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1.
Am J Perinatol ; 38(3): 291-295, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-31550735

RESUMO

OBJECTIVE: The aim of the study is to obtain insights on the short and long-term safety and effectiveness of isoxsuprine hydrochloride as a tocolytic agent in the management of PTL. STUDY DESIGN: In this prospective, single-center, noncomparative study, patients (with preterm labor at gestational age of 24-37 weeks) were administered intravenous (IV) infusion of 40-mg isoxsuprine hydrochloride until uterine quiescence, followed by intramuscular (IM) injection of isoxsuprine hydrochloride 10 mg/4-hourly for first 24 hours and maintained with retard 40-mg sustained release capsule (two times a day) till the time of delivery or 37 completed weeks of pregnancy. RESULTS: All patients (n = 50) achieved successful tocolysis in 24 hours and 48 hours postadministration of isoxsuprine hydrochloride (IV/IM/oral). Mean (±SD) gestation age at the time of delivery was 39.8 ± 2.1 weeks, with latency period of 58.5 ± 18.7 days. Pregnancy outcomes were normal in all the patients and no congenital anomaly/fetal infection was reported. Mean (±SD) fetal birth weight was 2.7 ± 0.3 kg; mean (±SD) Apgar score at 1 and 5 minutes were 7.5 ± 0.6 and 9.2 ± 0.4, respectively. Maternal tachycardia and vomiting (8.0% each) were the commonly reported adverse drug reactions, which were resolved with dose adjustment. CONCLUSION: Isoxsuprine was found to be an effective and well-tolerated tocolytic agent in arresting PTL, in turn resulting in the overall improvement in maternal and perinatal outcomes.


Assuntos
Isoxsuprina/administração & dosagem , Trabalho de Parto Prematuro/tratamento farmacológico , Tocólise/métodos , Tocolíticos/administração & dosagem , Adulto , Feminino , Idade Gestacional , Humanos , Índia , Recém-Nascido , Injeções Intramusculares , Isoxsuprina/efeitos adversos , Gravidez , Resultado da Gravidez , Nascimento Prematuro/prevenção & controle , Estudos Prospectivos , Taquicardia/induzido quimicamente , Tocolíticos/efeitos adversos , Vômito/induzido quimicamente , Adulto Jovem
2.
Cochrane Database Syst Rev ; (12): CD004733, 2015 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-26645888

RESUMO

BACKGROUND: Twin pregnancies are associated with a high risk of neonatal mortality and morbidity due to an increased rate of preterm birth. Betamimetics can decrease contraction frequency or delay preterm birth in singleton pregnancies by 24 to 48 hours. The efficacy of oral betamimetics in women with a twin pregnancy is unproven. OBJECTIVES: To assess the effectiveness of prophylactic oral betamimetics for the prevention of preterm labour and birth for women with twin pregnancies. SEARCH METHODS: We searched the Cochrane Pregnancy and Childbirth Group Trials Register (21 September 2015), MEDLINE (January 1966 to 31 July 2015), EMBASE (January 1985 to 31 July 2015) and reference lists of retrieved studies. SELECTION CRITERIA: Randomised controlled trials in twin pregnancies comparing oral betamimetics with placebo or any intervention with the specific aim of preventing preterm birth. Quasi-randomised controlled trials, cluster-randomised trials and cross-over trials were not eligible for inclusion. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trials for inclusion and risk of bias, extracted data and checked them for accuracy. Two authors assessed the quality of the evidence using the GRADE approach. MAIN RESULTS: Overall, the quality of evidence is low for the primary outcomes. All of the included trials had small numbers of participants and few events. Preterm birth, the most important primary outcome, had wide confidence intervals crossing the line of no effect.Six trials (374 twin pregnancies) were included, but only five trials (344 twin pregnancies) contributed data. All trials compared oral betamimetics with placebo.Betamimetics reduced the incidence of preterm labour (two trials, 194 twin pregnancies, risk ratio (RR) 0.37; 95% confidence interval (CI) 0.17 to 0.78; low quality evidence). However, betamimetics did not reduce prelabour rupture of membranes (one trial, 144 twin pregnancies, RR 1.42; 95% CI 0.42 to 4.82; low quality evidence), preterm birth less than 37 weeks' gestation (four trials, 276 twin pregnancies, RR 0.85; 95% CI 0.65 to 1.10; low quality evidence), or less than 34 weeks' gestation (one trial, 144 twin pregnancies, RR 0.47; 95% CI 0.15 to 1.50; low quality evidence). Mean neonatal birthweight in the betamimetic group was significantly higher than in the placebo group (three trials, 478 neonates, mean difference 111.22 g; 95% CI 22.21 to 200.24). Nevertheless, there was no evidence of an effect of betamimetics in reduction of low birthweight (two trials, 366 neonates, average RR 1.19; 95% CI 0.77 to 1.85, random-effects), or small-for-gestational age neonates (two trials, 178 neonates, average RR 0.90; 95% CI 0.41 to 1.99, random-effects). Two trials showed that betamimetics significantly reduced the incidence of respiratory distress syndrome (388 neonates, RR 0.30; 95% CI 0.12 to 0.77), but the difference was not significant when the analysis was adjusted to account for the non-independence of twins (194 twins, RR 0.35; 95% CI 0.11 to 1.16). Three trials showed no evidence of an effect of betamimetics in reducing neonatal mortality, either with the unadjusted analysis, assuming twins are completely independent of each other (452 neonates, average RR 0.90; 95% CI 0.15 to 5.37, random-effects), or in the adjusted analysis, assuming non-independence of twins (226 twins, average RR 0.74; 95% CI 0.23 to 2.38, random-effects). A maternal death was reported in one trial without a significant difference between the groups (144 women, RR 2.84; 95% CI 0.12 to 68.57). AUTHORS' CONCLUSIONS: There is insufficient evidence to support or refute the use of prophylactic oral betamimetics for preventing preterm birth in women with a twin pregnancy.


