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PubMed1990

Lack of tumorigenicity of aminopyrine orally administered to B6C3F1 mice.

To test the tumorigenic potential of aminopyrine, an antipyretic analgesic, it was administered in drinking water at levels of 0 (control), 0.04 and 0.08% to 50 male and 50 female B6C3F1 mice for 100 weeks, and the mice were subsequently maintained without aminopyrine for a further 4 weeks. The most frequent types of tumor, in both treated and control groups, were hepatocellular tumor in male mice and malignant lymphoma/lymphoid leukemia in female mice. No statistically significant differences were observed in the incidences of these tumors between treated and control groups. The incidences of several other tumors in male and female mice also showed no statistically significant differences between treated and control groups. Therefore, no tumorigenic effect of orally administered aminopyrine in B6C3F1 mice was apparent in the present study.

Administration, Oral↗
PubMed1979

The [14C]-aminopyrine breath test. A comparison of different forms of analysis.

1 Following ingestion of [14C]-aminopyrine, breath 14CO2 data were analysed from normal individuals, patients with hepatic disease, epileptics receiving anticonvulsant therapy and volunteers before and after treatment with glutethimide. 2 The 'standard' 2 h [14C]-aminopyrine breath test discriminated successfully between the main groups but failed to detect the change in microsomal enzyme function produced by glutethimide. 3 A 'modified' form of the 2 h breath test calculated from the area under the breath specific activity curve detected the increase in demethylation following glutethimide. 4 The breath elimination constant (Kb) derived from the breath 14CO2 disappearance curve was as sensitive as the 'modified' 2 h breath test and was simpler to compute. 5 Glutethimide 500 mg/day for 14 days resulted in a 42% increase in the metabolic clearance of antipyrine and a 26% increase in demethylation of [14C]-aminopyrine.

Aminopyrine↗
PubMed1980

Kinetics and metabolism of pyrazolones (propyphenazone, aminopyrine and dipyrone).

1 Propyphenazone 220 mg was administered orally to volunteers. Maximum plasma concentrations between 1.5 microgram/ml and 3.5 micrograms/ml were found 30 min later. After comparable doses plasma concentrations in dog and rabbit were lower. The distribution volumes were 2 l/kg. 2 The major metabolic route of propyphenazone is demethylation. The main urinary metabolite is the enolglucuronide of N-(2)-demethylpropyphenazone. 3 Aminopyrine is rapidly and almost completely absorbed after oral administration. Maximum plasma concentrations of 10 microgram/ml are reached 1.5 h after a 500 mg dose. The biological half-life is 2-3 h, the relative distribution volume 60% on average, and binding to plasma proteins approximately 15%. 4 Unchanged aminopyrine is only excreted in small quantities. The major routes of metabolism are demethylation (4-methylaminoantipyrine and 4-aminoantipyrine) and acylation (4-acetyl and 4-formylaminoantipyrine). There are other biotransformation products. 5 After oral administration of [14C]-dipyrone 480 mg the maximum serum concentration of 13.4 +/- 0.8 microgram/ml occurred at 1-1.5 hours. 6 Dipyrone was not detectable in serum or urine. Four of seven metabolites were identified, and were identical with the main metabolites of aminopyrine.

Administration, Oral↗
PubMed1978

Polymorphic acetylation and aminopyrine demethylation in Gilbert's syndrome.

Polymorphic acetylation was investigated in twenty-seven patients with Gilbert's syndrome using the sulphadimidine test. Whereas the finding of 51% slow acetylators in seventy-eight control persons agreed well with the expected frequency in a continental European population, the prevalence of slow acetylators in Gilbert's syndrome was increased to 78% (P less than 0.03, Woolf's G-test). After oral administration of 14C-aminopyrine there was no significant difference between seventeen patients with Gilbert's syndrome and twenty-seven normal controls in total plasma clearance of aminopyrine (280 +/- SD 100 and 270 +/- 60 ml/min) and in the disappearance curve of 14CO2 in breath (0.23 +/- 0.04 and 0.22 +/- 0.03 h-1, respectively). Thus, whereas aminopyrine metabolism appears unaffected in the examined patients, the data documents a new association between slow acetylator status and Gilbert's syndrome.

