Front | Back |
Agonists:
|
Produce effects similar to the neurotransmitter.
Direct agonists mimic the neurotransmitter at the receptor site.
Indirect agonists attach to a binding site on a reception (other than the one used by the neurotransmitter) and facilitate the action of the neurotransmitter.
|
Inverse Agonists:
|
Produce an effect opposite of a neurotransmitter or agonist.
|
Partial Agonists:
|
Produce effects similar but less than a neurotransmitter or agonist.
|
Antagonists:
|
Produce no activity in the cell.
Reduce or block neurotransmitter or agonist.
|
Drugs and Older adults:
|
Changes in absorption distribution, metabolism and excretion.
Start low and go slow.
|
Drugs and Race/Ethnicity:
|
Asians, and to a lesser degree
AA, slower/poorer metabolizers of drugs. Start low and go slow.
|
Traditional/Conventional Antipsychotics are best at:
|
Useful to alleviate positive symptoms, most often for schizophrenia, acute mania, hallucinations in MDD and psychosis.
Alleviate positive symptoms by not effective for negative symptoms.
|
Traditional/conventional antipsychotics side effects:
|
Extrapyramidial including tardive dyskensia
neuroleptic malignant syndrome
Anticholinergic Effects
|
neuroleptic malignant syndrome
|
(rapid onset muscle rigidity, autonomic instability, delirium. Stop drug immediately),
|
Anticholinergic Effects
|
(blocks acetylcholine) including dry mouth, blurred vision, urinary retention/constipation, tachycardia.
Develop early and tolerance in a few weeks.
|
Tardive Dyskinesia:
|
Worst of extrapyramidial side effects.
Similar to Huntington’s disease involuntary rhythmic movement of jaw, lips, extremities.
|
Is tardive dyskenesia reversable?
|
Typically irreversible, may be alleviated with benzo or GABA agonist.
|
Atypical/Novel Antipsychotics:
|
Address both positive and negative symptoms, often work when traditionals have failed.
|
Atypical/Novel Antipsychotics advantage and disadvantage:
|
Address both positive and negative symptoms, often work when traditionals have failed.
Disadvantage is may have slower onset than traditionals.
|
Atypical/Novel Antipsychotics side effects:
|
Anticholinergic effects, lowered seizure threshold, sedation.
Extrapyramidial side effects are much less common and less likely to produce tardive dyskinesia.
Can produce aranulocytosis/decrease in white blood cells so need blood monitoring.
May cause neuroleptic malignant syndrome.
|