SABIIA - Sistema Aberto e Integrado de Informação em Agricultura (Sabiia)

There is evidence for participation of peripheral β-adrenoceptors in delayed liquid gastric emptying (GE) induced in rats by dipyrone (Dp), 4-aminoantipyrine (AA), and antipyrine (At). The present study aimed to determine whether β-adrenoceptors are involved in delayed GE induced by phenylpyrazole derivatives and the role of the prevertebral sympathetic nervous system in this condition. Male Wistar rats weighing 220-280 g were used in the study. In the first experiment rats were intravenously pretreated with vehicle (V), atenolol 30 mg/kg (ATE, β1-adrenergic antagonist), or butoxamine 25 mg/kg (BUT, β2-adrenergic antagonist). In the second experiment, rats were pretreated with V or SR59230A 2 mg/kg (SRA, β3-adrenergic antagonist). In the third experiment,...

An electronic pressure-meter nociception paw test for rats

Palavras-chave: Gastric emptying; Dipyrone; 4-aminoantipyrine; Antipyrine; Β2-Adrenoceptor; Prevertebral sympathetic ganglia.

Ano: 2016

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2016000300603

Vivancos,G.G.; Verri Jr.,W.A.; Cunha,T.M.; Schivo,I.R.S.; Parada,C.A.; Cunha,F.Q.; Ferreira,S.H..

The objective of the present investigation was to compare the sensitivity of an electronic nociceptive mechanical paw test with classical mechanical tests to quantify the intensity variation of inflammatory nociception. The electronic pressure-meter test consists of inducing the hindpaw flexion reflex by poking the plantar region with a polypropylene pipette tip adapted to a hand-held force transducer. This method was compared with the classical von Frey filaments test and with the rat paw constant pressure test, a modification of the Randall and Selitto test developed by our group. When comparing the three methods, the electronic pressure-meter and the rat paw constant pressure test, but not the von Frey filaments test, detected time vs treatment...

Evidence of the effect of dipyrone on the central nervous system as a determinant of delayed gastric emptying observed in rats after its administration

Palavras-chave: Hyperalgesia; Nociception; Dipyrone; Indomethacin; Von Frey filaments; Constant pressure test.

Ano: 2004

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2004000300017

Collares,E.F.; Vinagre,A.M..

Dipyrone administered intravenously (iv) delays gastric emptying (GE) in rats. The objectives of the present study were to assess: 1) the effect of the dose of dipyrone and time after its iv administration on GE in rats, 2) the effect of subdiaphragmatic vagotomy (VgX) and bilateral electrolytic lesion of the paraventricular nucleus (PVNX) on the delayed GE induced by the drug, and 3) the intracerebroventricular (icv) action of dipyrone and of one of its metabolites, 4-aminoantipyrine on GE. Male Wistar rats received saline labeled with phenol red intragastrically as a test meal. GE was indirectly assessed by the determination of percent gastric retention (GR) of the test meal 10 min after administration by gavage. Dipyrone delays GE in a dose- and...

Effect of the GABA B agonist baclofen on dipyrone-induced delayed gastric emptying in rats

Palavras-chave: Gastric emptying; Dipyrone; Paraventricular nucleus; Vagus nerve.

Ano: 2003

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003001000014

Collares,E.F.; Vinagre,A.M..

Dipyrone administered intravenously (iv) or intracerebroventricularly (icv) delays gastric emptying (GE) in rats. Gamma-aminobutyric acid (GABA) is the most potent inhibitory neurotransmitter of the central nervous system. The objective of the present study was to determine the effect of icv baclofen, a GABA B receptor agonist, on delayed GE induced by dipyrone. Adult male Wistar rats received a saline test meal containing phenol red as a marker. GE was indirectly evaluated by determining the percent of gastric retention (%GR) of the meal 10 min after orogastric administration. In the first experiment, the animals were injected iv with vehicle (Civ) or 80 mg/kg (240 µmol/kg) dipyrone (Dp iv), followed by icv injection of 10 µl vehicle (bac0), or 0.5...

Presurgical ketoprofen, but not morphine, dipyrone, diclofenac or tenoxicam, preempts post-incisional mechanical allodynia in rats

Palavras-chave: Gastric emptying; Dipyrone; GABA; GABA B receptors; Baclofen.

