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A-CNS Pharma > Anxiolytics + Sedative/Hypnotics > Flashcards

Anxiolytics + Sedative/Hypnotics Flashcards

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1
Q

بسم الله الرحمن الرحيم وبه نستعين
______________________
Anxioltics sedative hypnotics used in ?
__________________
Define anxiety

A

Anxiety + insomina
________________
unpleaseant state of tension or apprhension in case of GAD (Generalized Anxiety disorder )
Phobia or Panic
Accompanied by?
Physical sytomps of Sympathatic overactivity as
Tachycardia , palpitations , sweating and trembling )

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2
Q

Classifications of anxio sed antihyp drugs according to Mechanism
mention

A

1-Drugs facilitating GABA action
2-5HT1A partial agonists Buspirone
3-Melationin Reamleton

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3
Q

Mention drug faciliating GABA CTION

A

Barbituarsas
benozdizepine
Zolepidem zoleplon
ALCOHOL

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4
Q

Mention Atypical anxiolytic and sedatives

A

=Antidepressants as TCA and nirtazapine
=Antipsychotocis as queitapine and clozapine
=Antihistamnics : Diphenhydramine and doxylamine
BBs as inderal propranolol

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5
Q

Compare between GABA A &GABA B receptros

A

GABA A :-
for sedatives and hypnotics
Benzo barb 2z alco
Working by its IoNotropc effect on Cl- channels casuing hyperplorization and Neuronal inhibiton in CNS
____________________
GABA B: Metabotropic by G protein
casuing pre and post synaptic inhibiton in spinal cord
presunaptic by blocking Ca channels blocking NTs release
Postsynaptic opening K+ Channels casuing K outflux causing Hyperplorization

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6
Q

Baclofen type?

A

Working on GABA B receptors for Muscle relaxant and spasitisy and rigidity

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7
Q

GABA A receptor formed Of

A

2alpha 2 beta 1 gamma subunits with specific sites for
1-Benzodiazpinte to increase frequency of opening of the channel
2-Barbitureate increasing the duration of opening of the channel

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8
Q

Baributares is stonger than BZDS?

A

Yes is is more powerful CNS depressan since :
GABA mimetic effect
Glutamate AMPA receptor Antagonist inhibitory
but has Lower TI beacuse of Medullary inhibtion

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9
Q

Mention pharmacological actions of barbitaures ?

A

Sedation — hypnosis - anastheis - coma and death why ?
due to medullary depression and CVS And respiratory derpession as follow :
Making body insensitive to increased CO2
Inhibiting VMC

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10
Q

Mention members of barbituares and its uses

A

Thiopental ultrashort IV anasthetic
__________________
Pentobarbital
Secobarbital
Short and Intermediate No longer used due to addiction
__________________
Phenobarbital Long acting used as antiepleptic
_______________________

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11
Q

Mention side effects of barbiturates

A

N2D2EA
1- Narrow TI
2-No antidote
3-Tolerance dynamic and kinetic ?
4- Depedence
5-Enzyme induction as increasing CYP 1A2 2C9 2C19 3A4 increasing theri catabolism kinetic
6-Acute prophyria increasing ALA synthetase activity
_______________
Tremors -vertigo - Nasues -dowisness

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12
Q

Prophyria =

A

NVDA
_______+
Prophyria cutanea tarda
_________
Pschyosis
Neurological abnormalities
______________
muscle weakness

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13
Q

How to manage barbiturate toxicity ?

A

Correction of the life threatening conditions as Artifical respiration o2 and co2 and Giving fluid and vasopressores to correct BP
___________________-
Absorption prevention:
Emisis-gastric lavage - activated chracol -cathartics
_____________________
Removal Facilitation :
Urine Alkalinzation
Forced Diuersis
Peritoneal dialysis - hemodialysis - hemoperfusion
_______________________

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14
Q

Mention withdrawal effects of barbiturates and Mangemetn

A

Excitement - Insmonia - dilireum - hallucination and toxic psychosis
give:? antipsychotics : halopridol for higly agitated patients or Olanzopine
___________________
Convulsions gives : ?
Antiepileptics: Valoprate and Carbamazebine for decreasing Impulsivty
________________________
Corner stone :
PhenoBarbitone as Longer acting with smoother withdrawal over 3-4 weeks
_____________________

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15
Q

BZ receptors classified to BZ1 AND 2 ACCOEDING TO ?

