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nortriptyline (Pamelor, Aventyl)

 

Classes: Antidepressants, TCAs

Dosing and uses of Pamelor, Aventyl (nortriptyline)

 

Adult dosage forms and strengths

capsule

  • 10mg
  • 25mg
  • 50mg
  • 75mg

oral solution

  • 10mg/5mL

 

Depression

25mg PO q6-8hr

No more than 150 mg/day

Dosing considerations

  • Total daily dose can be given HS

 

Chronic Urticaria, Nocturnal Pruritus, Angioedema (Off-label)

75mg/day PO

 

Smoking Cessation (Off-label)

25 mg PO qDay; start 1-2 weeks before quit date; may titrate to 75-100 mg/day 10-28 days prior to selected quit date

 

ADHD (Off-label)

25 mg PO q6-8hr

 

Postherpetic Neuralgia (Off-label)

10-25 mg PO qHS; may increase to 75 mg qHS or divided q12hr if tolerated

 

Dosing Modifications

Hepatic impairment: Administer lower dose and titrate at a slower rate

 

Pediatric dosage forms and strengths

capsule

  • 10mg
  • 25mg
  • 50mg
  • 75mg

oral solution

  • 10mg/5mL

 

Depression (Off-label)

<6 years: Safety and efficacy not established

6-12 years: 1-3 mg/kg/day PO divided q6-8hr, OR 10-20 mg/day PO divided q6-8hr

>12 years: 30-50 mg PO qDay, divided or single dose

See Black Box Warning

 

Nocturnal Enuresis (Off-label)

6-7 years (20-25 kg): 10 mg PO qHs

8-11 years (26-35 kg): 10-20 mg PO qHs

>11 years (36-54 kg): 25-35 mg PO qHs

 

ADHD (Off-label)

0.5 mg/kg/day PO, titrated to maximum 2 mg/kg/day or 100 mg, whichever is less

 

Geriatric dosage forms and strengths

 

Depression

Initial: 30-50 mg PO qDay or in divided doses

May increase to 75-100 mg/day if tolerated

 

Pamelor, Aventyl (nortriptyline) adverse (side) effects

Frequency not defined

Fatigue

Lethargy

Sedation

Weakness

Dry mouth

Constipation

Blurred vision

Agitation

Anxiety

Headache

Insomnia

Nausea

Vomiting

Sweating

Orthostatic hypotension, ECG changes, tachycardia

Confusion, extrapyramidal symptoms, dizziness, paresthesia, tinnitus

Rash

Increased LFTs

Sexual dysfunction

Seizure

Agranulocytosis

Eosinophilia

Leukopenia

Thrombocytopenia

SIADH

 

Warnings

Black box warnings

In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 years) taking antidepressants for major depressive disorders or other psychiatric illnesses

This increase was not seen in patients aged over age 24 years; a slight decrease in suicidal thinking was seen in adults over age 65 years

In children and young adults, risks must be weighed against the benefits of taking antidepressants

Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during the initial 1-2 months of therapy and dosage adjustments

The patient’s family should communicate any abrupt changes in behavior to the healthcare provider

Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy

This drug is not approved for use in pediatric patients

 

Contraindications

Hypersensitivity

Any drugs or conditions that prolong QT intervaL

Acute recovery post-MI

Coadministration with serotonergic drugs

  • Concomitant with or within 14 days of MAOIs (serotonin syndrome)
  • Starting nortriptyline in a patient who is being treated with linezolid or IV methylene blue is contraindicated because of an increased risk of serotonin syndrome
  • If linezolid or IV methylene blue must be administered, discontinue nortriptyline immediately and monitor for CNS toxicity; may resume nortriptyline 24 hours after last linezolid or methylene blue dose or after 2 weeks of monitoring, whichever comes first

 

Cautions

BPH

Urinary/GI retention

Hyperthyroidism

Seizure disorder

Brain tumor

Respiratory impairment

Bipolar mania

Clinical worsening and suicidal ideation may occur despite medication in adolescents and young adults (18-24 years)

Potentially life-threatening serotonin syndrome reported when coadministered with drugs that impair serotonin metabolism (in particular, MAOIs, including nonpsychiatric MAOIs, such as linezolid and IV methylene blue)

Risk of anticholinergic side effects

May cause bone marrow suppression (rare)

May cause orthostatic hypotension

Risk of mydriasis; may trigger angle closure attack in patients with angle closure glaucoma with anatomically narrow angles without a patent iridectomy

May cause sedation and impair physical or mental abilities

Withdraw gradually

Bone fractures have been associated with antidepressant treatment; consider possibility of bone fractures in patients if antidepressant treated patient presents with unexplained bone pain, swelling, bruising or point tenderness

Use with caution in patients who would not tolerate frequent hypotensive episodes, including patients with cardiovascular disease, hypovolemia or with concurrent medication that predisposes for hypotension/bradycardia

Use caution in patients with cardiovascular disease, diabetes mellitus (may alter glucose regulation), hepatic/renal impairment, and the elderly

Abrupt discontinuation or interruption of antidepressant therapy has been associated with a discontinuation syndrome, which may include vomiting, diarrhea, headaches, dizziness, chills, tremors, paresthesias, somnolence, fatigue, and sleep disturbances

May increase the risk of adverse effects associated with electroconvulsive therapy; discontinue therapy prior to electroconvulsive therapy if possible

Due to risk of drug interaction with anesthesia and of cardiac arrhythmia, discontinuation of therapy prior to elective surgery recommended

 

Pregnancy and lactation

Pregnancy category: d

Lactation: Excreted in breast milk; do not nurse (AAP states effect on nursing infants is unknown but may be of concern)

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Pamelor, Aventyl (nortriptyline)

Mechanism of action

Neurotransmitter (especially norepinephrine and serotonin) reuptake inhibitor; increases concentration of neurotransmitter in the CNs

 

Absorption

Onset of action: 1-3 weeks

Peak plasma time: 7-8.5 hr

Steady-state therapeutic plasma concentration: 50-150 ng/mL

 

Distribution

Protein bound: 93-95%

Vd: 21 L/kg

 

Metabolism

Hepatic CYP2D6

 

Elimination

Half-life: 28-31 hr

Excretion: Urine, feces