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1. Benzodiazepines.
2. Buspirone.
3. Barbiturates
4. β-Blockers
5. Sedative antihistamines
6. Antidepressants
7. antiepileptic drugs
8. Zolpidem.( for insomnia)
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Benzodiazepines. This is the most important group, used as anxiolytic and
hypnotic agents. Anxiolytics, particularly the benzodiazepines, have
been termed ‘minor tranquillisers’.
1. Buspirone. This 5-HT1A receptor agonist is
anxiolytic but not appreciably sedative.
2. β-Adrenoceptor antagonists (e.g.
propranolol ) These are used to treat some
forms of anxiety, particularly where physical
symptoms such as sweating, tremor and
tachycardia are troublesome. Their
effectiveness depends on block of peripheral
sympathetic responses rather than on any
central effects. They are sometimes used by
actors and musicians to reduce the symptoms
of stage fright.
3. Barbiturates. These are now largely
obsolete, superseded by benzodiazepines.
Their use is now confined to anaesthesia and
the treatment of epilepsy .
4.
5. Sedative antihistamines such as
diphenhydramine & promethazine, are
sometimes used as sleeping pills, intended to
improve children's sleep patterns.they have
antagonistic effect on H1 –receptor in the
brain.
6.
7. Antidepressants as Selective serotonin
reuptake inhibitors such as fluoxetine and
sertraline are used to treat certain anxiety
disorders.Their action in this context appears
to be independent of their antidepressant
effects.
8.
9. Various drugs that enhance the effects of
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GABA, developed primarily as antiepileptic
drugs ,may also be effective in treating
anxiety disorders ,They include gabapentin ,
and valproate.
10.
11. Zolpidem. This hypnotic acts similarly
to benzodiazepines, although
chemically distinct, but lacks
appreciable anxiolytic activity.It is
approved for the short-term (usually
about two to six weeks) treatment
of insomnia.
Benzodiazepines
Benzodiazepines cause:
1. reduction of anxiety and aggression
2.sedation, leading to improvement of insomnia Although { long-term
use of benzodiazepines as sleeping pills is undesirable, owing to
.
3 Benzodiazepines decrease the time taken to get to sleep, and increase
the total duration of sleep, Both effects tend to decline when
benzodiazepines are taken regularly for 1-2 weeks. Long-acting drugs
such as nitrazepam are no longer used as hypnotics.
4.muscle relaxation and loss of motor coordination ( clonazepam)
5.suppression of convulsions (antiepileptic effect) (e.g.
Clonazepam , diazepam ).
Side effects of benzo..
These may be divided into:
1. toxic effects resulting from acute overdosage
2. unwanted effects occurring during normal therapeutic use
3. tolerance and dependence
4. the appearance of a benzodiazepine withdrawal syndrome when the
benzodiazepines are stopped or the dose is reduced after long-term usage.
3
• The withdrawal symptoms may include anxiety & irritability
• sweating
• tremor
• sleep disorders
Side effects of benzo..
1. Drowsiness & confusion
2. amnesia .
3. impaired coordination, which considerably affects manual skills such as
driving performance.
Buspirone
Buspirone is a partial agonist at 5-HT1A receptors is used to treat various anxiety
disorders. It also binds to dopamine receptors, but it is likely that its 5-HT-related
actions are important in relation to anxiety suppression (e.g. ipsapirone).
Buspirone has side effects quite different from those of benzodiazepines. It does
not cause sedation or motor incoordination, nor have withdrawal effects been
reported.
side effects are nausea, dizziness, headache and restlessness, which generally seem
to be less troublesome than the side effects of benzodiazepines.
BARBITURATES
Barbiturates induce a high degree of tolerance and dependence. They also strongly
induce the synthesis of hepatic cytochrome P450 and conjugating enzymes, and
thus increase the rate of metabolic degradation of many other drugs.
OTHER POTENTIAL ANXIOLYTIC DRUGS
Antidepressants: Selective serotonin reuptake inhibitors
such as fluoxetine and sertraline are used to treat certain
anxiety disorders( including obsessive compulsive disorder
and panic). Their action in this context appears to be
independent of their antidepressant effects.
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Corticosteroids
barbiturates accelerate metabolism of corticosteroids
.
Coumarins
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barbiturates accelerate metabolism of coumarins .
Digitoxin
barbiturates accelerate metabolism of digitoxin .
Doxycycline
barbiturates accelerate metabolism of doxycycline .
Metronidazole
barbiturates accelerate metabolism of metronidazole .
Progestogens &oestrogenes
barbiturates accelerate metabolism of prog& oestro..( reduced
contraceptive
effect(
Propranolol
barbiturates possibly reduce plasma concentration of propranolol
Clonazepam
phenobarbital often reduces plasma concentration of clonazepam
Folates
plasma concentration of phenobarbital possibly reduced by folates
Rifampicin
phenobarbital possibly reduces plasma concentration of rifampicin
Valproate
plasma concentration of phenobarbital increased by valproate (also plasma
concentration of valproate reduced)
Alcohol
increased sedative effect when barbiturates given
with alcohol .
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Notes on hypnotics ('sleeping tablets') :
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