Protriptyline

Overview of the antidepressant medication Protriptyline

Protriptyline
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Protriptyline is a tricyclic antidepressant (TCA) used primarily in the treatment of depression. It is known for its stimulating effects and is often prescribed when patients experience lethargy or fatigue as part of their depressive symptoms.

Pharmacology

Protriptyline works by inhibiting the reuptake of norepinephrine and serotonin, two neurotransmitters that are believed to play a key role in mood regulation. By preventing the reabsorption of these neurotransmitters, protriptyline increases their availability in the synaptic cleft, thereby enhancing neurotransmission and improving mood.

Medical uses

Protriptyline is primarily indicated for the treatment of major depressive disorder. It is particularly useful in patients who exhibit symptoms of fatigue and low energy, as it has a more stimulating effect compared to other TCAs. Additionally, protriptyline has been used off-label for the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy.

Side effects

Common side effects of protriptyline include dry mouth, constipation, urinary retention, blurred vision, and increased heart rate. These effects are due to its anticholinergic properties. Patients may also experience dizziness, insomnia, and weight loss. Serious side effects can include cardiac arrhythmias, seizures, and orthostatic hypotension.

Contraindications

Protriptyline is contraindicated in patients with a history of myocardial infarction, arrhythmias, or severe liver disease. It should not be used in conjunction with monoamine oxidase inhibitors (MAOIs) due to the risk of serotonin syndrome.

Mechanism of action

Chemical structure of Protriptyline

Protriptyline acts primarily as a norepinephrine reuptake inhibitor, with secondary effects on serotonin reuptake. Its mechanism of action is similar to other tricyclic antidepressants, but it is distinguished by its relatively low sedative properties, making it suitable for patients who require an energizing antidepressant.

Dosage and administration

Protriptyline is typically administered orally in tablet form. The dosage varies depending on the patient's age, weight, and severity of symptoms. It is usually started at a low dose and gradually increased to minimize side effects. Regular monitoring of blood levels may be necessary to ensure therapeutic efficacy and safety.

History

Protriptyline was first introduced in the 1960s and has been used in clinical practice for several decades. It is one of the less commonly prescribed TCAs due to the availability of newer antidepressants with more favorable side effect profiles.

Related pages

• Tricyclic antidepressant
• Norepinephrine
• Serotonin
• Depression (mood disorder)