Sedative - Hypnotics

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models of anexity

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NA,GABA(A) res and serotonin res

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chronic NAregic over activity down regulates alpha 2 res in

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general anxity disor and PTSD and explain NA model

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under activity of ..........res

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GABAa

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5HT1a is primarly

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inhibtitory and play a role in anexity

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treatment of anxiety

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SH mainly but also antidepresants beta antagonist propranolol

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dreaming usually ocure at

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REM

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important for physical rest restoration

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NREM 3&4

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essential for mental restortion

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REM

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pardoxical sleep

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inhanced brain activity in REM

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insomnia

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cxed by sleep problem

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insomnia occurs when there is

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dec 5HT

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REM is turned on by

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cholinergics

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dopamine have

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alerting effect

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wakefulness include .... and ..... in the cortex

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NE and ACh

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wakefulness include .... and ..... in the hypothalamus

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histamine and neuropeptide ( substance p)

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drug treatment of insomnia

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SH, melatonin receptor agonist 'ramelteon',antihistamin.antidepresant

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effective Sedative

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reduce anexiety with out marked motor or mental function

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effective hypnotics

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facilitate the onset and mentainace of state of sleep

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classification of SH

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bz, barbi, newer agents,older SH, melatonin reseptor agonist, beta antagonist and anthihistamine

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newer againts

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buspirone, zolpidem, zalaplon, eszopiclone

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older SH

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alcohol, choral hydrates

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anti histamine

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dyphendramine ,doxylamine

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beta adrenergic antagonist

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relief performance anexiety but not the emotinal

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antihistamin use

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wakefull children, and mild insomnia

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the tope protine bound bz

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diazipam 99% and alprazolam 70 %

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short acting bz

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TOM
(mida,tria,oxa )zepam

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intermide Bz

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LATE
(esta and alpra )zolam,(tema,lora,)

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long BZ

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FC3DQ

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diazepam is metabolised to

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nordizepam t1/2 30 to 200 hrs

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alprazolam udergoes

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hydroxylation and glucurdation

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lorazpam under goes

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direc glucoridenation

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alprazolam used

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panic attack

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GAD

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diazepam,lora ,alpra

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prolonged tretme of anexity

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diazepam

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all bz produc

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inc NREM 2 and total sleep and dec NREM 4
no suppresion of REM

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long tret of siezure

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clonazepam

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status eplipticus

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lora mida and diaz`

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induction of anset

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lora diaz and mida(is preferd as it is short acting)

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........ of seizure threshold by bz

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increase

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spasmolytic "relief of spasm"

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bz especially diaze

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encase of bz overdose we use

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flumazenil

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flumazenil is also effective against

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eszopi,zalepion and zolpid

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flumanzile should be avoided in pts taking

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TCA and Bz b/c it unmask the epliptogenic effect of TCA

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bz adve E

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anterograded memory loose and impaired mental and psychomotor function and cleft in kids

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cimitidine and bz interaction

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cim inhbite bz degradation

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barbi and carbamazipine with bz

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increse bz metabolism

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long acting barbi

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phenobarbitol

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short actin barbi

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amo pento and seco barbitole

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ultra short acting barbi

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thiopental and methohexital

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MAC of barbi

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GABAa and inhibite AMPA by dissolving to the membrane like general anstiastia

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barbi effect on REM

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it decrease it and rebound nightmares

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barbi across the placent

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they readly cross the placenta

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induce microsomal enzyme

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p450 which precipitate porphoria

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drug of choice for young childern with recurenc fibrile seziure

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phenobarbitol

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induction of ansethasia

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thiopental

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grand mal eplipsy, status eplipticus and eclampsia

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also treated by phenobarbitol

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barbi contra indelicate with

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acute intermitent porphoria and pregnancy

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barbi induce metab of

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oral contraceptive and anticoagulant

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buspirone

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partial 5HT 1a agonist and have no withdrawal and rebound effect

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buspirone is not usefull for

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acutr panic attack b/c it require weaks for effect and social anexiety or phobias

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buspirone is usefull for

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GAD

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"z compounds" produce sedation with out

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anxiolytic, anticonvulsant or muscle relaxant effect and effect on REM

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"z compounds" are devoid of abuse potetial except

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escopiclone

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ramelteon

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potent MT1 and MT2 agonist whic are involved in sleep

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hypnotics usually in the elderly

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chloral hydrate