Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Although caffeine is the most widely used behaviorally active drug in the world, caffeine physical dependence has been poorly characterized in laboratory animals and only moderately well characterized in humans. In humans, a review of 37 clinical reports and experimental studies dating back to 1833 shows that headache and fatigue are the most frequent withdrawal symptoms, with a wide variety of other signs and symptoms occurring at lower frequency (e.g. anxiety, impaired psychomotor performance, nausea/vomiting and craving). When caffeine withdrawal occurs, severity can vary from mild to extreme (i.e. incapacitating). The withdrawal syndrome has an onset at 12-24 h, peak at 20-48 h, and duration of about 1 week. The pharmacological specificity of caffeine withdrawal has been established. The proportion of heavy caffeine users who will experience withdrawal symptoms has been estimated from experimental studies to range from 25% to 100%. Withdrawal symptoms have been documented after relatively short-term exposure to high doses of caffeine (i.e. 6-15 days of greater than or equal to 600 mg/day). Although animal and human studies suggest that physical dependence may potentiate the reinforcing effects of caffeine, human studies also demonstrate that a history of substantial caffeine intake is not a necessary condition for caffeine to function as a reinforcer. The similarities and differences between caffeine and classic drugs of abuse are discussed.
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PMID:Caffeine physical dependence: a review of human and laboratory animal studies. 313 89

Fifty-two patients, most of whom had had daily headaches for years, were examined and treated. Among them there were 40 who originally had migraine, the others had vasomotor or post-contusional headaches. Average duration of the migraine was 21 years, of chronic headache 7.6 years. All patients had been taking analgesics of a mixed type regularly and for a long time, on average 35.6 tablets or suppositories weekly. All patients had taken more than three different drugs. After an observation period of 3-6 months for grading the headaches and registering the amount of drug intake, all patients were admitted to hospital when all analgesics were at once discontinued. Changing degrees of withdrawal symptoms were the rule: increased headaches, nausea, vomiting, tachycardia, sweating, sleep disorders, and in some also hallucinations and cerebral episodes. At the end of the hospital stay chronic headache had completely disappeared or markedly improved in 77% of patients. Even after an average of 16 months of subsequent observation, chronic headache continued to be significantly improved in 70% of patients. There was a significant reduction in frequency and intensity of attacks in the patients with originally typical migraine. Regular intake of analgesics of the mixed type induces chronic headaches. These are most commonly caused by ergotamine tartrate and aminophenol derivatives, while psychological and physical dependence on anti-migraine drugs is initiated and maintained by additional barbiturates, caffeine and codeine.
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PMID:[Chronic analgesic-induced headache]. 614 24

This paper reports the DHE substitution clinical trial in 38 heroin addicts. The CINA (Clinical Institute Narcotic Assessment) scale was used to assess physical dependence potential. The CINA scale contains 10 opioid withdrawal signs (nausea, vomiting, gooseflesh, sweating, restlessness, tremor, larcrimation, nasal congestion, yawning, changes in heart rate and systolic blood pressure) and 3 opiate withdrawal symptoms (abdominal pain, muscle pain and feeling hot or cold). For each subject admitted to the Drug Detoxification and Treatment Center his (her) status on each of the 13 items of CINA were immediately rated. Then, naloxone 0.4 mg was injected iv to precipitate withdrawal symptoms and at 5, 10, 15 min after the naloxone injection, the CINA score of each patient was rated again. The differences among the scores of pre- and post-naloxone injection is a measurement of the degree of withdrawal symptoms. Then, a single dose of DHE was administered sublingually to each patient, all withdrawal symptoms disappeared. These results show that DHE can compete with naloxone for opioid receptors. A good dose-response relationship was found between the 100% suppressive withdrawal sign doses of DHE and the degree of withdrawal sign in heroin addicts. The physical dependence potential of DHE given to heroin addicts sublingually was probably more than that of methadone given to heroin addicts orally by making reference to the report of Dr. Peachy.
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PMID:[Clinical assessment of physical dependence potential of dihydroetorphine hydrochloride (DHE)]. 797 40

