificed 2 hours post-formalin injection. Immunohistochemistry testing was done on the brain sections. FLI was examined using a light microscope attached to an image analyser. The behaviour and FLI data were analysed using repeated measure analysis of variance and independent t-test respectively. Significance level was taken as p<0.05. Results: The control group has significantly higher pain scores compared to holothuria group (F (1) =13.635, p=0.003). There was significant reduction in the pain behaviour score in the holothuria group when compared to the control group in phase 1 (t (14) =2.9, p=0.012) and most of the time from 15 to 60 minutes post-formalin injection (t (12) =3.535, p=0.004). There was a significant reduction (P<0.05) in the number of FLI on the contralateral aspect of the ventral posterolateral thalamic nucleus in the group that received 4mg/kg of holothuria extract (63  3.18) compared to control group (84   6.36). Conclusion: This study showed that administration of holothuria extract significantly suppressed the pain behaviour and reduced the number of FLI in formalin injected rats compared to control.

SINGLE DOSE KINETICS OF CANNABIDIOL IN MAN

1984 ◽  
pp. 219-225 ◽  
Author(s):  
A. Ohlsson ◽  
J.E. Lindgren ◽  
S. Andersson ◽  
S. Agurell ◽  
H. Gillespie ◽  
...  
Keyword(s):  
Single Dose ◽  
Kinetics Of

scholarly journals Can Collagenase Be Used in the Treatment of Adhesive Capsulitis?

2019 ◽  
Vol 29 (2) ◽  
pp. 174-180
Author(s):  
Nazım Karahan ◽  
Güzelali Ozdemir ◽  
Duygu Kolukısa ◽  
Serda Duman ◽  
Fatih Arslanoğlu ◽  
...  
Keyword(s):  
Single Dose ◽  
Saline Solution ◽  
Adhesive Capsulitis ◽  
Cartilage Damage ◽  
Male Rats ◽  
Collagenase Clostridium Histolyticum ◽  
Joint Cartilage ◽  
The Third ◽  
Significant Difference ◽  
Shoulder Range

Background: The objective of this study was to evaluate the efficacy of subacromial injections of collagenase and corticosteroid in rats with experimentally induced adhesive capsulitis. Method: Thirty adult Wistar albino male rats were distributed into 3 groups of 10 rats each after stabilization of their shoulders for 3 weeks: the first group received a single dose of 0.002 mg (0.25 mL) subacromial collagenase; the second group received a single dose of 1.60 mg (0.25 mL) subacromial steroid, and the third group received a single dose of 0.25 mL subacromial saline solution. One week later, we investigated shoulder range of motions, collagen content of the shoulder, and joint cartilage structure. Results: There was no statistically significant difference in the cartilage damage between the groups (p > 0.05). Fibrosis measurements were significantly lower in the collagenase group than in the steroid and saline groups. There was no significant difference in fibrosis between the steroid and saline groups (p > 0.05). Abduction measurements were significantly higher in the collagenase group than in the steroid and saline groups (p < 0.001). No significant difference in the abduction measurements was observed between the saline and steroid groups (p > 0.05). Conclusion: We observed that subacromial injections of collagenase Clostridium histolyticum effectively treated adhesive capsulitis. The results suggest that this treatment could be considered for use in patients with an intact rotator cuff.

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