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Effects of etiocholanolone-induced fever on plasma antipyrine half-lives and metabolic clearance.

The plasma half-life and metabolic clearance rate of antipyrine, a drug metabolized by hepatic microsomal enzymes, were determined in 33 normal volunteers during a basal state and during fever induced with a single intramuscular injection of etiocholanolone. Of the 14 normal volunteers who achieved significant fever (fever index greater than 50), in 11 plasma antipyrine half-life was prolonged after a single oral dose of 10 mg/kg and antipyrine metabolic clearance rate was decreased. There was no significant change of these mean values in 19 normal volunteers who failed to develop significant fever (fever index smaller than 50). Therefore, under the conditions of this study plasma antipyrine half-life was prolonged, probably due to impaired hepatic metabolism, during etiocholanolone-induced fever, although no correlation was observed between the magnitude of fever and the extent to which plasma antipyrine half-life was prolonged. Failure to obtain such a correlation may be attributable to the very small range of temperature elevation, extending from 37.9 degrees C to 39.2 degrees C, in the group of 14 subjects achieving significant etiocholanolone-induced fever (fever index greater than 50). A higher dose of antipyrine (18 mg/kg) suppressed induction of fever by etiocholanolone; antipyrine is the only orally administered drug thus far shown to be effective in repressing etiocholanolone-induced fever.

Adolescent↗

Elimination of antipyrine from saliva as a measure of metabolism in man.

The salivary half-life of antipyrine was used as a convenient procedure for estimating the relative rates of drug metabolism in man. The concentration ratio of antipyrine in plasma and saliva was one over a 24-hr period following the oral or parenteral administration of the drug to man and rat. Phenobarbital, a known stimulator of drug metabolism in animals and man, increased markedly the elimination of antipyrine from saliva of rats, while SKF-525A, a potent inhibitor of drug metabolism, prolonged the elimination of antipyrine from rat saliva. In addition, the known sex difference in the metabolism of drugs in the rat was detected by measuring the elimination rate of antipyrine from saliva of male and female rats. The clinical application of the procedure indicated that a group of epileptic patients treated with anticonvulsants for more than 2 mo had a mean antipyrine salivary half-life of 4 hr, whereas a mean half-life of 13 hr was found in a group of normal volunteers. The results show that the elimination rate of antipyrine from saliva is a useful index of drug metabolism in animals and man.

Adolescent↗

Studies on the disposition of antipyrine, aminopyrine, and phenacetin using plasma, saliva, and urine.

In normal male subjects, the half-lives of antipyrine, aminopyrine, or phenacetin were not significantly different from the half-lives of each drug in saliva. Apparent volumes of distribution (aVd) in plasma and saliva differed by the extent to which each drug has been reported to bind to plasma proteins. Thus, the aVd of antipyrine in plasma and saliva was similar; there were significant differences in aVd for aminopyrine; even greater differences were observed for penacetin. The expression (see article) equals the fraction of the drug bound to plasma proteins. Rates of appearance in the urine of metabolites of antipyrine and aminopyrine were measured. General equations were used to show the relationship between half-life for elimination of the parent drug from the body and rate of excretion of metabolites. There were significant correlations between the half-life for elimination of antipyrine from the body and the half-life for production of 4-OH antipyrine (r equal 0.90), as well as between the plasma half-life of aminopyrine and the half-life of 4-aminoantipyrine (r equal 0.95). No significant correlation was observed in the same individual between the plasma half-lives of antipyrine and phenacetin (r equal 0.05, p greater than 0.05), of aminopyrine and phenacetin (r equal 0.11, p greater than 0.05), or of antipyrine and aminopyrine (r equal 0.50, p greater than 0.05).

Acetylation↗

Failure of hydrocortisone to alter acutely antipyrine disposition.