Ano: 2005

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005000100015

Prado,W.A.; Pontes,R.M.C..

The treatment of pain before it initiates may prevent the persistent pain-induced changes in the central nervous system that amplify pain long after the initial stimulus. The effects of pre- or postoperative intraperitoneal administration of morphine (2 to 8 mg/kg), dipyrone (40 and 80 mg/kg), diclofenac (2 to 8 mg/kg), ketoprofen (10 and 20 mg/kg), and tenoxicam (10 and 20 mg/kg) were studied in a rat model of post-incisional pain. Groups of 5 to 8 male Wistar rats (140-160 g) were used to test each drug dose. An incision was made on the plantar surface of a hind paw and the changes in the withdrawal threshold to mechanical stimulation were evaluated with Von Frey filaments at 1, 2, 6 and 24 h after the surgery. Tenoxicam was given 12 or 6 h...

Antinociceptive effects of Cremophor EL orally administered to mice

Palavras-chave: Preemptive analgesia; Morphine; Dipyrone; Diclofenac; Ketoprofen; Tenoxicam.

Ano: 2002

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2002000100016

Evidence for the involvement of peripheral β-adrenoceptors in delayed liquid gastric emptying induced by dipyrone, 4-aminoantipyrine, and antipyrine in rats

Tabarelli,Z.; Berlese,D.B.; Sauzem,P.D.; Mello,C.F.; Rubin,M.A..

Surfactants are frequently used to improve solubilization of lipophilic drugs. Cremophor EL (CrEL) is a polyoxyethylated castor oil surfactant used to solubilize water-insoluble drugs such as anesthetic, antineoplastic, immunosuppressive and analgesic drugs, vitamins and new synthetic compounds, including potential analgesics. The antinociceptive effect of CrEL (3.2, 6.4 and 10.6 g/kg, in 10 ml/kg body weight, by gavage) on the abdominal writhing response induced by intraperitoneal administration of acetic acid (0.8%, 10 ml/kg body weight) and on the tail immersion test was investigated in mice. Control animals received castor oil (10 ml/kg body weight) or saline (0.9% NaCl, 10 ml/kg body weight). CrEL reduced nociception in a dose-dependent manner in both...

Tipo: Info:eu-repo/semantics/other

Palavras-chave: Antinociception; Cremophor EL; Tail immersion test; Writhing test; Dipyrone; Morphine.

Ano: 2003

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003000100016

Dipyrone (Dp), 4-aminoantipyrine (AA), and antipyrine (At) delay liquid gastric emptying (GE) in rats. We evaluated adrenergic participation in this phenomenon in a study in male Wistar rats (250-300 g) pretreated subcutaneously with guanethidine (GUA), 100 mg·kg−1·day−1, or vehicle (V) for 2 days before experimental treatments. Other groups of animals were pretreated intravenously (iv) 15 min before treatment with V, prazosin (PRA; 1 mg/kg), yohimbine (YOH; 3 mg/kg), or propranolol (PRO; 4 mg/kg), or with intracerebroventricular (icv) administration of 25 µg PRO or V. The groups were treated iv with saline or with 240 µmol/kg Dp, AA, or At. GE was determined 10 min later by measuring the percentage of gastric retention (%GR) of saline labeled with phenol...

Phenylpyrazolone derivatives inhibit gastric emptying in rats by a capsaicin-sensitive afferent pathway

Palavras-chave: Gastric emptying; Dipyrone; 4-Aminoantipyrine; Antipyrine; Sympathetic nervous system; Adrenergic receptors.

Ano: 2013

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013000900735

Dipyrone (Dp), 4-aminoantipyrine (AA) and antipyrine (At) administered iv and Dp administered icv delay gastric emptying (GE) in rats. The participation of capsaicin (Cps)-sensitive afferent fibers in this phenomenon was evaluated. Male Wistar rats were pretreated sc with Cps (50 mg/kg) or vehicle between the first and second day of life and both groups were submitted to the eye-wiping test. GE was determined in these animals at the age of 8/9 weeks (weight: 200-300 g). Ten minutes before the study, the animals of both groups were treated iv with Dp, AA or At (240 μmol/kg), or saline; or treated icv with Dp (4 μmol/animal) or saline. GE was determined 10 min after treatment by measuring % gastric retention (GR) of saline labeled with phenol red 10 min...

