obat sedatif,2011 [compatibility mode]

8/16/2019 Obat SEDATIF,2011 [Compatibility Mode]

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Fathiyah SafthriLaboratorium Farmakologi FK-UMM

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OBAT HIPNOTIK-

SEDATIF

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Insomnia

Causes - noise, worries, stress, drugs, pain,uncomfortable temperature, disease, etc.

Types

& onset insomnia - trouble falling asleep

& maintenance insomnia - awaken frequently during thenight

& termination insomnia - wake up too early and cannotget back to sleep

Abnormalities of sleep


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Hypnotic Agents That Act by Enhancing

ABA Hypnotic Agents That Act by B!oc"ing#a"e-Promoting Ne$rotransmitterSystems

Hipnotic agents


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Benzodiazepin BARBITURAT




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A %r$cia! Di&erence

barbiturate

benzodiazepine




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Ben'o(ia'epin




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Mechanism:

Increase the frequency of opening

of the GABAreceptor, thereby

increasing the effect of GABA-

mediated hyperpolarization. Also

increase GABAbinding.




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Therapeutic!

'Anxiolytic diazepam,

alprazolam!

'"ypnotic triazolam!

'Muscle relaxant

diazepam, lorazepam!

'Anticon#ulsant

diazepam, lorazepam,

clonazepam!

'$edation midazolam!

Adverse:

'%ogniti#e impairment, decreased motor

s&ills, daytime sedation

'Additi#e %'$ depression ethanol,

antihistamines, opioids!

'(ependence

'Beha#ioral disinhibition paradoxical!

'Anterograde amnesia

'Abrupt )ithdra)al panic attac&,

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Benodiaepine e!ects



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Anxiolytic and Hypnotic Drugs

(# )e$asi! ↓ arousal* ↓ behaviour* ↓alertness* ↓ response

to stimuli

+# ,ypnotic!

- )emua se$ative"hypnotics pa$a $osis besar

menyebabkan ti$ur#

- ormal sleep ter$iri $ari beberapa stage ber$asarkan

. ukuran !electroencephalogram* electromyogram*

electronystagmogram#

- /$a + phases yang ter0a$i secara siklik tiap 12 min!(% on-rapi$ eye movement 34M%# 52-567 $ari total

sleep#

/$a 8 stages# ,ampir semua ti$ur stage +#

+% 3api$ eye movement 34M%# Fase mimpi $reams%#


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a! Menurunkan latency of sleep (waktu yang diperlukan untuk

mulai tidur).

b) Meningkatkan lama tidur stage 2 NREM

c) Memperpendek fase REM sleep

d) Memperpendek fase slow wave sleep (fase ter!adinya somnambulismdan nig"tmares occur)

Efek tolerance ter!adi setela" #2 minggu ($AR$%&'RA&)

($enodiaepin*+ M%N,,' $enodiaepin)

-eng"entianmendadak meningkatkan fase REM sleep(reboundeffects)

REM sleep ( (/& dan NE activity di RA0

,ypnotic




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"erubahan fase tidur setelahpemberian obat hipnotic


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3. Anesthesia:

Dosis besar enghilang!an !esadaran" anesia

#anterogade anesia$" dan hilangnya re%lex

Beberapa BARBs #Thiopental$ dan B&Ds #'idazola$

enyebab!an anestesia

(. Antieplepsi:

)%e! antiepilepsi sebai!nya diba**ah e%e! sedasi

+henobarbital"Diazepa",orazepa dipa!ai pada

status epilepticus

-.Rela!sasi otot bergaris #'uscle Relaxant$:

eua sedati/e0Hypnotic dosis besar rela!sasi

otot bergarisDiazepa dosis sedasi uscle relaxant

1.'edullary Depressant:

Dosis besar ene!an neuron di edulla repiratory

arrest" hypotensi"cardio/ascular collaps%atal


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2. Tolerance dan Drug Dependence:

'enyebab!an teradinya :tolerance" psychological dependence" physical

dependence +enghentian endada! enyebab!an

abstinencia syndroe #anxiety" hyperre%lexia" seizure$

ering pada golongan short0acting #+entobarbital"ecobarbital$Buspirone tida! enyebab!an !etergantungan obat




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Mec"anism:

-rolongs t"e open time of t"e

,A$Areceptor (a c"loride

c"annel) t"ereby increasing t"e

effect of ,A$Amediated

"yperpolariation.




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Therapeutic!

'Anticon#ulsant phenobarbital!

'Anesthesia thiopental!'$edati#e-hypnotic pentobarbital!

Adverse (narrow margin of safety):

'*espiratory depression

'Abuse potential and dependence

'-/ enzyme induction drug interactions

'Interferes )ith *0M sleep


Barbiturat e!ects



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Antidepressan#antiH$,

Antagonis%HT&' (olpidem Chloralhydrate Hydro)yine

*eprobamate#miripBA+B'

bat-obat lain


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Zolpidem

!.1

1

1

1

1

1

Merupa&an turunan Imidazopyridine bu&an B2(s!engobatan untu& insomnia profil mirip 3riazolam

0fe& : muscle relaxant dan anticon#ulsant sangat lemah, hang o#er

-!, addi&si -!, rebound insomnia -!

Metabolisme di li#erinacti#e metabolites t 4 :5- 6!6!..

7nset cepat, )a&tu paruh pende&

(osis harus di&urangi pada penderita dgn hepatic dysfunction,,usia

lan6ut, dan penderita yang mengguna&an cimetidine.

8ombinasi dengan 3%A,Antipsychotic,Antihistaminedepresi $$

mening&at

Me&anisme &er6a :1 Agonist sele&tif thd B2+ receptors.

1 Menyebab&an 9acilitates GABA--mediated neuronal inhibition.

1

0fe& diantagonist oleh 9lumazenil


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An)iolitics



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,olongan an1iolytic yang relatif baru

Mengurangi symptom an1iety (2* minggu)

Mekanisme ker!a:partial agonist pada presynaptic /Areceptor

(dorsal rap"e nuclei cerebral corte1 amygdala)

Metabolitenya:#-- mempunyai blokade 2 AR.

erivat baru : ,epirone %psapirone&andospirone

Buspirone #buspar'


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1

1

1

1

1

1

1

1

Mengurangian1iety

%ndikasi : kecemasan yang disertai depresi

Efek : sedasi () gangguan motor () antiepilepsi () dan

muscle rela1ant () addiksi () toleransi () reboundan1iety ()3wit"drawl()

Mula ker!a # 4 * minggu

5ombinasi dengan MA6 tekanan dara" naik

&idak mengadakan potentiasi t"d 7N0 depressants.Margin of safety sangat lebar

E0 : ringan mual munta" sakit kepala pening gelisa"bingung

Buspirone


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1

1

emberian p.o absorpsi cepat

Mengalami metabolisme di hepar hydroxylation dan

deal&ylation! beberapa acti#e metabolites e.g. +-;-pyrimidyl-piperazine, +-!

1 (apat ditolerir pada usia lan6ut, ttp mempunyai &liren

lambat

armakokinetik buspirone


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obat sedatif,2011 [compatibility mode]

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