Amitriptyline
Updated onBenjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.
More about the experts All content is checked by medical journalists.Amitriptyline is one of the most well-known active ingredients for depression and chronic pain. It is used very often in the field of psychiatry and neurology. Amitriptyline is one of the tricyclic antidepressants and therefore belongs to the first generation of antidepressant agents. It has been well studied and tested for tolerance. Here you can read everything you need to know about the effects of amitriptyline, side effects and use.
This is how amitriptyline works
Amitriptyline is a drug from the group of so-called tricyclic antidepressants. It has a mood-enhancing, anxiety-relieving and calming effect. Amitriptyline also alleviates pain intensity in nerve pain (neuropathic pain) and reduces the frequency of chronic tension headaches and migraines.
Amitriptyline develops these effects by influencing the sensitive balance of messenger substances (neurotransmitters) in the brain. These messenger substances transmit nerve signals between the individual brain cells:
The signals are generated by the release of a messenger substance from one nerve cell and its docking to certain binding sites (receptors) on the next nerve cell. After they have developed their effect, the messenger substances are taken up again by the original cell and thus "recycled".
Experts currently assume that the development of depression is due, among other things, to a lack of certain messenger substances in the brain (e.g. serotonin and norepinephrine). This is where tricyclic antidepressants (TCAs) such as amitriptyline come into play: They prevent the re-absorption of the messenger substances in the original cell so that they can develop their effect longer.
As a TCA, amitriptyline inhibits the re-uptake of various messenger substances only slightly selectively. It blocks the reuptake of serotonin and norepinephrine and also binds to numerous other receptors of the most diverse signaling pathways in the brain.
This spectrum of activity is different for almost every antidepressant, which means that numerous mental illnesses with a wide variety of facets can be treated.
The mood-enhancing effects of amitriptyline usually set in after two to three weeks of regular use. At the beginning of the therapy, the calming (sedative) effect is particularly noticeable, which at the same time can alleviate existing sleep problems.
Uptake, breakdown and excretion
The active substance amitriptyline is only slowly absorbed into the blood (over a period of one to five hours). The breakdown takes place in the liver, whereby the breakdown product also has an antidepressant effect.
After its metabolism, amitriptyline is excreted via the kidneys. It takes about 25 hours (half-life) for the body to break down and excrete half of the active ingredient.
When is amitriptyline used?
The active ingredient amitriptyline is approved for the treatment of:
- depressive illnesses
- neuropathic pain
- chronic tension headaches and migraines (for prophylaxis)
- Enuresis nocturna ("bed-wetting")
Outside of the approved indications, amitriptyline is also used for the following complaints (so-called "off-label use"):
- Attention Deficit (Hyperactivity) Syndrome, or ADD for short
- eating disorder
- Tinnitus
- Fibromyalgia
The application usually takes place over a longer period of time.
This is how amitriptyline is used
The active ingredient amitriptyline is mostly used in the form of tablets, sometimes with delayed release of the active ingredient. There are also amitriptyline drops and injection solutions on the German market.
The tablets are usually given over the day (morning - noon - evening). In the case of low amitriptyline doses or delayed release of active ingredients, it is usually taken in the evening, as fatigue can occur, especially at the beginning of therapy.
The dosage depends on the area of application. It is often chosen lower for neuropathic pain than for depression.
What are the side effects of amitriptyline?
Weight gain occurs in more than one in ten people treated and is therefore a very common side effect of therapy with amitriptyline. In addition, aggression, dizziness, drowsiness, increased heart rate, low blood pressure, nasal congestion, dry mouth, increased sweating, urinary retention and fatigue - especially at the beginning of treatment with amitriptyline.
The effect and side effects occur at different times. Initially, the side effects predominate. These usually subside after one to two weeks, and the actual antidepressant effect comes into play.
What should be considered when taking amitriptyline?
Contraindications
Amitriptyline should not be used for:
- Diseases of the heart
- severe liver dysfunction
- simultaneous treatment with monoamine oxidase inhibitors (MAO inhibitors - against depression and Parkinson's disease)
- Hypersensitivity to the active ingredient
Interactions
Amitriptyline may increase the effects of adrenaline, ephedrine, and phenylephrine (sympathomimetics) on the heart. Furthermore, it increases the effect of centrally acting antihypertensive agents (e.g. clonidine, methyldopa) and anticholinergics (e.g. tolterodine, oxybutynin).
Amitriptyline is broken down in the liver by certain enzymes, so taking inhibitors of these enzymes at the same time can lead to increased amitriptyline side effects. Such inhibitors are, for example, antifungal agents such as fluconazole and terbinafine, but also other antidepressants such as fluoxetine, paroxetine and bupropion.
The combination of amitriptyline with fluvoxamine (antidepressant) and tramadol (pain reliever) should be avoided. Other central depressant drugs (e.g. benzodiazepines) and alcohol increase the sedative effect of amitriptyline. As a result, the ability to drive and use machines can be significantly impaired.
Age restriction
Amitriptyline should not be used to treat depression in children and adolescents under 18 years of age due to a lack of studies on its effectiveness.
However, the active ingredient is approved for the treatment of nocturnal enuresis from the age of six if other measures have not led to the desired success.
pregnancy and breast feeding period
The active ingredient group of tricyclic antidepressants has been available for more than 60 years. Accordingly, a lot of experience is available on the effects and side effects - also during pregnancy and breastfeeding.
Studies with a total of around 1400 evaluated pregnancy courses have not provided any evidence of a teratogenic effect of amitriptyline. The active ingredient is therefore one of the antidepressants of choice for treatment-dependent depression during pregnancy.
Less extensive data on the use of amitriptyline are available for breastfeeding. So far, no complaints have been described in breastfed children. Amitriptyline is therefore one of the antidepressants of choice during breastfeeding if drug therapy is indicated.
How to get drugs with amitriptyline
In Germany, Austria and Switzerland, preparations containing the active ingredient amitriptyline require a prescription in every dosage and form of administration and can only be obtained from pharmacies.
Drops containing amitriptyline are only available in Germany, but not in Austria or Switzerland.
How long has amitriptyline been known?
The first representatives of the tricyclic antidepressants were developed in the early 1950s (later more and more descendants were added):
Imipramine was the first tricyclic antidepressant to be discovered and tested for the first time in 1955. As the second member of the tricyclic antidepressants, amitriptyline was introduced in the United States in 1961. Since then, it has been one of the most frequently prescribed antidepressants worldwide and is also used with success in many other areas of application.
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