NR 546 Week 3 Assignment; Antipsychotic Medications
Table
Antipsychotic
Medications
Kristin Reddy NR 546 September
2022
Drug name Indication (Bold = FDA approved) Half- Notable side effects (associate to pathway or NT)
Target symptoms: state if positive or
life
negative effect Potency (if noted. receptor
(T1/2),
occupancy if noted) Neurotransmitter(s)
metabolis
affected
m (CYP
450
enzyme)
Typical antipsychotics (conventional)
,Haloperidol Indication: Half Life ▪ Neuroleptic-induced deficit syndrome –
▪ Manifestations of psychotic Oral: Blocking of dopamine two receptors
excessively in the
disorders (oral, immediate-release Approximat
mesocortical and mesolimbic dopamine
injection) ely 12-38
▪ Tics and vocal utterances in Tourette’s pathways, specially at high doses, it can
hours
syndrome (oral,immediate-release injection) cause worsening of negative and cognitive
▪ Second-line treatment of severe behavior Decanoate:
symptoms
problems in children of combative, explosive ▪ Akathisia - Acute blockade of dopamine 2
approximat
receptors in the striatum
hyperexcitability (oral) ely 3 weeks
▪ Drug-induced parkinsonism - Acute
▪ Second-line short-term treatment of
blockade of dopamine 2 receptors in the
hyperactive children (oral)
striatum
▪ Treatment of schizophrenic patients who Metaboliz ▪ Tardive dyskinesia, tardive dystonia –
require prolonged parenteral antipsychotic ed by Chronic and acute blockade of dopamine 2
therapy (depotintramuscular decanoate) CYP450 - receptors in the striatum
▪ Bipolar disorder ▪ Risk of potentially irreversible
2D6, 3A4,
▪ Behavioral disturbances in dementias
▪ Delirium (with 3A5 involuntary dyskinetic movements
lorazepam) Target symptoms: may increase with cumulative dose
▪ Positive symptoms of psychosis and treatment duration
▪ Violent or aggressive ▪ Galactorrhea, amenorrhea – Blocking of
behaviorPotency: High dopamine 2 receptors in the pituitary can
Neurotransmitter(s) affected:
cause elevations in
▪ Blocks dopamine 2 receptors, reducing prolactin
positive symptoms of psychosis and ▪ Dizziness, sedation – Blocking of alpha 1
possibly combative, explosive, and adrenergic receptors
hyperactive behaviors ▪ Dry mouth, constipation, urinary
▪ Blocks dopamine 2 receptors in the retention, blurred vision, decreased
nigrostriatal pathway, improving tics and sweating – Blockade of muscarinic
other symptoms in cholinergic receptors
Tourette’s syndrome ▪ Hypotension, tachycardia, hypertension –
Blocking of alpha 1 adrenergic receptors
▪ Weight gain - Mechanism of weight gain
, and any possible increased incidence of
diabetes or dyslipidemia with
unconventional antipsychotics is
currently unknown
Thioridazine Indication: Half Life ▪ Neuroleptic-induced deficit syndrome –
Blocking of
, ▪ Schizophrenic patients who fail to 21–24 hours dopamine 2 receptors excessively in the
respond to treatment with other mesocortical and mesolimbic dopamine
antipsychotic drugs pathways, especially at high doses, it can
Target symptoms: Metabolize cause worsening of negative and cognitive
▪ Positive symptoms of psychosis in patients
d Primarily symptoms
who fail to respond to treatment with other
by CYP450 ▪ Akathisia - Acute blockade of dopamine 2
antipsychotics
- 2D6 receptors in the striatum
▪ Motor and autonomic hyperactivity in patients
▪ Priapism – Blocking of alpha 1 adrenergic
who fail to respond to treatment with other receptors
antipsychotics ▪ Drug-induced parkinsonism - Acute
Potency: Low blockade of dopamine 2 receptors in the
Neurotransmitter(s) striatum
affected: ▪ Tardive dyskinesia - Chronic blockade of
▪ Blocks dopamine 2 receptors, reducing dopamine 2 receptors in the striatum
positive symptoms of psychosis ▪ Risk of potentially irreversible
involuntary dyskinetic movements
may increase with cumulative dose
and treatment duration
▪ Galactorrhea, amenorrhea - Blocking of
dopamine 2 receptors in the pituitary
▪ Pigmentary retinopathy at high doses –
may be due to blockade of retinal D2/D4
receptors
▪ Dizziness, sedation - Antihistaminic
actions, blocking of alpha 1
adrenergic receptors
▪ Dry mouth, constipation, blurred vision,
decreased sweating, paralytic ileus –
Blocking of muscarinic cholinergic receptors
▪ Sexual dysfunction - Blockade of
