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Pharmacology Test 4 > Anxiolytics > Flashcards

Anxiolytics Flashcards

1
Q

Used to treat chronic anxiety, i.e. apprehension, restlessness, tension

A

anxiolytic drug

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2
Q

Decreases activity, moderates excitement and calms the patient

A

sedative drug

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3
Q

Produces drowsiness and facilitates the onset and maintenance of sleep

A

hypnotic drug

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4
Q

What are the clinical uses of CNS depressants? (7)

A

1) Reduce anxiety
2) Induce sleep
3) Sedation before surgery (amnesia-good)
4) Epilepsy
5) Balanced anesthesia for surgery
6) Control of withdrawal syndromes
7) Muscle relaxation

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5
Q

What’s the difference between Type A drugs and Type B drugs?

A

Type A lead to coma/death with increased dosage. Type B level off around hypnosis

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6
Q

Type A drugs (5)

A

Barbiturates, alcohol, chloral hydrate, GHB, some other general anesthetics

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7
Q

Type B drugs - what does this mean?

A

Benzodiazepines - great as anxiolytics!

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8
Q

Phenobarbital (Barbiturate) vs. Diazepam (benzo) : therapeutic index?

A

Diazepam’s is 10x that of phenobarbital’s

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9
Q

What is GABA?

A

primary inhibitory NT in brain

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10
Q

What are GABAa receptors like? What do they do?

A

ligand-gated, fast response. They allow Cl ions to go through membrane which keeps cell’s potential negative which makes AP’s less likely

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11
Q

How do benzodiazepines work on GABAa receptors? What don’t they do?

A

they increase the GABAa receptors’ affinity for GABA.They do NOT alone open the Cl channel

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12
Q

How do barbiturates work on GABAa receptors?

A

they increase the amount of opening by GABA AND at high concentrations can open the channel in the absence of GABA

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13
Q

What is the main mechanism of action of benzos? How do they do this? Are benzos agonists?

A

potentiation of GABA-stimutlation of GABA receptors. They bind to the GABA receptor and cause GABA to bind to the receptor with a higher affinity. They do NOT stimulate the receptor alone!! Therefore, NOT an agonist!! They increase GABA transmission, but only through GABA that has already been released into the synapse.

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14
Q

What do anxiolytics do in animal studies?

A

“release punishment suppressed behavior”

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15
Q

What are the two main classifications and which is the principle type*?

A

Type A: Barbituates, Type B: Benzodiazepines*

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16
Q

What is the model agent of barbiturates?

A

Pentobarbital

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17
Q

What are the model agents of benzodiazepines?

A

Alprazolam, Diazepam, Lorazepam, Triazolam, Midazolam

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18
Q

What determines the choice of benzodiazepines? What’s an exception?

A

Pharmacokinetics. Exception: alprazolam for panic disorders and agoraphobia

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19
Q

Where are benzos metabolized?

A

liver

20
Q

What’s significant about benzos (metabolites)? Exceptions?

A

There are many active metabolites with long half-lives >24 hours. Exceptions: Lorazepam and Oxazepam are fast acting and rapidly metabolized. Triazolam is also special- it has an active metabolite but both Triazolam and its metabolite have short half lives.

21
Q

Are benzos bound to plasma proteins?

A

Yes. Up to 90% and not easily displaced

22
Q

What should be a concern about giving benzos to elderly pts?

A

metabolism is slow…give in low dosages

23
Q

What are the short acting benzos (5)? Which one is special?

A

Alprazolam, Lorazepam, Midazolam, Oxazepam, Triazolam. Oxazepam is special because it is IV only (very rapid!)

24
Q

What are the long acting benzos (1)?

A

Diazepam

25
Q

What are the therapeutic effects of benzos (4)?

A

antianxiety, sedation, hypnosis, anticonvulsants

26
Q

at low doses, are the anxiolytic actions of benzos associated with little or great CNS depression?

A

little

27
Q

at low doses of benzos, what’s up with sedation?