A

Alpha subunit :
Alpha 1 = sedative hypnotics and Z hypnotic
Alpha 2= Anxiolytic + Muscle relaxant
_____________________
Benzodiaepine increases the Frequency of Cl - channel openings

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16
Q

GR/ Benzodiazpines has advantages over barbiutrates

A

1-Wide safety margin
2-Antidote (flumazenil)
3-Less tolerance and dependence
4-No enzyme induction
5-No prophyria
6-Less CVS and Resp dep

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17
Q

Classify BZs according to duration of action

A

Shote TM ;
Triazolam
Midazolam
_______________
Intermdiatea ALO
AlprazolaM
Lorazepam
_______________
Long DiC
Diazepam
Clonazepam

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18
Q

BZs is ……philic and absorbed …….. and distribute to …..and …..

A

Lipophilic
Orally
Body+ CNS

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19
Q

IMI of BZs describe

A

SLower erratic than oral absorption except ? Lorazepam

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20
Q

IMI of BZs SLower erratic than oral absorption except ?

A

Lorazepam

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21
Q

BZs and theri metabolites are excreted in ?

A

Urine

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22
Q

What are the casues of the long duration of BZs?

A

ASF
Active metabolites having t1/2 more than parents
________________
Slow Receptor Disscoication rates
___________________
Resditribution to Fatty tissue

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23
Q

Give example of BZs has metabilites with longer T1/2

A

Flurazepam &Diazepam

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24
Q

Lorazepam
oxazepam
Temaepam

A

are conjgate directly
_________________
less cumultice and resiudla effects
not affected by enzyme inducers and inhibitors as other BZs

