Docsity Cns Lectures About Drugs 1 PDF

CNS lectures about drugs
Medicine
Islamic University of Gaza
60 pag.
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Chapter 22
Sedative and hypnotics

Control substances schedule
• Schedule I, a category of drugs not considered legitimate for
medical use. Included are heroin, lysergic acid diethylamide (LSD),
and marijuana.
• Schedule II, a category of drugs considered to have a strong

potential for abuse or addiction but that also have legitimate medical
use. Included are opium, morphine, and cocaine.
• Schedule III, a category of drugs that have less potential for abuse
or addiction than Schedule I or II drugs and have a useful medical
purpose. Included are short-acting barbiturates and amphetamines.

Control substances schedule
• Schedule IV, a medically useful category of drugs that
have less potential for abuse or addiction than those of
Schedules I, II, and III. Included are diazepam and
chloral hydrate.
• Schedule V, a medically useful catiegory of drugs that

have less potential for abuse or addiction than those of
Schedules I through IV. Included are antidiarrheals and
antitussives with opioid derivatives.

Anxiolytics (sedatives) and
hypnotics

• Anxiolytic
• Hypnotic
• Anesthesia
• Coma
• Death

Most anxiolytics (‘sedatives’) will induce
sleep when given at night and most
hypnotics will sedate when given during
the day
Not all BD are hypnotics but all are

anxiolytics

Benzodiazepine
• The most commonly used anxiolytics and
hypnotics
• Unjustified use
• Lowest dose for shortest period
• Minor tranquilizer

Actions
• Reduction of anxiety
• Hypnotic
• Anticonvulsant
• Muscle relaxant
• Anesthesia
• Anterograde amnesia

Dormicum
(midazolam)
• Onset of action
– IV 5 minutes
– IM 15 minutes
– Oral 20 minutes
• Duration 1-6 hrs

Dormicum
(midazolam)
• Midazolam is superior to diazepam in

impairing memory of endoscopy
procedures

Anxiolytics
• Should not be used for normal daily stress
• Clinical uses
• Panic attacks
• Post traumatic syndrome
• Obsessive compulsive disorders
• Extreme phobias

hypnotic
• Hangover and rebound insomnia

– Hangover for long acting hypnotics
– Rebound for short acting hypnotics
• Amnesia
– Antegrade amnesia

Pharmacokinetics
• Rapidly and completely absorbed
– Bioavailability might reach to 100%
• Cross placenta

Dependence
• Physical and psychological dependence
• Tolerance to BZ effect can be developed in 3-
14 days
• Withdrawal symptoms
– Confusion, anxiety
– Agitation, restless
– Insomnia, tension
– Rarely seizure

• Tolerance
– Decrease response to a drug following repeated
exposure
• Physiologic dependence
– Altered physiologic state that requires continuous
drug administration to prevent an abstinence or
withdrawal syndrome
• Psychological dependence
– Psychological dependence is a dependency of the mind,
and leads to psychological withdrawal symptoms (such as
cravings, irritability, insomnia, depression, anorexia etc).

Transient Insomnia
may occur in those who normally sleep well
and may be due to extraneous factors
such as noise, shift work, and jet lag. If a
hypnotic is indicated one that is rapidly
eliminated should be chosen, and only one
.or two doses should be given

Short Term Insomnia
usually related to an emotional problem or
.serious medical illness
It may last for a few weeks and may recur; a
hypnotic can be useful but should not be
given for more than three weeks (preferably
. only one week)
Intermittent use is desirable with omission of
some doses. A short-acting drug is usually
appropriate

The use of benzodiazepines to treat short-
. term ‘mild’ anxiety is inappropriate
Benzodiazepines should be used to treat

insomnia only when it is severe, disabling,
.or causing the patient extreme distress

Chronic Insomnia
rarely benefited by hypnotics and is
sometimes due to mild dependence
caused by injudicious prescribing of
hypnotics

Children
The prescribing of hypnotics to children,
except for occasional use such as for night
terrors and somnambulism (sleep-walking),
.is not justified
Elderly
Hypnotics should be avoided in the elderly,
because the elderly are at greater risk of
becoming ataxic and confused, leading to
.falls and injury

Pregnancy
There is a risk of neonatal withdrawal
symptoms when benzodiazepines are used
.during pregnancy
Avoid regular use and use only if there is a
clear indication such as seizure control
High doses administered during late
pregnancy or labour may cause neonatal
hypothermia, hypotonia, and respiratory
depression

• A benzodiazepine can be withdrawn in steps of about
one-eighth (range one-tenth to one-quarter) of the daily
dose every fortnight.
• Transfer to equivalent dose of diazepam (at night)
• Reduce dose every 2-3 weeks by 2-2.5 mg
• Maintain dose if symptoms appear
• Reduce slowly rather than rapidly
• Stop completely, 4 weeks to 1 year

Approximate equivalent doses, diazepam 5 mg
≡chlordiazepoxide 15 mg
≡loprazolam 0.5–1 mg
≡lorazepam 0.5–1 mg
≡lormetazepam 0.5–1 mg
≡nitrazepam 5 mg
≡oxazepam 15 mg
≡temazepam 10 mg
Steps may be adjusted according to initial dose and
duration of treatment

Side effects
• Drowsiness and confusion

– Agitaion (Paradox)
• Liver disease
• Combination with alcohol

Benzodiazepam antagonists
• Flumazenil
• Under supervision of experienced

consultant
• Reversal of respiratory suppression of BZ

after anesthesia and similar procedure

Flumazenil
• IV
• Half life 1 hour
• Repeated dose until recovery
• Contraindication
– Life threatening status epilepticus and
increased intracranial pressure

