Sedative and hypnotic drugs work by depressing the central nervous system. Sedatives produce calm and relaxation and are used to treat anxiety, while hypnotics induce sleep and are used for insomnia. Benzodiazepines are commonly used sedative-hypnotic drugs that work by enhancing the effects of the inhibitory neurotransmitter GABA, causing sedation, sleep induction, anti-anxiety effects, and muscle relaxation. They can cause side effects like drowsiness, confusion, and dependence or addiction with long-term use.

1. P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs
SEDATIVE & HYPNOTIC DRUGS
5-HT R β-adrenergic R
BNZ Barbiturates Other Z-Hypnotics
Agonists blockers
Intermediat Intermediat Anti- Chloral
Long acting Short acting Long acting Buspirone Propranolol Clonidine Zaleplon
acting acting histamines Hydrate
Chlordiazepox Diphenhydra
Alphazolam Oxazepam Phenobarbital Secobarbital Zolpidem
ide mine
Ultra-short
Diazepam Lorazepam Triazolam Short acting
acting
• drugs that produce
Clonazepam Hexobarbital Thiopental
Sedatives calm & relaxation.
• used for anxiety.
• drugs that put user
Hypnotics in sleep.
• used for insomnia.
DEATH
coma both of them
anesthesia
depress CNS but
Hypnotic more
hypnosis
sedation

2. P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs
 Benzodiazepines (BNZ)
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Chlordiazepoxide Absorption Mechanism of action 1) Sedative preoperatively.  Drowsiness.
 Orally / I.M. / I.V.  BNZ hyperpolarizes the membrane of 2) Epilepsy in emergency.  Confusion.
Long acting
(1-3 days)
Diazepam the post-synaptic neurons by: 3) Treatment of muscle plasticity in cerebral  Amnesia.
Distribution  Binding to GBC binding site. palsy & tetanus  Impairment of motor
Clonazepam  Pass BBB & placenta.   affinity of the R to GABA. coordination.
+
 Secreted into breast milk.   Cl permeability.  Dependence & addiction.
 Hyperpolarize the
Alphazolam membrane. 1) Sleep disorder, insomnia.
Metabolism
 Inhibition of the neurons. 2) Control alcohol withdrawal symptoms.
 It is done by hebatic microsomal system.
3) Treatment of muscle plasticity in cerebral
 The metabolites: Psychological dependence.
Action palsy & tetanus
o Active.  Stop administration cause:
Intermediate acting
o Have longer T1/2. 1) Reduction of anxiety.  Craving.
(10-20 hrs)
o Cause hangover effect. 2) Sedation which encourage sleep by:
Lorazepam  The T1/2 depend on the metabolism not   latency. 1) Short term relief of sever anxiety. Physical dependence.
excretion.   non-REM. 2) Sleep disorder, insomnia.  Stop administration cause
  REM. 3) Control alcohol withdrawal symptoms. withdrawal symptoms:
Excretion 3) Reduction of muscle tone & 4) Treatment of muscle plasticity in cerebral  Insomnia.
 coordination. palsy & tetanus
It is done by kidney.  Anxiety.
 4) Anti-convulsant.
 Autonomic over activity.
 5) Prolonged sleep with over dose.
It safe on over dose if it taken alone.   HR & BP.
 6) Tolerance.
It is the most widely used sedative because:  Tremors.
Oxazepam  High Ti.  It is pharmacodynamic ( 1) Sleep disorder, insomnia.  Diaphoresis.
 Low risk of dependence. the sensitivity of the 2) Control alcohol withdrawal symptoms.  Muscle cramps.
Short acting
receptors).
(3-8 hrs)
 Acute overdose or toxicity is treated 3) Treatment of muscle plasticity in cerebral  Confusion.
 Develop after chronic use palsy & tetanus.
by:  Seizures.
Triazolam  FLUMAZENILE. (1-2 wks).
 Irritability.
 Ataxia.
Anxiety
 Fear-induced situation. Uses of BNZ
 It has: 1) Short term relief of sever anxiety.
 CNS symptoms: 2) Sedative preoperatively.
 Insomnia. 3) Sleep disorder, insomnia.
 Anorexia. 4) Epilepsy in emergency.
 Muscle tension. 5) Control alcohol withdrawal symptoms.
 Peripheral symptoms: 6) Treatment of muscle plasticity in cerebral
 Sweating. palsy & tetanus.
 Tremors.
 Palpitation.
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3. P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs
 Barbiturates ( acids)
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Thiopental Absorption  Depression of the neural activity by : NOT used as sedative or hypnotic drugs but  Death in high dose due to:
Ultra-Short
 Orally / I.M. / I.V.  Enhancement of they are only used for:  CVS depression.
acting
GABAergic pathway. 1) I.V. anesthesia.  Respiratory depression
Distribution  Blocking excitatory NT. 2) Epilepsy.  Dependence.
 To all body 3) Hyperbilirubinemia.  Drug-drug interaction.
Hexobarbital Metabolism  Paradoxical excitement of
acting
Short
 It is done by hebatic microsomal system. children.
 This system cause drug-drug iteractoin.  Prolonged hangover.
NOT used as sedative or hypnotic drugs but  Porphyria.
Secobarbital Excretion they are only used for:  Tolerance
Intermedia
te acting
 It is done by kidney. 1) Epilepsy.  It is pharmaco-
 It is pH dependence. 2) Hyperbilirubinemia. dynamic (enzyme
 Alkalization of urine with NaHCO3 enhance induction).
barbiturates renal execrerion.
Phenobarbital  So, used for treatment of
acti
Lon
ng
g
overdose.
 5-HT Receptors Agonists
Buspirone  Mixed agonist- antagonist.  Anxiolytic action ( 1-3 wks).  Generalized anxiety.  Nervousness.
 Minimal risk of dependence.  Little sedation.  Dizziness.
 Little impairment of coordination.  Headache.
 Minimal risk of dependence.  Nausea & vomiting.
 NO hypnotic , NO euphoria.
 β-adrenergic Blockers
Propranolol  non-selective β-blocker.   peripheral symptoms of anxiety 1) Anxiety. 
 Sweating, Tremors & 2) Social phobia.
Palpitation. 3) NOT for (asthma, COPD, diabetes)
 Reduce performance anxiety such:
 Public speech or Interview.
 Other sedative & hypnotic
Diphenhydramine  Anti-histamine.  Has anit-cholinergic action. 1) Insomnia. 
Anit-H
2) Anxiety & agitation.
Chloral Hydrate   Used to induce sleep in children 
 to perform certain medical
procedure.
Clonidine  α2 agonist.  1) Control sympathetic overactivity 
associated with:
 Narcotic withdrawal.
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 Acute anxiety.
2) Panic attack of anxiety.
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4. P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs
 Z-hypnotic
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Zaleplon  Selective for α1 subunite of BNZ receptor  Depression of the neural activity by
comlex. enhancement of GABAergic pathway.
1) Less risk of tolerance.
2) Less risk of amnesia.
3) Minimal rebound:
Zolpidem  Insomnia.
 Anxiety.
 Hagover effect.
 The acton is antagonized by
Flumazenil
 that impact sleep stage.
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