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25
Mention uses of benzodiazepines
Anxiolytics sedative hypnotics Anasthesia Anticonvulsant Skeletal muscle relaxant Alcohol withdrawal
26
Describe use of benzodizepines as anxiolytics
Potentiate GABA in limbic system __________________:- Anxiety disorders Intermediate + Long acting Alprazolam + Lorazepam + Clonzepam + Diazepam _____________________ Panic disorders : Alprazolam +Clonzaepam
27
Describe use of BZs in Sedation and hypnosis
Sedation in low but hypnosis in high dose ________________________ Treating insomnia by : Promotion of sleep Inceasing Stage 2NREM _____________________ Treating Night mares by decreasing REM but casuign loss of consolidation and anterograde amnesia _____________________ Treating night terroes by dcreasing deep sleep as stage 3.4 but casuing impaired quality sleep _______________________
28
Mention the effects of BZs in sleep patterns ?
Decreasing sleep latency + Increasing Stage 2 NREM CAUSING? less insomina _________________ decrasing stage 3,4 NREM of deep sleep treating Night terrors but causing imparired qulaity sleep __________________ Decreasing REM Sleep casuing ? trasting night mares but? Less consolidation so anterograde amenesia {__________________ not used more than 4-6 weeks for no depedncece
29
Describe use of BZs as Anasthertic drug ?
Due to its amenisa and sedation effect and Potentiation of Narcotics as Opioids ______________________ Consoucs sedation : Midazolam + Fentanyl Pra anasthetic Balanced Anasthesia as midazolam
30
Descrtibve BZs as anticonvulsant ?
=Epilipsy not 1st line as clonazepam _________________________ Status epiliptxus First line as LMD lorazepam Midazolam and Diazepam
31
Describe BZs as sKELETEAL MUSCLE RELAXANT
work on spinal and supraspinal levels to be inhibited _____________________ Diazepam ! Used in Muscle spasticity due to ? ctmi 1-Inflammation 2-Trauma 3-Cerebral palsy 4-MS
32
uSed for smoother withdrawal of Alcohol ?
Diazepam BZs long acting smoothing Withdrawal replacing alochol from receptor
33
Mention BZs adverse effects
1-Drowisness confusion and less cognition with Hangover in Intermediate and long acting ________________________ 2-Amenisa anterograde 3-ataxia 4-addiction 5-additive CNS depression 6-abnormal response as paradoxical excitements due to genetic receptor alteration 7-withdrawal of hypnotics casuing > Rebound insmonia + Increased REM night mares
34
Mention BZs adverse effects
1-Drowisness confusion and less cognition with Hangover in Intermediate and long acting ________________________ 2-Amenisa anterograde 3-ataxia 4-addiction 5-additive CNS depression 6-abnormal response as paradoxical excitements due to genetic receptor alteration 7-withdrawal of hypnotics casuing > Rebound insmonia + Increased REM night mares WAD X5 وادي
35
Rebound insomina increases with withdrawal of?
Short and intermdeiate BZs
36
Why shold we decrease the dose of BZs in elderly ?
Due to reduced liver metabolism we need prevent accumulation of metabolites _-___________________ Ataxia + confusion
37
BZs toxicity and mangements DESCRIBE
CNS depression casuing prolonged sleep CVS and resp depression esp IV rapidly Or with other CNS depressants ______________________ Mangements:- Support respiations and Circulation as barbituates Antidote fLUMAZENIL
38
Describe flumazenil
Compettivive antagonist of Benzos & Z hypnotics ans zolpeidm _________________________ Short t1/2 re adminstered after 1 hours ____________________ indications : BZs and Z hypnotic toxicity Termination of action of Anasthetic BZs ______________________ Adverse effects: Agitation Withdrawal syndrome of convulsions in BZs dependent
39
Benzodizepine withdrawal and magnements SHOW
Exictatio insmonia delerium hallucination psychosis anti psychotics Antidepressants Convulsion aniteplipetics __________________ Replacing short acting with Long acting Diazepam for clonzepam and alprazolam
40
Z Hypnotics as ? anatgonized by? Selective,,,,,,,,, working on ........ so not used in ,,,,,,,,,,
Zolpeidm + Zaleplon zopiclone Eszopiclone _____________ Flumazenil ________________ Sedative - alpha1 gaba A receptors ____ Anxiety induced Insomnia
41
Mention advantages of Zhypnotics over BZs
Rapid onset short duration so less hangover ________________ Less SCTH less supression of REM SLEEP so less ameisa Less congitive inmpairment less tolerance +depednence + wthdrawal + rebound insomnia but possibly occuring as nightcalm less hangover
42
Zolpedim describe
short acting hypnotic has SR Or Extending relaeas 5 hours
43
Z hypnotics cc by rapid elimnination ?>
Zaleplon has fewer resiudal effects on cognitive and psychomoto functions
44
Eszopiclone
Night calm ______________ Anxiety dry moth Somonelence Headache Peripheral edema Unpleasent taste __________________ Has risk of abuse and addiction
45
Selective hypnotic IS MT1 and MT2 receptors agonist in suprachiastmatic Nucleus and casuign decreas in testosterone and Increase in Prolactin ?
Ramelton
46
A selectiv hypnotic decreasing lactency of sleep and with minimal abuse or withdrawal or rebound insomnia ? mentio side effects
Ramelton ______________ Dizzness smonlence Fatigue
47
Drug interactions of Ramelton mention
Never be taken with CYP inhibitor CYP1A2 Ciproflxacin + fluvoxamine CYP2C9 Fluconazole ________________________ due to its effect on increasing Prolactin decreasing Testosterone
48
Selective Anxiolytic used in CHRONIC ANXIETY? METNION MEACHNISM OF ACTION
Buspirone _____________ 5HT1A Agonist Full presynpatic partial postsynaptic _________________ working onD2 AND 5HT2A
49
USED IN GENRALIZED ANXIETY DIORDERS ONLY?
Buspirone
50
Buspirone differs fomr BZD in ?
Selective anxiolytic GAD NO AAAAA AMENISA ATAXIA ABUSE ADDITIVE CNS Derpession
51
Mention disadvantages of Buspirone
Delayed onset 1-2 weeks _________________ Does not treat insomnia or panic attacks _________________ Nause headche dizzness NVA
52
sEDATIV HYPNOTICS esp BZs used for?
4-6 WEEK FOR NO DEPNCENE
53
Termination of therapy should be?
Gradual to avoid withdrawal syndrome
54
Preferred for insomnia
Rapid Onset short duration drugs to avoid hang over Midazolam
55
Insminic with ealy morning awakenings ? needing anxiolytic
Longer acting BZD Diazepam casuing hang over!!!!
56
Chronic insomnia due to anxiety and deprtsiion
gIVE Antidepressants as Mirtazapine also hypnotic increasing stage 34
57
GAD !
anti depressants SSRI escitalopram +BZDs+ Inderal ______________ Benzo = rapid onset then gradual withdrawal ater month for month SSRI = delayed onset for 6 months
58
Panic disorder
alprazolam with antepressant effect buspirone not useful as it is anxioltiyc
59
Liver dysfunction which BZDs could be give?
Lorazepam Temazepam oxzaepam
60
Most BDZ are metabolized in liver so ?
Dose adjustment in liver cirrhosis is obligatory
61
"قال سنشد عضدك بأخيك ونجعل لكما سلطانا فلا يصلون إليكما بآياتنا انتما ومن أتبعكما الغالبون فلما جاءهم موسي بآيتنا بينات قالوا ماهذا إلا سحرٌ مفتري وماسمعنا بهذا في آبائنا الأولين وقال موسي ربي أعلم بمن جاء بالهدي من عنده ومن تكون له عاقبة الدار إنه لا يفلح الظالمون "

A-CNS Pharma (11 decks)

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