Assuntos
Agonistas Adrenérgicos beta/administração & dosagem , Gravidez de Gêmeos , Nascimento Prematuro/prevenção & controle , Tocolíticos/administração & dosagem , Administração Oral , Adulto , Albuterol/administração & dosagem , Feminino , Fenoterol/administração & dosagem , Ruptura Prematura de Membranas Fetais/prevenção & controle , Idade Gestacional , Humanos , Isoxsuprina/administração & dosagem , Gravidez , Ensaios Clínicos Controlados Aleatórios como Assunto , Ritodrina/administração & dosagem , Terbutalina/administração & dosagem
3.
Int J Biol Macromol ; 70: 506-15, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-25062990

RESUMO

Isoxsuprine HCl-loaded microbeads using sodium alginate (SA)-carboxymethyl cashew gum (CMCG) polymer-blends were developed through ionotropic-gelation technique using ZnSO4 as cross-linker. Effects of polymer-blend ratio and cross-linker concentration on drug encapsulation efficiency (DEE) and cumulative drug release at 7 h (R7 h) were optimized by 3(2) factorial design. Optimized microbeads were of excellent combination of high DEE (79.92±2.51%) and suitable sustained drug release pattern over a prolonged period of 7 h (58.67±2.26%). The microbead surface morphology was analyzed by SEM. The physical state of isoxsuprine HCl within the optimized microbead matrix was analyzed by FTIR and DSC. In vitro isoxsuprine HCl release from alginate-CMCG microbeads in phosphate buffer (pH, 6.8) showed prolonged sustained drug release and Korsmeyer-Peppas model (R2=0.9959-0.9992) over 7 h.


Assuntos
Alginatos/química , Anacardium/química , Portadores de Fármacos , Liberação Controlada de Fármacos , Microesferas , Gomas Vegetais/química , Zinco/química , Agonistas Adrenérgicos beta/administração & dosagem , Análise de Variância , Varredura Diferencial de Calorimetria , Química Farmacêutica , Sistemas de Liberação de Medicamentos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Isoxsuprina/administração & dosagem , Tamanho da Partícula , Espectroscopia de Infravermelho com Transformada de Fourier
4.
Cochrane Database Syst Rev ; (9): CD004733, 2012 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-22972074

