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Antipsychotics Flashcards

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1
Q

Striatal interneuron

A

Ach Containing

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2
Q

Nigrostraital

A

A9 Dopamine neuron Substantia nagra pars compacta- Corpus striatum
DA release in straitum is essental for normal extrapyramidal motor function

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3
Q

Striatonigral

A

GABAnergic Neuron VTA-Corpus Striatum

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4
Q

Mesolimbic

A

A10 DA neuron VTA- Nucleus accumbens

DA release is important for normal affect, orderly thinking, drive states, pleasure/reward

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5
Q

DA receptor subtypes

A

D1 (D1,D5)

D2 (D2,D3,D4) Exist in 2 isoforms D2 long, D2 short

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6
Q

D1 receptors

A

Stimulate adenylate cyclase and increase cAMP
Affinity for phenothiazines > butyrophenones
small intracellular loop, large carboxy tail

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7
Q

D2 receptors

A

Not associated w/stimulation of Adenyate cyclase and may inhibit it
Affinity for butyrophenones > phenothiazines
Large intracellular loop, small carboxy tail

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8
Q

DA receptors are…

A

GPCRs

7 transmembrane spanning receptors

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9
Q

D1 couple

A

Gs, Golf

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10
Q

D2 couple

A

Gi/o

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11
Q

Symptoms and diagnosis of psychosis

A

Charecterized by impared behavior. Inability to think coherrently and comprehend reality.
+ve symptoms- “added” hallucinations, delusions, paranoia etc.
-ve symptoms- withdrawl, depersonalization
cognative- impared attention, deficits in learning and memory.

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12
Q

Organic Psychosis

A

Known cause. Can be due to:

Impared cerebral tissue function, intellecutual decline, drug abuse, tramua etc.

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13
Q

Idiopathic psychosis

A

Cause is not known. May have a genetic component (twin studies)
Schizophrenia

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14
Q

Dopamine theory

A

Upregulation of dopamine, excessive DA transmission- in limbric striatum and cortical areas innervted by A10 causes Schizophrenia.
* Terminal regions of A10 Dopamine pathways- Limbic cortex, and nucleus accumbens

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15
Q

Evidence for DA theory

A

Drugs blocking D2 like receptors reduce psychotic symptoms (+ve)
Drugs increasing synaptic DA cause psychosis (amphetamines, LDOPA)

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16
Q

Problems with DA theory

A

Other transmitter systems (seratonin, glutamate) and brain areas (Cortex, thalamus) are also likely involved
This theory alone is not enough to explain schitzophrenia. Multiple genes/systems are likely involved
Upregulation of dopa- negative symptoms??!

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17
Q

Pharmacological basis of therapuetics in Schizophrenia

A

Reduce DA transmission in terminal regions (A10 mesolimbic)
D2 blockers
Therapeutic problems arise as its difficult to block DA receptors only in limbic terminal areas (leading to SAs)

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18
Q

Classes of Antipyschotics

A

Typical- older generation- blockade D2 w/greater affinity than 5-HT2A
Atypical- newer generation- blockade 5-HT2A> D2 receptors. 2nd & 3rd Generation

