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Pharmacology > Anxiolytics and sedatives > Flashcards

Anxiolytics and sedatives Flashcards

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

A

1) Temazepam
2) Flurazepam

22
Q

BDZ used pre-operative sedation/pre-anesthetic medication

A

Lorazepam
Diazepam

23
Q

BDZ used for Induction Anaesthesia

A

Midazolam: has sedative hypnotic effects

24
Q

BDZ that aids in Endoscopy

A

Diazepam

25
Q

BDZ used in Status Epilepticus and other convulsions

A

IV diazepam
Clobazam
Clonazepam
(too sedative for maintenance therapy)
For emergency situations ONLY

26
Q

BDZ used in skeletal muscle disorder

A

Diazepam
(in chronic muscle spasms, spasticity in people with cerebral palsy, tetanus)

27
Q

BDZ used in Delirium Tremens

A

Its alcohol withdrawal syndrome
1) Diazepam
2) Chlordiazepoxide

28
Q

Unwanted effects of BDZs during Therapeutic Used

A

Drowsiness
Over-sedation esp. in elderly patients
Confusion
Amnesia
Impaired motor co-ordination

29
Q

Acute Overdosage of BDZ effects

A

Prolonged sleep (patient is rousable; no serious CVS and Respiratory depression)

30
Q

BDZ overdose+ alcohol cause

A

Severe Respiratory depression

31
Q

Antidote for BDZ overdose+alcohol

A

Flumazenil

32
Q

MOA of Flumazenil in Overdose

A

Competitively binds to BDZ R= antagonises its activity

33
Q

CIs of Flumazenil

A

Dependence
Mixed dose with CVS/Respiratory drugs
CNS toxic drugs (TCAs)
Lithium

34
Q

BDZ Withdrawal symptoms

A

Mild anxiety
Insomnia
Nausea
Tremors
Rarely: Psychosis
Convulsions

35
Q

Effects of SSRIs

A

Have slow onset of Action
Minimal effects in acute anxiety states (may increase anxiety for several weeks before beneficial effects are seen)

36
Q

MOA of SSRIs

A

Prevent the Presynaptic reuptake of 5HT
=more 5HT to stimulate postsynaptic 5HT Receptors (5HT1: antidepressant and anxiolytic effects)

37
Q

SSRI drugs

A

FESP
Fluoxetine
Escitalopram
Sertraline
Paroxetine

38
Q

SE of SSRIs

A

Nausea
Diarhoea
Restlessness
Insomnia
Sexual Dysfunction
Anorexia (fluoxetine in first few months)

39
Q

DIs of SSRIs

A

MAOIs; Fluoxetine can inhibit CYP450=Metabolism of B-Blockers including Propranolol and Metoprolol+ hypotension, bradycardia

40
Q

MOA of Non-BDZ drugs

A

selectively bind to BDZ1 receptors (known as the Z drugs)

41
Q

Which are the Non-BDZ drugs

A

Zopiclone
Zolpidem
Zalepron

42
Q

Effects of Non-BDZ drugs

A

They have shorter T1/2 than BDZs
Have reduced propensity to cause tolerance and have less abuse liability

43
Q

Effect of Zalepron

A

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
Q

SE of Zolpiden

A

nightmares
visual hallucination with alcohol
*Zopiclone and Zalepron have less SEs

45
Q

Which Antihistamines are used as hypnotics

A

Diphenhydramine
Hydroxyzine

46
Q

Which other hypnotics are used?

A

Busiprone
Ramelteon

47
Q

MOA of Busiprone

A

Acts as a partial 5HT1 Receptor agonist but also acts with D2 REceptor
* not associated with rebound activity

48
Q

How long before effects of Busiprone are seen

A

1-2 weeks

49
Q

MOA of Ramelteon

A

Is a Melatonin agonist: M1 and M2 receptors
*doesnt have same abuse potential as BDZ

50
Q

TU of Ramelteon

A

Generalized anxiety state and sleep disorder

Pharmacology (50 decks)

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