Anxiolytics

ANTIANXIETY DRUGS
Anxiety

 Anxiety an emotional state, unpleasant in nature, associated with uneasiness,

discomfort and concern or fear about some defined or undefined future threat.
Antianxiety drugs

 Antianxiety drugs :- There are mostly mild CNS depressant, which are aimed to
control the symptoms of anxiety, produce a restful state of mind without
interfering with normal mental or physical functions.
Classification

 1. Benzodiazepines :- Diazepam, Chlordiazepoxide, Oxazepam, Lorazepan,

Alprazolam
 2. Azapirones :- Buspirone, Ispapirone (used in mild and
 3. Sedature Antihistaminic :- Hydroxyzine
 4. ß-Blockers :- Propranolol
" SSRIs ( Serotonin reuptake inhibition) given to cases with OCD, phobia, panic
& other severe GAD.
BENZODIAZEPAM

 BZDs have little effect on other body systems, to have lower dependence
producing Liability withdrawal syndrome is milder and delayed due to their
long half lives.
Side Effects

 Sedation, light headedness, psychomotor and cognitive impairment, vertigo,

confusional state (specially in elderly), increased appetite and weight gain.
 ° Women fail to ovulate while on regular use of BZDs
 ° Potential to produce dependence
 Mechanism of action

Alpha receptors of Stimulate GABA to Calcium ion channel Increased influx of Hyperpolarisation of Anxiety
Diazepam
GABA receptor bind to its receptor opens calcium ion in neural membrane symptoms relieved
Examples

Drugs T/2 Daily Dose

Chlordiazepoxide 5-10 Hours 20-100mg

Diazepam 1 Hour 5-30mg

2mg/5ml syrup

Lorazepam 10-20 Hours 1-6mg

4mg/2ml inj.

Alprazolam 12 Hours 0.25-1mg TDS

upto 6mg/day in panic
disorder
Interactions

 • BZDs synergise with alcohol and other CNS depressant, leading to excessive
impairment.• Concurrent use with sodium valporate has provoked psychotic
symptom. • Oral contraceptives also retard BZD metabolism
Azapirones (Buspirone, Gepirone,
Ispapirone)
 Relieves mild-to-moderate generalized anxiety, but is ineffective in
severe cases (eg.OCD).
Mechanism of action
Serotonin (happy hormone)

Increased 5HT2

Increased excitation / anxiety

NORMAL CASE

Serotonin present on axons

Happy signals

Serotonin released by exocytosis

5ht2 binds with receptor

Excitation/ anxiety

Now buspirone binds partially with 5 ht2 receptor (acts as partial agonist)

Reduced excitement
Pharmacokinetics

 Rapidly absorbed
 Undergo extensive first pass metabolism (liver) bioavailability <5%.
 Excretion :- Urine/Stool.
 T/2 - 2-3.5 hours.
Side Effects

 Dizziness
 Nausea
 Headache
 Light headedness
 Rarely excitement
Antihistaminic (Hydroxyzine)

 Antihistaminic with Sedative

 Antiemetic
 Antimuscarinic & spasmolytic properties.
ß-Blockers (Proponolol)

Decreased Shaking,
Propanolol Beta blockers blood pressure tremors

Blocks Dilates blood Palpitations

vessels

Given in combination with BENZODIAZEPAMs to reduce social phobias/

examination fear
Indications

 Management of anxiety disorders.

 Short-term relief of symptoms of anxiety.
 Short-term treatment of insomnia.
 Maybe useful in patients with seizures.
Unlabeled Use

 Treatment of panic attacks

 Acute alcohol withdrawal syndrome
 Chemotherapy-induced nausea and vomiting
 Psychogenic catatonic depression
 PMS and treatment of IBS (Irritable Bowel Syndrome).
Contraindications

 Hypersensitivity
 Pregnancy :- Risk of congenital malformations, neonatal withdrawal syndrome.
 During Labor/Delivery :- Floppy Infant syndrome
 Lactation :- Infants become lethargic and lose weight
 Use cautiously with Impaired hepatic or renal function, debilitation.
Adverse Effects
 CNS :- Mild drowsiness initially, sedation, lethargy, depression, apathy, episodes
of maniacs and hypomanic confusion.
 CV :- Bradycardia/Tachycardia, CV collapse, palpitations, edema.
 Dermatologic :- Skin rash, dermatitis, urticaria.
 EENT :- Visual and auditory disturbances, depressed hearing.
 GI :- Constipation, diarrhea, dry mouth, nausea, Vomiting.
 Genito Urinary :- Incontinence & retention.
 Others :- Drug dependence with withdrawal syndrome, when drug is
discontinued; more common with abrupt discontinuation of higher dosage used
for longer than 4 months.
Nursing Consideration

Assessments

History/Hypersensitivity Physical
Interventions
 Keep addiction-prone patients under careful surveillance.
 Monitor Liver function, blood counts in patients on long term therapy.
 Ensure ready access to washroom, if GI upset occurs.
 Provide frequent small meals, frequent mouth care.
 Provide measures appropriately to care of urinary problems (protective clothing,
bed change).
 Establish safety precautions if CNS changes occurs (e.g. Side-rails, accompany
patients).
 Monitor patients for therapeutic drug levels while being used.
 Taper dosage gradually after long-term therapy, especially patients with epilepsy,
arrange to substitute another epileptic.
Teaching Points

 Take drug exactly as prescribed, don't stop taking drugs.

 Avoid alcohol, sleep inducing drugs or over the counter drugs.
 May experience side effects.
 Take drugs with food.
 Report severe dizziness, weakness, drowsiness if persists, rash/skin lesions,
difficulty in voiding palpitations, swelling in extremities.