Benzodiazepine

Buspirone

Barbiturate
Chloral
Hydrate

Pharm Completely absorbed from

acokin
GI tract.
etics Erratic absorption after IM
route.
Cross BBB and placenta.
Metabolised in liver.

Others
Ethanol
(Alcohol)

Rapidly absorbed from GI tract. High

lipid solubility allows rapid transport
across the BBB and results in a rapid
onset.
Widely distributed. Removal from the
brain occurs via redistribution to the
other tissues results in short
duration of action.
Metabolized in liver.
Excretion via the renal route.
1. CNS
CNS depression, ranging from mild
sedation to surgical anesthesia
Sedation, relief of anxiety, ataxia,
hypnosis, anticonvulsant action,
anesthesia.
2. Respiratory depression
Suppress the hypoxic and
chemoreceptor response to CO2.
3.Enzyme induction
Induce CYP450 enzymes in the liver.
Chronic administration can diminish
the action of many drugs that are
dependent on CYP450 metabolism
to reduce their concentration

Pharm 1. CNS
acolog Sedation and hypnosis
ical
depending on the dose,
action
increase the total duration
s
of sleep.
Decrease anxiety
(alprazolam)
Muscle relaxation
(clonazepam)
Anticonvulsant activity
(clonazepam,
flunitrazepam, nitrazepam,
triazolam, bromazepam,
nordazepam).
Anterograde amnesia
Development of tolerance to
anticonvulsant activity
limits its uselfulness in
seizures.
2. CVS
Minor effect.Preanesthetic
dose decreases : BP
Preanesthetic dose
increases : heart rate IV
diazepam increases
coronary flow
3. GIT
Markedly decreased
nocturnal gastric acid
secretion.
Mecha Benzodiazepines attach to

nism
specific site on the GABA

of
receptor/chloride channel
action
complex by opening
Chloride ion channels in
the cells.
GABA binds to them, they
change shape slightly to
allow ions to pass through
their central channel. This
channel mainly allows
negatively charged
chloride ions to enter the
neuron, thus reducing its
excitability.
Uses Anxiolytic Hypnotic
Used for

Anticonvulsant Muscle
anxiety
relaxant
(chronic
treatment
Safe when taken for their
of GAD)
intended use and not used
Efficacy
in excess
comparab
Administered: Oral, SL, IM,
le to
IV.
benzodiaz
epines.
Lacks of
anticonvu

Barbiturates potentiate GABA action

Barbiturates bind to the receptor at
Beta subunit.

Induction of surgical anesthesia

(Thiopentone IV).
Treatment of epilepsy
Use as sedative-hypnotic agents.
Treatment of hyperbilirubinemia and
kernicterus in the neonate.

Relatively Has an
safe,
anxiolytic
inducing
and
sleep in a
sedative
half hour
effect.
and
CNS
lasting
depression
about 6h.
producing
Used
sedation
mainly in
and
patients
hypnosis
when
with

lsant
property.
shows less
interferen
ce with
motor
functions

Durati Long acting

on
Intermediate acting
Short acting

failed to
increase
other
dosage.
drug.
Given orally.
Disadvanta
ges
Irritant to
skin and
mucosa
and has
unpleasa
nt taste.

Advers Acute toxicity: Bzs in acute

e
overdose are considerably
effects
less dangerous than other
sedative-hypnotic drugs.
Cause prolonged sleep,
without serious depression
of respiration or
cardiovascular.
Memory impairment:
drowsiness, confusion,
amnesia
Tolerance
Dependence (both physical
and psychic)
Abrupt withdrawal may
produce rebound insomnia
Psychomotor dysfunction
Tolera Tolerance develop
nce, Physical dependence and
depen
abuse
dence
and
Withdrawal symptoms Bzs
withdr Tachycardia, Tremors,
awal
Severe headache, Weight
loss, Confusion, Insomnia,
Agitation (Anxiety),
Hyperreflexia, Convulsions
(in severe withdrawal)

Psycho Relaxation
logical Drowsy
Effects Distracts you from other
problems going on around
you and in your own life
Effects Unconsciousnesso
in
Respiratory depressiono
Overd Collapse of heart and heart
ose
functions
CNS depression
Shallow breathing
Drug Potentiate the effects of CNS
Intera
depressants e.g. alcohol.
ctions

Chest pain Similar to Bzs: hangover---dizzy,

drowsiness, amnesia, impaired
Tachycardia,
judgment, disorientation, Tolerance,
palpitatio
Dependence.
ns

Acute
poisoning: respiratory
Pupillary
depression and circulatory shock
constricti
(fatal).
on
Can cross the placental barrier during
Dizziness,
pregnancy and secrete to breast
nervousn
milk.
ess,
tinnitus
GI distress

Tolerance develop
Physical dependence and abuse
Withdrawal symptoms: anxiety,
insomnia, and convulsions (in
severe withdrawal)

Ethanol or
Alcohol
withdrawal
DOC for
alcohol
withdrawal
is bzs.
Carbamazepi
nes as
secondary
treatment
in treating
convulsive
episodes
during
withdrawal
.

Coma
Severe respiratory depression
Hypotension leading to cardiovascular
collapse
Renal failure.
Potentiate the effects of CNS
depressants and alcohol.
Eg. Of enzyme induction
The following clinical scenario
describes a case of drug interaction:
A 68-year-old white woman taking
warfarin, whose condition was
previously well controlled on a
stable dose, has recently been
difficult to anticoagulate to a
therapeutic level. Review of her
medications reveals the addition of
daily barbiturates for insomnia. The
physician recognizes the drug
interaction between warfarin and
barbiturate as a potential cause and
switches the patient to an alternate
hypnotic and sedative agent.

With other
sedative
agents and
can
produce
more
severe CNS
depression.
Chronic
consumpti
on can
lead to
liver
disease,
gastiritis
and
nutritional
deficiency
and
cardiomyo
pathy (a
consequen
ce of
heavy

drinking).
Excretion
mainly via
kidney.
Intoxic Taken alone in overdose
ation
rarely cause severe
complications.
Take more than the
prescribed dose can
simply feel drowsy and
sleep for a few hours.
Taken in overdose together
with alcohols and CNS
depressant drugs can
produce
Very dangerous effects
(potentiate CNS and
respiratory depressants
effects).
Antag Flumazenil, a GABA receptor
onist
antagonist, can rapidly
reverse the effects of Bzs
(IV only).
Rapid onset, short duration
of action (half life: 1 hour).