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32 Cards in this Set
- Front
- Back
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Drug examples of ssri? |
Drug examples of ssri are 1. citalopram 2.dapoxetine 3.escitalopram 4. fluoxetine 5. fluvoxamine 6. paroxetine 7. setraline 8. vortioxetine. |
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Examples of snri |
Drug examples of snri i.e serotonin and norepinephrine reuptake inhibitors are 1. desvenlafaxine 2. duloxetine 3. levomilnacipran 4. venlafaxine |
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Ssri vs Snri |
?Ssri block serotonin reuptake while snri stop the reuptake of both serotonin and norepinephrine. The reuptake process reduces the availability of neurotransmitters because the brain reabsorbs them. Therefore by blocking this process, reuptake inhibitors increase the availability of neurotransmitters |
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90% of the body’s total 5HT is found in the ____.It is synthesized and stored (in secretory granules) in the _________.It is also made in some nerves (serotonergic nerves) which make up a minor component of the myenteric plexus. |
90% of the body’s total 5HT is found in the GIT.It is synthesized and stored (in secretory granules) in the enterochromaffin cells.It is also made in some nerves (serotonergic nerves) which make up a minor component of the myenteric plexus |
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________ take up serotonin very efficiently so that there are only trace amounts of 5HT in the blood. Serotonin is taken up via a ______ carrier mediated uptake in the blood. This uptake can create concentration gradient of 1000: 1 (serotonin in platelets : blood) It is bound tightly to granules found in the platelets. It is not synthsised by the platelets. It has a very slow turnover. |
Platelets take up serotonin very efficiently so that there are only trace amounts of 5HT in the blood. Serotonin is taken up via a Na+dependent carrier mediated uptake. This uptake can create concentration gradient of 1000: 1 (serotonin in platelets : blood) It is bound tightly to granules found in the platelets. It is not synthsised by the platelets. It has a very slow turnover. |
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Serotonin is Synthesized de novo by _____ neurones in the CNS and why? |
Serotonin is Synthesized de novo by tryptaminergic neurones. This is because serotonin cannot pass through the blood brain barriers and so neurons must be able to produce it. |
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Serotonin can be found in the ____ |
GIT. Blood and CNS |
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All 5HT receptors are 7 transmembrane spanning receptors except ____?. |
All 5HT receptors are 7 transmembrane spanning receptors except 5HT3. |
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Characteristics and mech of action of 5H |
5HT1. Has 5 members (5HT1A, B, D,E, F) The receptor is G coupled. Decreases the amount of cAMP (by inhibiting adenylate cyclase). 5HT1A Activates receptor operated K+channels. Inhibits voltage gated Ca2+.. k and Ca activation/inhibition affect ion conduction in the brain |
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Characteristics and mech of action of 5H |
5HT1. Has 5 members (5HT1A, B, D,E, F) The receptor is G coupled. Decreases the amount of cAMP (by inhibiting adenylate cyclase). 5HT1A Activates receptor operated K+channels. Inhibits voltage gated Ca2+.. k and Ca activation/inhibition affect ion conduction in the brain |
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5HT1D is expressed in |
Substantia nigra and basal ganglia |
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5HT1D receptors are also found on _______ (causing vasoconstriction)---this is important because ? |
5HT1D receptors are also found on pial and coronary vessels (causing vasoconstriction)--- important because sometimes use of 5HT1D agonist (sumatriptan) for migranes may also cause coronary vasoconstriction, and in people with coronary atherosclerosis, a reduction in luminal radius will result in coronary ischemia. |
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Autoreceptors are found on ???? The presence of these inhibitory autoreceptors acts as safeguards to _______ |
Autoreceptors are found on the raphe nuclei in the brain stem. The presence of these inhibitory autoreceptors acts as safeguards to prevent overactivity of these nerves. |
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5HT1A is a _________ inhibitory autoreceptor on serotonergic nerves in the raphe nucleus of the brainstem. 5HT1D is a __________ inhibitory autoreceptor. |
5HT1A is a somatodendritic inhibitory autoreceptor on serotonergic nerves in the raphe nucleus of the brainstem. 5HT1D is a presynaptic inhibitory autoreceptor. |
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serotonin acts at a distance from its target, yes /no? |
In the brain, serotonin acts at a distance from its target(most neurotransmitters are released close to the target receptor and act locally). |
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serotonin can act as both a neurotransmitter and neuromodulator yes/no? |
Yes |
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Location of 5HT2A? |
Found everywhere in the brain. Found on platelets(plays a role in platelet aggregation) Found on smooth muscle cells (contraction). Also G coupled. |
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5HT2B location |
Found in the stomach fundus(contraction of the smooth muscle found there). |
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5HT2C Location |
Found in the choroid plexus(unknown function). |
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5HT2C Location |
Found in the choroid plexus(unknown function). |
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5HT3 location |
It is a 4 transmembrane spanning ligand gated ion channel. It gates the ions Na+ and K+ Found on peripheral sensory (afferent) nerves. Located on vagal and splanchnic afferents Also in the nucleus tractus solitaries Also found in the area postrema. Are neuroexcitatory. |
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Regions that play an I.oirtant role in emesis? |
Located on vagal and splanchnic afferents Also in the nucleus tractus solitaries Also found in the area postrema. |
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5HT4 mech of action and location. |
Increases cAMP and Neuroexcitatory. Locations: Found in the hippocampus Found in the gut Myenteric plexus Smooth muscle cells Secretory cells (promote secretion). |
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_______ facilitate the peristaltic reflex. |
Myenteric plexus Smooth muscle cells Secretory cells (promote secretion). |
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_______ facilitate the peristaltic reflex. |
Myenteric plexus Smooth muscle cells Secretory cells (promote secretion). |
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5HT7, 5HT6, 5HT5 |
5HT6 and 5HT7- increases cAMP. T7 is also found in the GIT |
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Possible disease found in 5HT |
Carcinoid syndrome Overproduction of serotonin as a result of a tumor of enterochromaffin cells. Results in hypotension/cardiovascular system disorders. Flushing(due to vasodilatation) Bronchospasm Diarrhea. |
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Treatment of carcinoid syndrome |
Fenclanine. A serotonin synthesis inhibitor.Tends to be the preferred treatment. Cyproheptadine |
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Serotonin is also involved in the following : |
Migraine Emesis(vomiting) Anxiety Psychosis/Schizophrenia Appetite Depression Obsessive compulsive disorders. |
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What is serotonin relationship with platelets |
Serotonin is not synthesized by platelets. It is taken up by platelets and stored in high concentration in dense core granules. |
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Mention factors that promote platelet aggregation |
The injured endothelium triggers the release of serotonin from platelets(along with ADP, thrombin, thromboxaneA2). |
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What is serotonins effect on 5HT2A receptors? |
On other platelets enhances platelet aggregation. On vascular smooth muscle causes direct vasoconstriction. |
