Anxiolytics and Sedatives Flashcards
What is a barbiturate?
- CNS depressant
- Obsolete as anxiolytics
- Associated with addiction
- Used as IV induction (bipentone) agents and anti-convulsants
Name different classes of drugs which can be used to treat anxiety [symptoms] ?
- Antidepressants
- Benzodiazepines
- Z-drugs
- B-blockers
- Melatonin
- Sedating antihistamine
What are properties associated with benzodiazepines?
- Highly lipophilic
- Well absorbed orally
- Highly protein bound (95%)
- Hepatic metabolism
- Active metabolites
- Excreted as glucoronide conjugate
What are the 5 main effect of benzodiazepines?
- Anxiolytic: reduce anxiety (a2 and a3)
- Hypnotic: induce sleep (a1)
- Reduce muscle tone
- Anterograde amnesia (pros and cons)
- Anticonvulsant effect
What is the main difference between different benzodiazepines?
Duration of action
How can benzodiazepines be given?
- Orally
- IV
- Intranasal or rectal
- NOT IM
What are the short acting benzodiazepines?
- Lorazepam
- Temazepam
- t1/2: 8 - 12 hours
What are the intermediate benzodiazepines?
Flunitrazepam
What are the long-acting benzodiazepines?
Diazepam
- t1/2: 20 - 100 hours
Describe the structure of GABA(A) receptors?
- Pentameric arrangement
- 2 alpha sub units, 2 Beta sub units and 1 gamma sub unit
- Central ion channel pore
- 18 possible sub units
What do benzodiazepines bind to?
Act allosterically GABA receptors - increase frequency of opening
- Different part of GABA receptor to GABA
What can act on GABA(A) receptors?
- Benzodiazepines
- Alcohol
- General anaesthetics
- Z-drugs
What travels throught the central ion channel?
Cl-
What is flumazenil used for clinically?
- Reverse the effect of benzodiazepines
- Competitive benzodiazepine antagonist
- Short half-life compared with benzodiazepines
- May precipitate agitation and seizures
- Given IV in 100mcg increments
- Side effects of nausea and vomiting
What are Z drugs?
- Alternatives to benzodiazepines - bind to benzodiazepines on GABA receptors
- Structurally different but have a very similar pharmacodynamic profile,slightly shorter acting
Name the “Z” drugs
- Zopiclone
- Zaleplon
- Zolpidem
What is the definition of tolerance?
A physiological state characterized by a decrease in the effects of a drug with chronic administration