SLEEPY + SPAZ

Question 1

Benzodiazepines

Answer 1

Short (6-12 Hours)- Alprazolam, Oxazepam, temazepam
Medium (12-24 hours)- Lorazepam
Long (>24 hours)- diazepam, nitrazempam

Potentiate inhibitory effects of GABA, resulting in antiepileptic effects

Uses- Anxiety, Panic Disorder, Spasticity, Insomnia, Epilepsy

Question 2

How do Benzodiazepines effect GABA

Answer 2

Potentiate the inhibitory effects of GABA

Allows for greater CL influx decrease neuronal excitability

Bind to GABAa at allosteric site affecting muscle tone, arousal, memory formation

Question 3

Precautions and Sides Benzodiazepines

Answer 3

Elderly= Falls, increased risk of oversedation, confusion, respiratory depression

Dependence (physical and psychological) = tolerance + misuse and withdrawals if stopped sudden

Sides= Drowsy, oversedation, light headed, slurred speech

Question 4

Z-drugs for insomnia

Answer 4

Zolpidem, Zopiclone.

Short term treatment of insomnia, potentiation of GABA at GABAa receptors

Binds to alpha-1 subunit of GABAa

Less muscle relaxant and anxiolytic properties

Short acting = less daytime sedation. Reduction in sleep onset by 5-15mins. Increase sleep duration 30-60mins

Question 5

Melatonin

Answer 5

Acts on MT1 MT2 receptors in the brain the brain

Short term monotherapy in primary insomnia, poor sleep quality. Jetlag

Sides- Headache, back pain, arthralgia

Question 6

Sedating antihistamines

Answer 6

Diphenhydramine, Doxylamine

Short-term management of insomnia, shouldn’t be routinely recommended

Inverse agonists at H1 receptors- affects histamine regulating sleep + wakefulness. Stabilises receptor in its inactive state

Sides- Sedation + falls, psychomotor impairment, dizziness, anticholinergic effects (dry mouth, constipation)

Limit use to <10 days

Question 7

Muscle Relaxants

Answer 7

Dantrolene
Baclofen
Diazapam

Dose and frequency given to patient differs compared to mood disorders

Question 8

Dantrolene

Answer 8

Direct acting skeletal muscle relaxant

Lowers muscle contraction, interferes with ca from sarcoplasmic reticulum

Antagonises Ryanodine receptor.

No calcium binding to troponin; prevents actin myosin bridge

Question 8

Baclofen

Answer 8

Muscle relaxant

Structural analogue of GABA. GABAb agonist, inhibits neurotransmission at spinal level and depresses CNS

Chronic spasticity associated with MS and Spinal cord lesions

Drowsiness, withdrawals