Oxford shoter- antipsychotics
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Questions and Answers

Antipsychotic drugs are primarily used to treat anxiety disorders.

False

The term 'neuroleptic' refers to the therapeutic effects of antipsychotic drugs.

False

The discovery of antipsychotic drugs led to a decline in the treatment of schizophrenia.

False

Antipsychotic drugs work by blocking serotonin receptors.

<p>False</p> Signup and view all the answers

The potency of antipsychotic drugs in blocking dopaminergic receptors in vitro has no relationship to their therapeutic strength.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are only used to treat schizophrenia.

<p>False</p> Signup and view all the answers

The term 'major tranquillizer' accurately describes the therapeutic effects of antipsychotic drugs.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are only used to treat acute symptoms of psychosis.

<p>False</p> Signup and view all the answers

Chlorpromazine was introduced in the 1960s.

<p>False</p> Signup and view all the answers

The British National Formulary uses the term 'neuroleptic' to describe antipsychotic drugs.

<p>False</p> Signup and view all the answers

The term atypical antipsychotic agent was introduced to distinguish the newer antipsychotic drugs from conventional typical agents, such as risperidone and olanzapine.

<p>False</p> Signup and view all the answers

The D1 receptor is critical for antipsychotic action.

<p>False</p> Signup and view all the answers

PET studies suggest that an antipsychotic effect is obtained when D2-receptor occupancy lies in the range 80–90%.

<p>False</p> Signup and view all the answers

Low-potency conventional antipsychotic drugs such as haloperidol have a high risk of producing extrapyramidal symptoms.

<p>False</p> Signup and view all the answers

The risk of tardive dyskinesia is higher with the newer antipsychotic drugs.

<p>False</p> Signup and view all the answers

Clozapine has proven efficacy against negative or cognitive symptoms.

<p>False</p> Signup and view all the answers

Most authorities believe that the terms ‘atypical’ and ‘typical’ antipsychotic are still useful.

<p>False</p> Signup and view all the answers

Chlorpromazine antagonizes β2-adrenoceptors, histamine H2-receptors, and muscarinic cholinergic receptors.

<p>False</p> Signup and view all the answers

α1-adrenoceptor blockade by chlorpromazine causes hypertension.

<p>False</p> Signup and view all the answers

Histamine H1-receptor blockade by chlorpromazine gives it a stimulating profile.

<p>False</p> Signup and view all the answers

Thioxanthenes and butyrophenones are potent dopamine-receptor antagonists, with few effects at other neurotransmitter receptors and are sedating.

<p>False</p> Signup and view all the answers

Atypical antipsychotic drugs such as sulpiride and amisulpride are highly selective D1-receptor antagonists.

<p>False</p> Signup and view all the answers

Risperidone is a potent antagonist at both 5-HT1 receptors and dopamine D1 receptors.

<p>False</p> Signup and view all the answers

Olanzapine has a low propensity to cause movement disorders and is less sedating than quetiapine.

<p>False</p> Signup and view all the answers

Lurasidone is a weak 5-HT2 and D2 receptor antagonist.

<p>False</p> Signup and view all the answers

Asenapine binds potently to D2 receptors but weakly to 5-HT2 receptors.

<p>False</p> Signup and view all the answers

Sertindole is a weak 5-HT2-receptor antagonist with potent D2-receptor-antagonist effects.

<p>False</p> Signup and view all the answers

Ziprasidone is another 5-HT1 and D1-receptor antagonist.

<p>False</p> Signup and view all the answers

Piperazine compounds such as trifluoperazine and fluphenazine are less selective dopamine-receptor antagonists.

<p>False</p> Signup and view all the answers

Thioxanthenes are similar in structure to the butyrophenones.

<p>False</p> Signup and view all the answers

Butyrophenones are potent dopamine-receptor antagonists, with few effects at other neurotransmitter receptors and have a low propensity to cause extrapyramidal side effects.

<p>False</p> Signup and view all the answers

Substituted benzamides such as sulpiride and amisulpride are highly selective D1-receptor antagonists.

<p>False</p> Signup and view all the answers

Risperidone is a potent antagonist at both 5-HT1 receptors and dopamine D2 receptors.

<p>False</p> Signup and view all the answers

Paliperidone is an active metabolite of olanzapine and has very similar pharmacological properties when given orally.