RESUMO

BACKGROUND: Twin pregnancies are associated with a high risk of neonatal mortality and morbidity due to an increased rate of preterm birth. Betamimetics can decrease contraction frequency or delay preterm birth in singleton pregnancies by 24 to 48 hours. The efficacy of oral betamimetics in women with a twin pregnancy is unproven. OBJECTIVES: To assess the effectiveness of prophylactic oral betamimetics for the prevention of preterm labour and birth for women with twin pregnancies. SEARCH METHODS: We searched the Cochrane Pregnancy and Childbirth Group Trials Register (31 January 2012), the Central Register of Controlled Trials (The Cochrane Library 2012, Issue 2), MEDLINE (January 1966 to 1 February 2012) and EMBASE (January 1985 to 1 February 2012). SELECTION CRITERIA: Randomised controlled trials in twin pregnancies comparing oral betamimetics with placebo or any intervention with the specific aim of preventing preterm birth. Quasi-randomised controlled trials, cluster-randomised trials and cross-over trials were not included. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trials for inclusion and trial quality. Two review authors extracted data. Data were checked for accuracy. MAIN RESULTS: Six trials (374 twin pregnancies) were included, but only five trials (344 twin pregnancies) contributed data. All trials compared oral betamimetics with placebo.Betamimetics reduced the incidence of preterm labour (one trial, 50 twin pregnancies, risk ratio (RR) 0.40; 95% confidence interval (CI) 0.19 to 0.86). However, betamimetics did not reduce preterm birth less than 37 weeks' gestation (four trials, 276 twin pregnancies, RR 0.85; 95% CI 0.65 to 1.10) or less than 34 weeks' gestation (one trial, 144 twin pregnancies, RR 0.47; 95% CI 0.15 to 1.50). Mean neonatal birthweight in the betamimetic group was significantly higher than in the placebo group (three trials, 478 neonates, mean difference 111.22 g; 95% CI 22.2 to 200.2). Nevertheless, there was no evidence of an effect of betamimetics in reduction of low birthweight (two trials, 366 neonates, average RR 1.19; 95% CI 0.77 to 1.85, random-effects) or small-for-gestational age neonates (two trials, 178 neonates, RR 0.92; 95% CI 0.52 to 1.65). Two trials (388 neonates) showed that betamimetics significantly reduced the incidence of respiratory distress syndrome but the difference was not significant when the analysis was adjusted for correlation of babies from twins. Three trials (452 neonates) showed no evidence of an effect of betamimetics in reducing neonatal mortality (RR 0.80; 95% CI 0.35 to 1.82). AUTHORS' CONCLUSIONS: There is insufficient evidence to support or refute the use of prophylactic oral betamimetics for preventing preterm birth in women with a twin pregnancy.


Assuntos
Agonistas Adrenérgicos beta/administração & dosagem , Gravidez de Gêmeos , Nascimento Prematuro/prevenção & controle , Tocolíticos/administração & dosagem , Administração Oral , Adulto , Albuterol/administração & dosagem , Feminino , Fenoterol/administração & dosagem , Idade Gestacional , Humanos , Isoxsuprina/administração & dosagem , Gravidez , Ensaios Clínicos Controlados Aleatórios como Assunto , Ritodrina/administração & dosagem , Terbutalina/administração & dosagem
5.
Drug Test Anal ; 4(6): 515-8, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21381222

RESUMO

Isoxsuprine is a beta-agonist that can be used for growth promotion in cattle, but it is also used as registered veterinary medicine. To investigate if veterinary treatment of cows could lead to residues of isoxsuprine in the hair of their newborn calves, an animal experiment was performed. Four cows, treated on veterinary indication with isoxsuprine lactate (Duphaspasmin) before a caesarian section, were included in the experiment. Hair samples from cows and from their calves were analyzed. The animals were shaved every week for 16 weeks and levels of isoxsuprine were measured in hair. In the cows, the levels of isoxsuprine were highest (>15 µg/kg) just after administration of the isoxsuprine lactate. After two weeks in two cows, a sort of plateau was reached and then the levels decreased. After approximately 10-15 weeks the levels were around the CCα level of the method used (0.5 µg/kg). In calves, for the first two weeks after birth, no isoxsuprine was found above CCα level in three of the four animals. At about 20-30 days old, a maximum concentration of 4 µg/kg was found. Then the levels dropped again under the CCα level, after 60 days no levels above CCα level were found. In one animal, the levels never reached CCα level. We conclude that veterinary treatment of cows with isoxsuprine may temporarily lead to low levels of isoxsuprine in the hair of their newborn calves which can be measured for a maximum of 60 days after birth.


Assuntos
Cesárea/veterinária , Cabelo/química , Isoxsuprina/análogos & derivados , Tocolíticos/farmacocinética , Animais , Animais Recém-Nascidos , Bovinos , Cesárea/métodos , Feminino , Isoxsuprina/administração & dosagem , Isoxsuprina/farmacocinética , Masculino , Gravidez , Fatores de Tempo , Tocolíticos/administração & dosagem
6.
Arzneimittelforschung ; 59(9): 455-60, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19856793

