2015-10-12
Benzodiazepines
Anxiolytic drugs
Benzodiazepines
Alprazolam
Chlordiazepoxide
Clonazepam
Diazepam
Lorazepam
Oxazepam
Estazolam
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2015-10-12
Mechanism of action
Glutamate,
aspartate
GABA,
Glycine
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2015-10-12
BDZ facilitates GABA binding and increase the
frequency of chloride channel opening
Barbiturates increase the duration of
chloride channel opening both in the
presence and in the absence of GABA
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2015-10-12
BDZ and barbiturates are
positive allosteric modulators
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2015-10-12
Omega-1 and Omega-2 receptors
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2015-10-12
Mechanism of action
GABA – Gamma-Aminobutyric Acid
GABA is the main inhibitory transmitter in
the brain
GABA acts on two distinct types of
receptor:
GABA-A receptor – occurs mainly
postsynaptically; is directly coupled to chloride
channels
GABA-B receptor is G-protein coupled receptor
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2015-10-12
GABA
GAD – glutamic acid
decarboxylase
metabolism
- Valproic acid
- Vigabatrin
GABAtransaminase
+ Valproic acid
Succine
semialdehyde
dehydrogenase
-Valproic acid
GABA metabolism
Tiagabine
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2015-10-12
You know that:
Activation of GABA-B-receptor causes
closing Ca channel and openinig and
increasing K conductance.
How does it influence the skeletal
muscle?
BACLOFEN
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2015-10-12
Oxazepam, temazepam
Task
• Please list the important points that you
should consider before prescribing BDZ.
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2015-10-12
β-adrenoceptor antagonist:
Propranolol or atenolol
Stage fright or performance anxiety refers to an
anxiety, fear or persistent phobia related to
performance in front of an audience or camera.
This form of anxiety can precede or accompany
participation in any activity involving public selfpresentation.
It has numerous manifestations:
Fluttering or pounding heart
Tremor in hands and legs
Diarrhea
Facial nerve tics
Dry mouth
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2015-10-12
Insomnia occurs if there is
Difficulty initiating sleep –taking 30
minutes or more to fall asleep
Difficulty maintaining sleep
Sleep disturbance at least 3 night a
week
Significant impairment of daytime
functioning caused by the disrupted
sleep
Classification of insomnia
Transient insomnia
Short-term insomnia
Chronic insomnia
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2015-10-12
Psychobehavioral interventions
(also known as sleep hygiene)
Go to bed with the intention of going to
sleep and only when sleepy
Do not use the bed for anything except
sleep and sexual activity
Create a dark, comfortable bedroom
environment
Establish a bedtime ritual
Do not spend longer than
10 minutes lying in bed trying
to sleep
Psychobehavioral interventions
(also known as sleep hygiene)
Get up at the same time every morning,
including weekends, regardless of how you
slept
Do not nap during the day
Decrease excessive time in bed
Decrease or eliminate the use of caffeine
and alcohol
Increase exercise and aerobic fitness
Avoid nicotine before bedtime
Do not go to bed hungry; try a light snack
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2015-10-12
Drugs act on
GABA-A
GABA-B
Disorder
BDZ-1
Drugs used in disorders
In status epilepticus
In panic disorders
In generalized anxiety disorder
In sleep-onset insomniae
(difficulty falling asleep)
In sleep-maintenance insomnia
(difficulty staying asleep)
In jet-lag
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2015-10-12
Differences
Diazepam
Midazolam
Mechanism of action
Pharmacokinetic
Therapeutic uses
alprazolam
buspiron
Mechanism of
action
Onset of action
Therapeutic uses
Side effects
Differences
midazolam
zolpidem
Mechanism of action
Therapeutic using
Side effects
diazepam
phenobarbital
Mechanism of
action
Therapeutic using
Side effects
Pharmacokinetic
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2015-10-12
Differences
lorazepam
alprazolam
Mechanism of action
Pharmacokinetic
Therapeutic uses
alprazolam
hyroxizine
Mechanism of
action
Onset of action
Therapeutic uses
Side effects
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