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MM20705
Drugs - Anxiolytics, anti-psychosis
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Give 3 classifications of anxiolytics
Benzodiazepines
, Barbiturates, Anti-depressants
Give 4 examples of benzodiazepines (Mnemonic: Anxiety &
Depression Love Order
)
Diazepam
,
Alprazolam
,
Lorazepam
,
Oxazepam
Give 2 example drugs of barbiturates (Mnemonic: Pen & Phen)
Pentobarbital
&
Phenobarbital
Benzodiazepine
&
barbiturates
Acts on
preferentially
on midbrain
ascending
reticular formation &
limbic
system
Benzodiazepine
&
barbiturates
Mainly work by
enhancing activity
of
gamma-aminobutyric acid
(
GABA
), which is the main
inhibitory neurotransmitter
in
CNS
Benzodiazepine & barbiturates
Bind
to specific
GABA A receptor subunits neuronal synapses
Benzodiazepine & barbiturates
Increases
affinity
of
GABA
receptors, which enhances
inhibitory
effects of
GABA
on
CNS
Mechanism of action of benzodiazepine & barbiturates
1.
Facilitates frequency
of
GABA-mediated chloride ion channel opening
2.
Enhances membrane hyperpolarization
3.
Decreases neuronal excitability
Benzodiazepine
&
barbiturates
Causes
depressants
effects on
CNS
-
sedation
& relief of
anxiety
Clinical indications of benzodiazepines and barbiturates
acute anxiety states
panic disorders
generalised anxiety disorders
insomnia
&
sleep disorders
for
sedation
before and during
medical
&
surgical procedures
Adverse effects of barbiturates & benzodiazepines
benzodiazepines
are safer anxiolytics than
barbiturates
CNS depressant effects
-
drowsiness
,
confusion
,
amnesia
,
impaired coordination
such as during driving
enhance depressant effect
of
other drugs
such as alcohol
tolerance
&
dependence
2 classifications of stimulates
naturally-occurring
stimulants:
Caffeine
,
nicotine
,
cocaine
synthetic
stimulants:
amphetamines
MOA of stimulants
cocaine increase
extracellular dopamine
,
serotonin
and
norepinephrine
by
binding differentially
to their
transport proteins
hence,
preventing re-uptake
into these
pre-synaptic neurons
Adverse effects of stimulants
anorexia
,
confusion
,
exhaustion
blood-borne infections
with
intravenous
usage
MI
in
pregnancy
, will
damage CNS
of
foetus
(Crack baby)
withdrawal
symptoms:
excessive
sleep,
fatigue
,
mild
depression
Clinical indications
of
anti-depressants
clinical depression
obsessive compulsive disorders
(OCD)
post-traumatic stress disorder
(PTSD)
generalised anxiety disorder
long-term
chronic pain
2 classifications
of
anti-depressants
selective serotonin reuptake inhibitor
(SSRIs) &
serotonin-norepinephrine reuptake inhibitors
(SNRIs)
Give 3 drugs of SSRIs. Mnemonic: Feel Calm Soon
Fluoxetine
,
Citalopram
,
Sertraline
Give 2 drugs of SNRIs. Mnemonic: Dual Victory
Duloxetine
,
Venlafaxine
MOA of SSRIs & SNRIs
SSRIs are
highly selective
, blocking the
serotonin transporter
, resulting in
acute increase serotonergic activity
SNRIs & TCAs (
Tricyclic anti-depressants
) selectively block
norepinephrine
&
serotonin transporter
, resulting in
acute increase
in
serotonergic
&
adrenergic synaptic activity
Adverse effects of SSRIs & SNRIs
SSRIs:
Well-tolerated
but can cause
anti-cholinergic
effects (
dry mouth
,
blurred vision
,
constipation
) &
sexual dysfunction
SNRIs: causes
anti-cholinergic
effects
TCAs: causes
weight gain
,
arrhythmias
,
seizures
when
overdose
Clinical indication of anti-psychotics
Schizophrenia
&
schizoaffective
disorders
acute mania
in
bipolar
disorders
major depressive
disorders with
psychotic features
severe agitation
Classifications of anti-psychotics with 3 example drugs each
1st
gen (typical):
Phenothiazines
,
Thioxanthene
, Butyrophenone
2nd
gen (atypical):
Clozapine
,
Olanzapine
,
Risperidone
MOA of anti-psychotics
blocks
dopamine
receptors, specifically
D2
receptors in various areas of brain
this helps regulate the
excessive dopamine activity
which contributes to psychotic symptoms:
hallucinations
,
delusions
,
disorganised thinking
some anti-psychotics influences other
neurotransmitter systems
, including:
serotonin
,
glutamate
,
norepinephrine
difference between 1st gen & 2nd gen anti-psychotic drugs
1st
gen block
D2
dopamine
receptors, while 2nd gen blocks
D2
dopamine
and
serotonin
receptor antagonist action
1st
has more
side effects
than
2nd gen
1st
gen is
better
to
treat
+ve
symptoms, while
2nd
gen can treat
+ve
&
-ve symptoms
of
schizophrenia
Adverse effects of anti-psychotic drugs
high
incidence
in
extrapyramidal
side
effects
(EPS), especially in
1st
gen
anti-cholinergic
side effects
sedation
arrhythmias