<p>False</p> Signup and view all the answers

Olanzapine has a higher potency of dopamine D2-receptor blockade than risperidone.

<p>False</p> Signup and view all the answers

Lurasidone is a potent 5-HT2 and D2 receptor antagonist.

<p>False</p> Signup and view all the answers

The risk of tardive dyskinesia is lower with the newer antipsychotic drugs.

<p>False</p> Signup and view all the answers

Asenapine binds potently to D2 receptors but weakly to 5-HT1 receptors.

<p>False</p> Signup and view all the answers

Chlorpromazine antagonizes α1-adrenoceptors, histamine H1-receptors, and muscarinic cholinergic receptors.

<p>True</p> Signup and view all the answers

Sertindole is a potent 5-HT2-receptor antagonist with weak D2-receptor-antagonist effects.

<p>False</p> Signup and view all the answers

Quetiapine is a potent 5-HT2 and D2 receptor antagonist.

<p>False</p> Signup and view all the answers

Asenapine binds potently to D2 receptors and has a significant effect on weight gain and sedation.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are absorbed mainly from the duodenum when taken by mouth

<p>False</p> Signup and view all the answers

Sertindole is a potent 5-HT2-receptor antagonist with strong D2-receptor-antagonist effects.

<p>False</p> Signup and view all the answers

Ziprasidone is a potent 5-HT2 and D2 receptor antagonist with a high liability to cause weight gain and sedation.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are not highly protein-bound

<p>False</p> Signup and view all the answers

The plasma half-life of most antipsychotic drugs is around 3 hours

<p>False</p> Signup and view all the answers

Aripiprazole is a potent 5-HT2-receptor antagonist with a high propensity to cause weight gain and sedation.

<p>False</p> Signup and view all the answers

Quetiapine has a half-life of around 20 hours and can be dosed once daily

<p>False</p> Signup and view all the answers

Clozapine is a potent dopamine D2-receptor antagonist with a high affinity for 5-HT2 receptors and a low liability to cause movement disorders.

<p>True</p> Signup and view all the answers

The therapeutic plasma range for clozapine is 600–1000 μg/l.

<p>False</p> Signup and view all the answers

Depot preparations of antipsychotic drugs have a similar pharmacokinetic profile to standard preparations

<p>False</p> Signup and view all the answers

The majority of antipsychotic drugs are excreted unchanged by the kidney

<p>False</p> Signup and view all the answers

Zuclopenthixol acetate is used for the long-term maintenance of psychotic patients.

<p>False</p> Signup and view all the answers

Risperidone, paliperidone, aripiprazole, and olanzapine are conventional antipsychotic drugs.

<p>False</p> Signup and view all the answers

The plasma concentrations of antipsychotic drugs are commonly used in everyday clinical work to monitor treatment

<p>False</p> Signup and view all the answers

Chlorpromazine is metabolized to produce only a few active and inactive metabolites

<p>False</p> Signup and view all the answers

Depot antipsychotic drugs are used for patients who respond well to antipsychotic medication but can take it regularly.

<p>False</p> Signup and view all the answers

Zuclopenthixol acetate is an exception to the depot preparations in terms of pharmacokinetic profile

<p>True</p> Signup and view all the answers

regarding depot -Relapse after treatment discontinuation is likely to occur immediately

<p>False</p> Signup and view all the answers

Tardive dyskinesia is a disorder that improves immediately after stopping the drug.

<p>False</p> Signup and view all the answers

Clozapine is the most effective atypical agent in treating tardive dyskinesia but is best reserved for patients who respond to other atypicals.

<p>False</p> Signup and view all the answers

Vitamin E is a well-established treatment for tardive dyskinesia.

<p>False</p> Signup and view all the answers

Tetrabenazine is a dopamine-enhancing agent used to treat tardive dyskinesia.

<p>False</p> Signup and view all the answers

Anticholinergic drugs are effective in treating tardive dystonia.

<p>False</p> Signup and view all the answers

Clozapine has been reported to be useful in treating tardive dystonia.

<p>True</p> Signup and view all the answers

Local injection of botulinum toxin into the affected muscle group is not a treatment option for tardive dystonia.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are associated with a decreased risk of venous thrombosis and pulmonary embolus.

