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)

In 66 patients who had to undergo radical abdominal hysterectomy because of cancer of the cervix uteri, the plasma concentrations of beta-endorphin were observed intra- and postoperatively. Two anaesthetic techniques were used: neuroleptanalgesia and thoracolumbar epidural analgesia with sedation and controlled inhalation of a mixture of oxygen and nitrous oxide. While the higher dosage of analgesics administered intraoperatively resulted in markedly lower plasma concentrations of beta-endorphin, there was no such effect in the postoperative phase. Patients with epidural analgesia who were absolutely painless postoperatively had, during that stage, higher concentrations of beta-endorphin in the plasma than those patients who had been given neuroleptanalgesia. They had received no analgetic treatment during the postoperative observation period. These differences are attributed to an increased adaptability of patients subsequent to neuroleptanalgesia. The neuronal block can result in a decrease in functional activity of the suprarenal medulla and impair adaptability. The stress-induced opioid analgesia can be suppressed by circulating enkephalin from the suprarenal medulla.
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PMID:[The quality of analgesia in relation to the plasma concentration of beta-endorphin during neuroleptanalgesia and epidural analgesia]. 214 17

The mechanism of action of opioids and clinically relevant differences among the opioid analgesics are described. Both endorphins (endogenous morphine-like substances) and exogenous opioids (opium alkaloids and their derivatives) bind to opioid receptors in the human central nervous system to provide analgesia and other effects. Some drugs, such as morphine, are true agonists, i.e., they bind to and activate receptors. Some are partial agonists, binding to part of the receptor and causing effects that are similar to, but perhaps less pronounced than, the effects produced by agonists. Others are antagonist, i.e., they bind to the receptor but do not cause the associated effects. Some drugs, termed agonist-antagonist opioids, act as antagonists at one type of receptor and agonists at another type of receptor. True agonists tend to have relatively straight-line dose-response curves; in other words, their effect increases with increasing doses over a broad dosage range. Partial agonists and agonist-antagonists tend to have ceiling effects; that is, they do not have the broad dosage range of drugs such as morphine, methadone, hydromorphone, and other "strong" opioids. This fact mediates against the use of partial agonists and agonist-antagonists in cancer patients who have chronic pain that may increase as the disease progresses. Three major factors that should be considered when a drug is selected for clinical use are (1) relative affinities for the different opioid receptor types, (2) pharmacokinetic characteristics that influence onset and duration of action, and (3) whether the opioids are strong or weak. For treatment of cancer pain, drugs with long durations of action are preferable.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Clinically relevant differences among the opioid analgesics. 216 10

To determine the relationship between changes in plasma methadone concentration and pharmacodynamic effects, plasma methadone profiles and pharmacodynamics (analgesia and sedation) were measured during and after the continuous infusion of methadone for 180 to 270 minutes in 15 patients with pain caused by cancer. An increase in plasma methadone concentration resulted in a rapid increase in pain relief or sedation. The estimates of values of 50% of maximum effect (Css50) for pain relief and sedation obtained with a pharmacokinetic-pharmacodynamic model varied tenfold to twentyfold among patients; the mean Css50 value for pain relief (0.359 +/- 0.158 [SD] micrograms/ml) was virtually the same as the mean Css50 value for sedation (0.336 +/- 0.205 [SD] micrograms/ml). Similarly, the mean gamma (slope function) for pain relief (4.4 +/- 3.8 [SD]) and sedation (5.8 +/- 5.4 [SD]) did not differ. Examination of hysteresis plots of data obtained during the infusion and for 4 to 5 hours after cessation of the infusion revealed a very rapid equilibration between plasma methadone values and the sites mediating pain relief. There was no indication of the development of tolerance to the pharmacodynamic effects of methadone during the study. This report describes a method for quantitating the pharmacokinetic-pharmacodynamic relationships of the desirable and undesirable effects of opioid analgesics.
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PMID:Pharmacokinetic-pharmacodynamic relationships of methadone infusions in patients with cancer pain. 218 71

The pathogenesis of cancer pain, the incidence of pain associated with specific types of malignant tumors, and the nature of acute and chronic pain are discussed, and alternative delivery systems for pain management are described. More than 80% of cancer patients with advanced metastatic disease suffer moderate to severe pain. Most cancer pain is caused by direct tumor infiltration; approximately 20% of cancer pain may be attributed to the effects of surgery, radio-therapy, or chemotherapy. The incidence of cancer pain is related to tumor type; 70% or more of patients with tumors of the bone, cervix, and ovaries suffer cancer-related pain, while only 5% of patients with leukemia have pain. Pain is defined by the organs involved. Somatic pain is usually dull and well localized; visceral pain is generalized and difficult to describe. Other types of pain, including deafferentation pain and referred pain, are particularly difficult to manage. Cancer pain may be acute or chronic. The latter may cause psychological reactions that make effective treatment more challenging. Opiate analgesic agents, administered by the epidural or intrathecal routes, block pain more selectively and produce fewer adverse reactions than systemic analgesic agents. The duration and onset of analgesia depend on the lipophilicity of the agent used. Because pain is the most common complaint of the patient with cancer, clinicians should be aware of the range of pharmacologic and nonpharmacologic analgesic modalities available to them. Familiarity with newer modalities and delivery routes, such as spinal administration of opiate analgesics, is recommended.
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PMID:Understanding cancer pain. 220 10

