mode of action and synthesis of diazepam , lorazepam and bromazepam

1. Govt. Institute of Science
“ Mode of action and Synthesis of
Diazepam, Lorazepam &
Bromazepam ”
Seminar On :
Akash Nandgaye
M.Sc. 2nd Yr (III Sem )
Organic Chemistry

2. 1. Diazepam, Lorazepam and Bromazepam are the three drugs belong
to a family benzodiazepine.
2. Benzodiazepine are anti-anxiety drug also known as minor
tranquilizer these drugs also exhibit sedative and hypnotics
properties.
3. mechanism: so the gap between the two neuron known as synapse
and synapse containing the neurotransmitter and these
neurotransmitter containing about 40% GABA.
Mode of action of benzodiazepine

3. 4. So what is GABA ? GABA means the (Gamma Amino butyric Acid) it is
the enzyme which is secreted or controlled by master gland i.e.
pituitary gland.
5. GABA is the primary neurotransmitter having inhibitory effect.
6. GABA receptor is commonly
three types i.e. GABA (A),
GABA(B), GABA(C)
7. Now the function of GABA(A)
and GABA(C) are the receptor
containing channels through
which the chloride ion passes
from outer side to inner side
where as GABA(B) is receptor
containing channel through
which K+ passes from inner side
to outer side.
8. GABA is the enzyme and bind to the receptor (A) and this is known
as GABA(A) receptor after the bind chloride channel is open and Cl
-
ion transfer from outer side to inner side.

4. 9. But sometime disturb the function of GABA(A) because some
disturbance in pituitary gland and this gland controlled the function of
GABA.
10. This time channel continuously open and hence the increase the
concentration of Cl
-
ion and some symptoms occur like fear, anxiety and
convulsion and also sometime heart rate increases.
11. This time benzodiazepine taken bind to the GABA(A) receptor and
inhibit the transformation of Cl
-
ion from outer side to inner side until
the GABA proper work or balance concentration Cl
-
ion .
12.Benzodiazepine delay or increases the signal catching time from one
neuron to other neuron.
Activity:
Diazepam- rapid- 1 hour
Lorazepam- inter. Rapid- 1-1.5 hour
Bromazepam- inter. - 1-4 hour

5. What is the beauty of below structure ?
Lorazepam bromazepam

6. Synthesis of diazepam
Diazepam is the generic name and Valium is the brand name
Diazepam was first made by Leo Sternbach and commercialized by
Hoffman La Roche and launch in 1963.
Amino benzophenone Diazepam

7. Uses
• Treatment off or certain types of seizures.
• Add on treatment for skeletal muscle.
• Symptoms caused by alcohol withdrawal such as agitation.
• Short term treatment of insomnia.
• Treatment anxiety.
• Epilepsy.
Overdoses
• Coma
• Mental confusion
• Tiredness
• Headache
• Vomiting
• Dizziness

8. Synthesis of Lorazepam
Lorazepam was initially patent in 1963 and went on sale in the united
state in 1977 and brand name is Ativan.
Lorazepam
Amino benzophenone

9. Uses
• Treat anxiety disorder.
• Alcohol withdrawal.
• Sedation.
• Seizures .
• Agitation.
• Trouble sleeping.
Overdose
• Death.
• Respiratory depression.
• Coma
• Drowsiness

10. Synthesis of Bromazepam
Patented by Roche in 1963 and brand name is Lexotan
HCl

11. Uses
• Excessive anxiety
• Tension
• Nervousness
• Short term treatment of insomnia.
Overdoses and side effect
• Dizziness
• Drowsiness
• Dry mouth
• Rapid heartbeat
• Changes in vision
• Depression
• Confusion
• Allergic reaction like rash.