<p>False</p> Signup and view all the answers

Chlorpromazine is not associated with weight gain due to its histamine H1-receptor antagonism.

<p>False</p> Signup and view all the answers

Depression is a rare side effect of antipsychotic drugs.

<p>False</p> Signup and view all the answers

Akathisia is a feeling of physical restlessness and a need to move that is reliably controlled by antiparkinsonian drugs.

<p>False</p> Signup and view all the answers

Antipsychotic-induced parkinsonism is characterized by akinesia, an expressionless face, and lack of associated movements when walking.

<p>True</p> Signup and view all the answers

Tardive dyskinesia is more common among men, the young, and patients who have localized brain pathology.

<p>False</p> Signup and view all the answers

The incidence of tardive dyskinesia is higher with atypical antipsychotic agents such as clozapine, olanzapine, and risperidone than with haloperidol.

<p>False</p> Signup and view all the answers

The cause of tardive dyskinesia is due to a decrease in dopamine levels as a result of prolonged dopaminergic blockade.

<p>False</p> Signup and view all the answers

Antipsychotic drugs should be prescribed prophylactically to prevent tardive dyskinesia.

<p>False</p> Signup and view all the answers

Tardive dyskinesia always recovers when the antipsychotic drug is stopped.

<p>False</p> Signup and view all the answers

Antipsychotic-induced parkinsonism usually appears within the first few days of treatment with antipsychotic drugs.

<p>False</p> Signup and view all the answers

Akathisia is characterized by chewing and sucking movements, grimacing, and choreoathetoid movements.

<p>False</p> Signup and view all the answers

The symptoms of antipsychotic-induced parkinsonism can be controlled with anticholinergic drugs.

<p>False</p> Signup and view all the answers

Weight gain due to antipsychotic drugs is not associated with an increased risk of type 2 diabetes.

<p>False</p> Signup and view all the answers

Antipsychotic drugs such as haloperidol, amisulpride, aripiprazole, and lurasidone are associated with increased lipid levels.

<p>False</p> Signup and view all the answers

The presence of the metabolic syndrome in patients taking antipsychotic drugs does not significantly increase the risk of cardiovascular disease.

<p>False</p> Signup and view all the answers

Schizophrenia itself is not associated with an increased risk of diabetes.

<p>False</p> Signup and view all the answers

Antipsychotic drugs do not increase the risk of cardiovascular disease through mechanisms independent of weight gain.

<p>False</p> Signup and view all the answers

The majority of patients taking antipsychotic drugs do not have the metabolic syndrome.

<p>False</p> Signup and view all the answers

Antipsychotic drugs do not contribute to the increase in overall mortality seen in patients with schizophrenia.

<p>False</p> Signup and view all the answers

Weight gain is the most likely problem with haloperidol, amisulpride, aripiprazole, and lurasidone.

<p>False</p> Signup and view all the answers

The risk of cardiovascular disease is not increased in patients with schizophrenia taking antipsychotic drugs.

<p>False</p> Signup and view all the answers

Antipsychotic drugs do not have any negative effects on glucose metabolism.

<p>False</p> Signup and view all the answers

Clozapine should be given with carbamazepine to potentiate its therapeutic effect.

<p>False</p> Signup and view all the answers

Fluoxetine and paroxetine increase the hepatic metabolism of antipsychotic drugs like haloperidol and risperidone.

<p>False</p> Signup and view all the answers

Acute dystonia is more commonly observed in elderly women.

<p>False</p> Signup and view all the answers

Butyrophenones are associated with a low risk of extrapyramidal side effects.

<p>False</p> Signup and view all the answers

The therapeutic effects of antipsychotic drugs are mainly related to their anticholinergic properties.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are absorbed mainly from the small intestine when taken by mouth.

<p>True</p> Signup and view all the answers

Torticollis is a common feature of acute dystonia.

<p>True</p> Signup and view all the answers

Piperazine compounds, such as trifluoperazine and fluphenazine, are highly selective dopamine-receptor antagonists.

<p>False</p> Signup and view all the answers

The British National Formulary is a reference guide for antipsychotic drugs.

<p>True</p> Signup and view all the answers

Antipsychotic drugs are only used to treat positive symptoms of psychosis.

