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Query: UMLS:C0278080 (physical dependence)
 1,658 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

1. Structure-activity relationship studies with new semi-synthetic isomorphine derivatives revealed that substitution of an azido group in position 6 (azidomorphines) greatly increases the analgesic potency whereas tolerance and dependence liability tend to decrease. 2. Azidomorphine (6-deoxy-6-azidodihydroisomorphine) and 14-hydroxyazidomorphine (6-deoxy-6-azidodihydro-14-hydroxyisomorphine) being in animal tests 40-300 times more potent than morphine, are the most effective analgesics among the semi-synthetic morphine alkaloids. 3. As demonstrated on mice, rats and rhesus monkeys, a remarkable dissociation between the analgesic potency and physical dependence capacity was the result of the introduction of the 6-azido group into dihydroisomorphine. 4. A dichotomy between analgesic effect and tolerance and addiction liability was demonstrated with azidomorphine also in man and the new substance proved to exert significantly less untoward effects than either morphine or pentazocine. 5. Rymazolium (Probon) a new non-narcotic analgesic which strongly potentiates the analgesic and antagonizes the respiratory depressant effect of morphine alkaloids in animals proved to hinder the development of tolerance to morphine in animals and man. 6. The azidomorphine-rymazolium association was found to be less respiratory depressant than azidomorphine administered alone. In patients with chronic intractable pain, an association of azidomorphine (0.5 mg) and rymazolium (150 mg) achieved total pain relief without noticeable euphoria and none of the twelve patients showed, according to the Himmelsbach scoring system, acute abstinence syndromes after nalorphine administration.
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PMID:Azidomorphines: a new family of potent analgesics with low dependence capacity. 4 67

Narcotic analgesics and related drugs act as agonists on several receptors that are responsible for their effects on pain perception, mood and feeling state, and respiration, as well as other pharmacologic actions. Naloxone is the first discovered antagonist that is devoid of agonistic activity and appears to be a competitive antagonist at several receptors. The ability of naloxone to displace or prevent the binding of agonistic narcotics is partly responsible for its antagonistic effects. The ability of naloxone to rectify narcotic-depressed homeostats and precipitate abstinence is also related to its antagonistic activity. Certain cautions and principles apply in the use of naloxone in treating narcotic overdose, reversing surgical analgesia, and the treatment of neonates and children. Unapproved uses of naloxine include reversing the psychotomimetic effects of certain agonists-antagonists, terminating narcotic-induced convulsions and coma, reversing non-narcotic depression, diagnosing physical dependence, and treating narcotic addicts.
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PMID:Naloxone. 18 95

The chemistry, pharmacology, uses, side effects, pharmacokinetics and dosage of butorphanol tartrate, a narcotic analgesic with antagonist properties, are reviewed. When administered intramuscularly or intravenously, butorphanol tartrate appears to be as effective for relieving moderate to severe pain as are pentazocine, meperidine and morphine. Butorphanol produces sedation more commonly and, at therapeutic dosages, depresses respiration as much as these other narcotic analgesics. A limited number of long-term clinical studies suggest a lower physical dependence liability with butorphanol than with other narcotic analgesics. Butorphanol is more expensive than morphine and, for most patients, offers no significant advantages over morphine for short-term use. Because butorphanol's cardiovascular effects are not completely understood, morphine also remains the drug of choice for pain associated with myocardial infarction.
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PMID:Drug therapy reviews: evaluation of butorphanol tartrate. 39 9

This prospective and comparative study was designed to determine the role of cancer pain and attitudes towards morphine in attenuating the intensity and duration of physical dependence following chronic morphine treatment. Morphine was administered via a stepwise ladder approach in order of oral, spinal and intravenous routes depending on the adequacy of analgesia. On-demand titration of a dose, either upward or downward, was liberal and unlimited. Withdrawal strategy was evaluated and initiated either by patients (PI group) or their families (FI group). The manifestation of physical dependence on morphine was compared between patients who successfully withdrew (total withdrawal), and patients who failed to withdraw (episodic withdrawal), from morphine for a period of more than two weeks. Eighty-eight out of 627 patients (14.1%) were excluded from our protocol; 75% of these exclusions were due to objections toward morphine as the major form of analgesic. Drop-out due to poorly tolerated side effects was relatively rare (18.2%). Fifty-four (10.0%) achieved total withdrawal and 212 (39.3%) experienced episodic withdrawal. Non-pain-related abstinence symptoms were highly prevalent but were tolerable for both groups. Pain-related symptoms were more exaggerated during episodic withdrawal. Intolerable pain, rather than physical dependence, contributed to the failure to withdraw from morphine. Among a total of 539, addiction was found in only one patient (0.18%) who began drug use long before entering our protocol. Attitudes towards morphine affect the acceptance of treatment and hasten the withdrawal strategy. Families were more anxious about morphine than the patients themselves which led to more aggressive, but less tolerable, withdrawal.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Can cancer pain attenuate the physical dependence on chronic long-term morphine treatment? 135 30