Effect of antipyrine on the gastric emptying of liquid in rats

Palavras-chave: Gastric emptying; Dipyrone; 4-Aminoantipyrine; Antipyrine; Capsaicin.

Ano: 2009

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2009001100014

Soares,A.C.F.; Vinagre,A.M.; Collares,E.F..

Antipyrine (At) and dipyrone (Dp) delay gastric emptying (GE) in rats. The objective of the present study was to assess the effects of intravenous (iv) and intracerebroventricular (icv) administration of At and Dp on the GE of liquid by rats. GE was assessed in male Wistar rats (5-10 in each group) 10 min after the icv or iv drug injection by measuring percent gastric retention (%GR) of a saline test meal labeled with phenol red 10 min after administration by gavage. The At iv group was significantly higher (64.4 ± 2.6%) compared to control (33.4 ± 1.5%) but did not differ from the Dp group (54.3 ± 3.8%). After icv administration of At, %GR (34.2 ± 2%) did not differ from control (32.6 ± 1.9%), but was significantly higher after Dp (54.5 ± 2.3%)....

Limited-sampling strategy models for estimating the pharmacokinetic parameters of 4-methylaminoantipyrine, an active metabolite of dipyrone

Palavras-chave: Gastric emptying; Dipyrone; Antipyrine; GABA B receptors; Vagus nerve.

Ano: 2006

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2006001100015

Suarez-Kurtz,G.; Ribeiro,F.M.; Estrela,R.C.E.; Vicente,F.L.; Struchiner,C.J..

Bioanalytical data from a bioequivalence study were used to develop limited-sampling strategy (LSS) models for estimating the area under the plasma concentration versus time curve (AUC) and the peak plasma concentration (Cmax) of 4-methylaminoantipyrine (MAA), an active metabolite of dipyrone. Twelve healthy adult male volunteers received single 600 mg oral doses of dipyrone in two formulations at a 7-day interval in a randomized, crossover protocol. Plasma concentrations of MAA (N = 336), measured by HPLC, were used to develop LSS models. Linear regression analysis and a "jack-knife" validation procedure revealed that the AUC0-<FONT FACE=Symbol>¥</FONT> and the Cmax of MAA can be accurately predicted (R²>0.95, bias <1.5%, precision...

Effects of dipyrone on the digestive tract

Palavras-chave: Dipyrone; 4-methylaminoantipyrine; Limited-sampling models; Pharmacokinetics; Bioequivalence.

Ano: 2001

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2001001100017

Collares,E.F.; Troncon,L.E.A..

Dipyrone (metamizole), acting through its main metabolites 4-methyl-amino-antipyrine and 4-amino-antipyrine, has established analgesic, antipyretic, and spasmolytic pharmacological effects, which are mediated by poorly known mechanisms. In rats, intravenously administered dipyrone delays gastric emptying (GE) of liquids with the participation of capsaicin-sensitive afferent fibers. This effect seems to be mediated by norepinephrine originating from the sympathetic nervous system but not from the superior celiac-mesenteric ganglion complex, which activates β2-adrenoceptors. In rats, in contrast to nonselective non-hormonal anti-inflammatory drugs, dipyrone protects the gastric mucosa attenuating the development of gastric ulcers induced by a number of...

Dipyrone in association with atropine inhibits the effect on gastric emptying induced by hypoglycemia in rats

Palavras-chave: Dipyrone; Gastric emptying; Gastric mucosa; Sphincter of Oddi; Intestinal Motility; Adrenergic receptors.

Ano: 2019

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2019000200301

Collares,E.F.; Vinagre,A.M.; Collares-Buzato,C.B..

Atropine (AT) and dipyrone (Dp) induce a delay of gastric emptying (GE) of liquids in rats by inhibiting muscarinic receptors and activating β2-adrenergic receptors, respectively. The objective of the present study was to determine the effects of pretreatment with AT and Dp, given alone or in combination, on the effect of hypoglycemia in the liquid GE in rats. Male Wistar adult rats (280-310 g) were pretreated intravenously with AT, Dp, AT plus Dp or their vehicle and then treated 30 min later with iv insulin or its vehicle (n=8-10 animals/group). Thirty min after treatment, GE was evaluated by determining, in awake rats, the percent gastric retention (%GR) of a saline meal labeled with phenol red administered by gavage. The results indicated that insulin...

