Anxiolytics & Sedatives/Hypnotics

Question 1

Diazepam

Answer 1

• Benzodiazepine.
• Muscle relaxant and anticonvulsant.
• Administered orally, IV or IM.
• Metabolized in the liver, excreted in urine.
• Side effects include acute toxicity (OD), sedation, confusion, impaired coordination, rebound insomnia, tolerance and dependence.
• 2-4 weeks use optimal, withdrawal requires tapering.

Question 2

Temazepam

Answer 2

• Benzodiazepine.
• Used for insomnia.
• Administered orally, IV or IM.
• Metabolized in the liver, excreted in urine.
• Side effects include acute toxicity (OD), sedation, confusion, impaired coordination, rebound insomnia, tolerance and dependence.
• 2-4 weeks use optimal, withdrawal requires tapering.

Question 3

Zolpidem

Answer 3

• New generation BZDs.
• Short acting with no active metabolites.
• Less daytime sedation, tolerance and dependence.

Question 4

Flumazenil

Answer 4

• Competitive antagonist of BZDs.
• Used in BZ overdose and to reverse anaesthesia.
• Administered via IV.
• Adverse effects include anxiety, confusion and nausea.

Question 5

Phenobarbital

Answer 5

• non-selective CNS depressant used as an anticonvulsant in children
• positive allosteric modulator - enhances GABA transmission by increasing GABA pore opening duration
• inhibits glutamate transmission
• ADRs: dangerous in OD (resp depression), tolerance, dependence, drug-drug interactions, CYP inducer, decreases plasma concentration of steroids, OCs and warfarin. - Given IV for status epileptics.
• Broad spectrum AED.

Question 6

What is generalized anxiety disorder (GAD)?

Answer 6

General symptoms of motor tension, autonomic hyperactivity, etc. for > 1 month.

Question 7

What is phobic anxiety?

Answer 7

• Simple phobias such as agoraphobia

- Social phobias

Question 8

What is panic disorder?

Answer 8

Characterized by acute attacks of fear as compared to the chronic presentation of GAD.

Question 9

What are obsessive-compulsive behaviours?

Answer 9

Patients show repetitive behaviours (compulsions) and ideas (obsessions).

Question 10

What brain regions are affected by GAD?

Answer 10

• Increase metabolic rates in cerebral cortex, cerebellum & thalamus
• Decreases serotonergic activity in dorsal raphe nucleus
• Decreased GABA activity in frontal cortex
• Overactivity of noradrenergic neutrons in locus coeruleus

Question 11

What are the manifestations of anxiety?

Answer 11

• Verbal: pt complains of being anxious, nervy, edgy
• Somatic and autonomic: pt is restless and agitated, tachycardia, increased sweating, weeping and often GI symptoms
• Social: interference with normal productive activities

Question 12

Anxiety can be…

Answer 12

Drug induced or medical.

Question 13

What are the medical causes of anxiety and how does this affect treatment of anxiety?

Answer 13

• Respiratory
• Endocrine
• Cardiovascular
• Metabolic
• Neurologic
  Treat cause first then anxiety.

Question 14

What drugs can induce anxiety and how to you treat?

Answer 14

• Stimulants: amphet, cocaine, TCAs, caffeine
• Sympathomimetics: ephedrine, Ad, NA
• Anticholinergics/Antihistaminergics: benztropine
• Dopaminergics: Amantadine, bromocriptine, L-Dopa, carbidopa/levodopa
  Treat by correcting the pt’s drug regime.

Question 15

What drugs can be used to treat anxiety?

Answer 15

Anxiolytics - sedatives and hypnotics

• ADs - most widely used
• BZDs
• Propranolol (suppresses HR, effective in acute anxiety symptoms)
• Recreational - alcohol (not recommended)