RESUMO

Isoxsuprine (1-(4-hydroxyphenyl)-2-(1-methyl-2-phenoxyethylamino)-1-propanol, CAS 395-28-8) is a peripheral vasodilator that also stimulates beta-adrenergic receptors. It causes a direct relaxation of vascular and uterine smooth muscles and produces positive inotropic and chronotropic effects. It is widely used to arrest premature labour and miscarriage. The aim of this trial was to investigate the pharmacokinetics of isoxsuprine hydrochloride administered orally to healthy young female volunteers as an extended-release formulation at the doses of 30, 60 and 90 mg compared to 10 mg by i.m. route. A randomised, crossover, four-period, multisequence, single-dose design was adopted. Plasma and urine concentrations of free and total isoxsuprine were evaluated by tandem mass spectrometry that reached a low quantification limit of 1 ng/ml. From plasma concentrations Cmax, tmax, AUC(0-t), AUC(0-infinity), t1/2 and Vd and from urine concentration CUE(0-24h) were evaluated by the non-compartmental model. The free drug was present only in plasma after i.m. route, whereas total isoxsuprine, namely the drug after an enzymatic hydrolysis of the conjugate form, was detected in all plasma and urine samples. The distribution volume of the free drug proved to be 2.5 times higher than that of total isoxsuprine, which indicates a good penetration of the free drug into tissue compartments. Oral absorption was evaluated from the p.o./i.m. percentualized ratio of AUC and CUE and proved to be on average around 51%, being linearly correlated with the three doses administered. The oral absorption proved to be sustained as expected from the zero-order kinetics of the drug release from the core of the extended-release formulation. This has justified different values of half-life that was on average 2.2 h after the i.m. route and around 10 h after the three oral doses. After isoxsuprine administration, both oral and i.m. routes, the heart rate increased from baseline during the 9 h monitoring period. This was an expected finding attributable to the stimulating activity of beta-adrenergic receptors. The tolerability of isoxsuprine proved to be very good with all the four administrations performed.


Assuntos
Agonistas Adrenérgicos beta/farmacocinética , Isoxsuprina/farmacocinética , Administração Oral , Adolescente , Agonistas Adrenérgicos beta/administração & dosagem , Agonistas Adrenérgicos beta/efeitos adversos , Adulto , Área Sob a Curva , Disponibilidade Biológica , Estudos Cross-Over , Relação Dose-Resposta a Droga , Feminino , Frequência Cardíaca/efeitos dos fármacos , Humanos , Injeções Intramusculares , Isoxsuprina/administração & dosagem , Isoxsuprina/efeitos adversos , Reprodutibilidade dos Testes , Solubilidade , Distribuição Tecidual , Adulto Jovem
7.
J Avian Med Surg ; 21(3): 215-9, 2007 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-18087939

RESUMO

A 35-year-old yellow-naped Amazon parrot (Amazona ochrocephala auropalliata) was presented for gradually increasing inappetence, ataxia, weakness, and lethargy. Radiographic and ultrasonographic findings were strongly suggestive of atherosclerosis. Isoxsuprine, a peripheral vasodilator demonstrated to be of benefit in humans with intermittent limb pain, weakness, and lameness secondary to occlusive vascular disease, was selected for treatment. The bird's clinical signs resolved during treatment but recurred after varying periods of time when the medication was stopped intermittently. Nearly 3 years after the initial examination, the parrot was doing well on isoxsuprine therapy, with normal prehension of food with its feet and no recurrence of clinical signs.


Assuntos
Agonistas Adrenérgicos beta/uso terapêutico , Doenças das Aves/tratamento farmacológico , Doença da Artéria Coronariana/veterinária , Isoxsuprina/uso terapêutico , Papagaios , Administração Oral , Agonistas Adrenérgicos beta/administração & dosagem , Animais , Doenças das Aves/diagnóstico , Doenças das Aves/diagnóstico por imagem , Doenças das Aves/patologia , Doença da Artéria Coronariana/tratamento farmacológico , Diagnóstico Diferencial , Feminino , Isoxsuprina/administração & dosagem , Radiografia
8.
J Vet Pharmacol Ther ; 25(2): 81-7, 2002 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-12000527

RESUMO

Isoxsuprine hydrochloride has been suggested for use in horses for treatment of navicular syndrome and laminitis. The drug has been shown to be a beta-adrenoreceptor antagonist with beta-adrenoreceptor agonistic properties, with both characteristics contributing to vasodilation and uterine relaxation. In addition, the drug is capable of decreasing blood viscosity and platelet aggregation. Studies have shown i.v. isoxsuprine to have a plasma half-life of <3 h with a large apparent volume of distribution. Cardiovascular effects resolve rapidly following i.v. administration, but are absent with oral dosing. Oral bioavailability is 2.2% with a high first pass effect. Isoxsuprine has an apparent affinity for melanin that may contribute to extended renal excretion. Clinical trials appear to support the use of isoxsuprine for treatment of navicular disease. However, poor bioavailability, lack of cardiovascular effects following oral administration, superficial support in clinical trials, and new evidence regarding the pathogenesis of navicular syndrome indicate that the use of isoxsuprine for treatment of navicular syndrome or laminitis is questionable at best.