Acetylation↗
PubMed1982

The determination of aminopyrin elimination for control of the metabolic capacity of the liver in man.

The kinetics of plasma and breath elimination of aminopyrine after 14C-aminopyrine given orally were studied using an open one-compartment model and first order rates of elimination. The study comprised eight healthy volunteers and two groups with histologically verified chronic liver diseases (cirrhosis, n = 12, and chronic aggressive hepatitis, n = 12). Elimination rates from plasma and breath were significantly reduced in the group with cirrhosis, but only so in chronic aggressive hepatitis when they were expressed relative to each other. Monomethylaminopyrine was eliminated more rapidly compared to aminopyrine, and the rate of formaldehyde formation was positively correlated to the excretion rate of CO2 (r = 0.53, P less than 0.002). No correlation was found with clinical or other laboratory data in the groups of liver diseases studied. The test is a quantitative indicator of the drug metabolizing mixed function oxidases of the endoplasmatic reticulum of the liver, and may reflect the degree of damage to this system in chronic liver disease.

Adult↗
PubMed1991

Gastrin potentiates histamine-stimulated aminopyrine accumulation in isolated rat parietal cells.

Rat gastric mucosal cells, containing 25-35% parietal cells, were obtained by a modified isolation procedure involving protease, ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid, and mechanical treatments. Parietal cell responsiveness to secretagogues was assessed by the accumulation of the weak base [14C]aminopyrine in intracellular acidic compartments. Histamine, without phosphodiesterase inhibitors, dose dependently stimulated aminopyrine accumulation with an effective concentration producing 50% of maximal response of 13 microM and a maximal effective dose of 100 microM. Pentagastrin and rat gastrin-17 alone were ineffective but potentiated dose dependently the action of 100 microM histamine. The mean potentiating effect varied from 32 to 70% for 100 nM pentagastrin and from 36 to 95% for 100 nM rat gastrin-17. Pentagastrin (100 nM) also potentiated the effect of 1 mM dibutyryladenosine 3',5'-cyclic monophosphate (cAMP) by 44%, but it did not increase further the stimulation by carbachol. The potentiating effect of pentagastrin on histamine- and dibutyryl cAMP-stimulated aminopyrine accumulation was also observed after enrichment of parietal cells to 65-85%. The endogenous histamine was insufficient to stimulate acid production. Therefore gastrin appears to have a direct action also in rat parietal cells.

Aminopyrine↗
PubMed1990

Enhancing effect of pyrrolidone derivatives on the transdermal penetration of sulfaguanidine, aminopyrine and Sudan III.

The enhancing effect of pyrrolidone derivatives on the percutaneous penetration of sulfaguanidine, aminopyrine and sudan III was investigated using in vitro technique and excised rat skin. 1-Methyl (MP), 1-hexyl (HP) and 1-lauryl-2-pyrrolidone (LP) were used as penetration enhancers. Aminopyrine showed high penetration through skin although sulfaguanidine and sudan III showed little penetration. Pyrrolidone derivatives enhanced their penetrations. Especially HP and LP enhanced the penetration of sulfaguanidine to a high extent. Sudan III was not detected in the receptor phase regardless of the presence of enhancer. Pyrrolidone derivatives significantly increased the skin accumulation of sulfaguanidine, aminopyrine and sudan III. Penetration of pyrrolidone derivatives was also determined. MP and HP showed high penetrations. LP was not detectable in the receptor phase. MP, HP and LP showed high skin accumulations. These results suggested the usefulness of pyrrolidone derivatives as percutaneous penetration enhancers.

Administration, Cutaneous↗
PubMed1980

Inhibitory action of the combination of aminopyrine and secobarbital on EEG activation, neocortical recruiting and augmenting responses in rabbits.

