Benzodiazepines are a class of drugs commonly used to treat anxiety. They work by enhancing the effects of the neurotransmitter GABA at GABAA receptors in the brain. The most commonly prescribed benzodiazepines include diazepam, alprazolam, lorazepam, and clonazepam. While effective for treating anxiety, benzodiazepines can cause side effects like sedation and memory impairment. They also carry risks of tolerance, dependence, and withdrawal symptoms with long-term use. Benzodiazepines should only be used short-term to treat severe anxiety, insomnia, or muscle spasms, and are not recommended for mild or occasional

1. Anxiolytics
Presented by-
Afreen Hashmi
B.Pharm 3rd year
Roll no.1439150030
Guided by-
Mr. Anand Srivastava
Assistant Professor
Mahatma Gandhi Institute of
Pharmacy
MAHATMA INSTITUTE OF PHARMACY
LUCKNOW

2. OUTLI
NE
• Anxiety – Symptoms of anxiety
• Treatment of anxiety
• Antianxiety drugs
• Benzodiazepines
• Structure-activity Relationship(SAR)
• Mode of Action
• Most commonly prescribed
benzodiazepines
• Use of benzodiazepines
• pharmacokinetic
• Pharmacodynamics
• Adverse effects
• Side effects
• Tolerance
• Dependence
• Indications
• Interactions
• Effects on Pregnancy
• Conclusions

3. presentation
A
I have a tough exam
I have an important interview
I have a tough exam
I have an important interview
ANXIETY
 I Have a Presentation
 I Have a Tough Exam
 I Have an Important Interview
Should I be anxious ?

4. 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
ANXIETY

5. SYMPTOMS OF ANXIETY
o Psychic or emotional state.
o Somatic or physical symptoms.

6. EMOTIONAL SYMPTOMS OF
ANXIETY
• Irrational and excessive fear and wor
• Irritability
• Restlessness
• Trouble concentrating
• Feeling tense

7. PHYSICAL SYMPTOMS OF
ANXIETY
* Tachycardia
* sweating
* fatigue
* weakness
* agitation
* restlessness
* sleep disturbances

8. TREATMENT OF ANXIETY
Psychotherapy (Cognitive
behavioral therapy)
 Anxiolytics

9. ANXIOLYTICS
 An anxiolytic (also antipanic or antianxiety
agent) is a medication or other intervention
that inhibits anxiety .
Antianxiety agents, formly called minor
transquilisers and also known as anxiolytics
and tensiolytics, are used to control neuroses
and stress.
Drowsiness is the most common untoward
effect of antianxiety agents and also
stimulation of apetite.
An axiogenic or panocogenic substances is

10. ANTIANXIETY DRUGS - 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.

11. 1.Benzodiazepines –
Diazepam, Chlordiazepoxide,
Oxazepam
Lorazepam, Alprazolam.
2. Azapirones - Buspirone, Gepirone,
Ispapirone.
3. Sedative antihistaminic - Hydroxyzine
4. β blocker - Propranolol
Classification

12. WHAT ARE
BENZODIAZEPINES?
• Benzodiazepines are a group of drugs that
act on the central nervous system. Used to
treat anxiety, stress, sleeping problems and
other disorders.
Brand Generic
Valium Diazepam
Xanax Alprazolam
Ativan Lorazepam
Librium Chlordiazepoxide

13. SAR
 An electron withdrawing group such as Cl, Br,
CN at position-7 is required for activity.
 Position 6, 8 and 9 should not be
substituted.
 A phenyl at position-5 promotes activity. If
the phenyl group is ortho(2`) or diortho(2`,6`)
substituted with electron-attracting
substituent, activity is increased. On the other
hand, para substitution decreases activity
greatly.
Saturation of the 4,5 double bond or shift of

14. Replacement of the carbonyl function with 2
hydrogen in the 2-position gives medazepam,
less potent the diazepam.
Alkyl substitution at the 3-position decreases
activity.
Replacement of 1 of the hydrogen with a OH
group on 3-position lowers activity on the one
hand and aids elimination on the other hand.
The presence or absence of the 3-hydroxyl is
important pharmacokineticallly.
Compounds without the hydroxyl are non-
polar have long half-lives and undergo hepatic
oxidation.
Compounds with the hydroxyl are much more
polar and are readly converted to theexcreted

15. SITE AND STRUCTURE OF
ACTION
Site of action is the GABAA receptor
Structure of GABAA receptor
- Comprised of 5 subunits
o 2 α subunits (to which GABA binds)
o 2 β subunits (to which barbiturates
bind)
1 γ subunit (to which benzodiazepines
bind)

17. MODE OF ACTION
 BZD act by inhancing presynaptic/postsynaptic
inhibition through a specific BZD receptor which
is an integral part of the GABAa receptor
chloride channel complex.
The subunit of this complex form a pentameric
transmembrane anion channel gated by the
primary ligand(GABA), and modulated by
secondary ligand which includes BZDs.
The binding site for GABA is located on the
beta subunit, while alpha/gama subunit
interface carries the BZD binding site.
The modulatory BZD receptor increases the
frequency of chloride channel opening induced