Assuntos
Doenças dos Cavalos/tratamento farmacológico , Cavalos/metabolismo , Isoxsuprina/farmacocinética , Isoxsuprina/uso terapêutico , Osteíte/veterinária , Vasodilatadores/farmacocinética , Vasodilatadores/uso terapêutico , Administração Oral , Animais , Disponibilidade Biológica , Doenças do Pé/tratamento farmacológico , Doenças do Pé/veterinária , Infusões Intravenosas/veterinária , Isoxsuprina/administração & dosagem , Coxeadura Animal/tratamento farmacológico , Osteíte/tratamento farmacológico , Ossos do Tarso/irrigação sanguínea , Vasodilatadores/administração & dosagem
9.
Urology ; 58(1): 95-7, 2001 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-11445487

RESUMO

OBJECTIVES: To determine the effectiveness and safety of high-dose isoxsuprine for the treatment of mixed-type erectile dysfunction. METHODS: Forty-four patients who had vasculogenic impotence diagnosed on the basis of their sexual history, physical examination, laboratory analysis, polysomnographic recording of nocturnal erections, and dynamic color Doppler sonography of the cavernosal arteries were entered into a randomized, double-blind, placebo-controlled, crossover comparison of a placebo with high-dose isoxsuprine hydrochloride (60 mg/day orally). The treatment consisted of two 30-day courses. After a 14-day washout period, the patients who initially received the placebo for 30 days switched to isoxsuprine hydrochloride for 30 days and vice versa. Erectile function, ejaculation, interest in sex, and physical examination findings were investigated before treatment and at the end of each drug period. RESULTS: Thirty-six patients (82%) completed the entire treatment schedule. Positive clinical results (complete and partial responses) were obtained in 6 men (16.6%) at the end of the isoxsuprine phase and in 7 men (19.4%) after the placebo period. The statistical analysis disclosed no significant difference when isoxsuprine was compared with placebo (P >0.05). Significant drug-related adverse effects occurred in the isoxsuprine group and treatment was discontinued in 2 patients. CONCLUSIONS: Isoxsuprine is no better than placebo as a first-line treatment for mixed-type erectile dysfunction.


Assuntos
Disfunção Erétil/tratamento farmacológico , Impotência Vasculogênica/tratamento farmacológico , Isoxsuprina/administração & dosagem , Vasodilatadores/administração & dosagem , Adulto , Método Duplo-Cego , Humanos , Hipotensão/induzido quimicamente , Isoxsuprina/efeitos adversos , Masculino , Pessoa de Meia-Idade , Medição da Dor/efeitos dos fármacos , Resultado do Tratamento , Vasodilatadores/efeitos adversos
10.
Can J Vet Res ; 64(2): 112-6, 2000 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-10805250

RESUMO

Isoxsuprine is routinely recovered from enzymatically-hydrolyzed, post-administration urine samples as parent isoxsuprine in equine forensic science. However, the specific identity of the material in horse urine from which isoxsuprine is recovered has never been established, although it has long been assumed to be a glucuronide conjugate (or conjugates) of isoxsuprine. Using ESI/MS/MS positive mode as an analytical tool, urine samples collected 4-8 h after isoxsuprine administration yielded a major peak at m/z 554 that was absent from control samples and resisted fragmentation to daughter ions. Titration of this material with increasing concentrations of sodium acetate yielded m/z peaks consistent with the presence of monosodium and disodium isoxsuprine-glucuronide complexes, suggesting that the starting material was a dipotassium-isoxsuprine-glucuronide complex. Electrospray ionization mass spectrometry negative mode disclosed the presence of a m/z 476 peak that declined following enzymatic hydrolysis and resulted in the concomitant appearance of peaks at m/z 300 and 175. The resulting peaks were consistent with the presence of isoxsuprine (m/z 300) and a glucuronic acid residue (m/z 175). Examination of the daughter ion spectrum of this putative isoxsuprine-glucuronide m/z 476 peak showed overlap of many peaks with those of similar spectra of authentic morphine-3- and morphine-6-glucuronides, suggesting they were derived from glucuronic acid conjugation. These data suggest that isoxsuprine occurs in post-administration urine samples as an isoxsuprine-glucuronide conjugate and also, under some circumstances, as an isoxsuprine-glucuronide-dipotassium complex.


