Antipsychotics Flashcards
Parkinsonism in a person taking antipsychotics can be treated with…
(4)
and what should NEVER be given
can be treated with conventional
antiparkinsonism drugs of the antimuscarinic type (benztropine or trihexyphenidyl)
with diphenhydramine, or
amantadine.
Levodopa should never be used in these patients.
which antipsychotic is being described: has much more potent antidopaminergic and much less potent antimuscarinic activity than clozapine.
Unlike clozapine, it can cause extrapyramidal reactions and hyperprolactinemia.
Risperidone
SEIZURES are especially common with what two antipsychotics
chlorpromazine (classical) and clozapine (atypical)
Some of the atypical antipsychotic drugs produce more weight gain and increases in lipids than some typical antipsychotic drugs. Weight gain is especially prominent with (what 2 drugs)
Adverse effects of weight gain include increased risk of new-onset or worsening of type 2 diabetes mellitus, hypertension, and hyperlipidemia. (metabolic syndrome)
clozapine and olanzapine.
Labels of all atypical antipsychotics must carry a warning about the increased risk of hyperglycemia and diabetes.
Antipsychotic drugs are pregnancy category C.
Only_________is category B.
clozapine
the only antipsychotic drug that causes retinal deposits, which in advanced cases may resemble retinitis pigmentosa. The deposits are usually associated with “browning” of vision.
Thioridazine
which two atypical antipsychotics are least likely to cause EPRs
Clozapine and quetiapine are the agents least likely to induce EPR.
D1-like dopamine receptors: activate or inhibit adenylyl cyclase?
D2-like dopamine receptors: activate or inhibit adenylyl cyclase?
D1-like dopamine receptors: D1 & D5: activate adenylyl cyclase
D2-like dopamine receptors: D2, D3, D4: inhibit adenylyl cyclase
what are some COMMON PROPERTIES OF ATYPICAL ANTIPSYCHOTICS
- Most atypical drugs exhibit dual antagonism at 5-HT2A and D2 receptors. They are sometimes referred to as serotonin-dopamine antagonists (SDA).
- They appear to exert part of their action by blocking 5HT receptors.
They are much less likely to cause extrapyramidal reactions than classical agents.
They are less likely to cause tardive dyskinesia
They are less likely to cause increases in prolactin
They are more effective at treating negative symptoms.
They are effective in treatment of refractory populations.
Low potency, high anticholinergic activity, low affinity for D2 recpetors at basal ganglia, less EPRs
is that describing the class that thioridazine and chlorpromazine belong to or haloperidol and fluphenazine?
Low-potency conventional antipsychotic drugs chlorpromazine or thioridazine
deposits in the anterior portions of the eye (cornea and lens).
Chlorpromazine
what is the most important adverse effect of antipsychotic drugs.
TARDIVE DYSKINESIA
Late-occurring syndrome of abnormal choreoathetoid movements.
Patients display involuntary movements including lateral jaw movements and fly-catching motions of the tongue. Disfiguring and potentially irreversible disorder. Probably due to long-term dopamine receptor blockade, causing dopamine receptors to up-regulate.
The drugs most commonly used to manage akathisia (restless leg syndrome) are..
(2)
clonazepam or propranolol.
- Classical antipsychotics are subclassified according to their potency:
- Name the High-potency drugs:
- Name the Low-potency drugs:
H + -azines
(4)
High-potency drugs: Fluphenazine and haloperidol. More likely to produce EPRs.
Low-potency drugs: Chlorpromazine and thioridazine. Less likely to produce EPRs and more likely to produce sedation and postural hypotension.
Blocking α1 receptors results in orthostatic hypotension..common with what drug
chlorpromazine (classical)
are antimuscarinic effects in relation to antipsychotics beneficial in relation to extrapyramidal side-effects or not beneficial
YES beneficial
With the exception of (these two atypical antipsychotics), most neuroleptics have antiemetic effects mediated by blockade of D2 receptors of the chemoreceptor trigger zone of the medulla.
aripiprazole and thioridazine
(no anti-emetic properties)
which drug causes agranulocytosis in 1-2% of patients.
Clozapine
High potency, low anticholinergic activity, high affinity for D2 recpetors at basal ganglia, more EPRs
is that describing the class that thioridazine and chlorpromazine belong to or haloperidol and fluphenazine?
High potency: haloperidol and fluphenazine
is a partial agonist at D2 and 5HT1A receptors and an antagonist at 5HT2A receptors
which Atypical antipsycholtic is that
Aripiprazole
why is Sedation more likely with low-potency antipsychotics and with the atypical agents?
It is due to blockade of central H1 receptors
list the atypical antipsycholtics
ATYPICAL ANTIPSYCHOTICS
Clozapine
Olanzapine
Quetiapine
Risperidone
Paliperidone
Aripiprazole
CARDIAC TOXICITY
Thioridazine is associated with a significant risk of QT prolongation and lethal torsade de pointes.
As a result, the FDA has issued a “black box” warning recommending use of thioridazine be reserved for patients who have failed adequate courses of other antipsychotics.
which AE is being described
Rare and potentially fatal reaction to antipsychotic drugs. Characterized by severe rigidity, tremor, hyperthermia, altered mental status, autonomic instability, elevated white cell count, elevated serum creatine kinase, and sometimes myoglobinemia with potential nephrotoxicity.
how is it treated
NEUROLEPTIC MALIGNANT SYNDROME
Dantrolene [ryanodine receptor antagonist] or bromocriptine [dopamine agonist] may be helpful.
Switching to an atypical drug after recovery is indicated.
Do Classical or Atypical antipsychotic drugs have higher affinities for other receptors than for the D2 receptor?
Atypical antipsychotic drugs
Clozapine: has high affinity for D1, D4, 5HT2, muscarinic and α−adrenergic receptors, but it is also a D2 blocker.
Risperidone: blocks 5HT2 to a greater extent than it does D2.
