sedatives and hypnotics and anxiolytics

2.  Drugs that have a calming effect or that depress
the CNS are referred to as sedatives and
hypnotics.
 Clinical uses:
 Anxiety relief.
 Insomnia.
 Preaneasthesia.

3.  Anxiolytic: drug used to depress the central
nervous system (CNS); prevents the signs and
symptoms of anxiety.
 Sedatives reduce nervousness, excitability, and
irritability without causing sleep.
 Hypnotics cause sleep and have a much more
potent effect on the CNS than do sedatives.

4.  Using these drugs for long time leads to tolerance
and dependence so that you can’t get asleep
without having them and the effectiveness
decrease.
 We should look for the causes of insomnia.
 Drugs for insomnia should be used for short time
as much as possible.

5.  Sedative-hypnotics can be classified
chemically into three main groups:
 Barbiturates.
 Benzodiazepines.
 Miscellaneous drugs.

12.  Benzodiazepines.
 Buspirone.
 Beta-blockers.
 Antideprassants.

13.  Diazepam.
 Lorazepam.
 Midozolam.

14.  All anxiolytic drugs decrease anxiety by reducing
overactivity in the CNS.

16.  Anxiety
Sleep disorders-----intermediate andshort
Skeletal muscle relaxation
Seizure disorders
Amnesia-------midazolam
 Adjuvant therapy for depression
 Alcohol withdrawal==chlordiazepoxide,
clorazepate, diazepam, lorazepam, and
oxazepam

17.  known drug allergy.
 Narrow-angle glaucoma.
 Pregnancy.

18.  Somnolence, Confusion, Coma, and Diminished
reflexes
 Do not cause hypotension and respiratory
depression unless taken with other CNS
depressants
 Treatment: symptomatic and supportive.
Use Flumazenil as an antidote.

19.  It has varied uses:
 Treatment of anxiety.
 Anesthesia adjunct.
 Anticonvulsant therapy.
 Skeletal muscle relaxation.

20.  Usual Adult Dose for
Benzodiazepine Overdose
 Initial dose: 0.2 mg IV one time over
30 seconds.
Repeated doses: 0.5 mg may be
given every minute.
Maximum total dose 3 mg.
 Patients responding partially at 3 mg
may receive additional doses up to 5
mg.
 Most patients respond to 1 to 3 mg.

21.  Is an indirect GABA receptor antagonist insimilar
way of action on brain receptors.
 Rapid onset of action with short duaration.
 Administration may preceipitate withdrawal
symptoms in dependent patients or may cause
seizure in epileptic patients if he on
benzodiazepine treatment.
 Side effects: dizziness, nausea and vomiting

23.  Alprazolam:
 It is effective for short and long treatment of panic
disorders when sympathetic discharge is high and
aggressive.
 Flurazepam:
 Long acting.
 Reduce both sleep induction time and number of
awakening and increases duration of sleep.
 Causes little rebound insomnia.

24.  Temazepam:
 Intermediate, useful in patients with frequent
awakening situations.
 Triazolam:
 Short, sleep induction in early insomnia.
 Clonazepam:
 Useful in chronic treatment of epilepsy.

25.  1. Absorption and distribution:
 The benzodiazepines are lipophilic. They are
rapidly and completely absorbed after oral
administration, distribute throughout the body and
penetrate into the CNS.
 2. Duration of action:
 The half-lives of the benzodiazepines are
important clinically, because the duration of action
may determine the therapeutic usefulness.

26.  Most benzodiazepines, including chlordiazepoxide and diazepam, are
metabolized by the hepatic microsomal system to compounds that are also
active.
 For these benzodiazepines, the apparent half-life of the drug represents the
combined actions of the parent drug and its metabolites.
 Drug effects are terminated not only by excretion but also by redistribution.
 The benzodiazepines are excreted in the urine as glucuronides or oxidized
metabolites.
 All benzodiazepines cross the placenta and may depress the CNS of the
newborn if given before birth. The benzodiazepines are not recommended
for use during pregnancy. Nursing infants may also be exposed to the drugs
in breast milk.

27.  Drowsiness and confusion.
 Ataxia at high doses.
 Cognitive impairment.
 Psychological and physical dependent.
 Drug abuse.
 Withdrawal symptoms: confusion, anxiety,
agitation, restlessness and insomnia.
 Long acting BDZ are producing less severe
withdrawal symptoms than short acting one.

28.  No sedative action.
 No risk of dependence.
 Nausea and headache.
 The actions of buspirone appear to be mediated
by serotonin (5-HT1A) receptors, although it also
displays some affinity for D2 dopamine receptors
and 5-HT2A receptors.

29.  Beta blockers: propranolol.
 Antidepressants.

30.  Insomnia can, however, cause feelings of anxiety,
inability to concentrate.
 Reasons ????????

31.  Sleep architecture:
 Rapid eye movement (REM) sleep.
 Non-REM sleep.
 Prolonged sedative-hypnotic use lead to REM
interference.
 On discontinuance of a sedative-hypnotic drug, REM
rebound can occur.

32.  Benzodiazepines.
 Nonbezodiazepines: Zaleplon and zolpidem.
 Ramelteon.
 Barbiturates.

33.  Nonbenzodiazepines function as benzodiazepine
but are chemically distinct from them.
 Zaleplon and zolpidem.

34.  Although isn’t a BDZ but can act on their receptor.
 It has no anticonvulsant or muscle relaxing.
 No with withdrawal symptoms and exhibit
minimum rebound insomnia with no or little
tolerance in prolonged use.
 Rapidly absorb from GIT.
 Rapid onset and short half life.
 Adverse effects: night mares, agitation, headache,
GI upset and daytime drowsiness.

36.  Ultra short-acting
◦ Thiopental
 Short-acting
◦ Pentobarbital, secobarbital
 Intermediate-acting
◦ Butabarbital
 Long-acting
◦ Phenobarbital.

37.  Ultra short-acting
◦ Anesthesia for short surgical procedures,
other uses
 Short-acting
◦ Sedation/sleep induction and control of convulsive
conditions
 Intermediate-acting
◦ Sedation/sleep induction and control of convulsive
conditions
 Long-acting
◦ Sleep induction, epileptic seizure prophylaxis

38.  Barbiturates have a very narrow therapeutic index
 Body System
Adverse Effects
 CNS Drowsiness, lethargy, vertigo, mental
depression.
 Respiratory Respiratory depression, apnea,
bronchospasms, cough.
 GI Nausea, vomiting, diarrhea, constipation
 Other Agranulocytosis, hypotension,
Stevens-Johnson syndrome

39. They act by
reducing the
nerve impulses
traveling to the
area of the brain
called the
cerebral cortex.

40. Old generation
antihistamines
have a hypnotic
effect as an
adverse effect.

41.  Give hypnotics 30 to 60 minutes before
bedtime.
 benzodiazepines cause REM rebound.
 Instruct patients to avoid CNS depressants

42.  Rebound insomnia may occur for a few nights
after a 3- to 4-week regimen has been
discontinued

43.  Safety is important
◦ Keep side rails up, or use bed alarms
◦ Do not permit smoking
◦ Assist patient with ambulation (especially the elderly)
◦ Keep call light within reach
 Monitor for adverse effects