Chemical Dependence Process
Use of benzodiazepines <ul><li>Not for chronic anxiety disorders </li></ul><ul><li>Not for the elderly </li></ul><ul><li>N...
Pharmacodynamics <ul><li>GABA A  receptor interactions </li></ul><ul><ul><li>Benzodiazepine agonists, eg. diazepam </li></...
Localized pharmacodynamics <ul><li>Low-dose antianxiety effects: hippocampus and amygdala </li></ul><ul><li>Mental confusi...
Pharmacokinetics <ul><li>Study administration, absorption and distribution in textbook. </li></ul><ul><li>Metabolism is un...
Uses and side effects of benzodiazepines <ul><li>Panic attacks and phobias: alprazolam (Xanax) </li></ul><ul><li>Alcohol w...
Benzodiazepine miscellany <ul><li>Fetal effects have been reported for BDZ taken in the first trimester, but other researc...
Second generation anxiolytics <ul><li>Zolpidem (Ambien, 1993): Not a BDZ, it is a specific agonist at GABA A1  receptors. ...
Second generation anxiolytics <ul><li>Buspirone (BuSpar): A weak agonist of    5-HT 1A  receptors, so no crossing or syner...
Controversial anti-anxiety drugs <ul><li>Triazolam (Halcion) </li></ul><ul><li>Flunitrazepam (Rohypnol) </li></ul><ul><ul>...
Future directions in anxiety control <ul><li>Find partial agonists of BDZ receptors </li></ul><ul><ul><li>Abecarnil, used ...
Antiepileptic drugs <ul><li>Epileptic seizures, foci/lesions, and kindling </li></ul><ul><li>Sodium channel blocking </li>...
Other uses of antiepileptics <ul><li>Kindling may be part of a set of psychiatric disorders characterized by impulse contr...
Antiepileptic drugs <ul><li>Identify the three main groups of antiepileptic drugs. </li></ul><ul><li>In which group would ...
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Chemical Dependency Process

