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Major Uses
A. Anxiety state
B. Insomnia
C. Epilepsy
D. Muscle spasticity
E. Induction of amnesia
F. Adjunct in alcohol withdrawal
G. For differential psychiatric diagnosis.
Classification
According to their chemical structure, antianxiety agents can be
divided into five classes:
1.
2.
3.
4.
5.
1. Benzodiazepines
1) 3H-1,4-benzodiazepines
Chlordiazepoxide (librium)
Indications: anxiety, parenteral for
preanesthetic use, status epilepticus,
chemotherapy induced N/V, acute
alcohol withdrawl, psychogenic
catatonia, chronic insomnia
0.5, 1.2 mg tablets, oral solution
concentrate, injection
7-Chloro-2-methylamino-5-phenyl-3H1,4-benzodiazepine-4-oxide
N
Cl
CH3
NH
N
O
Synthesis
a)
b)
c)
d)
c)
d)
e)
f)
g)
h)
Diazepam (valium)
7- Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4benzodiazepin-2-one
Synthesis
Uses: It is used for the control of anxiety and tension state, the
relief of muscle spasm. It is also helpful in combating withdrawal
symptoms in chronic alcoholics.
It has shown effectiveness in certain types of epilepsy and in
labour it has many advantages over other drugs.
It is metabolized to nordiazepam which is also active with half
life of 60 hrs.
Assay: A sample (0.5) is dissolved in glacial acetic acid (80ml).
The solution is titrated with 0.1 N perchloric acid and the
end point is determined potentiometrically.
Dose: 5 to 30mg daily in divided doses.
Metabolism
Biotransformation of benzodiazepines takes place in the liver by
microsomal metabolizing system. N-demethyation gives active
metabolite with longer life than the parent drug. Diazepam and
Chlorzepate to active metabolite such as N-desmethyl diazepam
(nordiazepam).
Hydroxylation at position 3 followed by glucuronidation is the
main metabolic pathway.
Mode of action
2. Non-benzodiazepines
Alpidem (Ananxyl)
It is an imidazopyridine antianxiety agent with anticonvulsant
properties.
It is the first non-benzodiazepine anxiolytic to show selectivity for
omega-1 modulatory site of the GABA receptors.
It is similar to benzodiazepines, but is significantly better tolerated
with lower abuse potential.
3. Propandiol Carbamates
CH3
O
H2N
O
H3C
NH2
O
Meprobamate - Equanil,
Miltown, Neuramate
4. Antihistaminic
OH
Cl
Hydroxyzine - Atarax, Vistaril
5. Miscellaneous
Buspirone HCl - Buspar
5-H Agonist