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53 Cards in this Set

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Where do all of antipsychotics cause their pharmacodynamic effects?
They interact with neurotransmitter receptors in both central and the autonomic nervous system. (the effects of antipsychotics at the autonomic receptors are usually considered to be adverse effects)
Most antipsychotics act as _____ at the receptors they bind to.
What are 2 mechanisms which attribute to antipsychotic drugs efficacy?
1. Blockade of D2 receptors (a type of dopamine receptor) in the CNS
2. Blockade of serotonin (5-HT) receptors in the CNS. (5-HT2A subtype appears to be especially impt. with regard to antipsychotic efficacy)
The individual receptor blockade profile of each antipsychotic is an impt. factor in determining two things:
1. the efficacy of the antipsychotic for treatment of various symptoms of schizophrenia and
2. the adverse effect profile of the antipsychotic
What does the 5-HT2A/D2 Ki ratio represent?
It represents the relative affinity of an antipsychotic for 5-HT2A blockade versus D2 blockade.
What does a smaller Ki value mean?
It means that a drug has a higher affinity for binding to and blocking a specific receptor.
What happens if the Ki is lower for 5-HT2A bloackade then for D2 bloackade?
Then the ratio will be a number less than 1. Since a lower Ki value means higher affinity, a 5-HT2A/D2 Ki ratio of less than 1 results.
What does a 5-HT2A/D2 Ki ratio of less than 1 indicate?
It indicates that the drug has a higher affinity for 5-HT2A receptor blockade than it does for D2 receptor blockade.
Name 7 Atypical antipsychotics.
Aripiprazole, Clozapine, Olanzapine, Paliperidone, Quetiapine, Risperidone, Ziprasidone
Name 4 Conventional antipsycotics.
Chlorpromazine, Fluphenazine, Haloperidol, Perphenazine
All conventional drugs are variations of which core chemical ring system?
What is significant about chlorpromazine's chemistry?
It's aliphatic chemistry decreases affinity for D2 receptor blockade. (aliphatic phenothiazine)
What is significatn about fluphenazine's chemistry?
It's piperazine ring increases affinity for D2 receptor blockade. (piperazine phenothiazine)
What is the most commonly used conventional antipsychotic?
What is haloperidol classified as?
What is the chemistry of Haloperidol?
piperazine phenothiazine. It has much higher affinity for blackade of D2 receptors than any other CNS receptors.
Which 2 conventional drugs are marketed as ester prodrug derivatives for use as depot injections?
Haloperidol and Fluphenazine
Chemically, what two esters are added to the drugs, resulting in prodrugs that will be converted to active drug upon injection into the body?
Deconoate or enanthate esters
What is the significance of prodrugs are formulated in sesame seed oil, which allows for deep IM injection.
It results in a depot of drug in muscle tissue which significantly delays release and activation of prodrugs. They are especially useful for noncompliant patients.
TRUE/FALSE. Most of the atypical antipsychotics are structurally unique in that they do not share a core ring structure.
Paliperidone is an active metabolite of?
Paliperidone, as it is 9-hydroxyl-risperidone, an active metabolite of the atypical antipsychotic drug risperidone.
What is a common difference between atypical and conventional antipsychotics?
Most atypical antipsychotics have a lower 5-HT2A/D2 Ki ratior relative to conventional antipsychotics. This means they have higher selectivity for blocking serotonin receptors then dopamine receptors.
Atypical drugs versus conventional drugs:
1. Increased efficacy of atypical antipsychotics against negative symtoms of schizophrenia relative to conventional antipsychotics and
2. a lower incidence of adverse effects caused by D2 receptor blockade relative to conventional antipsychotics
Name the 6 positive schizophrenia symtoms.
1. Delusions
2. Hallucinations
3. Disorganized speech
4. Disorganized thinking
5. Diorganized behavior
6. Catatonia
Name the 4 negative schizophrenia symptoms.
1. Flattened affect
2. Social withdrawal
3. Avolition
4. Alogia
Why are atypical antipsychotics superior for the treatment of negative schizophrenia symptoms?