The effect of the combination of aminopyrine and secobarbital at a molar ratio of 2:1, the mixture and molecular compound, on rabbit EEG activation was examined. Secobarbital 40 mg/kg p.o. elevated threshold voltages in the neocortical and hippocampal EEG activation by high frequency electrical stimulation of the midbrain reticular formation (MRF), nucleus centralis medialis (CM) of the thalamus, and posterior hypothalamus (PHA) by 40, 40 and 80% respectively. Aminopyrine 80 mg/kg p.o. alone did not affect the arousal responses. The molecular compound 120 mg/kg p.o. has more potent and long-lasting actions in inhibiting the arousal responses induced by the stimulation of MRF (80%) and CM (50%) than with secobarbital alone. The inhibitory action of the mixture 120 mg/kg p.o. on the PHA-arousal response (40%) was significantly weaker than that of the molecular compound (80%). Secobarbital and the molecular compound slightly inhibited the neocortical augmenting and recruiting responses. Our findings suggest that although aminopyrine exerts a synergistic effect with secobarbital in inhibiting the EEG activation produced by MRF stimulation, in inhibiting the PHA-arousal response, there is no synergistic effect of the two drugs when they were given as the mixture. Moreover, the molecular compound rather than the mixture has a more potent inhibitory action on the EEG activation, particularly with PHA stimulation.

Aminopyrine↗
PubMed1992

Binding of epidermal growth factor to receptors in preparations of enriched porcine parietal cells and inhibition of aminopyrine uptake.

Preparations of isolated porcine gastric cells, enriched in parietal cells, were used to study binding of epidermal growth factor (EGF) to receptors and subsequent inhibition of [14C]aminopyrine uptake. EGF in concentrations from 10(-10) to 10(-7) M inhibited aminopyrine uptake stimulated by 10(-5) M histamine with an IC50 of 3 x 10(-10) M. [125]EGF bound in a saturable and specific manner to sites on cells in preparations containing 40-90% parietal cells. Mean apparent dissociation constant for the sites was 1.6 x 10(-9) M, with an average number of approximately 20,000 sites per cell. Endocytosis of ligand by parietal cells was limited, amounting to 10-20% of bound EGF after 1 h of incubation at 37 degrees C. Occupation of a fraction of the receptors caused a maximal reduction by 40% of aminopyrine uptake in histamine-stimulated cells, suggesting the occurrence of spare receptors. The results indicate the existence of specific receptors for EGF on porcine parietal cells exerting a regulatory influence on acid secretion.

Aminopyrine↗
PubMed1993

Effects of carbachol and gastrin on 14C-aminopyrine accumulated in rabbit gastric glands and cells.

The present study examines the possible existence of a mechanism regulating emptying of the secretory canaliculi content of the parietal cell and the possible effects of carbachol and gastrin on such a mechanism. In rabbit gastric glands stimulated with carbachol, 14C-aminopyrine accumulation reached a maximum after 15 min and then started to decrease. This decrease was not accompanied by a decrease in oxygen consumption, nor was any decrease of accumulated 14C-aminopyrine seen in dispersed gastric cells. In glands but not in cells stimulated with histamine together with 3-isobutyl-1-methylxanthine (IMX), carbachol induced a reduction in the accumulated 14C-aminopyrine content, whereas the effect of gastrin was less pronounced. The carbachol-induced reduction was counteracted by atropine but was not accompanied by a decrease in oxygen consumption. It is suggested that there exists a mechanism that controls the emptying of the secretory canaliculi content of the parietal cell, and that carbachol, in addition to stimulating acid production, also contributes to this emptying. Paracrine factors may be involved in this latter mechanism.

1-Methyl-3-isobutylxanthine↗
PubMed1981

Device for monitoring 14CO2 in the expired air from beagle dogs: its use in the study of aminopyrine demethylation.

1. A device for serial collection of samples for determination of 14CO2 in the expired air of the beagle dog is described. 2. The device has been evaluated using [14C]aminopyrine as a model compound. The rate of 14C excretion in the expired air initially correlated with the plasma concentrations of aminopyrine rather than the plasma concentrations of 14C. 3. The dog demethylated aminopyrine at the slower rate than the rat. Both species demethylate the unchanged drug more readily than subsequent metabolites.

