Sedatives and hypnotics act on the central nervous system to reduce anxiety and promote sleep. Benzodiazepines are the most commonly used class, enhancing the effect of the inhibitory neurotransmitter GABA. They have sedative, anxiolytic, muscle relaxing, and anticonvulsant effects. While effective, they can cause tolerance, dependence, and withdrawal symptoms with long-term use. The ideal hypnotic would have rapid onset, sustained nighttime effects, and no morning residual effects, but this is difficult to achieve without risk of rebound insomnia or withdrawal.
The document discusses sedative/hypnotic and anxiolytic drugs. It describes their mechanisms of action, which primarily involve enhancing GABAergic transmission in the brain. Benzodiazepines and barbiturates act as agonists at GABA-A receptors. These drugs can relieve anxiety and induce sleep, but have side effects like sedation, respiratory depression, and dependence with long-term use. Newer non-benzodiazepine drugs like zolpidem are also discussed.
This document is a lecture on sedative-hypnotic and anxiolytic drugs given by Dr. Marc Imhotep Cray. The learning objectives cover the GABAA receptor structure and drug binding sites, pharmacokinetics of benzodiazepines, similarities and differences among benzodiazepines and between benzodiazepines and barbiturates, factors in drug selection, and abuse potential of sedative-hypnotics. The lecture discusses mechanisms of action, side effects, clinical uses including treatment of anxiety and insomnia, and specifics of benzodiazepines, barbiturates, and other agents.
This document provides information on antianxiety drugs. It discusses that anxiety is an unpleasant emotional state associated with unease from an unknown threat. Treatment is needed when anxiety is disproportionate or excessive. It then describes various classes of antianxiety drugs including benzodiazepines, azapirones, barbiturates, beta blockers, and antidepressants. The document focuses on benzodiazepines, explaining their mechanism of action by enhancing GABA through binding sites on GABA receptors. It discusses their therapeutic uses for anxiety disorders, seizures, muscle disorders and as amnesia for medical procedures. Potential adverse effects and drug interactions are also summarized.
This document discusses anxiolytics, or anti-anxiety drugs. It defines anxiety and differentiates it from fear. It outlines the learning objectives which are to define key terms, list classes of anxiolytic drugs, and describe the mechanisms of action, effects, pharmacokinetics, adverse effects, and interactions of anxiolytics. The major classes of anxiolytics discussed are benzodiazepines, azapirones, and beta-blockers. Benzodiazepines are described as the most important sedative-hypnotics, with properties including a wide margin of safety but risk of dependence with prolonged use. Buspirone is discussed as an azapirone anxi
This document discusses the mechanisms of action of benzodiazepines. It notes that benzodiazepines augment the effects of the inhibitory neurotransmitter GABA at GABA-A receptors. They can be selective for different GABA receptor subunits involved in sleep, anxiety, or addiction. The hypnotic and anxiolytic effects of benzodiazepines are explained by their actions on GABA receptors in the amygdala, hippocampus, and hypothalamic regions involved in sleep/wake regulation. Adverse effects and issues with dependence and withdrawal are also covered. Novel approaches to anxiolytic drugs targeting GABA receptors without addiction liability are mentioned.
This document summarizes information about benzodiazepines, including their pharmacodynamics, pharmacokinetics, uses, side effects, and alternatives. Benzodiazepines work by enhancing GABA effects in the brain and are used short-term to treat anxiety, insomnia, and alcohol withdrawal, but have risks for the elderly, risks of abuse and dependence, and side effects like sedation and amnesia. Newer non-benzodiazepine drugs that target specific receptor subtypes or serotonin systems aim to provide similar effects with fewer side effects and risks.
The document summarizes information about sedative-hypnotics presented in a lecture. It discusses the properties of individual benzodiazepines (BZDs) like diazepam, flurazepam, alprazolam, and midazolam. It also covers non-BZD hypnotics like zopiclone, zolpidem, and zaleplon that act on specific BZD receptor subunits. Melatonin and ramelteon, which act as melatonin receptor agonists, are also discussed. The concluding section notes that long-acting BZDs can cause next day sedation while flumazenil acts as a BZD antagonist to
Here are the key points regarding SAR of HDAC inhibitors from the research article:
- Hydroxamic acid zinc binding group is essential for HDAC inhibitory activity. Removing this group drastically reduced potency.
- Variations in the cap group (portion above hydroxamic acid) had significant effects on isoform selectivity.
- Shorter linker lengths between the cap and hydroxamic acid improved potency and selectivity for certain HDAC isoforms.
- Hydrophobic substituents on the phenyl ring of the cap group enhanced potency, while polar groups decreased it.
- Introducing methyl groups in the ortho and para positions of the phenyl ring improved potency and selectivity.
- Bicy
The document discusses sedative/hypnotic and anxiolytic drugs. It describes their mechanisms of action, which primarily involve enhancing GABAergic transmission in the brain. Benzodiazepines and barbiturates act as agonists at GABA-A receptors. These drugs can relieve anxiety and induce sleep, but have side effects like sedation, respiratory depression, and dependence with long-term use. Newer non-benzodiazepine drugs like zolpidem are also discussed.
This document is a lecture on sedative-hypnotic and anxiolytic drugs given by Dr. Marc Imhotep Cray. The learning objectives cover the GABAA receptor structure and drug binding sites, pharmacokinetics of benzodiazepines, similarities and differences among benzodiazepines and between benzodiazepines and barbiturates, factors in drug selection, and abuse potential of sedative-hypnotics. The lecture discusses mechanisms of action, side effects, clinical uses including treatment of anxiety and insomnia, and specifics of benzodiazepines, barbiturates, and other agents.
This document provides information on antianxiety drugs. It discusses that anxiety is an unpleasant emotional state associated with unease from an unknown threat. Treatment is needed when anxiety is disproportionate or excessive. It then describes various classes of antianxiety drugs including benzodiazepines, azapirones, barbiturates, beta blockers, and antidepressants. The document focuses on benzodiazepines, explaining their mechanism of action by enhancing GABA through binding sites on GABA receptors. It discusses their therapeutic uses for anxiety disorders, seizures, muscle disorders and as amnesia for medical procedures. Potential adverse effects and drug interactions are also summarized.
This document discusses anxiolytics, or anti-anxiety drugs. It defines anxiety and differentiates it from fear. It outlines the learning objectives which are to define key terms, list classes of anxiolytic drugs, and describe the mechanisms of action, effects, pharmacokinetics, adverse effects, and interactions of anxiolytics. The major classes of anxiolytics discussed are benzodiazepines, azapirones, and beta-blockers. Benzodiazepines are described as the most important sedative-hypnotics, with properties including a wide margin of safety but risk of dependence with prolonged use. Buspirone is discussed as an azapirone anxi
This document discusses the mechanisms of action of benzodiazepines. It notes that benzodiazepines augment the effects of the inhibitory neurotransmitter GABA at GABA-A receptors. They can be selective for different GABA receptor subunits involved in sleep, anxiety, or addiction. The hypnotic and anxiolytic effects of benzodiazepines are explained by their actions on GABA receptors in the amygdala, hippocampus, and hypothalamic regions involved in sleep/wake regulation. Adverse effects and issues with dependence and withdrawal are also covered. Novel approaches to anxiolytic drugs targeting GABA receptors without addiction liability are mentioned.
This document summarizes information about benzodiazepines, including their pharmacodynamics, pharmacokinetics, uses, side effects, and alternatives. Benzodiazepines work by enhancing GABA effects in the brain and are used short-term to treat anxiety, insomnia, and alcohol withdrawal, but have risks for the elderly, risks of abuse and dependence, and side effects like sedation and amnesia. Newer non-benzodiazepine drugs that target specific receptor subtypes or serotonin systems aim to provide similar effects with fewer side effects and risks.
The document summarizes information about sedative-hypnotics presented in a lecture. It discusses the properties of individual benzodiazepines (BZDs) like diazepam, flurazepam, alprazolam, and midazolam. It also covers non-BZD hypnotics like zopiclone, zolpidem, and zaleplon that act on specific BZD receptor subunits. Melatonin and ramelteon, which act as melatonin receptor agonists, are also discussed. The concluding section notes that long-acting BZDs can cause next day sedation while flumazenil acts as a BZD antagonist to
Here are the key points regarding SAR of HDAC inhibitors from the research article:
- Hydroxamic acid zinc binding group is essential for HDAC inhibitory activity. Removing this group drastically reduced potency.
