Podcast
Questions and Answers
What is the primary amino acid from which serotonin (5-HT) is synthesized?
What is the primary amino acid from which serotonin (5-HT) is synthesized?
- Histidine
- Tyrosine
- Phenylalanine
- Tryptophan (correct)
Where is serotonin predominantly stored within the blood?
Where is serotonin predominantly stored within the blood?
- Red blood cells
- Platelets (correct)
- Plasma
- Lymphocytes
Which enzyme is primarily responsible for the degradation of serotonin?
Which enzyme is primarily responsible for the degradation of serotonin?
- Aldose reductase
- Comt
- Monoamine oxidase (MAO) (correct)
- Phenylalanine hydroxylase
In what form is serotonin excreted in urine after its metabolism?
In what form is serotonin excreted in urine after its metabolism?
Which stimulus does NOT lead to the release of serotonin from enterochromaffin cells?
Which stimulus does NOT lead to the release of serotonin from enterochromaffin cells?
Which statement about serotonin's ability to cross the blood-brain barrier (BBB) is accurate?
Which statement about serotonin's ability to cross the blood-brain barrier (BBB) is accurate?
Which process does NOT involve the action of serotonin?
Which process does NOT involve the action of serotonin?
What primarily triggers the release of serotonin from serotonergic neurons?
What primarily triggers the release of serotonin from serotonergic neurons?
Which condition is NOT associated with disturbed serotonin levels?
Which condition is NOT associated with disturbed serotonin levels?
What is one of the main actions of serotonin in the central nervous system?
What is one of the main actions of serotonin in the central nervous system?
Which receptor type is primarily implicated in the hallucinogenic effects of drugs like LSD?
Which receptor type is primarily implicated in the hallucinogenic effects of drugs like LSD?
Which of the following statements about SSRIs is TRUE?
Which of the following statements about SSRIs is TRUE?
In the context of pain transmission, serotonin has which type of effect?
In the context of pain transmission, serotonin has which type of effect?
Which of the following drug properties is associated with MDMA?
Which of the following drug properties is associated with MDMA?
Antipsychotic drugs that act on 5-HT2C receptors typically lead to what effect?
Antipsychotic drugs that act on 5-HT2C receptors typically lead to what effect?
Which neurotransmitter is often intertwined with serotonin in the regulation of mood?
Which neurotransmitter is often intertwined with serotonin in the regulation of mood?
Which drug is primarily used as an antidepressant and anxiolytic agent?
Which drug is primarily used as an antidepressant and anxiolytic agent?
What is the function of 5-HT 3 receptor antagonists like ondansetron?
What is the function of 5-HT 3 receptor antagonists like ondansetron?
Which receptor agonists are primarily effective in treating migraines?
Which receptor agonists are primarily effective in treating migraines?
Which inflammatory mediator is NOT associated with migraine pathophysiology?
Which inflammatory mediator is NOT associated with migraine pathophysiology?
What effect does a reduction in 5-HT levels have in the context of migraines?
What effect does a reduction in 5-HT levels have in the context of migraines?
Which of the following drugs would be classified as a 5-HT 2 antagonist used for migraines?
Which of the following drugs would be classified as a 5-HT 2 antagonist used for migraines?
Cortical Spreading Depression is linked to which aspect of migraines?
Cortical Spreading Depression is linked to which aspect of migraines?
Which of the following describes a complication of the trigemino-vascular system activation in migraines?
Which of the following describes a complication of the trigemino-vascular system activation in migraines?
Which agent is known to inhibit cerebral vasoconstriction during the first phase of a migraine?
Which agent is known to inhibit cerebral vasoconstriction during the first phase of a migraine?
What is the primary therapeutic aim during the second phase of a migraine?
What is the primary therapeutic aim during the second phase of a migraine?
What type of drugs are Pizotifen, Valproate, and Amitriptyline classified as?
What type of drugs are Pizotifen, Valproate, and Amitriptyline classified as?
Which class of drugs includes Propranolol, Metoprolol, and Timolol, and is considered first-line for migraine prophylaxis?
Which class of drugs includes Propranolol, Metoprolol, and Timolol, and is considered first-line for migraine prophylaxis?
Which of the following compounds is produced by the fungus Claviceps purpurea?
