High‐dose rectal and oral acetaminophen in postoperative patients – serum and saliva concentrations

Hahn, Tae Won; Mogensen, Torben; Lund, Christian; Schouenborg, Lars; Rasmussen, Martin Krøyer

doi:10.1034/j.1399-6576.2000.440314.x

Cited by 33 publications

(27 citation statements)

References 22 publications

(35 reference statements)

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“…Furthermore, we cannot rule out the possibility that the observed effects are the result of dietary influence on phase 3 excretion of the various APAP metabolites. Saliva APAP concentrations have been shown to correlate well with plasma concentrations of free APAP (Adithan and Thangam, 1982;al-Obaidy et al, 1995;Hahn et al, 2000), making this a convenient, noninvasive method of conducting pharmacokinetic studies in larger-scale studies. Although there is fairly good agreement between these measures, there are several factors that may limit its utility, including differences in salivary flow rate, individual collection, and residual oral drug.…”

Section: Discussionmentioning

confidence: 99%

UGT1A6andUGT2B15Polymorphisms and Acetaminophen Conjugation in Response to a Randomized, Controlled Diet of Select Fruits and Vegetables

Navarro

Chen

et al. 2011

Drug Metab Dispos

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ABSTRACT:Acetaminophen (APAP) glucuronidation is thought to occur mainly by UDP-glucuronosyltransferases (UGT) in the UGT1A family. Interindividual variation in APAP glucuronidation is attributed in part to polymorphisms in UGT1As. However, evidence suggests that UGT2B15 may also be important. We evaluated, in a controlled feeding trial, whether APAP conjugation differed by UGT1A6 and UGT2B15 genotypes and whether supplementation of known dietary inducers of UGT (crucifers, soy, and citrus) modulated APAP glucuronidation compared with a diet devoid of fruits and vegetables (F&V). Healthy adults (n ‫؍‬ 66) received 1000 mg of APAP orally on days 7 and 14 of each 2-week feeding period and collected saliva and urine over 12 h. Urinary recovery of the percentage of the APAP dose as free APAP was higher (P ‫؍‬ 0.02), and the percentage as APAP glucuronide (APAPG) was lower (P ‫؍‬ 0.004) in women. The percentage of APAP was higher among UGT1A6*1/*1 genotypes, relative to *1/*2 and *2/*2 genotypes (P ‫؍‬ 0.045). For UGT2B15, the percentage of APAPG decreased (P < 0.0001) and that of APAP sulfate increased (P ‫؍‬ 0.002) in an allelic dosedependent manner across genotypes from *1/*1 to *2/*2. There was a significant diet ؋ UGT2B15 genotype interaction for the APAPG ratio (APAPG/total metabolites ؋ 100) (P ‫؍‬ 0.03), with *1/*1 genotypes having an approximately 2-fold higher F&V to basal diet difference in response compared with *1/*2 and *2/*2 genotypes. Salivary APAP maximum concentration (C max ) was significantly higher in women (P ‫؍‬ 0.0003), with F&V (P ‫؍‬ 0.003), and among UGT1A6*2/*2 and UGT2B15*1/*2 genotypes (P ‫؍‬ 0.02 and 0.002, respectively). APAP half-life was longer in UGT2B15*2/*2 genotypes with F&V (P ‫؍‬ 0.009). APAP glucuronidation was significantly influenced by the UGT2B15*2 polymorphism, supporting a role in vivo for UGT2B15 in APAP glucuronidation, whereas the contribution of UGT1A6*2 was modest. Selected F&V known to affect UGT activity led to greater glucuronidation and less sulfation.

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Section: Discussionmentioning

confidence: 99%

UGT1A6andUGT2B15Polymorphisms and Acetaminophen Conjugation in Response to a Randomized, Controlled Diet of Select Fruits and Vegetables

Navarro

Chen

et al. 2011

Drug Metab Dispos

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“…Children who receive 45 mg/kg for the antipyretic effects will have a T-max of 4.2 h; however, 20 mg/kg produces subtherapeutic doses [60]. Also, a 20-mg/kg dose in aqueous solution is not effective for postoperative pain.…”

Section: Acetaminophenmentioning

confidence: 98%

“…Pharmacokinetics following administration of medications in suppository form are approximately the same in adults and children [14]. Slow absorption and the lack of effective concentrations within 1-4 h make rectal acetaminophen suboptimal as a postoperative analgesic [60].…”

Section: Acetaminophenmentioning

confidence: 99%

Symptom control in cancer patients: the clinical pharmacology and therapeutic role of suppositories and rectal suspensions

Davis¹,

Walsh²,

LeGrand

et al. 2002

Support Care Cancer

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Rectally administered medications are essential in palliative medicine, particularly in the last days of life. They are underutilized. The pharmacology of rectally administered medications relates not only to the medication but also to the suppository base, additives, drug ionization, p K(a), absorptive surface of the rectum, and rectal health. The pharmacokinetics may differ from those of orally administered medications owing to reduced hepatic first-pass clearance. In this review the pharmacology of rectally administered palliative medications is reviewed and the use of individual drugs is outlined.

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“…[2,54]. Al ler dings soll te bei rek taler Gabe eine In iti al do sis von 40 mg*kg -1 KG nicht un ter schrit ten wer den und die Ap pli kati on soll te bei oder be reits vor Nar ko seein lei tung ge sche hen [7,40]. Eine Do sis über 90 mg*kg -1 KG und Tag über mehr als zwei Tage soll te zur Si cher heit nicht erfol gen, um Le ber to xi zi tät zu ver mei den.…”

Section: Pa Ra Ce Ta Molunclassified

Anästhesiologisches Management bei Korrekturen von Lippen-Kiefer-Gaumenspalten bei Kindern

Machotta

2005

Anaesthesist

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We have developed a modern strategy for the anesthetic management of pediatric cleft lip and cleft palate repair using anesthetic drugs such as sevoflurane, desflurane, acetaminophen, remifentanil, and pirtitramide together with new techniques. It provides best conditions for the surgeon and maximum safety for the pediatric patient. A team of pediatricians, neonatologists, pediatric surgeons, and pediatric anesthetists have tackled the problem of management of children with craniofacial abnormalities such as cleft lip and cleft palate. The best and safest anesthetic techniques are outlined and the most frequent complications are discussed, e.g. management of the difficult airway, the airway in patients with complex craniofacial abnormalities, fiberoptic endotracheal intubation through a laryngeal mask, intraoperative dislocation of the endotracheal tube, postoperative airway obstruction and perioperative bleeding.

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High‐dose rectal and oral acetaminophen in postoperative patients – serum and saliva concentrations

Cited by 33 publications

References 22 publications

UGT1A6andUGT2B15Polymorphisms and Acetaminophen Conjugation in Response to a Randomized, Controlled Diet of Select Fruits and Vegetables

UGT1A6andUGT2B15Polymorphisms and Acetaminophen Conjugation in Response to a Randomized, Controlled Diet of Select Fruits and Vegetables

Symptom control in cancer patients: the clinical pharmacology and therapeutic role of suppositories and rectal suspensions

Anästhesiologisches Management bei Korrekturen von Lippen-Kiefer-Gaumenspalten bei Kindern

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