ºÝºÝߣshows by User: SharmeenAsad / http://www.slideshare.net/images/logo.gif ºÝºÝߣshows by User: SharmeenAsad / Sun, 05 Mar 2017 03:41:38 GMT ºÝºÝߣShare feed for ºÝºÝߣshows by User: SharmeenAsad Sedative hypnotics /slideshow/sedative-hypnotics-72818436/72818436 sedative-hypnotics-170305034138
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 ]]>
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 ]]> Sun, 05 Mar 2017 03:41:38 GMT /slideshow/sedative-hypnotics-72818436/72818436 SharmeenAsad@slideshare.net(SharmeenAsad) Sedative hypnotics SharmeenAsad 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 <img style="border:1px solid #C3E6D8;float:right;" alt="" src="https://cdn.slidesharecdn.com/ss_thumbnails/sedative-hypnotics-170305034138-thumbnail.jpg?width=120&amp;height=120&amp;fit=bounds" /><br> 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
Sedative hypnotics from Sharmeen Asad
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