Aminopyrine↗
PubMed1988

Aminopyrine metabolism in primary monolayer cultures of diabetic rat hepatocytes.

1. A new support system has been used which provides long-term maintenance of rat liver parenchymal cells in monolayer cultures. The cells, maintained on collagen gel/polychlorinated vinylidene film, expressed aminopyrine metabolizing activity for up to 5 days. This culture system was utilized to study the metabolism of aminopyrine in the liver cells isolated from normal, alloxan- and streptozotocin-diabetic rats. 2. Aminopyrine was metabolized at a slower rate in both types of cultured diabetic rat hepatocytes than in cultured normal rat hepatocytes, as judged from higher levels of the unchanged drug in the culture medium. 3. The formation of the metabolites 4-monoaminoantipyrine, 4-acetylaminoantipyrine and 4-formylaminoantipyrine decreased in the cultured diabetic rat hepatocytes, while that of 4-aminoantipyrine was at the same levels as controls. In contrast, 3-hydroxymethyl-2-methyl-4-dimethylamino-1-phenyl-3-pyrazolin-5-on e (AM-CH2OH) formation in the cultured diabetic rat hepatocytes increased over control value. These findings agree with in vivo results which have been reported by the authors. 4. The increase in AM-CH2OH was prevented by insulin in a dose-dependent manner. However, insulin did not affect the formation of other metabolites. These findings indicate that the amount of cytochrome P-450 isozyme involved in the oxidation of 3-methyl group may be regulated by insulin. 5. The present results, indicate that this primary culture system is a useful tool for the study of drug metabolism in diabetes.

Aminopyrine↗
PubMedDate not supplied

[Mechanism of the action aminopyrine].

In acute experiments on unanesthetized cats with a single and paired stimulation the effect of aminopyrine (5-30 mg/kg, intravenously) on bioelectric reactions in the conduction system of afferent impulsation at the thalamo-cortical level was studied. Aminopyrine is shown to highten the amplitude of an evoked potential of the somato-sensory cortex and of the specific transmitting nucleus of the thalamus upon stimulation of the radial nerve and to significantly lengthen with paired stimulation the regeneration period of the neuronic systems excitability in the structures under review. Investigations into the states of the cortical neuronic systems proper showed aminopyrine capable of increasing the number of high-frequency oscillations and the amplitude of the interzonal response as well as to lengthen with paired stimulation the restoration period of the neuronic systems excitability.

Aminopyrine↗
PubMed1990

Effect of Ostertagia ostertagi secretions and various putative secretagogues and inhibitors on aminopyrine accumulation in dispersed bovine abomasal gland cells.

Aminopyrine accumulation in suspensions of isolated gastric glands was used to determine the effect of Ostertagia ostertagi secretions and putative secretagogues and inhibitors on abomasal parietal cells. Parasite secretions did not affect acid production nor did histamine. Dibutyryl cyclic adenosine monophosphate (cAMP) and pentagastrin significantly increased aminopyrine accumulation by gastric glands and cimetidine, omeprazole and thiocyanate significantly decreased aminopyrine accumulation confirming their roles as stimulators and inhibitors of gastric acid production, respectively.

Abomasum↗
PubMed1975

Comparison of gastric mucosal blood flow as determined by aminopyrine clearance and gamma-labeled microspheres.

