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CNS > Pharma 5: Anxiolytic And Hypnotic Drugs > Flashcards

Pharma 5: Anxiolytic And Hypnotic Drugs Flashcards

1
Q

Benzodiazepines

Administered

A

Orally

IV for status epilepticus (diazepam) and anesthesia (midazolam)

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2
Q

Use of benzodiazepines is declining in favor of

A

Antidepressants and behavioral therapy

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3
Q

Benzodiazepines replaced

A

Barbiturates since theyre safer and more effective

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4
Q

Benzodiazepines MOA

A

Bind selectively to GABA-A modulatory site—>increased the affinity of GABA for receptor—> facilitate opening of GABA activated Cl channels—> enhance response to GABA—> better cns inhibition through GABA

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5
Q

Pharmacological effects of Benzodiazepines

A

Reduce anxiety and aggression

Sedate + induces sleep

Reduce muscle tone and coordination

Anticonvulsant

Anterograde amnesia

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6
Q

The only BZD with antidepressant effects

A

Alprazolam

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7
Q

BZDs and irritability/aggression

A

Due to the withdrawal syndrome associated with BZDs—> more pronounced with short acting BZDs like:

Triazolam (withdrawn from UK)

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8
Q

Diazepam duration of action in reduction of anxiety, agression

A

Long acting and used for prolonged periods

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9
Q

Alprazolam used for

A

Panic disorders whether short or long term

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10
Q

What happens during slow wave sleep

A

Metabolic rate and adrenal steroids are at their lowest and GH at its highest

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11
Q

The effect of hypnotics on REM sleep proportion

A

REDUCE!

BZDs less so (slight decrease in slow wave)+ do not affect growth hormone secretion

Zolpidem—> LEAST!

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12
Q

BZDs and induction of sleep

A

They decrease the time it takes to get to sleep AND the duration of sleep in pt who sleep < 6hrs

BUT these effects decline within 1 to 2 weeks

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13
Q

Long term use of BZDs as sleeping pills…recommended?

A

NOT RECOMMENDED because of tolerance, dependence and hangover effects.

Ok if occasionally used

THEY SHOULD NOT BE USED AS HYPNOTICS FOR MORE THAN 3 WEEKS

1 week preferred

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14
Q

BZDs used for sedation and sleep induction

A

Flurazepam; long acting

Temazepam; intermediate acting

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15
Q

The effect on anxiety on muscle tone and its consequences

A

Anxiety—> increased muscle tone—> headaches, aches, pains

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16
Q

BZDs effect on the increased muscle tone associated with anxiety

A

REDUCE muscle tone by central action INDEPENDENT from sedative effect and without obvious loss of coordination

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17
Q

BZD used for reduction of muscle tone in anxiety

A

DIAZEPAM

Treats SKM spasms from:

  1. muscle strain
  2. spasticity from MS, CP
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18
Q

BZDs used as anticonvulsants

A

Clonazepam—> selectively anticonvulsant

Diazepam—> status epilepticus

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19
Q

BZDs, anterograde amnesia and putting it to good use

A

Memories experienced while under BZD is obliterated—> minor surgical procedures are performed without the pt having to remember it.

This is peculiar to BZDs]

MIDAZOLAM—> IV anesthesia

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20
Q

Drug misused for its anterograde amnesia

A

FLUNITRAZEPAM (rohypnol)

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21
Q

BZDs administration

A

Orally
IV
IM—> slow absorption

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22
Q

BZDs pharmacokinetcis

A
  • bind strongly to plasma proteins
  • high lipid solubility—> gradually accumulates in body fat
  • can be short, medium or long acting
  • some have active metabolites—> CUMULATIVE effects—>longer hangovers if given regularly
23
Q

Nordazepam metabolization

A

Noradazepam—>N-desmethyleiazepam

T1/2—> 60 hrs

24
Q

BZDs side effects are due to

A

The long and unpredictable duration of action of these drugs which cause day after impairment

25
Q

BZDs side effects

A 
Drowsiness
Confusion
Amnesia
Impaired coordination 
Enhanced depressant effect of other drugs like alcohol
26
Q

Chronic treatment of BZDs

A

Cognitive impairment

Tolerance

Dependence

! BZDs should only be used 2-4 weeks

27
Q

When should u be careful in terms of administering BZDs

A

Pt with liver disease

Pt on other cns depressants and alcohol consumers

28
Q

Tolerance and BZDs

A
  • All BZDs have tolerance as SE
  • Less severe than tolerance with barbituates
  • little tolerance to hypnotic effect
  • tolerance to euphoric effect
  • tolerance to anxiolytic effect…significant?
29
Q

