Sedatives

last authored:
last reviewed:

 

 

Caution surrounding Psychotropics

Effect size of antidepressants for anxiety = 1.2

Effect size of antidepressants for depression = 0.7

 

Introduction

return to top

 

 

Types of Sedatives

Likely the most common sedative family worldwide is the benzodiazepines (BZPs). In general population in Canada, 8% have used benzos in the past year; 2% have used them for over a year.

 

BZPs differ from each other primarily regarding speed of onset and duration.

Other sedatives include barbituates and buspirone.

 

 

 

Uses

should be given for at most weeks or months due to potential for dependence and side effects.

 

 

Side Effects

long term use can result in cognitive decreases

 

 

Adverse Drug Reactions

Overdose: give flumazinil

 

Interactions

There are varying effects of alcohol on benzo concentrations.

Synergistic pharmacological interactions occur.

 

 

Overuse, misuse, abuse

People with the below risk factors should be prescribed BZPs extremely carefully, if at all, given the risk of abuse:

Specific drugs also carry increased risk for abuse, due to rapid onset/offset and euphoriant effects. These include:

 

 

Withdrawal

 

Symptoms of BZD withdrawal syndrome:

 

risk factors:

lose dose: tachycardia, hypertension, insomnia

high dose: seizures, psychosis

 

Stopping Treatment

Tapering often takes place over months, with a 10% reduction in dose per week. It may be challenging to assess whether symptoms are related to anxiety or to the taper.

 

To stop treatment, in general you should taper off with all psychotropics.

Go really slow at the end of the taper (asymptotic)

get patient involved in drafting the schedule

have a treatment plan for break-through emergence of symptoms (PRNs)

switch to long-acting BZP prior to taper (ie clonazapam or diazepam)

 

Benzo agonists

facilitate GABA action: zolpidem, zaleplon, eszopiclone

antagonists: used in overdose: flumazenil

inverse agonists: act as negative allosteric modulators of GABA receptors

 

 

Mechanism of action

Benzodiazepines bind to chloride channels in neurons, causing conformational changes that increase GABA binding and subsequent chloride channel opening. This leads to hyperpolarization and inhibits CNS activity.

 

 

 

Pharmacokinetics

down-regulation of GABAA receptors occurs a lot

acts on the GABAA receptor

 

   
  • onset
  • hypnotic utility
  • abuse potential
  • lipophilicity
  • duration of effect
  • onset/offset of effect
  • half-life
  • dosing frequency
  • risk of accumulation
  • withdrawal syndrome
  • hepatic metabolism
  • specific populations: elderly, hepatic impairment
   
   

 

Phase I capacity decreases with age, meaning half life will be increased in the elderly.

Non-phase I metabilized drugs: lorazepam, o, tamazapam

 

 

Buspirone

A sedative-hypnotic

 

Uses

Mechanism

adverse effects

contraindications

 

 

 

Resources and References

return to top