Term
What is the synthetic and degradative pathway of Gaba and its degradation? |
|
Definition
Alpha-KetoGlutarate->(GABA-T)->Glutamic Acid->(GAD)->GABA->(GABA-T)->Succinic Semi-Aldehyde->(SSADH)->Succinic Acid |
|
|
Term
What are the reuptake pathways for Gaba after its release into the synapse |
|
Definition
GABA transporter back into GABA neuron or
GABA transoport into Glial Cell-> (Transamination)-> Glutamine-> transport to presynaptic neuron-> conversion to glutamate->(GAD)-> GABA |
|
|
Term
Why are benodiazepines safer than barbituates? |
|
Definition
Benzos show plateauing of their dose response curves |
|
|
Term
What is the mechanism of benzodiazepines and how does it differ from barbituates? |
|
Definition
Bind GABAa receptors at BZ1 and BZ2 sites causing incresed sensitivity of neurons to GABA generating higher chloride conductance and hyperpolarizing postsynaptic cells
Barbituates increase the duration of GABA chloride channel opening and cause opening in high doses |
|
|
Term
What are the effects of each of the benzodiazepine receptor sites? |
|
Definition
BZ1: Sedative, Anti-convulsive
BZ2: Anti-Anxiety, Anti-cognitive |
|
|
Term
What is the mechanism, use, and adverse effects of flumazenil |
|
Definition
Benzodiazepine antagonist used in benzo toxicity
Adverse: Seizures |
|
|
Term
What is the BZ1 selective agonist and what is it used for? |
|
Definition
Zolpidem
Used as a Hyponotic |
|
|
Term
What benzos shouold be used if the patient is very old or has hepatic damage |
|
Definition
|
|
Term
which benzos are dealkylated or hydroxylated followed by conjugation |
|
Definition
Diazepam Flurazepam Chlordiazepoxide |
|
|
Term
What rxn inactivates benzos |
|
Definition
|
|
Term
What are the adverse effects of benzodiazepines |
|
Definition
Sedation
Tolerance: Rapid in sedative qualities, months in anti-anxiety effects
CV Failure and Respiratory depression:With Alcohol or Barbituates
Dependence: Rebound Anxiety and Insomnia, Seizures with long prolonged dosing
Toxicity: Impaired speech, Uncoordination, Stupor, Respiratory depression |
|
|
Term
What benzos usually exhibit short term withdrawal symptoms? |
|
Definition
Short Acting(lorazepam, oxazepam) |
|
|
Term
What are the main uses of benzos? |
|
Definition
Hypnotic
Sugical Anesthesia Adjunct
Anticonvulsants
Muscle Relaxants
Replacement for drug withdrawal |
|
|
Term
What is the mechanism, advantages and disadvantages of buspirone? |
|
Definition
5HT1A Agonist
D2 Antagonist
Advantages: Nonsedating,
Won't potentiate alcohol
Disadvantages: High Protein Binding
Wait time til Effect
Patients don't like if previously treated with Benzos |
|
|
Term
|
Definition
Clomipramine
NSRI's
Benzos |
|
|
Term
How are benzos typically used to treat anxiety clincally? |
|
Definition
Used short-term for acute exacerbations |
|
|
Term
What is the typically pharmacological management panic disorder |
|
Definition
Acutely: High dose Alprazolam
Long term use Fluoxetine |
|
|