The difference between the development of physical dependence on morphine administered via Alzet miniosmotic pumps as well as syringe injection (twice a day) at fixed times was examined in conscious dogs. Physical dependence was quantified by polygraphically measuring naloxone-precipitated withdrawal signs on the day 8 after the subcutaneous implantation of miniosmotic pumps which supplied morphine at 1-5 mg/kg/day. Morphine plasma levels were maintained at 19-25 and 41-47 ng/mL during infusions of morphine at doses of 2.5 and 5 mg/kg/day, respectively. Morphine withdrawal was characterized by hyperactivity, biting, digging, tremors, nausea, hyperthermia, and increased wakefulness, and by electroencephalographic (EEG) activation in the amygdala and hippocampus, followed by dissociation of the EEG in the cortex (fast wave) from that in the limbic (slow wave) system, increased heart rates, and raised blood pressure. These morphine withdrawal signs seemed to be more severe than those exhibited in animals that had received syringe injections of morphine at the same doses. These results suggest that the use of miniosmotic pumps in dogs may be a very convenient and useful method for both evaluating drug dependence and studying its mechanisms.
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PMID:Physical dependence on morphine induced in dogs via the use of miniosmotic pumps. 829 85

Although controversial, opioid analgesics have been prescribed for patients with chronic facial pain. Based primarily on survey data and a few well-controlled clinical trials, long-term opioid treatment provides adequate pain reduction in 41% to 100% of patients with chronic nonmalignant pain. However, only 25% of chronic facial pain patients reported adequate pain relief with chronic opioid treatment. Work, home, and school function are generally reestablished or maintained during chronic opioid treatment, but 25% to 38% of patients remain dysfunctional, and one study indicated that 20% of patients became dysfunctional during treatment. Chronic opioid treatment is associated with many transient side effects; constipation, dizziness, nausea, vomiting, itching, and fatigue have been reported in 5% to 42% of patients taking opioids over 1 year. Although survey studies suggest that the risks of addiction are low in typical patients, drug abuse rates up to 17.3% and prescription abuse rates up to 27.6% were reported within groups of chronic opioid users. Chronic opioid use induces analgesic tolerance and physical dependence, which may result in a serious abstinence syndrome in users and children born to users. Chronic opioid use also may induce harmful immune system changes, diminish cognitive and motor function, and produce nociceptive hyperexcitability. This article shows that the use of long-term opioids for chronic facial pain is not justified based on the available data. Despite these perceived problems, there is anecdotal evidence that chronic facial pain patients will respond positively to opioid analgesics. In our experience, the pain assessment scale and a modification of the World Health Organization's three-step analgesic ladder, which prescribes nonopioid analgesics, can be the starting point for the successful management of chronic facial pain.
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PMID:The use of nonopioid drugs in management of chronic orofacial pain. 973 70

This report reviews the causes of ocular pain and discusses the pharmacology, pharmacokinetics, efficacy, adverse effects, and dosage of tramadol, a novel non-narcotic oral analgesic. Tramadol is a synthetic analog of codeine with a dual mechanism of action that involves agonist activity at the mu opioid receptor, as well as inhibition of monoaminergic (norepinephrine and serotonin) re-uptake. Unlike opiate analgesics, tramadol has very low propensity toward physical dependence. Common dose-related adverse effects of tramadol include dizziness, nausea, vomiting, dry mouth, and/or drowsiness. Clinically, tramadol has been shown to be equivalent to acetaminophen (325 mg)-codeine (30 mg) combinations for the treatment of moderate or severe nonocular pain. Tramadol appears to be an effective analgesic agent for pain control due to postoperative surgical trauma, as well as in various chronic malignant and nonmalignant disease states. Tramadol has shown variable effectiveness in the control of pain related to dental procedures. The usefulness of tramadol in pain states from ophthalmic origin has yet to be clinically established.
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PMID:Analgesics in ophthalmic practice: a review of the oral non-narcotic agent tramadol. 1044 36

Cough is an important defensive reflex of the upper airway and is also a very common symptom of respiratory disease. Cough following an upper respiratory viral infection is transient, and persistent cough is associated with a whole range of conditions, such as asthma, rhino-sinusitis and gastro-oesophageal reflux. Treatment directed at these conditions may improve the associated cough. There is often a need, however, to control cough itself whatever the cause. The most effective drugs in this class are the opioids, such as morphine, codeine or pholcodeine, but at effective doses they have side effects including drowsiness, nausea, constipation and physical dependence. Investigations into the cough reflex and into the potential mechanisms of sensitised cough reflex have uncovered several potential targets for novel drugs. New opioids apart from mu-agonists such as kappa- and delta -receptor agonists, have been developed, in addition to non-opioids such as nociceptin. Neurokinin receptor antagonists, bradykinin receptor antagonists, vanniloid receptor VR-1 antagonists may be beneficial by blocking effects of tachykinins and sensory nerve activation. Local anaesthetics, blockers of sodium-dependent channels and maxi-K Ca2+-dependent channel activators of afferent nerves are inhibitors of the cough reflex. Some of these novel agents may act centrally or peripherally or at both sites as antitussives. Large scale trials of these novel compounds have not been carried out in cough in man but there is a serious need for more effective antitussives devoid of side effects.
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PMID:Cough: potential pharmacological developments. 1208 6

