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Drugs and the                         Brain                         Psychotropic Medications -                         Eff...
Why Do We Get Side Effects FromDrugs?             Any time you alter you body chemistry             you will have some for...
Sometimes The Risks Do NotOutweigh The Benefits
Current Psychotropic Drugs Are Not“Smart” Drugs   They travel to every area of the body including the    brain
Let’s Follow the DrugBrain Compartments
First Compartment: The Brain Vessels
Extracellular Space - BetweenCapilaries and Cells
Second Compartment: The SpaceBetween The Cells
The Firewall (Blood Brain Barrier) The    blood-brain barrier (BBB) is located between the blood vessels (capilaries) and...
Blood Brain Barrier (BBB) Endotelialcells Astrocyte endfeet                        Trans-cellular                       ...
Crossing the MembranesPenetration of a molecule from the bloodstream to the neuronsand glial cells is dependent on the com...
Targets of psychotropic drugs   30% of psychotropic drugs target transporter    proteins   30% of psychotropic drugs tar...
Transporter Protein and G Protein(60% of psychotropic drugs)Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’...
Ligand Gated Ion Channels, Voltage Sensitive        Ion Channels and Enzymes        (40% of psychotropic drugs)Stahl SM St...
Transporter ProteinsTransporters are receptors that bind neurotransmitters (they go inand out of the neuronal membrane 12x...
All Antidepressants (except MAO inhibitors) Target and Block Transporter ProteinsSerotonin Transporter(SERT); Norepinephri...
Antidepressants Bind to        Transporters1. When Na binds to thetransporter, serotonin alsobinds and renders thetranspor...
G Protein Linked ReceptorsG protein linked receptors (7 transmembrane regions, one intracellularand one extracellular port...
Ligand-Gated Ion Channels (20%      of Psychotropic Drugs)Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s ...
N Methyl D Aspartate Receptors
GABA Receptors
VOLTAGE SENSITIVE CHANNELS Voltage -sensitive sodium channels Voltage-sensitive calcium channels
Voltage-Sensitive Sodium          ChannelsStahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Some Mood Stabilizers’Binding Sites Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Voltage-Sensitive CalciumChannels
Alpha 2 Delta Ligands
Antihypertensive Calcium ChannelBlockers
Enzymes Directly Targeted by          Psychotropic Drugs   Some Enzymes Create New   Molecules.   Others Destroy Existing ...
Enzymes as Targets of Psychotropic   DrugsStahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Irreversible Enzyme Inhibitor                                 An irreversible inhibitor of an enzyme binds                ...
Reversible Enzyme Inhibitor
Dopamine PathwaysI wish I could inhibit only the mesolimbic pathway, but I cannotbecause the drugs are not “smart”.
All antipsychotics (typicaland atypical) aredopamine D2 blockers, butunfortunately they affectother receptors as well-adve...
Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Tardive Dyskinesia (TD)   Up regulation of the postsynaptic dopamine    receptors.   5% of patients maintained on typica...
QuestionWhich of the following risk factors for thedevelopment of TD is most important? Age Gender Mood disorders Subs...
QuestionThe estimated annual rate of TD inolanzapine treated patients is: 0.5% 1.0% 2.0% 3% 4%
What happens in theTuberoinfundibular pathway? With   D2 blockade With   5HT2A blockade
Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Cardiometabolic SyndromeWeight gain is mediated by: 5HT2C H1 M3
Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
Drugs and the brain
Drugs and the brain
Drugs and the brain
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Drugs and the brain

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Drugs and the brain

  1. Drugs and the Brain Psychotropic Medications - Effects and Adverse Effects Adonis Sfera, MDNeurovascular coupling
  2. Why Do We Get Side Effects FromDrugs? 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 Risks Do NotOutweigh The Benefits
  4. Current Psychotropic Drugs Are Not“Smart” Drugs They travel to every area of the body including the brain
  5. Let’s Follow the DrugBrain Compartments
  6. First Compartment: The Brain Vessels
  7. Extracellular Space - BetweenCapilaries and Cells
  8. Second Compartment: The SpaceBetween The Cells
  9. The Firewall (Blood Brain 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 MembranesPenetration of a molecule from the bloodstream to the neuronsand glial cells is dependent on the compounds liposolubility.
  12. Targets of psychotropic drugs 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 and G Protein(60% of psychotropic drugs)Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  14. Ligand Gated Ion Channels, 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 ProteinsTransporters are receptors that bind neurotransmitters (they go inand out of the neuronal membrane 12x) Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  16. All Antidepressants (except MAO inhibitors) Target and Block Transporter ProteinsSerotonin Transporter(SERT); Norepinephrine Transporter(NET);Dopamine Transporter(DAT)
  17. Antidepressants Bind to Transporters1. When Na binds to thetransporter, serotonin alsobinds and renders thetransporter ready.2. When the antidepressantbinds to the transporter itdisplaces serotonin and Na,blocking the transporterStahl SM Stahl’s Essential Psychopharmacology;The Prescriber’s Guide 4th ed 2011
  18. G Protein Linked ReceptorsG protein linked receptors (7 transmembrane regions, one intracellularand 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 D Aspartate Receptors
  21. GABA Receptors
  22. VOLTAGE SENSITIVE CHANNELS Voltage -sensitive sodium channels Voltage-sensitive calcium channels
  23. Voltage-Sensitive Sodium ChannelsStahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  24. Some Mood Stabilizers’Binding Sites Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  25. Voltage-Sensitive CalciumChannels
  26. Alpha 2 Delta Ligands
  27. Antihypertensive Calcium ChannelBlockers
  28. Enzymes Directly Targeted by Psychotropic Drugs Some Enzymes Create New Molecules. Others Destroy Existing Molecules.Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’sGuide 4th ed 2011
  29. Enzymes as Targets of Psychotropic DrugsStahl 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. Reversible Enzyme Inhibitor
  32. Dopamine PathwaysI wish I could inhibit only the mesolimbic pathway, but I cannotbecause the drugs are not “smart”.
  33. All antipsychotics (typicaland atypical) aredopamine D2 blockers, butunfortunately they affectother receptors as well-adverse effectsStahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  34. Stahl SM Stahl’s Essential 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 treatmentKane JM in Bloom FE, Kupfer DJ, Psychopharmacology: The fourth generation ofprogress. Philadelphia Raven 1996National Alliance on Mental illness. Tardive dyskinesia Available atwww.nami.org/ContentGroups/Helpline1/Tardive_Dyskinesia.html
  36. QuestionWhich of the following risk factors for thedevelopment of TD is most important? Age Gender Mood disorders Substance abuse
  37. QuestionThe estimated annual rate of TD inolanzapine treated patients is: 0.5% 1.0% 2.0% 3% 4%
  38. What happens in theTuberoinfundibular pathway? With D2 blockade With 5HT2A blockade
  39. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  40. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  41. Cardiometabolic SyndromeWeight gain is mediated by: 5HT2C H1 M3
  42. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  43. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011
  44. Stahl SM Stahl’s Essential Psychopharmacology; The Prescriber’s Guide 4th ed 2011

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