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CNS > Pharma 5: Anxiolytic And Hypnotic Drugs > Flashcards

Pharma 5: Anxiolytic And Hypnotic Drugs Flashcards

(54 cards)

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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Triazolam (withdrawn from UK)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

Study These Flashcards
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

Study These Flashcards
A

Noradazepam—>N-desmethyleiazepam

T1/2—> 60 hrs

24
Q

BZDs side effects are due to

Study These Flashcards
A

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

25
BZDs side effects
``` Drowsiness Confusion Amnesia Impaired coordination Enhanced depressant effect of other drugs like alcohol ```
26
Chronic treatment of BZDs
Cognitive impairment Tolerance Dependence ! BZDs should only be used 2-4 weeks
27
When should u be careful in terms of administering BZDs
Pt with liver disease Pt on other cns depressants and alcohol consumers
28
Tolerance and BZDs
- 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
Dependence and BZDs
- 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
Dependence with short acting BZDs
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
Flumazenil Structure
Similar to BZDs
32
Flumazenil
BZD anatgonist
33
Flumazenil uses
- Counteracts BZDs over dose comatose pt even before diagnosis is confirmed - When severe resp depression occurs - Reverse effects of bzds after minor surgery
34
Flumazenil Duration of action
Short acting (2hrs)
35
Pathways other than GABAnergic involved in anxiety and panic disorders
5-HT NA CCK
36
5-HT role in CNS
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
5-HT1A RECEPTOR
- 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
Buspirone MOA
Activates inhibitory presynaptic 5HT1A receptor—> reduce 5-HT and other mediator’s release Takes days/weeks therefore cant treat acute anxiety states
39
Buspirone Uses
Treat generalized lied anxiety disorders
40
Buspirone Side effects
Dizziness Nausea Headache Restlessness
41
Buspirone advantages over BZDs
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
Z drugs
Zolpidem Zaleploj Zopiclone
43
Z drugs recommended regimen length
Max of 4 weeks
44
Z drugs MOA
Act on subgroup of GABA-A like BZDs—> enhance membrane hyperpolarizayion
45
Z drugs Uses
Sleep disorders (difficulty falling asleep)
46
Z drugs Effects
Rapid onset hypnosis Few amnesic or day after psychomotor depression/somnolence
47
Z drugs Side effects
Zolpidem and zaleplon: nightmares, agitation, headache, gi upset dizziness Zopiclone: taste alteration, amnesia, impaired driving, palpitations after withdrawal following prolonged use
48
3Zs Toxicity
extensions of C N S depressant effects & dependence
49
Z drugs | Interactions
additive CNS depression with ethanol and many other drugs
50
Z drugs Addiction and Tolerance
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
Ramelteon MOA
agonist at MT1 & MT2 (melatonin ) receptors in the SupraChiasmatic Nucleus thought to be involved maintaining circadian rhythm
52
Ramelteon Uses
sleep disorders esp. in patients who have trouble falling asleep
53
Ramelteon Effects
rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms and no effects on sleep architecture
54
Ramelteon Side effects
Diziness Somnolence Fatigue Endocrine changes (increased prolactin,,decreases testosterone)

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