- Variations in the cap group (portion above hydroxamic acid) had significant effects on isoform selectivity.
- Shorter linker lengths between the cap and hydroxamic acid improved potency and selectivity for certain HDAC isoforms.
- Hydrophobic substituents on the phenyl ring of the cap group enhanced potency, while polar groups decreased it.
- Introducing methyl groups in the ortho and para positions of the phenyl ring improved potency and selectivity.
- Bicy
This document summarizes various anti-anxiety drugs including benzodiazepines, 5-HT1A agonists, melatonin receptor agonists, and barbiturates. It describes how these drugs work by potentiating GABA receptors in the brain to produce sedative and anxiolytic effects. Specific drugs mentioned include diazepam, buspirone, remelteon, phenobarbital, and thiopental. The document also discusses the pharmacokinetics, uses, and side effects of these different classes of anti-anxiety medications.
MANAGEMENT OF SUBSTANCE RELATED PSYCHIATRIC DISORDERSEDATIVE, HYPNOTIC AND A...Dr Slayer
SEDATIVE, HYPNOTIC AND ANXIOLYTIC - 3 groups of drugs associated with this class of substance-related disorders
Associated with physical and psychological dependence also withdrawal symptoms
This document discusses anxiety disorders and treatments for anxiety. It notes that anxiety involves feelings of tension, apprehension and fear from unknown sources, along with physical symptoms like increased heart rate. Mild anxiety is common, but severe chronic anxiety can be treated with anti-anxiety medications or therapy. Benzodiazepines are commonly used anti-anxiety drugs that work by enhancing the inhibitory neurotransmitter GABA, but can cause dependence with long-term use. Other options include antidepressants, buspirone, barbiturates, and newer non-benzodiazepine drugs.
This document discusses anxiolytic and hypnotic drugs. It describes how these drugs work by modulating neurotransmitters like GABA and glutamate. Common classes of anxiolytic drugs are benzodiazepines and 5-HT1A agonists which enhance the effects of the inhibitory neurotransmitter GABA. Benzodiazepines bind to GABA receptors to open chloride channels more frequently. Barbiturates also potentiate GABA but prolong the opening of chloride channels. These drugs are used to treat anxiety disorders and insomnia by their sedative, anxiolytic, and muscle relaxing effects. Common side effects include drowsiness but benzodiazepines have a lower risk of dependence than barbiturates
Sedative-hypnotic drug, chemical substance used to reduce tension and anxiety and induce calm (sedative effect) or to induce sleep (hypnotic effect). and An anxiolytic is a medication or other intervention that inhibits anxiety. This effect is in contrast to anxiogenic agents, which increase anxiety. Together these categories of psychoactive compounds or interventions may be referred to as anxiotropic compounds or agents.
This document discusses anxiolytics and hypnotics such as benzodiazepines and barbiturates. It describes how these drugs work by enhancing the effects of the neurotransmitter GABA at GABA receptors in the brain, resulting in sedation, anxiety reduction, and sleep induction. Both classes of drugs are controlled substances due to their potential for dependence and withdrawal symptoms. While benzodiazepines are still commonly used, barbiturates have been largely replaced due to greater safety and tolerability of benzodiazepines.
This document discusses sedatives and hypnotics. It defines sedatives as drugs that reduce excitement and produce calming effects without inducing sleep, while hypnotics produce sleep resembling natural sleep. Both act through GABA receptors in the brain. Common classes discussed are benzodiazepines, which potentiate GABA receptors, and barbiturates, which directly activate chloride channels. Specific drugs are described along with their mechanisms, effects, uses, and toxicity risks. Sleep cycles and how different drug classes impact sleep stages are also outlined.
The document discusses various classes of drugs used to treat anxiety disorders, including benzodiazepines, SSRIs, TCAs, buspirone, beta-blockers, and MAOIs. Benzodiazepines are commonly used for generalized anxiety, OCD, phobias, and panic attacks but can cause dependence, tolerance, and withdrawal symptoms. SSRIs like fluoxetine are also often used as first-line treatments for their anxiety disorders due to their safety profile. TCAs may be used for anxiety associated with depression or panic attacks. Buspirone is used for mild anxiety disorders. Beta-blockers can help reduce the somatic symptoms of anxiety. MAOIs require dietary restrictions
This document provides information about sedatives and hypnotics. It defines sedatives as drugs that reduce excitement and calm patients without inducing sleep, while hypnotics produce sleep resembling natural sleep. Both act through facilitating GABA neurotransmission. Common classes discussed are benzodiazepines, barbiturates, antihistamines, and other newer non-benzodiazepine drugs. Their mechanisms, clinical uses, and side effects are explained. Sedatives are used to relieve anxiety and cause sedation, while hypnotics are used for sleep initiation or maintenance.
This document discusses sedative/hypnotics and anxiolytics. It begins by explaining how these drugs work in the nervous system, producing sedation, hypnosis, and effects ranging from confusion to coma and death depending on dose. It then focuses on benzodiazepines and barbiturates, the two major classes of these drugs. Both act by enhancing GABAergic transmission but differ in their mechanisms and properties. Benzodiazepines are generally safer with less respiratory depression but can cause dependence, while barbiturates have greater toxicity and abuse potential. The document emphasizes using these drugs only short-term to avoid adverse effects.
Benzodiazepines are commonly prescribed sedative-hypnotic agents that were introduced in 1960. They are used for conditions like anxiety, insomnia, alcohol withdrawal, and seizures by enhancing the effects of the inhibitory neurotransmitter GABA. While generally safe, benzodiazepines can cause side effects with prolonged use or overdose like dependence, withdrawal symptoms, and respiratory depression. The effects of different benzodiazepines vary based on their ability to cross the blood-brain barrier and metabolism, with short-acting agents having faster onsets but shorter durations of action.
Reviews the uses for benzodiazepines and barbiturates, the signs of intoxication and withdrawal, impact on sports performance. Continuing Education for mental health and substance abuse counselors and therapists.
Sedative-hypnotic drugs act on the central nervous system to produce a calming effect. Barbiturates were commonly used but have been largely replaced by benzodiazepines due to their safer profile. Both classes of drugs act by enhancing the effects of the inhibitory neurotransmitter GABA at GABA receptors in the brain. This causes sedation, hypnosis, anxiety relief and other effects depending on the specific drug and dose. While effective for treating conditions like anxiety, these drugs can also cause side effects like dependence and withdrawal symptoms with prolonged use.
The document discusses anti-anxiety drugs such as benzodiazepines. Researchers discovered that these drugs act by enhancing the effects of the neurotransmitter GABA, which has an inhibitory effect in the brain. Specifically, benzodiazepines were found to bind to GABA receptor sites and stimulate GABA activity, reducing anxiety. Extensive research over decades uncovered that GABA, benzodiazepines, barbiturates, and other sedative drugs act on the same receptor complex to increase the flow of chloride ions into neurons, hyperpolarizing the cells and decreasing neuronal excitability. However, the exact endogenous ligand that normally binds to the benzodiazepine site on the GABA receptor remains unknown
This document summarizes sedative hypnotic drugs, including their mechanisms of action, pharmacokinetics, and clinical uses. It discusses how these drugs act on GABA receptors in the central nervous system to produce sedation, hypnosis, and anesthesia. Specific drug classes covered include benzodiazepines, barbiturates, buspirone, zolpidem, zaleplon, and ramelteon. Ideal properties of hypnotic drugs and their unwanted effects such as tolerance and dependence are also summarized.
The document discusses sedative-hypnotic drugs and their uses. It describes the phases of sleep including non-REM sleep and REM sleep. Some key points are:
- Benzodiazepines are commonly used as hypnotics for insomnia and as anxiolytics for acute anxiety. Short acting BDZs are preferred to avoid daytime sedation.
- BDZs potentiate the effects of GABA by binding to sites adjacent to the GABA receptor. This increases chloride ion conductance and membrane hyperpolarization.
- While effective, long-term BDZ use can cause tolerance, dependence, and cognitive impairment so they should only be used short-term for severe anxiety and insomnia.
