Migraine serotonin

The triptans are considered specific therapies in that they target the pathophysiology underlying migraine.33 They abort headache through beneficial effects on neuronal imbalances.11 Triptans inhibit neurotransmission in the trigeminal complex and activate serotonin lb/Id pathways that modulate nociception in the brain stem. They also decrease the release of vasoactive peptides leading to vascular reactivity and pain.34 Triptans are a welcome addition to the therapeutic armamentarium in that they are available in intranasal, subcutaneous, and oral... 

Ferrari MD, Roon KI, Lipton RB, Goadsby PJ. Oral triptans (serotonin 5-HT1BAD agonists) in acute migraine treatment A meta-analysis of 53 trials. Lancet 2001 358 1558-1575. 

Substance P, an undecapeptide, is abundant both in the periphery and in the central nervous system. It is usually co-localized with one of the classical neurotransmitters, most commonly serotonin. Substance P is thought to have a role in the regulation of pain, asthma, psoriasis, inflammatory bowel disease and, in the CNS, emesis, migraine, schizophrenia, depression and anxiety. The substance-P-preferring receptor neurokinin-1 has been focused on most intensively in drug development, and existing... 

Selective serotonin reuptake inhibitors are considered to be less effective than TCAs for migraine prophylaxis and should not be considered first- or second-line therapy. However, they may be beneficial when depression is a significant contributor to headache. Preliminary data suggest a possible benefit with venlafaxine. 

Serotonin 5-HT1A Human cDNA Alzheimer s disease, anxiety, depression, schizophrenia, hypertension, inflammation, pain, migraine, spasticity ulcers, obesity glaucoma Somatodendritic autoreceptor in hippocampus and raphe nuclei, circadian rhythm, somatodendritic heteroreceptor at cholinergic terminals of myenteric plexus... 

Sumatriptan is a 5HT (serotonin) agonist indicated in the treatment of migraine. Sumatriptan causes vasoconstriction and must therefore be used with caution in patients with coronary heart disease, such as angina. Concurrent administration of the agonist, sumatriptan and antagonists, such as fluoxetine, which is a selective serotonin re-uptake inhibitor, leads to increased CNS toxicity. 

Serotonin syndrome (sibutramine) The rare, but serious, constellation of symptoms also has been reported with the concomitant use of selective serotonin reuptake inhibitors and agents for migraine therapy (eg, sumatriptan, dihydroergotamine), certain opioids (eg, dextromethorphan, meperidine, pentazocine, fentanyl), lithium, or tryptophan. Because sibutramine inhibits serotonin reuptake, it should not be administered with other serotonergic agents. 

Sumatriptan (Imitrex) [Antimigraine Agent/Selective 5-HTi Receptor Agonist] Uses Rx acute migraine Action Vascular serotonin receptor agonist Dose Adults. SQ 6 mg SQ as a single dose PRN repeat PRN in 1 h to a max of 12 mg/24 h PO 25 mg, repeat in 2 h, PRN, 100 mg/d max PO dose max 300 mg/d Nasal spray 1 spray into 1 nostril, repeat in 2 h to 40 mg/24 h... 

Parthenolide inhibits serotonin release, an action that is thought to be a likely source of its effectiveness in migraine. Extracts have also been shown to reduce the production of prostaglandins (another possible mechanism) and leukotrienes. Interestingly, melatonin has been identified in feverfew, a possibly significant observation, since chronic migraines have been associated with low melatonin levels. 

Mechanism of Action A serotonin receptor agonist that binds selectively to vascular receptors, producing a vasoconstrictive effect on cranial blood vessels. Therapeutic Effect Produces relief of migraine headache. 

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