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KG - pharmacology 3 > KG - Pharm 3, Exam 1, Antipsychotics & Mood Stabilizers > Flashcards

KG - Pharm 3, Exam 1, Antipsychotics & Mood Stabilizers Flashcards

1
Q

positive symptoms schizophrenia?

A
  • hallucinations
  • delusions
  • disorganized speech
  • disorganized thinking
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2
Q

What is cause of positive symptoms of schizophrenia?

A
  • OVER ACTIVE DOPAMINE PATHWAYS IN LIMBIC SYSTEM

- -> MESOLIMBIC

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3
Q

negative symptoms schizophrenia?

A
  • apathetic
  • withdrawn
  • anti-social
  • lack of motivation
  • depressed
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4
Q

what is cause of negative symptoms of schizophrenia?

A
  • UNDER ACTIVE DOPAMINE PATHWAYS IN FRONTAL CORTEX

- -> MESOCORTICAL

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5
Q

classical antipsychotics: info

A
  • “neuroleptics”
  • BLOCK DOPAMINE D2 RECEPTORS
  • target MESOLIMBIC SYSTEM
  • alleviate POSITIVE SYMPTOMS
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6
Q

atypical antipsychotics: info

A
  • BLOCK 5-HT2a & DOPAMINE RECEPTORS
  • target MESOCORTICAL SYSTEM
  • alleviate both NEGATIVE & POSITIVE SYMPTOMS
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7
Q

antipsychotics: general effects

A
  • delayed onset, 6 wks
  • decreased aggression, restlessness, anxiety
  • slowed psychomotor function
  • sedation
  • reduce spontaneous movements
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8
Q

role of PROCHLORPERAZINE?

A
  • antiemetic
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9
Q

antipsychotics: side effects

A
  • very common (poor compliance)
  • decreased seizure threshold
  • weight gain, increased prolactin secretion
  • ANTICHOLINERGIC = dry mouth, blurred vision, tachycardia, constipation
  • ALPHA ADRENERGIC = postural hypotension
  • HISTAMINE - sedation
  • xerostomia, bruxism
  • EXTRAPYRAMIDAL SYMPTOMS
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10
Q

which class of drug causes more EPS?

A

classical antipsychotics > atypicals

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11
Q

describe: Parkinson’s like-EPS

A
  • tremor, rigidity, akathisia, packing, restlessness, anxiety, dystonia
  • IMBALANCE OF STRIATAL DA & ACh
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12
Q

Parkinson’s EPS: tx?

A

Benztropine

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13
Q

describe: tardive dyskinesia

A
  • uncontrollable mouth/facial movements
  • occurs late dz following long term tx
  • hard to treat, often irreversible
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14
Q

Tardive dyskinesia: tx?

A
  • discontinue drug
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15
Q

which drugs least likely to cause tar dive dyskinesia?

A

Clozapine & Olanzapine

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16
Q

describe: Neuroleptic Malignant Syndrome

A
  • LIFE THREATENING
  • muscle rigidity, hyperpyrexia, changes in BP/HR
  • block of DA D2 receptors in striatum & hypothalamus
  • DA agonists used to stimulate DA receptors
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17
Q

neuroleptic malignant syndrome: tx?

A

Dantrolene

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18
Q

antipsychotics: drug interactions

A
  • anticholinergics = more side effects
  • SEDATIVE HYPNOTICS = INCREASED SEDATION
  • TCAs = SEIZURES, CARDIAC EFFECTS
  • DRUGS THAT INDUCE CYP450s (CARBAMAZEPINE - don’t give to control seizures, cimetidine)
  • SMOKING - INDUCES CYP450s
  • unpredictable w/ antihypertensives
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19
Q

classical antipsychotics: pharmacokinetics

A
  • absorbed by gut
  • high first pass metabolism
  • half lives 20-35 hrs
  • effects last weeks
  • metabolized by CYP450s
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20
Q

Chlorpromazine: use

A
  • psychosis w/ mania & drugs of abuse

- pre-anesthetic

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21
Q

Chlorpromazine: moa

A
  • blocks DA D2 receptors
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22
Q

Why is chlorpromazine less likely to cause EPS than other drugs?

A
  • high anticholinergic effects
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23
Q

Chlorpromazine: side effects

A
  • sedation, postural hypotension, blurred vision, constipation, decreased GI motility, inhibition of ejaculation, jaundice
  • DECREASES SEIZURE THRESHOLD
  • RETINAL DEPOSITS??? (browning of vision)
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24
Q

