Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Ketorolac is a new chiral nonsteroidal anti-inflammatory drug (NSAID) which is marketed for analgesia as the racemate. The drug is administered as the water soluble tromethamine salt and is available in tablets or as an intramuscular injection. The absorption of ketorolac is rapid, Cmax being attained between 20 to 60 min. Its oral bioavailability is estimated to range from 80 to 100%. The drug is extensively bound (> 99%) to plasma proteins and has a volume of distribution (0.1 to 0.3 L/kg) comparable with those of other NSAIDs. Only small concentrations of ketorolac are detectable in umbilical vein blood after administration to women in labour. The elimination half-life is between 4 and 6h and is moderate in comparison with other NSAIDs. The area under the plasma concentration-time curve of ketorolac is proportional to the dose after intramuscular administration of therapeutic doses to young healthy volunteers. Ketorolac is extensively metabolised through glucuronidation and oxidation; little if any drug is eliminated unchanged. Most of the dose of ketorolac is recovered in the urine as conjugated drug. Although ketorolac is excreted into the breast milk, the amount of drug transferred comprises only a small fraction of the maternal exposure. Little stereoselectivity was present in the pharmacokinetics of ketorolac in a healthy volunteer receiving single intravenous or oral doses. The elderly exhibit reduced clearance of the drug. Renal insufficiency appears to cause an accumulation of ketorolac in plasma, although hepatic disease may not affect the pharmacokinetics.
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PMID:Clinical pharmacokinetics of ketorolac tromethamine. 2751 22

Providing adequate pain control with minimal side effects in inpatient and ambulatory settings is a continuous challenge to the PACU nurse. Ketorolac tromethamine (Toradol, Syntex, Palo Alto, CA) is a new parenteral nonsteroidal anti-inflammatory drug (NSAID) approved for use in the United States. Ketorolac is useful in the management of short term, moderate to severe postoperative pain. It is used by itself or as an adjunct to traditional opioid analgesics. Ketorolac, like other NSAIDs, has analgesic, anti-inflammatory, and antipyretic properties. Unlike morphine or meperidine, ketorolac does not bind to opioid receptors and is not a centrally acting agent. Administered intramuscularly, peak plasma levels are reached in 45 to 50 minutes. It is administered as a 30- or 60-mg intramuscular (IM) loading dose followed by 15- or 30-mg doses IM every 6 hours, with a maximum first-day dose of 150 mg and 120 mg on subsequent days up to a recommended maximum of 5 days. The lower dose range is recommended for elderly patients, patients weighing less than 50 kg, and patients with impaired kidney function. Initial studies show that use of ketorolac decreases the overall amount of opioid analgesia needed for postoperative pain control. To date, reported occurrence of side effects is low. A case study presents a healthy ambulatory surgical patient admitted for inguinal hernia repair using epidural anesthesia. Use of ketorolac has shown initial favorable results. More research is needed to further define its role and side effects in postoperative pain management.
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PMID:Ketorolac: a new parenteral nonsteroidal anti-inflammatory drug for postoperative pain management. 149 90

This case report describes a general anesthetic where ketorolac tromethamine was used instead of a narcotic. The patient was a 37-year-old male, ASA II category, who underwent general anesthesia for a cholecystectomy. The drug is discussed in terms of preoperative, intraoperative, and immediate postoperative effects. During the preoperative phase, no effect was demonstrated. Intraoperatively, the drug performed poorly to attenuate responses to intense stimulation as noted by an increase in pulse and blood pressure of greater than 20% during intubation, incision, and abdominal wall retraction. During the immediate postoperative phase, the drug performed well to provide analgesia related to incisional pain. Ketorolac has not been previously discussed in terms of intraoperative uses. The mechanism of action by which it provides analgesia is through the inhibition of prostaglandin synthesis. It is similar in structure to the other nonsteroidal anti-inflammatory drugs and may offer certain advantages over traditional agents used to provide analgesia, including the absence of respiratory depression, addictive potential, euphoria, a decrease in gastric motility, and cardiovascular effects. These properties may help in the management of certain types of patients who are at risk for respiratory depression or in those who have a contraindication to narcotics.
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PMID:Ketorolac tromethamine: a nonsteroidal anti-inflammatory analgesic used as an adjunct for general anesthesia. 163 59

We have compared the renal effects of ketorolac trometamol 10 mg administered 4-hourly by intermittent i.m. injection or by continuous i.m. infusion with placebo in a double-blind study in 67 patients who had undergone upper abdominal surgery. Ketorolac was supplemented during the 48-h postoperative study period with bolus doses of morphine delivered by a patient controlled analgesia system. The only significant effect of ketorolac on renal function compared with patients who received placebo was reduced excretion of potassium. The overall changes caused by surgery alone were of much greater magnitude. Bleeding time was increased with ketorolac, but there were no adverse events related to this.
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PMID:Effects of ketorolac trometamol on renal function. 164 36

Ketorolac tromethamine is the first injectable nonsteroidal anti-inflammatory drug approved for the management of acute pain. In analgesic potency and ability to relieve postoperative pain, it is comparable to morphine. The advantages of ketorolac over opiates are the absence of respiratory depression and lack of drug abuse potential. Ketorolac has a longer duration of action than morphine, but it has less effect on the central nervous system. Ketorolac should not be used for obstetric analgesia.
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PMID:Ketorolac: an injectable NSAID. 198 89