<p>False</p> Signup and view all the answers

Antipsychotic drugs can increase the risk of osteoporosis in some patients.

<p>True</p> Signup and view all the answers

Chlorpromazine is not associated with photosensitivity and skin pigmentation.

<p>False</p> Signup and view all the answers

Phenothiazines are not associated with cholestatic jaundice.

<p>False</p> Signup and view all the answers

Antipsychotic drugs do not lower the seizure threshold in epileptic patients.

<p>False</p> Signup and view all the answers

Hypothermia is not a significant unwanted effect in the elderly.

<p>False</p> Signup and view all the answers

Galactorrhoea and amenorrhoea are not induced in some women by high prolactin levels.

<p>False</p> Signup and view all the answers

The treatment of the NMS involves the use of a specific antidote.

<p>False</p> Signup and view all the answers

Blood cell dyscrasias are a common side effect of antipsychotic drugs.

<p>False</p> Signup and view all the answers

Skin rashes are not a side effect of antipsychotic drugs.

<p>False</p> Signup and view all the answers

Dantrolene is a drug that is commonly used to treat malignant hyperthermia.

<p>True</p> Signup and view all the answers

Bromocriptine is a dopamine antagonist that is used to treat the syndrome.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are not associated with metabolic changes affecting general health.

<p>False</p> Signup and view all the answers

Low-libido and sexual dysfunction are not side effects of antipsychotic drugs.

<p>False</p> Signup and view all the answers

Support in an intensive care unit is usually necessary for patients who develop the syndrome.

<p>True</p> Signup and view all the answers

Patients who have developed the syndrome can never be given the same drug again.

<p>False</p> Signup and view all the answers

At least 1 week should elapse before antipsychotic drug treatment is reinstated.

<p>False</p> Signup and view all the answers

The syndrome is usually treated with antipsychotic drugs.

<p>False</p> Signup and view all the answers

Diazepam is a drug that is commonly used to treat muscle stiffness in the syndrome.

<p>True</p> Signup and view all the answers

The syndrome is more common in patients who are treated with atypical antipsychotic drugs.

<p>False</p> Signup and view all the answers

If an antipsychotic drug has to be used again, it is recommended to restart treatment with a typical agent.

<p>False</p> Signup and view all the answers

Clozapine is associated with a significant risk of agranulocytosis.

<p>True</p> Signup and view all the answers

Weekly blood counts are mandatory for the first year of treatment with clozapine.

<p>False</p> Signup and view all the answers

The concomitant use of carbamazepine with clozapine is generally recommended.

<p>False</p> Signup and view all the answers

Clozapine is likely to cause extrapyramidal movement disorders, including tardive dyskinesia.

<p>False</p> Signup and view all the answers

Seizures are a common side effect of clozapine at any dose.

<p>False</p> Signup and view all the answers

Clozapine is associated with an increased risk of myocarditis and myopathy.

<p>True</p> Signup and view all the answers

The neuroleptic malignant syndrome is a common side effect of antipsychotic drugs.

<p>False</p> Signup and view all the answers

The mortality rate of neuroleptic malignant syndrome is typically around 1%.

<p>False</p> Signup and view all the answers

Patients who survive neuroleptic malignant syndrome usually have residual disability.

<p>False</p> Signup and view all the answers

Clozapine has been reported to cause neuroleptic malignant syndrome.

<p>True</p> Signup and view all the answers

Antipsychotic drugs are contraindicated in patients with myasthenia gravis.

<p>True</p> Signup and view all the answers

Chlorpromazine can be safely used in patients with liver disease.

<p>False</p> Signup and view all the answers

Antipsychotic drugs can increase the risk of stroke in elderly patients with pre-existing cerebrovascular disease.

<p>True</p> Signup and view all the answers

Clozapine is recommended for patients with Parkinson's disease.

<p>True</p> Signup and view all the answers

Antipsychotic drugs can produce movement disorders in patients with dementia.

<p>True</p> Signup and view all the answers

Renal disease is not a contraindication to antipsychotic medication.

<p>False</p> Signup and view all the answers

Glaucoma is a contraindication to antipsychotic medication if the drug has significant anticholinergic activity.

<p>True</p> Signup and view all the answers

Addison's disease is not a contraindication to antipsychotic medication.