Fluphenazine: info

A
  • SIMILAR to Chlorpromazine
  • selective for DA D2 receptors
  • less anticholinergic activity
  • MORE EPS
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25
Haloperidol: moa
- POTENT BLOCKER DA D2 RECEPTORS | - also affinity for DA D1, 5-HT2, alpha 1 RECEPTORS
26
Haloperidol: use
- acute situations - may be injected - long half life
27
Haloperidol: info
- "VIT H" - NO ANTICHOLINERGIC ACTIVITY - EPS
28
atypical antipsychotics: moa
- BLOCK 5-HT RECEPTORS & DA D2 RECEPTORS | - alleviate neg & pos symptoms
29
Clozapine: moa
- BLOCK 5-HT2a & DA D4 RECEPTORS (some DA D2)
30
Clozapine: info
- EPS, tardive dyskinesia rare - rapid relapse if discontinued abruptly - DRUG OF LAST CHOICE --> AGRANULOCYTOSIS (BLOOD MUST BE MONITORED)
31
Clozapine: side effects
- hypersalivation - sedation - postural hypotension - tachycardia - weight gain
32
Olanzapine: moa
- BLOCK 5-HT2a RECEPTORS & DA D4/D2 RECEPTORS | - some anticholinergic activity
33
Olanzapine: info
- EPS rare | - used for bipolar disorder
34
Olanzapine: side effects
- w/ TYPE II DIABETES - HYPERGLYCEMIA - EPS rare - sedation, orthostatic hypotension, weight gain
35
main diff between Clozapine & Olanzapine?
Olanzapine = NO AGRANULOCYTOSIS
36
Risperidone: info
- FIRST LINE DRUG PSYCHOSIS | - EPS, tardive dyskinesia RARE
37
Risperidone: moa
- BLOCKS 5-HT2a & DA D2 receptors | - NO sig effect on DA neurotransmission in nigrostriatal pathway
38
Risperidone: side effects
- hypotension, weight gain, insomnia, anxiety, QT prolongation
39
Ziprasidone: moa
- BLOCKS DA D2 & 5-HT2a RECEPTORS | - SOME ANTIDEPRESSANT ACTIVITY
40
Ziprasidone: uses
- Tourette's | - acute mania
41
Ziprasidone: info
- orally or injected | - metabolized by CYP3A4
42
Ziprasidone: side effects
- PROLONGS QT INTERVAL - causes SEDATION - impairs cog/motor skills - use w/ caution in pts q/ hx SEIZURES
43
Quetiapine: moa
- BLOCKS 5-HT & DA D2 RECEPTORS
44
Quetiapine: info
- sim to Clozapine - to promote sleep onset - few EPS symptoms - NO AGRANULOCYTOSIS
45
Quetiapine: side effects
- does NOT elevate prolactin - VERY SEDATING - dizziness, constipation, xerostomia, orthostatic hypotension, weight gain
46
Aripiprazole: moa
- PARTIAL AGONIST FOR DA D2 & 5-HT - ANTAGONIST FOR 5-HT2a - "DOPAMINE SYSTEM STABILIZER" - -> when dopaminergic tone low, DA receptors activated - -> when dopaminergic tone high, DA receptors blocked - blocks alpha 1 and histamine receptors
47
Aripiprazole: info
- low incidence EPS - metabolized by CYP3A4, CYP 2D6 - no increase prolactin - does not increase QT interval
48
Aripiprazole: side effects
- hyperglycemia, seizures, sedation, increased glucose, orthostatic hypotension - DECREASES ESOPHAGEAL MOTILITY
49
describe: bipolar disorder
- pts alternate between manic phases and deep depression
50
bipolar disorder: tx
- lithium - anticonvulsants *Pts usu treated w/ combos of these drugs and antipsychotics (ie: Olanzapine)
51
Lithium: absorption?
- absorbed from gut - distributed from body - reabsorbed by PROXIMAL TUBULE in kidney --> COMPETES WITH SODIUM for reabsorption
52
Lithium: possible outcomes when competing w/ sodium in proximal tubule?
- Na+ decreases --> Li absorption increases = TOXICITY - Na+ increases --> Li absorption decreases; excretion increases - Li increases --> Na+ absorption decreases = HYPONATREMIA
53
Lithium: moa
- SUPPRESS 2nd MESSENGERS (IP3) - EXTREMELY toxic in overdose - SMALL THERAPEUTIC WINDOW
54
Lithium: toxicity
- Levels > 2 = nausea, diarrhea, anorexia, weakness, HA, tremor, confusion, memory impairment - Levels > 2.5 = confusion, slurred speech, sedation, nystagmus, seizures, renal failure, cardiac arrhythmias, coma, death NORMAL = 0.6-1.2
55
lithium: side effects
- hypothyroidism - DIABETES INSIPIDUS (Li inhibits ADH, tubule can't conserve H2O, increased thirst, increased urine output) - NOT REC IN PREGNANCY
56
W/ lithium, DI tx?
Amiloride | - blocks entry of Li into collecting duct
57
lithium: drug interactions
- antidepressants = mania may incr - BENZOS & ANTIPSYCHOTICS = SAFE! - DIURETICS can alter Li clearance - NSAIDS = increase Li toxicity - Sodium = reduce Li concentration
58
what are alternatives to lithium for bipolar disorder?
- anticonvulsants - -> Valproic acid - -> Gabapentin
59
Valproic acid: uses (for b.d.)
- RAPID CYCLING/DEPRESSIVE PHASES | - rapid onset
60
Valproic acid: moa (for b.d.)
- unknown - inhibition ion channels, incr GABA
61
Valproic acid: side effects (for b.d.)
- GI upset - liver enzyme induction - weight gain - SURGICAL BLEEDING (dental) - TERATOGENIC!!!
62
Gabapentin: uses (for b.d.)
- for RAPID CYCLING
63
Carbamazepine: uses (for b.d.)
- REFRACTORY BIPOLAR DISORDER (used in combo w/ lithium)
64
Carbamazepine: side effects (for b.d.)
- GI upset, sedation, CNS toxicity, hypersensitivity, rashes, hematologic rxns - SJS
65
Carbamazepine: drug interactions (for b.d.)
- competes for metabolism w/ Cimetidine, isoniazid, fluoxetine, erythromycin - INCREASES TOXICITY
66
Carmamazepine: SJS
- toxic epidermal necrosis | - testing for human antigen now required
67
Lamotrigine: uses (for b.d.)
- for prevention of relapse, depressive state following mania, acute mania

KG - pharmacology 3 (11 decks)

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