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Neuro 4 Mine > General Pharmacology and Anti Psychotics > Flashcards

General Pharmacology and Anti Psychotics Flashcards

1
Q

Drugs with shorter half lives have _______ abuse potential.

A

-higer

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2
Q

Typical Antipsychotic Agents

A
  • first generation
  • high D2/5HT2A blocking ratio
  • good efficacy against positive sxs
  • high incidence of extrapyramidal toxicity
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3
Q

Haloperidol

A
  • typical antipsychotic agent: D2 antagonist
  • high potency typical antipsychotic agent
  • inc. D2 side effects
  • watch for extrapyramidal side effects
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4
Q

Chlorpromazine

A
  • typical antipsychotic agent: D2 antagonist
  • low potency typical antipsychotic agent
  • adverse drug reaction (ADR) from M-H1-a1 block
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5
Q

Atypical Antipsychotic Agents

A
  • 2nd generation
  • low D2/5HT2A blocking ratio
  • poor D2 block yet good antipsychotic efficacy
  • good 5HT2A block good efficacy against negative symptoms
  • poor D2 block + good 5HT2A block reduced incidence of EPSE
  • clozapine, ariprprazole, olanzapine, quetiapine
  • lower incidence of extrapyramidal side effects
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6
Q

Extrapyramidal Side Effects

A
  • tremor
  • slurred speech
  • dystonia
  • anxiety
  • parania
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7
Q

Muscarinic Block Adverse Reactions

A
  • dry mouth
  • blurred vision
  • urination difficulty
  • constipation
  • tachycardia
  • sedation
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8
Q

Alpha 1 Adrenergic Block Adverse Reactions

A

-orthostatic hypotension

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9
Q

H1 Histamine Block Adverse Reactions

A

-sedation

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10
Q

D2 Block Extrapyramidal Side Effects

A
  • acute dystonia (tx: anticholinergic agents ie. diphenhydramine-benztropine)
  • akasthisia (tx: reduce dose, change drug, anticholinergic, beta blocker, benzodiazapine)
  • pseudoparkinsonism (tx: anticholinergic agents)
  • tardive dyskinesia (tx. rarely effective, prevention is best)
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11
Q

Pseudoparkinsons

A
  • antipsychotic block of D2

- loss of inhibition of inhibitory indirect pathway leads to drug-induced movement disorder

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12
Q

Clozapine

A
  • atypical antipsychotic agent: D2/5HT2 antagonist
  • adverse rxns: lowered seizure threshold, AGRANULOCYTOSIS
  • agranulocytosis- dose related
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13
Q

Antipsychotic Adverse Reactions

A
  • muscarinic block
  • alpha 1 adrenergic block
  • H1 histamine block
  • weight gain- risk of Type 2 diabetes
  • D2 block- extrapyramidal side effects (acute dystonia, akathisia, pseudoparkinsonism, tardive dyskinesia)
  • agranulocytosis
  • altered thermoregulation
  • photosensitivity
  • lowered seizure threshold
  • neuroleptic malignant syndrome
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14
Q

Absorption of Antipsychotic Agents

A
  • incompletely absorbed
  • variation can be reduced with use of liquid formulation
  • significant first pass effect
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15
Q

Antipsychotic Agents Distribution

A
  • extensively protein bound in plasma
  • high lipid solubility
  • cross the placenta to exert effects in the fetus
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16
Q

Antipsychotic Agents Metabolism- Excretion

A
  • almost completely metabolized to more polar substances
  • oxidized by CYP450 system, then conjugated
  • can be excreted in breast milk
17
Q

Psyc Drug Development in Past 50 Years

A
  • most drugs mechanistically the same

- but newer drugs have fewer/better side effects

18
Q

Pharmacodynamic Tolerance

A
  • lessened response to active target site to the same drug concentration
  • due to changes in receptor sensitivity or other adaptive changes
  • a reduced effect of the drug generated by repeated administration of the drug in a particular environment
19
Q

Metabolic (Dispositional) Tolerance

A
  • change in pharmacokinetics results in lowered drug Cp at the active site
  • inc. in metabolism is the primary mechanism
20
Q

Cross Tolerance

A

-tolerance develops to one drug- then will be seen to other drugs of the same class/target

21
Q

Learned Tolerance

A
  • reduction in effects of a drug due to learned compensatory mechanisms
  • behavioral tolerance and conditioned tolerance
22
Q

Reverse Tolerance

A
  • most common in CNS stimulants
  • sensitization (inc. response) to drug following repeated doses
  • sensitization in nucleus accumbens may play role in drug craving properties
23
Q

Physical Dependence

A
  • stop use abruptly -> withdrawal sxs
  • neuroadaptation produced by repeated drug administration that necessitates continued administration to prevent the withdrawal syndrome from occuring
24
Q

Psychological Dependence

A
  • perceived need for drug (craving)

- related to pathologic learning in reward pathway

25
Q

Cross Dependence

A
  • ability of one drug to suppress the withdrawal associated with physical dependence on another drug
  • related to pharmacological effects at target, not chemical similarities
  • ex. EtOH and BDZs
26
Q

Withdrawal

A
  • characterized by rebound effects
  • effects generally opposite of acute effects of drug
  • can be fatal and may require emergent interventions
27
Q

Quetiapine

A

-atypical antipsychotic agent: D2/5HT2 antagonist

28
Q

D2 Receptor Block: Mesolimbic Pathway

A

-dec. positive sx of schizophrenia

29
Q

D2 Receptor Block: Mesocortial Pathway

A

-inc. negative symptoms of schizophrenia

30
Q

D2 Receptor Block: Nigrostiatal Pathway

A
  • inc. extrapyramidal side effects:
  • acute dystonia- tx with anticholinerics (diphenhydramine, benztropine)
  • akathisia- tx with reduced dose, anticholinergic, beta blocker, BDZ
  • pseudoparkinsonism- tx with anticholinergic agents
  • tardive dyskinesia- tx: rarely effective, prevention
31
Q

D2 Receptor Block: Tuberinfundibular Pathway

A

-hyerprolactinemia

32
Q

D2 Receptor Block: Hypothalamus

A
  • poikilothermia

- weight gain

33
Q

D2 Receptor Block: Chemoreceptor Trigger Zone

A

-anti-emetic effects

34
Q

5HT2A Receptor Block: Mesocortical Pathway

A
  • dec. negative sx of schizophrenia

- CNS- weight gain

35
Q

Muscarinic Cholinergic Block Side Effects

A
  • ANS- blurred vision, dry mouth, constipation, difficulty urinating
  • CNS- toxic confusional state
36
Q

Alpha 1 Receptor Block Side Effects

A

-ANS- orthostatic hypotension, impotence, failure to ejaculate

37
Q

Histamine H1 Receptor Block

A

-CNS- weight gain, sedation

Neuro 4 Mine (14 decks)

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