TRANQUILLIZERS

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 Definition

These are the agents which cause sedation.

They change the behavior of the animal
towards external stimuli from the environment.
They induce the state of calmness and tranquility from
emotional stress without unduly sedation

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 Classification
 Phenothiazine derivatives
 Butyrophenol derivatives
 Rauwolfia alkaloids
 Benzodiazipine
 α2 – adrenergic agonists
 Central muscle relaxants

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 Phenothiazine derivatives
Members
 Chlorpromazine
 Promazine
 Acepromazine
 Propiopromazine
 Triflupromazine

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 Phenothiazine Derivates
► Classification

A: Aliphatic side chain Phenothiazine

Promazine (sedative)
Chlorpromazine (sedative, antiemetic, tranquilizer)
Acepromazine (sedative, antiemetic,
tranquilizer,preanesthetic)
Triflupromazine (sedative, preanesthetic)
B: Piperazine side chain Phenothiazine
Prochlorperazine (antiemetic, antidiarrheal)
Perphanazine (antiemetic)
Fluphenazine (neuroleptic)
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C: Piperadine side chain Phenothiazine
Thioridazine (neuroleptic)
Piperacetazine (sedative, antiemetic, antipruritic)

► Substitution at R2 increases efficacy

► Aliphatic side chain at R1 causes low potency but good
clinical efficacy, sedation
► Piperazine group at R1, potent antipsychotic agent but
mild sedation
► Piperadine group at R1 increased antimuscarinic activity.

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 Properties
 They are major tranqulizers
 Cause sedation
 Block dopamine receptor
 Depress cortical areas
 Block α1 – receptors
 Antihistamne, anticholinergic, antisposmotic
activity
 Vasodilation, decrease B.P
 No analgesia
 Poor relaxation

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 Uses
a) Tranqulizer
b) Preanaesthetic
c) Control or restrain
d) Sedation, calm
e) Anti-emetic
f) May potentiate O.P toxicity
g) Paramphymosis
Dose: Acepromazine: 0.05mg/kg
Chlorpromazine: 0.5 – 1 mg/kg
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 Butyrophenone Derivatives
Members
 Droperidol
 Haloperidol
 Azaperine

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 Properties

 Dopamine blocking

 α1 block, less
 Less sedative
 Anti-emetic potent
 More potent than chlorpromazine as an atiemetic
Innovar – vet (Droperidol + Fentanyl)
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 Rauwolfia alkaloids
Members
Reserpine

Properties
 Depletion of N.E from storage vesicles
 Cause sedation
 Effect for a longer period

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 Benzodiazepines
Members

 Diazepam (Valium)
 Zolezepam
 Chlorodiazepoxide (Librium)
 Midazolam

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 Properties
 Enhance binding of GABA, open Cl- channel,
hyperpolarization
 Minor tranqulizer
 Sedative
 Poor analgesic
 Relaxation of muscle
 Anti-convulsant
 Pre-anaesthetic
 Antidote: Flumazenil

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 α2 – Agonist
Members
 Xylazine
 Detomidine
 Clonidine
 Medetomidine

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 Properties
 Sedative
 Hypnotic
 Analgesic
 Relaxation
 Pre-anaesthetic
 α2 –
agonist
 Dose dependant
 Decrease Insulin, increase glucose
 Yohimbine (Antidote)

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 Central Muscle Relaxants

Members
 Meprobamate
 Mephenesin
 Guaifenesin [Glyceryl Guaicolate Ether] (GGE)

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 Properties

 Centralmuscle relaxation
 Pre-anaesthetic
 Poor anaesthetic
 Poor sedative
 Poor analgesic

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