ANTIDEPRESSANT MEDICATION TABLES
Table 1: MOOD DISORDERS: ANTIDEPRESSANTS
|
Drug |
Typical Starting Dosage (mg) |
Typical Dosage Range (mg/day) |
FDA Indication(s) |
ProposedTherapeutic PlasmaConcentration (ng/mL) |
|
Amitriptyline (Elavil, Endep, Enovil) |
25 TID or |
50-300 |
Depression |
120-250 |
|
Bupropion (Wellbutrin) Bupropion SR (Wellbutrin SR) |
100 BID |
200-450 |
Depression |
<100 |
|
Citalopram (Celexa) |
20 QD |
20-60 |
Depression |
------ |
|
Clomipramine (Anafranil) |
25-100 QD in divided doses within first 2 weeks |
25-250 |
Obsessive-compulsive disorder (OCD) |
100-250 |
|
Desipramine (Norpramin, Pertrofrane) |
25 TID |
100-300 |
Depression |
115-180 |
|
Fluoxetine (Prozac) |
20 QD |
20-80 |
Depression, OCD, bulimia nervosa |
----- |
|
Imipramine (Janimine, Tofranil) |
25 TID |
75-300 |
Depression, childhood enuresis |
200-250 |
|
Mirtazapine (Remeron) |
15 QHS |
15-45 |
Depression |
----- |
|
Nefazodone (Serzone) |
100BID |
200-600 |
Depression |
----- |
|
Nortriptyline (Aventyl, Pamelor) |
25TID/QID |
75-150 |
Depression |
50-150 |
|
Paroxetine (Paxil) |
20 QAM |
10-60 |
Depression, OCD, panic disorder |
------ |
|
Phenelzine (Nardil) |
15TID |
15-90 |
Depression, atypical depression |
----- |
|
Sertraline (Zoloft) |
50 QAM |
50-200 |
Depression, OCD, panic disorder |
----- |
|
Tranylcypromine (Parnate) |
Individualized |
30-60 |
Depression, depression without melancholia |
----- |
|
Trazodone ( Desyrel) |
50 TID |
150-600 |
Depression |
----- |
|
Venlafaxine (Effexor) |
37.5 BID |
75-375 |
Depression |
----- |
|
Venlafxine XR (Effexor XR) |
37.5-75QD |
75-225 |
Depression |
----- |
Table 2: CNS NEUROTRANSMITTERS: SELECTED ANTIDEPRESSANT EFFECTS
|
Serotonin |
Norepinephrine |
Dopamine |
Serotonin |
Norepinephrine |
Dopamine |
||
|
Amitriptyline |
++++ |
++++ |
0 |
Mirtazapine |
+++ |
++ |
0 |
|
Amoxapine |
+++ |
+++ |
0 |
Nefazodone |
+++ |
0/+ |
0 |
|
Bupropion |
0/+ |
+ |
++ |
Nortriptyline |
++ |
+++ |
0 |
|
Desipramine |
+ |
++++ |
0/+ |
Paroxetine |
++++ |
0 |
0/+ |
|
Doxepin |
+++ |
+ |
0 |
Protriptyline |
+ |
++++ |
0 |
|
Fluoxetine |
++++ |
0 |
0/+ |
Sertraline |
++++ |
0 |
0/+ |
|
Fluvoxamine |
++++ |
0 |
0/+ |
Trazodone |
++ |
0 |
0 |
|
Imipramine |
+++ |
++ |
0/+ |
Trimipramine |
++ |
++ |
0 |
|
Lithium |
0/++ |
0 |
0 |
Venlafaxine |
++++ |
+++ |
0/+ |
|
Maprotiline |
0 |
++++ |
0 |
Citalopram |
++++ |
0 |
0/+ |
Table 3: POTENTIAL OF SOME ANTIDEPRESSANTS TO INHIBIT CYPP450 ISOENZYMES
|
Relative ranking |
CYP 1A2 |
CYP 2CP9/CYP2C19 |
CYP 2D6 |
CYP 3A4 |
|
High |
Fluvoxamine |
Fluvoxamine (9,19) |
Paroxetine |
Nefazodone |
|
Moderate to low |
Secondary TCAs Fluoxentine (high-dose) Tertiary TCAs |
Fluxotine (19) |
Secondary TCAs |
Fluxoetine |
|
Low to minimal |
Nefazodone |
Venlafaxine |
Fluvoxamine |
Mirtazapine |
Table 4: EXAMPLES OF DRUGS THAT MIGHT INTERACT WITH AN ANTIDEPRESSANT
|
CYP 1A2 |
CYP 2C19 |
CYP 2C9 |
CYP 2D6 |
CYP 3A4 |
|
Acetaminophen |
Barbiturates |
Diclofenac |
Amphetamines |
Androgens |
Tables 1-4 from 1998 Black Book of Psychotropic Dosing and Monitoring, by A. Schatzburg, MD, C. DeBattista, MD, G.Overman, PharmD,BCPP, and Ereshefsky, PharmD,BCPP. Adapted from Primary Psychiatry July 1997, Vol. 4, No 7.