This document discusses anti-anxiety drugs and classifies them into different categories. It describes how benzodiazepines are commonly used anti-anxiety drugs that work by binding to GABA receptors in the brain to reduce anxiety symptoms. Azapirone drugs like Buspirone are newer anti-anxiety medications that relieve mild to moderate anxiety without the side effects of benzodiazepines. Beta blockers can provide symptomatic relief from physical anxiety symptoms but do not affect the underlying psychological symptoms. Anti-anxiety drugs aim to control anxiety symptoms and produce a calm state of mind without impairing normal brain and body function.
This document discusses sedative-hypnotic drugs. It notes that this drug classification is based on clinical uses of sedation and encouraging sleep rather than chemical structure. Common sedative-hypnotic drugs include benzodiazepines, barbiturates, and newer nonbenzodiazepine hypnotics like zolpidem, zaleplon, and eszopiclone. These drugs work by enhancing the effects of the inhibitory neurotransmitter GABA at GABA receptors in the brain. Their clinical uses include treatment of anxiety, insomnia, and as sedatives for medical and surgical procedures.
Sedatives and Hypnotics
Pharmacology
Clinical uses
Sedation
Coping with stress and anxiety
Smoothing effects of stimulants
Potentiation of narcotics
Treatment of serious mental disorders
Pleasurable sensations, including intoxication
Classifications
Benzodiazepines
Diazepam, Clonazepam, Oxazepam, Clobazam, Clordiazepoxide, Midazolam
Barbiturates
Phenobarbitone, Amobarbital, Thiopental-Na
Newer drugs
Zolpidem, Zaleplon, Buspirone
Chloral hydrate
Paraldehyde
Diphenhydramine
Benzodiazepines
Properties
High therapeutic index (high LD50)
Relatively safe in overdose
Develop tolerance slowly
Less addiction liability
Benzodiazepines
Benzodiazepines
Most commonly prescribed Benzodiazepines
All Benzodiazepines are classified as Controlled Drugs in some countries.
Most are CD Schedule 4
Diazepam (Valium,Anxicalm)
Alprazolam (Xanax)
Bromazepam (Lexotan)
Clobazam (Frisium)
Lormetazepam (Noctamid)
Nitrazepam (Mogadon)
Clonazepam
Two are CD Schedule 3
Flurazepam (Rohypnol)
Temazepam (Nortem)
Structure Activity Relationship
In ring A an electron – withdrawing group such as Cl, Br, NO2 or CN at position 7.
A methyl Group is attached to the nitrogen atom in position 1 in ring B. However, substituents at position 1 that are metabolically are still clinically useful e.g. Flurazepam.
Replacement of the carbonyl function with two hydrogens in position 2 gives medazepam, less potent than diazepam.
Replacement of one of the hydrogen with a OH group on position 3 lower the activity on the one hand and aids elimination on the other.
Introduction of a carbonyl function in the 3 position increases the duration of action and also favours formation of water soluble salts.
e) α-pyridyl derivative and cycloalkyl substituent at 5 position give potent compounds.
f) Electronegative substituents such as Cl or F at the ortho and disubstituted in both ortho positions in ring C.
g) Derivatives with additional rings joining the diazepine nucleus at the 1 and 2 positions are generally more active than the corresponding 1-methylbenzodiazepines.
h) Replacement of the benzene ring by heteroaromatic (e.g. pyrazole) resulted in compounds with interesting anxiolytic properties ( e.g. ripazepam).
i) Saturation of the 4,5- double bond reduces potency, as does a shift of the unsaturation into the 3,4-position.
Barbiturates
Barbiturates
Barbiturates
Barbiturate poisoning
Treatment of Barbiturate poisoning
Buspirone
This document classifies anxiolytics and sedative/hypnotic drugs according to their mechanism of action. It divides them into four main categories: 1) drugs that facilitate GABA-A action like barbiturates and benzodiazepines, 2) 5-HT1A partial agonists like buspirone, 3) melatonin receptor agonists like ramelteon, and 4) orexin receptor antagonists like lemborexant. It also lists some non-primary anxiolytic or sedative drugs that can have anxiolytic or hypnotic effects, such as certain antidepressants, antipsychotics, antihistamines, and beta blockers.
This document summarizes different classes of sedative-hypnotic drugs, including benzodiazepines, barbiturates, non-benzodiazepine hypnotics (Z-drugs), melatonin agonists, and orexin antagonists. It describes their mechanisms of action, indications, pharmacokinetics, adverse effects, and contraindications. Sedative-hypnotics work by enhancing the effects of the inhibitory neurotransmitter GABA or by antagonizing orexin receptors to reduce arousal. Common side effects include drowsiness, respiratory depression, and withdrawal symptoms upon discontinuation. Long-term use carries risks of tolerance and dependence that limit the use of certain agents like
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This document summarizes various anti-anxiety drugs including benzodiazepines, 5-HT1A agonists, melatonin receptor agonists, and barbiturates. It describes how these drugs work by potentiating GABA receptors in the brain to produce sedative and anxiolytic effects. Specific drugs mentioned include diazepam, buspirone, remelteon, phenobarbital, and thiopental. The document also discusses the pharmacokinetics, uses, and side effects of these different classes of anti-anxiety medications.
MANAGEMENT OF SUBSTANCE RELATED PSYCHIATRIC DISORDERSEDATIVE, HYPNOTIC AND A...Dr Slayer
SEDATIVE, HYPNOTIC AND ANXIOLYTIC - 3 groups of drugs associated with this class of substance-related disorders
Associated with physical and psychological dependence also withdrawal symptoms
This document discusses anxiety disorders and treatments for anxiety. It notes that anxiety involves feelings of tension, apprehension and fear from unknown sources, along with physical symptoms like increased heart rate. Mild anxiety is common, but severe chronic anxiety can be treated with anti-anxiety medications or therapy. Benzodiazepines are commonly used anti-anxiety drugs that work by enhancing the inhibitory neurotransmitter GABA, but can cause dependence with long-term use. Other options include antidepressants, buspirone, barbiturates, and newer non-benzodiazepine drugs.
This document discusses anxiolytic and hypnotic drugs. It describes how these drugs work by modulating neurotransmitters like GABA and glutamate. Common classes of anxiolytic drugs are benzodiazepines and 5-HT1A agonists which enhance the effects of the inhibitory neurotransmitter GABA. Benzodiazepines bind to GABA receptors to open chloride channels more frequently. Barbiturates also potentiate GABA but prolong the opening of chloride channels. These drugs are used to treat anxiety disorders and insomnia by their sedative, anxiolytic, and muscle relaxing effects. Common side effects include drowsiness but benzodiazepines have a lower risk of dependence than barbiturates
Sedative-hypnotic drug, chemical substance used to reduce tension and anxiety and induce calm (sedative effect) or to induce sleep (hypnotic effect). and An anxiolytic is a medication or other intervention that inhibits anxiety. This effect is in contrast to anxiogenic agents, which increase anxiety. Together these categories of psychoactive compounds or interventions may be referred to as anxiotropic compounds or agents.
This document discusses anxiolytics and hypnotics such as benzodiazepines and barbiturates. It describes how these drugs work by enhancing the effects of the neurotransmitter GABA at GABA receptors in the brain, resulting in sedation, anxiety reduction, and sleep induction. Both classes of drugs are controlled substances due to their potential for dependence and withdrawal symptoms. While benzodiazepines are still commonly used, barbiturates have been largely replaced due to greater safety and tolerability of benzodiazepines.
This document discusses sedatives and hypnotics. It defines sedatives as drugs that reduce excitement and produce calming effects without inducing sleep, while hypnotics produce sleep resembling natural sleep. Both act through GABA receptors in the brain. Common classes discussed are benzodiazepines, which potentiate GABA receptors, and barbiturates, which directly activate chloride channels. Specific drugs are described along with their mechanisms, effects, uses, and toxicity risks. Sleep cycles and how different drug classes impact sleep stages are also outlined.