The disposition of intravenously administered antipyrine in single doses of 40 mg/kg was studied in 3 dogs at 7:00 A.M. and 3 wk later at 7:00 P.M. Our purpose was to determine whether hydrocortisone differentially affected antipyrine disposition according to a circadian pattern. After each intravenous dose of antipyrine, saline was infused for 3 hr followed by intravenous hydrocortisone (2 mg/15 kg loading dose; 2 mg/15 mg/hr infusion for 3 hr). This regimen of hydrocortisone failed at either 7:00 A.M. or 7:00 P.M. to alter acutely antipyrine decay curves. Furthermore, in 4 normal male volunteers, no inflection in the salivary antipyrine decay curve occurred when hydrocortisone was injected 8 hr after antipyrine. In the human volunteers an intravenous injection of 3 mg was followed immediately by an additional 6 hr of continuous hydrocortisone infusion at 3 mg/hr. These experiments show that hydrocortisone alters the pharmacokinetics of previously administered antipyrine in neither dogs nor man.

Adult↗

Antipyrine and acetaminophen kinetics in the rat: comparison of data based on blood samples from the cut tail and a cannulated femoral artery.

Antipyrine and acetaminophen kinetics were determined from concentration data obtained by simultaneous blood sampling from the cut end of the tail and a cannulated femoral artery in the rat. Significant differences in concentrations and kinetics for both drugs were found by comparison of the two sampling sites. The hypothesis that the differences were due to a low tail blood flow was tested. The tail blood flow was measured with a microsphere technique, and tail antipyrine concentrations were calculated from the relationship between arterial antipyrine concentration, tail flow, and time for comparison with the observed antipyrine concentrations. Mean blood flow of the rat tail was 0.02 ml/min/ml tail tissue at 22 degrees, which was 8.8 and 0.9% of the liver and kidney flow, respectively. Tail flow increased more than twofold by elevation of the tail temperature to 37 degrees. The calculated tail antipyrine concentration versus time curve showed a very close correspondence to the observed antipyrine tail concentration versus time curves. The results show that tail flow is a major determinant of antipyrine tail concentration in the rat. Kinetic data based on blood samples from the cut end of the tail, therefore, should be interpreted with caution.

Acetaminophen↗

Effect of the immunomodulator tilorone on antipyrine disposition in the rat.

A wide variety of immunomodulators, including the synthetic interferon inducer tilorone (2,7-bis[2-(diethylamino)ethoxy]fluoren-9-one), have been shown to inhibit cytochrome P-450-dependent drug metabolism in vitro. In an effort to determine if tilorone also inhibits drug metabolism in vivo, we examined the effect of this agent on the disposition of antipyrine in the rat. Administration of tilorone hydrochloride (50 mg X kg-1 X d-1) 4 d resulted in a 42% reduction in antipyrine clearance and a 71% increase in plasma half-life. Administration of a single dose of tilorone hydrochloride (50 mg/kg) 48 h prior to antipyrine was found to cause a similar alteration in antipyrine clearance and half-life. Both treatment regimens were also found to produce a substantial weight loss in the pretreated animals. Preliminary studies indicated that tilorone treatment reduced food and water consumption in the rat. Therefore, the effect of a 75% decrease in food and water consumption on antipyrine disposition was also examined. This magnitude of restriction had no detectable effect on antipyrine elimination. Thus, tilorone results in a substantial reduction of the in vivo metabolic clearance of antipyrine and appears to be a useful compound for studying the dynamic interaction between the drug metabolizing and immune systems in vivo.

Animals↗

Preparative isolation and purification of urinary conjugates in antipyrine metabolism in man and rat.