Table 5: PHARMACOKINETIC COMPARISON OF ANTIDEPRESSANTS
|
|
Sertraline |
Fluoxetine |
Paroxetine |
Citalopram |
Nefazodone |
Fluvoxamine |
Venlafaxine |
Clomipramine |
Amitriptyline |
Bupropion |
|
Half-life |
25 |
48 – 90 |
12 (single dose) 24 (mutiple dose) |
36 |
2-4 |
18 |
5 |
35 |
12-30 |
14 |
|
Metabolite Activity |
10-30% |
Equal |
None |
None |
3 variably active |
Numerous |
Equal |
Equal |
Equal |
3 variably active |
|
Metabolic half-life (h) |
48-96 |
120-330 |
-- |
-- |
1.5-18 |
≤ 24 |
11 |
70 |
16-40 |
8-24 |
|
Steady State (d) |
5-1C |
21-56 |
5 |
7 |
< 5 |
7 |
3 |
7-14 |
5-10 |
5-7 |
|
Dose-proport, |
Yes |
No |
No |
Yes |
No |
Yes |
Yes |
No |
Yes |
Yes |
|
Protein Binding |
98% |
95% |
95% |
80% |
99% |
77% |
20-30% |
95% |
91-95% |
75-85% |
|
Dose reduction elderly |
No |
Yes |
Yes |
No |
Yes |
Yes |
No |
Yes |
Yes |
Yes |
Table 6: ADVERSE EFFECTS OF ANTIDEPRESSANTS
|
|
Anticholinergic Effects |
Arrhythmias |
Sedation |
Seizures* |
Orthostasis |
GI |
Sexual Dysfunction |
Toxicity in Overdose |
|
Amitriptyline |
5 |
5 |
5 |
2 |
4 |
2 |
3 |
4 |
|
Bupropion |
0 |
0 |
0 |
4 |
0 |
1 |
0 / 1 |
3 |
|
Citalopram |
0 |
0 |
0 |
0/+ |
0 |
3 |
3 |
|
|
Clomipramine |
5 |
5 |
4 |
4 |
4 |
3 |
4 |
5 |
|
Desipramine |
2 |
4 |
2 |
2 |
3 |
1 |
3 |
4 |
|
Fluoxetine |
0 |
0 |
0 / 1 |
0 |
0 |
4 |
4 |
1 |
|
Imipramine |
3 |
5 |
3 |
2 |
4 |
2 |
3 |
5 |
|
Lithium |
0 |
1 |
1 |
1 |
0 |
3 |
1 |
5 |
|
Meclobemide |
1 |
0 |
0 |
0 |
2 |
1 |
2 |
2 |
|
Nefazodone |
1 |
0 |
3 |
0 |
1 |
3 |
1 |
1 |
|
Nortriptyline |
3 |
4 |
2 |
2 |
1 |
2 |
3 |
5 |
|
Paroxetine |
2 |
0 |
1 / 2 |
0 |
0 |
4 |
4 |
1 |
|
Setraline |
0 |
0 |
0 / 1 |
0 |
0 |
4 |
4 |
1 |
|
Trazodone |
0 |
1 |
4 |
1 |
3 |
1 |
2 |
2 |
|
Trimipramine |
4 |
5 |
5 |
2 |
3 |
2 |
4 |
5 |
|
Venlafxine |
1 |
0 |
0 / 1 |
0 |
0 / 1 + |
5 |
2 / 3 |
1 |