Psych Drugs Flashcards
Generally speaking, blocking which receptors causes orthostatic hypertension?
A1-adrenergic receptors
Blocking A1-adrenergic receptors causes
orthostatic hypertension
Generally speaking, blocking which receptors causes sedation only?
H1 histamine receptors
Blocking H1 histamine receptors causes
sedation
Generally speaking, blocking which receptors causes sedation and dry mouth?
Muscarinic cholinergic receptors
Blocking muscarinic cholinergic receptors causes:
sedation + dry mouth
Generally speaking, blocking which receptors may contribute to anti-psychotic effect?
5HT serotonin receptors
Blocking 5HT serotonin receptors may cause:
anti-psychotic effect
What receptor may mediate the antipsychotic effect of these drugs?
5HT serotonin receptors
What receptor may mediate the dry mouth + sedation effects?
Muscarinic cholinergic receptors
Which receptor may mediate the sedation-only effect?
H1 histamine receptors
Which receptor may mediate the orthostatic hypertensive effect?
A2 adrenergic receptors
Tardive dyskinesias occur when what receptors are blocked in what part of the body?
D2 receptors; corpus striatum
Tardive dyskinesia can occur when D2 receptors are blocked in the:
corpus striatum
What may happen when D2 receptors are blocked in the corpus striatum?
Tardive dyskinesias
Chlorpromazine is a typical anti-psychotic drug in that it blocks:
dopamine receptors
What types of receptors does chlorpromazine have an effect? Highest to lowest.
Chlorpromazine affects 1 adrenergic receptors (orthostatic hypertension) + 5HT serotonin receptors (anti-psychotic) equally. Then it works on D2 receptors (beware tardive dyskinesias), then D1 receptors.
What are the chances of extrapyramidal effects while using Chlorpromazine (tardive dyskinesias)?
Works on D2 receptors, but not as much as it does on A1 + 5HT receptors, so moderate risk
Level of sedation while on Chlorpromazine?
high
What are the chances of hypotension while using Chlorpromazine?
moderate
Haloperidol is a typical anti-psychotic, meaning it acts on:
dopamine receptors
What types of receptors does haloperidol act on? Highest to lowest affinity?
D2 (tardive dyskinesias) > D1, but affinity for D1 and D4 is equal. Then affinity for A1 (orthostatic hypertension), then affinity for 5HT serotonin receptors (anti-psychotic)
Chances of extrapyramidal activity while taking haloperidol?
High
Level of sedation offered by haloperidol?
Low
Chances of hypotension while using haloperidol?
Moderate
Which drug causes hyperprolactinemia?
Haloperidol
Haloperidol can cause hyperprolactinemia because it:
has a high affinity for D2 receptors.
Haloperidol has a high affinity for what type of receptors? Therefore it can cause?
D2 receptors
hyperprolactinemia
Is Clozapine a typical or atypical anti-psychotic?
Atypical
Receptors that clozapine works on? In order of affinity?
D4 = A1 adrenergic receptors (orthostatic hypertension), the 5HT serotonin receptors (anti-psychotic), then D2 (tardive dyskinesias = D1
Clozapine occupies which receptors more briefly than other anti-psychotics?
D2 receptors
Extrapyramidal effect of clozapine?
Very low
Sedative effect of clozapine?
Moderate
Hypotensive effect of clozapine?
Low-moderate
If patients are resistant to anti-psychotics, what drug may be an effective treatment?
Clozapine
What percentage of patient develop agranulocytes while on clozapine?
3%
3% of patients develop what while using clozapine?
Agranulocytes
Class of aripipraole?
DSS; dopamine system stabilizer
Is aripipraole a typical or atypical anti-psychotic?
atypical
Is aripipraole a dopamine receptor antagonist?
NO, it is a dopamine system stabilizer (DSS)
Aripipraole is a partial agonist of what receptors?
D2 dopamine receptors + 5HT1A receptors
Aripipraole is an antagonist of what receptors?
