Amitriptyline, an antidepressant medication, was first approved in 1961 and initially sold under the brand name Elavil. This tricyclic antidepressant differs from selective serotonin reuptake inhibitors (SSRIs) such as Prozac, Celexa, and Zoloft.
Amitriptyline is a tricyclic antidepressant medication with a range of uses and potential side effects.
Amitriptyline is a tricyclic antidepressant used for a variety of conditions, primarily related to nerve pain[1]Moore RA, Derry S, Aldington D, Cole P, Wiffen PJ. Amitriptyline for neuropathic pain and fibromyalgia in adults. Cochrane Database of Systematic Reviews. 2012(12)..
Although primarily an antidepressant, it has numerous off-label uses and is more often prescribed for other purposes. The World Health Organization (WHO) lists amitriptyline as an essential medicine due to its versatility in treating various conditions[.
In this article, we’ll discuss the medication’s uses, common side effects, and important precautions to consider when taking amitriptyline.
As always, the information provided here is for informational purposes only and is not intended to replace consultation, diagnosis, or medical treatment from a qualified physician or healthcare provider.
Amitriptyline sedating effects
One of the most prominent characteristics of amitriptyline is its sedating effect, which is primarily attributed to its ability to block histamine H1 receptors[2]McClure EW, Daniels RN. Classics in chemical neuroscience: Amitriptyline. ACS chemical neuroscience. 2021 Jan 13;12(3):354-62..
In addition, this medication interacts with several neurotransmitter systems, including norepinephrine and serotonin. Its sedating properties are helpful in managing insomnia or sleep disturbances associated with the aforementioned conditions[3]Lawson K. A brief review of the pharmacology of amitriptyline and clinical outcomes in treating fibromyalgia. Biomedicines. 2017 May 17;5(2):24..
However, the sedation can be significant, making it crucial for patients to take the medication at night, typically a few hours before bedtime to avoid daytime drowsiness.
Amitriptyline – sleepiness and drowsiness
The sedative effects of amitriptyline can lead to several side effects, the most common of which are sleepiness and drowsiness[4]Nakano S, Hollister LE. Chronopharmacology of amitriptyline. Clinical Pharmacology & Therapeutics. 1983 Apr;33(4):453-9..
These side effects can impact an individual’s daily functioning, as they may struggle to remain alert and focused during the day. The intensity of sleepiness and drowsiness may vary from person to person, with some individuals experiencing only mild drowsiness, while others may find it difficult to stay awake[5]Bryson HM, Wilde MI. Amitriptyline: a review of its pharmacological properties and therapeutic use in chronic pain states. Drugs & aging. 1996 Jun;8:459-76..
Moreover, these side effects can potentially interfere with tasks that require a high level of alertness, such as driving or operating machinery, posing a safety risk for both the individual and others around them.
Uses of Amitriptyline
Amitriptyline is commonly used to treat various conditions such as chronic fatigue, fibromyalgia, chronic headaches, migraine prevention, interstitial cystitis (bladder pain), irritable bowel syndrome, and general nerve pain.
The medication is often prescribed when other treatments have failed and nerve-related issues persist. The typical starting dosage ranges from 25 to 50 milligrams, with a maximum daily dosage of 300 milligrams, although most patients usually take between 50 and 100 milligrams.
| Age | Dosage |
|---|---|
| Pediatric | 2.5-5 mg once daily, increase by 5-10 mg increments not to exceed 30 mg/day |
| Adult | 25 mg once daily, may increase by 25-50 mg increments not to exceed 300 mg/day |
For other conditions, lower doses are generally prescribed. Due to its sedative properties, amitriptyline is typically taken an hour to an hour and a half before bedtime.
Off-Label Uses
- Treating depression
- Addressing anxiety
- Attention deficit hyperactivity disorder (ADHD)
- Pain
- Low back pain
- Fibromyalgia
- Chronic fatigue syndrome
- Neuropathic pain (associated with diabetes or shingles)
- Migraine prevention
- Tension headaches
- Insomnia
- Urinary urgency
- Obsessive-compulsive disorder
- Chronic cough
- Irritable bowel syndrome
- Cyclic vomiting syndrome
- Persistent itchiness
- Post-surgery dry heaves
- Biliary dyskinesia
- Nighttime bedwetting
- Early-stage Parkinson’s disease accompanied by depression
Common Side Effects of Amitriptyline
Amitriptyline is associated with several side effects, including dry mouth, blurry vision, sleepiness, constipation, weight gain, difficulty urinating, urinary retention, low blood pressure upon standing, headache, and sexual dysfunction[6]Lawson K. A brief review of the pharmacology of amitriptyline and clinical outcomes in treating fibromyalgia. Biomedicines. 2017 May 17;5(2):24..
