Protriptyline, Vivactil®

Brand name

  • Vivactil®

Drug Class

  • Tricyclic Anti-depressant (TCA)

Preparations

  • Tablets: 5 mg and 10 mg

Indications

  • Major Depressive Disorders (MDDs)
  • Migraine
  • Neuropathic pain
  • Obesity (to lose weight)

Pharmacology

Mechanism of action & Pharmacodynamics:

  • It is effect in the case of depression by decreasing the reuptake of norepinephrine and serotonin in the central nervous system.
  • Slow therapeutic effects with significant effects after 14 days imitation.

 

Metabolism

Pharmacokinetics:

  • Absorption: gastrointestinal tract
  • Distribution: penetrates the brain rapidly
  • Metabolism: hepatic (Metabolized by Cytochrome P450 2D6)with 8-12 hours peak plasma time and 55-92 hours half-life
  • Excretion: urine

Dosing

1. Adults:

  • Initial: start at low dose 15 to 40 mg/day divided q6-8hr
  • Maximum dose: 60 mg/day

2. Adolescent and Elderly Patients:

  • Initial: 15 mg/day divided into 3 doses

Drug Interactions

  1. Cimetadine
  2. Antidepressants: MAOI, SSRI, and TCA
  3. Alcohol
  4. Ephedrine or pseudoephedrine
  5. Cisapride
  6. Tramadol
  7. Quinidine
  8. Phenothiazines
  9. Propafenone
  10. Flecainide

Adverse Effects

1%- 10% :

  1. Nausea
  2. Vomiting
  3. Fatigue
  4. Headache
  5. Agitation
  6. Lethargy
  7. Anxiety
  8. Dry mouth
  9. Insomnia
  10. Muscle rigidity
  11. Disturbed concentration

Less than 1% :

  1. Cardiovascular: Myocardial infarction , stroke, hypotension
  2. Psychiatric: anxiety, restlessness, agitation, disorientation, delusions
  3. Neurological: Seizures, incoordination, ataxia, tremors, peripheral neuropathy
  4. Anticholinergic: Paralytic ileus, hyperpyrexia, urinary retention, delayed micturition
  5. Allergic: Drug fever, petechiae, skin rash, urticaria, itching
  6. Hematologic: Agranulocytosis, bone marrow depression, leukopenia
  7. Endocrine: Impotence, increased or decreased libido, gynecomastia in the male; breast enlargement and galactorrhea in the female
  • Manifestation of protriptyline toxicity: cardiac arrhythmias, significant hypotension, seizures, and coma. Changes in the electrocardiogram, particularly in QRS axis or width.

Contraindications

  1. Hypersensitivity to this drug
  2. Avoid prescribe with monoamine oxidase inhibitors(risk of hyperpyretic crises, severe convulsions, and death)
  3. In the setting of substitute protripyline for monoamine oxidase inhibitors (MAOi), it should be a period of 14 days after discontinuation MAOi to initiate this drug.
  4. Severe cardiovascular disorders: It is contraindicated to prescribe protriptyline in patient who is consuming cisaprideà QT prolongation, cardiac arrhythmias, and conduction system disturbances.
  5. Narrow angle glaucoma

Pregnancy and Breastfeeding

  • Pregnancy: Category C
  • Lactation: Excretes in milk => Not Recommended in nursing women

Precautions

1. If it is prescribed to treat the depressive component of schizophrenia, psychotic symptoms may be seen.


2. Paranoid delusions with or without hostility may be aggravated.


3. In agitated or overactive cases anxiety or agitation are possible.


4. The probability of suicide in depressed cases exists until dramatic remission.


5. Be cautious in administration of protriptyline and electro-convulsive shock therapy (ECT) simultaneously.


6. Discontinue this medication several days before surgery If possible.


7. Chance of lowering and elevation of blood sugar


8. Risk of manic episodes in bipolar disorders


9. Not recommended in pediatrics < 18 y/o.


10. Use with caution in elderlies! >>> Monitor cardiovascular system if dose goes beyond 20 mg/day >>> When relief of symptoms are observed, reduce to lowest dosage in which no symptoms return

Important Notice

This document is prepared by the “Mental Health for All” team. This document is provided for information purposes only and does not necessarily represent endorsement by or an official position of the Essentials of Medicine. Advice on the treatment or care of an individual patient should be obtained through consultation with a physician who has examined that patient or is familiar with that patient’s medical history.

References:

  1. http://www.fda.gov/downloads/drugs/drugsafety/ucm089820.pdf

One Comment

  • Dr. Siavash Jafari says:

    Special thanks to Dr. Abbas Mohammadi (MD) for his assistance in preparing this material.

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