Buspirone
• Generalized anxiety disorder
• 5HTA1 receptors (partial agonists)
• Low frequency of side effects
• Little tolerance
• Sedation and psychomotor and cognitive dysfunction are

minimal, and dependence is unlikely

Buspirone
• Slow onset of action (1-2 weeks)
• it is, however, licensed for short-term use
only (but specialists occasionally use it for
several months).
• Does not alleviate BZ withdrawal symptoms

• Avoid in pregnancy
• S.E. tachycardia, parasthesia, GIT, myosis

Zolpidem and Zaleplon
• Zolpidem the most frequently prescribed hypnotic in USA
• Structurally unrelated to diazepam
• Specific α1 BZ1 receptors
• Less tolerance and rebound insomnia
• Short half lives
• For short term treatment only

Drug Tmax1 (hours) t1/22 (hours) Comments

Alprazolam 1–2 12–15 Rapid oral absorption
Chlordiazepox 2–4 15–40 Active metabolites; erratic bioavailability from

ide IM injection
Clorazepate 1–2 (nordiazepam) 50–100 Prodrug; hydrolyzed to active form in stomach
Diazepam 1–2 20–80 Active metabolites; erratic bioavailability from

IM injection
Eszopiclone 1 6 Minor active metabolites
Flurazepam 1–2 40–100 Active metabolites with long half-lives
Lorazepam 1–6 10–20 No active metabolites
Oxazepam 2–4 10–20 No active metabolites
Temazepam 2–3 10–40 Slow oral absorption
Triazolam 1 2–3 Rapid onset; short duration of action
Zaleplon <1 1–2 Metabolized via aldehyde dehydrogenase
Zolpidem 1–3 1.5–3.5 No active metabolites

there have been very few reports of
tolerance development when eszopiclone,
zolpidem, or zaleplon was used for less
than 4 weeks
shows few withdrawal effects, and exhibits

minimal rebound insomnia, and little or no
tolerance occurs with prolonged use
Zolpidem Still it is controlled substances

Ramelteon
• Agonist at melatonin receptors MT1 and MT2
• Light, retina, pineal gland and melatonin
• Induce and promote sleep

• Little tolerance and dependence
• Licenced for short term treatment for patients
upove 55 years

Antihistamine
– Mild anxiety
– Anticholenergic, and psychomotor side effects
– BZ are better
– Many over the counter preparation
– Is not controlled substances
BNF
– The use of antihistamines (e.g. hydroxyzine) for their
sedative effect in anxiety is not appropriate.

Propranolol
• do not affect psychological symptoms of
anxiety, such as worry, tension, and fear,
• but they do reduce autonomic symptoms, such

as palpitation and tremor
• Beta-blockers are therefore indicated for
patients with predominantly somatic symptoms
• this, in turn, may prevent the onset of worry
and fear.

Barbiturate
• Largely replaced by benzodiazepines
– tolerance
– Drug metabolizing enzymes
– Physical dependence
– Severe withdrawal symptoms
– Coma at toxic concentration

Actions
• CNS suppression
– Sedation, hypnosis, anesthesia, coma and
death
• Respiratory suppression
• CYP induction

Therapeutic applications
• Anesthesia
• Anticonvulsant
• Anxiety

Ethanol
Alcoholism is a serious medical and social
problem.
‫فيهما إثم كبير‬
Ethanol has anxiolytic and hypnotic effect
‫و منافع للناس‬
but its toxic potential outweighs its benefits
‫و إثمهما اكبر من نفعهما‬

Ethanol hazards
• Hepatic failure
• Gastritis
• Nutritional deficiency
• Cancer
• cancer
• Road traffic accidents
• Domestic violence

WHO and Alcohol
• 3.3 million death every year from alcohol
consumption
• 1.5 million youth deaths 15-40 years
• 250 000 deaths from alcohol related road traffic

accidents
• Wars kill 1% whereas Alcohol kill 5.6%


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CNS lectures about drugs

Document shared on www.docsity.com

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• Schedule II, a category of drugs considered to have a strong

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• Schedule V, a medically useful catiegory of drugs that

Document shared on www.docsity.com

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Not all BD are hypnotics but all are

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• Lowest dose for shortest period

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• Duration 1-6 hrs

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• Midazolam is superior to diazepam in

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• Hangover and rebound insomnia

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Benzodiazepines should be used to treat

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• Transfer to equivalent dose of diazepam (at night)

• Reduce dose every 2-3 weeks by 2-2.5 mg

• Maintain dose if symptoms appear

• Reduce slowly rather than rapidly

• Stop completely, 4 weeks to 1 year

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• Drowsiness and confusion

• Combination with alcohol

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• Under supervision of experienced

• Reversal of respiratory suppression of BZ

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• Repeated dose until recovery

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• 5HTA1 receptors (partial agonists)

• Low frequency of side effects

• Sedation and psychomotor and cognitive dysfunction are

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• Does not alleviate BZ withdrawal symptoms

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• Zolpidem the most frequently prescribed hypnotic in USA

• Structurally unrelated to diazepam

• Specific α1 BZ1 receptors

• Less tolerance and rebound insomnia

• Short half lives

• For short term treatment only

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Alprazolam 1–2 12–15 Rapid oral absorption

Chlordiazepox 2–4 15–40 Active metabolites; erratic bioavailability from

Clorazepate 1–2 (nordiazepam) 50–100 Prodrug; hydrolyzed to active form in stomach

Diazepam 1–2 20–80 Active metabolites; erratic bioavailability from