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1.
Braz. j. med. biol. res ; 52(2): e8103, 2019.
Article in English | LILACS | ID: biblio-974278

ABSTRACT

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 agents. Clinically, it has been demonstrated that dipyrone is effective in the control of colic-like abdominal pain originating from the biliary and intestinal tracts. Since studies in humans and animals have demonstrated the presence of β2-adrenoceptors in biliary tract smooth muscle and β2-adrenoceptor activation has been shown to occur in dipyrone-induced delayed GE, it is likely that this kind of receptors may participate in the reduction of smooth muscle spasm of the sphincter of Oddi induced by dipyrone. There is no evidence that dipyrone may interfere with small bowel and colon motility, and the clinical results of its therapeutic use in intestinal colic appear to be due to its analgesic effect.


Subject(s)
Animals , Rats , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Ampyrone/pharmacology , Antipyrine/pharmacology , Dipyrone/pharmacology , Gastric Emptying/drug effects , Autonomic Nerve Block , Dipyrone/administration & dosage , Rats, Wistar
2.
Braz. j. med. biol. res ; 50(10): e5948, 2017. tab, graf
Article in English | LILACS | ID: biblio-888932

ABSTRACT

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 induced hypoglycemia in a dose-dependent manner resulting in a significant reduction in %GR of liquid only at the highest dose tested (1 U/kg). Pretreatment with AT significantly increased %GR in the rats treated with 1 U/kg insulin. Surprisingly, after pretreatment with AT, the group treated with the lowest dose of insulin (0.25 U/kg) displayed significantly lower %GR compared to its control (vehicle-treated group), which was not seen in the non-pretreated animals. Pretreatment with Dp alone at the dose of 40 mg/kg induced an increase in %GR in both vehicle and 0.25 U/kg-treated rats. A higher dose of Dp alone (80 mg/kg) significantly reduced the effect of a marked hypoglycemia induced by 1 U/kg of insulin on GE while in combination with AT the effect was completely abolished. The results with AT suggest that moderate hypoglycemia may render the inhibitory mechanisms of GE ineffective while Dp alone and in combination with AT significantly overcame the effect of hypoglycemia on GE.


Subject(s)
Animals , Male , Rats , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Atropine/pharmacology , Dipyrone/pharmacology , Gastric Emptying/drug effects , Hypoglycemia/physiopathology , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Atropine/administration & dosage , Dipyrone/administration & dosage , Dose-Response Relationship, Drug , Drug Therapy, Combination , Hypoglycemia/chemically induced , Hypoglycemic Agents/administration & dosage , Insulin/administration & dosage , Models, Animal , Premedication , Rats, Wistar
3.
Braz. j. med. biol. res ; 49(3): e5011, Mar. 2016. graf
Article in English | LILACS | ID: lil-771943

ABSTRACT

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, rats were subjected to surgical resection of the celiac-superior mesenteric ganglion complex or to sham surgery. The groups were intravenously treated with saline (S), 240 µmol/kg Dp, AA, or At, 15 min after pretreatment with the antagonists or V and nine days after surgery. GE was determined 10 min later by measuring the percentage of gastric retention (%GR) of saline labeled with phenol red 10 min after gavage. The %GR (means±SE, n=6) values indicated that BUT abolished the effect of Dp (BUT+Dp vs V+Dp: 35.0%±5.1% vs 56.4%±2.7%) and At (BUT+At vs V+At: 33.5%±4.7% vs 52.9%±2.6%) on GE, and significantly reduced (P<0.05) the effect of AA (BUT+AA vs V+AA: 48.0%±5.0% vs 65.2%±3.8%). ATE, SRA, and sympathectomy did not modify the effects of treatments. These results suggest that β2-adrenoceptor activation occurred in delayed liquid gastric emptying induced by the phenylpyrazole derivatives dipyrone, 4-aminoantipyrine, and antipyrine. Additionally, the released neurotransmitter did not originate in the celiac-superior mesenteric ganglion complex.