The document discusses various classes of drugs used to treat anxiety disorders, including benzodiazepines, SSRIs, TCAs, buspirone, beta-blockers, and MAOIs. Benzodiazepines are commonly used for generalized anxiety, OCD, phobias, and panic attacks but can cause dependence, tolerance, and withdrawal symptoms. SSRIs like fluoxetine are also often used as first-line treatments for their anxiety disorders due to their safety profile. TCAs may be used for anxiety associated with depression or panic attacks. Buspirone is used for mild anxiety disorders. Beta-blockers can help reduce the somatic symptoms of anxiety. MAOIs require dietary restrictions
This document provides information about sedatives and hypnotics. It defines sedatives as drugs that reduce excitement and calm patients without inducing sleep, while hypnotics produce sleep resembling natural sleep. Both act through facilitating GABA neurotransmission. Common classes discussed are benzodiazepines, barbiturates, antihistamines, and other newer non-benzodiazepine drugs. Their mechanisms, clinical uses, and side effects are explained. Sedatives are used to relieve anxiety and cause sedation, while hypnotics are used for sleep initiation or maintenance.
This document discusses sedative/hypnotics and anxiolytics. It begins by explaining how these drugs work in the nervous system, producing sedation, hypnosis, and effects ranging from confusion to coma and death depending on dose. It then focuses on benzodiazepines and barbiturates, the two major classes of these drugs. Both act by enhancing GABAergic transmission but differ in their mechanisms and properties. Benzodiazepines are generally safer with less respiratory depression but can cause dependence, while barbiturates have greater toxicity and abuse potential. The document emphasizes using these drugs only short-term to avoid adverse effects.
Benzodiazepines are commonly prescribed sedative-hypnotic agents that were introduced in 1960. They are used for conditions like anxiety, insomnia, alcohol withdrawal, and seizures by enhancing the effects of the inhibitory neurotransmitter GABA. While generally safe, benzodiazepines can cause side effects with prolonged use or overdose like dependence, withdrawal symptoms, and respiratory depression. The effects of different benzodiazepines vary based on their ability to cross the blood-brain barrier and metabolism, with short-acting agents having faster onsets but shorter durations of action.
Reviews the uses for benzodiazepines and barbiturates, the signs of intoxication and withdrawal, impact on sports performance. Continuing Education for mental health and substance abuse counselors and therapists.
Sedative-hypnotic drugs act on the central nervous system to produce a calming effect. Barbiturates were commonly used but have been largely replaced by benzodiazepines due to their safer profile. Both classes of drugs act by enhancing the effects of the inhibitory neurotransmitter GABA at GABA receptors in the brain. This causes sedation, hypnosis, anxiety relief and other effects depending on the specific drug and dose. While effective for treating conditions like anxiety, these drugs can also cause side effects like dependence and withdrawal symptoms with prolonged use.
The document discusses anti-anxiety drugs such as benzodiazepines. Researchers discovered that these drugs act by enhancing the effects of the neurotransmitter GABA, which has an inhibitory effect in the brain. Specifically, benzodiazepines were found to bind to GABA receptor sites and stimulate GABA activity, reducing anxiety. Extensive research over decades uncovered that GABA, benzodiazepines, barbiturates, and other sedative drugs act on the same receptor complex to increase the flow of chloride ions into neurons, hyperpolarizing the cells and decreasing neuronal excitability. However, the exact endogenous ligand that normally binds to the benzodiazepine site on the GABA receptor remains unknown
This document summarizes sedative hypnotic drugs, including their mechanisms of action, pharmacokinetics, and clinical uses. It discusses how these drugs act on GABA receptors in the central nervous system to produce sedation, hypnosis, and anesthesia. Specific drug classes covered include benzodiazepines, barbiturates, buspirone, zolpidem, zaleplon, and ramelteon. Ideal properties of hypnotic drugs and their unwanted effects such as tolerance and dependence are also summarized.
The document discusses sedative-hypnotic drugs and their uses. It describes the phases of sleep including non-REM sleep and REM sleep. Some key points are:
- Benzodiazepines are commonly used as hypnotics for insomnia and as anxiolytics for acute anxiety. Short acting BDZs are preferred to avoid daytime sedation.
- BDZs potentiate the effects of GABA by binding to sites adjacent to the GABA receptor. This increases chloride ion conductance and membrane hyperpolarization.
- While effective, long-term BDZ use can cause tolerance, dependence, and cognitive impairment so they should only be used short-term for severe anxiety and insomnia.
This document discusses anti-anxiety drugs and classifies them into different categories. It describes how benzodiazepines are commonly used anti-anxiety drugs that work by binding to GABA receptors in the brain to reduce anxiety symptoms. Azapirone drugs like Buspirone are newer anti-anxiety medications that relieve mild to moderate anxiety without the side effects of benzodiazepines. Beta blockers can provide symptomatic relief from physical anxiety symptoms but do not affect the underlying psychological symptoms. Anti-anxiety drugs aim to control anxiety symptoms and produce a calm state of mind without impairing normal brain and body function.
This document discusses sedative-hypnotic drugs. It notes that this drug classification is based on clinical uses of sedation and encouraging sleep rather than chemical structure. Common sedative-hypnotic drugs include benzodiazepines, barbiturates, and newer nonbenzodiazepine hypnotics like zolpidem, zaleplon, and eszopiclone. These drugs work by enhancing the effects of the inhibitory neurotransmitter GABA at GABA receptors in the brain. Their clinical uses include treatment of anxiety, insomnia, and as sedatives for medical and surgical procedures.
Sedatives and Hypnotics
Pharmacology
Clinical uses
Sedation
Coping with stress and anxiety
Smoothing effects of stimulants
Potentiation of narcotics
Treatment of serious mental disorders
Pleasurable sensations, including intoxication
Classifications
Benzodiazepines
Diazepam, Clonazepam, Oxazepam, Clobazam, Clordiazepoxide, Midazolam
Barbiturates
Phenobarbitone, Amobarbital, Thiopental-Na
Newer drugs
Zolpidem, Zaleplon, Buspirone
Chloral hydrate
Paraldehyde
Diphenhydramine
Benzodiazepines
Properties
High therapeutic index (high LD50)
Relatively safe in overdose
Develop tolerance slowly
Less addiction liability
Benzodiazepines
Benzodiazepines
Most commonly prescribed Benzodiazepines
All Benzodiazepines are classified as Controlled Drugs in some countries.
Most are CD Schedule 4
Diazepam (Valium,Anxicalm)
Alprazolam (Xanax)
Bromazepam (Lexotan)
Clobazam (Frisium)
Lormetazepam (Noctamid)
Nitrazepam (Mogadon)
Clonazepam
Two are CD Schedule 3
Flurazepam (Rohypnol)
Temazepam (Nortem)
Structure Activity Relationship
In ring A an electron – withdrawing group such as Cl, Br, NO2 or CN at position 7.
A methyl Group is attached to the nitrogen atom in position 1 in ring B. However, substituents at position 1 that are metabolically are still clinically useful e.g. Flurazepam.
Replacement of the carbonyl function with two hydrogens in position 2 gives medazepam, less potent than diazepam.
Replacement of one of the hydrogen with a OH group on position 3 lower the activity on the one hand and aids elimination on the other.
Introduction of a carbonyl function in the 3 position increases the duration of action and also favours formation of water soluble salts.
e) α-pyridyl derivative and cycloalkyl substituent at 5 position give potent compounds.
f) Electronegative substituents such as Cl or F at the ortho and disubstituted in both ortho positions in ring C.
g) Derivatives with additional rings joining the diazepine nucleus at the 1 and 2 positions are generally more active than the corresponding 1-methylbenzodiazepines.
h) Replacement of the benzene ring by heteroaromatic (e.g. pyrazole) resulted in compounds with interesting anxiolytic properties ( e.g. ripazepam).
i) Saturation of the 4,5- double bond reduces potency, as does a shift of the unsaturation into the 3,4-position.
Barbiturates
Barbiturates
Barbiturates
Barbiturate poisoning
Treatment of Barbiturate poisoning
Buspirone
This document classifies anxiolytics and sedative/hypnotic drugs according to their mechanism of action. It divides them into four main categories: 1) drugs that facilitate GABA-A action like barbiturates and benzodiazepines, 2) 5-HT1A partial agonists like buspirone, 3) melatonin receptor agonists like ramelteon, and 4) orexin receptor antagonists like lemborexant. It also lists some non-primary anxiolytic or sedative drugs that can have anxiolytic or hypnotic effects, such as certain antidepressants, antipsychotics, antihistamines, and beta blockers.