<p>False</p> Signup and view all the answers

Antipsychotic drugs should be used with caution in patients with epilepsy.

<p>True</p> Signup and view all the answers

The British National Formulary is not a reference guide for antipsychotic drugs.

<p>False</p> Signup and view all the answers

Adequate dopamine D2-receptor blockade can be obtained with high doses of conventional antipsychotic drugs.

<p>False</p> Signup and view all the answers

Higher doses of antipsychotic drugs are associated with a lower risk of cardiac arrhythmias.

<p>False</p> Signup and view all the answers

Combining antipsychotic drugs with a benzodiazepine is not a safer and more effective means of producing rapid sedation than high doses of antipsychotic drugs.

<p>False</p> Signup and view all the answers

Antipsychotic drugs do not alter cardiac conduction.

<p>False</p> Signup and view all the answers

The increased risk of sudden death in patients taking antipsychotic drugs is related to decreasing dose.

<p>False</p> Signup and view all the answers

PET data are not usually available to allow clear dosage recommendations for newer antipsychotic drugs.

<p>False</p> Signup and view all the answers

Lower recommended doses of antipsychotic drugs do not produce an adequate antipsychotic effect in the majority of patients.

<p>False</p> Signup and view all the answers

The dosage of individual drugs can be found in the manufacturer’s literature or a comparable work of reference, but not in the British National Formulary.

<p>False</p> Signup and view all the answers

Doses should not be lower for the elderly, patients with brain damage or epilepsy, and the physically ill.

<p>False</p> Signup and view all the answers

There has been a trend towards the recommendation of higher doses of typical antipsychotic drugs such as haloperidol.

<p>False</p> Signup and view all the answers

Haloperidol is available as an oral preparation only.

<p>False</p> Signup and view all the answers

Aripiprazole is less effective than olanzapine in emergency situations.

<p>True</p> Signup and view all the answers

Intramuscular olanzapine should be given with parenteral benzodiazepines.

<p>False</p> Signup and view all the answers

Respiratory depression is a concern primarily in children.

<p>False</p> Signup and view all the answers

Flumazenil is used to treat respiratory depression.

<p>False</p> Signup and view all the answers

Hypoglycaemia is a medical condition that should not be considered in the differential diagnosis of disturbed behaviour.

<p>False</p> Signup and view all the answers

Antipsychotic drugs can be safely used in patients with a history of head injury.

<p>False</p> Signup and view all the answers

Alcohol consumption does not potentiate the sedative effects of antipsychotic drugs and benzodiazepines.

<p>False</p> Signup and view all the answers

Postepileptic states are not a consideration in the differential diagnosis of disturbed behaviour.

<p>False</p> Signup and view all the answers

Antipsychotic drugs and benzodiazepines are used to control psychomotor excitement, hostility, and other abnormal behavior resulting from anxiety disorders.

<p>False</p> Signup and view all the answers

The addition of olanzapine (10 mg) can be helpful if the patient is already taking an antipsychotic drug.

<p>False</p> Signup and view all the answers

Risperidone (1–2 mg) is not recommended for use in controlling acute behavioral disturbance.

<p>False</p> Signup and view all the answers

Haloperidol (5 mg) is recommended for use without pre-treatment ECG monitoring in an emergency situation.

<p>False</p> Signup and view all the answers

Psychological or behavioral approaches should be used before drug treatment to control acute behavioral disturbance.

<p>True</p> Signup and view all the answers

Quetiapine (100–200 mg) is not a suitable option for controlling acute behavioral disturbance.

<p>False</p> Signup and view all the answers

Antipsychotic drugs are used to treat acute behavioral disturbance resulting from chronic psychosis.

<p>False</p> Signup and view all the answers

Lorazepam (1–2 mg) is used to treat chronic behavioral disturbance.

<p>False</p> Signup and view all the answers

The goal of drug treatment in acute behavioral disturbance is to sedate the patient as quickly as possible.

<p>False</p> Signup and view all the answers

Promethazine (25 mg) is not used in combination with haloperidol (5 mg) to control acute behavioral disturbance.

<p>False</p> Signup and view all the answers

Phenothiazines are a type of antipsychotic drug that includes Chlorpromazine and Trifluoperazine.