Assuntos
Cavalos/fisiologia , Isoxsuprina/urina , Vasodilatadores/urina , Animais , Feminino , Medicina Legal/métodos , Glucuronídeos , Isoxsuprina/administração & dosagem , Isoxsuprina/metabolismo , Espectrometria de Massas/veterinária , Vasodilatadores/administração & dosagem , Vasodilatadores/metabolismo
11.
Equine Vet J ; 32(2): 119-24, 2000 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-10743967

RESUMO

We used isolated equine digital arteries to study the vasodilatory mechanism of isoxsuprine, and fowl caecum preparations to investigate the affinity of the drug for beta-adrenoceptors. Isoxsuprine is a potent vasodilator of arterial smooth muscle that has been precontracted by an alpha-adrenoceptor agonist such as noradrenaline (log EC50 = -6.33 [-5.98; -6.68]). The present study indicates that its effect is due to alpha-adrenoceptor blockade since: (1) after a long lasting exposure to cumulative doses of isoxsuprine the vasoconstricting action of noradrenaline cannot be restored; (2) isoxsuprine does not promote relaxation on preparations precontracted by PGF2alpha; (3) isoxsuprine shifts the dose-response curve of noradrenaline to the right; and (4) its affinity (pK(B) = 6.90 [6.60; 7.20]) in this experiment is comparable to that in noradrenaline-precontracted preparations and is 14 times lower than that of the selective alpha1-adrenergic antagonist prazosin [pK(B) = 8.04 (7.40; 8.68]). The affinity of isoxsuprine for beta-adrenoceptors was 100 times lower than that of isoprenaline when tested on fowl caecum. This preparation has a large beta-adrenoceptor and negligible alpha-adrenoceptor population concerned with the control of smooth muscle motility. Our data suggest that the alpha-mediated effect of isoxsuprine on horse arterial smooth muscle is due to higher affinity of the drug for alpha- than beta-adrenoceptors rather than low concentration or functionality of beta-sites at this site. According to these data, pure beta2-agonists seem to be more profitable tools to determine vasodilation of the arterial bed in horses legs.


Assuntos
Agonistas Adrenérgicos beta/farmacocinética , Artérias/metabolismo , Membro Anterior/irrigação sanguínea , Cavalos/metabolismo , Isoxsuprina/farmacocinética , Músculo Liso Vascular/metabolismo , Vasodilatação , Antagonistas Adrenérgicos alfa/metabolismo , Agonistas Adrenérgicos beta/administração & dosagem , Animais , Galinhas , Relação Dose-Resposta a Droga , Isoproterenol/metabolismo , Isoxsuprina/administração & dosagem , Receptores Adrenérgicos beta/metabolismo
12.
Vet Surg ; 28(3): 154-60, 1999.
Artigo em Inglês | MEDLINE | ID: mdl-10338160

RESUMO

OBJECTIVE: To quantitate blood flow in the palmar digital artery and dorsal laminae of the hoof in standing, unmedicated, nonsedated horses, and in horses treated with oral isoxsuprine, oral pentoxifylline, and intravenous acetylpromazine as a positive control. STUDY DESIGN: Experimental study; treatments administered in a random cross-over design. ANIMALS: A total of 6 healthy horses selected with at least one nonpigmented forelimb hoof wall and determined to be free of laminitis. METHODS: All horses were instrumented with a flow probe placed around one palmar digital artery under general anesthesia and a laser doppler flow probe placed within a hole in the dorsal hoof wall to measure digital blood flow and laminar perfusion respectively. Baseline readings of palmar digital blood flow and laminar perfusion were recorded before and between treatments. Horses were randomly assigned to one of two groups and treated with either isoxsuprine (1.2 mg/kg, orally twice daily for 10 days) or pentoxifylline (4.4 mg/kg, orally every 8 hours for 10 days) in a random cross-over design. Digital blood flow (DBF) and laminar perfusion (LP) were measured on days 2, 5, 7, and 10 of treatment. Horses also received acetylpromazine as a positive control (0.066 mg/kg, intravenously) during the washout period, and measurements were taken every 15 minutes until measurements returned to baseline readings. Data were analyzed by using repeated measures ANOVA. RESULTS: Digital blood flow (11.2 to 97.7 mL/min) and laminar perfusion (1.0 to 11.1 Capillary Perfusion Units) differed between horses. No statistically significant increases in DBF or LP were detected over the 10 day treatment period with either isoxsuprine or pentoxifylline. Acepromazine resulted in a significant increase (P = .0007) in DBF for approximately 75 minutes beginning 15 minutes after treatment. A mild but insignificant increase in LP was identified after acetylpromazine treatment. CONCLUSION: Neither isoxsuprine nor pentoxifylline increased blood flow to the digit or dorsal laminae in healthy horses. Acepromazine caused an increased blood flow to the digit. Based on the results of this study acetylpromazine potentially would have a greater effect on improving digital blood flow than oral isoxsuprine or pentoxifylline when treating ischemic conditions of the foot in horses.