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19
Q

Typical antipsychotic classes

A

Phenothiazine
Thioxanthene
Butyrophenone

Miscellaneous

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20
Q

Chlorpromazine

A

Phenothiazine

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21
Q

Thioridazine

A

Phenothiazine

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22
Q

Trifluoperazine

A

Phenothiazine

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23
Q

Perphenazine

A

Phenothiazine

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24
Q

Fluphenazine

A

Phenothiazine

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25
Haloperidol
Butyrophenone
26
Pimozide
Misc.
27
Loxapine
A-typical | dibenzoxazepine
28
Clozapine
``` dibenzodiazepine A-typical No extrapyramidal SAs May suppress tardive dyskinesia Effective in drug resistant cases- reduces +/- symptoms Blocks many receptors besides DA- muscarinic, 5-HT2A, a1, h1. D4 blockade as well D4=a1>5HT2A>D2=D1 ```
29
Risperidone
A-typical | Low incidence of extrapyramidal and tardive dyskinesia. D2 5HT receptor blocking
30
Quetiapine
A-typical H1>a1>D2>5HT2A low incidence of extrapyramidals +/- symptoms
31
Olanzapine
``` A-typical 5HT2A>H1>D4>D2 +/- Symptoms Low incidence of extrapyramidal Weight gains! ```
32
Ziprasidone
A-typical Acute treatment for agitated or violent encounters Serious cardiac arrhythmias
33
Aripiprazole
A-typical- 3rd generation Partial agonist D2=5HT2A>D4>A1=H1>>D1 DA stabilizer since its a partial. No extrapyrmaidals
34
Receptors
All have similar binding pockets, all ligands are monoamine NTs
35
CNS SA's
Sedation- tolerance Antianxiety- +ve! Suppression of spontaneous movement, lack of initative, disinerest, lack of pleasure
36
Endocrine SA's
Increased Prolactin- causing breast enlargement in males. Increased female and decreased male libido. Inc appetite, weight gain. More prominent in typical antipsychotics and risperidone
37
Autonomic SA's
``` Anticholinergic- muscarinic blockade (ACh) blurred vision, dry mouth Antiadrenergic effects (GPCR)- orthostatic hypotention and reflex tachycardia ```
38
Cardio SA's
Hypotention
39
Blood Disorders
Decrease WBC- leukopenia Increase certain elements (eosinophilia) Clozapine- can cause bone marrow suspension and frank agranulocytosis
40
EPS SA's
More common w/typical.
41
Parkinsonian
EPS 5-30 day onset. Treatment w/anticholinergic drugs
42
Acute Dystonic Rxn
1-5 day onset- spasms of muscles in face, back, mimic seizures Treatable w/anticholinergics
43
Akathisia
5-6 day onset; restlessness | Reduce dose of antipsych to treat
44
Neuroleptic Malignant Syndrome
Onset is weeks. Can persist for days after stopping a neuroleptic. Fever, unstable BP, can be fatal STOP antipsychotic, dantrolene or bromocriptine may help.
45
Tardive dyskinesia
Months to years Irreversible orofacial dyskinesias No effective treatment Prevention- use lowest effective dose of antipyscs.
46
Skin Reactions
Phenothiazines
47
Lowering of seizure threshold
Contraindicated during alc withdrawl or CNS depression
48
Interactions
Potentiates effects of CNS Depressents, sedative/hypnotics, alcs, antihistamines, opiates.
49
Asenapine
Atypical Schizophrenia and acute manic episodes BPD Reduced extrapyramidal symptoms, no changes in prolactin
50
Lurasidone
Atypical MDD BPD Blocks 5HT2A, D2, AND 5HT7 w/high affinity Extrapyramidal- akathisia (restlessness)
51
Other uses
Huntingtons | Tourettes
52
1st Generation Antipsyhcs
Typical, block +ve symptoms. | Little to no discrimination between D2-D1
53
2nd Generation Antipsychs
Selective for D2, HT2A | +'ve symptoms, -ve symptoms
54
3rd Generation Antipsychs
Partial agonists. | No metabolate syndrome
55
Phenothiazine Derivatives
Phenol, Sulfer, Nitrogen. Non-selective DA antagonist. Lipophobic- good to pass BBB some Hydrophillic properties- needed to dissolve and absorb in GI
56
Long Acting Neuroleptics
Increase patient compliance. More lipophillic in nature, injected IM. Prodrug design- not active. Bioactivation occurs via esterases in blood stream.
57
Alkyl chain size for optimal antipsychotic activity
3. 2c- antihystamines 1c, 4c+ do not work
58
Antipsychotic potency trend
Piperazine>piperidine>aliphatics
59
EPS frequency trend
Piperazine>piperidine>aliphatics
60
Sedation trend
Aliphatics~piperidines>piperazines
61
Hypotensive effects
Aliphatics>piperidines>piperazines
62
Metabolism of Phenothiazines and Thioxanthenes
Oxidase Demethylate, -OH addition, sulfoxides, sulfones
63
Butyropheones SAR
3' Amino group is essential for neuroleptic activity Variations on 3' amino group, ie rings retain activity Lengthening alkyl chain- reduces activity (dont want >3carbons)
64
-OH/COOH on a butyrophenone
Conversion top a LA Neuroleptic. Esterify it.
65
Metabolism of Haloperidol
Extensively metabolized in the body. See pic | Potentt neuroleptic- associated with high incidence of TD.
66
Dibenzazepines
Neuroleptics that utilize Tricyclic dibenzazepine heterocyte. Lipophillic, weakly basic.
67
Dibenzodiazepine
X substituted for: NH | ex. Clozapine, Olanzapien
68
Dibenzoxazepine
X substituted for: O | ex. Loxapine, Amoxapine
69
Dibenzothiazepine
X substituted for: S | ex. Quetiapine
70
Benzisoxazoles
Risperidone balanced DA/5HT2A antagonism Reduced EPS, +/- effects
71
Risperidone Metabolism
Alicyclic hydroxylation, Oxidative N-dealkylation, Benzisooxazole Ring clevage

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