<p>True</p> Signup and view all the answers

Dibenzothiazepine is a type of antipsychotic drug that includes Risperidone and Quetiapine.

<p>False</p> Signup and view all the answers

Olanzapine is a type of Butyrophenones antipsychotic drug.

<p>False</p> Signup and view all the answers

Aripiprazole is a type of Quinolinone antipsychotic drug.

<p>True</p> Signup and view all the answers

Sulpiride is a type of Substituted benzamides antipsychotic drug.

<p>True</p> Signup and view all the answers

Which antipsychotic drug is least associated with weight gain?

<p>Aripiprazole</p> Signup and view all the answers

Which of the following antipsychotic drugs has the highest propensity to cause prolactin elevation?

<p>Sulpiride</p> Signup and view all the answers

Which antipsychotic drug has been associated with agranulocytosis?

<p>Clozapine</p> Signup and view all the answers

Which of the following antipsychotic drugs is associated with a low risk of extrapyramidal symptoms?

<p>Clozapine</p> Signup and view all the answers

Which antipsychotic drug is associated with a higher risk of QT prolongation?

<p>Lurasidone</p> Signup and view all the answers

Which of the following antipsychotic drugs has been associated with a higher risk of insomnia and agitation?

<p>Lurasidone</p> Signup and view all the answers

What is the time to peak plasma for Flupenthixol decanoate?

<p>3-7 days</p> Signup and view all the answers

Which depot antipsychotic drug has a time to steady state of 2 weeks?

<p>Fluphenazine decanoate</p> Signup and view all the answers

What is the typical clinical dose of Haloperidol decanoate?

<p>100 mg</p> Signup and view all the answers

Which depot antipsychotic drug has a licensed dosing interval of 1 month?

<p>Paliperidone palmitate</p> Signup and view all the answers

What is the time to peak plasma for Pipotiazine palmitate?

<p>7-14 days</p> Signup and view all the answers

Fluphenazine decanoate takes 1-2 days to reach peak plasma concentration.

<p>True</p> Signup and view all the answers

The typical clinical dose of Zuclopenthixol decanoate is 50 mg.

<p>False</p> Signup and view all the answers

Risperidone microspheres have a time to peak plasma concentration of 2-4 days.

<p>False</p> Signup and view all the answers

Paliperidone palmitate has a licensed dosing interval of 4 weeks.

<p>False</p> Signup and view all the answers

Aripiprazole has a time to peak plasma concentration of 7 days and a licensed dosing interval of monthly.

<p>True</p> Signup and view all the answers

What is a common anticholinergic effect of antipsychotic drugs?

<p>Reduced sweating</p> Signup and view all the answers

Which of the following effects is associated with antihistaminic effects of antipsychotic drugs?

<p>Sedation</p> Signup and view all the answers

What is a possible antiadrenergic effect of antipsychotic drugs?

<p>Postural hypotension</p> Signup and view all the answers

What is a possible movement disorder associated with antipsychotic drugs?

<p>All of the above</p> Signup and view all the answers

What is a metabolic effect associated with antipsychotic drugs?

<p>Metabolic syndrome</p> Signup and view all the answers

What is the frequency of monitoring body mass index for patients taking antipsychotic drugs?

<p>Once every 4 weeks for 12 weeks, then at least biannually</p> Signup and view all the answers

What is an alternative intervention for patients who have experienced weight gain while taking antipsychotic drugs?

<p>Switching to an antipsychotic drug less likely to cause weight gain</p> Signup and view all the answers

What is the recommended frequency of blood glucose monitoring for patients taking antipsychotic drugs?

<p>Fasting or random: 12 weeks, 6 months, and then annually</p> Signup and view all the answers

What is the recommended management for patients who have developed diabetes, dyslipidaemia, or hypertension while taking antipsychotic drugs?

<p>Medical management according to NICE guidelines</p> Signup and view all the answers

What is the purpose of enquiring about tobacco smoking and alcohol use at each visit?

<p>To identify potential lifestyle interventions</p> Signup and view all the answers

What is the relative dose of Chlorpromazine?

<p>100</p> Signup and view all the answers

What is the D2-receptor occupancy in vivo of Trifluoperazine?

<p>NA</p> Signup and view all the answers

What is the maximum BNF dose of Haloperidol?

