Antipsychotic agents Flashcards
Chlorpromazine Fluphenazine Haloperidol (Haldol) Loxapine Perphenazine Primozide (Orap) Prochlorperazine Thioridazine Thiothixene (Navane) Trifluoperazine
Typical Antipsychotic agents (conventional)
first generation
typical
newer, novel antipsychotics
atypical
antipsychotics work by blocking post synaptic dopamine receptors in the basal ganglia, hypothalamus, limbic system, brainstem and medulla.
-varying affinity for cholingergic alpha, -adrenergic, and histaminic receptors
typical antipsychotics
possible related to inhibition of dopamine mediated transmission of neural impulses at the synapses.
Antipsychotic effects
aripiprazole (Abilify) asenapine (Saphris) clozapine (Clozaril) iloperidone (Fanapt) lurasidone (Latuda) olanzapine (Zyprexa) paliperidone (Invega) quetianpine (Seroquel) risperidone (Risperdal) ziprasidone (Geodon)
Atypical antipsychotics
are weaker dopamine receptors antagonists than the conventional antipsychotics, more potent antagonists of the serotonin (5-hydroxytryptamine) type 2A (5HT2A) receptors
-They also exhibit antagonisms for cholinergic, histaminic and adrenergic receptors
Atypicals
Blockage of the dopamine receptors is thought to be responsible for controlling positive symptoms of schizophrenia.
-also results in EPS side effects and prolactin elevation.
Antipsychotics effects
muscle weakness
akinesia
cont. restlessness and fidgeting
Akathisia
involuntary muscular movements (spasms) of face, arms, legs, and neck
-men and in people younger than 25 years
Dystonia
uncontrolled rolling back of the eyes
Oculogyric crisis
bizarre facial & tongue movements, stiff neck and difficulty swallowing
-more common with typical antipsychotics
Tardive dyskinesia
more common with typical than atypical antipsychotics
*rare, but fatal
routine temp and check for Parkinsonian symptoms. Muscle rigidity, high fever, tachycardia, tachypnea, fluc of bp, diaphoresis, rapid deteriation of mental status
stupor, coma
Neuroleptic Malignant syndrome (NMS)
become 1st line of therapy, and treat both positive and negative symptoms of schizophrenia. They have a more favorable side effect profile than the conventional (typical) antipsychotics
Atypical antipsychotics
most meds have their effects @ the neuronal synapse, producing changes in neurotransmitter release and the receptors to which they bind.
How psychotics work
most antidepressants work by blocking the reuptake of neurotransmitters, specifically serotonin and norepinehrine
How most antidepressants work
the process of neurotransmitters inactivation by which the neurotransmitters is reabsorbed into the presynaptic neuron from which it had been released.
-blocking the reuptake process allows more of the neurotransmitter to be available for neuronal transmission.
Reuptake
inhibit reuptake of serotonin (5-HT)
-reduces depression, controls anxiety, controls obsessions.
side effects: nausea, agitation, headache, sexual dysfunction
SSRI’s
inhibit reuptake of serotonin (5-HT), inhibits of norepinephrine (NE), blocks NE receptor blocks ACh receptor, blocks histamine (H1) receptor
-reduces depression, relief of severe pain, prevent panic attacks
side effects: sexual dysfunction, sedation, weight gain, dry mouth, constipation, blurred vision, urinary retention, postural hypotension, and tachycardia
Tricyclic Antidepressants
Increase NE & 5Ht by inhibiting the enzyme that degrades them MAO-A
Reduces depression, controls anxiety
side effects: sedation, dizziness, sex dysfunction, hypertensive crisis (interaction with tyramine)
MAOI’s
inhibit reuptake of NE and dopamine D
reduces depression, aids in smoking cessation, decreases symptoms of ADHD
side effects: Insomnia, dry mouth, tremor seizures
Bupropion
Benzodiazepines
binds to BZ receptor sites on the GABA receptor complex; increases receptor affinity for GABA
Relief of anxiety sedation,
side effects: Dependence (with long term use)
confusion, memory impairment, motor incoordiation
Antianxiety meds
Aripiprazole=Abilify
Dopamine-serotonin system stabilizer DSS
partial agonist at Dopamine receptor & serotonin (5-HT 1A)
Acts as antagonist at Dopamine receptor in high dopamine activity.
Acts as agonist in low dopamine activity
5 HT 2A antagonist.
Unwanted side effects (EPS, weight gain, prolactin elevation, gulcose & lipid abnormalities, cardiac abnormalities, prolongation of QT interval) are not a problem with this antipsychotic! Only time will prove its efficacy. Insomnia, nausea & vomiting
3rd generation Antipsychotics (DSS)
Cholorpromazine
Thorazine; first tricyclic antihistamine
Butyrophenone
Haldol; typical antipsychotic dopamine receptor antagonists
Blocking 5-HT serotonin receptors decreases negative symptoms and EPS
- Serotonin inhibits dopamine release
- Positive symptoms assoc. with hyperdopaminergic condition in limbic lobe-more
- D2 receptors here, so D2 blocking prevails
5-HT seratonin receptors
Aripiprazole extended release (Abilify) Fluphenazine decanoate (fluphenazine-LAI) 4 weeks Haloperidol decanoate (haloperidol-LAI) 4 weeks Olanzapine pamoate (Zyprexa Relprevv) 3 weeks Paliperidone palmitate (Invega Sustenna) 4 weeks Risperidone microspheres (Risperdo Consta) 2 weeks
Deck Shot; not compliant with oral meds
Sometimes need an oral dose in between to hold blood levels stable. Also may require more than one loading dose.
Long Acting Medication