dopamine D2 receptors in the
Table
Antipsychotic
Medications
Kristin Reddy NR 546 September
2022
Drug name Indication (Bold = FDA approved) Half- Notable side effects (associate to pathway or NT)
Target symptoms: state if positive or
life
negative effect Potency (if noted. receptor
(T1/2),
occupancy if noted) Neurotransmitter(s)
metabolis
affected
m (CYP
450
enzyme)
Typical antipsychotics (conventional)
,Haloperidol Indication: Half Life ▪ Neuroleptic-induced deficit syndrome –
▪ Manifestations of psychotic Oral: Blocking of dopamine two receptors
excessively in the
disorders (oral, immediate-release Approximat
mesocortical and mesolimbic dopamine
injection) ely 12-38
▪ Tics and vocal utterances in Tourette’s pathways, specially at high doses, it can
hours
syndrome (oral,immediate-release injection) cause worsening of negative and cognitive
▪ Second-line treatment of severe behavior Decanoate:
symptoms
problems in children of combative, explosive ▪ Akathisia - Acute blockade of dopamine 2
approximat
receptors in the striatum
hyperexcitability (oral) ely 3 weeks
▪ Drug-induced parkinsonism - Acute
▪ Second-line short-term treatment of
blockade of dopamine 2 receptors in the
hyperactive children (oral)
striatum
▪ Treatment of schizophrenic patients who Metaboliz ▪ Tardive dyskinesia, tardive dystonia –
require prolonged parenteral antipsychotic ed by Chronic and acute blockade of dopamine 2
therapy (depotintramuscular decanoate) CYP450 - receptors in the striatum
▪ Bipolar disorder ▪ Risk of potentially irreversible
2D6, 3A4,
▪ Behavioral disturbances in dementias
▪ Delirium (with 3A5 involuntary dyskinetic movements
lorazepam) Target symptoms: may increase with cumulative dose
▪ Positive symptoms of psychosis and treatment duration
▪ Violent or aggressive ▪ Galactorrhea, amenorrhea – Blocking of
behaviorPotency: High dopamine 2 receptors in the pituitary can
Neurotransmitter(s) affected:
cause elevations in
▪ Blocks dopamine 2 receptors, reducing prolactin
positive symptoms of psychosis and ▪ Dizziness, sedation – Blocking of alpha 1
possibly combative, explosive, and adrenergic receptors
hyperactive behaviors ▪ Dry mouth, constipation, urinary
▪ Blocks dopamine 2 receptors in the retention, blurred vision, decreased
nigrostriatal pathway, improving tics and sweating – Blockade of muscarinic
other symptoms in cholinergic receptors
Tourette’s syndrome ▪ Hypotension, tachycardia, hypertension –
Blocking of alpha 1 adrenergic receptors
▪ Weight gain - Mechanism of weight gain
, and any possible increased incidence of
diabetes or dyslipidemia with
unconventional antipsychotics is
currently unknown
Thioridazine Indication: Half Life ▪ Neuroleptic-induced deficit syndrome –
Blocking of
, ▪ Schizophrenic patients who fail to 21–24 hours dopamine 2 receptors excessively in the
respond to treatment with other mesocortical and mesolimbic dopamine
antipsychotic drugs pathways, especially at high doses, it can
Target symptoms: Metabolize cause worsening of negative and cognitive
▪ Positive symptoms of psychosis in patients
d Primarily symptoms
who fail to respond to treatment with other
by CYP450 ▪ Akathisia - Acute blockade of dopamine 2
antipsychotics
- 2D6 receptors in the striatum
▪ Motor and autonomic hyperactivity in patients
▪ Priapism – Blocking of alpha 1 adrenergic
who fail to respond to treatment with other receptors
antipsychotics ▪ Drug-induced parkinsonism - Acute
Potency: Low blockade of dopamine 2 receptors in the
Neurotransmitter(s) striatum
affected: ▪ Tardive dyskinesia - Chronic blockade of
▪ Blocks dopamine 2 receptors, reducing dopamine 2 receptors in the striatum
positive symptoms of psychosis ▪ Risk of potentially irreversible
involuntary dyskinetic movements
may increase with cumulative dose
and treatment duration
▪ Galactorrhea, amenorrhea - Blocking of
dopamine 2 receptors in the pituitary
▪ Pigmentary retinopathy at high doses –
may be due to blockade of retinal D2/D4
receptors
▪ Dizziness, sedation - Antihistaminic
actions, blocking of alpha 1
adrenergic receptors
▪ Dry mouth, constipation, blurred vision,
decreased sweating, paralytic ileus –
Blocking of muscarinic cholinergic receptors
▪ Sexual dysfunction - Blockade of
dopamine D2 receptors in the