This document summarizes different classes of sedative-hypnotic drugs, including benzodiazepines, barbiturates, non-benzodiazepine hypnotics (Z-drugs), melatonin agonists, and orexin antagonists. It describes their mechanisms of action, indications, pharmacokinetics, adverse effects, and contraindications. Sedative-hypnotics work by enhancing the effects of the inhibitory neurotransmitter GABA or by antagonizing orexin receptors to reduce arousal. Common side effects include drowsiness, respiratory depression, and withdrawal symptoms upon discontinuation. Long-term use carries risks of tolerance and dependence that limit the use of certain agents like
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Benzodiazepines are a class of drugs commonly used to treat anxiety. They work by enhancing the effects of the neurotransmitter GABA at GABAA receptors in the brain. The most commonly prescribed benzodiazepines include diazepam, alprazolam, lorazepam, and clonazepam. While effective for treating anxiety, benzodiazepines can cause side effects like sedation and memory impairment. They also carry risks of tolerance, dependence, and withdrawal symptoms with long-term use. Benzodiazepines should only be used short-term to treat severe anxiety, insomnia, or muscle spasms, and are not recommended for mild or occasional
This document discusses drugs that act on the central nervous system (CNS), specifically sedative-hypnotic drugs. It covers the classification of CNS depressants like benzodiazepines and barbiturates. It describes their mechanisms of action, effects on the CNS, cardiovascular system, respiratory system, and liver. It also discusses their therapeutic uses, adverse effects, dependence and abuse potential, as well as management of overdoses.
This document provides an overview of the pharmacology of anxiolytics and hypnotics. It defines anxiety and its pathological forms. Anxiolytics such as benzodiazepines act by enhancing GABAergic transmission in the brain. Hypnotics like benzodiazepines and barbiturates produce sedation and hypnosis by increasing the effect of the inhibitory neurotransmitter GABA. Both classes have the potential for dependence and withdrawal symptoms with prolonged use. The document discusses the mechanisms, pharmacokinetics, effects and side effects of major anxiolytic and hypnotic drug classes and agents.
Sedative hypnotics are drugs that can reduce anxiety and induce sleep. Common classes include barbiturates and benzodiazepines. Barbiturates act by facilitating GABA activity while benzodiazepines enhance the effect of GABA at its receptor. Benzodiazepines are preferred over barbiturates due to their higher therapeutic index and less impact on respiration. They are used to treat anxiety, insomnia, and seizures. Side effects include drowsiness and dependence with long term use. Newer non-benzodiazepine drugs like zolpidem are also used as hypnotics while buspirone treats anxiety through serotonin receptor agonism with less sedation
This document discusses various sedative and hypnotic drugs. It describes how sedatives produce calming effects while hypnotics induce sleep. Both can cause CNS depression. It then covers the classification, mechanisms of action, pharmacological effects, and uses of benzodiazepines, newer agents like melatonin and ramelteon, 'Z' hypnotics, and barbiturates. It provides details on how each group of drugs works, their advantages over other groups, and important considerations for their use.
This document summarizes different classes of sedative and hypnotic drugs. It discusses barbiturates, benzodiazepines including long-acting and short-acting types, non-benzodiazepine agonists at BZD receptors, imides, alcohols, and miscellaneous sedatives/hypnotics. For each class, it provides examples of drugs, their mechanisms of action, effects, and metabolic pathways. The document was prepared by a pharmacy student as part of their coursework.
This document discusses insomnia and treatments for it, focusing on hypnotic medications. It defines insomnia as difficulty initiating or maintaining sleep. Cognitive behavioral therapy and sleep hygiene measures are recommended for long-term insomnia to address anxiety and behaviors that worsen sleep. Hypnotic medications like benzodiazepines are recommended for short-term use by targeting the GABA system to reduce arousal and promote sleep. While effective, benzodiazepines can cause dependence and withdrawal symptoms with long-term use. The document compares properties of different classes of hypnotic medications and their mechanisms of action and metabolism.
The document summarizes information about various sedative-hypnotic drugs including barbiturates, benzodiazepines, and other related compounds. It describes their mechanisms of action, pharmacokinetics, therapeutic uses, precautions, and adverse effects. Specifically, it notes that while barbiturates were widely used in the 20th century, their use has been replaced by benzodiazepines and other drugs due to the barbiturates' high abuse potential and narrow therapeutic window.
This document summarizes different classes of sedative hypnotics and antianxiety drugs. It discusses benzodiazepines, barbiturates, nonbenzodiazepine hypnotics, melatonin receptor agonists, and selective serotonin reuptake inhibitors. The main points covered are the mechanism of action, pharmacological effects, uses, and adverse effects of these drug classes. Specific examples are provided for different drugs within each class.
This document discusses sedatives and hypnotics, including their classification, pharmacology, and mechanisms of action. Sedatives calm without inducing sleep, while hypnotics induce sleep. Barbiturates, benzodiazepines, and non-benzodiazepines are common classes of hypnotics and sedatives. Barbiturates act primarily at GABA receptors to potentiate inhibition, while benzodiazepines enhance GABA effects through binding a separate site on GABA-A receptors. Newer non-benzodiazepine hypnotics like zolpidem and zopiclone act selectively on receptor subunits involved in sleep induction. Together these drugs provide options
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)NarminHamaaminHussen
Sedative and hypnotic drugs act on the central nervous system by depressing activity. Sedatives decrease excitement without causing drowsiness, while hypnotics produce sleep. The same drugs can act as sedatives at low doses and hypnotics at higher doses in a dose-dependent manner. Most sedatives and hypnotics work by enhancing the effects of the inhibitory neurotransmitter GABA at GABAA receptors. Benzodiazepines are a commonly used class of sedative and hypnotic drugs that work through this GABAergic mechanism of action. Their effects and pharmacokinetic properties depend on their chemical structure and metabolism.
complete and detail study of the topic of sedative and hypnotics under the guidance of faculty member. the ppt is made for the benefit of all the peoples
Benzodiazepines are a class of drugs that enhance the effect of the neurotransmitter GABA at the GABAA receptor, resulting in sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant properties. They are used to treat anxiety, insomnia, seizures and muscle spasms. Common side effects include drowsiness. Prolonged use can lead to tolerance, physical dependence and withdrawal symptoms when discontinued. Buspirone is an anxiolytic drug used to treat generalized anxiety disorder that acts on serotonin and dopamine receptors without sedative effects. Beta blockers reduce physiological symptoms of anxiety by blocking adrenaline receptors but are not FDA approved for anxiety disorders.
This document summarizes information about sedative hypnotics. It describes sedatives as drugs that calm without inducing sleep, hypnotics as drugs that induce and maintain sleep, and anxiolytics and amnesiacs as drugs that relieve anxiety and cause memory loss respectively. It discusses how the same drug can have different effects at different doses. The document then focuses on benzodiazepines, describing their mechanism of action on GABA receptors, pharmacological effects, pharmacokinetics, clinical uses, adverse effects, tolerance, dependence, and withdrawal symptoms. It also discusses the benzodiazepine antagonist flumazenil.
This document discusses various sedative-hypnotic drugs including benzodiazepines, barbiturates, non-benzodiazepine hypnotics, melatonin agonists, and atypical anxiolytics. It provides details on their mechanisms of action, effects on sleep, pharmacokinetics, therapeutic uses, adverse effects, and guidelines for treatment of insomnia. Hypnotics that act at GABAA receptors like benzodiazepines are preferred over barbiturates due to greater safety. Drugs with shorter half-lives are favored for sleep-onset insomnia while those with longer half-lives can be used for daytime anxiety. Non-pharmacological therapies are
Introduction
What are Sedatives??
“A drug that subdue excitement and calms the patient without inducing sleep. Though the drowsiness may
be produced.”
► It also refers to the decrease in responsiveness to stimulation, along with this ,it also decrease the
alertness,ideation, and motor activities.
What are Hypnotics???
► “ These are the drugs that causes the sleep which resembles with the natural sleep”.
