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Drugs and the brain
1. The document discusses how psychotropic medications work in the brain and their potential side effects. It describes how drugs travel through different compartments in the brain, including the blood vessels, extracellular space, and between brain cells, before reaching their targets. 2. Many psychotropic drugs target neurotransmitter transporter proteins, G protein-linked receptors, ligand-gated ion channels, voltage-sensitive ion channels, or enzymes in the brain. Their effects are not selective to specific brain regions, which can contribute to side effects. 3. Common side effects discussed include tardive dyskinesia from long-term use of antipsychotics and weight gain from some atypical antipsychotics, which
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More from Adonis Sfera, MD
Drugs and the brain
- 1. Drugs and the Brain Psychotropic Medications - Effects and Adverse Effects Adonis Sfera, MD Neurovascular coupling
- 2. Why Do WeGet Side Effects From Drugs? Any time you alter you body chemistry you will have some form of side effect. The benefits of the medication will often outweigh the cost of the side effects by improving heath or allowing people to function in daily life. It is up to us to decide.
- 3. Sometimes The RisksDo Not Outweigh The Benefits
- 4. Current Psychotropic DrugsAre Not “Smart” Drugs They travel to every area of the body including the brain
- 5. Let’s Follow theDrug Brain Compartments
- 6. First Compartment: TheBrain Vessels
- 7. Extracellular Space -Between Capilaries and Cells
- 8. Second Compartment: TheSpace Between The Cells
- 9. The Firewall (BloodBrain Barrier) The blood-brain barrier (BBB) is located between the blood vessels (capilaries) and the extracellular space of the brain.
- 10. Blood Brain Barrier(BBB) Endotelialcells Astrocyte endfeet Trans-cellular passage of drugs Passage of drugs from the bloodstream to the brain is dependent on the ability of the molecules to penetrate through cell membranes.
- 11. Crossing the Membranes Penetrationof a molecule from the bloodstream to the neurons and glial cells is dependent on the compound's liposolubility.
- 12. Targets of psychotropicdrugs 30% of psychotropic drugs target transporter proteins 30% of psychotropic drugs target G protein linked receptors 20% of psychotropic drugs target ligand- gated ion channels 10% of psychotropic drugs target voltage sensitive ion channels 10% of psychotropic drugs target enzymes
- 13. Transporter Protein andG Protein (60% of psychotropic drugs) Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 14. Ligand Gated IonChannels, Voltage Sensitive Ion Channels and Enzymes (40% of psychotropic drugs) Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 15. Transporter Proteins Transporters arereceptors that bind neurotransmitters (they go in and out of the neuronal membrane 12x) Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 16. All Antidepressants (exceptMAO inhibitors) Target and Block Transporter Proteins Serotonin Transporter(SERT); Norepinephrine Transporter(NET); Dopamine Transporter(DAT)
- 17. Antidepressants Bind to Transporters 1. When Na binds to the transporter, serotonin also binds and renders the transporter ready. 2. When the antidepressant binds to the transporter it displaces serotonin and Na, blocking the transporter Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 18. G Protein LinkedReceptors G protein linked receptors (7 transmembrane regions, one intracellular and one extracellular portion)
- 19. Ligand-Gated Ion Channels(20% of Psychotropic Drugs) Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 20. N Methyl DAspartate Receptors
- 21.
- 22. VOLTAGE SENSITIVE CHANNELS Voltage -sensitive sodium channels Voltage-sensitive calcium channels
- 23. Voltage-Sensitive Sodium Channels Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 24. Some Mood Stabilizers’ BindingSites Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 25.
- 26. Alpha 2 DeltaLigands
- 27.
- 28. Enzymes Directly Targetedby Psychotropic Drugs Some Enzymes Create New Molecules. Others Destroy Existing Molecules. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 29. Enzymes as Targetsof Psychotropic Drugs Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 30. Irreversible Enzyme Inhibitor An irreversible inhibitor of an enzyme binds to the enzyme in such a way that permanently prevents a substrate from binding. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 31.
- 32. Dopamine Pathways I wishI could inhibit only the mesolimbic pathway, but I cannot because the drugs are not “smart”.
- 33. All antipsychotics (typical andatypical) are dopamine D2 blockers, but unfortunately they affect other receptors as well -adverse effects Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 34. Stahl SM Stahl’sEssential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 35. Tardive Dyskinesia (TD) Up regulation of the postsynaptic dopamine receptors. 5% of patients maintained on typical antipsychotics will develop TD in 1 year (25% in 5 years). TD in elderly can be as high 25% in the first year of treatment Kane JM in Bloom FE, Kupfer DJ, Psychopharmacology: The fourth generation of progress. Philadelphia Raven 1996 National Alliance on Mental illness. Tardive dyskinesia Available at www.nami.org/ContentGroups/Helpline1/Tardive_Dyskinesia.html
- 36. Question Which of thefollowing risk factors for the development of TD is most important? Age Gender Mood disorders Substance abuse
- 37. Question The estimated annualrate of TD in olanzapine treated patients is: 0.5% 1.0% 2.0% 3% 4%
- 39. What happens inthe Tuberoinfundibular pathway? With D2 blockade With 5HT2A blockade
- 40. Stahl SM Stahl’sEssential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 42. Stahl SM Stahl’sEssential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 43. Cardiometabolic Syndrome Weight gainis mediated by: 5HT2C H1 M3
- 44. Stahl SM Stahl’sEssential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 45. Stahl SM Stahl’sEssential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
- 47. Stahl SM Stahl’sEssential Psychopharmacology; The Prescriber’s Guide 4th ed 2011