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anxiolytic agents Flashcards

1
Q

What are the different levels of “graded response” of the CNS to sedative hypnotics?

A

• Least to most
• Sedation, disinhibition, anxiolysis
○ Therapeutic window for possible selective anticonvulsant and muscle-relaxant
• Hypnosis
• Anestheisa
○ Benzodiazepines start leveling off in ability at about this point
• Medullary depression
• Coma
○ Barbituates get you here
○ There are times where induction of a coma is indicated

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2
Q

What is dangerous about really high doses of barbituates?

A

• As you increase the dose of these drugs above that needed for hypnosis/sleep
○ Reach general anestheia
○ Progression to depression of respiratory and vasomotor centers
• Ultimate worry is coma and death with overdose

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3
Q

What’s the major difference in dose considerations between beznodiazepines and barbituates?

A
  • Benzodiazepines are non-linear in their dose response relationship
    • They need much greater dosage increments to achieve CNS depression
    • Greater margin of safety as a result
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4
Q

What are the 4 categories of drugs used in treatment of anxiety?

A

• Antidepressants
○ SSRIs and SNRIs are most commonly used
• Benzodiazepines
○ Useful in acute or situational anxiety
• Buspirone
○ Weaker, but fewer side effects
• Barbituates
○ Try not to use these for day-day treatment of anxiety

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5
Q

Sedative and hypnotic drugs are separately classified from other CNS depressants how?

A
  • Graded, dose-dependent depressant effects
    • Augment GABA neuronal inhibition and/or inhibit glutamate neuronal excitation
    • Sedative - decreasing activity, moderating excitement, calming
    • Hypontic - drowsiness, facilitate onset and maintenance of sleep that resembles natural sleep and from which recipient can be easily aroused
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6
Q

What is the most common mechanism of action for the sedative-hypnotic drugs?

A

• Vast majority act to facilitate the action of GABA at the GABA-a receptor
○ This is a chloride ion channel complex
• GABA is major inhibitory transmitter in the CNS
• Increasing Cl conductance will hyperpolarize the neuron
• Hyperpolarization leads to diminished neuronal excitability and neurotransmission
• Molecular level - usually facilitate opening but does not directly initiate cl current

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7
Q

What do benzodiazepines vs. barbituates in particular do to the GABA receptor?

A

• Benzos - Intensify the effect of GABA
○ Barbituates will prolong GABA effect
• Benzos - need GABA for effect (thus can’t be used for surgical anesthesia)
○ Barbituates at high concentrations will interact with GABA receptor directly
• Barbituates are less selective and also depress excitatory NT
○ Lower safety margin

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8
Q

Flumazenil does what?

A
  • Antagonist of benzodiazepines

* Competitive inhibitor, binds at benzo site on GABA channel complex

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9
Q

Zolpidem is an example of what type of drug?

A
  • Z drug

* Non-benzodiazepines that interact with the benzodiazepine binding site as agonists

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10
Q

What importance do the different alpha subunits of the GABA-a Cl channel have on drug effect?

A

• Alpha-1 subunit vs. alpha-2/5 subunit
• These subunits are differentially expressed in different areas of the brain and allow for more targeted treatments
• Alpha-1 is expressed in the cortex
• Alpha-2/5 is expressed in the limbic system and brain stem
○ Benzo’s - both subunit types
○ Produce sedative (sleep), amnestic, anxiolytic and anticonvulsant actions
○ Z-drugs are alpha-1 specefic and produce sleep but no anxiolysis

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11
Q

Anxiolysis and sedation are considered the same thing. Why?

A

• Described as a decrease in responsiveness to a given level of stimulation
• Allows for relief of anxiety (valence attributed to situation and stimuli)
• Anxiolysis is usually accompanied by some impairment of psychomotor function
○ Behavioral disinhibition may also occur
• Non-sedative anxiolytics exist
○ Buspirone and propanolol

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12
Q

How can benzo treatment help with muscle spasms?

A
  • Action to inhibit spinal cord polysynaptic reflexes may aid in muscle spasms
    • Effect requires high doses, usually accompanied by significant CNS depression
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13
Q

Describe the anticonvulsant effects of the sedative-hypnotic drugs.

A

• Higher doses of most barbiturates and some benzos inhibit formation and spread of seizure activity in cortical neurons
• Some do so at does that do not cause severe sedation or effects on mental or motor activity
○ Phenobarbital, clonazepam
• Diazepam (or lorazepam) is drug of choice for status epilepticus

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14
Q

Describe the use of these drugs for anesthesia

A
  • Short-acting barbitruates (thiopental) used to induce or maintain surgical anesthesia
    • Bezos are not capable of inducing or maintaining anesthesia but are used as adjuncts for their anxiolytic and amnesia producing properties
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15
Q

Describe the attributes of psychologic and physical dependence on the sedative-hypnotic drugs

A

• Desirable effects frequently lead to compulsive misuse and pscychologic dependence
○ Relief of anxeity, euphoria, disinhibition, promotion of sleep
• ALL cause physical dependence if used on a chronic basis
○ Need to titrate down if you want to get off of them
• Withdrawal syndrome includes
○ Decreased appetite, nausea, fatigue, tachycardia, insomnia, depression, weight loss
○ May also see a state of increased excitability (anxiety, tremors, hyperreflexes)
○ These excited brain functions can lead to convulsions
• The shorter the 1/2 life, the worse the withdrawal

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16
Q

Can tolerance to sedative and hypnotic drugs occur?