Subject(s)
Animals , Male , Adrenergic beta-Antagonists/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antipyrine/administration & dosage , Ganglionectomy , Gastric Emptying/drug effects , Receptors, Adrenergic, beta/metabolism , Adrenergic beta-Antagonists/administration & dosage , Ampyrone/pharmacology , Atenolol/pharmacology , Butoxamine/pharmacology , Dipyrone/pharmacology , Dose-Response Relationship, Drug , Ganglia, Sympathetic/surgery , Models, Animal , Propanolamines/pharmacology , Rats, Wistar , Sympathetic Nervous System/drug effects
4.
Braz. oral res. (Online) ; 30(1): e11, 2016. tab, graf
Article in English | LILACS | ID: lil-768253

ABSTRACT

Abstract The purpose of the present study was to evaluate the effect of common pediatric liquid medicines on surface roughness and tooth structure loss and to evaluate the pH values of these medicines at room and cold temperatures in vitro. Eighty-four bovine enamel blocks were divided into seven groups (n = 12): G1-Alivium®, G2-Novalgina®, G3-Betamox®, G4-Clavulin®, G5-Claritin®, G6-Polaramine® and G7-Milli-Q water (negative control). The pH was determined and the samples were immersed in each treatment 3x/day for 5 min. 3D non-contact profilometry was used to determine surface roughness (linear Ra, volumetric Sa) and the Gap formed between treated and control areas in each block. Scanning electron microscopy (SEM) and energy dispersive spectrometry (EDS) were also performed. The majority of liquid medicines had pH ≤ 5.50. G1, G4, and G5 showed alterations in Ra when compared with G7 (p < 0.05). According to Sa and Gap results, only G5 was different from G7 (p < 0.05). Alteration in surface was more evident in G5 SEM images. EDS revealed high concentrations of carbon, oxygen, phosphorus, and calcium in all tested groups. Despite the low pH values of all evaluated medicines, only Alivium®, Clavulin®, and Claritin® increased linear surface roughness, and only Claritin® demonstrated the in vitro capacity to produce significant tooth structure loss.


Subject(s)
Animals , Cattle , Analgesics/chemistry , Anti-Bacterial Agents/chemistry , Dental Enamel/drug effects , Amoxicillin-Potassium Clavulanate Combination/chemistry , Amoxicillin-Potassium Clavulanate Combination/pharmacology , Cold Temperature , Chlorpheniramine/chemistry , Chlorpheniramine/pharmacology , Dental Enamel/chemistry , Dipyrone/chemistry , Dipyrone/pharmacology , Hardness Tests , Hydrogen-Ion Concentration , Loratadine/chemistry , Loratadine/pharmacology , Microscopy, Electron, Scanning , Spectrometry, X-Ray Emission , Statistics, Nonparametric , Surface Properties/drug effects
5.
Rev. méd. Chile ; 143(2): 147-157, feb. 2015. graf, tab
Article in Spanish | LILACS | ID: lil-742565

ABSTRACT

Background: There is a gap between the number of patients requiring a renal allograft and the number of potential deceased donors (DD). One alternative is using allografts from non-related living donors (NRLD). Aim: To compare survival and complications of renal allograft recipients from DD, related living donors (RLD) and NRLD. Material and Methods: Observational study of a cohort of renal allograft recipients. Of 253 transplants performed in a Chilean region between 1981 and 2003, 20 patients received and allograft from a NRLD. Graft and patient survival of these patients were compared with those of 93 patients receiving an allograft from a related living donor and 140 receiving it from a DD. Patients were followed for 10 years or until death or dialysis requirement. Results: No significant differences between groups in graft and patient survival, deaths with a functioning graft or return to dialysis were observed. Receptors of DD had more hospital admissions during the first years after receiving the graft, usually due to infections. Also a delayed graft function was more common among them. Glomerular filtration rate ten years after the graft was similar among the three groups. Conclusions: No differences in graft or patient survival was observed between patients receiving a renal allograft from NRLD, RLD or DD.