Which of the following compounds is produced by the fungus Claviceps purpurea?
What is the expected outcome of using NSAIDs like Naproxen and Fenoprofen at the start of a migraine attack?
What is the expected outcome of using NSAIDs like Naproxen and Fenoprofen at the start of a migraine attack?
Which of the following is NOT a type of antidepressant used for migraine prophylaxis?
Which of the following is NOT a type of antidepressant used for migraine prophylaxis?
What historical condition was caused by consuming grains infected with Claviceps purpurea?
What historical condition was caused by consuming grains infected with Claviceps purpurea?
What is one proposed mechanism of action for ergotamine in treating migraines?
What is one proposed mechanism of action for ergotamine in treating migraines?
Which condition should contraindicate the use of ergotamine?
Which condition should contraindicate the use of ergotamine?
What serious side effect is associated with methysergide?
What serious side effect is associated with methysergide?
What is a common adverse reaction of ergotamine?
What is a common adverse reaction of ergotamine?
Triptans primarily act as agonists for which receptors?
Triptans primarily act as agonists for which receptors?
Which statement is true regarding the clinical use of methysergide?
Which statement is true regarding the clinical use of methysergide?
Which neuropeptide's release is inhibited by ergotamine through 5-HT1D receptor activation?
Which neuropeptide's release is inhibited by ergotamine through 5-HT1D receptor activation?
What is a primary use for triptans in migraine treatment?
What is a primary use for triptans in migraine treatment?
What is the primary function of triptans in migraine treatment?
What is the primary function of triptans in migraine treatment?
Which of the following is a common adverse drug reaction (ADR) associated with triptans?
Which of the following is a common adverse drug reaction (ADR) associated with triptans?
What is the mechanism of action for lasmiditan?
What is the mechanism of action for lasmiditan?
Which class of medications should not be used within 24 hours of triptan administration?
Which class of medications should not be used within 24 hours of triptan administration?
What is the first line treatment for acute migraine attacks?
What is the first line treatment for acute migraine attacks?
What condition can occur as a serious side effect of combining SSRIs with triptans?
What condition can occur as a serious side effect of combining SSRIs with triptans?
Which of the following drugs is not classified as a triptan?
Which of the following drugs is not classified as a triptan?
What is a significant benefit of anti-CGRP monoclonal antibodies in migraine treatment?
What is a significant benefit of anti-CGRP monoclonal antibodies in migraine treatment?
Flashcards
What is serotonin?
What is serotonin?
Serotonin, also known as 5-hydroxytryptamine (5-HT), is a neurotransmitter and hormone. It's synthesized from the amino acid tryptophan.
Where is serotonin synthesized?
Where is serotonin synthesized?
Enterochromaffin cells in the GI tract and 5-HT neurons in the CNS (Central Nervous System) are the primary sites of serotonin synthesis.
Where is serotonin found in high concentrations?
Where is serotonin found in high concentrations?
Serotonin is found in higher concentrations in the intestinal wall, blood (specifically platelets), and certain regions of the midbrain.
What are the roles of serotonin in the body?
What are the roles of serotonin in the body?
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How is serotonin broken down?
How is serotonin broken down?
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What happens to serotonin after it's broken down?
What happens to serotonin after it's broken down?
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What cells actively take up serotonin from the blood?
What cells actively take up serotonin from the blood?
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Can serotonin cross the blood-brain barrier?
Can serotonin cross the blood-brain barrier?
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Serotonin's role in digestion
Serotonin's role in digestion
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Serotonin and smooth muscle
Serotonin and smooth muscle
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Serotonin and blood clotting
Serotonin and blood clotting
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Serotonin and pain perception
Serotonin and pain perception
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Serotonin in the brain
Serotonin in the brain
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Serotonin as a modulator
Serotonin as a modulator
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Hallucinogenic drugs and serotonin
Hallucinogenic drugs and serotonin
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Serotonin and mood disorders
Serotonin and mood disorders
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What is migraine?
What is migraine?
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What is Cortical Spreading Depression?
What is Cortical Spreading Depression?
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What is the role of the trigemino-vascular system in migraine?
What is the role of the trigemino-vascular system in migraine?
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How is vasodilation involved in migraine?
