Species comparison of oral bioavailability, first-pass metabolism and pharmacokinetics of acetaminophen

Neirinckx, Eva; Vervaet, Chris; Boever, Sandra De; Remon, Jean Paul; Gommeren, Kris; Daminet, Sylvie; Backer, Patrick De; Croubels, Siska

doi:10.1016/j.rvsc.2010.02.002

Cited by 60 publications

(92 citation statements)

References 44 publications

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“…These properties could contribute to enhance TZR solubility and its absorption processes in broilers compared to other species. Furthermore, the greater tendency towards high first-pass loss in birds were reported since gastric and intestinal emptying time hardly influence the absorption of liquid dosage forms of readily soluble drugs (Dorrestein, 1992;Neirinckx et al, 2010). In the present study, TZR was shown relatively higher C max at earlier T max in broilers as compared to other mammalian species.…”

Section: Resultssupporting

confidence: 45%

Pharmacokinetics and Metabolism of Toltrazuil and Its Major Metabolites after Oral Administration in Broilers

et al. 2013

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Toltrazuril is a symmetrical tiazinetrione compound. It is active against all intracellular developmental stages including those of schizogony and gametogony. In this study the disposition kinetics of toltrazuril (TZR) and its major metabolites (TZR-SO and TZR-SO 2 ) in broiler chickens after single oral administrations of 10 or 20 mg/kg were investigated. Mean plasma concentrations of TZR peaked at 16.4 and 25.2 μg/mL at 5.0 and 4.7 h after dosing, respectively. TZR was converted to the short-lived intermediary metabolite toltrazuril sulfoxide (TZR-SO), and then further metabolized to the reactive toltrazuril sulfone (TZR-SO 2 ) being actually more slow eliminated with 80.3 and 82. 9 h than TZR (10. 6 and 10. 7 h) or TZR-SO (14. 8 and 15. 3 h) in low and high dosing groups, respectively. Prolonged elimination half-life of TZR-SO 2 could be interpreted as the persistent clinical efficacy of TZR in the treatment of protozoal parasites infection.Key words: broiler, pharmacokinetics, toltrazuril, toltrazuril sulfone, toltrazuril sulfoxide J. Poult. Sci., 50: 257-261, 2013 Introduction Coccidiosis is a particularly dangerous disease in the poultry industry where chickens are maintained on the floor (Greif, 2000). Anticoccidial drugs of many different chemical types have been the dominant means to prevent and control the coccidiosis (Polozowski, 1993;Greif et al., 2001). However, the massive and uncontrolled use of anticoccidial drugs has resulted in the emergence of drug-resistant parasites (Suo X et al., 2006)., 5-triazinane-2, 4, 6-trione, is a symmetrical triazinetrione compound. It has coccidiocidal action against all intracellular developmental stages including those of schizogony and gametogony (Mehlhorn et al., 1984;Haberkorn and Stoltefuss, 1987). It has been reported to be effective against all coccidial species in most animal species, such as chickens (Mehlhorn et al., 1984), ducks (Chauve et al., 1994), dogs (Daugschies et al., 2000), mice (Haberkorn et al., 1983), pigeons (Van Reeth and Vercruysse, 1993), piglets (Mundt et al., 2007) and rabbits (Peeters and Geeroms, 1986).TZR undergoes extensive metabolism to toltrazuril sulfoxide (TZR-SO) and then to TZR-SO 2 , which appears to have anticoccidial activity (Benoit et al., 1993;Lang et al., 1996;Bach et al., 2003;Mundt et al., 2007) (Fig. 1). Generally, triazines produced the same types of metabolites in most species, but the ratios of the metabolites showed the species differences (Furr and Kennedy, 2000;MacKay, 2006;Kim et al., 2010;Lim et al., 2010). Also, TZR is almost exclusively metabolized to TZR-SO 2 , also known as ponazuril (PZR), which has been recognized as the marker metabolite in a number of tissues. Although TZR is commonly used for the prevention and treatment of coccidosis in broilers, the pharmacokinetic and metabolic profiles of TZR in broilers have received minimal investigation. There must be assessed not only in terms of good clinical efficacy but also considering the pharmacokinetics and metabolism of TZR in broilers for the rat...