Subject(s)
Animals , Female , Mice , Rats , Analgesics , Anti-Inflammatory Agents, Non-Steroidal , Niacinamide/analogs & derivatives , Niacinamide/pharmacology , Amides/pharmacology , Carrageenan , Dipyrone/pharmacology , Edema/chemically induced , Edema/drug therapy , Formaldehyde , Hot Temperature , Isomerism , Motor Activity/drug effects , Pain Measurement/drug effects , Picolinic Acids/pharmacology , Poly(ADP-ribose) Polymerases/antagonists & inhibitors , Postural Balance/drug effects , Rats, Wistar
6.
Braz. j. med. biol. res ; 42(11): 1086-1089, Nov. 2009. ilus
Article in English | LILACS | ID: lil-529097

ABSTRACT

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 percent gastric retention (GR) of saline labeled with phenol red 10 min after orogastric administration. Percent GR (mean ± SEM, N = 8) in animals pretreated with Cps and treated with Dp, AA or At (35.8 ± 3.2, 35.4 ± 2.2, and 35.6 ± 2 percent, respectively) did not differ from the GR of saline-treated animals pretreated with vehicle (36.8 ± 2.8 percent) and was significantly lower than in animals pretreated with vehicle and treated with the drugs (52.1 ± 2.8, 66.2 ± 4, and 55.8 ± 3 percent, respectively). The effect of icv administration of Dp (N = 6) was not modified by pretreatment with Cps (63.3 ± 5.7 percent) compared to Dp-treated animals pretreated with vehicle (62.3 ± 2.4 percent). The results suggest the participation of capsaicin-sensitive afferent fibers in the delayed GE induced by iv administration of Dp, AA and At, but not of icv Dp.


Subject(s)
Animals , Male , Rats , Afferent Pathways/drug effects , Ampyrone/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antipyrine/pharmacology , Dipyrone/pharmacology , Ampyrone/administration & dosage , Animals, Newborn , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Antipyrine/administration & dosage , Capsaicin , Dipyrone/administration & dosage , Dose-Response Relationship, Drug , Gastric Emptying/drug effects , Rats, Wistar
7.
Rev. AMRIGS ; 53(3): 251-256, jul.-set. 2009. ilus
Article in Portuguese | LILACS | ID: lil-566958

ABSTRACT

Introdução: Relatos das prevalências de interações medicamentosas em hospitais brasileiros são escassos. Objetivos: Descrever a prevalência de interações medicamentosas potenciais entre os fármacos prescritos nas enfermarias clínicas e cirúrgicas de um hospital-escola. secundariamente, descrever as características dessas interações e relacionar a sua ocorrência com o número de medicamentos prescritos e a idade dos pacientes. Pacientes e Métodos: Os dados foram coletados durante uma semana de out/2007, de 2a a 6a feira, a partir da última ficha de prescrição encontrada nos prontuários, envolvendo 128 fichas de prescrição com 10,5±4,1 fármacos. Os pacientes tinham 58,6±16,9 anos e 51,2% eram homens. A doença cardiovascular foi a enfermidade principal (23,4%) e a comorbidade (42,5%) mais frequentemente encontrada. A análise das interações foi feita através de consulta a um sistema interativo (Micromedex®). Resultados: 485 interações foram encontradas, estando presentes em 79,7% (IC95%: 72,6-86,8) das fichas de prescrição (média 3,8). A interação mais frequente foi captopril/dipirona (9,7%), seguida por dipirona/furosemida (4,5%), e os fármacos mais envolvidos foram dipirona (29,3%) e captopril (21,2%). A maioria das interações tinha mecanismo farmacodinâmico (65,5%), gravidade moderada (55,5%), começo tardio (61,3%) e bom embasamento científico (71,1%). A prevalência de interações esteve associada fortemente com o número de fármacos prescritos (r=0,65, p<0,001) e fracamente com a idade do paciente.