How is vasodilation involved in migraine?
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What is the influence of pain modulation in migraine?
What is the influence of pain modulation in migraine?
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What is CGRP and its role in migraine?
What is CGRP and its role in migraine?
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What is serotonin's role in migraine?
What is serotonin's role in migraine?
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How does sumatriptan work to treat migraine?
How does sumatriptan work to treat migraine?
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What are the main factors involved in migraines?
What are the main factors involved in migraines?
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Describe the first phase of a migraine.
Describe the first phase of a migraine.
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What happens during the second phase of a migraine?
What happens during the second phase of a migraine?
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What's the therapeutic aim for the first phase of a migraine, and which type of drug can help?
What's the therapeutic aim for the first phase of a migraine, and which type of drug can help?
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What's the therapeutic aim for the second phase of a migraine, and which type of drug can help?
What's the therapeutic aim for the second phase of a migraine, and which type of drug can help?
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What is the purpose of prophylactic migraine medications?
What is the purpose of prophylactic migraine medications?
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Give examples of commonly used beta-blockers for migraine prevention.
Give examples of commonly used beta-blockers for migraine prevention.
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What are some examples of older, traditional medications used to treat acute migraine symptoms?
What are some examples of older, traditional medications used to treat acute migraine symptoms?
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What are triptans? (Migraine treatment)
What are triptans? (Migraine treatment)
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What drug interaction is important to know about triptans?
What drug interaction is important to know about triptans?
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What other migraine medication should triptans NOT be used with?
What other migraine medication should triptans NOT be used with?
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What serious condition might occur with triptan use?
What serious condition might occur with triptan use?
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What is lasmiditan?
What is lasmiditan?
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What are gepants?
What are gepants?
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What are anti-CGRP mabs?
What are anti-CGRP mabs?
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What is the CGRP system?
What is the CGRP system?
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How does ergotamine work for migraines?
How does ergotamine work for migraines?
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When is ergotamine used for migraines?
When is ergotamine used for migraines?
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What is methysergide primarily used for now?
What is methysergide primarily used for now?
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How does methysergide work?
How does methysergide work?
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What are some potential side effects of ergotamine?
What are some potential side effects of ergotamine?
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What is the most concerning side effect of methysergide?
What is the most concerning side effect of methysergide?
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What are triptan medications used for?
What are triptan medications used for?
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How do triptans work to relieve migraines?
How do triptans work to relieve migraines?
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Study Notes
Pharmacology of Serotonin
- Lesson 28
- 3rd Medicine
- Professor: Vittoria Carrabs PhD
- Academic year: 2024/25
Index
- Introduction
- Functional aspects
- Clinically used drugs
- Drugs used for migraine
- Carcinoid syndrome
Introduction
- Serotonin (5-HT) is an amine synthesized from the amino acid tryptophan.
- Synthesis: Occurs in enterochromaffin cells of the gastrointestinal tract and 5-HT neurons of the central nervous system (CNS).
- Location: Highest concentration in the intestinal wall (enterochromaffin cells and myenteric plexus), blood (platelets), and localized regions of the midbrain within the CNS.
- Bloodstream transport: 5-HT released by enterochromaffin cells enters the bloodstream, taken up by platelets, and acts on vessel dilation and homeostasis.
- Function: Acts as a neurotransmitter and a local hormone in the peripheral vascular system. Its metabolism closely resembles noradrenaline.
- Degradation: Primarily through monoamine oxidase (MAO) and excreted in urine.
- Blood-Brain Barrier (BBB): 5-HT does not cross the BBB.
Functional aspects
- Main Actions: Increased gastrointestinal motility, contraction of other smooth muscles (bronchi, uterus), platelet aggregation, stimulation of nociceptive peripheral nerve endings, and stimulation/inhibition of CNS neurons. Serotonin controls appetite, sleep, mood, hallucinations, behavior, pain perception, and vomiting.
- Clinical conditions related to disturbed 5-HT: Migraine, carcinoid syndrome, pulmonary hypertension, mood disorders, and anxiety.
- Hallucinogenic Effects: Many hallucinogenic drugs (e.g., LSD) are agonists of 5-HT2A receptors. MDMA ('ecstasy') increases 5-HT release.
