Trazodone: Restore Restful Sleep and Mood Balance
| Product dosage: 100mg | |||
|---|---|---|---|
| Package (num) | Per pill | Price | Buy |
| 60 | $0.88 | $53.06 (0%) | 🛒 Add to cart |
| 90 | $0.81 | $79.59 $73.08 (8%) | 🛒 Add to cart |
| 120 | $0.78 | $106.12 $93.10 (12%) | 🛒 Add to cart |
| 180 | $0.75 | $159.18 $134.15 (16%) | 🛒 Add to cart |
| 270 | $0.72 | $238.77 $194.22 (19%) | 🛒 Add to cart |
| 360 | $0.71
Best per pill | $318.36 $254.28 (20%) | 🛒 Add to cart |
Synonyms | |||
Trazodone hydrochloride is a prescription medication belonging to the class of serotonin antagonist and reuptake inhibitors (SARIs), primarily indicated for the treatment of major depressive disorder (MDD). While its antidepressant efficacy is well-established, its pronounced sedative properties have made it a widely utilized agent in the management of insomnia, particularly when a sleep disturbance coexists with depressive or anxiety symptoms. Its unique pharmacological profile offers a distinct alternative to traditional hypnotics, balancing therapeutic effect with a generally favorable side effect and safety spectrum. This makes it a versatile tool in the psychiatric and neurological armamentarium for improving both nocturnal rest and daytime functioning.
Features
- Active Pharmaceutical Ingredient: Trazodone Hydrochloride
- Standard Available Strengths: 50 mg, 100 mg, 150 mg, and 300 mg oral tablets
- Pharmacologic Class: Serotonin Antagonist and Reuptake Inhibitor (SARI)
- Mechanism of Action: Primarily acts as a potent antagonist of the 5-HT2A serotonin receptor and a inhibitor of the serotonin transporter (SERT)
- Bioavailability: Approximately 65-80% when administered orally with food
- Half-life: Biphasic; initial phase is 3-6 hours, secondary phase is 5-9 hours
- Time to Peak Plasma Concentration (Tmax): Roughly 1-2 hours post-ingestion when taken on an empty stomach; delayed with food
- Metabolism: Extensively hepatically metabolized via cytochrome P450, primarily CYP3A4, to an active metabolite, meta-chlorophenylpiperazine (mCPP)
- Excretion: Predominantly renal (70-75%) with the remainder excreted in feces
Benefits
- Promotes the initiation and maintenance of sleep by blocking wakefulness-promoting 5-HT2A receptors, leading to improved sleep architecture with increased restorative slow-wave sleep.
- Alleviates core symptoms of major depression, including low mood, anhedonia, and psychomotor agitation, by enhancing serotonergic neurotransmission.
- Offers a non-habit-forming alternative to benzodiazepines and Z-drugs (e.g., zolpidem) for chronic insomnia management, mitigating concerns regarding tolerance and dependence.
- Demonstrates anxiolytic (anti-anxiety) effects, making it particularly beneficial for patients with depression or insomnia comorbid with anxiety disorders.
- Lacks significant anticholinergic side effects common to many older tricyclic antidepressants, resulting in a lower incidence of dry mouth, constipation, and urinary retention.
- Provides a flexible dosing regimen, allowing clinicians to tailor treatment based on the primary indication (e.g., lower doses for sleep, higher doses for depression).
Common use
Trazodone is FDA-approved for the treatment of major depressive disorder (MDD). In clinical practice, its use has expanded significantly for the treatment of insomnia, both as a primary condition and when it is secondary to other psychiatric or medical disorders. It is considered a first-line pharmacological option for chronic insomnia by many sleep specialists and is frequently used off-label for this purpose. It is also employed in the management of anxiety disorders, such as generalized anxiety disorder (GAD), and for mitigating sleep disturbances associated with substance withdrawal syndromes. Its efficacy in treating agitation and sleep problems in patients with dementia is also a common, though off-label, application.
Dosage and direction
For Depression: The initial adult dose is typically 150 mg per day in divided doses. The dose may be increased by 50 mg per day every three to four days. The maximum dose for outpatients usually should not exceed 400 mg per day in divided doses. In hospitalized patients, doses of up to 600 mg per day may be used. For Insomnia (Off-label): The dose for sleep is significantly lower, usually initiating at 25 mg to 50 mg taken orally 30 minutes before bedtime. This dose can be titrated upward based on efficacy and tolerability, rarely exceeding 100-150 mg for sleep induction. Administration: Should be taken shortly after a meal or light snack to minimize the potential for dizziness and lightheadedness and to increase its relative bioavailability. Tablets should be swallowed whole and not crushed, chewed, or split unless advised by a physician or pharmacist.
Precautions
- Suicidality: Antidepressants may increase the risk of suicidal thinking and behavior in children, adolescents, and young adults. Patients of all ages started on therapy should be monitored closely for clinical worsening, suicidality, or unusual changes in behavior.
- Serotonin Syndrome: There is a potential for developing a life-threatening serotonin syndrome, especially with concomitant use of other serotonergic drugs. Symptoms include agitation, hallucinations, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, nausea, and diarrhea.