18. BZD do not themselves increase chloride ion
conductance; have only GABA facilatatory but
no GABAmimetic action.
BZD-agonist inhance GABA induce
hyperpolarization(due to influx of
chloride ion), and decrease firing rate of
neurons.
BZD-inverse agonist like
DMCM(dimethoxy ethyl carbomethoxy
beta carboline) inhibit GABA action and
or convulsants.
The competitive BZD-antagonist

19. MOST COMMONLY PRESCRIBED
BENZODIAZEPINES
(Benzodiazepines are classified as Controlled Drugs
in some countries.)
 Diazepam (Valium,
Anxicalm)
 Alprazolam (Xanax)
 Lormetazepam (Noctamid)
 Nitrazepam (Mogadon)
 Clonazepam
 Flurazepam (Rohypnol)
 Temazepam (Nortem)
Lorazepam (Ativan)
Midazolam

21. USES OF
BENZODIAZEPINES
Chlordiazepoxide and diazepam were
introduced around 1960 as antianxiety
drugs.
It is used for the control of anxiety and
tension states, the relief of muscle
spasm.
Diazepam is also helpful in combating
withdrawal symptoms in chronic
alcoholics.
It has shown effectiveness in certain

22. BENZODIAZEPINES
 Pharmacokinetics
 Pharmacodynamics
 Adverse Effects
 Side Effects of Benzodiazepines

23. Mostly oral, some available
parenterally.
Peak plasma concentrations are
achieved
in about one hour
Absorption -
Distribution -
Metabolism -
Elimination -
Metabolized in liver
Through urine
 Pharmacokinetics

24. Produces sedation and promotes good sleep (w/o
anxiolytic, anticonvulsant, or muscle-relaxant effects).
Memory is affected.
Flumazenil reported to reverse memory impairments
and overdoses.
Flumazenil also reported to improve memory and
learning, thus suggesting a possible role of
endogenous benzo’s in memory function
 Pharmacodynamics

25.  Drowsiness, dizziness, and
nausea at therapeutic doses.
 Severe nausea and vomiting
greatly limit overdoses.
 Adverse Effects

26.  Side effects of
benzodiazepines
• Drowsiness & Light-headedness the next day
• Confusion & Ataxia (especially in the elderly)
• Increase in fractures -> increase in
hospitalisation
• Amnesia
• Dependence, Tolerance
• Respiratory depression (more so if taken with
alcohol or other CNS depressants) -
decreases. B.P
• Paradoxical increase in aggression
• Demotivation - Inhibition of learning
behaviour, academic performance
• Coma

27. Tolerance to the sedative and euphoric
effects are rapid, but non existent to
anti-anxiety and antipanic effects.
Toleran
ce

28. DEPENDE
NCE
Normal

ANXIOLYTIC
_________  _________________
Drowsiness/decrease reaction time

HYPNOSIS

Confusion, Delirium, Ataxia

Surgical Anesthesia

Coma

DEATH
*Dependence can develop even
following only therapeutic dosages

29. Respiratory
Depression
Coma/
Anesthesia
Sedation
Anxiolytic
Anticonvulsant
DOSE
BDZs

30. INDICATIO
NS
• Anxiety
– Short term relief (two to four weeks only) of anxiety
that is severe, disabling, or causing the patient
unacceptable stress.
• Insomnia
– Benzodiazepines should be used to treat insomnia
only when it is severe, disabling or causing the
patient extreme distress.
• Chronic Muscle Spasm or spasticity associated with MS
• Status epilepticus
• Febrile Convulsions
• Hypnotic (sleep inducing)
• Withdrawal treatment
• Panic disorder with anxiety
*THE USE OF BENZODIAZEPINES FOR SHORT TERM MILD

31. INTERACTI
ONS
• Increased Effects
with
– Alcohol
– Analgesics (Fentanyl)
– Antibacterial
(Clarithromycin,
Isoniazid)
– Antifungals
(ketokonazole,
itraconazole)
– Antipsycotics
– Antivirals
• Decreased Effects
with
– Antibacterial
(Rifampicin)
– Probenecid
– Theophylline
– Neoquinolone

32. EFFECTS ON PREGNANCY
- Benzodiazepines (and their metabolites) can
freely cross the placental barrier and accumulate
in fetal circulation.
o Administration during the first trimester can
result in fetal abnormalities.
O Administration in third trimester (close to the
time of birth) can result in fetal dependence, or
“floppy-infant syndrome”.
- Benzodiazepines are also excreted in the
breast milk

33. CONCLUSI
ON
• Benzodiazepines are safe when used within the
guidelines
• They are highly addictive even when used for short
periods
• Cause many road traffic accidents due to driving
under the influence of drugs
• They can be fatal when used with other drugs/alcohol
• Are Controlled drugs and require medical supervision
• Should be taken only by the pt they are prescribed
for.
• Directions for use should be followed exactly
• Withdrawal from long term use of Benzodiazepines is
difficult but with motivation & support is possible

34. THANK
YOU