Butriptyline: Characteristics, Uses And Side Effects
Antidepressant drugs include a series of medications used to treat depressive symptoms and behavioral alterations associated with low mood. Within the category of antidepressants is the group of tricyclics, among which are butriptyline, a medication that differs from the rest of tricyclics due to its peculiar mechanism of action
In this article we explain what butriptyline is and what tricyclic antidepressants consist of, what is the mechanism of action of this drug, what type of side effects it causes, and what is its clinical effectiveness, compared to other similar medications.
Butriptyline is a drug from the group of tricyclic antidepressants, chemically related to amitriptyline and imipramine It is a medication that has been used in various European countries, including Spain, in the treatment of depression. Because it has a somewhat different pharmacological action than other tricyclic antidepressants, it has been described as an “atypical” or “second generation” drug.
Since its development in 1974 by Wyeth (formerly known as American Home Products), one of the largest pharmaceutical companies in the world, and its subsequent marketing in the United Kingdom, it has been dispensed very rarely compared to other antidepressant drugs in the same group. It was marketed under the brand names Evadene, Evasidol, Evadyne and Centrolese.
Although butriptyline has been considered an antidepressant drug from the tricyclic group, its mechanism of action differs significantly from prototypical tricyclics such as imipramine or amitriptyline. Next, let’s see what the mechanism of action of tricyclic antidepressants is, in order to compare them with that of butriptyline.
Tricyclic antidepressant medications are used in the treatment of depressive disorders and other behavioral pathologies, as is butriptyline. These types of drugs act as monoamine agonists Its main effects occur on serotonin receptors, norepinephrine receptors and, to a lesser extent, dopaminergic receptors.
The therapeutic activity of tricyclic antidepressants occurs by inhibiting the reuptake of these neurotransmitters, which leads to an increase in the availability of these monoamines in the synaptic cleft. However, these medications also act, although secondarily, on histamine and cholinergic receptors (related to acetylcholine), exerting an antagonistic effect on them.
The mechanism of action of tricyclics is not very specific, since Its therapeutic targets go beyond the most relevant neurotransmitter receptors, and affect another series of receptors ; This means that although they may be effective in relieving depressive symptoms, they can also cause serious side effects and adverse reactions.
Mechanism of action
In studies carried out in vitro, butriptyline has been shown to be a potent antihistamine and anticholinergic drug, with moderate antagonistic effects on the 5-HT2 serotonergic receptor and the α1 adrenergic receptor, and with a very weak or negligible action as an inhibitor of norepinephrine reuptake.
This mechanism of action seems to give this medication a profile very similar to that of the drugs iprindole and trimipramine, whose antagonistic effects on serotonin receptors could be responsible for its effectiveness in improving mood.
However, in several clinical trials using similar doses, butriptyline has been found to be equally effective as amitriptyline and imipramine in treating depressive symptoms, despite the fact that these two antidepressant drugs have a more potent effect. as 5-HT2 antagonists and as serotonin-norepinephrine reuptake inhibitors.
It has been suggested that the mechanism of action of butriptyline is different from that of other tricyclic antidepressants and that, perhaps, it works as a prodrug, converting to an active metabolite once it is introduced into the body, thus acting with a different pharmacodynamics.
Side effects
Butriptyline, as we have mentioned, It is closely linked to amitriptyline and has side effects similar to this tricyclic antidepressant However, it seems that in the case of butriptyline, the sedation caused by its consumption is lower, compared to other tricyclics, as well as the risk of interactions with other medications.
Since this drug has relatively weak effects as an α1 antagonist and virtually no effects as a norepinephrine reuptake inhibitor, it has almost none of the anti-adrenergic and adrenergic side effects.
Definitely, The most notable side effects and adverse reactions of butriptyline are related to the potent antihistamine and anticholinergic effects that produces. Below are the most common ones:
Clinical efficacy
To evaluate the effectiveness of a drug, it is usually compared with another from the same group and under appropriate experimental conditions. In this sense, in a multicenter study in which two experimental groups and a control group were randomly assigned, under double-blind conditions, the efficacy of butriptyline versus amitriptyline was compared in a group of 77 patients between 18 and 70 years old and diagnosed with primary depression.
Butriptyline and amitriptyline were administered on an identical increasing schedule, up to 150 mg daily in the first week and a flexible schedule during the last 3 weeks of the trial. The mean daily doses were 145 mg butriptyline and 142 mg amitriptyline after 2 weeks; and 77.5 mg of amitriptyline and butriptyline, after 4 weeks. Nitrazepam (a hypnotic anxiolytic drug) and haloperidol (a conventional antipsychotic drug) were also allowed (if necessary).
Symptoms and antidepressant efficacy of drugs were assessed using the following tests: the Hamilton Depression Rating Scale, the General Depression Scale, the Brief Psychiatric Rating Scale (BPRS), and the Clinical Global Impression Scale (CGI). ), as well as a checklist of side effects.
After the initial comparison of the two treatment groups, the results showed that antidepressant effects were significantly better with butriptyline with respect to the number of withdrawals, in the total score and in the following factors of the General Depression Scale: depression, guilt, anxiety, somatization and somatic complaints. Furthermore, the frequency of haloperidol prescription was significantly lower in patients who were treated with butriptyline compared to those who used amitriptyline.
The general frequency of side effects and other parameters (hematological and biochemical variables, electrocardiogram, etc.) were the same in both groups. In conclusion, it was observed that butriptyline It has the same indications as amitriptyline, but shows better antidepressant efficacy at the same dose as well as greater relief from anxiety, somatization and somatic complaints.
