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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  • withdrawn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
Q

Haloperidol: moa

A
  • POTENT BLOCKER DA D2 RECEPTORS

- also affinity for DA D1, 5-HT2, alpha 1 RECEPTORS

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26
Q

Haloperidol: use

A
  • acute situations
  • may be injected
  • long half life
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27
Q

Haloperidol: info

A
  • “VIT H”
  • NO ANTICHOLINERGIC ACTIVITY
  • EPS
28
Q

atypical antipsychotics: moa

A
  • BLOCK 5-HT RECEPTORS & DA D2 RECEPTORS

- alleviate neg & pos symptoms

29
Q

Clozapine: moa

A
  • BLOCK 5-HT2a & DA D4 RECEPTORS (some DA D2)
30
Q

Clozapine: info

A
  • EPS, tardive dyskinesia rare
  • rapid relapse if discontinued abruptly
  • DRUG OF LAST CHOICE –> AGRANULOCYTOSIS (BLOOD MUST BE MONITORED)
31
Q

Clozapine: side effects

A
  • hypersalivation
  • sedation
  • postural hypotension
  • tachycardia
  • weight gain
32
Q

Olanzapine: moa

A
  • BLOCK 5-HT2a RECEPTORS & DA D4/D2 RECEPTORS

- some anticholinergic activity

33
Q

Olanzapine: info

A
  • EPS rare

- used for bipolar disorder

34
Q

Olanzapine: side effects

A
  • w/ TYPE II DIABETES - HYPERGLYCEMIA
  • EPS rare
  • sedation, orthostatic hypotension, weight gain
35
Q

main diff between Clozapine & Olanzapine?

A

Olanzapine = NO AGRANULOCYTOSIS

36
Q

Risperidone: info

A
  • FIRST LINE DRUG PSYCHOSIS

- EPS, tardive dyskinesia RARE

37
Q

Risperidone: moa

A
  • BLOCKS 5-HT2a & DA D2 receptors

- NO sig effect on DA neurotransmission in nigrostriatal pathway

38
Q

Risperidone: side effects

A
  • hypotension, weight gain, insomnia, anxiety, QT prolongation
39
Q

Ziprasidone: moa

A
  • BLOCKS DA D2 & 5-HT2a RECEPTORS

- SOME ANTIDEPRESSANT ACTIVITY

40
Q

Ziprasidone: uses

A
  • Tourette’s

- acute mania

41
Q

Ziprasidone: info

A
  • orally or injected

- metabolized by CYP3A4

42
Q

Ziprasidone: side effects

A
  • PROLONGS QT INTERVAL
  • causes SEDATION
  • impairs cog/motor skills
  • use w/ caution in pts q/ hx SEIZURES
43
Q

Quetiapine: moa

A
  • BLOCKS 5-HT & DA D2 RECEPTORS
44
Q

Quetiapine: info

A
  • sim to Clozapine
  • to promote sleep onset
  • few EPS symptoms
  • NO AGRANULOCYTOSIS
45
Q

Quetiapine: side effects

A
  • does NOT elevate prolactin
  • VERY SEDATING
  • dizziness, constipation, xerostomia, orthostatic hypotension, weight gain
46
Q

Aripiprazole: moa

A
  • 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
Q

Aripiprazole: info

A
  • low incidence EPS
  • metabolized by CYP3A4, CYP 2D6
  • no increase prolactin
  • does not increase QT interval
48
Q

Aripiprazole: side effects

A
  • hyperglycemia, seizures, sedation, increased glucose, orthostatic hypotension
  • DECREASES ESOPHAGEAL MOTILITY
49
Q

describe: bipolar disorder

A
  • pts alternate between manic phases and deep depression
50
Q

bipolar disorder: tx

A
  • lithium
  • anticonvulsants

*Pts usu treated w/ combos of these drugs and antipsychotics (ie: Olanzapine)

51
Q

Lithium: absorption?

A
  • absorbed from gut
  • distributed from body
  • reabsorbed by PROXIMAL TUBULE in kidney –> COMPETES WITH SODIUM for reabsorption
52
Q

Lithium: possible outcomes when competing w/ sodium in proximal tubule?

A
  • Na+ decreases –> Li absorption increases = TOXICITY
  • Na+ increases –> Li absorption decreases; excretion increases
  • Li increases –> Na+ absorption decreases = HYPONATREMIA
53
Q

Lithium: moa

A
  • SUPPRESS 2nd MESSENGERS (IP3)
  • EXTREMELY toxic in overdose
  • SMALL THERAPEUTIC WINDOW
54
Q

Lithium: toxicity

A
  • 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
Q

lithium: side effects

A
  • hypothyroidism
  • DIABETES INSIPIDUS (Li inhibits ADH, tubule can’t conserve H2O, increased thirst, increased urine output)
  • NOT REC IN PREGNANCY
56
Q

W/ lithium, DI tx?

A

Amiloride

- blocks entry of Li into collecting duct

57
Q

lithium: drug interactions

A
  • antidepressants = mania may incr
  • BENZOS & ANTIPSYCHOTICS = SAFE!
  • DIURETICS can alter Li clearance
  • NSAIDS = increase Li toxicity
  • Sodium = reduce Li concentration
58
Q

what are alternatives to lithium for bipolar disorder?

A
  • anticonvulsants
  • -> Valproic acid
  • -> Gabapentin
59
Q

Valproic acid: uses (for b.d.)

A
  • RAPID CYCLING/DEPRESSIVE PHASES

- rapid onset

60
Q

Valproic acid: moa (for b.d.)

A
  • unknown - inhibition ion channels, incr GABA
61
Q

Valproic acid: side effects (for b.d.)

A
  • GI upset
  • liver enzyme induction
  • weight gain
  • SURGICAL BLEEDING (dental)
  • TERATOGENIC!!!
62
Q

Gabapentin: uses (for b.d.)

A
  • for RAPID CYCLING
63
Q

Carbamazepine: uses (for b.d.)

A
  • REFRACTORY BIPOLAR DISORDER (used in combo w/ lithium)
64
Q

Carbamazepine: side effects (for b.d.)

A
  • GI upset, sedation, CNS toxicity, hypersensitivity, rashes, hematologic rxns
  • SJS
65
Q

Carbamazepine: drug interactions (for b.d.)

A
  • competes for metabolism w/ Cimetidine, isoniazid, fluoxetine, erythromycin
  • INCREASES TOXICITY
66
Q

Carmamazepine: SJS

A
  • toxic epidermal necrosis

- testing for human antigen now required

67
Q

Lamotrigine: uses (for b.d.)

A
  • for prevention of relapse, depressive state following mania, acute mania

KG - pharmacology 3 (11 decks)

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