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Pharm III Unit I > 6 Antipsychotics and Mood Stabilizers > Flashcards

6 Antipsychotics and Mood Stabilizers Flashcards

1
Q

What are some hypotheses for the causes of schizophrenia?

A

Dopamine
• DA receptors may be greater in schizophrenics
• Drugs that increase DA neurotransmission can induce psychosis
• Most antipsychotics block DA receptors

Serotonin (LSD, mescaline)
• 5HT receptors are altered in schizophrenics
• 5HT receptors mediate DA transmission

Glutamate (PCP, ketamine)

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2
Q

What are the “positive” symptoms of schizophrenia?

A

Hallucinations (auditory and visual) and delusions

Catatonic behavior, disorganized speech and thinking

Over-active dopamine pathways in limbic system (mesolimbic)

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3
Q

What are the “negative” symptoms of schizophrenia?

A

Affective behavior, apathetic, withdrawn, anti-social, lack of motivation, depressed

Under-active dopamine pathways in frontal cortex (mesocortical)

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4
Q

What happens to schizophrenics cognitively?

A

Distracted, disorganized thought, memory loss

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5
Q

What are the four dopamine pathways?

A
  1. Mesolimbic - VTA to limbic system (EMOTION)
  2. Mesocortical - VTA to frontal cortex (Cognition, emotion)
  3. Nigrostriatal - SN to striatum (Motor control)
  4. Tuberoinfundibular - Hypothalamus to pituitary (Prolactin)
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6
Q

MOA for “classical” antipsychotics

A

“Neuroleptics”

Block DA D2 receptors

Target the mesolimbic system

Alleviate the POSITIVE symptoms

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7
Q

MOA for “atypical” antipsychotics

A

Block 5HT-2a and DA receptors

Target the mesocortical and mesolimbic system

Alleviate both negative and positive symptoms

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8
Q

_______ receptors predominate in the mesolimbic region

A

DA D2

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9
Q

______ receptors are distributed in the mesocortical region

A

DA D4

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10
Q

DA D2 receptors predominate the ________ region while DA D4 receptors are distributed in the _________ region

A

Mesolimbic

Mesocortical

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11
Q

General effects of antipsychotics

A

Delayed onset - 6 weeks

Decrease aggression, restlessness, anxiety

Psychomotor function is slowed, initiative/motivation decrease

Reduce spontaneous movements

Sedation

Antiemetic (Prochlorperazine)

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12
Q

Most antipsychotics also block _______, _________, and ________ receptors in the brain and periphery

A

Muscarinic

Alpha-adrenergic

Histamine

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13
Q

Why is compliance usually poor with antipsychotics

A

Very common, not very pleasant side effects

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14
Q

Side effects of antipsychotics

A

Decreased seizure threshold

Endocrine - weight gain, increased prolactin secretion

Autonomic - anticholinergic sx, postural hypotension, sedation

Dental - xerostomia and bruxism (grinding teeth)

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15
Q

What are Extrapyramidal Symptoms (EPS)?

A

DA receptor antagonists also block DA receptors in the nigrostriatal pathway —> Parkinson’s like tremor, rigidity, dyskinesias, rocking, pacing, restlessness, anxiety, dystopia

Due to imbalance of striata DA and ACh

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16
Q

How do you treat Extrapyramidal Symptoms?

A

Anticholinergics such as benztropine (Cogentin) to restore ACh/DA balance

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17
Q

Degree of EPS a patient experiences is based on…

A

The anticholinergic activity of the antipsychotic drug (chlorpromazine vs. haloperidol)

Classical antipsychotics tend to cause more EPS than atypicals

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18
Q

Choreiform, uncontrollable, jerky movements of face and limbs, occurring in late disease following long term treatment

A

Tardive dyskinesia (15-25% of patients)

Difficult to treat, often irreversible - d/c drug

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19
Q

Which drugs are most likely to cause tardive dyskinesia?

A

Clozapine and Olanzapine

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20
Q

Life threatening side effect of antipsychotics —> muscle rigidity, hyperpyrexia, changes in BP and HR

A

Neuroleptic Malignant Syndrome

Block of DA D2 receptors in the striatum and hypothalamus

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21
Q

How do you treat Neuroleptic Malignant Syndrome?

A

Dantrolene (Dantrium)

Can also use DA agonists (bromocriptine) to stimulate DA receptors

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22
Q

What happens if you mix antipsychotics with anticholinergics?

A

Just more of the same side effects (dry mouth, urinary retention, constipation etc)

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23
Q

What happens if you mix sedative-hypnotics with antipsychotics?

A

Will increase sedation

24
Q

What happens if you mix TCAs with antipsychotics?

A

Seizures and cardiac effects

25
Q

What does smoking do if you’re on antipsychotics?

A

Induces CYP450s - so the antipsychotics don’t work as well

26
Q

MOA for classical antipsychotics

A

Block DA D2 receptors

Requires ~60% receptor occupancy

27
Q

Pharmacokinetics of classical antipsychotics

A

Readily absorbed from gut following oral administration

Most have high first pass metabolism

Half lives range from 20 to 35 hours

Effects persist for weeks after last administration

Metabolized by CYP450s

28
Q

How is Chlorpromazine (Thorazine) used?