Because of their high affinity for 5-HT receptor bloackade, particularily 5-HT2A
EPS (Extrapyramidal side effects) are more likely to occur with _________ antipsychotics and is less frequent with ______ antipsychotics.
conventional antipsychotics, atypical antipsychotics
What is EPS due to?
potent blockade of D2 receptors in motor control regions of the brain.
What kind of dose do conventional drugs with a high affinity for blocking D2 receptors?
conventional antipsychotics high affinity for blocking D2 receptors are more potent, and therefore require a lower daily dose.
What kind of dose do conventional drugs with a low affinity for blocking D2 receptors?
conventional antipsychotics low affinity for blocking D2 receptors are less potent, and therefore require a higher daily dose.
TRUE/FALSE. High potency conventional antipsychotics (haloperidol) are more likely to cause EPS than are low potency conventional antipsychotics (chloropromazine) or atypical antipsychotics (quetiapine).
Name the 3 major symptoms that EPS is divided into.
1. Dystonia,
2. Akathisia
3. Pseudoparkinsonism
What is dystonia?
sudden muscle rigidity of the neck, pharyngeal-laryngeal areas, tongue, and other areas of the upper body
What does Akathisia mean?
The inability to sit still and is manifested as extreme restlessness.
What is pseudoparkinsonism?
Symotoms are similar to those seen in parkinson's disease (this should make sense, as parkinson's disease is due to loss of dopaminergic activity in motor control regions of the brain.)
What are used to treat or prevetn dystonias and pseudoparkinsonism?
Antimuscarinic drugs. Examples include benzotropine and diphenyhydramine.
What is used for the management of akathisia?
Beta adrenergic antagonist with significant CNS activity (propranolol)
What is the cause for tardive dyskinesia?
The exact cause is unknown, but is probably due to a "supersensitisation" of dopamine receptors secondary to chronic administration of an antipsychotic. It usually sppears after a long period (months to years) of exposure to an antipsychotic.
Tardive antipsychotics are rare with _______ antipsychotics.
atypical antipsychotics
What is tardive dyskinesia?
Tardive dyskinesia consists of involuntary motor movements, of which the patient is often completely unaware.
What are the symptoms of tardive dyskinesia?
Symptoms usually involve the face, but can also involve extremities. Typical symptoms are tongue protrusion, lip smacking, eyebrow arching, excessive blinking, grimacing, pelvic thrusting, and extension of fingers and toes.
How can you treat tardive dyskinesia?
changing antipsychotics, but usually some portion of the symotoms of tardive dyskinesia are permanent
Which drugs cause the most ANS toxicities?
Low potency (high dose) conventional antipsychotics, such as chlorpromazine.
What are the common symptoms of ANS toxicities resulting from a blockade of muscarinic and alpha-1 adrenergic receptors?
Antimuscarinic effects (dry mouth, constipation, urinary retention) and orthostatic hypotension.
Which atypical antipsychotic has strong antimuscarinic effects?
clozapine. Instead of causing dry mouth, it causes extreme excess in drooling.
What are the sedative/drowsiness effects of antipsychotics due to?
Blockade of histamine receptors in the CNS
What is an adverse effect of clozapine?
life-threatening agranulocytosis
What is an adverse effect in many antipsychotics? Which drug is the worst and which drug is the mildest?
significant weight gain. Olanzapine is the worst and Ziprasidone is the mildest.
What is an adverse effect of ziprasidone?
life-threatening widening of the QT interval, and must be used with ccaution in patients with certain cardiac diseases.
What is an adverse effect of atypical antipsychotics
increased risk for development of hyperlipidemia and type II diabetes mellitus
TRUE/FALSE. Due to the numerous CNS and autonomic receptors bloacked by antipsychotics, there are many potential pharmacodynamic drug interactions that may occur with other medicines administered concurrently.
Pharmacokinetic drug interactions involving antipsychotic are due to....
inhibition of CYP450 enzymes
The majority of antipsychotics are metabolized by?
CYP2D6, a specific isoform of CYP450. Other drugs that inhibit this isoform may increase blood levels of many antipsychotics and lead to increased adverse effects.