Introduction: Reports of the prevalence of drug interactions in Brazilian hospitals are scarce. Aims: To describe the prevalence of potential drug interactions among the medical drugs prescribed in the clinical and surgical units of a teaching hospital. Secondarily, to describe the characteristics of drug interactions and relate their occurrence to the number of prescribed medications and patient age. Patients and Methods: The data were collected from Monday to Friday of a week in Oct 2007, starting from the last prescription form found in the medical charts, and involved 128 prescription forms with 10.5±4.1 drugs. The patients’ mean age was 58.6±16.9 years and 51.2% were males. Cardiovascular disease was the main disease (23.4%) and the most frequently found comorbidity (42.5%). The analysis of interactions was done through consultation with an interactive system (Micromedex®). Results: 485 cases of drug interactions were found, being present in 79.7% (CI95%: 72.686.8) of the prescription forms (mean 3.8). The most frequent interaction was captopril/dipyrone (9.7%), followed by ipyrone/furosemide (4,5%), and the most frequently involved drugs were dipyrone (29.3%) and captopril (21.2%). Most of the interactions had a pharmacodynamic mechanism (65.5%), moderate severity (55.5%), late onset (61.3%), and a good scientific basis (71.1%). The prevalence of interactions was strongly associated with the number of drugs prescribed (r=0.65, p<0.001) and weakly associated with patient age.


Subject(s)
Humans , Male , Female , Captopril/administration & dosage , Captopril , Captopril/adverse effects , Dipyrone/administration & dosage , Dipyrone , Dipyrone/adverse effects , Dipyrone/pharmacology , Drug Prescriptions , Prevalence , Homeopathic Prescription , Hospitals, Teaching/organization & administration , Hospitals, Teaching , Hospitals, Teaching/trends
8.
Cir. & cir ; 76(3): 241-246, mayo-jun. 2008. graf, tab
Article in Spanish | LILACS | ID: lil-567102

ABSTRACT

BACKGROUND: Combinations of analgesic drugs have been used as an option for treating pain because some types of pain are difficult to relieve with conventional analgesics. This group of drugs has been combined with analgesics or drugs without analgesic effect and is called adjuvant. One such drug is caffeine. METHODS: We undertook the present study to analyze if caffeine is able to potentiate the antinociceptive effect of metamizole in the formalin model. RESULTS: Metamizole produced a dose-dependent antinociceptive effect with ED(50) = 329.61 mg/kg in the formalin model. Caffeine at the following doses (3.16, 10.0, 17.8 and 31.6 mg/kg) also showed antinociceptive effect. When a subeffective dose of metamizole (100 mg/kg) was combined with caffeine (3.16, 10.0, 17.8 or 31.6 mg/kg), higher antinociceptive effects were produced than the corresponding effects produced by metamizole alone. One combination presented potentiation effect; the other combination showed antinociceptive effect that was not different from the effects of metamizole alone. Two combinations showed an effect lower than the corresponding effect produced by metamizole alone. CONCLUSIONS: Adjuvant caffeine is able to change the effect of metamizole in the inflammatory pain model, in which caffeine also presents an antinociceptive effect.


Subject(s)
Animals , Male , Rats , Analgesics/pharmacology , Caffeine/pharmacology , Dipyrone/pharmacology , Dose-Response Relationship, Drug , Drug Synergism , Rats, Wistar
9.
Braz. j. med. biol. res ; 40(7): 903-909, July 2007. graf
Article in English | LILACS | ID: lil-455993

ABSTRACT

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 æmol/kg and 4 æmol/animal, respectively) and on gastric compliance when administered iv (240 æmol/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 volume-pressure curves during intragastric infusion of a saline meal. Compliance was significantly greater in animals receiving Dp (mean ± SEM = 0.26 ± 0.009 mL/mmHg) and AA (0.24 ± 0.012 mL/mmHg) than in controls (0.19 ± 0.009 mL/mmHg). AA and Dp administered iv significantly increased GR (64.4 ± 2.5 and 54.3 ± 3.8 percent, respectively) compared to control (34 ± 2.2 percent), a phenomenon observed only with Dp after icv administration. Subdiaphragmatic vagotomy reduced the effect of AA (GR = 31.4 ± 1.5 percent) compared to sham-treated animals. Baclofen, a GABA B receptor agonist, administered icv significantly reduced the effect of AA (GR = 28.1 ± 1.3 percent). We conclude that Dp and AA increased gastric compliance and AA delayed GE, with the participation of the vagus nerve, through a pathway that does not involve a direct action of the drug on the central nervous system.