A series of six major urinary conjugates in the metabolism of antipyrine in man and rat has been investigated. A preparative isolation procedure has been developed using chromatography of methanolic extracts from urine on silica gel. In a two-step chromatographic procedure, methanolic extracts are first separated in 1) a "free fraction", containing unconjugated phase-I-metabolites and unchanged antipyrine, 2) a sulfate fraction and 3) a glucuronide fraction. Sulfate and glucuronide fraction, respectively, are each subjected to a second run for separation into their three components. Thus, the following conjugates have been prepared: 4-hydroxy-antipyrine sulfate, norantipyrine sulfate, 4,4'-dihydroxy-antipyrine sulfate, and 4-hydroxy-antipyrine glucuronide, norantipyrine glucuronide, 3-hydroxymethyl-antipyrine glucuronide. Methodology is also applicable to bile fluid and liver perfusate. Stability of isolated conjugates against acid hydrolysis has been studied to show that strongly marked differences exist in this series of conjugates. Field desorption mass spectrometry has been used for the direct identification of intact conjugates in an underivatized form. Using 13C-NMR, the structure of norantipyrine glucuronide has been established as an 5-enol glucuronide. By analogy, a structure of 5-enol sulfate is proposed for norantipyrine sulfate. From a semiquantitative examination by TLC of urine extracts from man and rat, it becomes apparent, that in the rat, at the dose level studied, sulfate formation is the predominant conjugation pathway. In man, glucuronides are the most prominent type of conjugates. Formation of sulfates is minimal up to a dose of 15 mg/kg antipyrine.

Adult↗

Cimetidine-phenytoin interaction: effect on serum phenytoin concentration and antipyrine test.

In a prospective study in nine patients the effects of phenytoin and of cimetidine (1000 mg/day) + phenytoin on the antipyrine test and serum phenytoin concentrations were studied. Serum phenytoin increased from the steady state level of 5.7 +1.3 mg/l to 9.1 +1.4 mg/l after three weeks on cimetidine (p less than 0.01), and fell to 5.8 +1.2 mg/l within two weeks after withdrawal of cimetidine. The protein binding of phenytoin was not changed by cimetidine. After use of phenytoin for 2-4 months, antipyrine clearance increased from 0.67 +0.06 ml/min/kg to 1.61 +0.22 ml/min/kg, and antipyrine half-live fell from 10.9 +1.3 h to 4.5 +0.6 h as compared to the values before phenytoin treatment (p less than 0.01). After three weeks combined use of cimetidine and phenytoin, antipyrine clearance was decreased to 1.01 +0.07 ml/min/kg and antipyrine half-life was prolonged to 6.1 +0.5 h, (p less than 0.01) compared to the values on phenytoin alone. The distribution volume of antipyrine was not affected by phenytoin nor by cimetidine + phenytoin. The half-life of cimetidine was 2.8 +0.3 h in the patients in the longterm phenytoin treatment. There was a significant positive correlation (p less than 0.001) between the increase in serum phenytoin concentration and the prolongation of antipyrine half-life caused by cimetidine. Thus, cimetidine increases serum phenytoin concentration, very probably by inhibiting its metabolism. Care should be taken in the concomitant use of cimetidine ad phenytoin, and the dose of phenytoin should be modified according to the clinical symptoms and serum phenytoin concentrations.

Adult↗

The effect of induction with phenobarbital on the kinetics and bioavailability of antipyrine in the dog.

In dogs, the chronic administration of 400 mg/d of phenobarbital produced peak plasma concentrations of 78 micrograms/ml which so markedly induced the metabolism of antipyrine that the conventional schemes by which antipyrine kinetics assess induction were rendered invalid. The bioavailability of antipyrine was only 20% due to first-pass metabolism. Induction raised the observed antipyrine clearance to 31 ml/min/kg, a value approaching hepatic blood flow. If one assumes antipyrine was an ideal test compound, one would calculate that metabolism was induced by a factor of 3.8. Acknowledging that antipyrine is nonideal, one can calculate a correct induction factor of 13.6. Oral, rather than intravenous, antipyrine is the metabolism test of choice under these conditions.

Administration, Oral↗

Membrane permeability and antipyrine absorption in a rat model of ischemic colitis.