► These are having quicker action,shorter duration and steeper DRC while sedatives having slow on set of
action with flatter DRC
► Hypnotics at lower dose sedative
► There are different grades of CNS depressants
► Sedation Hypnosis General anaesthesia
Difference between Sedative &
Hypnotics
Sedative
► A drug that reduces excitement,calms the
patient without inducing sleep
► Sedative in therapeutic doses are
anxiolytics
► At larger doses causes hypnosis
► Site of action is on limbic system
► Examples- diazepam,lorazepam,etc.
Hypnotics
► Sleep producing drugs
► Used for inititation or maintain the sleep
► At high doses causes general anaesthesia
► Site of action is in midbrain & acending
RAS which maintains wakefullness
► Examples – zopiclone,phenobarbitone
DRC for two hypothetical
sedative - Hypnotics
• Drug A – An increase in dose higher than that needed for
hypnosis may lead to state of general anaesthesia.
• With higher doses , the durg will depresses the respiratory and
vasomotor centers which leads to coma.
• Steeper DRC, Narrow margin of safety
• Drug A is an example of alcohol and Barbiturates.
• Drug B – Needs greater dose to achieve CNS depression
• Drug B is an example of benzodiazepine and newer hypnotics
• Flatter DRc, greater margin of safety
► Sleep
1. NREM – In this there is no fast movement of eyes.It occurres between stage 0 to 4
2. REM – In this eye movements are very fast.
► Stage of NREM-
► Stage 0 [ awake]- It is condition from lying down to falling a sleep(1-2%)
► Stage 1 [dosing]– Eye movement decrease,body muscles relax (5-10%)
► Stage 2 [unequivocal sleep]– more decrease in eye movements, person may arousable.(50%)
► Stage 3 deep sleep transition]– Deeper sleep with minimum eye movements,not easily arousal.
► Stage 4[cerebral sleep] – deepest level of sleep, GH secretion increased, no eye movements, muscles are
fully relaxed, if awakened causes disorientation.(20%)
► REM – dreaming, HR,breathing rate, brain activity increases and relaxation of voluntary muscles.
Classification
► Benzodizepines1. Hypnotics-Diazepam,flurazepam,Nitrazepam,Alprazolam,Lorazepam,Templepatrick,Triazolam
2. Antianxiety-Diazepam, Chlordiazeperoxide, Oxazepam, Lorazepam, Alprazolam, Clonazepam
3. Anticonvulsant- Clonazepam, clobazam, Diazepam, Loranzepam
► Barbiturates1. Long acting- phenobarbitone
2. Short acting- butobarbitone, Phenobarbitone
3. Ultrashort acting- Thiopentone, Methohexitone
Non- benzodiazepines- Zopiclone, Eszopiclone, Zolpidem, Zaleplon, Etisalat
► Other Hypnotics- Triclofos, Melatonin, Ramelteon, Suvorexant
The document provides an overview of key concepts for working with spreadsheets in Excel, including spreadsheet components like cells, ranges, and worksheets; entering labels and values; using formulas and functions; formatting cells and worksheets; and creating different types of charts to visually represent numeric data. The summary covers the essential elements of working with Excel spreadsheets, such as entering data into cells, writing formulas, formatting cells and worksheets, and creating charts to analyze and present numeric data.
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The document provides information about a book titled "Practical Research Methods" by Dr. Catherine Dawson. The book offers practical guidance for conducting research and assumes no prior experience. It covers topics such as defining a research project, choosing methodologies and methods, conducting interviews and focus groups, analyzing data, and reporting findings. The book aims to help turn research ideas into workable projects and provide advice throughout the research process.
1. Nuclear magnetic resonance spectroscopy uses radio waves and strong magnetic fields to analyze organic molecules. It can identify carbon-hydrogen frameworks and determine the number and type of hydrogen and carbon atoms in a molecule.
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Powders can be prepared on a small scale using mortars and pestles or spatulas for mixing. Larger scale mixing uses specialized equipment to rapidly and uniformly blend ingredients. Divided powders contain individually weighed doses packaged in paper or foil for administration. Bulk powders include oral powders mixed with water, dentifrices, dusting powders, and insufflations introduced into body cavities. Special techniques are needed for volatile, hygroscopic, or deliquescent substances to avoid degradation or inaccuracies in dosing.
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4. The document also covers prescription handling, labeling requirements, and fundamental operations involved in compounding like weights and measures, size reduction,
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In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
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These lecture slides, by Dr Sidra Arshad, offer a simplified look into the mechanisms involved in the regulation of respiration:
Learning objectives:
1. Describe the organisation of respiratory center
2. Describe the nervous control of inspiration and respiratory rhythm
3. Describe the functions of the dorsal and respiratory groups of neurons
4. Describe the influences of the Pneumotaxic and Apneustic centers
5. Explain the role of Hering-Breur inflation reflex in regulation of inspiration
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7. Explain the role of peripheral chemoreceptors in regulation of respiration
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2. Chapter 36, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 13, Human Physiology by Lauralee Sherwood, 9th edition
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2. • An effective sedative (anxiolytic) agent should
reduce anxiety and exert a calming effect. The
degree of central nervous system depression
caused by a sedative should be the minimum
consistent with therapeutic efficacy.
• A sedative drug decreases activity, moderates
excitement, and calms the recipient.
3. • A hypnotic drug should produce drowsiness and
encourage the onset and maintenance of a state
of sleep. Hypnotic effects involve more
pronounced depression of the central nervous
system than sedation, and this can be achieved
with many drugs in this class simply by increasing
the dose.
• Graded dose-dependent depression of central
nervous system function is a characteristic of
most sedative-hypnotics.
4. • Hypnotic drug produces drowsiness and
facilitates the onset and maintenance of a
state of sleep that resembles natural sleep in
its electroencephalographic characteristics
and from which the recipient can be aroused
easily.
5. Anxiety disorders as recognised clinically include:
• generalised anxiety disorder (an ongoing state of
excessive anxiety lacking any clear reason or focus)
• panic disorder (sudden attacks of overwhelming fear
occur in association with marked somatic symptoms,
such as sweating, tachycardia, chest pains, trembling
and choking). Such attacks can be induced even in
normal individuals by infusion of sodium lactate, and
the condition appears to have a genetic component)
6. • phobias (strong fears of specific objects or
situations, e.g. snakes, open spaces, flying,
social interactions)
• post-traumatic stress disorder (anxiety
triggered by recall of past stressful
experiences)
• obsessive compulsive disorder (compulsive
ritualistic behaviour driven by irrational
anxiety, e.g. fear of contamination).
7. CLASSIFICATION OF ANXIOLYTIC AND
HYPNOTIC DRUGS
• Benzodiazepines. This is the most important
group, used as anxiolytic and hypnotic agents.
• Buspirone. This 5-HT1A receptor agonist is
anxiolytic but not appreciably sedative.
8. • β-Adrenoceptor antagonists (e.g. propranolol).
These are used to treat some forms of anxiety,
particularly where physical symptoms such as
sweating, tremor and tachycardia are
troublesome. Their effectiveness depends on
block of peripheral sympathetic responses rather
than on any central effects. They are sometimes
used by actors and musicians to reduce the
symptoms of stage fright, but their use by
snooker players to minimise tremor is banned as
unsportsmanlike.
9. • Zolpidem. This hypnotic acts similarly to
benzodiazepines, although chemically distinct,
but lacks appreciable anxiolytic activity.
• Barbiturates. These are now largely obsolete,
superseded by benzodiazepines. Their use is
now confined to anaesthesia and the
treatment of epilepsy.
10. • Miscellaneous other drugs (e.g. chloral
hydrate, meprobamate and methaqualone).
They are no longer recommended, but
therapeutic habits die hard and they are
occasionally used. Sedative antihistamines,
such as diphenhydramine, are sometimes
used as sleeping pills, particularly for wakeful
children. They are included in various over-
the-counter preparations intended to improve
children's sleep patterns.
11. Benzodiazepines
• The first benzodiazepine, chlordiazepoxide,
was synthesised by accident in 1961, the
unusual seven-membered ring having been
produced as a result of a reaction that went
wrong in the laboratories of Hoffman-la
Roche. Its unexpected pharmacological
activity was recognised in a routine screening
procedure, and benzodiazepines quite soon
became the most widely prescribed drugs in
the pharmacopoeia.
