Drugs - Anxiolytics, anti-psychosis

Cards (25)

  • Give 3 classifications of anxiolytics
    Benzodiazepines, Barbiturates, Anti-depressants
  • Give 4 examples of benzodiazepines (Mnemonic: Anxiety & Depression Love Order)

    Diazepam, Alprazolam, Lorazepam, Oxazepam
  • Give 2 example drugs of barbiturates (Mnemonic: Pen & Phen)
    Pentobarbital & Phenobarbital
  • Benzodiazepine & barbiturates
    Acts on preferentially on midbrain ascending reticular formation & limbic system
  • Benzodiazepine & barbiturates
    Mainly work by enhancing activity of gamma-aminobutyric acid (GABA), which is the main inhibitory neurotransmitter in CNS
  • Benzodiazepine & barbiturates
    Bind to specific GABA A receptor subunits neuronal synapses
  • Benzodiazepine & barbiturates
    Increases affinity of GABA receptors, which enhances inhibitory effects of GABA on CNS
  • Mechanism of action of benzodiazepine & barbiturates
    1. Facilitates frequency of GABA-mediated chloride ion channel opening
    2. Enhances membrane hyperpolarization
    3. Decreases neuronal excitability
  • Benzodiazepine & barbiturates
    • Causes depressants effects on CNS - sedation & relief of anxiety
  • Clinical indications of benzodiazepines and barbiturates
    • acute anxiety states
    • panic disorders
    • generalised anxiety disorders
    • insomnia & sleep disorders
    • for sedation before and during medical & surgical procedures
  • Adverse effects of barbiturates & benzodiazepines
    • benzodiazepines are safer anxiolytics than barbiturates
    • CNS depressant effects - drowsiness, confusion, amnesia, impaired coordination such as during driving
    • enhance depressant effect of other drugs such as alcohol
    • tolerance & dependence
  • 2 classifications of stimulates
    • naturally-occurring stimulants: Caffeine, nicotine, cocaine
    • synthetic stimulants: amphetamines
  • MOA of stimulants
    • cocaine increase extracellular dopamine, serotonin and norepinephrine
    • by binding differentially to their transport proteins
    • hence, preventing re-uptake into these pre-synaptic neurons
  • Adverse effects of stimulants
    • anorexia, confusion, exhaustion
    • blood-borne infections with intravenous usage
    • MI
    • in pregnancy, will damage CNS of foetus (Crack baby)
    • withdrawal symptoms: excessive sleep, fatigue, mild depression
  • Clinical indications of anti-depressants
    • clinical depression
    • obsessive compulsive disorders (OCD)
    • post-traumatic stress disorder (PTSD)
    • generalised anxiety disorder
    • long-term chronic pain
  • 2 classifications of anti-depressants
    selective serotonin reuptake inhibitor (SSRIs) & serotonin-norepinephrine reuptake inhibitors (SNRIs)
  • Give 3 drugs of SSRIs. Mnemonic: Feel Calm Soon
    Fluoxetine, Citalopram, Sertraline
  • Give 2 drugs of SNRIs. Mnemonic: Dual Victory
    Duloxetine, Venlafaxine
  • MOA of SSRIs & SNRIs
    • SSRIs are highly selective, blocking the serotonin transporter, resulting in acute increase serotonergic activity
    • SNRIs & TCAs (Tricyclic anti-depressants) selectively block norepinephrine & serotonin transporter, resulting in acute increase in serotonergic & adrenergic synaptic activity
  • Adverse effects of SSRIs & SNRIs
    • SSRIs: Well-tolerated but can cause anti-cholinergic effects (dry mouth, blurred vision, constipation) & sexual dysfunction
    • SNRIs: causes anti-cholinergic effects
    • TCAs: causes weight gain, arrhythmias, seizures when overdose
  • Clinical indication of anti-psychotics
    • Schizophrenia & schizoaffective disorders
    • acute mania in bipolar disorders
    • major depressive disorders with psychotic features
    • severe agitation
  • Classifications of anti-psychotics with 3 example drugs each
    1st gen (typical): Phenothiazines, Thioxanthene, Butyrophenone
    2nd gen (atypical): Clozapine, Olanzapine, Risperidone
  • MOA of anti-psychotics
    • blocks dopamine receptors, specifically D2 receptors in various areas of brain
    • this helps regulate the excessive dopamine activity which contributes to psychotic symptoms: hallucinations, delusions, disorganised thinking
    • some anti-psychotics influences other neurotransmitter systems, including: serotonin, glutamate, norepinephrine
  • difference between 1st gen & 2nd gen anti-psychotic drugs
    • 1st gen block D2 dopamine receptors, while 2nd gen blocks D2 dopamine and serotonin receptor antagonist action
    • 1st has more side effects than 2nd gen
    • 1st gen is better to treat +ve symptoms, while 2nd gen can treat +ve & -ve symptoms of schizophrenia
  • Adverse effects of anti-psychotic drugs
    • high incidence in extrapyramidal side effects (EPS), especially in 1st gen
    • anti-cholinergic side effects
    • sedation
    • arrhythmias