The aim of this study was to determine whether the duration of ischemia affects antipyrine absorption in the large intestine. This was carried out in a rat model of ischemic colitis in which ischemia and associated inflammation was induced by marginal vessel ligation. Blood flow was disrupted by positioning an o-ring around the distal rectum and ligating the marginal vessel at two locations in the hind-gut ligament artery region. Ligation was performed for 1, 2, 3, and 5h. We assessed large intestine damage by measuring key indicators of inflammation, myeloperoxidase (MPO) activity and thiobarbituric acid reactant substrates (TBARS) in the mucosa and by histological staining with hematoxylin-eosin stain. Antipyrine membrane permeability was assessed in Ussing-type diffusion chambers, and related pharmacokinetics were calculated from antipyrine plasma concentration measurements following colon administration of the drug. Vessel ligation caused some sloughing of epithelial cells and elevated the MPO and TBARS levels. Prolonged ligation failed to affect the apparent permeability coefficient (P(app)) of antipyrine. Prolonged ligation, however, gradually increased plasma antipyrine concentrations to near control levels. This increase was paralleled by increases in the absorption rate constant AUC and antipyrine bioavailability. Taken together, these results suggest that the absorption kinetics of antipyrine may depend on blood flow changes in the large intestine that occur with inflammation.

Animals↗

Effect of antipyrine and phenobarbital on renal gamma-glutamyltransferase excretion in human urine.

Serum gamma-glutamyltransferase is used as a marker of hepatic enzyme induction. The kidney contains high activities of gamma-glutamyltransferase in the brush border membrane of the proximal tubule, from which it is released into urine. This study investigated the effect of phenobarbital and antipyrine, two inducers of hepatic monoxygenases and gamma-glutamyltransferase, on the urinary excretion of renal gamma-glutamyltransferase. Three groups (n = 6) of healthy male volunteers received 100 mg phenobarbital for 7 and 14 days and 1200 mg antipyrine for 7 days, respectively. Antipyrine and phenobarbital increased antipyrine elimination, serum gamma-glutamyltransferase, and the urinary excretion of renal gamma-glutamyltransferase, whereas urinary beta-N-acetylglucosaminidase, beta-glucuronidase, and total protein and glucose excretion were unchanged. No correlation was found between serum and urinary gamma-glutamyltransferase or both enzymes and antipyrine elimination. Increases in antipyrine elimination were positively correlated to increases in serum, but not urinary gamma-glutamyltransferase. The findings suggest that antipyrine and phenobarbital increase urinary gamma-glutamyltransferase excretion. However, the increase in urinary gamma-glutamyltransferase does not reflect the magnitude of hepatic enzyme induction.

Adolescent↗

The effect of age and sex on metabolism and urinary excretion of antipyrine.

BACKGROUND: Drug-metabolizing capacity is generally reduced in the elderly. The purpose of this investigation was to study antipyrine clearance and metabolite excretion in old subjects of both sexes. METHODS: Saliva clearance of antipyrine and the production clearances of antipyrine metabolites were studied in young and elderly volunteers of both sexes. Seventy-six elderly subjects (mean age 81 years) were compared with a group of 24 young subjects (mean age 29 years). RESULTS: After oral administration, salivary antipyrine clearance declined with age in both males and females, whether or not this variable was corrected for weight, and antipyrine half-life was significantly prolonged in elderly groups of either sex. The percentage urinary excretion of the antipyrine metabolites (hydroxymethylantipyrine, HMA; norantipyrine, NORA; and 4-hydroxyantipyrine, OHA) was reduced at 48 h in the elderly compared to young subjects by 23%, 31%, and 10%, respectively, in males, and by 41%, 41%, and 24%, respectively, in females. The formation clearance of HMA was reduced by 47% in males and by 52% in females. NORA clearance declined by 42 and 56%, respectively, in males and females. A decrease of 30% in males and 44% in females was observed in OHA clearance. CONCLUSIONS: The findings suggest that aging leads to altered disposition of antipyrine in both males and females and that the main metabolic pathways of the compound are not different in the elderly.

Administration, Oral↗

The plasma half-life of antipyrine in chromic uraemic and normal subjects.

