Articles: acetaminophen.
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J. Pharmacol. Exp. Ther. · Nov 2000
Altered hepatobiliary disposition of acetaminophen glucuronide in isolated perfused livers from multidrug resistance-associated protein 2-deficient TR(-) rats.
Previous studies have demonstrated that phenobarbital treatment impairs the biliary excretion of acetaminophen glucuronide (AG), although the transport system(s) responsible for AG excretion into bile has not been identified. Initial studies in rat canalicular liver plasma membrane vesicles indicated that AG uptake was stimulated modestly by ATP, but not by membrane potential, HCO(3)(-), or pH gradients. To examine the role of the ATP-dependent canalicular transporter multidrug resistance-associated protein 2 (Mrp2)/canalicular multispecific organic anion transporter (cMOAT) in the biliary excretion of AG, the hepatobiliary disposition of acetaminophen, AG, and acetaminophen sulfate (AS) was examined in isolated perfused livers from control and TR(-) (Mrp2-deficient) Wistar rats. ⋯ AG and AS perfusate concentrations were significantly higher in livers from TR(-) compared with control rats. Pharmacokinetic modeling of the data revealed that the rate constant for basolateral egress of AG increased significantly from 0.028 to 0.206 min(-1), consistent with up-regulation of a basolateral organic anion transporter in Mrp2-deficient rat livers. In conclusion, these data indicate that AG biliary excretion is mediated by Mrp2, and clearly demonstrate that substrate disposition may be influenced by alterations in complementary transport systems in transport-deficient animals.
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Ann Fr Anesth Reanim · Nov 2000
Clinical Trial[Postoperative pain and surgical treatment of trapeziometacarpal osteoarthritis of the thumb after ambulatory surgery].
The course of pain and the incidence of the side effects from analgesics were evaluated for 15 days in 26 consecutive outpatients who underwent a surgical cure of trapeziometacarpal osteoarthritis of the thumb under regional block. ⋯ The surgical correction of trapeziometacarpal osteoarthritis of the thumb is frequently performed according to an ambulatory setting. The fact that 50% of patients reported severe pain during the early postoperative period emphasize the inadequacy of our postoperative pain management for this surgical procedure.
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British dental journal · Oct 2000
Comparative Study Clinical Trial Controlled Clinical TrialPain control after routine dento-alveolar day surgery: a patient satisfaction survey.
An audit study which examines patient's opinions on the efficiency of two analgesic regimes prescribed to them following dento-alveolar surgery in our Day Unit. ⋯ Telephone contact with patients 24 and 48 hours post-surgery provides a valuable assessment of pain control following discharge from a day surgery unit. Ibuprofen offered satisfactory control of pain for 65% (95) of patients who underwent routine dento-alveolar surgery. Discharge prescriptions must be given with verbal and written instructions to ensure that patients take the correct dose and self-prescription is within safe doses.
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Acetaminophen, also known as paracetamol, is a nonsteroidal anti-inflammatory drug with potent antipyretic and analgesic actions but with very weak anti-inflammatory activity. When administered to humans, it reduces levels of prostaglandin metabolites in urine but does not reduce synthesis of prostaglandins by blood platelets or by the stomach mucosa. Because acetaminophen is a weak inhibitor in vitro of both cyclooxygenase (COX)-1 and COX-2, the possibility exists that it inhibits a so far unidentified form of COX, perhaps COX-3. ⋯ This may be evidence that there are >2 isoforms of the enzyme. Recently, a variant of COX-2 induced with high concentrations of nonsteroidal anti-inflammatory drugs was shown to be highly sensitive to inhibition by acetaminophen. Therefore COX-3 may be a product of the same gene that encodes COX-2, but have different molecular characteristics.
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TREATMENT OF PAIN: Undertreatment of postoperative pain in children is a problem in clinical practice. This is due to a lack of both knowledge about age-specific aspects of physiology and pharmacology, and routine pain assessment. ⋯ NON-OPIOID ANALGESICS: Non-opioid analgesics are recommended for basic pain treatment after minor surgical procedures. Instead of using the whole multitude of drugs available, the doctor should stick to those drugs he is familiar with (acetaminophen, ibuprofen, diclofenac, dipyrone).