Assuntos
Membro Anterior/irrigação sanguínea , Isoxsuprina/farmacologia , Pentoxifilina/farmacologia , Vasodilatadores/farmacologia , Acepromazina/farmacologia , Administração Oral , Análise de Variância , Animais , Estudos Cross-Over , Antagonistas de Dopamina/farmacologia , Cavalos , Isoxsuprina/administração & dosagem , Pentoxifilina/administração & dosagem , Fluxo Sanguíneo Regional/efeitos dos fármacos , Vasodilatação/efeitos dos fármacos , Vasodilatadores/administração & dosagem
13.
Equine Vet J ; 30(4): 294-9, 1998 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-9705111

RESUMO

Isoxsuprine is reported to be a peripheral vasodilator used in human and veterinary medicine to treat ischaemic vascular disease. In horses, it is generally administered orally to treat navicular disease and other lower limb problems. To define the scope and duration of its pharmacological responses after oral administration, 6 horses were dosed with isoxsuprine HCl (1.2 mg/kg bwt) q. 12 h for 8 days and then tested to assess the duration and extent of pharmacological actions. There was no significant difference between isoxsuprine and control treatment values for heart rate, spontaneous activity, sweat production, anal muscle tone, core and skin temperatures, and cutaneous blood flow. The lack of pharmacological effect following oral administration was in sharp contrast to the marked response following i.v. dosing reported in earlier experiments.


Assuntos
Cavalos/fisiologia , Isoxsuprina/farmacologia , Vasodilatadores/farmacologia , Administração Oral , Canal Anal/efeitos dos fármacos , Canal Anal/fisiologia , Ração Animal , Animais , Temperatura Corporal/efeitos dos fármacos , Feminino , Frequência Cardíaca/efeitos dos fármacos , Isoxsuprina/administração & dosagem , Isoxsuprina/farmacocinética , Atividade Motora/efeitos dos fármacos , Tono Muscular/efeitos dos fármacos , Pós , Fluxo Sanguíneo Regional/efeitos dos fármacos , Respiração/efeitos dos fármacos , Pele/irrigação sanguínea , Temperatura Cutânea/efeitos dos fármacos , Sudorese/efeitos dos fármacos , Vasodilatadores/administração & dosagem , Vasodilatadores/farmacocinética
15.
Gac Med Mex ; 133(5): 403-6, 1997.
Artigo em Espanhol | MEDLINE | ID: mdl-9580102

RESUMO

The objective of this paper is to demonstrate that isoxsuprine is an effective, quick hypotensive of easy management in the hypertension of pregnancy that does not have adverse effects on the mother-fetus binomial. This study was carried out at the Obstetric Intensive Care Unit at the Gyneco-Obstretrics Hospital in the Centro Médico Nacional La Raza of the IMSS. Fifty patients were chosen and managed according to the protocol management of the hospital; they had a diagnosis of severe toxemia or preeclampsia in patients with 24 weeks or more of pregnancy, with hypertension, edema, convulsions and/or coma state or without concomitant or previous pathological states. All of the patients received isoxsuprine (50 mg in 250 ml of DW5%). We evaluated the hypotensive effect of isoxsuprine according to the time and average dose administered, and its effect on the mother and fetus heart frequency according to the basal values. We valued the APGAR score at minute one and minute five, seconds after the delivery. We analyzed according to the degrees of toxemia and at the end of the obstetric event. We demonstrated a significant decrease in the arterial tension after administration fifteen minutes later with a dose of nine drops (0.29 mcg/min) average and demonstrated at the same time that there are no adverse effects on the mother fetus binomial. Isoxsuprine is an affective, quick and economical hypotensive of easy management that has no adverse effects on mother-fetus glycemia, obstetric bleeding and APGAR score.


