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Pharmacology > Anxiolytics and sedatives > Flashcards

Anxiolytics and sedatives Flashcards

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1
Q

What is anxiety?

A

its a disorder characterised by a feeling of apprehension, uncertainty and fear without any apparent stimuli

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2
Q

Symptoms of Anxiety

A

Tachycardia
Tremors
Sweating/Perspiration
Palpitations
Hyperventilation
NV
diarrhea
Insomnia
Hysteria
Phobic conditions

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3
Q

Goals for anxiety treatment

A

-fear extinction
-Blocking reconsolidation of fear memories

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4
Q

Drugs used to treat Anxiety

A

Benzodiazepines BDZ
Barbiturates
SSRIs

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5
Q

MOA of BDZ

A

They bind to a specific regulatory R site on GABAa R= enhance inhibitory effect of GABA
- Allosteric enhancement of Cl: increase frequency of channel opening
= Incr. HYperpolaristaion

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6
Q

What are the Anxiolytic effects of BDZs

A

Anxiolytic: reduction of anxiety without reducing conc. of motor activity

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7
Q

Sedation effects of BDZs

A

Sedation: reduction of anxiety with reduction of conc. and motor act.: drowsiness

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8
Q

Hypnotic effects of BDZ

A

Hypnosis: induction of sleep/loss of consciousness (person has to be awoken by external stimuli)

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9
Q

Anaesthesia effects of BDZ

A

Anesthesia/coma: loss of consciousness (person not awoken by external stimuli)

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10
Q

How can BDZs cause Death as an effect?

A

toxicity
depression of respiratory and CVS centers in CNS
reduction of muscle tone and coordination
anticonvulsant effects

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11
Q

How are BDZs classified

A

They are: 1) Sedative Hypnotics
2) Anxiolytics (Tranquilisers)

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12
Q

DOA of Sedative Hypnotics

A

Are usually short acting:
short and ultra-short

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13
Q

Which are the Sedative Hypnotics

A

MOTT
Midazolam
Oxazepam
Triazolam
Temazepam

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14
Q

DOA of Sedative Drugs

A

Midazolam: Ulta-short DOA
Oxazepam: Short DOA

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15
Q

DOA of Anxiolytics (tranquilisers)

A

Are usually long and intermediate acting.

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16
Q

Which are the Tranquiliser drugs

A

Lorazepam
Diazepam
Chlordiazepoxide
Flunitrazepam

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17
Q

DOA of the Tranquiliser drugs

A

Lorazpam: intermediate acting
Diazepam: long acting

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18
Q

TI of BDZ for anxiety

A

Indicated for severe anxiety, short term
They are agonist at the site, favourable TI

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19
Q

BDZs used for Anxiety

A

1)Diazepam
2) Chlordiazepoxide

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20
Q

TI of BDZ for Insomnia

A

short-term use,
safe,
Impossible to commit suicide with large amounts

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21
Q

BDZ used for Insomnia

Study These Flashcards
A

1) Temazepam
2) Flurazepam

22
Q

BDZ used pre-operative sedation/pre-anesthetic medication

Study These Flashcards
A

Lorazepam
Diazepam

23
Q

BDZ used for Induction Anaesthesia

Study These Flashcards
A

Midazolam: has sedative hypnotic effects

24
Q

BDZ that aids in Endoscopy

25
BDZ used in Status Epilepticus and other convulsions
IV diazepam Clobazam Clonazepam (too sedative for maintenance therapy) For emergency situations ONLY
26
BDZ used in skeletal muscle disorder
Diazepam (in chronic muscle spasms, spasticity in people with cerebral palsy, tetanus)
27
BDZ used in Delirium Tremens
Its alcohol withdrawal syndrome 1) Diazepam 2) Chlordiazepoxide
28
Unwanted effects of BDZs during Therapeutic Used
Drowsiness Over-sedation esp. in elderly patients Confusion Amnesia Impaired motor co-ordination
29
Acute Overdosage of BDZ effects
Prolonged sleep (patient is rousable; no serious CVS and Respiratory depression)
30
BDZ overdose+ alcohol cause
Severe Respiratory depression
31
Antidote for BDZ overdose+alcohol
Flumazenil
32
MOA of Flumazenil in Overdose
Competitively binds to BDZ R= antagonises its activity
33
CIs of Flumazenil
Dependence Mixed dose with CVS/Respiratory drugs CNS toxic drugs (TCAs) Lithium
34
BDZ Withdrawal symptoms
Mild anxiety Insomnia Nausea Tremors Rarely: Psychosis Convulsions
35
Effects of SSRIs
Have slow onset of Action Minimal effects in acute anxiety states (may increase anxiety for several weeks before beneficial effects are seen)
36
MOA of SSRIs
Prevent the Presynaptic reuptake of 5HT =more 5HT to stimulate postsynaptic 5HT Receptors (5HT1: antidepressant and anxiolytic effects)
37
SSRI drugs
FESP Fluoxetine Escitalopram Sertraline Paroxetine
38
SE of SSRIs
Nausea Diarhoea Restlessness Insomnia Sexual Dysfunction Anorexia (fluoxetine in first few months)
39
DIs of SSRIs
MAOIs; Fluoxetine can inhibit CYP450=Metabolism of B-Blockers including Propranolol and Metoprolol+ hypotension, bradycardia
40
MOA of Non-BDZ drugs
selectively bind to BDZ1 receptors (known as the Z drugs)
41
Which are the Non-BDZ drugs
Zopiclone Zolpidem Zalepron
42
Effects of Non-BDZ drugs
They have shorter T1/2 than BDZs Have reduced propensity to cause tolerance and have less abuse liability
43
Effect of Zalepron
it has such a short half life that it can be used to treat middle-of-night insomnia as long as 5hrs elapses before driving or operating machinery
44
SE of Zolpiden
nightmares visual hallucination with alcohol *Zopiclone and Zalepron have less SEs
45
Which Antihistamines are used as hypnotics
Diphenhydramine Hydroxyzine
46
Which other hypnotics are used?
Busiprone Ramelteon
47
MOA of Busiprone
Acts as a partial 5HT1 Receptor agonist but also acts with D2 REceptor * not associated with rebound activity
48
How long before effects of Busiprone are seen
1-2 weeks
49
MOA of Ramelteon
Is a Melatonin agonist: M1 and M2 receptors *doesnt have same abuse potential as BDZ
50
TU of Ramelteon
Generalized anxiety state and sleep disorder

Pharmacology (50 decks)

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