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pharm exam 3 > anxiolytics > Flashcards

anxiolytics Flashcards

1
Q

Benzodiazapenes

A
  1. Alprazolam
  2. Chlorazepate
  3. Diazepam
  4. Flurazepam
  5. Lorazepam
  6. Midazolam
  7. Oxazepam
  8. Temazepam
  9. Triazolam
  10. Flunitrazepam**date rapists

azepam, azolam, azepate

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2
Q

Benzodiazepine antagonist (antidote)

A

Flumazenil

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3
Q

Benzodiazepine-related Drugs - Newer Hypnotics (Z-drugs)

A
  1. Eszopiclone
  2. Zol[idem
    * pi*
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4
Q

Barbiturates

A
  1. Pentobarbital
  2. Phenobarbital
  3. Thiopental
    * barbitol and pental, al*
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5
Q

Melatonin receptor agonists

A

Ramelteon

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6
Q

5HT Receptor Agonist (Non-sedating Anxiolytic)

A

Buspirone

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7
Q

B-blocker

A

Propanolol

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8
Q

Other

A

Diphenhydramine (Benadryl)
Ethanol
Hydroxyzine (Vistaril)
Propofol (anesthetic)

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9
Q

Date rape drug

A

Flunitrazepam

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10
Q

Benzodiazepine Sedative-Hypnotic

A
  1. Flurazepam*
  2. Temazepam*
  3. Triazolam*
  4. Midazolam*
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11
Q

Benzodiazepene anxiolytic

A 
Alprazolam*
Clorazepate*
Diazepam*
Lorazepam*
Oxazepam*
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12
Q

Other anxiolytic agents

A

Beta blocker and 5-Ht agonist propaolol and buspirone

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13
Q

CNS depressants sedative hypnotics

A

Barbiturates
Pentobarbital*
Phenobarbital*
Thiopental*

Melatonin agonist
Ramelteon*

Antihistamines
Hydroxyzine*
Diphenhydramine*

Alcohols
Ethanol*

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14
Q

Linear slope (higher doses no plateou lead to anesthesia, coma, death)

A

barbiturates and ethanol

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15
Q

Non linear slope, reaching plateua, safer

A

Benzodiazepense and newer hypnotics

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16
Q

Therapeutic uses of sedative hypnotics

A
  1. Relief of anxiety
    a. primary
    b. Secondary anxiety states (e.g., acute myocardial infarction, GI ulcers, etc.)
  2. Relief of insomnia
    3) Sedation and amnesia - before and during medical and surgical procedures
  3. Treatment of epilepsy and seizure states

5) Control of ethanol or other sedative-hypnotic withdrawal states
6. Muscle relaxation

17
Q

Pharmakokinetics benzos

A

Absorption
Good by oral route

Metabolism: Liver

18
Q

inactive water soluble, rapid metab, short duration, less cum effects)

A

Lorazepam

oxazepam

19
Q

Weakly active, short lived matabs, short duration, little clin use

A

Alprozolam

triazolam

20
Q

Long lived active metabs, useful clinically

A

All the rest (ie diazepam)

21
Q

Metabolism influence of age benzos

A

In the elderly (>65) hepatic processing slows for some reactions

Increase in age:

  • Decreased lean body mass
  • Increased Vd for many lipid soluble drugs
  • Decreased rate of elimination (Ve)

(oxazepam and lorazepam) are not influenced by age (Ke is age independent)

(diazepam) will be influenced by age (Ke is age dependent)

22
Q

MOA benzos

A

Potentiate effects of GABA at the GABAA receptors (chloride ion channels)

  • ***1.Increase the frequency of opening and conductance of the Cl- channels
  • Bind to BZ sites between α1 and γ2 subunits to facilitate channel opening
  1. Influx of chloride ion

Increased membrane hyperpolarization and overall neuronal inhibition

  1. Potentiate GABAergic inhibition at all levels of the neuraxis
23
Q

Sides and toxicity benzos

A

1.Drowsiness and sedation
Mental confusion and impaired judgment

2.Ataxia – Diminished motor coordination

*3.Respiratory depression – dose related
Can be lethal if combined with other depressants

*4.Anterograde amnesia – Used as date
rape drugs (e.g., flunitrazepam)

