Anti-Psychotic & Anti-Manic Drugs Part 2 Flashcards Preview

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Flashcards in Anti-Psychotic & Anti-Manic Drugs Part 2 Deck (23):
1

What are the available Typical Antipsychotic Drugs?

  • Phenothiazines
    • Chlorpromazine, Triflupromazine 
    • Thioridazine, Mesoridazine
    • Trifluoperazine, Fluphenazine, Perphenazine, Prochlorperazine
  • Thioxanthine derivatives
    • Chlorprothixene, Thiothixene
  • Butyrophenone derivative 
    • Haloperidol 
  • Pimozide 

 

2

What are the 3 types of Phenothiazines? 

  • Aliphatic side chain 
  • Piperidine side chain 
  • Piperazine side chain 

3

Phenothiazines: Aliphatic side chain 

Examples 

Potency

Actions

  • Chlorpromazine, Triflupromazine 
  • Low to medium potency
  • Sedative
  • Pronounced anti-cholinergic actions 

4

Phenothiazines: Piperidine side chain

Examples

Potency

Actions

  • Thioridazine, Mesoridazine
  • Low potency
  • Sedative
  • Less extrapyramidal actions, anti-cholinergic 

5

Phenothiazines: Piperazine side chain 

Examples

Potency

Actions

  • Trifluoperazine, Fluphenazine, Perphenazine, Prochlorperazine 
  • High potency 
  • Less sedative
  • More extrapyramidal actions, less anticholinergic 

6

Thioxanthine Derivatives

Examples

Pharmacology 

  • Chlorprothixene, Thiothixene
  • Non-nitrogen containing analogs of the phenothiazines 
  • Pharmacology is similar to their equivalent phenothiazines 

7

Butyrophenone Derivative 

Example

Pharmacology 

  • Haloperidol 
  • Not chemically related to phenothiazines
  • Pharmacologically similar to high-potency piperazine derivatives 

8

Pimozide 

Mechanism of Action

Use

 

  • Potent neuroleptic 
  • Many side effects
  • Approved for treatment of Tourette's 
  • Commonly used when haloperidol doesn't 

9

What are the Atypical Antipsychotic Agents? (10)

  • Clozapine
  • Olanzapine
  • Risperidone
  • Quetiapine
  • Aripiprazole
  • Ziprasidone
  • Paliperidone
  • Asenapine 
  • Iloperidone 
  • Lurasidone

10

Clozapine

Mechanism of Action

Side effects

  • Blocks D4 & 5-HT2 receptors
  • Little effect on D2
  • Muscarinic antagonist 
  • Improves positive symptoms even in patients not helped by other drugs
  • Improves negative symptoms
  • Lowers seizure thresholds more than other antipsychotics (5-10%)
  • Can cause fatal agranulocytosis (monitor) 

11

Olanzapine 

Mechanism of Action

Side Effects 

  • Related to clozapine
  • Potent 5-HT2 antagonist 
  • D1 & D2 antagonist, some D4
  • Side effects
    • Few extrapyramidal symptoms (5-HT>D)
    • Less seizure incidence than clozapine 
    • No agranulocytosis 
    • Weight gain & diabetes related adverse events 
    • Reports of olanzapine abuse 

12

Risperidone 

Mechanism of Action

Side Effects

Pharmacokinetics 

  • Combined D2 & 5-HT2 antagonist 
  • Greater reduction in negative symptoms & less extrapyramidal symptoms than traditional antipsychotics 
  • Less seizure activity & less antimuscarinic than clozapine
  • Paliperidone is the active metabolite of risperidone 
    • Both available as IM depot preparations

13

Quetiapine

Mechanism of Action

Pharmacokinetics

Use

Side Effects

  • Mechanism of Action
    • Structurally related to clozapine
    • Similar to risperidone & olanzapine in effects on schizophrenia symptoms & side effects 
  • Pharmacokinetics: shorter t1/2
  • Use
    • Approved for augmentation in depression
  • Side Effects
    • Some reports of abuse 

14

Ziprasidone 

Mechanism of Action

Side effects 

  • 5-HT2 & D2 antagonist 
  • May have 5-HT1a activity (anxiolytic?)
  • No weight gain 

15

Aripiprazole 

Mechanism of Action

Use

  • Partial D2 agonist 
  • 5-HT2 antagonist 
  • Approved as an adjunct in depression (augmentation)

16

What is the mechanism of action of Lithium?

  • monovalent cation of the lightest alkali metal
  • one of few psychotherapeutic drugs that have no behavioral effects in “normals”
  • blocks manic behavior
  • Mechanism
    • inhibits phosphatase that converts IP2 to IP1
    • inhibits recycling of inositol substrates
    • causes depletion of second-messenger source PIP2 & therefore reduces release of IP3 & DAG

17

Pharmacokinetics of Lithium

  • complete absorption = ____ hrs
  • peak serum levels = ____ hrs
  • serum t1/2 = ____ hrs (young adults); _____ hrs (elderly)
  • ________ to plasma proteins
  • volume of distribution = ____
  • CSF conc = _____% of plasma concentration
  • ____% of single dose eliminated in urine

  • complete absorption = 6-8 hrs
  • peak serum levels = 2-4 hrs
  • serum t1/2 = 18-24 hrs (young adults); 30-36 hrs (elderly)
  • unbound to plasma proteins
  • volume of distribution = TBW
  • CSF conc = 40-50% of plasma concentration
  • 95% of single dose eliminated in urine

18

Na+ levels (do/don't) affect Li levels

DO

  • increased Na excretion = clinically significant increases in Li levels
  • thiazide diuretics, losses of fluids or electrolytes

19

Lithium has a ______ therapeutic window. 

narrow

important to monitor 

20

What 2 classes of drugs raise Li levels?

  • ACE inhibitors  
  • AngII receptor blockers 

21

What is Lithium used for? 

  • treat mania & prevent recurrences of bipolar disease
  • may be useful in preventing recurrences of unipolar depression in some patients
  • Schizoaffective disorder (off-label)
  • Cluster headaches (off-label)

22

What are some side effects & toxic reactions of Lithium? (8)

  • fatigue & muscular weakness
  • tremor (treated w/ β-blockers)
  • GI symptoms
  • slurred speech & ataxia
  • serious toxicity at plasma levels 2-3X (impaired consciousness, rigidity & hyperactive deep reflexes, coma)
  • lithium levels affected by plasma Na levels --> interactions w/ diuretics & anti-hypertensives
  • narrow therapeutic window – monitor Li levels
  • use in caution w/ pregnant women

23

What are the alternatives the treatment w/ Lithium? (4)

  • Carbamazepine
    • Na+ channel
    • CNS side effects: sedation, confusion, ataxia
  • Valproic acid & divalproex sodium
    • 1st line drug in bipolar disorder 
    • Sedating 
  • Lamotrigene & topiramate
    • Antiseizure agents 
    • Na+ channels or glutamate receptors
    • Warning: suicidal ideation
  • Symbyax 
    • Combination of olanzapine & fluoxetine
    • Bipolar disorder, depressive & treatment resistant major depressive disorder 
  • Initial control of manic symptoms
    • Haloperidol
    • Clonazepam (off label)