- Antipsychotic Drugs: Some antipsychotic drugs are antagonists of 5-HT2A receptors (as well as D2 receptors).
- Feeding and Appetite: Serotonin induces satiety. Antagonists acting on 5-HT2c receptors associated with several antipsychotic drugs increase appetite and lead to weight gain.
- Mood Regulation: Strong evidence suggests 5-HT plays a crucial role in mood regulation alongside norepinephrine.
Sensory Transmission
- 5-HT exerts an inhibitory effect on transmission in the pain pathway, both in the spinal cord and in the brain.
- There's a synergistic effect between 5-HT and analgesics such as morphine.
5-HT Receptors Location
- Detailed table listing different 5-HT receptor types, locations, and corresponding main effects. Includes agonist and antagonist drug examples.
Clinically used drugs
- 5-HT Reuptake Inhibitors: (e.g., fluoxetine) are used to treat depression and anxiety.
- 5-HT receptor agonists: (e.g., sumatriptan) are used to treat migraine.
- 5-HT receptor antagonists: (e.g., ondansetron) are used as antiemetics.
- Antipsychotic drugs: (e.g., clozapine) efficacy is at least partly related to the action on 5-HT2 receptors.
- 5-HT4 receptor agonists: (e.g., metoclopramide) can stimulate coordinated peristaltic activity and used to treat gastrointestinal disorders..
- Other 5-HT2 antagonists are used to control symptoms of carcinoid tumors.
Migraine Pathophysiology
- Chronic Neurological Pathology: Characterized by pulsatile intracranial pain, recurrence, and sensory alterations (photophobia, phonophobia).
- Origin of the term: Derived from Ancient Greek "hÄ“mikranÃa," meaning "pain on one side of the head."
- Neurological Dysfunction and Activation of Trigemino-Vascular System: Involves activation, and release of neuropeptides like CGRP causing vasodilation and neurogenic inflammation.
- Cortical Spreading Depression: Reduction in neuronal activity spreading across the cortex, linked to aura and causing vascular and inflammatory changes.
- Pain Modulation and Neurotransmitters: Pain control mechanisms are altered; reduced 5-HT levels contribute to pain pathway sensitization. Drugs targeting 5-HT1B/D/F receptors are often used.
- Genetic, Environmental and Hormonal Factors: Genetic predisposition to migraine triggers from environmental (e.g., stress, diet), and hormonal imbalances (e.g., estrogen affecting onset and duration).
- Phases of Migraine: Early phase is characterized by vasoconstriction, later by vasodilation and pain.
Drugs Used for Migraines
- Prophylactic Agents: Used in patients with migraine predisposition to prevent attacks (e.g., antihistamines, antiepileptics, antidepressants, beta-blockers, calcium channel blockers).
- Acute Attack Treatments: Analgesics (paracetamol, NSAIDs), Triptans (5-HT1B/D/F agonist e.g., sumatriptan, rizatriptan, zolmitriptan, almotriptan), ergotamine, and others like lasmiditan.
- Drugs Acting on the CGRP System: (rimegepant, ubrogepant) provide prophylactic and acute relief.
- Specific Drugs Methysergide, is a 5-HT2 receptor antagonist used for migraine prophylaxis. Ergot derivatives (ergotamine, dihydroergotamine) are effective for acute migraine treatment.
Carcinoid Syndrome
- Rare Disorder: Associated with malignant tumors of enterochromaffin cells, frequently originating in the small intestine and metastasizing to the liver.
- Chemical Mediators: Tumors release various chemical mediators, including 5-HT, substance P, and others.
- Symptoms: Flushing, abdominal cramps, diarrhea, bronchoconstriction, hypotension, dizziness. Severe cases can involve fibrotic stenosis of heart valves leading to cardiac failure.
- Diagnosis: Measured by elevated urinary excretion of 5-HT metabolite (5-HIAA).
- Treatment: Symptom control with drugs like cyproheptadine (5-HT2 antagonist).
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Description
Test your knowledge on serotonin, its synthesis, storage, and degradation in the body. This quiz covers key concepts such as the roles of serotonin in the central nervous system, its interaction with drugs, and conditions associated with serotonin levels. Perfect for students and enthusiasts of neuropharmacology.
