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ANTIANXIETY DRUGS
Mr. Mangesh Bansod
Asst. Professor
SDDVCPRC, Panvel
ANXIETY
 It is an emotional state, unpleasant in nature, associated
with uneasiness, discomfort and concern or fear about
some defined or undefined future threat.
 Some degree of anxiety is a part of normal life.
 Treatment is needed when it is disproportionate to the
situation and excessive.
 Some psychotics and depressed patients also exhibit
pathological anxiety.
 Cardiac neurosis (unfounded fear of heart disease—
palpitation, functional precordial pain); g.i. neurosis
(fixation on bowel movement, distention, reflux, acidity);
social anxiety (fear of being observed and evaluated by
others); obsessive-compulsive disorder (OCD), post-
traumatic stress disorder and various forms of phobias are
some specific types of anxiety disorders.
ANTIANXIETY DRUGS
 These are an ill-defined group of drugs, mostly mild
CNS depressants, which are aimed to control the
symptoms of anxiety, produce a restful state of
mind without interfering with normal mental or
physical functions.
 The anxiolytic-sedative drugs differ markedly from
antipsychotics, and more closely resemble
sedative-hypnotics.
CLASSIFICATION
BENZODIAZEPINES
 Some members have a slow and prolonged action,
relieve anxiety at low doses without producing
significant CNS depression.
 At antianxiety doses, cardiovascular and respiratory
depression is minor.
 BZDs act primarily by facilitating inhibitory GABAergic
transmission.
 Adverse effects- Side effects that occur in their use to
relieve anxiety are—sedation, light-headedness,
psychomotor and cognitive impairment, confusional
state (especially in the elderly), increased appetite and
weight gain.
 The long-term use for anxiety disorders is their
potential to impair mental functions and to produce
dependence.
INDIVIDUAL BZDS RECOMMENDED FOR
ANXIETY
 1. Chlordiazepoxide - It was the first BZD to be used clinically.
Oral absorption is slow. A smooth long lasting effect is produced.
It is preferred in chronic anxiety states. BZD used to cover
alcohol withdrawal.
 2. Diazepam- It is quickly absorbed; produces a brief initial
phase of strong action followed by prolonged milder effect. It is
preferred in acute panic states and anxiety associated with
organic disease.
 3. Lorazepam - Has slow oral absorption. it is the only BZD
recommended for i.m. use. It has been preferred for short lasting
anxiety states, panic, OCD and tension syndromes, as well as for
psychosomatic diseases and for i.v. use in status epilepticus.
 4. Alprazolam - A high potency anxiolytic BZD which in
addition has some mood elevating action in mild depression. As
BUSPIRONE
 It is the first azapirone, a new class of antianxiety drugs,
distinctly different from BZDs. Buspirone:
• Does not produce significant sedation or cognitive/functional
impairment.
• Does not interact with BZD receptor or modify GABAergic
transmission.
• Does not produce tolerance or physical dependence.
• Does not suppress BZD or barbiturate withdrawal
syndrome.
• Has no muscle relaxant or anticonvulsant activity.
 Buspirone relieves mild-to-moderate generalized anxiety.
 The mechanism of anxiolytic action is on selective partial
agonistic action on 5-HT1A receptors.
 By stimulating presynaptic 5-HT1A autoreceptors, it
reduces the activity of dorsal raphe serotonergic
neurones.
 Buspirone has weak dopamine D2 blocking action but
no antipsychotic or extrapyramidal effects. A mild
mood elevating action has been noted occasionally,
which may be due to facilitation of central
noradrenergic system.
 Side effects are minor: dizziness, nausea, headache,
light-headedness, rarely excitement.
 It may cause rise in BP in patients on MAO inhibitors,
but does not potentiate CNS depressants.
 Though most patients on buspirone remain alert,
those operating machinery/motor vehicles should be
cautioned.
HYDROXYZINE
 An H1 antihistaminic with sedative, antiemetic,
antimuscarinic and spasmolytic properties.
 It is claimed to have selective anxiolytic action, but
the accompanying sedation is quite marked.
 Hydroxyzine may be used in reactive anxiety or that
associated with marked autonomic symptoms.
 Due to antihistaminic and sedative property, it is
useful in pruritus and urticaria
Β BLOCKERS
 Many symptoms of anxiety (palpitation, rise in BP,
shaking, tremor, gastrointestinal hurrying, etc.) are
due to sympathetic overactivity, and these symptoms
reinforce anxiety.
 Propranolol and other nonselective β blockers help
anxious patients troubled by these symptoms, by
cutting the vicious cycle and provide symptomatic
relief.
 They do not affect the psychological symptoms such
as worry, tension and fear, but are valuable in acutely
stressful situations (examination fear, unaccustomed
public appearance, etc.).
 They may be used for performance/situational anxiety
or as adjuvant to BZDs. The role of β blockers in
anxiety disorders is quite limited.
TREATMENT OF ANXIETY
 Anxiety is a universal phenomenon, and to experience it in
appropriate circumstances is the normal response.
 However, if anxiety symptoms are frequent and persist in a severe
form, they are a cause of distress/suffering and markedly impair
performance.
 Anxiety should be treated with drugs only when excessive and
disabling in its own right.
 The established drugs are BZDs which act quickly, while buspirone
and SSRIs/SNRIs act only after chronic treatment.
 The drug should be withdrawn as soon as it is no longer required.
 Long-term use of BZDs is of questionable merit due to cognitive
impairment and risk of dependence.
 Buspirone is a nonsedating alternative to BZDs for chronic
treatment of less severe forms of generalized anxiety.
 The SSRIs are now drugs of choice for social anxiety, OCD, eating
disorders and PTSD in which BZDs, though effective, carry abuse
potential on long-term use.
