Twenty-four-Hour Pharmacokinetics of Rectal Acetaminophen in Children

Birmingham, Patrick K.; Tobin, Michael; Henthorn, Thomas K.; Fisher, Dennis M.; Berkelhamer, Maura C.; Smith, Frederick; Fanta, K.B.; Coté, Charles J.

doi:10.1097/00000542-199708000-00010

Cited by 174 publications

(86 citation statements)

References 21 publications

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“…The higher rectal dose is often used in intraoperative conditions but cannot be recommended for use in routine clinical care. 44,45 The use of higher loading doses in clinical practice would add potential risks for dosing confusion leading to hepatotoxicity; therefore, such doses are not recommended.…”

Section: Acetaminophenmentioning

confidence: 99%

Fever and Antipyretic Use in Children

Sullivan¹,

Farrar²

2011

Pediatrics

366

313

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Fever in a child is one of the most common clinical symptoms managed by pediatricians and other health care providers and a frequent cause of parental concern. Many parents administer antipyretics even when there is minimal or no fever, because they are concerned that the child must maintain a “normal” temperature. Fever, however, is not the primary illness but is a physiologic mechanism that has beneficial effects in fighting infection. There is no evidence that fever itself worsens the course of an illness or that it causes long-term neurologic complications. Thus, the primary goal of treating the febrile child should be to improve the child's overall comfort rather than focus on the normalization of body temperature. When counseling the parents or caregivers of a febrile child, the general well-being of the child, the importance of monitoring activity, observing for signs of serious illness, encouraging appropriate fluid intake, and the safe storage of antipyretics should be emphasized. Current evidence suggests that there is no substantial difference in the safety and effectiveness of acetaminophen and ibuprofen in the care of a generally healthy child with fever. There is evidence that combining these 2 products is more effective than the use of a single agent alone; however, there are concerns that combined treatment may be more complicated and contribute to the unsafe use of these drugs. Pediatricians should also promote patient safety by advocating for simplified formulations, dosing instructions, and dosing devices.

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Section: Acetaminophenmentioning

confidence: 99%

Fever and Antipyretic Use in Children

Sullivan¹,

Farrar²

2011

Pediatrics

366

313

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“…The absorption from the rectal route of administration is erratic and unpredictable (8,60), with reported values of bioavailability ranging from 24 to 98% (28,59,146,150,190) the mean absorption half-life is 35 min with 40 min lag time (7), but is largely dependent on the physical composition of the suppositories, which varies between manufacturers (60,113), so that the time to peak plasma concentration ranges from 107 to 288 min after rectal administration (9,24,123). In children, an initial rectal dose of 40 mg/kg has been recommended in order to achieve therapeutic plasma concentrations (24); a rectal dose of 45 mg/kg has been reported to produce in children a mean peak plasma concentration of 13 ìg/mL (146), comparable with that obtained with an oral dose of 10-15 mg/kg (188).…”

Section: Pharmacokineticsmentioning

confidence: 99%

Paracetamol: New Vistas of an Old Drug

et al. 2006

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Paracetamol (acetaminophen) is one of the most popular and widely used drugs for the treatment of pain and fever. It occupies a unique position among analgesic drugs. Unlike NSAIDs it is almost unanimously considered to have no antiinflammatory activity and does not produce gastrointestinal damage or untoward cardiorenal effects. Unlike opiates it is almost ineffective in intense pain and has no depressant effect on respiration. Although paracetamol has been used clinically for more than a century, its mode of action has been a mystery until about one year ago, when two independent groups (Zygmunt and colleagues and Bertolini and colleagues) produced experimental data unequivocally demonstrating that the analgesic effect of paracetamol is due to the indirect activation of cannabinoid CB 1 receptors. In brain and spinal cord, paracetamol, following deacetylation to its primary amine (p-aminophenol), is conjugated with arachidonic acid to form N-arachidonoylphenolamine, a compound already known (AM404) as an endogenous cannabinoid. The involved enzyme is fatty acid amide hydrolase. N-arachidonoylphenolamine is an agonist at TRPV1 receptors and an inhibitor of cellular anandamide uptake, which leads to increased levels of endogenous cannabinoids; moreover, it inhibits cyclooxygenases in the brain, albeit at concentrations that are probably not attainable with analgesic doses of paracetamol. CB 1 receptor antagonist, at a dose level that completely prevents the analgesic activity of a selective CB 1 receptor agonist, completely prevents the analgesic ac- 250CNS Drug Reviews Vol. 12, No. 3-4, pp. 250-275 © 2006 tivity of paracetamol. Thus, paracetamol acts as a pro-drug, the active one being a cannabinoid. These findings finally explain the mechanism of action of paracetamol and the peculiarity of its effects, including the behavioral ones. Curiously, just when the first CB 1 agonists are being introduced for pain treatment, it comes out that an indirect cannabinomimetic had been extensively used (and sometimes overused) for more than a century.

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“…Limited data are available on the pharmacokinetics of acetaminophen (paracetamol) in newborns (86)(87)(88). Acetaminophen does not reduce the response to pain due to heel lance procedures (89), but it may provide some reduction in pain following circumcision (90).…”

Section: Nonsteroidal Anti-inflammatory Drugsmentioning

confidence: 99%

Prevention and Management of Pain and Stress in the Neonate

Blackmon¹,

Kanto²,

Macdonald³

et al. 2000

Pediatrics

294

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This statement is intended for health care professionals caring for neonates (preterm to 1 month of age). The objectives of this statement are to: 1. Increase awareness that neonates experience pain;2. Provide a physiological basis for neonatal pain and stress assessment and management by health care professionals;3. Make recommendations for reduced exposure of the neonate to noxious stimuli and to minimize associated adverse outcomes; and4. Recommend effective and safe interventions that relieve pain and stress.

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Twenty-four-Hour Pharmacokinetics of Rectal Acetaminophen in Children

Abstract: The current recommended rectal acetaminophen dose of 10-15 mg/kg yields peak serum concentrations less than the antipyretic serum concentration of 10-20 microg/ml. Based on the observed kinetics, the authors recommend that the initial dose should be approximately 40 mg/kg.

Cited by 174 publications

References 21 publications

Fever and Antipyretic Use in Children

Fever and Antipyretic Use in Children

Paracetamol: New Vistas of an Old Drug

Prevention and Management of Pain and Stress in the Neonate

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