A

• Yes.
• Common feature when agents are used continuously in high doses
• May require increase in dose to maintain effect
• Metabolica nd pharmacodynamic components of tolerance are seen
• Occurs rapidly to sedative and anticonvulsant effects
○ Less tolerance to anxiolytic effects

17
Q

Which diazepines have a fast onset of action when taken by the oral route and are therefore good for prn usage?

A
  • Diazepam, alprazolam, triazolam

* Oxazepam and temazepam have SLOW absorption so don’t use these orally for prn use

18
Q

How are the hypnotic-sedative drugs eliminated?

A

• As lipid soluble drugs, benzodiazepines require biotransformation to more water-soluble metabolites
○ 1/2 life depends mainly on actiivity of drug metabolizing enzymes
§ CYP2C19 and CYP3A4
• Most benzos undergo CYP450 oxidations
○ Phase I
• Then subsequent inactivation via conjugation by glucuronidation
○ Phase II
• After phase II there is renal elimination (it’s soluble enough to be eliminated renally)
• Barbiturates are oxidiezed to inactive metabolites via CYP450, excreted as glucuronide

19
Q

Thiopental can lose its efficacy pretty quickly. It’s not due to 1/2 life but what is it due to?

A
  • Super lipid soluble, so it gets into CNS quickly. BUT, it also gets rapidly redistributed everywhere else
    • The redistribution is associated with the loss in efficacy
20
Q

What benzo has fast and reliable intramuscular absorption?

A
  • Lorazepam

* Diazepam and chlordiazepoxide have poor IM bioavailability

21
Q

Diazepam, chlordizepoxide and flurazepam can all end up causing an elderly person to be sedated in the daytime and other CNS effects. Why?

A
  • The elderly have slower drug elimination routes/processes
    • These drugs all have phase I metabolites that are still active, but have longer 1/2 lives.
    • Thus, you can get a build up of this metabolite over time with repeated doses. Take this into account with elderly patients
22
Q

What are the drug-drug interactions you need to think of with sedative-hypnotic drugs?

A

• Barbiturates are classic inducers of CYP450 enzymes
• Represent a major source of clinically significant drug interactions
○ One of the many reasons for declining use
• Drug interactions are possible whenever benzos are given with inducers or inhibitors of CYP450
○ Chronic benzo use DOES NOT induce CYP450

23
Q

What are the three notable extension effects of benzodiazepines?

A

• Sedation and performance impairment
○ Excessive drowsiness, psychomotor incoordination, decreased concentration, cognitive deficits, impaired judgment
○ More likely to be seen with use of high doses or benzos with long or intermediate 1/2 lives
○ Shorter the 1/2 life, less the daytime sedation
○ These are more likely in older patients (impaired elimination)
• Drug-drug interactions
○ Safe to use alone but they have additive depressant effects if given with alcohol, opioids, antipsychotics, anticonvulsants, antihistamines, TCAs
• Anterograde amnesia
○ New memory is impaired
○ Happens through the enhancement of GABA function
○ Can use for uncomfortable procedures as they cooperate but don’t remember later
○ Criminal use in date rape
§ Flunitrazepam = roofies

24
Q

What’s the black box warning of benzo’s?

A
  • All drugs in this class have a black box warning relating to occurrence of strange sleep-related behavior and severe allergic reactions (anaphylaxis and facial swelling)
    • Use of oral benzo’s alone is safe but it can make chronic pulmonary disease worse as well as symptomatic sleep apnea
25
Q

If you use benzos during a surgical procedure and you want to hasten recovery, what benzo receptor antagonist can you use?

A
  • Flumazenil is a benzo receptor antagonist
    • Reverses sedative effects of benzos
    • Doesn’t help at all in barbiturate or ethanol toxicity
26
Q

What’s the drug regimen for Genarlized anxiety disorder?

A
  • First line - Ssris, snris,

* Second line - Benzos, buspirone, TCAs

27
Q

What’s the drug regimen for PTSD?

A
  • First line - CBT (behavioral), SSRIs and SNRIs

* There is no second line here, the first line are super effective

28
Q

What’s the drug regimen for Obsessive Compulsive disorder?

A
  • First line - CBT (behavioral), SSRIs and SNRIs

* Second line - augment with atypical antipsychotics

29
Q

What’s the drug regimen for Social Anxiety disorder?

A
  • Generalized - Ssris, snris,

* performance - Beta Blockers (propanolol) or high potency BDZs (alprazolam, clonazepam)

30
Q

What’s the drug regimen for Panic disorder?

A

• First line - high potency BDZs (alprazolam, clonazepam) for acute situation
○ Ssris for non-acute therapy
• Second line - Benzos, MAOIs, TCAs

31
Q

The benzodiazepines given to us in the LO to memorize are what? (6)

A
  • Diazepam (Designated)
    • Alprazolam (aphrodesiac)
    • Lorazepam (lotions)
    • Flumazenil (facilitate)
    • Oxazepam (overt)
    • Midazolam (movements)
32
Q

What are the two barbiturates French told us to memorize?

A
  • Phenobarbital

* pentobarbital

Neuro (59 decks)

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