Thank you . . .

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Antianxiety agents

  • 1. ANTIANXIETY DRUGS Mr. Mangesh Bansod Asst. Professor SDDVCPRC, Panvel
  • 2. ANXIETY  It is an emotional state, unpleasant in nature, associated with uneasiness, discomfort and concern or fear about some defined or undefined future threat.  Some degree of anxiety is a part of normal life.  Treatment is needed when it is disproportionate to the situation and excessive.  Some psychotics and depressed patients also exhibit pathological anxiety.  Cardiac neurosis (unfounded fear of heart disease— palpitation, functional precordial pain); g.i. neurosis (fixation on bowel movement, distention, reflux, acidity); social anxiety (fear of being observed and evaluated by others); obsessive-compulsive disorder (OCD), post- traumatic stress disorder and various forms of phobias are some specific types of anxiety disorders.
  • 3. ANTIANXIETY DRUGS  These are an ill-defined group of drugs, mostly mild CNS depressants, which are aimed to control the symptoms of anxiety, produce a restful state of mind without interfering with normal mental or physical functions.  The anxiolytic-sedative drugs differ markedly from antipsychotics, and more closely resemble sedative-hypnotics.
  • 5. BENZODIAZEPINES  Some members have a slow and prolonged action, relieve anxiety at low doses without producing significant CNS depression.  At antianxiety doses, cardiovascular and respiratory depression is minor.  BZDs act primarily by facilitating inhibitory GABAergic transmission.  Adverse effects- Side effects that occur in their use to relieve anxiety are—sedation, light-headedness, psychomotor and cognitive impairment, confusional state (especially in the elderly), increased appetite and weight gain.  The long-term use for anxiety disorders is their potential to impair mental functions and to produce dependence.
  • 6. INDIVIDUAL BZDS RECOMMENDED FOR ANXIETY  1. Chlordiazepoxide - It was the first BZD to be used clinically. Oral absorption is slow. A smooth long lasting effect is produced. It is preferred in chronic anxiety states. BZD used to cover alcohol withdrawal.  2. Diazepam- It is quickly absorbed; produces a brief initial phase of strong action followed by prolonged milder effect. It is preferred in acute panic states and anxiety associated with organic disease.  3. Lorazepam - Has slow oral absorption. it is the only BZD recommended for i.m. use. It has been preferred for short lasting anxiety states, panic, OCD and tension syndromes, as well as for psychosomatic diseases and for i.v. use in status epilepticus.  4. Alprazolam - A high potency anxiolytic BZD which in addition has some mood elevating action in mild depression. As
  • 7. BUSPIRONE  It is the first azapirone, a new class of antianxiety drugs, distinctly different from BZDs. Buspirone: • Does not produce significant sedation or cognitive/functional impairment. • Does not interact with BZD receptor or modify GABAergic transmission. • Does not produce tolerance or physical dependence. • Does not suppress BZD or barbiturate withdrawal syndrome. • Has no muscle relaxant or anticonvulsant activity.  Buspirone relieves mild-to-moderate generalized anxiety.  The mechanism of anxiolytic action is on selective partial agonistic action on 5-HT1A receptors.
  • 8.  By stimulating presynaptic 5-HT1A autoreceptors, it reduces the activity of dorsal raphe serotonergic neurones.  Buspirone has weak dopamine D2 blocking action but no antipsychotic or extrapyramidal effects. A mild mood elevating action has been noted occasionally, which may be due to facilitation of central noradrenergic system.  Side effects are minor: dizziness, nausea, headache, light-headedness, rarely excitement.  It may cause rise in BP in patients on MAO inhibitors, but does not potentiate CNS depressants.  Though most patients on buspirone remain alert, those operating machinery/motor vehicles should be cautioned.
  • 9. HYDROXYZINE  An H1 antihistaminic with sedative, antiemetic, antimuscarinic and spasmolytic properties.  It is claimed to have selective anxiolytic action, but the accompanying sedation is quite marked.  Hydroxyzine may be used in reactive anxiety or that associated with marked autonomic symptoms.  Due to antihistaminic and sedative property, it is useful in pruritus and urticaria
  • 10. Β BLOCKERS  Many symptoms of anxiety (palpitation, rise in BP, shaking, tremor, gastrointestinal hurrying, etc.) are due to sympathetic overactivity, and these symptoms reinforce anxiety.  Propranolol and other nonselective β blockers help anxious patients troubled by these symptoms, by cutting the vicious cycle and provide symptomatic relief.  They do not affect the psychological symptoms such as worry, tension and fear, but are valuable in acutely stressful situations (examination fear, unaccustomed public appearance, etc.).  They may be used for performance/situational anxiety or as adjuvant to BZDs. The role of β blockers in anxiety disorders is quite limited.
  • 11. TREATMENT OF ANXIETY  Anxiety is a universal phenomenon, and to experience it in appropriate circumstances is the normal response.  However, if anxiety symptoms are frequent and persist in a severe form, they are a cause of distress/suffering and markedly impair performance.  Anxiety should be treated with drugs only when excessive and disabling in its own right.  The established drugs are BZDs which act quickly, while buspirone and SSRIs/SNRIs act only after chronic treatment.  The drug should be withdrawn as soon as it is no longer required.  Long-term use of BZDs is of questionable merit due to cognitive impairment and risk of dependence.  Buspirone is a nonsedating alternative to BZDs for chronic treatment of less severe forms of generalized anxiety.  The SSRIs are now drugs of choice for social anxiety, OCD, eating disorders and PTSD in which BZDs, though effective, carry abuse potential on long-term use.
  • 12. Thank you . . .