Anxiolytic/Hypnotic Drugs Lec. 1 Flashcards
The sedative-hypnotics belong to a chemically heterogeneous class of drugs, almost all of which produce dose-dependent CNS
depressant effects that cause sedation (with relief of anxiety) or hypnosis (encourage sleep). What are The major subgroup ?
1_ benzodiazepines
but representatives of other subgroups, including:
2 _barbiturates
3_and miscellaneous agents (carbamates, and cyclic ethers) which are still in use.
4_Atypical drugs with distinctive characteristics
Include:
🛑the anxiolytic buspirone
🛑several widely used ,hypnotics (zolpidem, zaleplon, eszopiclone)
🛑melatonin agonists
🛑orexin antagonists, novel drugs used in sleep disorders
What is drug known as hypocretin, is a neuropeptide that regulates arousal, wakefulness, and appetite.
Blocking orexin can help to combat insomnia?
Orexin
What is drug use an oral tablet that’s approved in January 2022 to treat insomnia in adult and its belong to orexin receptor antagonists (ORAs
Daridorexant
اول مقطع منو يذكرني بكلمة داري 😁
What is drug use an antagonist of the orexin receptor, it is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset &/or maintenance in adult.
Suvorexant
اول مقطع منو يذكرني بكلمة سيڤ😁
What is drug with the highest lipid solubility enter the CNS rapidly and can be used as induction agents in anesthesia. The CNS effects of terminated by rapid redistribution of the drug from brain to other highly perfused tissues, including skeletal muscle and ultra short action
thiopental
Mechanism of action of Benzodiazepines
The targets for benzodiazepine actions are Gamma aminobutyric acid (GABAA) receptors.
[Note: GABA is the major inhibitory neurotransmitter in the central nervous system (CNS).]
Binding of GABA to its receptor triggers an opening of a chloride channel, which leads to an increase in chloride conductance . Benzodiazepines increase the frequency of channel openings produced by GABA. The influx of chloride ions causes hyperpolarization of the neuron and decreases neurotransmission by inhibiting the formation of action potentials (moves the postsynaptic potential away from its firing threshold).
Note: Binding of a benzodiazepine to its receptor site will increase the affinity of GABA for the GABA-binding site without actually changing the total number of sites.
The clinical effects of individual benzodiazepines correlate well with
the binding affinity of each drug for the GABA receptor–chloride ion channel complex.
What are PHARMACODYNAMICS pharmacological actions of Benzodiazepines?
The benzodiazepines have neither antipsychotic activity nor analgesic action, and they do not affect the autonomic nervous system. All benzodiazepines exhibit the following actions:
1. Reduction of anxiety: 🟨At low doses, the benzodiazepines are anxiolytic. They reduce anxiety by selectively enhancing GABAergic
transmission in neurons.In addition to sedative action that is occur with all drugs in this class.
2. hypnotic action: some can produce hypnosis (artificially produced sleep) at 🟨higher doses.
3.Anticonvulsant: Suppression of seizure activity occurs with 🟨high doses of some of the benzodiazepines, but this is usually at the cost of marked sedation. 🟨High doses of intravenous 🌸diazepam, lorazepam🌸are used in status epilepticus. In this condition, heavy sedation is desirable.
- Muscle relaxant: At high doses, the benzodiazepines relax the spasticity of skeletal muscle .diazepam is effective for specific spasticity states, including cerebral palsy.
- Anesthesia : 🟨at high doses of most older sedative-hypnotics, loss of consciousness may occur, with amnesia and suppression of reflexes. Anesthesia can be produced by certain benzodiazepines (eg. 🌸midazolam
- Tolerance and Dependence:
Psychological and physical dependence on benzodiazepines can develop if high doses of the drugs are given over a prolonged period.
Abrupt discontinuation of the benzodiazepines results in withdrawal symptoms, including confusion, anxiety, agitation, restlessness, insomnia, tension, and rarely, seizures.
What drug from BENZODIAZEPINES with Long - acting?
🌸Chlordiazepoxide
🌸Diazepam
🌸Flurazepam
The duration of it (1_3) days
What drug from BENZODIAZEPINES with Short - acting and What is duration ?
🌸Triazolam
🌸Midazolam
The duration of it (3_8)hour
What drug from BENZODIAZEPINES with Intermediate - acting and what duration?
Alprazolam Clonazepam Clorazepate Estazolam Lorazepam Oxazepam Quazepam Temazepam
The duration of it (10_20) hour
NONBENZODIAZEPINE HYPNOTICS ?
🌸Zaleplon 🌸Zolpidem 🌸Eszopiclone
MELATONIN AGONISTS ?
Ramelteon Tasimelteon
OTHER ANXIOLYTIC DRUGS ?
🌸Antidepressants
🌸Buspirone
🌸Meprobamate
BARBITURATES drugs ?
🌸Amobarbital (intermediate-acting )🌸Pentobarbital
🌸 (-long acting )Phenobarbital
🌸Secobarbital
🌸thiopental (short acting)