Subject(s)
Animals , Male , Rats , Ampyrone/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Dipyrone/pharmacology , Gastric Emptying/drug effects , Ampyrone/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Dose-Response Relationship, Drug , Dipyrone/administration & dosage , Injections, Intravenous , Injections, Intraventricular , Rats, Wistar , Time Factors , Vagus Nerve/drug effects
10.
RBCF, Rev. bras. ciênc. farm. (Impr.) ; 42(4): 514-522, out.-dez. 2006. graf
Article in Portuguese | LILACS | ID: lil-446372

ABSTRACT

O efeito analgésico de longa duração da dipirona foi avaliado em um modelo de dor neuropática assim como a participação da via óxido nítrico-GMPc neste mecanismo analgésico. Uma única administração intraplantar de dipirona (80 æg), no 14° dia após a instalação da hiperalgesia neuropática induzida pela constrição do nervo ciático exerceu um efeito analgésico, significativo e de longa duração. A inibição da óxido nítrico sintetase com L-NAME (50 ou 100 æg/pata), ou do óxido nítrico (NO) endógeno com hemoglobina (10 ou 30 æg/pata), bloquearam o desenvolvimento do efeito analgésico da dipirona. A L-arginina (500 æg/pata) reverteu o efeito do L-NAME. Cloreto de metiltionínio (azul de metileno) (500 æg/pata), ODQ (50 æg/pata) (bloqueadores da guanilil ciclase) ou glibenclamida (100, 200 ou 300 æg/pata) (bloqueador de canais de K+ sensíveis ao ATP) inibiram o efeito analgésico da dipirona. O nitroprussiato de sódio administrado no 14° dia após a instalação da hiperalgesia neuropática também exerceu efeito analgésico de longa duração, semelhante ao observado com a dipirona. Sugerimos que a ação analgésica periférica e de longa duração da dipirona, neste modelo experimental, ocorra devido a provável dessensibilização dos nociceptores, envolvendo a via óxido nítrico - GMPc e canais de K+ sensíveis ao ATP.


The long term analgesic effect of dipyrone was evaluated on a model of neuropathic pain and the role of nitric oxide/GMPc pathway in this antinociceptive mechanism. One intraplantar dipyrone administration (80 mg), at 14th day after the chronic constriction injury of the sciatic nerve, induced a significant and long term analgesic effect. The inhibition of nitric oxide synthase (NOS) with L-NAME (50 or 100 mg/paw) or scavenging of the endogenous NO with hemoglobin (10 or 30 mg/paw) inhibited the development of the dipyrone analgesia. L-arginine (500 mg/paw) could reverted the effect of L-NAME. Metylene blue (500 mg/paw) or ODQ (50 mg/paw) (blockers of guanyl cyclase), or glybenclamide (100, 200 or 300 mg/paw) (blocker of ATP-sensitive K+ channels) inhibited the development of dipyrone analgesia. The sodium nitroprussiate administered at 14th day after the chronic constriction injury of the sciatic nerve also induced a long term analgesic effect similar to that of dipyrone. Our data may support the suggestion that the peripheral and the long term analgesic action of dipyrone on this model experimental occurs due to a probable nociceptor desensitisation with involviment of activation of the nitric oxide-cGMP pathway, followed by an opening of ATP-sensitive K+ channels.


Subject(s)
Drug Evaluation , Dipyrone/pharmacology , Hyperalgesia/metabolism , Nitric Oxide , Sciatic Nerve/metabolism , Nociceptors
11.
Braz. j. med. biol. res ; 39(11): 1507-1512, Nov. 2006. ilus
Article in English | LILACS | ID: lil-437825

