Ken Farr Table 2 Anxiolytics
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Table 2. Anxiolytics (NOTE !!!!: SSRI’s AND SNRIs are frequently used in the Tx of Anxiety Disorders)
BENZODIAZEPINES
Agent
Sched ule
Approved Indications
Approv ed Oral Adult Dosage Range (mg/d)
Pharmacokinetic Parameters Dosa ge Form s
Onset (PO)
fast
Alprazolam Xanax, Pfizer; various
C-IV
anxiety disorders; panic disorder
0.25-4
L, T
Chlordiazep oxide Librium, Valeant; various
C-IV
anxiety; alcohol withdrawal; preoperative sedation
5-100
C IM
Clonazepam Klonopin, Roche; various Clorazepate Tranxene, Abbott; various
C-IV
seizure disorders; panic disorder
25-50 mg single dose 0.25-2
C-IV
Diazepam Valium, Roche; various
C-IV
anxiety; seizure disorders; alcohol withdrawal anxiety; alcohol withdrawal; muscle spasm; preoperative sedation; status epilepticus
Lorazepam Ativan, Baxter/Biovail; various
C-IV
anxiety; preoperative sedation
Oxazepam Serax, Faulding; various
C-IV
anxiety disorders; alcohol withdrawal
t-1/2
Active Metabolites
Comments
intermedi ate
alpha-hydroxyalprazolam
dependence may occur after shortterm use
fast
long
desmethylchlordiaz epoxide, demoxepam, desmethyldiazepam, oxazepam
variable bioavailability with IM dosing
T, ODT
moder ate
long
none
15-60
C, T
very fast
long
desmethyldiazepam , oxazepam
2-40
L, T
2-10 mg single dose
IM
1-8
L, T
1-4 mg single dose 30-120
very fast
long
desmethyldiazepam , 3-hydrozydiazepam, oxazepam
IM
fast
short
none
C, T
slow
short
none
variable bioavailability with IM dosing
OTHERS
Buspirone BuSpar, BrIstol-Myers Squibb; various Hydroxyzine Atarax/Vistaril , Pfizer; various
No
anxiety
15-60
T
0.5-1.5 h
N/A
N/A
do not use with MAOls; less sedating than benzodiazepine anxiolytics
No
anxiety; pruritus; preoperative and postoperative sedation
50-400
C, L, T IM
15-30 min (peak 2 h)
N/A
N/A
anticholinergic; sedation
50-100 mg single dose * Avoid alcohol and other CNS depressants with these agents (except buspirone); drowsiness may impair ability to drive; use caution.
Table 2. Anxiolytics (NOTE !!!!: SSRI’s AND SNRIs are frequently used in the Tx of Anxiety Disorders)
BENZODIAZEPINES
Agent
Sched ule
Approved Indications
Approv ed Oral Adult Dosage Range (mg/d)
Pharmacokinetic Parameters Dosa ge Form s
Onset (PO)
fast
Alprazolam Xanax, Pfizer; various
C-IV
anxiety disorders; panic disorder
0.25-4
L, T
Chlordiazep oxide Librium, Valeant; various
C-IV
anxiety; alcohol withdrawal; preoperative sedation
5-100
C IM
Clonazepam Klonopin, Roche; various Clorazepate Tranxene, Abbott; various
C-IV
seizure disorders; panic disorder
25-50 mg single dose 0.25-2
C-IV
Diazepam Valium, Roche; various
C-IV
anxiety; seizure disorders; alcohol withdrawal anxiety; alcohol withdrawal; muscle spasm; preoperative sedation; status epilepticus
Lorazepam Ativan, Baxter/Biovail; various
C-IV
anxiety; preoperative sedation
Oxazepam Serax, Faulding; various
C-IV
anxiety disorders; alcohol withdrawal
t-1/2
Active Metabolites
Comments
intermedi ate
alpha-hydroxyalprazolam
dependence may occur after shortterm use
fast
long
desmethylchlordiaz epoxide, demoxepam, desmethyldiazepam, oxazepam
variable bioavailability with IM dosing
T, ODT
moder ate
long
none
15-60
C, T
very fast
long
desmethyldiazepam , oxazepam
2-40
L, T
2-10 mg single dose
IM
1-8
L, T
1-4 mg single dose 30-120
very fast
long
desmethyldiazepam , 3-hydrozydiazepam, oxazepam
IM
fast
short
none
C, T
slow
short
none
variable bioavailability with IM dosing
OTHERS
Buspirone BuSpar, BrIstol-Myers Squibb; various Hydroxyzine Atarax/Vistaril , Pfizer; various
No
anxiety
15-60
T
0.5-1.5 h
N/A
N/A
do not use with MAOls; less sedating than benzodiazepine anxiolytics
No
anxiety; pruritus; preoperative and postoperative sedation
50-400
C, L, T IM
15-30 min (peak 2 h)
N/A
N/A
anticholinergic; sedation
50-100 mg single dose * Avoid alcohol and other CNS depressants with these agents (except buspirone); drowsiness may impair ability to drive; use caution.
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