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protriptyline (Vivactil)

 

Classes: Antidepressants, TCAs

Dosing and uses of Vivactil (protriptyline)

 

Adult dosage forms and strengths

tablet

  • 5mg
  • 10mg

 

Depression

Initiate at low dose (10 mg/day) and gradually titrate upward every 5-7 days

15-60 mg/day PO divided q6-8hr; not to exceed 60 mg/day

 

Pediatric dosage forms and strengths

tablet

  • 5mg
  • 10mg

 

Depression

<12 years: Safety and efficacy not established

≥12 years: 15-20 mg PO qDay

See Black Box Warning

 

Geriatric dosage forms and strengths

5 mg PO q8hr initially; increase by 5-10 mg q3-7days PRN; cardiovascular adverse effects may increase if doses exceed 20 mg/day

 

Vivactil (protriptyline) adverse (side) effects

1-10%

Sedation

Fatigue

Headache

Agitation

Insomnia

Blurred vision

Weakness

Lethargy

Anxiety

Dry mouth

Constipation

Nausea

Vomiting

Sweating

Weight change

 

Frequency not defined

Confusion

EPs

Dizziness

Tinnitus

Paresthesia

Seizure (rare)

Worsening depression/suicide (rare)

Orthostatic hypotension

ECG changes

Tachycardia

Paralytic ileus (rare)

Agranulocytosis (rare)

Thrombocytopenia (rare)

Eosinophilia (rare)

Leukopenia (rare)

Increased LFTs

Sexual dysfunction

Rash

SIADH (rare)

 

Warnings

Black box warnings

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

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

Severe cardiovascular disorder

Narrow angle glaucoma

Within 14 days of MAOIs (risk of serotonin syndrome); if linezolid or IV methylene blue (MAOIs) must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity; may resume 24 hr after last linezolid or methylene blue dose, or after 2 weeks of monitoring, whichever comes first

Any drugs or conditions that prolong QT intervaL

Acute recovery post-MI

 

Cautions

Caution in BPH, urinary/GI retention, hyperthyroidism, open-angle glaucoma, seizure disorder, brain tumor, respiratory impairment

Clinical worsening and suicide ideation may occur despite medication

Risk of anticholinergic side-effects

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

 

Pregnancy and lactation

Pregnancy category: C

Lactation: avoid

 

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 Vivactil (protriptyline)

Mechanism of action

Neurotransmitter (especially NE and serotonin) reuptake inhibitor; increases concentration of neurotransmitte in the central nervous system.

 

Pharmacokinetics

Half-Life: 54-92 hr

Peak Plasma Time: 24-30 hr

Protein binding: 92%

Bioavailability: Completely absorbed

Metabolism: Hepatic (oxidation, hydroxylation, glucuronidation)

Excretion: Urine