Trazodone ( Desyrel , Beneficat , Deprax , Desirel , Molipaxin , Thombran , Trazorel , Trialodine , Trittico ) is a psychoactive drug of the piperazine and triazolopyridine chemical classes that has antidepressant, anxiolytic, and hypnotic properties. It has been advertised that its therapeutic benefits become noticeable within the first week of administration. Trazodone has considerably less prominent anticholinergic (dry mouth, constipation, tachycardia) and sympatholytic (hypotension, sexual dysfunction consisting of erectile dysfunction and anorgasmia) side effects in comparison to most of the tricyclic antidepressants (TCAs) and tetracyclic antidepressants (TeCAs).
History
Trazodone was originally discovered and developed in Italy in the 1960s by Angelini research laboratories as a second-generation antidepressant. It was developed according to the mental pain hypothesis, which was postulated from studying patients and which proposes that major depression is associated with a decreased pain threshold. Trazodone was patented and marketed in many countries all over the world. It was approved by the Food and Drug Administration (FDA) at the end of 1981. It is closely related to nefazodone (Serzone).
Indications
- Clinical depression with or without anxiety.
- Insomnia. (in some countries, this is an off-label use)
- Fibromyalgia, to aid in sleeping.
- Control of nightmares or other sleep disturbances.
Off-label and Investigational Uses
- Panic disorder.
- Diabetic neuropathy.
- Bulimia nervosa.
- Obsessive-compulsive disorder (OCD).
- Alcohol withdrawal.
- Schizophrenia and other psychoses.
Antidepressant Augmentation
Trazodone is often used in conjunction with selective serotonin reuptake inhibitors (SSRIs), like fluoxetine (Prozac) and has been noted to help with the anxiety that can result from beginning treatment with such antidepressants. Trazodone has been prescribed to children as an aid to other antidepressants as well.
Pharmacology
Trazodone inhibits the reuptake of serotonin, but possesses a far lower affinity for the serotonin transporter (SERT) than drugs in the selective serotonin reuptake inhibitor (SSRI) class, such as fluoxetine (Prozac) and citalopram (Celexa). Trazodone's anxiolytic and antidepressant effects may be due to its antagonistic effects at the 5-HT 2A and 5-HT 2C receptors. Its sedative-hypnotic effects may stem from its strong antagonistic activity at the 5-HT 2A and alpha-1 adrenergic receptor in addition to its moderate antagonistic activity at the H 1 receptor.
Pharmacokinetics
Trazodone is well absorbed after oral administration with mean peak blood levels obtained at approximately 1 hour after ingestion. Absorption is somewhat delayed and enhanced by food. The mean blood elimination half-life is biphasic: the first phase's half-life is 3–6 hours, and the following phase's half-life is 5–9 hours. The drug is extensively metabolized with 3 or 4 major metabolites having been identified in the human body, some of which such as mCPP may contribute to the side effect profile of trazodone. mCCP has been shown to activate numerous serotonin receptors, including 5ht2c. Due to the short half-life of trazodone, if a dose is taken at night, mCCP would be present in the body during the following day, causing symptoms such as anorexia (behavioral symptoms), anxiety, hypolocomotion, headache, and depression. Approximately 70–75% of 14 C-labelled trazodone was found to be excreted in the urine within 72 hours. Trazodone is highly protein-bound.
Warnings
- If the patient has a known hypersensitivity to trazodone.
- If the patient is under 18 years of age and combines with other antidepressant medications it may greatly increase the possibility of suicidal thoughts or actions.
Precautions
Trazodone is metabolised by CYP3A4, a liver enzyme. Inhibition of this enzyme by various other substances may delay its degradation, leading to high blood levels of trazodone. CYP3A4 may be inhibited by many other medications, herbs, and foods, and as such, trazodone may interact with these substances. One drug-food interaction is grapefruit juice. Drinking grapefruit juice is discouraged in patients taking trazodone. One glass of grapefruit juice occasionally is not likely to have this effect on most people, but drinking large amounts, or drinking it regularly is proven to affect trazodone's clearance.
