Antianxiety Flashcards Preview

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Flashcards in Antianxiety Deck (23):
1

Classes of drugs used for anxiety

-BZDs, barbituates (in the past), BZ1 agonists (zolipidem), 5HT1a-R partial agonists (buspirone), all classes of antidepressants except the atypicals

2

BZDs

Diazepam
Chlordiazepoxide
Flurazepam
Clonazepam
Alprazolam
Temazepam, Triazolam
Lorazepam
Oxazepam (metab of diazepam)

3

Diazepam
Chlordiazepoxide
Flurazepam
Clonazepam
Alprazolam
Temazepam, Triazolam
Lorazepam
Oxazepam (metab of diazepam)

MOA

- MOA: enhance GABA’s inhibitory action in the CNS by interacting w/ BZD allosteric receptor (BZ1 and BZ2) on GABA-A complex but act at diff binding site from GABA
-increase frequency of channel opening; do not open channel!

4

Diazepam
Chlordiazepoxide
Flurazepam
Clonazepam
Alprazolam
Temazepam, Triazolam
Lorazepam
Oxazepam (metab of diazepam)

Pharm

-oral admin, completely absorbed but at different rates
- highly bound to plasma proteins (affects amt of free drug; in elderly proteins ↓ so drug ↑ but also Vd greater)
- do not induce hepatic microsomal enzymes
- ↓oxidative biotransformation @old age, hepatic damage, other drugs → accumulation, ↑duration of action
-Clorazapate converted to Desmethyl by acid in stomach
-while most are metabolized by the liver, Lorazepam and Oxazepam are not, so use them in people with liver problems

5

Diazepam
Chlordiazepoxide
Flurazepam
Clonazepam
Alprazolam
Temazepam, Triazolam
Lorazepam
Oxazepam (metab of diazepam)

AE, tolerance

-AE: the longer the half life, the higher the AEs
-Sedation
- AE’s related to dose, t½ of drug & active metabolites
-anti-anxiety effect w/ 1st dose!

Tolerance
- @chronic use ,for sedative, anticonvulsant actions, takes longer for tolerance to the anti anxiety to develop

6

Diazepam
Chlordiazepoxide
Flurazepam
Clonazepam
Alprazolam
Temazepam, Triazolam
Lorazepam
Oxazepam (metab of diazepam)

Physical dependence

-physical depend. develops w/ high dose/long use→ Sx @withdrawal
- Sx may be mild (anxiety, insomnia~cognitive) or somatic (autonomic hyperarousal—tachy, sweating, etc.)
- Sx may appear days after discontinuation if active metabolites w/ long t½
- rebound anxiety, insomnia after even 1st doses if very short t½
- abrupt withdrawal after long-term admin. of high doses → serious AE, seizures, esp. if short t½, w/o active metabolites; taper pts off

7

Diazepam
Chlordiazepoxide
Flurazepam
Clonazepam
Alprazolam
Temazepam, Triazolam
Lorazepam
Oxazepam (metab of diazepam)

Abuse

- tend to be self-administered w/ other agents
- psychological dependence can be serious problem (pts Tx w/ BZD,if given choice tended not to inc. doses when given the opportunity to do so)
- large therapeutic safety index but can potentiate actions of other sedating drugs (eg ethanol, barbiturates), can → CV, respiratory depression

8

BZ1 vs BZ2

Both are on GABA-A-R
-BZ1 mediates sedative and anticonvulsant actions
-BZ2 mediates anxiety and impairment of functions

9

BZ1 agonist

Zolipidem

10

Zolipidem

-BZ1 agonist
-sedative/hypnotic

11

Buspirone

-MECH: partial agonists @ pre and post synaptic 5-HT1A receptors
-DA2 antagonists
-PHARM: rapidly abs. orally
- highly bound to plasma proteins (>90%)
- metabolized by hepatic oxidation to 1-pyrimidinyl piperazine (active)
- t½ < 3 hr
- therapeutic lag: days to weeks to establish an anxiolytic effect, whereas BZDs work almost immediately
-USE: first available of a series of drugs targeted for modulating serotonergic function in the brain
-Advantages over BZDs: 1. relatively nonsedating profile 2. failure to potentiate depressant effects of EtOH (no interaction w/ EtOH)
-not used in OCD!
-AE: pts previously maintained w/ BZDs frequently report dissatisfaction & discontinue use

12

Situational anxiety

for somatic symptoms → β-blockers (eg Propranolol): dampens cues from sympathetic hyperactivity, could work on serotonin R, only for instant relief

13

Classes of drugs used for OCD

Tricyclic Antidepressants
SSRIs
SNRI
Benzodiazepines

14

TCA for OCD

Chlorimipramine (Clomipramine)
-1st drug used for OCD
- halogenated derivative of Imipramine, more potent as serotonin (5-HT) reuptake inhibitor → very effective
- significant activity inhibiting norepinephrine (NE) reuptake
-AE: cardiac toxicity associated w/ TCA’s (sympathomimetic effects long term, anti-musc & H1 blockers)

15

SSRIs for OCD

-DOC
- equally effective, generally safer (lack anticholinergic actions, quinidine-like effects on cardiac conduction)

16

SNRIs for OCD

Venlafaxine
Duloxetine
- block 5-HT & NE reuptake w/in usual therapeutic dose range; acts as SSRI @ low doses

17

BZDs for OCD

-used as adjuncts to decrease high levels of anxiety in OCD

18

Classes of drugs used in panic disorder

SSRIs, also SNRIs
Tricyclic Antidepressant
Monoamine Oxidase A/B Inhibitor
TriazoloBenzodiazepines

19

SSRIs and SNRIs in panic disorder

- drug of choice
- SNRI Venlafaxine will probably prove effective
-also works for PTSD & social anxiety

20

TCAs in panic disorder

Imipramine
- may be employed if SSRIs do not help

21

Monoamine Oxidase A/B Inhibitor in panic disorder

- Phenelzine
- may be employed if SSRIs do not help

22

Benzodiazepines in panic disorder

Alprazolam
- may be employed if SSRIs do not help
- doses used @panic disorder ~2-10x doses for generalized anxiety disorder - higher doses of alprazolam → ↑AE, withdrawal symptoms

23

Flumazenil

BZD antagonist -- use in BZD OD