1. Antipyrine was given intravenously in a dose of 18 mg/kg body weight to twelve patients with chronic renal failure (plasma creatinine greater than 4.9 mg/100 ml) who were not taking drugs and twenty normal subjects. 2. Plasma antipyrine levels were measured by a specific method, the plasma half-life of the drug was determined and used as an index of drug oxidation. 3. The mean (+/- s.d) plasma antipyrine half-life in patients with chronic renal failure (7.3 +/- 2.0 h) was significantly shorter than in normal subjects (13.2 +/- 4.3 h: P less than 0.002). There was no difference in the apparent volume of distribution of antipyrine between the two groups (P greater than 0.6). 4. Pretreatment of five patients with chronic renal failure and seven normal subjects with antipyrine or phenobarbitone for weeks significantly shortened the mean plasma antipyrine half-life from 7.4 +/- 2.5 h to 5.0 +/- 1.5 h in uraemics (P less than 0.005) and from 13.2 +/- 4.5 h to 6.9 +/- 1.5 h in normal subjects (P less than 0.0025).5. These results suggest that oxidation of antipyrine by hepatic microsomal enzymes is increased in patients with chronic renal failure, but a state of maximal induction of these enzymes was not observed. The clinical implication of this finding with regard to the association between liver microsomal enzyme induction and vitamin D resistant osteomalacia is discussed.

Administration, Oral↗

Effect of chloroquine and primaquine on antipyrine metabolism.

The effects of two antimalarial drugs, chloroquine and primaquine on antipyrine kinetics and metabolism have been studied in volunteers. Chloroquine (250 mg) given 2 h before antipyrine (600 mg orally) had no effect on salivary kinetics of antipyrine or on the urinary recovery of metabolites. Primaquine (45 mg) given 2 h before antipyrine (300 mg orally), increased antipyrine half-life (calculated from 0-24 h) from 12.7 +/- 3.2 (mean +/- s.d.) to 25.3 +/- 3.9 h and decreased clearance from 3.01 +/- 0.67 to 1.32 +/- 0.32 1 h-1. There was no change in the apparent volume of distribution. Antipyrine half life changed with time in the presence of primaquine and when calculated between 24 and 48 h had returned to control. After primaquine, the metabolic clearance (calculated from 0-24 h) of antipyrine to its three main metabolites, 3-hydroxymethylantipyrine, 4-hydroxyantipyrine and norantipyrine was significantly reduced. There was no selective effect on a particular metabolic pathway. There was no change in 6 beta-hydroxycortisol excretion (expressed as a ratio of total 17-hydroxy-corticosteroids) in the period 0-48 h following primaquine administration. The inhibition of hepatic metabolism by primaquine but not the structurally related chloroquine may be an example of a structure activity phenomenon and could be of clinical significance.

Adult↗

Dietary influences on the kinetics of antipyrine and aminopyrine in human subjects.

The possible dietary influences on in vivo antipyrine and aminopyrine kinetics with reference to energy (1500, 1800, 3000 kcal) and protein (5, 10, 15, 20% protein energy-PE) intake were studied in a carefully controlled metabolic experiment in young healthy adult male volunteers aged between 25-34 years. Antipyrine and aminopyrine were used to evaluate drug metabolism. On 1500 kcal intake with 10% PE, the metabolism of both aminopyrine and antipyrine were significantly reduced whereas on 1800 kcal with 10% PE intake, only aminopyrine metabolism decreased significantly as compared to 3000 kcal with 10% PE. Antipyrine clearance on 1800 kcal with 10% PE however had not decreased to the same extent as on 1500 kcal with 10% PE. The results indicate that on low calorie intake with 10% PE, the drug metabolism is decreased. When the protein intake on 1500 kcal was doubled (20% PE) there was a significant stimulation of both aminopyrine and antipyrine metabolism. Aminopyrine and antipyrine clearances on 3000 kcal with 5% PE were significantly reduced as compared to 3000 kcal with 10% and 15% PE indicating that unlike proteins, carbohydrate and/or fat calories per se do not significantly stimulate drug metabolism. When the protein energy in the diet was increased from 5% to 10% or 15% at 3000 kcal, there was a stimulation of both antipyrine and aminopyrine metabolism. Significant differences between 10% and 15% of protein energy were not observed when the energy was adequate (3000 kcal). Therefore it is necessary to consider both proteins and energy as important variables affecting drug clearances from plasma in malnourished conditions.

