Is Acute Tolerance to 5-Hydroxytryptamine Opioid Dependent? Its Absence in Migraine Sufferers

Sicuteri, F

doi:10.1046/j.1468-2982.1983.0303187.x

Cited by 8 publications

(4 citation statements)

References 11 publications

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“…Specifically, we showed 43.8% reduction of maximal/overall 5-HT contraction with accumulative doses (5 6 10 27 M, 3 6 10 26 M, 10 25 M, 3 6 10 25 M, 10 24 M, and 10 23 M) of 5-HT 30 minutes following initial same accumulative doses of 5-HT followed by washout 6 3 (initial: median 11.88 mg/mg, minimum 5.83 mg/ mg, maximum 25.65 mg/mg; at 30 minutes: median 6.68 mg/ mg, minimum 3.65 mg/mg, maximum 21.29 mg/mg; P , .02 Wilcoxon test, n 5 7 each group). Others had also shown similar 5-HT tachyphylaxis responses (Sicuteri, 1983;Javid et al, 1999;Whalen et al, 2000;Lopez-Tudanca et al, 2003). However, a single-dosage exposure of human cavernosal strips to 5-HT 10 23 M and subsequent same 5-HT reexposure 30 minutes after vehicle (distilled water) addition both gave similar 5-HT-mediated contractile responses, with no significant difference (Table 1).…”

Section: Organ Bath Studiesmentioning

confidence: 76%

Doxazosin and Serotonin (5‐HT) Receptor (1A, 2A, and 4) Antagonists Inhibit 5‐HT‐Mediated Human Cavernosal Contraction

Lau

Thompson

Bellringer

et al. 2006

Journal of Andrology

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Penile erection results from the balance between relaxation and contractile mechanisms of the corpus cavernosum. Only a few studies suggest a role for endogenous contractile agents such as 5-hydroxytryptamine (5-HT). Our aim was to confirm the possible role of 5-HT in human erection. The effect of 5-HT on human cavernosal tissues, as well as those of doxazosin (shown previously to have 5-HT inhibitory action), ketanserin (5-HT (2A) receptor antagonist), NAN-190 (5-HT (1A) receptor antagonist), and SB 203186 (5-HT (4) receptor antagonist) on 5-HT-mediated effects, were assessed using the organ bath technique, including electrical field stimulation study (EFS). Results are presented as median (mg/ mg 5 mg contraction/mg of tissue). Consistent 5-HT-mediated (10 23 M) contractions were demonstrated (n 5 18; 63 mg/mg). These contractions were inhibited with ketanserin by 90% (n 5 8), NAN-190 by 68% (n 5 12), and SB 203186 by 55% (n 5 12). Doxazosin showed a similar 5-HT inhibitory action in a concentrationdependent manner (10 24 M; 94% reduction; n 5 8, 10 26 M; 68.3% reduction; n 5 8). Our EFS studies indicated the presence of neuronally derived 5-HT and that a majority of the nonnoradrenogenic contraction (54%) was mediated via 5-HT(2A) receptors. These findings suggest that 5-HT may play a role in the human detumescence process via 5-HT(1A), 5-HT(2A), and 5-HT(4) receptors. Neuronally released 5-HT is probably an important contractile neurotransmitter in the erectile process. Doxazosin, ketanserin, and 5-HT(1A) and 5-HT(4) receptor antagonists may be useful as part of combination therapy used to treat erectile dysfunction.

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Section: Organ Bath Studiesmentioning

confidence: 76%

Doxazosin and Serotonin (5‐HT) Receptor (1A, 2A, and 4) Antagonists Inhibit 5‐HT‐Mediated Human Cavernosal Contraction

Lau

Thompson

Bellringer

et al. 2006

Journal of Andrology

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“…From PAG diffuse serotonergic projections go to the cerebral cortex and blood vessels. 5 TH ‐2 A receptors mediate neuronal hyperexcitability and potentiate nociceptive transmission (17, 18). After long‐term use of analgesic medications, Srikiathachorn et al.…”

Section: Discussionmentioning

confidence: 99%

“…From PAG diffuse serotonergic projections go to the cerebral cortex and blood vessels. 5 TH -2 A receptors mediate neuronal hyperexcitability and potentiate nociceptive transmission (17,18). After long-term use of analgesic medications, Srikiathachorn et al have demonstrated an up-regulation of the 5 HT -2 A receptors which mediate a hyperalgesic state, an increased frequency and severity of head pain (19)(20)(21).…”

