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Benzodiazepines - Lecture notes week 8

Pharmacology 1 (University of Technology Sydney)

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Benzodiazepines
- Remember drug classes
- Mechanisms of action

Drugs used to reverse effects of other drugs

Benzo – used as sedatives

Effects depend on how much given to patients
High dose – decrease wakefulness of person

Anxiolytic – hypnotic, fall asleep

Binds to GABA A receptor, other drugs can bind to GABA A receptor too

Receptor can change in behaviour when drugs bind to them

More Cl, hyperpolarise, more -, prevents cell from activation
Benzo makes Cl enter easier through receptor – increase Cl ion influx

Inbition enhance with benzo

Don’t need to remember combinations
Target alpha and gamma subunits

Metabolites produced once benzo absorbed in thebody

Some drugs can be converted to other metabolites that can be active
So, there will be duration of effect of other metabolites plus benzo
Duration effect increases, dependent on ALL active metabolites

Long – acting BZD - want better control

Long – converted to several metabolites – duration is longer

Inverse agonist
- binds to GABA a but produce opp effects
Gaba a receptor flips between 2 states
1 state – allows binding of benzo
2nd state – allow binding on inverse agonist
When switching, can produce anxiety and convulsions

Competitive antagonist
- if some one OD with benzo
- drug used to reverse OD is flumazenil
- convulsions, because relieving activiyu on 1GABA a receptor
Z.- drugs
- unrelated to benzo
Higher affinity to GABA A
Can be reversed by. Flumazenil

Barbiturates 2

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Can interact with other drugs when competing with metabolic pathways
Interfere with levels of drugs. In blood

Clinical use of BZD

antidepressants
insomnia (sedative) can you give it long term to a patient? No, because of the side
effects, can produce tolerance and drug dependence
- benzo, not first line, sleep therapy first
produce muscle relaxation – anaesthesia
anticonvulsants – for seizures

BZD adverse effects

Acute toxicity -
Therapeutic use has undesirable effects

Tolerance and dependence

Mechanism
Withdrawal

To avoid withdrawal, taper dose over time

Overdosing with benzo, can be lethal when used with other CNS depressants
Causes respiratory distress

Flumazil ris a ttreatment because it emoves benzo at t he receptor

Emergency department care

- removing benzo from site
activated charcoal – black slurpee, small dose, not given orally, placed through nose that
goes into gutt
drawback – given charcoal within 4 hours of ingestion of benzo because benzo would be
fully absorbed then
- charcoal minimises absorption and limit side effect

summary
- different doses have different effects
- whats the mechanism of action of benzo? Binds to GABA A receptor, allows more Cl
ions to come in. even in absence of benzo, gaba will always allow Cl ions in, it causes
hyperpolarisation of Cl, result – neuronal inhibition
- metabolism depends on metabolites because. They may be active metabolites
- flumazenil reverse effects of benzo
- to minimise absorption of benz, use activated charcoal within 4 hours

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