Wyniki wyszukiwania - Biblioteka Nauki

1

Tramadol and tapentadol hydrochloride: an old and a novel atypical opioid drug. An overview on their present and potential applications

100%

Giorgi M.

Medycyna Weterynaryjna

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2012

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tom 68

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nr 11

EN

Acute and chronic pain is a common presenting condition in both animal species and human beings. Classical opioids provide very effective pain relief, although they may be less effective in the treatment of chronic pain due to their limited therapeutic windows and the induced opioid receptor down regulation. Atypical opioids, such as tramadol and tapentadol, have a dual mechanism of action and have been designed to overcome these issues through an opiate-sparing effect. Tramadol activates mu opioid receptors and in addition, inhibits serotonin and noradrenalin reuptake. These actions are the result of the different enantiomers and tend to be reliant on their metabolism. Indeed, the O-desmethyltramadol phase I metabolite, is 200-300 times more potent for mu opioid receptor activation than the parental compound. For these reasons, the drug’s effectiveness can vary among subjects. In veterinary medicine its effectiveness, especially after oral administration, is still uncertain and controversial. Tapentadol is a novel, atypical opioid with a unique mechanism of action. It was launched on the European drug market at the end of 2011. It has been proposed as the first representative of a new pharmacological class of centrally acting analgesics, namely, the mu opioid receptor agonist, noradrenalin reuptake inhibitors. The first human studies describe this molecule as safe and effective (equianalgesic to morphine). The drug has great potential for veterinary use because it exists as a single enantiomer only, it does not require metabolic activation to be effective and adverse effects triggered by the serotonin reuptake inhibition action are negligible. For these reasons, TAP is a promising compound however at this stage, more investigation is required before it can be recommended for regular use in veterinary medicine, the possibility of undesirable effects is yet to be entirely excluded.

2

Transdermal lidocaine patch 5 percent and lidocaine cream 5 percent: a PK/PD approach in the horse

63%

Andreoni V. , Giorgi M.

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nr 09

EN

Transdermal absorption of four lidocaine (L) patches 5% was compared to the transdermal absorption of L cream 5% to evaluate the pharmacokinetics of the two formulations applied on the same anatomical region under dressing in eight horses. The animals were also assessed for the adequacy of analgesia after patches and cream removal, using a psychophysical method by pricking the patient’s skin to assess the response to pain according to a visual analogue scale. Horses were randomly assigned to four treatment groups: in groups I and II four L patches were applied for a period of 24 hours with and without alcohol pre-cleaning respectively; in group III, 5% L cream was applied every two hours over a period of 24 hours on the same anatomical site. Group IV was the control. No clinical side effects were noted with both formulations. L was detectable in plasma within 6 and 24 hours after patch application and the highest plasma concentrations were reached between 12 and 18 hours. The use of alcohol to pre-clean the skin appeared to reduce the transdermal drug absorption over time. The plasma drug level, after L cream application, reached the highest plasma concentration after 24 hours. Pain assessment after L patch or L cream application, revealed a decreased response when the L cream was used. The result of this study shows that there is an overall lower absorption from the L patches compared with the L cream in horses. Also the L cream treatment reduces significantly the intensity of pain quality as measured by the visual analogue scale.

3

Farmakoterapia / farmakoekonomia syndromu oddechowego bydła

63%

Giorgi M. , Corazza M.

Lecznica Dużych Zwierząt. Ogólnopolski Kwartalnik dla Lekarzy Weterynarii

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2011

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tom 06

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nr 2 Monografia

4

Farmakokinetyka tramadolu oraz jego glownych metabolitow po jednorazowym podaniu per os tabletki o przedluzonym uwalnianiu oraz czopkow per rectum u psow

51%

Lebkowska-Wieruszewska B. , Kowalski C. J. , Saccomanni G. , Giorgi M.

Medycyna Weterynaryjna

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2009

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tom 65

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nr 10

687-692

EN

The aim of the present study is to evaluate the pharmacokinetics of T and its major metabolites M1, M2 and M5 after the single oral administration of an SR tablet and rectal suppositories in dogs (4-6 mg·kg⁻¹ m.c.). The plasma concentration data after SR-tablet and rectal administration were fitted on the basis of a mono- and non-compartmental model, respectively. T plasma concentration after SR tablet administration was quantitatively detected in three dogs, M1 was quantized in only one dog while M2 and M5 were quantized in all the dogs. T showed median values of Cmax, Tmax and T₁/₂ of 40 (20-170) ng·mL⁻¹, 3 (4-2) and 1.88 (2.21-1.44) hours, respectively. M5 showed median values of Cmax, Tmax and T₁/₂ of 0.1 (90-190) ng·mL⁻¹, 2 (3-1) and 4.23 (6.58-1.85) hours, respectively. M2 showed median values of Cmax, Tmax and T₁/₂ of 220 (80-330) ng·mL⁻¹, 4 (7-3) and 4.49 (6.39-1.57) hours, respectively. Following rectal administration, T was detected from 5 minutes up to 10 h in a smaller amount than M5 and M2. T median value of Cmax was 140 ± 60 ng·mL⁻¹ in 0.56 ± 0.41 h (Tmax). K₀₁ t₁/₂ and K₁₀ t₁/₂ were 0.27 ± 0.25 h and 2.24 ± 1.82 h, respectively. M1 was detectable from 5 min up to 2 h, showing low values (7-28 ng·mL⁻¹). The present findings suggest oral SR tablet and suppository rectal formulation have similar pharmacokinetic behavior and would not have suitable pharmacokinetic characteristics to be administered once-a-day as an effective and safe treatment for pain in dogs.