Gastric mucosal blood flow was simultaneously determined by aminopyrine clearance and gamma-labeled microspheres (15 +/- 5 mu in diameter) in anesthetized dogs prepared with a chambered segment of stomach greater curvature. Paired flow measurements were made in 11 dogs (n = 28) secreting in response to intravenous histamine (1mug per kg per min), in 11 (n = 21) nonsecreting dogs given intravenous isoproterenol (0.5 or 1.0 mug per kg per min), and in 9 (n = 10) dogs given no drugs to stimulate secretion or blood flow (resting dogs). Eight additional injections were done in dogs receiving various combinations of isoproterenol and histamine. Isotonic HCl was maintained on the mucosal surface during all experiments. Regression analysis demonstrated a highly significant linear correlation between clearance and microsphere-measured flow in the histamine (P less than 0.001, r = 0.96) and isoproterenol (P less than 0.001, r = 0.78) experiments, with clearance averaging 83% of microsphere flow during histamine stimulation but only 25% during isoproterenol. The relationship between clearance and microsphere flow was not significantly different for the resting and isoproterenol experiments. Mucosal perfusion measured by microspheres was about 5 times the resting value for both histamine and isoproterenol-stimulated dogs. Perfusion calculated from aminopyrine clearance averaged 46, 38, and 90% of the microsphere value in the resting, isoproterenol, and histamine experiments, respectively. Pooled data from secreting dogs demonstrated a fairly constant ratio of microsphere-measured flow to clearance (1.25 +/- 0.06 mean +/- SEM), regardless of the secretory rate. Our results indicate that aminopyrine clearance reflects only a small fraction of mucosal blood flow in the nonsecreting stomach, even in the presence of exogenous acid.

Aminopyrine↗
PubMed1989

Aminopyrine-N-demethylase activity of rat liver after administration of crude cannabis extract.

The effect of cannabis extract, on the hepatic aminopyrine-N-demethylase activity was studied in rats. Daily administration of cannabis extract for 15 consecutive days increased the aminopyrine-N-demethylase activity which was significant on day 15 post-treatment at 2 and 10 mg/kg doses. At 20 mg/kg, a significant increase was observed from day 7 which continued up to day 15. These findings suggest that cannabis extract can induce hepatic aminopyrine-N-demethylase activity.

Aminopyrine N-Demethylase↗
PubMed1986

Bromsulfophthalein clearance and aminopyrine test in patients with Gilbert's syndrome.

Bromsulfophthalein (BSP) clearance and aminopyrine breath tests were performed in 13 patients with Gilbert's syndrome (GS) and six healthy volunteers. The BSP clearance was significantly lower in the GS patients (1.28 +/- 0.37 dl/min) than in the healthy volunteers (1.98 +/- 0.45 dl/min). The difference in clearance was not due to a significant difference in volume of distribution. The 13 patients with Gilbert's syndrome could be divided into three groups according to their BSP disappearance curves: in 7 the curves were normal; another 3 patients the disappearance rate of BSP was normal at the beginning, but became abnormally low later on; and in the last 3 patients, an abnormal BSP disappearance rate was observed during the whole experiment. Kinetic analysis of these BSP disappearance curves indicated increased regurgitation of BSP from the liver to the blood in the second group and defective hepatic BSP uptake in the third group. The aminopyrine breath test also demonstrated heterogeneity among the GS patients. There was no correlation between the impaired BSP clearance and the aminopyrine breath test.

Adolescent↗
PubMed1985

A simple method for routine determination of the metabolic liver capacity: the aminopyrine breath test.

In 16 healthy volunteers and in 39 patients with liver diseases (fatty liver, chronic persistent and chronic active hepatitis, hepatic cirrhosis) a simplified aminopyrine breath test (ABT) was carried out using a "tracer" dose of 3 mg (111 kBq) 14C-aminopyrine. The exhaled 14CO2 measured 1 h after intake amounted to values between 771 and 1337 DPM/mmol CO2/70 kg body weight in healthy controls. The amount of exhaled 14CO2 decreased in the order: fatty liver greater than chronic, active hepatitis greater than active, compensated cirrhosis greater than active, decompensated cirrhosis. Between the values of ABT and various conventional laboratory liver tests (alanine-aminotransferase, alanine-aminopeptidase, aspartate-aminotransferase, gamma-glutamyltransferase, total serum bilirubin) significant correlations were found (r = 0.6019 to 0.7765, n = 55; p less than 0.001). The proposed modification of the breath test is of advantage in that it requires a very low dose of aminopyrine and is easily practicable.

Adult↗