Profiles of opioid analgesia in humans after intravenous bolus administration: alfentanil, fentanyl and morphine compared on experimental pain

Chapman, C. Richard; Hill, Harlan F.; Saeger, Louis C.; Gavrin, Jonathan R.

doi:10.1016/0304-3959(90)90049-j

Cited by 58 publications

(44 citation statements)

References 15 publications

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“…Electrically-induced pain in the teeth and skin has been assessed by electroencephalogram (EEG) recordings. This type of pain assessment showed opioid analgesia in accordance with the psychophysical pain scoring [51,86].…”

Section: Figuresupporting

confidence: 60%

“…Electrical pain was unaffected in one study, whereas two studies found an effect on this pain modality [58][59][60]. Furthermore electrical dental pain has been tested and found to be attenuated by fentanyl [51,61]. Heat pain has been tested through various stimulation paradigms and conflicting results exist.…”

Section: Fentanyl (Table 3)mentioning

confidence: 99%

“…Morphine is generally effective towards pain from many different stimulus modalities [37,51,81,94,95]. However, the results are not as clear-cut as seen with alfentanil and this could be due to the complex pharmacokinetic profile of morphine.…”

Section: Figurementioning

confidence: 99%

“…The amount of morphine absorbed is very individual and this opioid enters the main effect site (the CNS), by crossing the blood brain barrier slowly [98]. All this causes increased variability of the individual subject's response to morphine, blurring the findings in experimental pain research [51,99].…”

Section: Figurementioning

confidence: 99%

See 3 more Smart Citations

Assessing analgesic actions of opioids by experimental pain models in healthy volunteers – an updated review

Staahl

Olesen

Andresen

et al. 2009

Brit J Clinical Pharma

113

131

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AIMExperimental pain models may help to evaluate the mechanisms of action of analgesics and target the clinical indications for their use. This review addresses how the efficacy of opioids can be assessed in human volunteers using experimental pain models. The drawback with the different study designs is also discussed. METHODA literature search was completed for randomized controlled studies which included human experimental pain models, healthy volunteers and opioids. RESULTSOpioids with a strong affinity for the m-opioid receptor decreased the sensation in a variety of experimental pain modalities, but strong tonic pain was attenuated more than short lasting pain and non-painful sensations. The effects of opioids with weaker affinity for the m-opioid receptor were detected by a more narrow range of pain models, and the assessment methods needed to be more sensitive. CONCLUSIONThe way the pain is induced, assessed and summarized is very important for the sensitivity of the pain models. This review gives an overview of how different opioids perform in experimental pain models. Generally experimental pain models need to be designed with careful consideration of pharmacological mechanisms and pharmacokinetics of analgesics. This knowledge can aid the decisions needed to be taken when designing experimental pain studies for compounds entering phase 1 clinical trials.

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Section: Figuresupporting

confidence: 60%

Section: Fentanyl (Table 3)mentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

Section: Figurementioning

confidence: 99%

See 2 more Smart Citations

Assessing analgesic actions of opioids by experimental pain models in healthy volunteers – an updated review

Staahl

Olesen

Andresen

et al. 2009

Brit J Clinical Pharma

113

131

View full text Add to dashboard Cite

show abstract

“…Oral morphine and hydromorphone are primarily metabolized in the liver through the uridine-diphosphoglucuronosyltransferase (UGT) system [68]. Fentanyl [69] and methadone [70] are metabolized by the CYP3A4 enzyme, which is responsible for the complete or partial metabolism of 50% of all known drugs. Genetic variation in CYP2D6 results in poor metabolism of the opioid codeine to its active metabolite morphine [66,71].…”

Section: Opioid Metabolismmentioning

confidence: 99%

Clinical Pharmacology and Pharmacotherapy of Opioid Switching in Cancer Patients

Ross¹,

Riley²,

Quigley³

et al. 2006

The Oncologist

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Pain is one of the most common and often most feared symptoms in patients with cancer. Ongoing or progressive pain is physically debilitating and has a marked impact on quality of life. Since a third of the population will die from cancer, and of these, 80% will experience severe pain in their final year of life, effective treatment of cancer-related pain remains both a high priority and an ongoing challenge in clinical practice. Individuals with moderate to severe cancer-related pain require treatment with strong analgesics, namely opioids.There is evidence to support the therapeutic maneuver of opioid switching in clinical practice, but further evidence is needed to elucidate the underlying mechanisms for interindividual differences in response to different opioids. Large, robust clinical trials will be needed if clinical differences among side-effect profiles of different opioids are to be clearly demonstrated. This review discusses candidate genes, which contribute to opioid response; many other genes have also been implicated in "pain" from animal or human studies. In order to continue to evaluate the genetic contributions to both pain susceptibility and analgesic response, further candidate genes need to be considered. Good pain control remains a high priority for clinicians and patients, and there is much work to be done to further individualize analgesic therapy for patients with cancer.

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Application of a Variable Direction Hysteresisminimization Approach in Describing the Central Nervous System Pharmacodynamic Effects of Alfentanil in Rabbits

Modi

Veng‐Pedersen

1994

Journal of Pharmaceutical Sciences

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Profiles of opioid analgesia in humans after intravenous bolus administration: alfentanil, fentanyl and morphine compared on experimental pain

Cited by 58 publications

References 15 publications

Assessing analgesic actions of opioids by experimental pain models in healthy volunteers – an updated review

Assessing analgesic actions of opioids by experimental pain models in healthy volunteers – an updated review

Clinical Pharmacology and Pharmacotherapy of Opioid Switching in Cancer Patients

Application of a Variable Direction Hysteresisminimization Approach in Describing the Central Nervous System Pharmacodynamic Effects of Alfentanil in Rabbits

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