Pharmacology Psychosis Fgas

Front 1

Describe chlorpromazine
Potency, anticholinergic effect, extrapyramidal effect, lowering bp effect, sedation (H1 block effect)

Back 1

Low potency
Anticholinergic: +++
Extrapyramidal: ++
Lowering BP: +++
Sedation: +++

Front 2

Describe thioridazine
Potency, anticholinergic effect, extrapyramidal effect, lowering bp effect, sedation (H1 block effect)

Back 2

Low potency
Anticholinergic: ++++
Extrapyramidal: +
Lowering BP: ++
Sedation: +++

Front 3

Describe trifluoperazine
Potency, anticholinergic effect, extrapyramidal effect, lowering bp effect, sedation (H1 block effect)

Back 3

High potency
Anticholinergic: +
Extrapyramidal: +++
Lowering BP: +
Sedation: +

Front 4

Describe haloperidol
Potency, anticholinergic effect, extrapyramidal effect, lowering bp effect, sedation (H1 block effect)

Back 4

High potency
Anticholinergic: +
Extrapyramidal: ++++
Lowering BP: +
Sedation: +

Front 5

Which drugs are phenothiazines?

Back 5

Chlopromazine
Trifluoperazine

Front 6

Describe the structure and action of phenothiazines

Back 6

-Competitive D2 agonist
-Cl to CF3 reduces anticholinergic actrivity while increasing antipsychotic and antiemetic effects
-Presence of piperazine ring at R1 markedly increases antipsychotic and antipyramidal effects
-Most potent ones have CF3 side chain

Front 7

Describe the administration, absorption, distribution, metabolism, and elimination of phenothiazines

Back 7

-Any route works
-Lipid-soluble
-Good guy absorption
-Crosses BBB
-Oral administration -> Tmax = 2-4 hours
-No correlation between plasma levels and response
->90% is protein bound
-t1/2=30hrs
-conc in brain > plasma
-Hydroxylation and conjugation are main metabolitc routes, mostly in liver
-Elimination through urine and feces

Front 8

What are the adverse drug interactions of phenothiazines?

Back 8

Chlorpromazine potentiates the effects of all CNS depressants

Front 9

What drugs are butyrophenones?

Back 9

-Haloperidol

Front 10

Compare/contrast the butyrophenones and the pehnothiazines

Back 10

The pharmacological effects are the same, but there are more extrapyramidal side effects from butyrophenone. Butyrophenones have a correlation between blood level and clinical response.

Front 11

What are the non-psychosis applications of butyrophenones?

Back 11

Haloperidol is useful in the treatement of Tourette's syndrome

Front 12

What are the side effects of FGAs?

Back 12

-Sedation
-Alpha1 receptor blockage
-Orthostatic hypotension
-Epinephrine reversal possible
-Impairment of ejaculation
-Muscarinic receptor blockade
-more problems with high dose therapy
-problems with vision, saliva, gut, and bladder
-Extrapyramidal symptoms
-Neuroendocrine side effects
-Cardiac effects
-Prolonged QT
-Neuroleptic malignant syndrome

Front 13

Describe the extrapyramidal symptoms of FGAs

Back 13

-High potency drugs have more severe side effects
-Parkinsonism-like symptoms
-Early in therapy and more severe with drugs that have little muscarinic receptor blocking activity
-Akathisia - restlessness
-Dystonias - prolonged tonic contraction
-Tardive dyskinesia - repetitive movements - seen after chronic exposure, usually seen after reduction in dose

Front 14

What causes tardive dyskinesia?

Back 14

Dopaminergic supersensitivity. Chronic dopamine receptor block causes an increase in hte number and sensitvity of hte postsymaptic dopamine receptors of the nigrostriatal pathway. Antimuscarinic drugs make this worse.

Front 15

What are the neuroendocrine side effects of FGAs?

Back 15

Amenorrhea
Galactorrhea
Increased weight
Gynecomastia
Breast tenderness
Decreaseed libido

Front 16

Describe Neuroleptic malignant syndrome

Back 16

Resbles a severe form of Parkinsonism with catatonia, fluctuations in the intesity of the course tremor, and autonomic instability (labile pulse and BP, hyperthermia). Mortality is 10%. Serum muscle enzymes are elevated typically.