Please enable JavaScript.
Coggle requires JavaScript to display documents.
SEDATIVES AND HYPNOTICS, Barbiturates, th (2), USES BZDs
**1.Anxiety…
SEDATIVES AND HYPNOTICS
Non-BZDs or Z- Compounds
- Zaleplon , zolpidem ,Eszopiclone
- Zaleplon ( SHORTEST T1/2) and zolpidem
- Effective in relieving sleep-onset insomnia.
- Approved by the FDA for use for up to 7-10 days at a time
- without occurrence of rebound insomnia on abrupt discontinuation
- Eszopiclone
-used for the long-term (~12 months) treatment of insomnia,
-for sleep maintenance,
- to decrease the latency to onset of sleep
-
-
MECHANISM
BZD
*GABA A action 
Cl influx
- Potentiate GABA action
*Increase the frequency of openings of Cl channel
- No GABA mimetic property
HYPNOTIC
- Diazepam
- Flurazepam
- Nitrazepam
- Alprazolam
- Temazepam
- Triazolam
ANTIANXIETY
- Chlordiazepoxide
- Diazepam
- Lorazepam
- Oxazepam
- Alprazolam
*ANTICONVULSANT
- Clonazepam
- Diazepam
- Clobazam
- Lorazepam
Toxicity
- specific antidote - FLUMAZENIL
BZDs/ Barbiturates
-
-
- Antihistamines -Diphenhydramine, hydroxyzine, and doxylamine (Anticholinergic adverse effects)
- Antidepressants -Doxepin(Doxepin is
FDA-approved for the treatment of sleep maintenance insomnia.) ,Trazodone , mirtazapine
- Suvorexant-antagonist of orexin receptor(Daytime somnolence and increased suicidal ideation )
Agomelatine, a melatonin receptor agonist and a 5HT2C receptor antagonist
- treatment of depression and may aid in ameliorating sleep disturbances
Ritanserin and other 5HT2A/2C receptor antagonist
- promote slow-wave sleep in patients with chronic primary insomnia or generalized anxiety
Pregabalin, an anxiolytic agent that binds to Ca2+ channel α2δ subunits,
- effective treatment of the insomnia seen in patients suffering from a generalized anxiety disorder
-
Barbiturates
Mechanism
- Prolongs GABA activity
- prolongs duration of Cl channel opening
- GABA mimetic- Higher dose
- block excitatory glutamate AMPA receptors.
- Induce CYP450 microsomal enzymes
Amobarbital
- Insomnia, preoperative sedation, emergency management of seizures
Butabarbital
- Insomnia, preoperative sedation,
daytime sedation
Mephobarbital
- Seizure disorders, daytime sedation
Methohexital
- Induction and maintenance of
anesthesia
Pentobarbital
Insomnia, preoperative and procedural sedation, emergency management of seizures
Phenobarbital
- First-line anticonvulsant, status epilepticus, daytime sedation (hyperbilirubinemia, off-label use)
Secobarbital
- Insomnia, preoperative sedation
Thiopental
- Induction/maintenance of anesthesia, preoperative sedation, emergency management of seizures, intracranial pressure
-
t
Toxicity
- forced diuresis and alkalinization
- In renal failure - hemodialysis
Hypovolemia must be corrected & blood pressure can be supported with dopamine.
ADVERSE EFFECTS
- CNS: cause drowsiness, impaired concentration.
- Drug hangover- Hypnotics
- Induce CYP450 microsomal enzymes- D/I
- C/I with acute intermittent porphyria.
- physical dependence
- Poisoning: May be due to automatism
- No specific antidote available
-
USES BZDs**1.Anxiety disorders
- Sleep disorders**
Short-acting-Triazolam – effective in treating individuals who have problems falling asleep.
Withdrawal and rebound insomnia
Intermediate-acting-Temazepam- -useful for patients who experience frequent awakenings and have difficulty staying asleep.
should be administered 1 to 2 hours before the desired bedtime
3. Amnesia- Midazolam(Preanesthetic and intra-operative medication ,anxiety disorders (agitation,alcohol withdrawal, seizure disorders,)
Remimazolam- Used as a sedative during medical procedures lasting 30 min or less
4.Seizures- Clobazam(Adjunctive treatment of seizures associated with Lennox-Gastaut syndrome)
lorazepam and diazepam - intravenous or rectal route-DOC status epilepticus
5.SMR (Diazepam )
- to reduce the withdrawal symptoms of physical dependence of Alcohol(diazepam, chlordiazepoxide)
-
-