Antipsychotic Drugs Flashcards
typical: first generation antipsychotics (FGAs)
phenothiazenes; thioxanthenes; dibenzoxazapines; butyrophenones and diphenylbutylpiperidines; dihydroindolone
phenothiazenes
chlropromazine; thioridazine; mesoridazine; fluphenazine; trifluoperazine; perphenazine
thioxanthenes
chlorprothixene; thiothixene
dibenzoxazapines
loxapine
butyrophenones and diphenylbutylpiperidines
haloperidol and pimozide
dihydroindolone
molindone
atypical: second generation antipsychotics (SGAs)
clozapine; risperidone; olanzapine; quetiapine; aripiprazole
delusions (false beliefs); hallucinations; disorganized thoughts and speech; restlessness
positive/active symptoms of schizophrenia
flat affect; social withdrawal; loss of drive; paucity of speech; impaired process planning and memory and personal hygiene
negative/passive symptoms of schizophrenia
most anti psychotic drugs block …
dopamine receptors
schizophrenia patients have increased density of …
dopamine receptors
newer neuroleptic drugs bind preferentially to … and …
serotonin 5-HT2 and dopamine D4 receptors
typical (FGAs) do not alleviate …
negative symptoms
atypical (SGAs) alleviate …
both positive and negative symptoms
hypo-frontality hypothesis of schizophrenia: 3 components
positive symptoms; negative symptoms; impaired cognition
meso cortical pathway
negative symptoms
meso limbic pathway
positive symptoms
instead of just affecting dopamine, now the idea is to balance the 3 neurotransmitters thought to be involved … … and …
dopamine, serotonin, glutamate
clinical potency of FGAs is generally correlated with degree of …
dopamine D2 antagonism
high liability for metabolic syndrome, weight gain, blood disorders
SGAs
phenothiazine; aliphatic chain at R1; low potency; high sedating potential
chlorpromazine
phenothiazine; aliphatic chain at R1; hight potency
trifluoperazine
phenothiazine; piperidine ring at R1; low potency; higher sedating potential; hypotensive
thioridazine
phenothiazine; piperazine ring at R1; hight potency; strong EPS; least sedating of the three groups
fluphenazine
thioxanthene; N replaced by C at position 10; high potency; EPS
thiothixene
thioxanthene; N replaced by C at position 10; high potency; high EPS
chlorprothixene
buterophenone; unrelated in structure to other 2 classes; hight potency; less sedating; strong EPS
haloperidol
dihydroindolone; structurally not related to other classes; pharmacologic profile resembles that of piperazine group of phenothiazine
molindole
dibenzoxapine; resembles TCA in structure; pharmacologic and clinical profile is similar to piperazine group of phenothiazine
loxapine
diphenylbutylpiperidine; approved for Tourettes syndrome; alleviates pos. symptoms of schizophrenia; selective D2 antagonism with anti psychotic and parkinson like side effects
pimozide
4 major pathways to dopaminergic system:
mesolimbic pathway; mesocortical pathway; nigrostriatal pathway; tuberoinfundibular pathway
Dopamine D2 blockade in … and … may be responsible for antipsychotic effects of FGAs
meso limbic and meso cortical
D2 blockade by FGA in … may cause EPS
basal ganglia (nigrostriatal)
D2 super sensitivity in … may cause tardive dyskinesia
nigrostriatal
involuntary muscle contraction, torticollis; Rx: anticholinergic (bentropine)
acute dystonia
inner restlessness and constant urge to move, restless leg syndrome; Rx: BZDs, propanolol
akathisia
bradykinesia, tremor, rigidity, postural instability; Rx: levo-dopa, bromocriptine
pseudoparkinsonism
repetitive, involuntary, purposeless movements; Rx: up the dose of neuroleptic; switch to an atypical neuroleptic drug (clozapine)
tardive dyskinesia
F of FEVER of neuroleptic malignant syndrome
fever (hypothalamic dopamine blockade)
1st E of FEVER of neuroleptic malignant syndrome
encephalopathy (delirium; coma)
V of FEVER of neuroleptic malignant syndrome
vital signs (autonomic instability; tachycardia; sweating; urinary and fecal incontinence)
2nd E of FEVER of neuroleptic malignant syndrome
Enzymes (muscle breakdown; myoglobinuria w/o RBC in urine; high creatine phosphokinase
R of FEVER of neuroleptic malignant syndrome
rigidity of muscles (dopamine blockade in the basal ganglia)
SGA dibenzodiazepines
clozapine and quetiapine
SGA benzisoxazole and most frequently prescribed in US
risperidone
SGA thienobenzodiazepine
olanzapine
SGA dihydrocarbostyril
aripiprazole
2 main side effects of clozapine
weight gain and agranulocytosis
used with lithium for treatment of bipolar disorder
risperidone
high potential for abuse with effects similar to barbiturates and other hypnotics
quetiapine
first of 3rd gen antipsychotic drug; also used for bipolar and autism spectrum disorders; lower liability for weight gain
aripiprazol
most frequently prescribed FGAs
haloperidol; chlorpromazine; thioridazine
most commonly prescribed SGAs
risperidone; olanzapine; aripiprazole