Other common side effects include:
- Sedation: More than 10% of people using amitriptyline may experience sedation, which is why the medication is often taken at bedtime. Although sedation may persist into the morning, many patients become accustomed to this side effect over time.
- Blurred vision, confusion, and mental confusion.
- Constipation, dizziness, sexual dysfunction, weight gain, and dry mouth.
- Urinary retention.
Precautions and Cautions
- Suicidal behavior: As with all antidepressants, amitriptyline carries a risk of suicidal behavior, although this is typically less of a concern when used for pain management.
- Bipolar mania: Amitriptyline can trigger mania in individuals with bipolar disorder.
- Heart problems: The medication can affect cardiac conditions.
- Glaucoma: Certain types of glaucoma may be exacerbated by amitriptyline.
- Low blood pressure: The medication can cause low blood pressure, potentially leading to dizziness, fainting, or falls.
- Withdrawal: Amitriptyline should not be stopped abruptly, as withdrawal symptoms may occur.
- Surgery: The medication may interfere with sedation used during surgery.
- Anticholinergic effects: Amitriptyline can cause urinary retention and dry mouth.
- Seizure disorders: Caution is advised for individuals with seizure disorders.
- Diabetes: Amitriptyline can affect blood sugar levels, so those with diabetes should monitor their sugars carefully.
- Increased risk of fractures.
- Rare blood effects: Regular doctor visits and lab work are recommended for patients on amitriptyline.
Drug Interactions
Amitriptyline can interact with several other medications, including SSRIs, SNRIs, triptans, antipsychotics, cimetidine, disulfiram, anti-thyroid medications, tramadol, levodopa, and alcohol.
The drug should not be taken within six weeks of a heart attack, stroke, or severe liver disorder.
Abrupt withdrawal from amitriptyline can cause transient withdrawal symptoms, such as nausea, headache, lack of energy, restlessness, irritability, and abnormal dreams.
Overdose Risks
Overdosing on amitriptyline can be dangerous, as it accounts for a significant proportion of antidepressant-related deaths.
Symptoms of overdose include dilated pupils, drowsiness or agitation, increased reflexes, muscle rigidity, vomiting, arrhythmias, heart failure, respiratory depression, convulsions, and coma.
The risk of overdose is higher in elderly individuals, particularly those with a history of an enlarged prostate.
Conclusion
Amitriptyline is a versatile antidepressant medication with numerous off-label uses. Despite its potential side effects and precautions, it remains an essential medicine for addressing a wide range of conditions.
To ensure safety and effectiveness, it is crucial to follow the prescribed dosage and consult with a healthcare professional before starting or discontinuing the medication.
Regular monitoring and communication with a healthcare provider can help minimize risks and optimize the benefits of amitriptyline.
Additionally, it is important for patients to communicate any concerns or changes in their sleep patterns to their healthcare provider, as adjustments in dosage or timing may be necessary. In some cases, alternative medications with fewer sedating effects may be considered if the side effects of amitriptyline become intolerable or severely impact daily functioning.
MD, PhD. Physical Medicine & Rehabilitation Physician from São Paulo - Brazil. Pain Fellowship in University of São Paulo.
References
| ↑1 | Moore RA, Derry S, Aldington D, Cole P, Wiffen PJ. Amitriptyline for neuropathic pain and fibromyalgia in adults. Cochrane Database of Systematic Reviews. 2012(12). |
|---|---|
| ↑2 | McClure EW, Daniels RN. Classics in chemical neuroscience: Amitriptyline. ACS chemical neuroscience. 2021 Jan 13;12(3):354-62. |
| ↑3, ↑6 | Lawson K. A brief review of the pharmacology of amitriptyline and clinical outcomes in treating fibromyalgia. Biomedicines. 2017 May 17;5(2):24. |
| ↑4 | Nakano S, Hollister LE. Chronopharmacology of amitriptyline. Clinical Pharmacology & Therapeutics. 1983 Apr;33(4):453-9. |
| ↑5 | Bryson HM, Wilde MI. Amitriptyline: a review of its pharmacological properties and therapeutic use in chronic pain states. Drugs & aging. 1996 Jun;8:459-76. |