5

Tramadol - nowy analgetyk opioidowy w zwalczaniu bolu u zwierzat towarzyszacych

51%

Lebkowska-Wieruszowska B. , Kowalski C. , Giorgi M.

Magazyn Weterynaryjny

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2008

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tom 17

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nr 11

1183-1185

6

Evolution of biogenic amine content during ripening time in two types of dry sausages: can grain matrix play a role?

51%

Forzale F. , Nuvoloni R. , Pedonese F. , Giorgi M.

Medycyna Weterynaryjna

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2012

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tom 68

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nr 11

EN

The biogenic amine (BA) content of two typical Italian sausages (salame Toscano and salame Garfagnino), differing only in the degree of refinement of the fat matrix, was tested at different time points throughout the ripening process (45 days length in total). The analyses were performed by an earlier validated HPLC method. The total BA content in salame Toscano was significantly lower compared to that in Garfagnino salami. Tyramine, spermine and putrescine were the BA detected in greatest concentrations. Cadaverine, spermidine and 2-phenylethylamine were detected in smaller amounts, whereas tryptamine and histamine were not detected. In summary, BA levels for both sausage types at the end of the ripening period were low and level variation could be accounted for by size differences in matrix particles.

7

Znaczenie komórek macierzystych w inicjacji nowotworów wątroby u szczurów

51%

Wojcik M. , Giorgi M. , Bobowiec R.

Medycyna Weterynaryjna

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2012

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tom 68

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nr 09

EN

Hepatic oval cells (OC) are considered to be the stem cells of the liver and have been linked to the development of hepatocellular carcinoma HCC, one of the most lethal cancers. The objective of this study was to analyse the proliferative response of OC obtained from rats receiving diethylnisamine DEN. In addition, we investigated the effects of resveratrol (Res) on the proliferation and oxidative markers of OC in vitro. OC isolated by in situ collagenase liver perfusion methods were treated with different concentrations of Res for 24, 48 and 72 hours. At the end of these periods the proliferative activity of OC, the release of superoxide anion by OC and the medium concentration of malonylodialdehyd were analyzed . The proliferation of OC cultured without Res increased from IP = 0.945 ± 0.02 to IP = 1.525 ± 0.031 after 24 and 72 hours respectively. A marked (p ≤ 0.05) inhibition of OC proliferation was observed in the presence of 1.0 µM, 25 µM and 100 µM of Res. A significant decrease in the release of O₂⁻. by OC, observed throughout the experimental period, was attributed to the presence of 25 µM of Res. Exposition of OC to 100 µM of Res inhibited the release of O₂⁻. only after 48 and 72 hours of incubation. The presence of 25 µM of Res resulted in the depletion of MDA level, which did not exceed 0.19±0.009 nM. Proliferative activity of OC isolated from carcinogenic rats intensified throughout the culture period. When subjected to the carcinogenic effect of DEN, Res exerts anti-proliferative influence on OC. Moreover, our results provide evidence that Res attenuates oxidative stress during hepatocarcinogenesis.

8

Dawkowanie tramadolu w postaci czopkow u psow z punktu widzenia farmakokinetyki

51%

Lebkowska-Wieruszewska B. , Kowalski C. , Giorgi M. , Saccomanni G.

Magazyn Weterynaryjny

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2009

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tom 18

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nr 10

1118

9

Simulation of road systems and queuing network models

51%

Pasini L. , Feliziani S. , Giorgi M.

TASK Quarterly : scientific bulletin of Academic Computer Centre in Gdansk

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2005

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tom Vol. 9, No 4

397-408

EN

The purpose of this paper is to describe the versatility of queuing network systems for modelling vehicular traffic flows in road systems. These techniques are applicable in a simulation context because of the complexity of the resulting models, which can not be solved by mathematical analytical solvers. Moreover, these techniques can be used to model and simulate the behaviour of an automatic control system of vehicular flow in the same frame.