ABSTRACT

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 ( percentGR) 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 percent) compared to control (33.4 ± 1.5 percent) but did not differ from the Dp group (54.3 ± 3.8 percent). After icv administration of At, percentGR (34.2 ± 2 percent) did not differ from control (32.6 ± 1.9 percent), but was significantly higher after Dp (54.5 ± 2.3 percent). Subdiaphragmatic vagotomy significantly reduced percentGR in the At group (30.2 ± 0.7 percent) compared to the sham group, but was significantly higher than in the controls (23.0 ± 0.5 percent). In the animals treated with At iv, baclofen significantly reduced percentGR (28.3 ± 2.4 percent) compared to vehicle-treated animals (55.2 ± 3.2 percent). The same occurred in the animals treated iv with vehicle and icv with baclofen. Although vagotomy and baclofen reduced percentGR per se, the reduction was twice more marked in the animals treated with At. The results suggest that At administered iv, but not icv, delays GE of liquid in rats with the participation, at least in part, of the vagus nerve and that this phenomenon is blocked by the activation of GABA B receptors in the central nervous system.


Subject(s)
Animals , Male , Rats , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antipyrine/pharmacology , Dipyrone/pharmacology , Gastric Emptying/drug effects , Baclofen/pharmacology , Dose-Response Relationship, Drug , GABA Agonists/pharmacology , Injections, Intraventricular , Rats, Wistar , Time Factors , Vagus Nerve/drug effects
13.
Braz. j. med. biol. res ; 38(1): 99-104, Jan. 2005. graf
Article in English | LILACS | ID: lil-405551

ABSTRACT

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 ( percentGR) 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 æmol/kg) dipyrone (Dp iv), followed by icv injection of 10 æl vehicle (bac0), or 0.5 (bac0.5), 1 (bac1) or 2 æg (bac2) baclofen. In the second experiment, the animals were injected icv with 5 æl vehicle (Cicv) or an equal volume of a solution containing 4 æmol (1333.2 æg) dipyrone (Dp icv), followed by 5 æl vehicle (bac0) or 1 æg baclofen (bac1). GE was determined 10 min after icv injection. There was no significant difference between control animals from one experiment to another concerning GR values. Baclofen at the doses of 1 and 2 æg significantly reduced mean percentGR induced by iv dipyrone (Dp iv bac1 = 35.9 percent and Dp iv bac2 = 26.9 percent vs Dp iv bac0 = 51.8 percent). Similarly, baclofen significantly reduced the effect of dipyrone injected icv (mean percentGR: Dp icv bac1 = 30.4 percent vs Dp icv bac0 = 54.2 percent). The present results suggest that dipyrone induces delayed GE through a route in the central nervous system that is blocked by the activation of GABA B receptors.


Subject(s)
Animals , Male , Rats , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Baclofen/pharmacology , Dipyrone/pharmacology , GABA Agonists/pharmacology , Gastric Emptying/drug effects , Receptors, GABA-B/agonists , Central Nervous System/drug effects , Rats, Wistar
14.
Indian J Exp Biol ; 2004 Jun; 42(6): 567-9
Article in English | IMSEAR | ID: sea-63185

ABSTRACT

Biliary, ureteric and intestinal colic are extremely common clinical conditions associated with smooth muscle spasm. In the present study, antispasmodic activity was carried out against acetylcholine (10-640 ng/ml)-induced contractions on guinea pig ileum. Acetylcholine (10-640 ng/ml) induced concentration-dependent contraction of smooth muscle. Diclofenac, in varying concentration (9.4 x 10(-5) mol/l and 14.1 x 10(-5) mol/l) shifted the concentration response curve of acetylcholine to the right without suppressing the maximal response. However, in higher concentration diclofenac (18.9 x 10(-5) mol/l) blocked the response in an unsurmountable fashion. Further, analgin (11.09 x 10(-5), 16.63 x 10(-5) and 22.18 x 10(-5) mol/l) in equimolar concentrations did not alter the concentration response curve of acetylcholine, but in higher concentration analgin (44.36 x 10(-5) mol/l) also blocked the response in an unsurmountable fashion. Pitofenone (2.5 x 10(-6) mol/l) also, shifted the concentration response curve of acetylcholine to right in a parallel fashion with no change in maximal response. The present study confirms the potent antispasmodic activity of diclofenac-pitofenone combination in comparison to analgin-pitofenone in molar equivalent concentration (in comparison to diclofenac) against acetylcholine-induced contractions of guinea pig ileum.


