butriptyline

Action and Spectrum

Actions and spectrum: 

Action: 

• Antidepressant: butriptyline exerts its primary therapeutic effect by inhibiting the reuptake of neurotransmitters, including serotonin and norepinephrine, in the brain. By doing so, it increases the levels of these neurotransmitters in the synaptic cleft, which can help to regulate mood and alleviate the symptoms of depression. 
• Norepinephrine Reuptake Inhibition: butriptyline, like other TCAs, has a stronger effect on the reuptake of norepinephrine compared to serotonin. This is believed to contribute to its antidepressant properties and may differentiate it from other antidepressants that primarily target serotonin reuptake. 

Spectrum of Use: 

• Depression: butriptyline is indicated for the treatment of major depressive disorders. It may be prescribed when other treatments, such as serotonin-norepinephrine reuptake inhibitors or selective serotonin reuptake inhibitors, have not been effective or are not well-tolerated. 
• Anxiety Disorders: While TCAs are not typically the first choice for anxiety disorders, some may have anxiolytic effects. However, butriptyline is primarily used for depression rather than anxiety disorders. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

tremor 

behavioral disturbances 

blood sugar changes 

Testicular enlargement 

galactorrhea 

movement disorders 

Fever  

sweating 

hypersensitivity reactions 

sexual dysfunction 

increased appetite 

Gynecomastia 

Convulsion 

dyskinesias 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with butriptyline. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with a known hypersensitivity or allergy to butriptyline or other tricyclic antidepressants (TCAs) should not use the medication. 
• Monoamine Oxidase Inhibitors (MAOIs): Concomitant use of butriptyline and monoamine oxidase inhibitors, a different class of antidepressants, is contraindicated. Concurrent use can lead to a life-threatening condition known as serotonin syndrome. 
• Recovery from Myocardial Infarction: butriptyline is contraindicated in individuals who are in the acute recovery phase following a myocardial infarction (heart attack) due to the risk of arrhythmias and other cardiovascular effects. 
• Cardiac Conduction Abnormalities: Individuals with preexisting cardiac conduction abnormalities, such as bundle branch block, should use butriptyline with caution or consider alternative treatments, as TCAs can affect heart rhythm.

Caution: 

• Elderly Patients: Elderly individuals may be more susceptible to the anticholinergic and sedative side effects of butriptyline. Lower initial doses and careful monitoring are often recommended. 
• Seizure Disorders: butriptyline can lower the seizure threshold, which may increase the risk of seizures. Caution is advised when prescribing butriptyline to individuals with a history of seizure disorders or conditions that may increase seizure risk. 
• Urinary Retention: butriptyline may exacerbate urinary retention, especially in individuals with conditions like benign prostatic hyperplasia. Monitoring for urinary symptoms and consideration of alternative treatments may be necessary. 
• Liver Impairment: Individuals with liver impairment may require dose adjustments when using butriptyline, as the medication is metabolized in the liver. 
• Renal Impairment: Patients with renal impairment may need adjustments to the dosing regimen due to potential changes in drug clearance.

Comorbidities: 

• Anxiety Disorders: Depression and anxiety often co-occur, and butriptyline may be prescribed in cases where an individual has comorbid depression and an anxiety disorder. 
• Chronic Pain: Some individuals with depression may also experience chronic pain conditions, such as neuropathic pain. butriptyline, like other tricyclic antidepressants, can be used to manage both mood and pain symptoms. 
• Psychiatric Disorders: butriptyline may be used to treat comorbid psychiatric conditions, such as bipolar disorder, schizoaffective disorder, or other mood disorders, when depression is a significant component of the clinical picture. 
• Thyroid Disorders: Thyroid disorders, including hypothyroidism, may be comorbid with depression. butriptyline’s effects on thyroid function should be considered when treating individuals with thyroid disorders. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: C 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

butriptyline is a tricyclic antidepressant (TCA) with a complex pharmacology primarily aimed at treating depression and mood disorders. Its pharmacological actions include the inhibition of reuptake of norepinephrine and serotonin in the brain. By blocking the reuptake of these neurotransmitters, butriptyline increases their levels in the synaptic cleft, facilitating improved mood regulation.

Additionally, butriptyline exhibits antagonistic effects on various receptors, including histamine and muscarinic acetylcholine receptors, which contribute to its side effect profile. These actions collectively alleviate depressive symptoms. However, its use has declined in recent years due to the introduction of newer antidepressant classes with improved side effect profiles. The pharmacological complexities of TCAs like butriptyline necessitate careful dosing and monitoring to achieve the desired therapeutic benefits while minimizing side effects.  

Pharmacodynamics: 

• Reuptake Inhibition: butriptyline, like other TCAs, primarily exerts its therapeutic effect by inhibiting the reuptake of neurotransmitters, including serotonin and norepinephrine, in the synaptic cleft. This action increases the neurotransmitters levels in the brain, enhancing their signalling and contributing to mood regulation. 
• Norepinephrine Reuptake Inhibition: butriptyline has a higher affinity for norepinephrine reuptake inhibition compared to serotonin reuptake. This strong effect on norepinephrine can contribute to its antidepressant properties and may differentiate it from other antidepressants that primarily target serotonin reuptake. 
• Serotonin Reuptake Inhibition: While butriptyline has a less pronounced effect on serotonin reuptake compared to norepinephrine, it still contributes to its antidepressant action, particularly in individuals with comorbid anxiety disorders. 
• Blockade of Certain Receptors: butriptyline may also have antagonistic effects on various receptors, including histamine and muscarinic acetylcholine receptors. These receptor actions can lead to side effects, such as sedation, weight gain, and anticholinergic effects.

Pharmacokinetics: 

Absorption 

butriptyline is typically administered orally in the form of tablets or capsules. It is well absorbed from the gastrointestinal tract after oral ingestion. 

Distribution 

butriptyline can cross the blood-brain barrier, allowing it to reach its target sites in the central nervous system, where it exerts its effects. 

Metabolism 

butriptyline undergoes hepatic (liver) metabolism primarily through a process known as demethylation. The metabolism of butriptyline involves cytochrome P450 enzymes, particularly CYP2D6 and CYP2C19, which are responsible for various drug-metabolizing reactions. 

Elimination and excretion 

The primary route of excretion for butriptyline and its metabolites is through the kidneys, where they are eliminated in the urine. Some unchanged butriptyline and its metabolites may also be excreted in feces. 

Adminstartion

Administration: 

• Dosage: The dosage of butriptyline is determined by the healthcare provider based on the individual’s specific condition, severity of symptoms, and their response to the medication. It is crucial to follow the prescribed dosage instructions carefully. 
• Oral Administration: butriptyline is usually administered orally, which means it is taken by mouth. It comes in tablet or capsule form. 
• Swallow Whole: The tablets or capsules should be swallowed whole with a glass of water and should not be crushed, broken, or chewed unless specifically instructed by the healthcare provider. 
• Duration: The duration of butriptyline treatment depends on the individual’s condition. It may be prescribed for a short-term acute episode or as a maintenance treatment for chronic conditions like depression. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: butriptyline 

Pronounced: (byoo-TRIP-ti-leen)  

Why do we use butriptyline? 

butriptyline, a tricyclic antidepressant (TCA), is primarily prescribed for the treatment of depression. butriptyline is indicated for the management of major depressive disorder (MDD) and other forms of depression. It is used to alleviate symptoms of depression, including loss of interest or pleasure, persistent sadness, fatigue, changes in appetite & sleep patterns, and feelings of worthlessness.