Assuntos
Agonistas Adrenérgicos beta/uso terapêutico , Anti-Hipertensivos/uso terapêutico , Isoxsuprina/uso terapêutico , Pré-Eclâmpsia/tratamento farmacológico , Vasodilatadores/uso terapêutico , Agonistas Adrenérgicos beta/administração & dosagem , Adulto , Anti-Hipertensivos/administração & dosagem , Índice de Apgar , Interpretação Estatística de Dados , Feminino , Humanos , Recém-Nascido , Infusões Intravenosas , Isoxsuprina/administração & dosagem , Gravidez , Estudos Prospectivos , Vasodilatadores/administração & dosagem
16.
Equine Vet J ; 28(4): 320-6, 1996 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-8818598

RESUMO

Isoxsuprine is a therapeutic medication used to treat navicular disease and other lower limb problems in horses and is one of the more frequently detected therapeutic agents in racing horses. In a crossover study, horses were administered isoxsuprine i.v. to determine the character and duration of its pharmacological effects. Isoxsuprine significantly increased heart rate 5-150 min following injection. Unrestrained activity following isoxsuprine treatment was significantly greater than control activity for 105 min after treatment. There was an apparent, although statistically nonsignificant, increased cutaneous blood flow resulting in visible water vapour and sweat production 5-60 min after administration. Initially, there was no difference in skin temperature between control and isoxsuprine treatment values; however, skin temperature decreased below control values 45-120 min after injection. Concurrently, there was a significant decrease in rectal temperature reflecting a decrease in body core temperature. Using infrared thermography, a significant decrease in superficial skin temperature of the front legs occurred 30-240 min after treatment. Isoxsuprine also reduced smooth muscle tone, which was apparent by decreased tone of the internal anal sphincter 10-180 min after treatment. It was concluded that the measurable pharmacological effects of i.v. isoxsuprine are short lived, since none of the above responses were apparent 4 h or more after i.v. administration.


Assuntos
Cavalos/fisiologia , Isoxsuprina/farmacologia , Vasodilatadores/farmacologia , Animais , Temperatura Corporal/efeitos dos fármacos , Temperatura Corporal/fisiologia , Feminino , Motilidade Gastrointestinal/efeitos dos fármacos , Motilidade Gastrointestinal/fisiologia , Frequência Cardíaca/efeitos dos fármacos , Frequência Cardíaca/fisiologia , Injeções Intravenosas , Isoxsuprina/administração & dosagem , Isoxsuprina/farmacocinética , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/fisiologia , Fluxo Sanguíneo Regional/efeitos dos fármacos , Fluxo Sanguíneo Regional/fisiologia , Respiração/efeitos dos fármacos , Respiração/fisiologia , Pele/irrigação sanguínea , Temperatura Cutânea/efeitos dos fármacos , Temperatura Cutânea/fisiologia , Sudorese/fisiologia , Fatores de Tempo , Vasodilatadores/administração & dosagem , Vasodilatadores/farmacocinética
17.
Rev. Asoc. Med. Crit. Ter. Intensiva ; 10(3): 115-7, mayo-jun. 1996. tab
Artigo em Espanhol | LILACS | ID: lil-180453

RESUMO

Introducción. La sepsis abdominal se acompaña con frecuencia de shock y vasoconstrición severa. Objetivo. Dar a conocer los efectos hemodinamico de la isoxuprina en el paciente con sepsis abdominal y shock. Pacientes y métodos. Evaluamos los efectos de la isoxsuprina en 24 pacientes de una UCI. Se les efectuaron mediciones hemodinámicas antes y después de tratarse con isoxsuprina (1.5 µg/kg.min). Resultados. Después del tratamiento disminuyó el índice de resistencia vasculares sistémicas (2703 ñ 1541 a 1632 ñ 720 din/s.cm-5, p< 0.004) y aumentó el índice cardiaco (3.12 ñ 1.44 a 3.9 ñ 1.15 mL/min, p< 0.04); las resistencias pulmonares, disponibilidad de oxígeno, consumo de oxígeno y el porcentaje de extracción de oxígeno permanecieron sin cambios. Conclusión. Este estudio documental los efectos benéficos de la isoxsuprina en el paciente crítico con sepsis abdominal


Assuntos
Humanos , Masculino , Feminino , Adulto , Hemodinâmica , Isoxsuprina/administração & dosagem , Isoxsuprina/farmacocinética , Sepse/tratamento farmacológico , Resistência Vascular/efeitos dos fármacos
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