Subject(s)
Acetylcholine/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Benzophenones/pharmacology , Cholinergic Agents/metabolism , Diclofenac/pharmacology , Dipyrone/pharmacology , Dose-Response Relationship, Drug , Female , Guinea Pigs , Ileum/drug effects , Male , Muscle Contraction , Muscle, Smooth/drug effects , Parasympatholytics/pharmacology , Spasm/drug therapy
16.
Rev. ADM ; 57(2): 50-3, mar.-abr. 2000. ilus, tab
Article in Spanish | LILACS | ID: lil-268002

ABSTRACT

El presente trabajo tuvo como objetivo establecer la influencia de la administración de dos analgésicos, el ácido acetilsalicílico y la pirazolona metamizol, en la respuesta de la pulpa dental a las pruebas térmica y eléctrica. El estudio se desarrolló en alumnos voluntarios de la Clínica Odontológica Almaraz. Los resultados muestran que la ingesta de estos analgésicos no modifica la respuesta pulpar, excepto la administración del ácido acetilsalicílico, el cual modificó la respuesta con la prueba eléctrica de manera significativa. Se discute la metodología y los resultados obtenidos y se plantea la posibilidad de continuar con esta línea de investigación


Subject(s)
Humans , Male , Female , Adult , Analgesics/administration & dosage , Aspirin/pharmacology , Dental Pulp/drug effects , Dipyrone/pharmacology , Cold Temperature , Dental Pulp Test , Hot Temperature , Data Collection/methods , Toothache/diagnosis
17.
Braz. j. med. biol. res ; 29(11): 1543-8, Nov. 1996. graf
Article in English | LILACS | ID: lil-187219

ABSTRACT

Paw edema was induced in male Wistar rats (200-250 g) by intraplantar (ipl) administration of 2.5 mug endotoxin (Etx). Etx, like carrageenin, produced two distinct edema formation phases, an early phase (75 min) followed by a late phase (7 h). We showed that the edema formation in the early phase was antagonized by dipyrone (80 mg/kg, ip) and indomethacin (1 mg/kg, ip) by 52 per cent and 52 per cent, respectively, and that the late phase was resistant to these drugs. These result suggest that in the early phase prostaglandins appear to be involved in the process. However, the activation of the kinin cascade leading to the release of other mediators may be involved in the increase of edema in the late phase. To test this hypothesis, we investigated whether the release of nitric oxide (NO) is involved in the mechanism of endotoxin-induced rat paw edema during the late phase, using Nw-nitro-L-arginine methyl ester (L-NAME) (50 mug, ipl) as inhibitor of NO synthase and L-arginine (1 mg, ipl) as substrate of NO synthase. The paw edema induced by Etx was inhibited by L-NAME by 56 per cent and increased by L-arginine by 81 per cent. Furthermore, L-arginine given in combination with L-NAME completely reversed the inhibitions of Etx-induced edema produced by L-NAME. These results support the hypothesis that in the late phase NO production is associated with the edema evoked by Etx.


Subject(s)
Rats , Animals , Male , Dipyrone/pharmacology , Edema/drug therapy , NG-Nitroarginine Methyl Ester/pharmacology , Nitric Oxide/metabolism , Edema/chemically induced , Extremities , Rats, Wistar
18.
Indian J Physiol Pharmacol ; 1995 Apr; 39(2): 154-6
Article in English | IMSEAR | ID: sea-108216

ABSTRACT

Cypermethrin a widely used insecticide of Pyrethroids (type II) group, was administered in mice at two dose levels (1/10 of LD50 i.e. 2.5 mg/kg and 1/5 of LD50 i.e. 5.0 mg/kg) and pharmacodynamic interactions of insecticide were studied with centrally acting drugs viz. pentobarbital sodium, amphetamine, pentylenetetrazole, acepromazine and analgin. Cypermethrin pretreatment potentiated the actions of pentobarbital and pentylene-tetrazole as evidenced by an increase in pentobarbital induced hypnosis and duration of pentylene-tetrazole induced chemoshock seizures. Tranquilizing action of acepromazine was potentiated but there was decrease in amphetamine influenced locomotor activity at both the dose levels. Cypermethrin pretreatment, however, did not have any pharmacodynamic interaction with analgin.