10

PK/PD evaluations of the novel atypical opioid tapentadol in red-eared slider turtles

45%

Giorgi M. , De Vito V. , Owen H. , Demontis M. P. , Varoni M. V.

Medycyna Weterynaryjna

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2014

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tom 70

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nr 09

EN

The aim of this study was to evaluate the pharmacokinetics and pharmacodynamics of tapentadol (TAP) in red-eared slider turtles after a single intramuscular injection of 5 mg/kg. Turtles (n = 9) were randomly assigned to two treatment groups, according to an open, single-dose, single-treatment, unpaired, two-period crossover design. Group A (n = 5) received a single IM dose of TAP (5 mg/mL) at 5 mg/kg. Group B (n = 4) received a single IM injection of saline (equivalent to the opioid in volume). After a one-month wash-out period, the groups were rotated, and the experiment was repeated. TAP plasma concentrations were evaluated by a validated HPLC-FL method, while an infrared thermal stimulus was applied to the plantar surface of the turtles’ hind limbs to evaluate the thermal withdrawal latency (TWL). TAP plasma concentrations were detectable between 1 and 24 h (2141 – 42 ng/mL, respectively). The TAP-treated group showed a dramatic increase in TWL one hour after drug administration (15.31 ± 4.73 s). Subsequently, TWL decreased with time. Significant differences between the treatment and control groups were apparent up to 10 h following treatment. A linear relationship (r2 = 0.98) between the TAP plasma concentration and effect was found. Given these qualities, TAP appears to be an attractive option for antinociception in turtles because of its rapid onset and acceptable duration of effect.

11

Zastosowanie tramadolu w iniekcji u psów

45%

Lebkowska-Wieruszewska B. , Kowalski C. J. , Saccomanni G. , Del Carlo S. , Giorgi M.

Magazyn Weterynaryjny

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2012

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tom 21

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nr 07

12

Pharmacokinetics of tramadol and metabolites after injective administrations in dogs

45%

Giorgi M. , Del Carlo S. , Lebkowska-Wieruszewska B. , Kowalski C. J. , Saccomanni G.

Polish Journal of Veterinary Sciences

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2010

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tom 13

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nr 4

EN

The aim of this study was to determine the pharmacokinetics of tramadol and its main metabolites after IV and IM injections. The pharmacokinetic cross-over study was carried out on 6 healthy male beagle dogs. Tramadol was administered by intravenous (IV) and intramuscular (IM) injection at 4 mg/kg. Tramadol and its main metabolites O-desmethyl-tramadol (M1), N-,N-didesmethyl-tramadol (M2) and N-,O-didesmethyl-tramadol (M5) concentrations were measured in plasma samples by a HPLC coupled with fluorimetric detection; pharmacokinetic evaluations were carried out with a compartmental and non-compartmental model for tramadol and its metabolites, respectively. The bioavailability of the drug, ranging between 84-102% (mean 92%), was within the generally accepted values for a positive bioequivalence decision of (80-125%). After the IM injection the mean plasma drug concentration peak was reached after a Tmax of 0.34 h with a Cmax of 2.52 μg/mL. No therapeutic relevant differences were observed between IM and IV administration. The minimal effective plasma concentration was reached after a few minutes and maintained for about 6-7 h in both administrations. M1 plasma concentration was low and the amounts of the other metabolites produced were analogous in both routes of administration. In conclusion, tramadol was rapidly and almost completely absorbed after IM administration and its systemic availability was equivalent to the IV injection. The different onset time and duration of action observed were very small and probably therapeutically irrelevant. The IM injection is a useful alternative to IV injection in the dog.

13

Biogenic amines content in Tuscan traditional products of animal origin

45%

Forzale F. , Nuvoloni R. , Pedonese F. , D'Ascenzi C. , Giorgi M.

Medycyna Weterynaryjna

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2011

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tom 67

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nr 02

EN

Biogenic amines can be naturally present in many foods and they can also be produced in high amounts by the activity of amino acid decarboxylases of microorganisms. If ingested in significant amounts they may produce direct or indirect effects on a consumer’s health. In food microbiology, their large presence has been associated to spoilage and fermentation processes. The aim of the present study was to assess the content of biogenic amines (single and total value) in Tuscan traditional cheeses and sausages. Thirty samples of these products were tested. Biogenic amines content was analyzed by a HPLC-UV method. Tyramine was, in all the matrices, the amine most often detected and quantified, followed by putrescine and cadaverine. In conclusion, except in dry sausages, the data obtained in the present study suggest these traditional foods have generally low biogenic amines total content.

14

Pharmacokinetics and pharmacodynamics (PK/PD) of irbesartan in Beagle dogs after oral administration at two dose rates

38%

Carlucci L. , Song K. H. , Yun H. I. , Park H. J. , Seo K. W. , Giorgi M.