*5.Tolerance (sedative effects)
Most clinical efficacy studies~ 12-14 days; ‘short-acting agents’

  • 6.Dependence – physical & psychological
    7. Dizziness, headache, nausea (uncommon
24
Q

Abrupt withdrawal benzos

A 
Restlessness
Anxiety
Nervousness
Irritability
Insomnia
Headache
GI distress
Seizures
*opp of what used to treat
solve by slow titration dose and using long acting
25
Q

Contraindication benzos

A
  1. Pregnancy
  2. Elderly
  3. Substance abuse a concern (though used in management of withdrawal)
  4. Sleep disorders - Patients with sleep apnea, narcolepsy, etc.
  5. When alertness is required
26
Q

Drug interactions of benzos, additive CNS depression*

A

Ethanol, opioids, anticonvulsants, phenothiazine, antihistamines, tricyclic antidepressants

27
Q

therapeutic use of benzos*

A

Anxiolytic - relief of anxiety (e.g., GAD)

Sedative/hypnotic – relief of insomnia

28
Q

MOA flumazenil (benzo antag)

A

Competitive inhibitor that binds to the BZ receptor

Can reverse the effects of benzodiazepines

29
Q

matab flumazenil

A 
Rapid absorption (usual route – i.v.)
Hepatic metabolism, Short duration (~ 2hr)
30
Q

Effects and uses for flumazenil

A

Effects
Generalized CNS arousal
Anxiogenic

Uses
Terminate benzodiazepine-induced sedation
Diagnosis and treatment of benzodiazepine toxicity
CNS depression (coma) in hepatic encephalopathy

31
Q

Benzo related newer hypnotics (moa, clin use and all)

A

Clinical Use: Newer sedative agents indicated for management of insomnia

NOT a benzodiazepine (chemically) – novel structures

Mecanism of Action: Selectively bind to BZ receptors on GABAA receptor and act as an agonist (only bind alpha1 subunit isoforms)

Rapidly acting

Short duration (t½ ~ 2-3 hr) – inactive metabolites

Longer lasting effects in the elderly

Similar effects as benzodiazepines

Antagonist – flumazenil

32
Q

Clinical uses of barbiturates

A
  1. Anesthesia (thiopental)
  2. Sedative / hypnotic
    Largely replaced by the benzodiazepines
    Used in combination with other agents
  3. Anticonvulsant (phenobarbital)
  4. Medically induced coma (pentobarbital)
33
Q

MOA barbiturates

A

1.**Increase the duration of the GABA-gated chloride channel opening

Bind to at a different site(s) from the benzodiazepine binding sites on GABAA receptors

2.Resulting in increased:
Membrane hyperpolarization
Neuronal inhibition

34
Q

Ramelteon (all)

A

Sedative agent - Indicated for management of insomnia

Effective in inducing sleep onset – especially used in patients with difficulties falling asleep (very little influence on sleep architecture)

*Mechanism of Action: Melatonin receptors agonist
MT1 (sleep onset) **
MT2 (circadian pattern)

Metabolism: Extensive first that forms an active metabolite with longer half-life

Minimal abuse liability, as regular use does not result in dependence; not a controlled substance

35
Q

Buspirone (All)

A

NON-sedating anxiolytic

Causes less psychomotor impairment than benzodiazepines and does not affect driving skills

Delayed onset of therapeutic response – not suitable for management of acute anxiety states and panic disorders

No amnesia, no muscle relaxant properties

*Mechanism of Action: Partial agonist at 5HT1A receptors

Metabolism: Half-life is 2-4 h, extensive first-pass metabolism

Minimal abuse liability

Adverse effects: Nonspecific chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, GI distress

36
Q

function of 5-Ht1A receptor

A

Activation of the 5-HT1A receptor reduces neuronal excitability, firing frequency and 5-HT release.

37
Q

Beta blockers

A

NOT an anxiolytic, but diminishes some of the somatic manifestations of anxiety (stage fright, performance anxiety)

38
Q

Anti histamines

A

Used as mild sedative/relaxant for multitude of procedures

Anxiolytic via a sedative action – common to most antihistamines

39
Q

Alcohol

A

Anxiolytic via a sedative action

Ethanol is probably the oldest and most commonly used anxiolytic

pharm exam 3 (2 decks)

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