<p>20</p> Signup and view all the answers

What is the relative dose of Clozapine?

<p>60</p> Signup and view all the answers

What is the D2-receptor occupancy in vivo of Sulpiride?

<p>74</p> Signup and view all the answers

Study Notes

Antipsychotic Drugs

  • Phenothiazines:
    • Chlorpromazine (prototypic phenothiazine)
    • Antagonizes α1-adrenoceptors, histamine H1-receptors, and muscarinic cholinergic receptors
    • Causes sedation, hypotension, and anticholinergic effects
  • Thioxanthenes:
    • Flupenthixol and clopenthixol
    • Similar in structure to phenothiazines
    • Therapeutic effects similar to piperazine group
  • Butyrophenones:
    • Haloperidol
    • Potent dopamine-receptor antagonists
    • Few effects at other neurotransmitter receptors
    • Not sedating, but high propensity to cause extrapyramidal side effects
  • Atypical Antipsychotic Drugs:
    • Selective D2-receptor antagonists:
      • Substituted benzamides (sulpiride and amisulpride)
      • Highly selective D2-receptor antagonists
      • Less likely to produce extrapyramidal movement disorders
      • Lack sedative and anticholinergic properties
    • 5-HT2-D2-receptor antagonists:
      • Risperidone, paliperidone, olanzapine, quetiapine, lurasidone, asenapine, ziprasidone, and aripiprazole
      • Differ significantly in potency of dopamine D2-receptor blockade and other aspects

Pharmacology of Antipsychotic Drugs

  • Block dopamine receptors, especially D2 receptors
  • 60-70% D2-receptor occupancy associated with antipsychotic effect
  • Higher levels associated with extrapyramidal side effects and hyperprolactinaemia
  • Other side effects attributable to binding to various receptors (anticholinergic, antiadrenergic, etc.)

Depot Antipsychotic Drugs

  • Slow-release preparations used for patients who cannot rely on taking medication regularly
  • Include fluphenazine decanoate, flupenthixol decanoate, zuclopenthixol decanoate, haloperidol decanoate, and pipotiazine palmitate
  • Given intramuscularly in an oily medium
  • Zuclopenthixol acetate reaches peak plasma levels within 1-2 days and has a shorter duration of action
  • Slow-release injections of atypical antipsychotic drugs (risperidone, paliperidone, aripiprazole, and olanzapine) also available

Pharmacokinetics of Antipsychotic Drugs

  • Well-absorbed from the jejunum

  • Subject to first-pass metabolism in the liver

  • Highly protein-bound

  • Extensively metabolized by the liver to produce active and inactive metabolites

  • Half-life of most antipsychotic drugs around 20 hours, allowing for once-daily dosing

  • Quetiapine has a shorter half-life (around 3 hours) and requires twice-daily dosing### Antipsychotic Drug Side Effects

  • Weight gain associated with antipsychotic drugs can lead to obesity, increasing the risk of type 2 diabetes, and schizophrenia itself is also linked to an increased risk of diabetes.

  • The risk of diabetes is likely increased by antipsychotic drugs, partly through weight gain and partly through other pharmacological properties, such as blockade of peripheral M3 muscarinic receptors.

  • Newer antipsychotic drugs like olanzapine, clozapine, and quetiapine are associated with increased lipid levels, which can contribute to the risk of cardiovascular disease and mortality.

Metabolic Syndrome

  • Approximately one-third of patients taking antipsychotic drugs have the 'metabolic syndrome', which significantly increases the risk of cardiovascular disease, including myocardial infarction and stroke.
  • The metabolic syndrome is a combination of central obesity with two or more of the following: hypertension, raised fasting glucose, low HDL cholesterol, and raised triglycerides.

Tardive Dyskinesia

  • Tardive dyskinesia is a serious side effect that may not improve after stopping antipsychotic drugs, characterized by chewing and sucking movements, grimacing, and choreoathetoid movements.
  • It is more common among women, the elderly, and patients with diffuse brain pathology, and a diagnosis of mood disorder is also a risk factor.
  • In about 50% of cases, tardive dyskinesia disappears when the antipsychotic drug is stopped, but the incidence is lower with atypical antipsychotic agents like clozapine, olanzapine, and risperidone.

