Psychiatry: Antipsychotics, Anxiolytics, Antidepressants Flashcards
What are anxiolytics?
A drug used to relieve anxiety
What is the first line Tx for anxiety disorders
SSRIs
SSRI full form?
Selective serotonin reuptake inhibitors
Examples of SSRIs
setraline
fluoxetine
What are other effect Tx for GAD
SNRIs (Serotonin and norepinephrine reuptake inhibitors )
pregabaline
Examples of anxiolytic agents
- Benzodiazepines
- Antidepressants
- Buspirone
- (Azapirones)
- Pregabalin
- Beta blockers
Examples of Benzodiazepine
lorazepam, temazepam
oxazepam
diazepam
Pharmocology of Benzodiazepines
GABAa receptors agonist.
No enzyme induction.
Phase 1 metabolism to form active
metabolites
Clinical effects of Benzodiazepines
Anxiolytic
Hypnotic
Anticonvulsant (seizures)
Sedation
Adverse effects of Benzodiazepines
- Drowsiness and dizziness.
- Confusion (elderly).
- Cleft lip / palate and respiratory depression (avoid in pregnancy).
- Cognitive and psychomotor impairment.
- Tolerance and cross-tolerance with alcohol.
- Withdrawal and discontinuation symptoms.
Pharmocology of Antidepressants
5-HT reuptake blockage
Examples of antidepressants
setraline
steraline, fluoxetine
Clinical effects of antidepressants
SSRIs: 1st line
pharmacological
treatment for anxiety
disorders.
Clomipramine: OCD
Buspirone Pharmocology
5-HT1A-
receptor partial
agonist.
Short
elimination
half-life so the body clears it quickly
Clinical effects of Buspirone
(Azapirones)
Effective in GAD
Less effective in treating acute anxiety or social phobia.
Not a good augmenting agent with SSRI in anxiety disorders
Adverse effects of Buspirone
(Azapirones)
Nausea, dizziness and akathisia
Pharmacology of pregabalin
- Has affinity for voltage-gated Ca2+
- channels.
- Eliminated unchanged via kidneys
pregabalin Clinical effects
- Effective in treating GAD
- and social phobia.
- Useful as an augmentation
- strategy for
- antidepressant-treated
- anxiety disorders
Adverse effects of pregabalin
- Well tolerated.
- Discontinuation syndrome.
- Drug of abuse.
- Deranged liver function.
- Vertigo, dizziness and weight
- gain.
Pharmacology of beta blockers
bloackage of beta adrenoceptors
Clinical effects of beta blockers
- Reduction in the physical
- symptoms of anxiety.
- Akathisia and lithium-
- induced fine tremor.
Adverse effects of beta blockers
Bradycardia and hypotension.
Bronchospasm (in asthma
patients)
WHat are the different types of Benzodiazepine agents? Give examples
- **Short-acting agents **- e.g. lorazepam and temazepam: have greater
potential for abuse and dependence, but may be safer in acute
situations.
* Long-acting agents - e.g. diazepamLong acting and short acting
- Benzodiazepines can be used for ______ ______ management of severe
anxiety
- Benzodiazepines can be used for short-term management of severe
anxiety
Longer-term anxiety is better managed by ________________,
changing the environmental situation or by other medications (e.g. ______).
Longer-term anxiety is better managed by psychotherapy,
changing the environmental situation or by other medications (e.g. SSRIs).
Can Buspironebe used longer-term for anxiety disorders?
- Buspirone can be used in the longer-term, but may be less efficacious
than alternative strategies and is rarely used in clinical practice.
What happens if you are addicted to benzodiazepine?
- For those addicted to benzodiazepines, conversion is required to a longacting drug (i.e. diazepam) before starting a very slow reducing regimen
What benzidiazepine is not used as anxiolytics?
The non-benzodiazepine “Z drugs” **(zopiclone, zaleplon and zolpidem) **are
not used as anxiolytics though they act on the benzodiazepine receptor.
They are commonly prescribed as hypnotics and have little to offer over
benzodiazepines
Benzodiazepine metabolism
- Most benzodiazepines undergo phase I metabolism (oxidation,
reduction, hydrolysis and demethylation by CYP450). - Phase II metabolism (conjugation) - lorazepam, oxazepam and
temazepam.
what are antipsychotics
Drugs that treat psychosis
Antipsychotics have affects on what types of neurotransmitters
Dopamine
Acetylcholine
histamine and sertonin pathways
Classification of antipsychotics
Broadly classified into two major groups - first generation antipsychotics
(FGAs) and second generation antipsychotics (SGAs).
* Currently, there is an increasing shift towards “neuroscience-based
nomenclature” classification. This classification system is based on
contemporary pharmacological knowledge rather than clinical indications,
i.e. antidepressants, antipsychotics, etc.
What are the four major dopamine pathways?
Mesolimbic pathway:
Mesocortical pathway:
Nigrostriatal pathway:
Tuberoinfundibular pathway:
Which dopamine pathway controls prolactin secretion
Tuberoinfundibular pathway:
Which dopamine pathway is linked to postive symptoms - delusions,
hallucinations, disorganized speech / thinking and disorganised or
catatonic behaviour in psychosis and schizophrenia
Mesolimbic pathway:
Which dopamine pathway is linked to negative symptoms - alogia,
affective flattening, avolition etc in psychosis and schizophrenia
Mesocortical pathway:
Which dopamine pathway is controls motor movements
Nigrostriatal pathway:
Name some Characteristics of first generation antipsychotics
- Antipsychotic effects predominantly on D2 receptors (antagonism) -
requires about 70% D2 receptor occupancy for efficacy. - Extrapyramidal side effects (EPSEs): dystonia, drug-induced parkinsonism,
akathisia, tardive dyskinesia (up to 78 % D2 receptor occupancy). - Prolactin elevation.
- Muscarinic (cholinergic)-blocking properties.
- Limited efficacy on negative symptoms of schizophrenia.
Examples of first geberation antipsychotics?
chlorpromazine, haloperidol, trifluoperazine, fluphenazine,
zuclopenthixol and flupenthixol.
Characteristics of second generation antipsychotics
- Lower D2 receptor affinity.
- High serotonin / dopamine-binding ratio.
- Have greater efficacy for both positive and negative symptoms.
- Reduced risk for the development of extrapyramidal symptoms.
- Linked to the development of metabolic abnormalities more than
conventional agents. These abnormalities include: obesity (truncal),
hypercholesterolaemia / dyslipidaemia, elevated B.P and diabetes /
impaired glucose tolerance.
Examples of second generation antipsychotics?
clozapine, amisulpride, risperidone, olanzapine, quetiapine, and
aripiprazole (aripiprazole exhibits unique dopamine modulatory effects).
Name some Antipsychotic agent?
Amisulpride
Aripiprazole
Lurasidone
Olanzapine
Paliperidone
Risperidone