A

suppression of responsiveness to a constant level of stimulation. tolerance develops within days

28
Q

Which type of benzos are best for hypnosis? When are another kind used?

A

Fast acting. Short-acting used if antianxiety action isn’t wanted.

29
Q

what are some characteristics of hypnotic effects of benzos? tolerance?

A

latency of onset reduced, stage 2 non-REM sleep increased, REM duration decreased, duration of slow wave reduced. Tolerance over days-weeks…rebound increase in REM with withdrawal

30
Q

Which benzo is used as an anticonvulsant?

A

Diazepam - status epilepticus and alcohol withdrawal

31
Q

What are some side effects of benzos (4)?

A

1) Respiration: depression if higher than sedating dose (except in pulmonary obstruction: greater sensitivity)
2) Euphoria: fast-acting, short-lived benzos are abused; psychological dependence common with long term use.
3) Paradoxical excitement: associated with “CNS disinhibition”
4) Anterograde amnesia: can’t remember things happening while under effects of drug

32
Q

What are drug interactions of benzos (4)?

A

1) additive or even synergistic CNS depression with other sedative hypnotics and alchohol
2) functional cross-tolerance with ethanol and other sedative hypnotics
3) oral contras reduce Diazepam eliminiation
4) asymmetric metabolic cross tolerance with ethanol and barbs

33
Q

Do benzodiazepines induce liver P450 enzymes?

A

NO

34
Q

Do EtOH and barbiturates induce liver P450 enzymes?

A

YES

35
Q

What does asymmetric metabolic cross tolerance with barbs and benzos mean?

A

barbs can induce the liver enzymes that metabolize BOTH barbs AND benzos! over time, half life of barbs becomes shorter. BARBS and BENZOS are metabolized by the same enzymes!

36
Q

reverse side of liver enzymes stuff?

A

benzos do NOT induce them. half-lives stay the same with benzo use over time.

37
Q

What is the antagonist vs. benzos?

A

Flumazenil

38
Q

What’s up with Flumazenil?

A

short half-life, IV only

39
Q

What are the actions of Barbiturates (3)?

A

1) Sedative-hypnotic
2) Anticonvulsant properties (but Diazepam preferred!!)
3) Induction of liver microsomal enzymes

40
Q

What are the (largely historical) therapeutic uses (3)?

A

1) IV Anesthetic
2) Sedatives
3) Epilepsy

41
Q

Which barbiturate is used as IV anesthetic? Is it short or long acting?

A

Thiopental. Ultra-short acting

42
Q

Which barbiturate is used as sedative?

A

Pentobarbital

43
Q

Whcih barbiturate is used for epilepsy?

A

Phenobarbital

44
Q

What is the mechanism of barbiturates?

A

Potentiation of inhibitory neurotransmission GABAa receptor

45
Q

What are 3 examples of barbiturates and what are their defining characteristics?

A

Thiopental - ultra short-acting
Phenobarbital - anti-epileptic
Pentobarbital - hypnotic, high abuse potential, replaced by benzos

46
Q

What are some non-sedative drugs used to treat anxiety (4)? What are their defining characteristics?

A

1) buspirone: very slow acting, novel structure
2) Beta-adrenergic blockers: decrease sympathetic tone, symptomatic relief of anxiety, e.g. speeches
3) Alpha 2 agonist: Clonidine
4) Tricyclic antidepressants: panic attacks

47
Q

What are some other sedative/hypnotics (5)? Some notes about them?

A

1,2) Zolipidem, Zaleplon: act at benzo binding site btu different structure. sedative>anxiolytic…lower abuse potential?

3) Chloral hydrate: restricted to instiutional use, inexpensive, significant toxicity, oral prep for pediatrics
4) Hydroxzine, Diphenhydramine: antihistamines, OTC sedatives/hypnotics, may synergize with morphine for analgesia, anticholinergic side effects (e.g. drymouth), contraindicated for pregnant women

Pharmacology Test 4 (10 decks)

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