Serotonin receptor agonists

Table 17. Serotonin and Serotonin Receptor Agonists and Antagonists...

Anxiolytics are drugs used for the treatment of anxiety disorders. Apart from benzodiazpines, a frequently used anxiolytic is the 5HT1A (serotonin) receptor agonist buspiron, which has no sedative, amnestic or muscle-relaxant side effects, but whose action takes about a week to develop. Furthermore, it is less efficaceous than the benzodiazepines. Buspiron s mechanism of action is not fully understood. 

TABLE 31-3. Comparison of Serotonin Receptor Agonists (Triptans)59-65... 

Serotonin receptor agonists (triptans) Monitor patients for flushing, palpitations, chest pain, and shortness of breath. Recommend electrocardiography if symptoms persist. 

Berge, O. G., Hole, K.., and Dahle, H. (1980) Nociception is enhanced after low doses and reduced after high doses of the serotonin receptor agonist 5-methoxy-N,N-dimethyltryptamine. Neurosci. Lett., 19 219-223. 

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... 

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. 

Contraindications Basilar or hemiplegic migraine, coronary artery disease, ischemic heart disease (including angina pectoris, history of Ml, silent ischemia, and Prinzmetal s angina), uncontrolled hypertension, use within 24 hours of ergotamine-contain-ing preparations or another serotonin receptor agonist, use within 14 days of MAOls... 

Challenge studies with the serotonin receptor agonist, m-chloro-... 

M. Dukat (2004). 5-HT3 serotonin receptor agonists a pharmacophoric journey. Curr. Med. Chem. CNS Agents 4 77-94. 

The Pharmacology and therapeutic potential of serotonin receptor agonists and antagonists, 17, 349... 

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