A

Psychosis associated with mania and drugs of abuse
Also an antiemetic (prochlorperazine) and a pre-anesthetic

May cause TD and neuroleptic malignant syndrome

High anticholinergic effects so low incidence of EPS

29
Q

Side effects of Chlorpromazine (Thorazine)

A

Sedation, postural hypotension, blurred vision, constipation, decreased GI motility, inhibition of ejaculation, jaundice

Decreases seizure threshold

May cause retinal deposits*** —> “browning” of vision

30
Q

Fluphenazine (Prolixin) is similar to chlorpromazine but…

A

Selective for DA D2 receptors —> less anticholinergic activity and more EPS

31
Q

Potent blocker of DA D2 receptors that is used frequently in acute situations

A

Haloperidol (“Vitamin H”)

Also has affinity for DA D1, 5HT-2, and H1 receptors

32
Q

Haloperidol has no __________ but does have __________

A

No anticholinergic activity

Extrapyramidal symptoms, esp when used chronically

33
Q

MOA for atypical antipsychotics

A

Block 5HT-2A receptors but also DA D2 and D4 receptors

Alleviate both the negative and positive symptoms

34
Q

Which antipsychotic is the drug of last choice due to agranulocytosis?

A

Clozapine (Clozaril)

Blood must be monitored

35
Q

What is Clozapine (Clozaril)?

A

Atypical antipsychotic that blocks 5HT-2A and DA D4

EPS and tardive dyskinesia very rare

Side effects - hypersalivation, sedation, dizziness, postural hypotension, tachycardia, weight gain

Decreased seizure threshold

Relapse if d/c abruptly

36
Q

Olanzapine (Zyprexa) is similar to clozapine but…

A

No agranulocytosis

Improves both positive and negative symptoms

Some anticholinergic activity

EPS symptoms rare

37
Q

Which antipsychotic can cause T2DM?

A

Olanzapine (Zyprexa)

“Zyprexa Diabetes” - hyperglycemia and weight gain are major side effects

But it’s also used for bipolar disorder

38
Q

First line drug for psychosis

A

Risperidone (Risperdal)

Blocks 5HT-2A and DA D2 receptors to improve both positive and negative symptoms

No significant effect on DA neurotransmission in nigrostriatal pathway so EPS and TD rare

39
Q

What are the side effects of Risperidone (Risperdal)

A

Hypotension, weight gain, insomnia anxiety

Some cardiac effects - Lenghtens QT INTERVAL

40
Q

What drug is used for Tourette’s syndrome and acute mania?

A

Ziprasidone (Geodon)

Blocks DA D2 and 5HT-2A receptors

Some antidepressant activity

41
Q

Side effects of Ziprasidone (Geodon)

A

Prolongs QT interval

Causes sedation, impair cognitive and motor skills

May cause hyperprolactinemia

Used with caution in patients with history of seizure disorders or with drugs that decrease seizure threshold

42
Q

Quetiapine (Seroquel) is similar to clozapine but…

A

No agranulocytosis and does not elevate prolactin

Used to promote sleep onset and maintenance

Few EPS but VERY sedating

43
Q

What is Aripiprazole (Abilify)

A

“Dopamine system stabilizer”
• When dopaminergic tone is low - DA receptors activated
• When dopaminergic tone is high - DA receptors blocked

Low incidence of EPS

44
Q

Major side effect of Aripiprazole (Abilify)

A

Decreases esophageal motility

45
Q

What is Lurasidone (Latuda)

A

Blocks D2 and 5HT-2A receptors, and partial agonist at 5HT-1A

No antihistamine or antimuscarinc effect

Used to treat depression associated with bipolar disorder

Some incidence of agranulocytosis and neutropenia, so monitor CBC

46
Q

What is thought to cause bipolar disorder?

A

A lack of GABAergic activity

47
Q

What are the two main treatments for bipolar disorder?

A

Lithium (Eskalith)
Anticonvulsants

Often treated with combos of these drugs and antipsychotics such as olanzapine (Zyprexa)

48
Q

What are the pharmacokinetics of Lithium (Li)

A

Readily absorbed from the gut

Distributed throughout the body (half-life 24 hours)

NO METABOLISM - excreted by the kidneys

49
Q

MOA for Lithium

A

Suppresses 2nd messengers (IP3), which may increase ACh, NE, and DA

Effective in about 60% of bipolar patients

Calming effect in manic patients

Poor compliance - extremely toxic in overdose

50
Q

Where is lithium absorbed?

A

By the proximal tubule in the kidney

Competes with sodium (Na+) for re-absorption
• If Na+ decreases —> Li absorption increases —> toxicity*
• If Na+ increases —> Li absorption decreases —> excretion increases
• If Li increases —> Na+ absorption decreases —> Hyponatremai*

51
Q

What are the main side effects of lithium

A

Small therapeutic window (optimal plasma concentration range 0.6-1.2 mEq/L)
• >2 mEqL - N/D, weakness, HA, tremor, confusion, etc
• >2.5 mEq/L = confusion, sedation, nystagmus, seizures, renal failure, arrhythmias, coma, DEATH

Thyroid function reduced

Diabetes Insipidus (b/c Li inhibits ADH) - treat with amiloride

Not recommended in pregnancy

52
Q

Is it a good idea to mix lithium with antidepressants?

A

Nope - may increase mania

53
Q

Is it ok to mix benzos or antipsychotics with lithium?

A

Sure - pretty safe

54
Q

What happens if you take diuretics with your lithium?

A

Alters sodium excretion —> can also alter Li clearance

55
Q

What happens if you take NSAIDs with your lithium?

A

Increased Li toxicity - decreased clearance, increased Li uptake

56
Q

What are the alternatives to Lithium for bipolar patients?

A

Valproic Acid (Depakene) - good for rapid cycling manic/depressive phases but causes surgical bleeding and TERATOGENIC

Gabapentin (Neurontin) - also good for rapid cycling

Carbamazepine (Tegretol) - good for refractory BD in combo with Li - inc chance of SJS

Lamotrigine (Lamictal) - approved for prevention of relapse, depressive state following mania, acute mania

Pharm III Unit I (9 decks)

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