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Serotonin

The document presents a seminar on the physiological and pathological roles of serotonin, highlighting its classification, synthesis, serotonin receptors, and pharmacological actions. Serotonin, primarily produced in the gastrointestinal tract, influences various body functions and is implicated in conditions like nausea, vomiting, and migraine. The seminar is part of the M.Pharm curriculum at Raghavendra Institute of Pharmaceutical Education and Research, emphasizing its importance in pharmacology.

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Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 Physiological and pathological role of serotonin A seminar as a part of curricular requirement for 1 year M.Pharm 1 semester Presented by k.Firdous banu (20L81S0105) Under the Guidance /Mentorship of A.Sudheer M. Pharm Associate professor department of pharmacology
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 2 Contents : • Autocoids • Classification • Serotonin introduction • synthesis • Serotonergic receptors • Physiological actions • Pathophysiological role
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 3 AUTOCOIDS  Auto means self and Akos means remedy. Autacoids can be released by various stimuli. when released they bring about many physiological changes such as reddening of the skin, pain, itching, bronchospasm, etc. These effects can sometimes be undesirable and cause death. To prevent these autacoids antagonists are used.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 4 Classification • 1) Decarboxylated amino acids: a) Histamine b) Serotonin • 2) Polypeptide: a) Angiotensin b) Plasmakinin c) Vasopressin • 3) Lipid derived: a) Leukotrienes b) Thromboxanes c) Prostaglandins
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 5 Serotonin • Serotonin is a monoamine neurotransmitter biologically derived from tryptophan. • Structurally it contain indole ring , hydroxyl group and ethyl amine group attached to the ring.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 6 • Approximately 90% of the human body's total serotonin is located in the enterochromaffin cells in the GI tract. • About 8% is found in platelets and 1–2% in the CNS. • Serotonin is metabolized mainly to 5-HIAA, chiefly by the liver.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 7 Synthesis
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 8 Types of serotonin receptors: 5-HT1- 5-HT7 • All are GPCRs expect 5-HT3(it is a ligand gated Na+channel). • All are cAMP expect 5-HT2. • 5-HT1 Inhibit cAMP and 5-HT4, 5-HT6 and 5HT7 increases cAMP. Serotonergic receptors
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 9
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 10
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 11
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 12 1. CVS :  It constrict large vessels , dilates arterioles.  BP: a triphasic response is classically seen on i.v. injection of 5-HT in animals. • Early sharp fall in BP—due to coronary chemoreflex. • Brief rise in BP—due to vasoconstriction and increased cardiac output. • Prolonged fall in BP—due to arteriolar dilatation and extravasation of fluid. Pharmacological actions
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 13 2. Visceral smooth muscles :  Peristalsis is increased and diarrhoea can occur.  It constricts bronchi, but is less potent than histamine. 3. Glands :  5-HT inhibits gastric secretion (both acid and pepsin), but increases mucus . It thus has ulcer protective property. 4. Nerve endings and adrenal medulla: Afferent nerve endings are activated causing tingling and pricking sensation, as well as pain.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 14 5. Platelets : By acting on 5-HT2A receptors 5-HT causes changes in shape of platelets, but is a weak aggregator. 6. CNS :  Direct injection in the brain produces sleepiness, changes in body temperature, hunger and a variety of behavioural effects.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 15 1.Neurotransmitter : 5-HT appears to be involved in sleep, temperature regulation, thought, cognitive function, behaviour and mood, appetite, vomiting and pain perception. 2. Precursor of melatonin : 5-HT is the precursor of melatonin in pineal gland. It is believed to regulate the biological clock and maintain circadian rhythm. 3. Neuroendocrine function : It regulate anterior pituitary hormone. Pathophysiological role
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 16 4. Nausea and vomiting :  Especially that evoked by cytotoxic drugs or radiotherapy is mediated by release of 5-HT and its action on 5-HT3 receptors in the gut. 5. Migraine :  initiate the vasoconstrictor phase of migraine and to participate in neurogenic inflammation of the affected blood vessels. 6. Haemostasis : Platelets release 5-HT during aggregation at the site of injury to blood vessel. 5-HT accelerates platelet aggregation and clot formation.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 17 Synthesis inhibitor • p-Chlorophenylalanine (PCPA) selectively inhibits tryptophan hydroxylase (rate limiting step) and reduces 5-HT level in tissues. It is not used clinically due to high toxicity. Uptake inhibitor • Tricyclic antidepressants inhibit 5-HT uptake along with that of NA. The selective serotonin reuptake inhibitors (SSRI) like fluoxetine, sertraline, etc. inhibit only 5-HT reuptake and have antidepressant antianxiety property. DRUGS AFFECTING 5-HT SYSTEM
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 18 Storage inhibitors • Reserpine blocks 5-HT uptake into storage vesicles by inhibiting VMAT-2, and causes depletion of all monoamines. Fenfluramine selectively releases 5-HT by promoting its reverse transport at serotonergic nerve endings in the brain, followed by its prolonged depletion, and has anorectic property. Degradation inhibitors • Nonselective MAO inhibitor (tranylcypromine) and selective MAO-A inhibitor (chlorgyline) increase 5-HT content by preventing its degradation.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 19 5-HT receptor agonists Azapirones like buspirone, gepirone and ipsapirone are a novel class of antianxiety drugs which do not produce sedation. They act as partial agonists of 5-HT1A receptors in the brain. sumatriptan and other triptans are selective 5-HT1D/1B agonists, constrict cerebral blood vessels and have emerged as the most effective treatment of acute migraine attacks . cisapride This prokinetic drug which increases gastrointestinal motility is a selective 5-HT4 agonist. Renzapride is still more selective for 5-HT4 receptors.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 20 1.Cyproheptadine: • H1 Receptor and 5-HT2A blocker. • Has sedation and anticholinergic effect. • Increases appetite. • Useful in carcinoid and post gastrectomy dumping syndrome. • Dry mouth, drowsiness, weight gain are some of the side effects. 2.ketanserin : • 5-HT antagonist and a1-blocker. • Has antihypertensive effect. 5-HT Antagonist
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 21 3.Ondansetron and Granisetron : • They are 5-HT3 receptor antagonist. • It control nausea and vomiting following administration of highly emetic anticancer drugs and radiotherapy. 4.Atypical Antipsychotics: • Clozapine, olanzapine, risperidone etc..,are 5-HT2 blockers used in schizophrenia. 5. Methysergide : • 5-HT2A/2C antagonist. • It was used for prophylaxis of migraine. • Long term use causes abdominal and pulmonary fibrosis.
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 22 Ergot alkaloids and their derivatives
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 23 • Cirillo C , Vanden Berghe P , Track J. Role of serotonin in gastrointestinal physiology and pathology. Edizioni Minerva Medica. 2011;36(4): 311-24. • David A. Levy. Histamine and Serotonin. Springer. 2015;32:141-161. • D.J David , A.M. Gardier. The pharmacological basis of serotonin system: Application to antidepressant response. Elsevier. 2016;42(3): 255-263. References
RIPER AUTONOMOUS NAAC & NBA (UG) SIRO- DSIR Raghavendra Institute of Pharmaceutical Education and Research - Autonomous K.R.Palli Cross, Chiyyedu, Anantapuramu, A. P- 515721 24 Thank you