- Priapism: Although rare, trazodone has been associated with priapism (prolonged and painful penile erection unrelated to sexual stimulation). This is a medical emergency requiring immediate treatment to avoid permanent erectile dysfunction. Patients should be advised to discontinue the drug and seek immediate medical attention if such an erection occurs.
- Cardiovascular Effects: Use with caution in patients with pre-existing cardiac disease, as trazodone has been associated with arrhythmias, including ventricular tachycardia. It can cause orthostatic hypotension.
- Activation of Mania/Hypomania: May precipitate a manic or hypomanic episode in patients with bipolar disorder. It should generally not be used without a concomitant mood-stabilizing agent in such patients.
- Cognitive/Motor Impairment: May cause drowsiness, sedation, and impaired cognitive and motor performance. Patients should be cautioned about operating hazardous machinery, including automobiles, until they are reasonably certain that trazodone does not adversely affect their performance.
- Discontinuation Syndrome: Abrupt discontinuation after prolonged use may lead to symptoms such as anxiety, agitation, and sleep disturbance. A gradual taper is recommended.
Contraindications
- Known hypersensitivity to trazodone hydrochloride or any components of the formulation.
- Concomitant use, or use within 14 days of discontinuing, monoamine oxidase inhibitors (MAOIs) due to the risk of serious, sometimes fatal, drug interactions characterized by hyperthermia, rigidity, myoclonus, and extreme agitation progressing to delirium and coma.
- Patients in the acute recovery phase after a myocardial infarction.
Possible side effect
Common side effects (≥5%) include:
- Sedation/Somnolence
- Dizziness/Lightheadedness
- Headache
- Dry Mouth
- Nausea
- Constipation
- Blurred Vision
Less common but serious side effects include:
- Priapism
- Serotonin Syndrome
- Suicidal Ideation and Behavior
- Orthostatic Hypotension and Syncope
- Cardiac Arrhythmias (e.g., ventricular premature beats, tachycardia)
- Hyponatremia (low sodium levels)
- Extrapyramidal Symptoms (rare)
Drug interaction
- Monoamine Oxidase Inhibitors (MAOIs): Contraindicated due to risk of serotonin syndrome and hypertensive crisis.
- Other CNS Depressants: Alcohol, benzodiazepines, opioids, other sedating antidepressants, and antipsychotics can potentiate sedation and cognitive/motor impairment.
- Strong CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir, clarithromycin): May significantly increase trazodone plasma levels, increasing the risk of adverse effects, including QT prolongation and sedation.
- Strong CYP3A4 Inducers (e.g., rifampin, carbamazepine, St. John’s Wort): May decrease trazodone plasma levels, potentially reducing its efficacy.
- Other Serotonergic Drugs: Concomitant use with SSRIs (e.g., fluoxetine), SNRIs, triptans, tramadol, and linezolid increases the risk of serotonin syndrome.
- Digoxin and Phenytoin: Trazodone may increase serum levels of these drugs.
- Antihypertensives: May potentiate the effects of antihypertensive drugs, increasing the risk of hypotension.
- Warfarin: May increase prothrombin time (PT); close monitoring of INR is recommended.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is close to the time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. Do not double the dose to make up for a missed one. For patients taking a single bedtime dose for insomnia, a missed dose should simply be skipped.
Overdose
Overdose of trazodone can be serious and potentially fatal. Predominant symptoms are an extension of its pharmacological effects and include excessive sedation, drowsiness, vomiting, priapism, respiratory depression, seizures, and cardiac arrhythmias. There is no specific antidote. Management involves securing the airway and providing supportive and symptomatic care. Gastric lavage may be considered if presentation is early. Forced diuresis is unlikely to be beneficial. ECG monitoring is essential due to the risk of arrhythmias.
Storage
Store at controlled room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Dispense in a tight, light-resistant container as defined in the USP. Keep out of reach of children and pets. Do not use after the expiration date printed on the bottle.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author and publisher are not responsible for any specific health or allergy needs that may require medical supervision and are not liable for any damages or negative consequences from any treatment, action, application, or preparation, to any person reading or following the information in this document.
Reviews
“Trazodone has been a cornerstone in my practice for treating insomnia comorbid with depression and anxiety. Its efficacy in restoring sleep architecture without the dependency profile of benzodiazepines is its greatest asset. Patient tolerance is generally good, with sedation being the most common, yet often desired, side effect at lower doses.” – Psychiatrist, 15 years experience
“As a sleep medicine specialist, I find low-dose trazodone to be an effective and well-tolerated option for chronic primary insomnia. It significantly improves sleep onset and maintenance for many of my patients. Monitoring for rare but serious side effects like priapism is a critical part of the prescribing process.” – Neurologist, Sleep Medicine Certified
“From a clinical pharmacology standpoint, trazodone’s dual action as a 5-HT2A antagonist and SERT inhibitor provides a unique mechanism that distinguishes it from SSRIs and typical hypnotics. This makes it a valuable tool, though its active metabolite and complex drug interaction profile require careful patient selection and monitoring.” – Clinical Pharmacologist