The possibility of suicide in depressed patients remains during treatment and until significant remission occurs. Therefore, the number of tablets prescribed at any one time should take into account this possibility, and patients with suicidal ideation should never have access to large quantities of trazodone.
Trazodone has been reported to cause seizures in a small number of patients who took it concurrently with other anti seizure medications.
While trazodone is not a true member of the SSRI class of antidepressants, it does still share many properties of the SSRIs, especially the possibility of discontinuation syndrome if the medication is stopped too quickly. Care must therefore be taken when coming off the medication, usually by a gradual process of tapering down the dose over a period of time.
A person who abruptly stops taking trazodone, even in doses as low as 25 mg (common for use as a sleep aid for people with anxiety disorders), may experience adverse mental reactions such as emotional instability, depressed mood, and suicidal thoughts. Although such warnings may be included in printed materials supplied with the drug, physicians prescribing trazodone, particularly those who are not psychiatrists, might not give oral warnings.
Pregnancy and Lactation
- Pregnancy: Sufficient data in humans is lacking. Use should be justified by the severity of the condition to be treated.
- Lactation: Sufficient data in humans is also lacking. Additionally, trazodone may be found in the maternal milk in significant concentrations. Women should not breastfeed while taking trazodone.
Side Effects
The most common adverse reactions encountered are drowsiness, nausea/vomiting, headache and dry mouth. Adverse reactions reported include the following:
Behavioral
Drowsiness, fatigue, lethargy, psychomotor retardation, lightheadedness, dizziness, difficulty in concentration, confusion, uncontrollable laughter, sex drive decrease.
Neurological
Tremor, headache, ataxia, migraine, akathisia, muscle stiffness, slurred speech, slowed speech, vertigo, tinnitus, tingling of extremities, paresthesia, weakness, complex partial seizures, and rarely, impaired speech, muscle twitching, numbness, dystonia, euphoria, and involuntary movements.
Autonomic
Dry or numb mouth, blurred vision, priapism, diplopia, miosis, nasal congestion, constipation, sweating, urinary retention, increased urinary frequency and incontinence.
Cardiovascular
Hypotension, tachycardia, palpitations, shortness of breath, apnea, syncope, arrhythmias, prolonged P-R interval, atrial fibrillation, bradycardia, ventricular ectopic activity (including ventricular tachycardia), myocardial infarction, and cardiac arrest.
Rare Side Effects
Recent clinical studies in patients with pre-existing cardiac disease indicate that trazodone may be arrhythmogenic in some patients in that population. Arrhythmias identified include isolated PVC's, ventricular couplets, and in 2 patients short episodes (3 to 4 beats) of ventricular tachycardia. There have also been several post-marketing reports of arrhythmias in trazodone-treated patients who have pre-existing cardiac disease and in some patients who did not have pre-existing cardiac disease. Until the results of prospective studies are available, patients with pre-existing cardiac disease should be closely monitored, particularly for cardiac arrhythmias. Trazodone is not recommended for use during the initial recovery phase of myocardial infarction.
Priapism
Trazodone has rarely been associated with the occurrence of priapism. In approximately 33% of the cases reported, surgical intervention was required and, in a portion of these cases, permanent impairment of erectile function or impotence resulted.
Priapism is a potentially harmful medical condition in which the erect penis does not return to its flaccid state (despite the absence of both physical and psychological stimulation) within about four hours. It is often painful. Male patients with prolonged or inappropriate erections should immediately discontinue the drug and consult their physician. If the condition persists for more than 24 hours, it would be advisable for the treating physician to consult a urologist or appropriate specialist in order to decide on a management approach.
In women, a similar condition of persistent arousal can be caused and is called persistent genital arousal disorder.
Gastrointestinal
Nausea, vomiting, diarrhea, gastrointestinal discomfort, anorexia,
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