Spinal cord injury (SCI) can cause paralysis; sensory impairment; autonomic nervous system dysfunction; and bowel, bladder, and sexual dysfunction. These impairments may lead to immobility, physical dependence, and alterations in lifestyle and self-esteem. The addition of chronic, intractable pain to these impairments can be truly devastating. Chronic pain superimposed on spinal cord injury can virtually drain the individual of strength, motivation, and will. For the spinal cord injury survivor who already faces functional loss, severe pain can further restrict even the diversional activities that are available. Thus, it may become impossible for the individual to escape his or her pain even temporarily. The various medical, physical, and surgical treatments considered to be efficacious in treating this pain are reviewed. However, although chronic pain in SCI may be managed by these therapies, a permanent cure may not result.
Clin J Pain 1992 Jun
PMID:Clinical management of chronic pain in spinal cord injury. 163 73

Inadequately treated acute and chronic pain remains a major cause of suffering, in spite of enormous advances in pharmacology and technology. Opioids provide a powerful, versatile, widely available means of managing this pain, but their use is too often restrained by ignorance and mistaken fears of addiction. The management of postoperative pain (perhaps the most common form of acute pain) is traditionally attempted with fixed dosages of analgesics by relatively unpredictable routes (e.g. oral, rectal and intramuscular). Intravenous opioid infusions (an improvement) risk respiratory depression and require close monitoring and titration. Patient-controlled analgesia (PCA), by contrast, permits the most efficacious medication (pure opioid agonist) by the optimal route (intravenous) under direct control of the patient, and provides high levels of satisfaction and safety. Ideally, any opioid use should be integrated with a wide spectrum of other analgesic modalities in an anaesthesiology-based 'acute pain service'. The use of opioids for chronic pain of nonmalignant origin remains controversial. There is a perceived conflict between patients' interests and those of society. However, problems (such as tolerance, physical dependence, addiction and chronic toxicity), anticipated from experience with animal experiments and pain-free abusers, seldom cause difficulties when opioids are used appropriately to treat pain (so-called 'dual pharmacology'). With sensible guidelines, and in the context of a multidisciplinary pain clinic, opioids may provide the only hope of relief to many sufferers of chronic pain.
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PMID:Treatment principles for the use of opioids in pain of nonmalignant origin. 171 22

This article examines misperceptions and barriers to adequate pain relief in cancer patients. Healthcare professionals have gaps in their knowledge of opioid drugs as well as misconceptions concerning tolerance, physical dependence, and addiction that often lead to the underprescribing of these agents. The pervasiveness of the "say no to drugs" message in our society and the fear of addiction on the part of patients and their families creates yet another barrier to the legitimate use of opioids to treat cancer pain. Legal and regulatory documents filled with arbitrary and ill-defined labels meant to promote the legitimate use of these drugs and curtail their misuse may instead intimidate healthcare professionals and negatively influence prescribing habits. Increased educational efforts for pharmacists and other healthcare professionals as well as the development of clinical role models and state cancer pain initiatives are cited as means to break down these barriers in order to achieve adequate pain relief for all cancer patients.
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PMID:Misperceptions and inadequate pain management in cancer patients. 172 70

The treatment of severe pain requires the use of potent opioid analgesic medications. Many patients with opioid sensitive pain are being undermedicated. This results in increased morbidity and needless suffering. The most important reason for this undertreatment is the fear of addiction engendered by opioids, a fear that is greatly out of proportion to the real risk. The risk of addiction is greatly overestimated in part because many people do not understand the distinctions between drug abuse and drug addiction, on the one hand, and physical dependence and tolerance, on the other. Dependence and tolerance are virtually inevitable outcomes of long-term opioid use, but they are neither sufficient to cause addiction nor the equivalent of it. Indeed, the evidence shows that only a tiny fraction of patients treated with opioids become addicted. There is little risk of addiction for those patients receiving properly administered opioids for pain.
J Pain Symptom Manage 1990 Feb
PMID:Perspectives on the medical use of drugs of abuse. 196 89

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

The novel and highly selective, conformationally restricted enkephalin analogue for delta-opioid receptors, [D-Pen2,D-Pen5]enkephalin (DPDPE; Pen = penicillamine), was studied in various in vivo tests for analgesia, tolerance and physical dependence. Intracerebroventricular (i.c.v.) administration of DPDPE caused a dose-dependent, naloxone-reversible antinociception, measured with the heat-irradiant (tail-flick) method. Acute tolerance developed to the antinociceptive effect of DPDPE. DPDPE also caused mild signs of physical dependence (withdrawal hypothermia and body weight loss) after repeated peptide treatment. Severe signs of morphine withdrawal (e.g. withdrawal jumping) on the other hand, could not be reversed by the administration of DPDPE. It is concluded that the activation of central delta-opioid receptors may play a role in controlling pain mechanisms, and that this activation is followed by the rapid development of a tolerance to this action.
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PMID:Analgesic and tolerance-inducing effects of the highly selective delta opioid agonist [D-Pen2,D-Pen5]enkephalin in mice. 284 84


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