Subject(s)
Acepromazine/pharmacology , Amphetamine/pharmacology , Animals , Central Nervous System Agents/pharmacology , Dipyrone/pharmacology , Drug Interactions , Insecticides/toxicity , Lethal Dose 50 , Male , Mice , Motor Activity/drug effects , Pentobarbital/pharmacology , Pentylenetetrazole/pharmacology , Pyrethrins/toxicity , Seizures/chemically induced , Sleep/drug effects
19.
Bol. méd. Hosp. Infant. Méx ; 52(2): 98-104, feb. 1995. tab
Article in Spanish | LILACS | ID: lil-149544

ABSTRACT

Introducción. El dolor es una manifestación clínica común en la práctica médica y una de las principales razones por la que los pacientes pediátricos solicitan y requieren atención médica. Por ello, el objetivo del presente trabajo fue el de describir la frecuencia con que se indican analgésicos y las características de dicha prescripción en el tratamiento del dolor posoperatorio en niños. Material y métodos. El diseño del estudio fue de cohortes comparativas retrolectivas y se llevó a cabo en un hospital pediátrico de tercer nivel de atención médica. Se estudiaron los expedientes clínicos de 125 niños, a quienes se les practicó una cirugía abdominal; en ellos se identificó la indicación de analgésico, el tipo, la dosis, la vía de administración y el número de dosis aplicadas. Resultados. Se prescribió analgésico en 107 pacientes (86 por ciento), el cual se aplicó en 92 (74 por ciento) y a dosis adecuadas en 28 (22 por ciento). El analgésico más utilizado fue la dimetilpirazolona (metamizol sódico) (87 por ciento), seguido de la nalbufina (12 por ciento) y el acetaminofén (1 por ciento). Se prescribió una dosis mayor a la recomendada en 77 casos (72 por ciento) y una dosis menor a los estándares en dos niños (2 por ciento). La sobredosificación ocurrió en todos los casos para la dimetilpirazolona (RM= 26.4, IC 95 por ciento = 4.7-90.9, P= 0.000002). La administración de los analgésicos ocurrió en el 44 por ciento de los neonatos y en 64 por ciento de los lactantes, comparados con el 88 por ciento de escolares y adolescentes (RM = 6.6,IC 95 por ciento = 1.7-27.3, P=0.002). Conclusiones. En niños posoperados de cirugía abdominal se administraron analgésicos en el 74 por ciento, los cuales se aplican correctamente en sólo el 22 por ciento de los mismos. Se observó una tendencia a una menor indicación y administración en los niños de menor edad


Subject(s)
Infant, Newborn , Infant , Child, Preschool , Child , Adolescent , Humans , Acetaminophen/administration & dosage , Acetaminophen/pharmacology , Dipyrone/administration & dosage , Dipyrone/pharmacology , Pain, Postoperative/drug therapy , Drug Utilization/statistics & numerical data , Drug Utilization/standards
20.
Bol. venez. infectol ; 4(1/2): 14-15, ene.-dic. 1994.
Article in Spanish | LILACS | ID: lil-721175

ABSTRACT

Se presenta un caso excepcional de síndrome febril prolongado debido a la infección simultánea por Salmonella notyphi y Brucella, en una paciente de 29 años, de origen portugués, que adquirió su enfermedad en una visita a una región rural de su país de origen, en donde ingirió leche y quesos no pasteurizados de vaca y de cabra. Se destacan la ocurrencia inusual de manifestaciones cutáneas y gastrointestinales, así como la necesidad de un tratamiento combinado adecuado por un período de tiempo prolongado para evitar la ocurrencia de recaídas.


Subject(s)
Humans , Adult , Female , Brucellosis/diagnosis , Dipyrone/administration & dosage , Chills/diagnosis , Fever/diagnosis , Salmonella Infections/diagnosis , Dipyrone/pharmacology , Infectious Disease Medicine
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