Adult↗

Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.

The influence of an 8-day therapy with rifampicin (600 mg daily) was studied on antipyrine plasma clearance and metabolite formation in seven patients with tuberculosis (age 18-79 years), who were also treated with isoniazid and pyrazinamide. After rifampicin treatment the elimination half-life of antipyrine had decreased in all patients from 12.9 +/- 5.0 to 8.8 +/- 2.0 h (P less than 0.05). Antipyrine clearance had increased from 2.2 +/- 0.9 to 2.9 +/- 0.7 l/h (P less than 0.05), while no change in apparent volume of distribution was observed. The increase in antipyrine clearance was primarily due to a selective increase in the rate of formation of norantipyrine by 80% from 6.9 +/- 3.4 to 12.4 +/- 3.4 ml/min. Rifampicin seems to induce preferentially the cytochrome P-450 (iso-) enzyme(s) involved in the demethylation of antipyrine to norantipyrine. Other pathways of antipyrine metabolism were hardly affected. This provides further evidence for the involvement of different iso-enzymes of the cytochrome P-450 system in antipyrine metabolism in man.

Adolescent↗

Antipyrine clearance and metabolite formation in patients with alcoholic cirrhosis.

The effect of liver cirrhosis on plasma clearance and metabolite profile of i.v. administered antipyrine was studied in 23 patients with alcoholic liver cirrhosis (age 37-70 years) and 17 healthy subjects (age 28-55 years). Liver volume was also measured and was found to be larger in patients than in controls, mean values being 1.86 and 1.36 l respectively. The elimination half-life of antipyrine in patients with alcoholic liver cirrhosis was significantly longer than in the healthy subjects (P less than 0.001). Mean values were 39.9 and 10.1 h respectively. Alcoholic liver cirrhosis had no effect on the apparent volume of distribution of antipyrine, but antipyrine plasma clearance was substantially reduced in the patients. Mean clearance values (ranges) were 13.5 (9.3-22.8) ml/min in the patients and 49.3 (31.1-103) ml/min in healthy subjects. Normalization of antipyrine plasma clearance for liver volume resulted in an only slightly increased distinction between patients and healthy subjects, mean values (ranges) being 7.8 (3.3-13.0) ml min(-1) 1(-1) and 36.1 (21.9-35.9) ml min(-1) 1(-1) respectively. The cumulative renal excretion of 4-hydroxyantipyrine (OHA) and norantipyrine (NORA) was significantly lower in patients with alcoholic liver cirrhosis than in healthy subjects, as was the total recovery of antipyrine and major metabolites from urine. Mean values were 15.0, 8.4 and 41.2% of dose in the patients respectively and 24.3, 25.8 and 68.9% of dose in the control subjects. Excreted amounts of total and unconjugated 3-hydroxymethylantipyrine (HMA) and of unchanged antipyrine were the same in the two groups.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

Antipyrine disposition in the dehydrated camel.

In the present study the effects of water deprivation in the camel (Camelus dromedarius) on the pharmacokinetic profile of antipyrine were assessed. A cross-over design was used. The pharmacokinetics of antipyrine in adult and young camels were compared. Antipyrine was administered intravenously to young and adult female camels when water was available ad libitum and to the adult camels after 14 days of dehydration. The elimination half-life of antipyrine in watered adult camels was 136.5 +/- 16.7 min. The half-life of elimination and the mean residence time of antipyrine were significantly prolonged following dehydration. The observed effects of water deprivation were not a function of age, as the pharmacokinetic profile of antipyrine in young camels was similar to that of the adults, but more likely due to the changes in oxidative metabolic capacity of the liver as a result of a reduced general metabolism. The results of the present study also show that the intrinsic clearance of antipyrine is proportional to the camel's body weight, as previously shown for other mammalian species.

Aging↗