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29 Cards in this Set
- Front
- Back
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Chlorpromazine MOA and type
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Conventional antipyschotic
MOA: Low potency D2 antagonist (also D3,D4) → depolarization blockade after several weeks (DA neurons become depolarized, voltage-gated Na channels deactivated) → dopaminergic transmission in nucleus accumbens |
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haloperidol MOA and type
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Conventional antipsychotic
MOA: High potency D2 antagonist → depolarization blockade after several weeks (DA neurons become depolarized, voltage-gated Na channels deactivated) → dopaminergic transmission in nucleus accumbens |
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fluphenazine MOa & type
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High potency
D2 antagonist → depolarization blockade after several weeks (DA neurons become depolarized, voltage-gated Na channels deactivated) → dopaminergic transmission in nucleus accumbens |
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perphenazine MOA & type
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Mid potency
D2 antagonist → depolarization blockade after several weeks (DA neurons become depolarized, voltage-gated Na channels deactivated) → dopaminergic transmission in nucleus accumbens |
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Clozapine Type & MOA
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atypical
* Serotonin dopamine antagonists (Block 5HT2A and D2 receptors) * D2 antagonists with rapid dissociation Less D2 blocking Binds D4, muscarinic, H1, & α1 receptors Tightly binds 5HT-2 A&C receptors & α2 receptors |
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olanzapine type and MOA
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Low affinity for D2 receptors
High affinity for 5HT-2, muscarinic, H1, & α1 receptors |
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risperidone type & moa
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Relatively high D2 binding for an atypical antipsychotic (risk of extrapyramidal effects)
High 5HT-2 & α2 binding Moderate H1 binding No muscarinic binding |
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quetiapine type & moa
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Main effects due to D2 & 5HT-2 antagonism
Side effects due to H1 antagonism (sedation) & α1 antagonism (orthostatic hypotension) No muscarinic binding |
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ziprasidone type & moa
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Main effects due to D2 & 5HT-2 antagonism
Side effects due to H1 antagonism (sedation) & α1 antagonism (orthostatic hypotension) No muscarinic binding |
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What is the order (from worst to best) of atypicals causing metabolic syndrome
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Clozapine>olanzapine>quetiapine> risperidone>ziprazidone>Aripiprazole
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aripiprazole type & MOA
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atypical (sometimes called 3rd generation)
MOA: Partial agonist at dopamine D2 receptor and at the 5-HT1A receptor Antagonist at 5-HT2A receptors Theoretically better able to modulate dopamine based on ambient dopamine tone |
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What is odd about clozapine?
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Despite being a weak D2 receptor antagonist its MOST EFFECTIVE of ALL antipsychotics!
Drug of choice for tx resistant schizophreniacs |
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Which atypical is most similar to typcial antipsychotics?
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Risperidone
At therapeutic doses occupies close to 100% of the 5HT2 receptors but only 65 - 70% of D2 receptors --> higher risk of extrapyramidal effects |
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What should you watch out for if administering Clozapine??
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AGRANULOCYTOSIS!!!
*must be on REGISTRY & NEEDS CONSTANT MONITORING *most often occurs in first 6 months of tx * can kill... Check CBC: weekly x 6mo, biweekly x 6 mo, then q4wks Contraindications: WBC< 3500, hx bone marrow disorder, or hx of clozapine-induced agranulocytosis |
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Should you give antipyschotics to the elderly?
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No!!!
2008 FDA warning: increased mortality with typical and atypical antipsychotic use in elderly patients treated for dementia-related psychosis |
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What tx do you typically start with for antipyschotics? atypical or typical?
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Usually start w/ atypical but beward of metabolic syndromes and risk factors
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What were results of CATIE?
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ATYPICAL – 1st line, CLOZAPINE --> 2nd line
CLOZAPINE & OLANZAPINE have an edge in effectiveness but are MUCH more likely to induce metabolic syndrome |
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What is the idea behind glutamate modulating agents?
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PCP blocks NMDA receptor and induces schizophrenia, ergo thought is low glutamate is causing schizo
Ergo, drug that activates Glutamate receptors could halt effects of schizo *Enhance NMDA receptor *Increase glutamate release a specific agonist of the so-called group II metabotropic glutamate receptors, mGlurR2 and mGluR3, was found to be effective in a small study of schizophrenic patients. |
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What drug is used for aggression & irratibility in children?
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Risperidone
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Benzodiazepine contraindication
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OBSTRUCTIVE SLEEP APNEA!
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Barbituate contraindication?
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Family hx of acute intermittent porphyria
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What type of drug is butalbital?
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Intermediate acting barbituate
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What type of drug is phenobarbital?
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Long acting barbituate
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What type of drug thiopental?
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short acting barbituate
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If a barbituate has high lipid solubility, will it be short or long acting?
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Short acting!
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What is ramelteon?
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Hypnotic that works at the melatonin receptor
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What is flumazenil?
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Antagonist at benzo receptor
Short half life |
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What is zolpidem?
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Non-benzo GABA-A receptor agonist
Selective for certain GABA-A heteromers Selective for alpha 1 --> sedation! |
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What are therapeutic indications for Temazepam?
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Insomnia
Off-label: Anxiety (its a benzodiazepne) |
