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

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

What are the available Typical Antipsychotic Drugs?

A
  • Phenothiazines
    • Chlorpromazine, Triflupromazine
    • Thioridazine, Mesoridazine
    • Trifluoperazine, Fluphenazine, Perphenazine, Prochlorperazine
  • Thioxanthine derivatives
    • Chlorprothixene, Thiothixene
  • **Butyrophenone derivative **
    • Haloperidol
  • Pimozide
2
Q

What are the 3 types of Phenothiazines?

A
  • Aliphatic side chain
  • Piperidine side chain
  • Piperazine side chain
3
Q

**Phenothiazines: Aliphatic side chain **

Examples

Potency

Actions

A
  • **Chlorpromazine, Triflupromazine **
  • Low to medium potency
  • Sedative
  • Pronounced anti-cholinergic actions
4
Q

Phenothiazines: Piperidine side chain

Examples

Potency

Actions

A
  • Thioridazine, Mesoridazine
  • Low potency
  • Sedative
  • Less extrapyramidal actions, anti-cholinergic
5
Q

**Phenothiazines: Piperazine side chain **

Examples

Potency

Actions

A
  • **Trifluoperazine, Fluphenazine, Perphenazine, Prochlorperazine **
  • High potency
  • Less sedative
  • More extrapyramidal actions, less anticholinergic
6
Q

Thioxanthine Derivatives

Examples

Pharmacology

A
  • Chlorprothixene, Thiothixene
  • Non-nitrogen containing analogs of the phenothiazines
  • Pharmacology is similar to their equivalent phenothiazines
7
Q

**Butyrophenone Derivative **

Example

Pharmacology

A
  • Haloperidol
  • Not chemically related to phenothiazines
  • Pharmacologically similar to high-potency piperazine derivatives
8
Q

Pimozide

Mechanism of Action

Use

A
  • **Potent neuroleptic **
  • Many side effects
  • Approved for treatment of Tourette’s
  • Commonly used when haloperidol doesn’t
9
Q

What are the Atypical Antipsychotic Agents? (10)

A
  • Clozapine
  • Olanzapine
  • Risperidone
  • Quetiapine
  • Aripiprazole
  • Ziprasidone
  • Paliperidone
  • Asenapine
  • Iloperidone
  • Lurasidone
10
Q

Clozapine

Mechanism of Action

Side effects

A
  • 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
Q

Olanzapine

Mechanism of Action

Side Effects

A
  • 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
Q

Risperidone

Mechanism of Action

Side Effects

Pharmacokinetics

A
  • **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
Q

Quetiapine

Mechanism of Action

Pharmacokinetics

Use

Side Effects

A
  • 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
Q

Ziprasidone

Mechanism of Action

Side effects

A
  • **5-HT2 & D2 antagonist **
  • May have 5-HT1a activity (anxiolytic?)
  • No weight gain
15
Q

Aripiprazole

Mechanism of Action

Use

A
  • **Partial D2 agonist **
  • 5-HT2 antagonist
  • Approved as an adjunct in depression (augmentation)
16
Q

What is the mechanism of action of Lithium?

A
  • 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
Q

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
A
  • 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
Q

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

A

DO

  • increased Na excretion = clinically significant increases in Li levels
  • thiazide diuretics, losses of fluids or electrolytes
19
Q

Lithium has a ______ therapeutic window.

A

narrow

important to monitor

20
Q

What 2 classes of drugs raise Li levels?

A
  • ACE inhibitors
  • AngII receptor blockers
21
Q

What is Lithium used for?

A
  • 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
Q

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

A
  • 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
Q

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

A
  • 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)