Section: Discussionmentioning

confidence: 99%

Placebo Response in a Patient with Chronic Migraine and Ergotic Overuse

2005

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Facilitation of nociceptive systems has been implicated in Chronic-Migraine pathogenesis. Daily consumption of medication may be a contributing factor. The patient was male, aged 76 years, with history of migraine without aura. Six years ago, he presented with a mild-moderate daily pulsating headache. He was overusing analgesics and ergotamine. After withdrawing, the patient started a nonpulsating headache, diffuse and constant. During follow up, he was refractive to several symptomatic and prophylactic treatments. When we treated him with placebo capsules, the headache responded very well. At first, pain-relief occurred for 6 h and progressively, extended. Two years later, when our patient started to use transdermal patches of fentanyl for treatment of a complex regional pain syndrome type 1, his headache did not improve. Patient has maintained prolonged response to placebo. Actually, he is pain-free for 2-3 days with 1 placebo capsule. We discuss mechanisms of chronic-migraine, drug-overuse, drug-induced headache and placebo addiction. Powerful psychological mechanisms could determine response to placebo in this patient.

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“…Sicuteri's work [5][6][7] demonstrates that natural opioids play a vital role in regulating pain. There appears to be an opioid deficiency in the mechanisms of migraine headache as well as in morphine abstinence.…”

Section: Commentsmentioning

confidence: 99%

Codeine Self‐medication in a Headache Patient

Eng

Lachenmeyer

1996

Headache

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Self-medicating behavior for the treatment of headaches is a widespread phenomenon with costly and hazardous consequences. The case presented illustrates the ramifications of such behavior and suggests an integrated approach to the management of headaches. Biological mechanisms for the aggravation of headaches by self-medication are discussed and integrated with psychological observations. The existing epidemiologic studies of self-medication are reviewed and reveal a need for further studies, particularly in the United States. Key words: codeine, self-medication (Headache 1996;36:452-455) The extent of self-medicating behavior for chronic headaches has had minimal attention in the medical literature. Yet, it is a widespread phenomenon in this common disorder. Limitations to the systematic study of self-medication in headaches include inconsistent patient contact with the medical community and inaccurate or underreporting of drug use. The latter is particularly common in instances of narcotic abuse. In the former case, it is quite clear that many individuals can bypass medical attention and obtain treatment at their local pharmacy, where a host of over-the-counter (OTC) medications advertise prompt headache relief. CASE HISTORYThe following is a case report of a chronic headache patient with a 25-year history of acetaminophen (Tylenol ® ) and codeine self-medication. The case illustrates the complications resulting from self-medicating behaviors. It also affords an opportunity to study the role of psychological treatments and how such treatments can be integrated into the management of chronic headaches.A 54-year-old patient was referred to a drug treatment program after he was caught by his pharmacist forging a prescription for Tylenol ® No. 4 with codeine. The patient stated that he "pops 6 to 15 pills a day" in order to medicate severe headaches which began when he was in his 20s. Initially, the headaches responded to acetaminophen alone but over the past 10 years, he began to abuse acetaminophen with codeine in gradually increasing doses. He obtained it by using forged prescriptions or from the "black market" to medicate the pain. He often took the pills at the slightest suggestion of a headache and sometimes even when he was asymptomatic in order to avert headaches, particularly when he had an important matter to take care of at work.The patient reported obtaining medical attention for his headaches many times in the past 10 years. Multiple evaluations, including physical examinations, neurological evaluations, complete blood screening, ECG, and several CT scans of the head, were unremarkable. The headaches were described as "stinging" and localized in the forehead. They might occur at any time of the day, and they often woke him at night. The headaches were not preceded by any aura or accompanied by visual, gastrointestinal, or neurological symptoms. His only other health problems were hypertension for 5 years treated with clonidine 0.1 mg orally tid for the past 5 years, a peptic ulcer which had been q...

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Is Acute Tolerance to 5-Hydroxytryptamine Opioid Dependent? Its Absence in Migraine Sufferers

Cited by 8 publications

References 11 publications

Doxazosin and Serotonin (5‐HT) Receptor (1A, 2A, and 4) Antagonists Inhibit 5‐HT‐Mediated Human Cavernosal Contraction

Doxazosin and Serotonin (5‐HT) Receptor (1A, 2A, and 4) Antagonists Inhibit 5‐HT‐Mediated Human Cavernosal Contraction

Placebo Response in a Patient with Chronic Migraine and Ergotic Overuse

Codeine Self‐medication in a Headache Patient

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