RESUMO
PT1 peptide isolated from the venom of spider Geolycosa sp. is a modulator of P2X3 receptors that play a role in the development of inflammation and the transmission of pain impulses. The anti-inflammatory and analgesic efficacy of the PT1 peptide was studied in a model of complete Freund's adjuvant-induced paw inflammation in CD-1 mice. The analgesic activity of PT1 peptide was maximum after intramuscular injection at a dose of 0.01 mg/kg, which surpassed the analgesic effect of diclofenac at a dose of 1 mg/kg. The anti-inflammatory activity was maximum after intramuscular injection at a dose of 0.0001 mg/kg; a decrease in paw thickness was observed as soon as 2 h after the administration of the PT1 peptide against the background of inflammation development. All tested doses of PT1 peptide showed high anti-inflammatory activity 4 and 24 h after administration. PT1 peptide at a dose of 0.01 mg/kg when injected intramuscularly simultaneously produced high anti-inflammatory and analgesic effects compared to other doses of the peptide. Increasing the dose of PT1 peptide led to a gradual decrease in its analgesic and anti-inflammatory activity; increasing the dose of intramuscular injection to 0.1 and 1 mg/kg is inappropriate.
Assuntos
Analgésicos , Anti-Inflamatórios , Inflamação , Peptídeos , Animais , Camundongos , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Inflamação/tratamento farmacológico , Inflamação/patologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/administração & dosagem , Masculino , Peptídeos/farmacologia , Peptídeos/administração & dosagem , Peptídeos/uso terapêutico , Injeções Intramusculares , Adjuvante de Freund , Venenos de Aranha/farmacologia , Diclofenaco/farmacologia , Diclofenaco/uso terapêutico , Diclofenaco/administração & dosagem , Modelos Animais de Doenças , Dor/tratamento farmacológicoRESUMO
AIM: To determine the functional diagnostics criteria for predicting the effectiveness of using 2% and 4% solutions articaine without vasoconstrictor and with epinephrine content of 1:200.000. MATERIAL AND METHODS: The study involved 357 patients (193 women and 164 men) aged 20 to 35 years. with the presence of intact single-rooted and multi-rooted teeth without periodontal pathology without pronounced general somatic pathology, and with a low level of situational anxiety according to the Spielberger-Khanin scale. All the patients received injection anesthesia by the infiltration method of 2% and 4% articaine solution without vasoconstrictor or with epinephrine concentration of 1:200.000. The effectiveness of local anesthesia was assessed by recording functional parameters (electrosensitivity threshold test and hemomicrocirculation) of the pulp of intact single-root and multi-root teeth before anesthesia, 5, 10, 15, 30, and 60 minutes after local anesthesia. The safety of the anesthesia was determined by continuous monitoring of the patient's hemodynamic parameters: blood pressure, heart rate, blood oxygen saturation before anesthesia and within 60 minutes after. RESULTS: Articaine solution 2% with epinephrine concentration of 1:200.000 used for infiltration or modified periodontal anesthesia resulted in pulp electrosensitivity threshold growth by 95.93% and 93.58%, respectively. There were no statistically significant differences in hemodynamic values between both study groups. CONCLUSION: Analysis of the data obtained showed the effectiveness and safe anesthesia with drugs based on 2% articaine with an epinephrine concentration of 1:200.000.
Assuntos
Anestesia Local , Carticaína , Anestésicos Locais , Teste da Polpa Dentária , Método Duplo-Cego , Feminino , Humanos , MasculinoRESUMO
The results of experimental investigations of the anti-inflammatory effect of ultrasound on the inflammatory process on a rat model of carrageenan-induced edema of the hind limb are given in this article. The technique used in the experiment showing ultrasound exposure parameters and how to control characteristics of the inflammatory process is described. The anti-inflammatory effect of ultrasound is established.
Assuntos
Modalidades de Fisioterapia , Som , Animais , Carragenina/toxicidade , Modelos Animais de Doenças , Membro Posterior/patologia , Membro Posterior/fisiopatologia , Inflamação/induzido quimicamente , Inflamação/patologia , Inflamação/fisiopatologia , Inflamação/terapia , RatosRESUMO
The kinetics of excretion of 2-(14)C-3-hydroxyphenazepam and its metabolites were studied upon a single transdermal and intravenous administration in mice. The main fraction of the total radioactivity (approximately 80%) was eliminated within approximately 84 h upon intravenous injection and within approximately 360 h after transdermal introduction. In the latter case, the ratio of lipophilic and hydrophilic metabolites is modified as well: the former fraction increases by a factor of 1.75, while the latter decreases by a factor of 1.2 as compared to the case of intravenous drug administration.
Assuntos
Temazepam/urina , Administração Cutânea , Animais , Injeções Intravenosas , Masculino , Camundongos , Temazepam/administração & dosagem , Temazepam/farmacocinéticaRESUMO
We studied the effect of lauric acid on transdermal penetration of phenazepam in vivo. It was found that treatment with lauric acid 3-fold increased the maximum anticonvulsive effect of phenazepam applied in a transdermal therapeutic system in comparison with the control. Study of the pharmacokinetics of phenazepam transdermal therapeutic system showed its higher bioavailability in the presence of lauric acid (f=0.9).
Assuntos
Anticonvulsivantes/farmacocinética , Benzodiazepinas/farmacocinética , Ácidos Láuricos/farmacocinética , Pele/efeitos dos fármacos , Administração Cutânea , Animais , Anticonvulsivantes/administração & dosagem , Anticonvulsivantes/sangue , Área Sob a Curva , Benzodiazepinas/administração & dosagem , Benzodiazepinas/sangue , Disponibilidade Biológica , Encéfalo/metabolismo , Sinergismo Farmacológico , Hidrogéis/farmacocinética , Ácidos Láuricos/farmacologia , Camundongos , Permeabilidade , Pele/metabolismoRESUMO
The kinetics of labeled 3-hydroxyphenazepam (active phenazepam metabolite) after its intravenous and transdermal administration was studied. Biphasic kinetic of drug distribution in the organism was revealed; pharmacokinetic parameters and biological availability (1.32 0.12 for the plasma and 1.21 0.10 for the brain) were determined on the basis of total radioactivity of the plasma and brain.
Assuntos
Administração Cutânea , Ansiolíticos/administração & dosagem , Ansiolíticos/farmacocinética , Benzodiazepinas , Animais , Anticonvulsivantes/farmacologia , Área Sob a Curva , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Relação Dose-Resposta a Droga , Cinética , Camundongos , Fatores de TempoRESUMO
We studied the rate of phenazepam absorption into the blood and its transport to the brain from a transdermal therapeutic system and bioavailability of the drug in this system. Hydrogel matrix consisting of polyvinyl alcohol and 1,2-propylene glycol was used for application. Transdermal application of 0.1-0.4 mg phenazepam in a dose of 14 mg/kg provided a stable level of this drug during application interval (1-48 h), while its bioavailability for blood plasma and brain was 0.63 and 0.2, respectively (determined for 0.4 mg phenazepam). The rate of drug penetration into the blood and brain was 46 and 60 ng/ml/h, respectively.