12. • Benzodiazepines (once thought to be acting as 'non-
specific depressants') act selectively on GABAA
receptors, which mediate fast inhibitory synaptic
transmission throughout the central nervous system
(CNS). Benzodiazepines enhance the response to GABA
by facilitating the opening of GABA-activated chloride
channels . They bind specifically to a regulatory site of
the receptor, distinct from the GABA-binding site, and
act allosterically to increase the affinity of GABA for the
receptor. Benzodiazepines do not affect receptors for
other amino acids, such as glycine or glutamate
13. • The GABAA receptor is a ligand-gated ion
channel consisting of a pentameric assembly
of different subunits, the main ones being α,β
and γ, each of which occurs in three or more
isoforms. The potential number of
combinations is therefore huge, but three
combinations predominate in the adult brain,
namely α1β2γ2, α2β3γ2 and α3β3γ2.
14. • The various combinations occur in different
parts of the brain, and linking this diversity
with physiological function and
pharmacological specificity presents a
difficult, although familiar, problem.
Sensitivity to benzodiazepines requires the
presence of both α and β subunits, and
mutation of a single amino acid (histidine) in
the α subunit eliminates benzodiazepine
sensitivity.
16. PHARMACOLOGICAL EFFECTS AND
USES
The main effects of benzodiazepines are:
• Reduction of anxiety and aggression
• Sedation and induction of sleep
• Reduction of muscle tone and coordination
• Anticonvulsant effect (clonazepam, nitrazepam,
lorazepam and diazepam)
• Anterograde amnesia.
• Anesthesia (diazepam, lorazepam and
midazolam)
17. • Benzodiazepine administration typically increases
total sleep time, largely by increasing the time
spent in stage 2 (which is the major fraction of
non-REM sleep). The effect is greatest in subjects
with the shortest baseline total sleep time.
• The number of shifts to lighter sleep stages (1
and 0) and the amount of body movement are
diminished. Nocturnal peaks in the secretion of
growth hormone, prolactin, and luteinizing
hormone are not affected.
18. BENZODIAZEPINE INVERSE AGONISTS
AND ANTAGONISTS
• The term inverse agonist is applied to drugs
that bind to benzodiazepine receptors and
exert the opposite effect to that of
conventional benzodiazepines, producing
signs of increased anxiety and convulsions.
Diazepam-binding inhibitor is an example, and
some benzodiazepine analogues act similarly.
19. • Benzodiazepine receptor exists in two distinct
conformations, only one of which (A) can bind
a GABA molecule and open the chloride
channel. The other conformation (B) cannot
bind GABA. Normally, with no benzodiazepine
receptor ligand present, there is an
equilibrium between these two
conformations; sensitivity to GABA is present
but submaximal.
20. • Benzodiazepine agonists (e.g. diazepam) are
postulated to bind preferentially to conformation
A, thus shifting the equilibrium in favour of A and
enhancing GABA sensitivity. Inverse agonists bind
selectively to B and have the opposite effect.
Competitive antagonists such as flumazenil bind
equally to A and B, and consequently do not
disturb the conformational equilibrium but
antagonise the effect of both agonists and inverse
agonists.
21. • Some of the molecular variants of the GABAA
receptor seem to show different relative
affinities for agonists, antagonists and inverse
agonists, and it is possible that this reflects
differences in the equilibrium between the A
and B states as a function of the subunit
composition of the receptor.
22. Pharmacological effects on other
organs
• Respiration
• At higher doses, such as those used for
preanesthetic medication or for endoscopy,
benzodiazepines slightly depress alveolar
ventilation and cause respiratory acidosis.
• These effects are exaggerated in patients with
chronic obstructive pulmonary disease
(COPD), and alveolar hypoxia and CO2 narcosis
may result.
23. • These drugs can cause apnea during
anesthesia or when given with opioids.
Patients severely intoxicated with
benzodiazepines only require respiratory
assistance when they also have ingested
another CNS-depressant drug, most
commonly ethanol.
24. • Hypnotic doses of benzodiazepines may
worsen sleep-related breathing disorders by
adversely affecting control of the upper airway
muscles or by decreasing the ventilatory
response to CO2. The latter effect may cause
hypoventilation and hypoxemia in some
patients with severe COPD, although
benzodiazepines may improve sleep and sleep
structure in some instances.
25. • Cardiovascular System
• In preanesthetic doses, all benzodiazepines
decrease blood pressure and increase heart rate.
• Diazepam increases coronary flow, possibly by an
action to increase interstitial concentrations of
adenosine, and the accumulation of this
cardiodepressant metabolite also may explain the
negative inotropic effects of the drug.
26. • GI Tract
• Benzodiazepines partially protect against
stress ulcers in rats, and diazepam markedly
decreases nocturnal gastric secretion in
humans.
27. PHARMACOKINETIC ASPECTS
Drugs active at the benzodiazepine receptor may be
divided into four categories based on their
elimination t1/2:
• Ultra-short-acting benzodiazepines, midazolam
• Short-acting agents (t1/2 <6 hours), including
triazolam, the non-benzodiazepine zolpidem (t1/2
~2 hours), and eszopiclone (t1/2 5-6 hours)
• Intermediate-acting agents (t1/2 6-24 hours),
including estazolam and temazepam
• Long-acting agents (t1/2 >24 hours), including
flurazepam, diazepam, and quazepam
28. • Benzodiazepines are well absorbed when
given orally, usually giving a peak plasma
concentration in about 1 hour. Some (e.g.
oxazepam, lorazepam) are absorbed more
slowly. They bind strongly to plasma protein,
and their high lipid solubility causes many of
them to accumulate gradually in body fat.
29. • They are normally given by mouth but can be
given intravenously (e.g. diazepam in status
epilepticus, midazolam in anaesthesia).
Intramuscular injection often results in slow
absorption. Diazepam can be used for alcohol
withdrawal
30. • Benzodiazepines are all metabolised and
eventually excreted as glucuronide conjugates in
the urine. They vary greatly in duration of action
Several are converted to active metabolites such
as N-desmethyldiazepam (nordiazepam), which
has a half-life of about 60 hours, and which
accounts for the tendency of many
benzodiazepines to produce cumulative effects
and long hangovers when they are given
repeatedly.
31. • The short-acting compounds are those that
are metabolised directly by conjugation with
glucuronide.
32. UNWANTED EFFECTS
• Toxic effects resulting from acute overdosage
• Benzodiazepines in acute overdose are
considerably less dangerous than other
anxiolytic/hypnotic drugs. Because such
agents are often used in attempted suicide,
this is an important advantage. In overdose,
benzodiazepines cause prolonged sleep,
without serious depression of respiration or
cardiovascular function.
33. • However, in the presence of other CNS
depressants, particularly alcohol,
benzodiazepines can cause severe, even life-
threatening, respiratory depression. The
availability of an effective antagonist,
flumazenil, means that the effects of an acute
overdose can be counteracted,3 which is not
possible for most CNS depressants.
34. • Unwanted effects occurring during normal
therapeutic use
• The main side effects of benzodiazepines are
drowsiness, confusion, amnesia and impaired
coordination, which considerably affects
manual skills such as driving performance.
Benzodiazepines enhance the depressant
effect of other drugs, including alcohol, in a
more than additive way.
35. • The long and unpredictable duration of action
of many benzodiazepines is important in
relation to side effects. Long-acting drugs such
as nitrazepam are no longer used as
hypnotics, and even shorter-acting
compounds such as lorazepam can produce a
substantial day-after impairment of job
performance and driving skill.
36. Ideal Hypnotic
• An ideal hypnotic agent would have a rapid
onset of action when taken at bedtime, a
sufficiently sustained action to facilitate sleep
throughout the night, and no residual action
by the following morning. Among the
benzodiazepines that are used commonly as
hypnotic agents, triazolam theoretically fits
this description most closely.
37. • Flurazepam might seem to be unsuitable for
this purpose because of the slow rate of
elimination of desalkylflurazepam. In practice,
there appear to be some disadvantages to the
use of agents that have a relatively rapid rate
of disappearance, including the early-morning
insomnia that is experienced by some patients
and a greater likelihood of rebound insomnia
on drug discontinuation
38. Tolerance and dependence
• Tolerance (i.e. a gradual escalation of dose
needed to produce the required effect) occurs
with all benzodiazepines, as does dependence,
which is their main drawback. They share these
properties with other hypnotics and sedatives.
