TCAs

Question 0

Tertiary Amines

Answer 0

• highly anticholinergic, more sedating, greater lethality in overdose
• amitriptyline (Elavil)
• Imipramine (Tofranil)
• Clomipramine (Anafranil)
• Doxepin (Sinequan)

Question 1

TCAs- General

Answer 1

• as move from tertiary to secondary amines get more NE reuptake inhibition
  - tertiary: amitriptyline, clomipramine (for OCD), doxepin, imipramine (urinary incontinence)
  - secondary: desipramine, nortriptyline, protriptyline
  - warning : cardiac arrhythmia in OD

Question 2

Amitriptyline (Elavil)

Answer 2

• useful in chronic pain, migraines, and insomnia

Question 3

Imipramine (Tofranil)

Answer 3

• has intramuscular form

- useful in enuresis and panic disorder

Question 4

Clomipramine (Anafranil)

Answer 4

• most serotonin specific, useful in treatment of OCD

Question 5

Doxepin (Sinequan)

Answer 5

• useful in treating chronic pain

- emerging use as a sleep aid in low doses

Question 6

Secondary Amines

Answer 6

• metabolites of tertiary amines
• less anticholinergic, less sedating
• nortriptyline (Pamelor, Aventyl)
• Desipramine (Norpramin)

Question 7

Nortriptyline (Pamelor, Aventyl)

Answer 7

• least likely to cause orthostatic hypotension
• useful therapeutic blood levels
• useful in treating chronic pain

Question 8

Desipramine (Norpramin)

Answer 8

• more activating, least sedating

- least anticholinergic

Question 9

TCAs- Side Effects

Answer 9

• antiadrenergic properties= CARDIOVASCULAR side effects: orthostatic hypotension, dizziness, reflex tachycardia, arrhythmias, and electrocardiographic (ECG) changes (widening QRS, QT, and PR intervals); avoid in pts with conduction abnormalities or recent MI
• anticholinergic effects: dry mouth, constipation, urinary retention, blurred vision, tachycardia, exacerbation of narrow angle glaucoma
• LETHAL in overdose: assess suicide risk in pts! Signs of overdose: agitation, tremors, ataxia, delirium, hypoventilation, myoclonus, hyperreflexia, seizures, coma
• Seizures: 0.3% chance, more common at higher plasma levels and with clomipramine & tetracyclics
• serotonergic effects: erectile/ejaculatory dysfunction in males, anorgasmia in females