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

Anxiolytics + Sedative/Hypnotics Flashcards

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
Q

Mention uses of benzodiazepines

A

Anxiolytics
sedative hypnotics
Anasthesia
Anticonvulsant
Skeletal muscle relaxant
Alcohol withdrawal

26
Q

Describe use of benzodizepines as anxiolytics

A

Potentiate GABA in limbic system
__________________:-
Anxiety disorders
Intermediate + Long acting
Alprazolam + Lorazepam + Clonzepam + Diazepam
_____________________
Panic disorders :
Alprazolam +Clonzaepam

27
Q

Describe use of BZs in Sedation and hypnosis

A

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
Q

Mention the effects of BZs in sleep patterns ?

A

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
Q

Describe use of BZs as Anasthertic drug ?

A

Due to its amenisa and sedation effect
and Potentiation of Narcotics as Opioids
______________________
Consoucs sedation : Midazolam + Fentanyl
Pra anasthetic
Balanced Anasthesia as midazolam

30
Q

Descrtibve BZs as anticonvulsant ?

A

=Epilipsy not 1st line as clonazepam
_________________________
Status epiliptxus First line as LMD
lorazepam Midazolam and Diazepam

31
Q

Describe BZs as sKELETEAL MUSCLE RELAXANT

A

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
Q

uSed for smoother withdrawal of Alcohol ?

A

Diazepam BZs long acting smoothing Withdrawal replacing alochol from receptor

33
Q

Mention BZs adverse effects

A

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
Q

Mention BZs adverse effects

A

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
Q

Rebound insomina increases with withdrawal of?

A

Short and intermdeiate BZs

36
Q

Why shold we decrease the dose of BZs in elderly ?

A

Due to reduced liver metabolism we need prevent accumulation of metabolites
_-___________________
Ataxia + confusion

37
Q

BZs toxicity and mangements DESCRIBE

A

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
Q

Describe flumazenil

A

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
Q

Benzodizepine withdrawal and magnements SHOW

A

Exictatio insmonia delerium hallucination psychosis
anti psychotics
Antidepressants
Convulsion
aniteplipetics
__________________
Replacing short acting with Long acting
Diazepam for clonzepam and alprazolam

40
Q

Z Hypnotics as ?
anatgonized by?
Selective,,,,,,,,, working on ……..
so not used in ,,,,,,,,,,

A

Zolpeidm + Zaleplon zopiclone Eszopiclone
_____________
Flumazenil
________________
Sedative - alpha1 gaba A receptors
____
Anxiety induced Insomnia

41
Q

Mention advantages of Zhypnotics over BZs

A

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
Q

Zolpedim describe

A

short acting hypnotic
has SR Or Extending relaeas 5 hours

43
Q

Z hypnotics cc by rapid elimnination ?>

A

Zaleplon
has fewer resiudal effects on cognitive and psychomoto functions

44
Q

Eszopiclone

A

Night calm
______________
Anxiety
dry moth
Somonelence
Headache
Peripheral edema
Unpleasent taste
__________________
Has risk of abuse and addiction

45
Q

Selective hypnotic IS MT1 and MT2 receptors agonist in suprachiastmatic Nucleus
and casuign decreas in testosterone and Increase in Prolactin ?

A

Ramelton

46
Q

A selectiv hypnotic decreasing lactency of sleep and with minimal abuse or withdrawal or rebound insomnia
? mentio side effects

A

Ramelton
______________
Dizzness
smonlence
Fatigue

47
Q

Drug interactions of Ramelton mention

A

Never be taken with CYP inhibitor
CYP1A2 Ciproflxacin + fluvoxamine
CYP2C9 Fluconazole
________________________
due to its effect on increasing Prolactin decreasing Testosterone

48
Q

Selective Anxiolytic used in CHRONIC ANXIETY? METNION MEACHNISM OF ACTION

A

Buspirone
_____________
5HT1A Agonist
Full presynpatic
partial postsynaptic
_________________
working onD2 AND 5HT2A

49
Q

USED IN GENRALIZED ANXIETY DIORDERS ONLY?

A

Buspirone

50
Q

Buspirone differs fomr BZD in ?

A

Selective anxiolytic GAD
NO AAAAA
AMENISA
ATAXIA
ABUSE
ADDITIVE CNS Derpession

51
Q

Mention disadvantages of Buspirone

A

Delayed onset 1-2 weeks
_________________
Does not treat insomnia or panic attacks
_________________
Nause headche dizzness
NVA

52
Q

sEDATIV HYPNOTICS esp BZs used for?

A

4-6 WEEK FOR NO DEPNCENE

53
Q

Termination of therapy should be?

A

Gradual to avoid withdrawal syndrome

54
Q

Preferred for insomnia

A

Rapid Onset short duration drugs to avoid hang over
Midazolam

55
Q

Insminic with ealy morning awakenings ?
needing anxiolytic

A

Longer acting BZD
Diazepam casuing hang over!!!!

56
Q

Chronic insomnia due to anxiety and deprtsiion

A

gIVE Antidepressants as Mirtazapine
also hypnotic
increasing stage 34

57
Q

GAD !

A

anti depressants
SSRI escitalopram +BZDs+ Inderal
______________
Benzo = rapid onset then gradual withdrawal ater month for month
SSRI = delayed onset for 6 months

58
Q

Panic disorder

A

alprazolam with antepressant effect
buspirone not useful as it is anxioltiyc

59
Q

Liver dysfunction which BZDs could be give?

A

Lorazepam
Temazepam
oxzaepam

60
Q

Most BDZ are metabolized in liver so ?

A

Dose adjustment in liver cirrhosis is obligatory

61
Q

“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

A-CNS Pharma (11 decks)

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