Tolerance is less marked than it is with
barbiturates, which produce pharmacokinetic
tolerance because of induction of hepatic drug-
metabolising enzymes -this does not occur with
benzodiazepines. Such tolerance as does occur
appears to represent a change at the receptor
level, but the mechanism is not well understood
39. Abstinence syndrome
• Physiologic dependence can be described as an
altered physiologic state that requires continuous
drug administration to prevent an abstinence or
withdrawal syndrome.
• This syndrome is characterized by states of
increased anxiety, insomnia, and central nervous
system excitability that may progress to
convulsions. Most sedative-hypnotics—including
benzodiazepines—are capable of causing
physiologic dependence when used on a long-
term basis.
40. • When higher doses of sedative-hypnotics are used,
abrupt withdrawal leads to more serious withdrawal
signs. Differences in the severity of withdrawal
symptoms resulting from individual sedative-hypnotics
relate in part to half-life, since drugs with long half-
lives are eliminated slowly enough to accomplish
gradual withdrawal with few physical symptoms. The
use of drugs with very short half-lives for hypnotic
effects may lead to signs of withdrawal even between
doses. For example, triazolam, a benzodiazepine with a
half-life of about 4 hours, has been reported to cause
daytime anxiety when used to treat sleep disorders.
41. Benzodiazepine Antagonists:
Flumazenil
• Flumazenil blocks many of the actions of
benzodiazepines, zolpidem, zaleplon, and
eszopiclone, but does not antagonize the central
nervous system effects of other sedative-
hypnotics, ethanol, opioids, or general
anesthetics.
• Flumazenil is approved for use in reversing the
central nervous system depressant effects of
benzodiazepine overdose and to hasten recovery
following use of these drugs in anesthetic and
diagnostic procedures.
42. • When given intravenously, flumazenil acts
rapidly but has a short half-life (0.7–1.3 hours)
due to rapid hepatic clearance. Because all
benzodiazepines have a longer duration of
action than flumazenil, sedation commonly
recurs, requiring repeated administration of
the antagonist.
43. • Adverse effects of flumazenil include agitation,
confusion, dizziness, and nausea. Flumazenil
may cause a severe precipitated abstinence
syndrome in patients who have developed
physiologic benzodiazepine dependence.
44.
45. BUSPIRONE
• Buspirone is a partial agonist at 5-HT1A receptors
and is used to treat various anxiety disorders. It
also binds to dopamine receptors, but it is likely
that its 5-HT-related actions are important in
relation to anxiety suppression, because related
compounds (e.g. ipsapirone and gepirone,
neither of which are approved for clinical use,
which are highly specific for 5-HT1A receptors;
show similar anxiolytic activity in experimental
animals). 5-HT1A receptors are inhibitory
autoreceptors that reduce the release of 5-HT
and other mediators.
46. • They also inhibit the activity of noradrenergic
locus coeruleus neurons and thus interfere
with arousal reactions. However, buspirone
takes days or weeks to produce its effect in
humans, suggesting a more complex indirect
mechanism of action. Buspirone is ineffective
in controlling panic attacks or severe anxiety
states.
47. • Buspirone has side effects quite different from
those of benzodiazepines. It does not cause
sedation or motor incoordination, nor have
withdrawal effects been reported. Its main
side effects are nausea, dizziness, headache
and restlessness, which generally seem to be
less troublesome than the side effects of
benzodiazepines.
48.
49. Zolpidem
• Zolpidem is a non-benzodiazepine sedative-
hypnotic drug. It is classified as an
imidazopyridine
• The actions of zolpidem are due to agonist effects
on GABAA receptors and generally resemble
those of benzodiazepines, it produces only weak
anticonvulsant effects in experimental animals,
and its relatively strong sedative actions appear
to mask anxiolytic effects in various animal
models of anxiety
50. • Zolpidem has little effect on the stages of
sleep in normal human subjects. The drug is as
effective as benzodiazepines in shortening
sleep latency and prolonging total sleep time
in patients with insomnia. After
discontinuation of zolpidem, the beneficial
effects on sleep reportedly persist for up to 1
week .
51. • Zolpidem is approved only for the short-term
treatment of insomnia.
• Incidence of adverse effects (e.g., GI
complaints or dizziness) is low.
• Little or no unchanged zolpidem is found in
the urine, elimination of the drug is slower in
patients with chronic renal insufficiency
52. Zaleplon
• Zaleplon preferentially binds to the
benzodiazepine-binding site on GABAA
receptors containing the 1 receptor subunit.
Zaleplon is absorbed rapidly and reaches peak
plasma concentrations in 1 hour.
• Zaleplon (usually administered in 5-, 10-, or
20-mg doses) has been studied in clinical trials
of patients with chronic or transient insomnia
53. Eszopiclone
• Eszopiclone has no structural similarity to
benzodiazepines, zolpidem, or zaleplon.
• Eszopiclone is used for the long-term
treatment of insomnia and for sleep
maintenance. It is prescribed to patients who
have difficulty falling asleep as well as those
who experience difficulty staying asleep
54. • Eszopiclone is believed to exert its sleep-
promoting effects through its enhancement of
GABAA receptor function at the
benzodiazepine binding site.
55. BARBITURATES
• The sleep-inducing properties of barbiturates
were discovered early in the 20th century, and
hundreds of compounds were made and tested.
Until the 1960s, they formed the largest group of
hypnotics and sedatives in clinical use.
Barbiturates all have depressant activity on the
CNS, producing effects similar to those of
inhalation anaesthetics. They cause death from
respiratory and cardiovascular depression if given
in large doses, which is one of the main reasons
that they are now little used as anxiolytic and
hypnotic agents.
57. • Pentobarbital, Uses: Insomnia, pre-op sedation,
emergency management of seizures, t1/2 : 15-50
hrs, dosage form: oral, IM, IV, rectal.
• Phenobarbital, Uses: Seizure disorders, status
epilepticus, daytime sedation, t1/2 : 80-120 hrs,
oral, IM, IV
• Secobarbital , Uses: Insomnia, preoperative
sedation, t1/2 : 15-40 hrs, oral
• Thiopental: Induction/maintenance of
anesthesia, pre-op sedation, emergency
management of seizures, t1/2 : 8-10 hrs, IV
58. • Pentobarbital and similar typical barbiturates
with durations of action of 6-12 hours are still
very occasionally used as sleeping pills and
anxiolytic drugs, but they are less safe than
benzodiazepines. Pentobarbital is often used as
an anaesthetic for laboratory animals.
• Barbiturates share with benzodiazepines the
ability to enhance the action of GABA, but they
bind to a different site on the GABAA
receptor/chloride channel, and their action is less
specific.
59. • As well as being dangerous in overdose,
barbiturates induce a high degree of tolerance
and dependence. They also strongly induce the
synthesis of hepatic cytochrome P450 and
conjugating enzymes, and thus increase the rate
of metabolic degradation of many other drugs,
giving rise to a number of potentially
troublesome drug interactions. Because of
enzyme induction, barbiturates are also
dangerous to patients suffering from the
metabolic disease porphyria.
60. Ramelteon
• It was approved in the U.S. in 2005 for the
treatment of insomnia, specifically sleep onset
difficulties.
• Two GPCRs for melatonin, MT1 and MT2, are
found in the suprachiasmatic nucleus, each
playing a different role in sleep. Binding of
agonists, such as melatonin, to MT1 receptors
promotes the onset of sleep while melatonin
binding to MT2 receptors shifts the timing of the
circadian system .
61. • Ramelteon binds to both MT1 and MT2
receptors with high affinity .
• Ramelteon is efficacious in combating both
transient and chronic insomnia. Subjects given
16 or 64 mg of ramelteon in a clinical trial
showed a significantly shorter latency to sleep
onset, as well as increased total sleep time,
compared to placebo controls
62. • The drug was generally well tolerated by
patients and did not impair next-day cognitive
function. Ramelteon is also useful in the
treatment of chronic insomnia, with no
tolerance occurring in its reduction of sleep
onset latency even after 6 months of drug
administration.