Cough is an important defensive reflex of the upper airway and is also a very common symptom of respiratory disease. Cough after an upper respiratory virus infection is transient, and persistent cough is associated with a whole range of conditions such as asthma, rhino-sinusitis, gastro-oesophageal reflux. Treatment directed at these conditions may improve the associated cough. There is often a need, however, to control cough itself, whatever the cause. The most effective drugs in this class are the opioids, such as morphine, codeine or pholcodeine, but at effective doses they have side-effects such as drowsiness, nausea, constipation and physical dependence. Investigations into the cough reflex and into the potential mechanisms of sensitised cough reflex have uncovered several potential targets for novel drugs. New opioids such as k- and d-receptor agonists apart from m-agonists have been developed, in addition to non-opioid, nociceptin. Neurokinin receptor antagonists, bradykinin receptor antagonists, vanilloid receptor VR-1 antagonists may be beneficial by blocking effects of tachykinins, and sensory nerve activation. Local anaesthetics, blockers of sodium-dependent channels, and maxi-K CA2+-dependent channel activators of afferent nerves are inhibitors of the cough reflex. Some of these novel agents may act centrally or peripherally or at both sites as antitussives. Large scale trials of these novel compounds have not been tried in cough in man, but there is a serious need for more effective antitussives devoid of side-effects.
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PMID:Therapy for cough: active agents. 1209 88

Dihydroetorphine (DHE) is one of the strongest analgesic opioid alkaloids known; it is 1000 to 12000 times more potent than morphine. Several in vitro and in vivo studies have shown that DHE is a selective mu-opioid receptor (OP(3)) agonist that also binds and activates all human recombinant mu-, delta-, and kappa-opioid receptors (OP(3), OP(1), and OP(2)). The onset of the analgesic effect of DHE in rodents is rapid, 5 to 15 min after parenteral administration; the duration of action is short, the analgesic effect disappears within 120 min after administration. By oral administration much higher doses of DHE are required to produce analgesic effects. These characteristics are accounted for by the pharmacokinetic properties of DHE in the rat, namely, by rapid distribution of DHE from the injection site to the brain and rapid metabolism by glucuronidation in the gut and liver followed by elimination into the bile. Continuous infusion and repeated administration of DHE lead to the development of tolerance to analgesia, physical dependence, and a rewarding effect in normal rats but not in animals with formalin-induced inflammation. Although formalin-induced inflammation is only one type of pain stimulus, these findings suggest that DHE addiction would be observed only in the case of pain-free conditions. Clinical reports in China show that sublingual doses of DHE, 20 to 180 microg, produce a potent analgesic effect with only mild side effects, including dizziness, somnolence, nausea, vomiting, constipation, and shortness of breath. To improve the short-lasting effect following sublingual administration, transdermal delivery of DHE via a patch has been investigated. The patch formulation of DHE produces continuous analgesic effect with minimal physical dependence and rewarding effect in rats suffering from chronic pain. This patch formulation, which is very suitable for DHE, may be viable for the treatment of severe pain and is likely to improve patients' quality of life.
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PMID:Dihydroetorphine: a potent analgesic: pharmacology, toxicology, pharmacokinetics, and clinical effects. 1248 Nov 94

Cough is an important defensive reflex of the airway and a common symptom of respiratory disease. After an upper respiratory tract virus infection, cough is transient, but is more persistent with conditions such as asthma, rhinosinusitis, gastroesophageal reflux, chronic obstructive pulmonary disease (COPD) and lung cancer. Treatment directed at these conditions may improve cough, but there remains a need to control cough directly. The most effective antitussives are opioids, such as morphine, codeine or pholcodeine, but they produce side effects including drowsiness, nausea, constipation and physical dependence. Opioids such as k- and d-opioid receptor agonists, non-opioids such as nociceptin, neurokinin and bradykinin receptor antagonists, vanilloid receptor VR(1) antagonists, blockers of sodium-dependent channels, and maxi-K calcium-dependent channel activators of afferent nerves may all represent novel antitussives and this needs to be confirmed in clinical trials.
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PMID:Current and future prospects for drugs to suppress cough. 1291 74


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