Moradol ("Galenika", Yugoslavia)/butorphanol tartrate ("Bristol--Mayers C.", USA)/, a synthetic analgesic representing a new generation of opiate receptors agonists-antagonists, devoid of any narcogenic potential has been used as the only analgesic at all stages of anesthesia during cancer surgery in 26 patients. For premedication moradol was used in a mean dose of 0.032 +/- 0.003 mg.kg-1 in combination with diazepam (0.153 +/- 0.005 mg.kg-1) and atropine (0.01 mg X X kg-1). For induction to anesthesia moradol was used in a dose of 0.72 +/- 0.003 mg.kg-1 and diazepam in a dose of 0.27 +/- 0.015 mg.kg-1. General anesthesia was maintained with moradol, diazepam, nitrous oxide and droperidol. The data presented in the paper demonstrate the advantages of moradol at all stages of intra- and postoperative analgesia, which ensures stable anesthetic background (according to hemodynamic parameters) and reduces considerably an overall postoperative analgesic dose.
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PMID:[Synthetic analgesic moradol at various stages of surgical treatment of patients with cancer]. 220 34

A potentially serious complication of long-term epidural catheterization in cancer patients is infection. The early signs of infection were studied in 350 patients in whom long-term epidural catheters were inserted. Three areas of the catheter track were found to be involved; exit site and superficial catheter track infection, and epidural space infection. The authors identified the early signs of infection in each area and the progress of the infection from the deep track to include the epidural space in four of these patients. All 19 patients who developed deep track or epidural infections were successfully treated with antibiotics and catheter removal. None of the patients required surgery for spinal cord decompression. Catheters were replaced in 15 of the 19 treated patients who requested them after treatment with no recurrent infections. It was concluded that use of long-term epidural catheterization is associated with a definable epidural infection rate. The use of epidural opioid analgesia is an effective and safe means of obtaining pain relief for terminally ill patients when patients are monitored for possible infection and receive prompt treatment when the diagnosis is established.
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PMID:Infection during chronic epidural catheterization: diagnosis and treatment. 224 Jun 80

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

1. Not every cancer patient suffers from pain, but approximately 30-40% of regular inpatients and 60-70% in terminal stages do. 2. Not every pain syndrome in a cancer patient is tumor-derived: its role and potential cause need to be thoroughly investigated and treated. 3. Successful antineoplastic treatment is the best and most durable pain prophylaxis in advanced cancer patients. 4. Locally applicable pain treatments such as anesthesiologic, radiotherapeutic and surgical measures should be discussed on an interdisciplinary basis. 5. With chronic tumor pain and no further effect of antineoplastic and locally active treatments, pharmacologic analgesia is the most adequate method of effective pain relief. 6. Prophylactic prescription of effective analgesics in adequate doses and at regular intervals, according to accepted "pain-ladders", is the most successful method of effective and lasting pain relief. 7. Public and medical bias against adequate use of oral opiates in chronic cancer pain must be overcome. 8. Effective pain relief leads to improvement of life quality as well as social reintegration of late stage cancer patients. 9. The influence of psychosocial variables on pain perception and the outcome of analgesia should not be underestimated.
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PMID:[Pain problems in oncology]. 239 63

We studied the cerebrospinal fluid (CSF) and plasma concentration-time profiles of morphine, methadone, and beta-endorphin after lumbar epidural or intrathecal injection in 17 patients with cancer. After epidural injection, all three drugs reached peak levels in lumbar CSF within 34 minutes that were 50 to 1300 times higher than free drug concentrations in plasma. The rate of decline of CSF levels correlated with drug lipid solubility (methadone [t1/2 = 73 minutes] greater than morphine [126 minutes] greater than beta-endorphin [317 minutes]). Plasma levels were comparable with those after intragluteal injection of the same dose. In four patients given intrathecal morphine or methadone, CSF at the C1-2 level contained high levels of morphine as early as 1 hour after injection, but levels of methadone were lower or undetectable. Three of 17 patients reported improved analgesia initially, but none were improved at 2 weeks after chronic therapy. We conclude that analgesia induced by intrathecal or epidural morphine injections is caused by drug acting at both spinal and supraspinal sites. The use of spinal opiates such as morphine is of limited value in patients whose pain is not adequately managed by high systemic doses of morphine-like drugs.
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PMID:Epidural and intrathecal opiates: cerebrospinal fluid and plasma profiles in patients with chronic cancer pain. 241 86

Little systematic research has been reported on analgesic use in terminal cancer patients. This paper presents data from the National Hospice Study on the use of analgesics by a sample of terminal cancer patients served in home based and hospital based hospice programs as well as conventional oncological settings. Patients in hospital based hospice programs were more likely than other patients to have an analgesic prescription and to have consumed analgesics. Patients in hospice settings were more likely to consume analgesia orally and less likely to have "prn" (as needed) analgesic prescriptions. The amount of analgesic consumption was inversely related to age. The paper discusses the implications of these and other findings for the treatment of pain in terminal cancer patients.
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PMID:Analgesic use in terminal cancer patients: report from the National Hospice Study. 241 49


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