Effect of 4-aminoantipyrine on gastric compliance and liquid emptying in rats

Palavras-chave: Hypoglycemia; Gastric emptying; Dipyrone; Atropine; Muscarinic receptors; Adrenergic receptors.

Ano: 2017

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2017001000610

Dipyrone (Dp) delays gastric emptying (GE) in rats. There is no information about whether 4-aminoantipyrine (AA), one of its metabolites, has the same effect. The objectives of the present study were to assess the effects of AA and Dp on GE when administered intravenously (iv) and intracerebroventricularly (icv) (240 µmol/kg and 4 µmol/animal, respectively) and on gastric compliance when administered iv (240 µmol/kg). GE was determined in male Wistar rats weighing 250-300 g (5-10 per group) after icv or iv injection of the drug by measuring percent gastric retention (GR) of a saline meal labeled with phenol red 10 min after administration by gavage. Gastric compliance was estimated in anesthetized rats (10-11 per group), with the construction of...

Intravenous dipyrone for the acute treatment of episodic tension-type headache: A randomized, placebo-controlled, double-blind study

Palavras-chave: Gastric emptying; Gastric compliance; 4-Aminoantipyrine; Dipyrone; Vagus nerve.

Ano: 2007

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2007000700003

Bigal,M.E.; Bordini,C.A.; Speciali,J.G..

Acute headaches are responsible for a significant percentage of the case load at primary care units and emergency rooms in Brazil. Dipyrone (metamizol) is easily available in these settings, being the most frequently used drug. We conducted a randomized, placebo-controlled, double-blind study to assess the effect of dipyrone in the acute treatment of episodic tension-type headache. Sixty patients were randomized to receive placebo (intravenous injection of 10 ml saline) or 1 g dipyrone in 10 ml saline. We used seven parameters of analgesic evaluation. The patients receiving dipyrone showed a statistically significant improvement (P<0.05) of pain compared to placebo up to 30 min after drug administration. The therapeutic gain was 30% in 30 min and 40% in...

An electronic pressure-meter nociception paw test for mice

Palavras-chave: Episodic tension-type headache; Acute treatment; Dipyrone; Metamizol; Placebo.

Ano: 2002

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2002001000005

Cunha,T.M.; Verri Jr.,W.A.; Vivancos,G.G.; Moreira,I.F.; Reis,S.; Parada,C.A.; Cunha,F.Q.; Ferreira,S.H..

The aim of the present investigation was to describe and validate an electronic mechanical test for quantification of the intensity of inflammatory nociception in mice. The electronic pressure-meter test consists of inducing the animal hindpaw flexion reflex by poking the plantar region with a polypropylene pipette tip adapted to a hand-held force transducer. This method was compared to the classical von Frey filaments test in which pressure intensity is automatically recorded after the nociceptive hindpaw flexion reflex. The electronic pressure-meter and the von Frey filaments were used to detect time versus treatment interactions of carrageenin-induced hypernociception. In two separate experiments, the electronic pressure-meter was more sensitive than...

Do endogenous opioids and nitric oxide participate in the anticonvulsant action of dipyrone?

Palavras-chave: Hyperalgesia; Nociception; Indomethacin; Dipyrone; Von Frey filaments.

Ano: 2004

URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2004000300018

Reis,G.M.L.; Doretto,M.C.; Duarte,I.D.G.; Tatsuo,M.A.K.F..

It was previously reported that systemic administration of dipyrone inhibited the tonic component of generalized tonic-clonic seizures in both the electroshock and the audiogenic seizure models. The aim of the present study was to investigate the mechanisms involved in the anticonvulsant action of dipyrone by assessing the role of nitric oxide and opioids in the electroshock (female 60- to 90-day-old Wistar rats, N = 5-11) and audiogenic seizure (female 60- to 90-day-old Wistar audiogenic rats, N = 5-11) models of epilepsy. Naloxone (5 mg/kg, sc) significantly reversed the anticonvulsant effect of dipyrone in rats submitted to the induction of audiogenic seizures (ANOVA/Bonferroni's test), suggesting the involvement of opioid peptides in this action. In...