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2013

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tom 16

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nr 3

EN

Irbesartan (Irb) is an angiotensin II type 1 receptor antagonist widely used in humans to treat hypertension. Age-related diseases such as hypertension are increasingly being diagnosed in dogs and there is the need for new drugs. The PK/PD of Irb was tested in Beagle dogs. Ten healthy Beagles were orally administered two dose rates (2 and 5 mg/kg), according to a cross over study design. Blood collections for PK analysis and systolic blood pressure (SBP), heart and respiratory rate, mucous membranes colour, capillary refill time and temperature evaluations were performed at scheduled intervals. The drug plasma concentration was dose dependent. The dogs administered 5 mg/kg showed a significant reduction in SBP, while in those receiving 2 mg/kg, this parameter was minimally affected. A counter clockwise hysteresis showed no direct correlation between SBP and plasma concentrations. The minimum effective concentration was theorized to be within the range 550-800 ng/mL. Although further studies are necessary, 5 mg/kg seems to be the more appropriate dose to obtain a hypotensive effect in Beagle dogs.

15

Pharmacokinetic profiles of 5 mg/kg ibudilast, a phosphodiesterase inhibitor, orally administered to dogs in fasted and non-fasted states. A preliminary study.

38%

Łebkowska-Wieruszewska B. , De Vito V. , Kowalski C. J. , Owen H. , Poapolathep A. , Lisowski A. , Giorgi M.

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16

Czy obecność pokarmu oraz sposób dawkowania mogą wpływać na skuteczność cimikoksybu u psów?

38%

Lebkowska-Wieruszewska B. , Kowalski C. J. , Kim T. W. , Owen H. , Yun H. , Giorgi M.

Magazyn Weterynaryjny

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2016

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tom 25

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nr 03

17

Wpływ pokarmu oraz sposobu dawkowania na farmakokinetykę cymikoksybu u psów

38%

Lebkowska-Wieruszewska B. , Kowalski C. J. , Kim T. W. , Owen H. , Yun H. , Giorgi M.

Medycyna Weterynaryjna

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2015

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tom 71

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nr 10

EN

Cimicoxib (CX) is a new non-steroidal anti-inflammatory drug from the “coxib” family, designed for dogs. In the available literature there is little information on the pharmacokinetics of CX. The aim of this study was to evaluate the effect of food intake on the pharmacokinetic characteristics of cimicoxib. Additionally, the pharmacokinetic profile after the administration of precise doses of CX (2 mg/kg b.w.) and an approximate dose (i.e. 80 mg tablet for animals of about 40 kg) were estimated. CX concentrations were determined by a HPLC validated method. The results of pharmacokinetic analysis were similar in both studies, regardless of the dose and the degree of filling of the gastrointestinal tract (fasted, fed). In addition, we estimated the duration of the minimum effective concentration (MEC), which turned out to be similar for all the concentrations tested. The results show that neither small variations in dosage nor the presence of food in the gastrointestinal tract change the therapeutic efficacy of the analgesic in terms of its blood concentration.

18

Flupirtyna - innowacyjny lek przeciwbólowy w medycynie weterynaryjnej

38%

Lebkowska-Wieruszewska B. , De Vito V. , Kowalski C. J. , Lisowski A. , Giorgi M. , Piskon J.

Magazyn Weterynaryjny

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2018

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tom 27

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nr 07-08

19

Plasma profile of cimicoxib in sheep after oral administration at two different rates

38%

Di Salvo A. , Giorgi M. , Lee H. K. , Vercelli C. , Rueca F. , Trabalza Marinucci M. , della Rocca G.

Polish Journal of Veterinary Sciences

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2017

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tom 20

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nr 3

EN

Sheep are often subjected to painful procedures and thus they need to be treated with analgesics. Nevertheless, knowledges about pharmacokinetic features of these drugs in this species are poor. The aim of this study was to evaluate plasma behaviour of cimicoxib in sheep after a single oral administration at two different dose rates (4 and 6 mg/kg). Maximum plasma concentrations of cimicoxib were equal to 273.78 (median value; range 189.00-567.32) and 565.01 (range 308.27-822.59) ng/mL after treatment with 4 and 6 mg/kg, respectively. The time of maximum concentration (Tmax) was achieved between 4 and 10 hours following treatment at the lower dose, and between 6 and 10 hours after the administration of the higher dose, with one sheep achieving the concentration peak at 0.75 hours. The slow absorption and the great individual variability in plasma concentration, probably due to ruminal effects, suggest that cimicoxib is not suitable for oral treatment in sheep.

20

Grapiprant - nowatorski lek przeciwbólowy w medycynie weterynaryjnej

38%

Lepkowska-Wieruszewska B. , Giorgi M. , Lisowski A. , De Vito V. , Poapolathep A. , Barsotti G. , Gazzano A.

Magazyn Weterynaryjny

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2020

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tom 29

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nr 04