5HT1A receptors
Aripipraole has both antagonistic and agonist effects at which receptor type?
5HT1A receptors
Which drug is a treatment for schizophrenia and bipolar disorder?
Aripipraole
In states of low dopaminergic tone, aripipraole has what effect on the D2 receptor?
Activates it
In states of high dopaminergic tone, aripipraole has what effect on D2 receptor?
Inhibits it
What drug is a tricyclic antidepressant?
Imipramine
Class of imipramine?
Tricyclic antidepressant
Which transport does imipramine inhibit?
Monoamine transporter
By inhibiting monoamine transporter, what effect does imipramine have?
It increases hippocampal neurogenesis because it increases 5HT serotonin transmission + postsynaptic 5HT serotonin receptors.
Does imipramine have a euphoric effect?
No; instead, it dulls depressive ideation.
What part of the brain does imipramine mainly affect?
Hippocampus
Side effects include sedation, anticholinergic, orthostatic Hypotension. arrhythmias, tachycardia, tremor
Imipramine
Which drug has a two-week latent period and therefore needs to be taken consistently?
Imipramine
Class of fluoxetine?
Selective serotonin reuptake inhibitor (SSRI) anti-depressant
Common name of fluoxetine?
Prozac
Fluoxetine blocks what transporter?
SERT, a serotonin transporter
Fluoxetine increases levels of what receptors?
5HT serotonin receptors
Fluoxetine increases 5HT serotonin receptor concentration at synapse, but what other effect do they have on 5HT receptors?
They are selective 5HT receptor inhibitors.
Fluoxetine has what effect?
Dulls depressive ideation
Which drug is more user friendly, imipramine or fluoxetine?
Fluoxetine has fewer problems with patient compliance
Name two MAO inhibitors.
Phenylzine + Tranylcypromine
Phenylzine is what class of drug?
Antidepressant, MAO inhibitor
Mechanism of phenylzine?
Irreversible inhibition of MAO increases levels of 5HT serotonin receptors, NE, and dopamine in the brain
Therapeutic latency of phenylzine?
2-3 weeks
MAO inhibitors are psychomotor ______________.
Stimulants
Do not use phenylzine with:
L-DOPA and tyramine
Side effects of phenylzine?
orthostatic hypotension, tremors, insomnia
Class of tranylcypromine?
Antidepressant; MAO inhibitor
Tranylcypromine mechanism of action?
Irreversible blockade of MAO causes increased levels of 5HT serotonin receptors, NE and dopamine PLUS inhibition of dopamine uptake
How does tranylcypromine differ from phenylzine?
Tranylcypromine has the same mechanism as phenylzine, but it also inhibits dopamine uptake.
Which is a more powerful psychomotor stimulant–tranylcypromine or phenylzine?
Tranylcypromine
Do not use tranylcypromine with:
L-DOPA or tyramine
Side effects of tranylcypromine?
orthostatic hypotension, tremors, insomnia
Lithium is an antipsychotic useful for treating:
acute mania
Class of lithium drug?
Antipsychotic for acute mania.
What two medications are useful in treating acute mania?
Lithium and Carbamezapine/Valproate
Lithium prevents metabolism of _____________ ____________ by blocking what enzyme?
inositol phosphate; inositol phosphatase
Lithium’s calming effect is slow to develop, so it is recommended to use it with:
Haloperidol
Lithium is a prophylactic measure in treating what disease?
Bipolar disorder
Therapeutic index of Lithium?
2-3
Therapeutic blood levels of Lithium?
0.9 to 1.4 meq/L
Lithium becomes toxic at blood levels of
2 meq/L
Severe toxicity and possible death may result if Lithium concentration in the blood reaches
3 meq/L
In addition to treating acute mania, Carbamezapine/Valproate treats what condition?
Epilepsy
Carbamezapine/Valproate class?
Antipsychotic; acute mania and anti-epileptic
