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Pharmacology Exam III > CNS Depressants > Flashcards

CNS Depressants Flashcards

1
Q

Pons and Medulla important for

A

respiration control

cardiovascular function

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2
Q

Reticular formation important for

A

control of consciousness, arousal and alertness

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3
Q

Selective Depressants

A

Sedative-hypnotics

Benzodiazepines
Barbiturates
Ethanol

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4
Q

Non-selective Depressants

A

Anti-histamines

Opioid analgesics

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5
Q

Sedative anxiolytics

A

calming effect or sedation with relief of anxiety at relatively low doses

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6
Q

Hypnotics

A

produce drowsiness and/or encourage onset and maintenance of state of sleep

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7
Q

What brain region is most affected with anxiety?

A

limbic system

hippocampus
amygdala
pre-frontal cortex

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8
Q

Sedative Hypnotic Benzo’s (4)

A

Flurazepam
Temazepam
Triazolam
Midazolam

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9
Q

Anxiolytic Benzo’s (5)

A 
Alprazolam
CLorazepate
Diazepam
Lorazepam
Oxazepam
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10
Q

Z Drugs (3)

sleep inducers

A

Zolpidem
Zaleplon
Eszopiclone

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11
Q

Linear slope Drugs

what occurs?

A

barbiturates
alcohol

as dose increases, effects increase all the way up to potentially coma

not as safe

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12
Q

Non-linear slope drugs

what occurs?

A

benzodiazepines
hypnotics (newer)

plateau occurs with increasing dose

SAFER

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13
Q

Sedative-Hypnotics Therapeutic Uses

A

Relief of - anxiety, insomnia

Sedation/amnesia - medical/surgical procedures

Epilepsy/Seizure tx

Withdrawal tx

Muscle relaxation

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14
Q

Benzodiazepines ending?

A

-epam

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15
Q

Benzodiazepine Pharmacokinetics

Metabolism occurs mainly where?

A

Good absorption ORALLY

Metabolized by the LIVER - (CYP3A4)

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16
Q

Benzo’s with rapid metabolism, short duration, less cumulative effects (2)

Why?

A

Lorazepam
Oxazepam

CONVERTED TO INACTIVE GLUCURONIDES - metabolites have no activity

17
Q

Benzo’s with short duration and weakly active metabolites (2)

A

Alprazolam

Triazolam

18
Q

Influence of age on metabolism of benzo’s

Affects what pharmacokinetic values (2)?

A

Elderly have DECREASED PHASE I METABOLISM

Slows hepatic processing

Vd increases
Ve decreases

19
Q

Which two benzo’s have AGE-INDEPENDENT elimination?

A

Oxazepam

Lorazepam

20
Q

Mechanism of action of benzodiazepins

A

Potentiate effects of GABA-A receptors

Increase frequency of OPENING/CONDUCTANCE of CHLORIDE ION CHANNELS

leads to HYPERPOLARIZATION – decreased neuronal firing

21
Q

Benzodiazepine Side effects/Toxicity

A

RESPIRATORY DEPRESSION - can be lethal if combined with other depressants

ANTEROGRADE AMNESIA

TOLERANCE - 12 to 14 days

DEPENDENCE - physical and psychological

WITHDRAWAL

22
Q

Withdrawal effects cause?

How to dissipate?

A

all of the effects that were being suppressed by the drug return more intensely

taper off drugs slowly

23
Q

5 contraindications of benzo’s

A 
pregnancy
elderly
substance abuser
sleep disorders
when alertness is required
24
Q

Major Drug INteraction of Benzo’s

A

ADDITIVE CNS DEPRESSION - when combined with other CNS depressants

25
Q

Benzo’s Major Therapeutic Uses (2)

A

Anxiolytic

Sedative/Hypnotic

26
Q

Flumenazil - type of drug?

MOA

Clinical use

A

BENZODIAZEPINE ANTAGONIST

Competitive inhibitor of BZ RECEPTOR

Counteract benzo overdose

27
Q

Eszopiclone
Zolpidem

type of drug?

MOA?

Clinical use

A

Newer SEDATIVES

Bind selectively to BZ RECEPTOR ON GABA-A receptor and act as AGONISTS

Used primarily for INSOMNIA

28
Q

Barbiturates (3)

A

Pentobarbital
Phenobarbital
Thiopental

29
Q

Barbiturates Clinical Uses

A

Anesthesia - thiopental

Anticonvulsant - phenobarbital

Medically induced coma - pentobarbital

30
Q

Barbiturates Pharmacokinetics

A

absorption/distribution varies with lipid solubility

SLOW LIVER METABOLISM

Little kidney excretion

Duration is DEPENDENT ON METABOLISM - except thiopental

31
Q

Barbiturates MOA

A

increase DURATION OF GABA-GATED CHLORIDE CHANNEL OPENING

Hyperpolarization - neuronal inhibition occurs

32
Q

Ramelteon

type of drug?

MOA?

Clinical use?

A

SEDATIVE

MELATONIN RECEPTOR AGONIST - MT1 and MT2 receptors

minimal abuse liability

33
Q

Buspirone

type of drug?

MOA?

CLinical use?

A

NON-SEDATING anxiolytic

PARTIAL 5HT-1a AGONIST - reduces neuronal excitability and firing frequency, also decreases 5-HT release

anti-anxiety for individuals who need more motor skills for work

34
Q

Beta blocker important for reducing MANIFESTATIONS of anxiety

A

Propanolol

35
Q

Antihistamines (2)

A

Hydroxyzine

Dyphenhydramine

Pharmacology Exam III (11 decks)

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