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Section: Resultssupporting

confidence: 45%

Pharmacokinetics and Metabolism of Toltrazuil and Its Major Metabolites after Oral Administration in Broilers

et al. 2013

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“…as determined in the present study in chicks are not found collectively in the literature concerning avian species (Davis and Westfall 1972;Lambert et al 1986;De Backer 2002, 2003;Neirinckx et al 2010). The plasma half-life of acetaminophen ranges between 1-4 h across various species which could increase in cases of overdose (St. Omer and Mohammad 1984;Bannwarth and Pehourcq 2003;Neirinckx et al 2010). Sodium salicylate administration in birds resulted in a plasma half-life of salicylic acid in the chicken (3.13 h) which was shorter than those in the pigeon and duck (Baert and De Backer, 2003).…”

Section: Resultscontrasting

confidence: 63%

“…The low plasma protein binding of acetaminophen together with its small molecular size favours distribution of the drug into the tissues (Bannwarth and Pehourcq 2003). However, animal species differ in their metabolism and plasma clearance of aspirin and acetaminophen (Davis and Westfall 1972;Livingston 2010;Neirinckx et al 2010). The differences between acetaminophen and aspirin concentrations in the plasma of the chicks could be attributed to the differences in the absorption rate, distribution, plasma protein binding and metabolism pattern between the two drugs (Davis and Westfall 1972;Livingston 2010;Neirinckx et al 2010;Hawkins and Paul-Murphy 2011).…”

Section: Resultsmentioning

confidence: 99%

“…Neirinckx et al (2010) reported the pharmacokinetics parameters of acetaminophen in five-week old chickens after intravenous and oral administration (10 mg/kg). Comparing the findings of the latter studies in the chicken (Davis and Westfall 1972;Lambert et al 1986;De Backer 2002, 2003;Neirinckx et al 2010) with those of the present one in chicks, the variations in absolute pharmacokinetic values could be attributed to the differences in the dosage, route of administration, dosage form and formulation as well as the age of the birds De Backer 2002, 2003;Machin 2005;Hawkins and Paul-Murphy 2011).…”

Section: Resultsmentioning

confidence: 99%

“…De Backer (2002, 2003) have reported the pharmacokinetic parameters of sodium salicylate after intravenous administration in adult chickens. A recent study reported several pharmacokinetic parameters of acetaminophen in the chicken after intravenous and oral administration of 10 mg/kg (Neirinckx et al 2010). The purpose of the present study was to examine the pharmacokinetics of aspirin and acetaminophen in 12-day old chicks after a single intraperitoneal administration at a dose of 100 mg/kg body weight.…”

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confidence: 96%

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Comparative single intraperitoneal dose pharmacokinetics of aspirin and acetaminophen in chicks

Mohammad¹,

Mansoor²,

Al-Zubaidy³

2012

Vet. Med. - Czech

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Limited information is available on the pharmacokinetics and bioavailability of aspirin and acetaminophen in young chicks. The purpose of the present study was to examine the pharmacokinetics of acetyl salicylic acid (aspirin) and acetaminophen in 12-day old chicks after a single intraperitoneal administration of each drug alone at the dose of 100 mg/kg body weight. Blood samples were collected from chicks (six/each time period) at 10, 20, 30, 60 and 120 min after each drug administration. The concentrations of aspirin and acetaminophen in the plasma were determined by spectrophotometric methods. The pharmacokinetic parameters of the drugs were calculated by a non-compartmental analysis. The elimination half-lives of aspirin and acetaminophen were 1.68 and 1.36 h with steady state volume of distributions 0.079 and 1.11 l/kg and total body clearances of 0.029 and 0.53 l/h/kg, respectively. The mean residence times of the drugs were 2.74 and 2.09 h and their area under the plasma concentration-time curves (0-∞) were 3486 and 188 μg·h/ml, respectively. In conclusion, the data show the pharmacokinetic profiles of single intraperitoneal doses of aspirin and acetaminophen in chicks and suggest that acetaminophen is well distributed in the body of the chicks and eliminated faster from the body compared to aspirin. These parameters should be taken into consideration in further therapeutic and toxicological studies of drugs in chickens.

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Non‐Steroidal Anti‐Inflammatory Drugs

Willette

2024

Pharmacology in Veterinary Anesthesia and Analgesia

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Species comparison of oral bioavailability, first-pass metabolism and pharmacokinetics of acetaminophen

Cited by 60 publications

References 44 publications

Pharmacokinetics and Metabolism of Toltrazuil and Its Major Metabolites after Oral Administration in Broilers

Pharmacokinetics and Metabolism of Toltrazuil and Its Major Metabolites after Oral Administration in Broilers

Comparative single intraperitoneal dose pharmacokinetics of aspirin and acetaminophen in chicks

Non‐Steroidal Anti‐Inflammatory Drugs

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