One-hundred twenty-eight outpatients with postoperative pain after the surgical removal of impacted third molars were randomly assigned, on a double-blind basis, to receive oral doses of ketorolac tromethamine 10 mg, aspirin 650 mg, a combination of acetaminophen 600 mg plus codeine 60 mg, or placebo. Using a self-rating record, subjects rated their pain and its relief hourly for 6 hours after medicating. All active medications were significantly superior to placebo. The acetaminophen-codeine combination was significantly superior to aspirin for peak analgesia. Ketorolac was significantly superior to aspirin for every measure of total and peak analgesia, and significantly superior to acetaminophen-codeine for measures of total effect. The analgesic effect of ketorolac was significant by hour 1 and persisted for 6 hours. Repeat-dose data also suggested that ketorolac 10 mg was superior to aspirin 650 mg and acetaminophen-codeine on the day of surgery. Differences among the active medications were trivial for the postoperative days 1-6 analyses. The frequency of adverse effects was over 4 times greater for acetaminophen-codeine than for ketorolac or aspirin.
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PMID:Evaluation of ketorolac, aspirin, and an acetaminophen-codeine combination in postoperative oral surgery pain. 208 17

Ketorolac, a prostaglandin synthetase-inhibiting analgesic, was compared with morphine for relief of pain after laparotomy for gynaecological surgery. Eighty patients were studied; they were given either ketorolac 30 mg intramuscularly followed by 10 mg 4-hourly as required, or morphine 10 mg intramuscularly 4-hourly as required, administered in a double-blind, randomised fashion. Pain scores (verbal and visual analogue) were recorded at baseline and assessed at 30 and 60 minutes and then hourly for 6 hours. Pain relief was measured at the same times. Pain and pain-relief scores were further assessed on the evening of day 1 and at 24 hours. Pain scores were similar in the two groups but pain-relief scores were better in the morphine group. A considerable number of patients suffered postoperative nausea and vomiting but there was no difference between the groups. One patient in the ketorolac group had unexplained hypotension. It is concluded that ketorolac can provide effective postoperative analgesia.
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PMID:Comparison of intramuscular ketorolac and morphine in pain control after laparotomy. 220 Dec 25

I.m. ketorolac trometamol 30 mg was compared with morphine sulphate 10 mg after cholecystectomy in a double-blind, multiple dose, randomized study of 100 patients. Assessments of pain were made immediately after operation (day 1), and the next morning (day 2). Pain intensity (verbal response score and visual analogue scale) was recorded before injection and then over a 6-h period. Pain relief was assessed also. The effect of ketorolac on operative blood loss and platelet function was examined. Time to commencing oral intake and the duration of administration of i.v. fluids were recorded. Adverse events were noted. Ketorolac produced significantly less analgesia than morphine on day 1, but on day 2 the two drugs produced a similar effect. Blood loss was not increased by ketorolac, although platelet function was impaired. Repeated i.m. administration of ketorolac did not produce any serious adverse effects.
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PMID:Comparison of i.m. ketorolac trometamol and morphine sulphate for pain relief after cholecystectomy. 224 12

Clinical studies of the injectable nonsteroidal anti-inflammatory agent (NSAIA) ketorolac tromethamine are reviewed, and the chemistry, pharmacology, pharmacokinetics, drug interactions, and adverse effects of ketorolac are described. Ketorolac exhibits anti-inflammatory, analgesic, and antipyretic activity. Although the exact mechanisms of action have not been determined, its effects appear to be associated principally with the inhibition of prostaglandin synthesis. After oral, i.m., or i.v. administration, ketorolac and its metabolites are excreted mainly in urine. Ketorolac tromethamine has been used for the symptomatic relief of moderate to severe postoperative pain, including that associated with abdominal, gynecologic, oral, orthopedic, or urologic surgery. Ketorolac has also been used for the relief of acute renal colic, pain associated with trauma, and visceral pain associated with cancer. When administered i.m., ketorolac produced analgesia comparable to that of i.m. doses of meperidine, pentazocine, or morphine. The most common adverse effects associated with short-term administration are nervous system and gastrointestinal effects; these are usually mild and occur in about 39% of patients. Unlike opiate analgesics, ketorolac does not appear to cause tolerance or physical dependence in patients receiving long-term therapy. Ketorolac tromethamine has been administered concomitantly with morphine or meperidine without apparent adverse interaction. For short-term pain management, an initial i.m. ketorolac tromethamine loading dose of 30 or 60 mg is recommended. Ketorolac tromethamine appears to be as effective as morphine or meperidine for short-term management of moderate to severe postoperative pain. It lacks the respiratory depressant effects of opiate analgesics but shares the toxic potentials of other NSAIAs.
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PMID:Ketorolac, an injectable nonnarcotic analgesic. 229 76

Ketorolac is a potent analgesic agent with antiplatelet properties which is known to cross the placenta. The aim of this study was to determine whether maternal administration of ketorolac in labour had any effect on neonatal platelet function as compared with maternal administration of pethidine and prochlorperazine. Eighteen parous women were studied in labour, twelve received pethidine (control) and six received ketorolac for analgesia. Immediately after delivery, blood was taken from the umbilical vein and anticoagulated with citrate. Platelet aggregation in whole blood was studied. Ketorolac significantly inhibited aggregation in response to arachidonic acid and collagen but not ADP. These findings confirm that ketorolac crosses the placenta. The antiplatelet effects are likely to be related to ketorolac's inhibitory effect on TxA2 production which is required for arachidonic acid and collagen-induced aggregation, but not the primary aggregation response induced by ADP. These effects suggest that ketorolac should be used with caution in patients whose neonates are at risk of haemostatic problems.
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PMID:Effect of maternal ketorolac administration of platelet function in the newborn. 326 21


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