Extrapyramidal Effects

  • Extrapyramidal effects are related to the antidopaminergic action of antipsychotic drugs on the basal ganglia, and can be divided into four groups:
    • Acute dystonia
    • Parkinsonian syndrome
    • Tardive dyskinesia
    • Akathisia

Akathisia

  • Akathisia is an unpleasant feeling of physical restlessness and a need to move, leading to an inability to keep still, and may be mistaken for a worsening of psychosis.
  • It usually occurs during the first two weeks of treatment with antipsychotic drugs, but may begin only after several months, and is not reliably controlled by antiparkinsonian drugs.

Parkinsonian Syndrome

  • Antipsychotic-induced parkinsonism is characterized by akinesia, an expressionless face, and lack of associated movements when walking, together with rigidity, coarse tremor, stooped posture, and, in severe cases, a festinant gait.
  • The symptoms can be controlled with antiparkinsonian drugs, but it is not good practice to prescribe them prophylactically as a routine.

Anticholinergic and Antihistaminic Effects

  • Anticholinergic effects of antipsychotic drugs include dry mouth, urinary hesitancy and retention, constipation, reduced sweating, blurred vision, and, rarely, the precipitation of glaucoma.
  • Antihistaminic effects cause sedation and increased appetite, leading to excessive weight gain and contributing to the development of the metabolic syndrome and type 2 diabetes.

Cardiovascular Effects

  • Cardiac conduction defects, including cardiac arrhythmias, are sometimes reported, and ECG changes are more common, particularly prolongation of the QT interval and T-wave changes.
  • Antipsychotic drugs are also associated with an increased risk of venous thrombosis and pulmonary embolus, which appears to be greater with newer agents and in those who have started treatment more recently.

Other Side Effects

  • Depression of mood has been reported, but it is difficult to evaluate, and may be related to excessive dopamine-receptor blockade in the mesolimbic forebrain.
  • Other side effects include sedation, postural hypotension, nasal congestion, and inhibition of ejaculation.

Clozapine

  • Clozapine is associated with a significant risk of leucopenia, which can progress to agranulocytosis, and requires intensive monitoring of white blood cell counts.
  • It is also associated with hypersalivation, drowsiness, postural hypotension, weight gain, and hyperthermia, and may cause seizures, particularly at higher doses.### Dosage of Antipsychotic Drugs
  • Doses should be lower for the elderly, patients with brain damage or epilepsy, and the physically ill
  • Dosage of individual drugs can be found in the British National Formulary or the manufacturer's literature
  • PET imaging studies suggest that lower doses of typical antipsychotic drugs like haloperidol can be effective

Antipsychotic Drugs and Sudden Death

  • Antipsychotic drug treatment is associated with a higher risk of sudden unexplained death
  • Patients with schizophrenia taking antipsychotic drugs have higher rates of cardiac arrest and ventricular arrhythmias
  • The risk of sudden death is related to increasing dose and may be due to the drugs' effect on cardiac conduction

Pharmacological Treatment of Acute Behavioural Disturbance

  • Antipsychotic drugs and benzodiazepines are used to control psychomotor excitement and abnormal behaviour
  • The goal is to bring behaviour under control quickly and safely
  • Psychological or behavioural approaches should be tried first, followed by drug treatment if necessary
  • Combination therapy with lorazepam or promethazine can be helpful

Medications Used in Acute Behavioural Disturbance

  • Olanzapine (10 mg), quetiapine (100-200 mg), risperidone (1-2 mg), and haloperidol (5 mg) can be used orally
  • Parenteral preparations of lorazepam (2 mg), promethazine (50 mg), and olanzapine (10 mg) are available for emergency use
  • Aripiprazole (9.75 mg) is licensed for emergency use and may be less likely to cause hypotension

Practical Considerations

  • Check for possible respiratory depression, particularly in the elderly and those with concomitant physical illness
  • Benzodiazepine antagonist flumazenil should be available
  • Differentiate between mania and schizophrenia, and consider medical conditions such as postepileptic states and hypoglycaemia

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This quiz covers the definition and characteristics of antipsychotic medications, including neuroleptics and major tranquillizers. Learn about the therapeutic and side effects of these drugs. Assess your knowledge of their clinical actions and uses.

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