Dependence and BZDs

A
  • Physiological (not as pronounced as with drugs of abuse)
  • abrupt discontinuation causes withdrawal symptoms (anxiety, restlessness, insomnia and tension) especially of the drug was given over a prolonged period at high doses

Withdrawal syndrome is slower in onset and intensity than with barbiturates due to the long plasma t1/2 of BZDs

30
Q

Dependence with short acting BZDs

A

More abrupt and severe withdrawal symptoms

Triazolam—> very short acting—> withdrawal effect a few hrs after single dose

Not much addiction but still hard to give up

31
Q

Flumazenil

Structure

A

Similar to BZDs

32
Q

Flumazenil

A

BZD anatgonist

33
Q

Flumazenil uses

A
  • Counteracts BZDs over dose comatose pt even before diagnosis is confirmed
  • When severe resp depression occurs
  • Reverse effects of bzds after minor surgery
34
Q

Flumazenil

Duration of action

A

Short acting (2hrs)

35
Q

Pathways other than GABAnergic involved in anxiety and panic disorders

A

5-HT
NA
CCK

36
Q

5-HT role in CNS

A

NT

With both inhibitory and excitatory effects according to the receptor it acts on—> 5HT1 is inhibitory—> inhibit transmitter release from nerve terminals presynaptically

Controls appetite, sleep, mood, hallucinations, stereotyped behavior, pain perception, vomiting

Therefore decreased 5-HT f(x)—> migraine, carcinoid syndrome, mood disorders and anxiety

37
Q

5-HT1A RECEPTOR

A
  • G-protein-coupled receptor
  • Inhibitory autoreceptor
  • Located in CNS
  • Main effects: neuronal inhibition
  • behavioural effects: sleep, feeding, thermoregulation &anxiety
  • Activation of receptor—>inhibition of AC—>decrease in cAMP—>no activation of protein kinases—>reduce the release of 5-HT & other mediators—>overall inhibition of neurotransmission
  • inhibit the activity of N A L.C neurons—> interfere with arousal reactions
38
Q

Buspirone

MOA

A

Activates inhibitory presynaptic 5HT1A receptor—> reduce 5-HT and other mediator’s release

Takes days/weeks therefore cant treat acute anxiety states

39
Q

Buspirone

Uses

A

Treat generalized lied anxiety disorders

40
Q

Buspirone

Side effects

A

Dizziness

Nausea

Headache

Restlessness

41
Q

Buspirone advantages over BZDs

A

No sedation

No loss of coordination

No withdrawal signs if withdrawn abruptly

Does not potentiate effect of sedative hypnotics or alcohol or TCAs

Elderly aren’t more sensitive

42
Q

Z drugs

A

Zolpidem

Zaleploj

Zopiclone

43
Q

Z drugs recommended regimen length

A

Max of 4 weeks

44
Q

Z drugs

MOA

A

Act on subgroup of GABA-A like BZDs—> enhance membrane hyperpolarizayion

45
Q

Z drugs

Uses

A

Sleep disorders (difficulty falling asleep)

46
Q

Z drugs

Effects

A

Rapid onset hypnosis

Few amnesic or day after psychomotor depression/somnolence

47
Q

Z drugs

Side effects

A

Zolpidem and zaleplon: nightmares, agitation, headache, gi upset dizziness

Zopiclone: taste alteration, amnesia, impaired driving, palpitations after withdrawal following prolonged use

48
Q

3Zs Toxicity

A

extensions of C N S depressant effects & dependence

49
Q

Z drugs

Interactions

A

additive CNS depression with ethanol and many other drugs

50
Q

Z drugs

Addiction and Tolerance

A

has been seen w ith all of these recently, despite the fact that they were thought to be better than BZDs in these aspects

51
Q

Ramelteon

MOA

A

agonist at MT1 & MT2 (melatonin ) receptors in the SupraChiasmatic Nucleus thought to be involved maintaining circadian rhythm

52
Q

Ramelteon

Uses

A

sleep disorders esp. in patients who have trouble falling asleep

53
Q

Ramelteon

Effects

A

rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms and no effects on sleep architecture

54
Q

Ramelteon

Side effects

A

Diziness

Somnolence

Fatigue

Endocrine changes (increased prolactin,,decreases testosterone)

CNS (28 decks)

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