How trazodone works
The active ingredient trazodone interferes with the brain’s neurotransmitter metabolism:
The nerve cells (neurons) in the brain communicate with each other with the help of various messenger substances (neurotransmitters). A cell can release a specific messenger substance, which then binds to specific docking sites (receptors) on the target cell and thus transmits a signal. To terminate the signal, the messenger is eventually reabsorbed into the cell of origin.
A deficiency or excess of neurotransmitters in the brain can lead to various brain-organic diseases. According to experts, serotonin, which is known as the “happiness hormone,” can lead to depression if there is a deficiency and to delusions and schizophrenia if there is an excess, for example.
Antidepressants such as trazodone inhibit the reuptake of the neurotransmitter serotonin into the cells of origin and are therefore also called serotonin reuptake inhibitors. By inhibiting reuptake, the neurotransmitter remains longer between the nerve cells and can thus act for longer. This compensates for a deficiency.
Other receptor subtypes blocked by trazadone include alpha and histamine receptors.
Absorption, degradation and excretion
After ingestion, the drug is rapidly and completely absorbed in the intestine. The highest blood levels are reached after half an hour to one hour.
After its breakdown in the liver, three-quarters of the drug is excreted in the urine by the kidneys. Five to eight hours after ingestion, about half of the ingested dose of trazodone has left the body.
When is trazodone used?
The active ingredient trazodone is used to treat depressive disorders. Because of its calming effect, it is prescribed especially for depression associated with anxiety disorders, sleep disorders, and post-traumatic stress disorder.
How trazodone is used
The antidepressant trazodone is taken in the form of tablets. Treatment is started gradually, i.e., by slowly increasing the trazodone dosage.
Usually, it is started with 100 milligrams per day. After one week, the dosage can be increased by 100 milligrams up to a maximum dose of 400 milligrams per day.
Therapy with trazodone should be discontinued gradually, i.e. by slowly reducing the dose.
The sedative effect of trazodone sets in immediately after the start of therapy, but the mood-lifting effect only after up to three weeks.
What are the side effects of trazodone?
One in ten to one hundred patients experience trazodone side effects such as drowsiness, dry mouth, and low blood pressure.
In one in one hundred to one thousand people treated, trazodone triggers weight gain or tremor.
What should I be aware of when taking trazodone?
Contraindications
Trazodone should not be taken by:
- acute myocardial infarction
- @ concomitant use of monoamine oxidase inhibitors (MAO inhibitors – also antidepressants)
- @ carcinoid syndrome (group of symptoms caused by certain hormone-producing tumors)
Drug interactions
The concomitant use of agents that are broken down by the same liver enzymes as trazodone may interfere with its breakdown, resulting in increased levels of trazodone in the body. Examples of such agents include antibiotics (for example, erythromycin, clarithromycin), antifungal agents (ketoconazole, itraconazole), and HIV medications containing the active ingredient ritonavir.
Agents that increase the concentration of serotonin in the brain should not be combined with trazodone, otherwise life-threatening serotonin syndrome may occur (with rapid heartbeat, increase in blood pressure, fever, nausea, vomiting, etc.). Such agents are, for example, antidepressants of the MAO inhibitor type (such as moclobemide or tranylcypromine), other antidepressants, St. John’s wort preparations, migraine drugs (such as sumatriptan and naratriptan), strong painkillers (opioids such as tramadol, fentanyl and pethidine) and serotonin precursors such as tryptophan and 5-hydroxytryptophan (5-HTP).
Trazodone affects the so-called QT interval – a certain section of the ECG. Therefore, it should not be taken with other drugs that also prolong the QT interval.
Patients taking anticoagulants from the group of vitamin K antagonists (such as phenprocoumon and warfarin) should monitor their coagulation status particularly closely during trazodone therapy.
Age Restrictions
Trazodone is contraindicated in pediatric and adolescent patients younger than 18 years of age. In elderly patients and patients with hepatic impairment, the trazodone dose must be adjusted accordingly.
Pregnancy and lactation
Limited data are available on the use of trazodone during pregnancy. Therefore, it should not be used during this period.
Studies on the transfer of trazodone into breast milk are only available after single doses. In these cases, only a very small proportion passed into breast milk. Breastfed infants should still be monitored closely to be on the safe side if the mother is taking trazodone.
How to obtain medication with trazodone
How long has trazodone been known?
The antidepressant was developed in Italy in the 1960s as a second-generation agent (with improved properties). It was first approved in the U.S. in 1981, then in many European countries from 1985.
Since patent protection expired, many inexpensive generics containing the active ingredient trazodone have come onto the market.