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Chemical Dependency Process

  1. 1. Chemical Dependence Process
  2. 2. Use of benzodiazepines <ul><li>Not for chronic anxiety disorders </li></ul><ul><li>Not for the elderly </li></ul><ul><li>Not for depression </li></ul><ul><li>For short-term treatment of stress-related anxiety: </li></ul><ul><ul><li>Acute situational grief </li></ul></ul><ul><ul><li>Acute stress reactions </li></ul></ul><ul><ul><li>Short-term anxiety-induced insomnia </li></ul></ul>
  3. 3. Pharmacodynamics <ul><li>GABA A receptor interactions </li></ul><ul><ul><li>Benzodiazepine agonists, eg. diazepam </li></ul></ul><ul><ul><li>Benzodiazepine antagonists, eg. flumazenil </li></ul></ul><ul><ul><li>Chloride ion channels and fast IPSPs </li></ul></ul><ul><li>GABA B receptor interactions </li></ul><ul><ul><li>Presynaptic for several neurotransmitters </li></ul></ul><ul><ul><li>Potassium ion channels and late IPSPs </li></ul></ul><ul><ul><li>Baclofen, a muscle relaxant and antispastic </li></ul></ul>
  4. 4. Localized pharmacodynamics <ul><li>Low-dose antianxiety effects: hippocampus and amygdala </li></ul><ul><li>Mental confusion and amnesia: hippocampus and cerebral cortex </li></ul><ul><li>Sedative-hypnotic effects: cerebral cortex </li></ul><ul><li>Different benzodiazepines have different relative effects, perhaps due to multiple subtypes of GABA A receptors. </li></ul>
  5. 5. Pharmacokinetics <ul><li>Study administration, absorption and distribution in textbook. </li></ul><ul><li>Metabolism is unusual: </li></ul><ul><ul><li>Intermediate metabolites may be psychoactive. </li></ul></ul><ul><ul><li>Intermediate metabolites may be long-lasting. </li></ul></ul><ul><ul><li>Elderly patients have difficulty metabolizing long-acting benzodiazepines, leading to profound dementia. May take 60 days to clear. </li></ul></ul>
  6. 6. Uses and side effects of benzodiazepines <ul><li>Panic attacks and phobias: alprazolam (Xanax) </li></ul><ul><li>Alcohol withdrawal and abstinence </li></ul><ul><li>Antiepileptic </li></ul><ul><li>Dose-related side effects: </li></ul><ul><ul><li>Drug-induced brain syndrome </li></ul></ul><ul><ul><li>Impaired functioning </li></ul></ul><ul><ul><li>Amnesia </li></ul></ul><ul><li>Severe interactions with alcohol </li></ul>
  7. 7. Benzodiazepine miscellany <ul><li>Fetal effects have been reported for BDZ taken in the first trimester, but other research disputes the claim. </li></ul><ul><li>If abused, BDZs are part of polydrug abuse, complicating flumazenil antagonistic effects </li></ul><ul><li>GABA A antagonists may enhance learning by facilitating cortical and hippocampal cholinergic activity </li></ul><ul><li>GABA B antagonists may enhance cognition and counter depression </li></ul>
  8. 8. Second generation anxiolytics <ul><li>Zolpidem (Ambien, 1993): Not a BDZ, it is a specific agonist at GABA A1 receptors. </li></ul><ul><ul><li>Rapid uptake and short elimination half-life make it an effective insomnia treatment </li></ul></ul><ul><ul><li>Little interference with normal sleep cycle </li></ul></ul><ul><ul><li>Safe, and high doses trigger vomiting </li></ul></ul><ul><ul><li>High doses produce problems in older people </li></ul></ul><ul><ul><li>Flumazenil antagonizes zolpidem </li></ul></ul>
  9. 9. Second generation anxiolytics <ul><li>Buspirone (BuSpar): A weak agonist of 5-HT 1A receptors, so no crossing or synergy with other CNS depressants </li></ul><ul><ul><li>Buspirone is also antidepressant </li></ul></ul><ul><ul><li>No sedation, little amnesia or confusion </li></ul></ul><ul><ul><li>Very slow development of main effect: several weeks tid. Minimal abuse, withdrawal symptoms. </li></ul></ul><ul><ul><li>Useful for GAD and anxiety in older people. </li></ul></ul><ul><ul><li>Postsynaptic inhibition of adenyl cyclase </li></ul></ul><ul><ul><li>Presynaptic inhibition of 5-HT synthesis </li></ul></ul><ul><ul><li>Remember grapefruit juice effect on buspirone </li></ul></ul>
  10. 10. Controversial anti-anxiety drugs <ul><li>Triazolam (Halcion) </li></ul><ul><li>Flunitrazepam (Rohypnol) </li></ul><ul><ul><li>Illegal in U.S.A. </li></ul></ul><ul><ul><li>Produces amnesia </li></ul></ul><ul><ul><li>Synergistic with alcohol: “Date-rape drug” </li></ul></ul><ul><ul><ul><li>Roughies, roofies, rochas </li></ul></ul></ul>
  11. 11. Future directions in anxiety control <ul><li>Find partial agonists of BDZ receptors </li></ul><ul><ul><li>Abecarnil, used for GAD </li></ul></ul><ul><li>Find drugs which act on different receptor subtypes, like Zolpidem </li></ul><ul><ul><li>Alpidem acts on GABA A1 and GABA A3 sites </li></ul></ul><ul><ul><li>Imidazenil has fewer side effects </li></ul></ul><ul><li>Nonhormonal neurosteroids (epalons) as GABA A agonists: Ganaxolone </li></ul><ul><li>Serotonin (5HT 1A ) agonists, like buspirone: gepirone, alnespirone, ipsapirone </li></ul>
  12. 12. Antiepileptic drugs <ul><li>Epileptic seizures, foci/lesions, and kindling </li></ul><ul><li>Sodium channel blocking </li></ul><ul><ul><li>carbamazepine, phenytoin (Dilantin) </li></ul></ul><ul><ul><li>lamotrigine, valproate/valproic acid </li></ul></ul><ul><li>GABA agonism </li></ul><ul><ul><li>reduce metabolism of GABA </li></ul></ul><ul><ul><li>facilitate GABA release: gabapentin </li></ul></ul><ul><ul><li>Enhance GABA action: benzodiazepines, valproic acid </li></ul></ul>
  13. 13. Other uses of antiepileptics <ul><li>Kindling may be part of a set of psychiatric disorders characterized by impulse control difficulty. </li></ul><ul><ul><li>Bipolar Disorder and mania </li></ul></ul><ul><ul><li>Conduct Disorder </li></ul></ul><ul><ul><li>Borderline Personality Disorder </li></ul></ul><ul><ul><li>Panic Disorder </li></ul></ul><ul><ul><li>Intermittent Explosive Disorder </li></ul></ul><ul><li>Antiepileptic drugs are sometimes helpful. </li></ul>
  14. 14. Antiepileptic drugs <ul><li>Identify the three main groups of antiepileptic drugs. </li></ul><ul><li>In which group would you place carbamazepine and valproic acid? </li></ul><ul><li>Construct a timeline of the drug treatment of seizure disorders, starting with bromide. </li></ul><ul><li>How do antiepileptic drugs relate to specific psychological disorders? </li></ul><ul><li>http://www.pslgroup.com/dg/2d9a6.htm </li></ul>

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