Trazodone HCl (Desyrel)

Trazodone hydrochloride is an antidepressant. It was discovered in Italy by the Angelini research laboratories. In the US the medicine was sold under the brand name Desyrel by Bristol-Myers Squibb. After drug's patent expiration generic version became widely available and the brand Desyrel is no longer manufactured.

Trazodone hcl has sedative, anxiolytic, and antidepressant properties. It has less prominent anticholinergic (dry mouth, constipation, increased heart rate, visual disturbances) and adrenolytic (hypotension, sexual disturbances) side effects than most tricyclic antidepressants.

The incidence of nausea and vomiting is relatively low compared to SSRIs. Unlike most new and old antidepressants, it is generally weight neutral, causing neither weight gain nor weight loss.

Trazodone is a sedating antidepressant, widely used for insomnia. It is especially effective for insomnia caused by other antidepressants1. However, Trazodone is used for the treatment of insomnia even in people without depressive symptoms. Polysomnographic studies of people with various kinds of insomnia have found that trazodone's main effect on sleep architecture is an increase in slow-wave (stages 3 and 4) sleep11,12.

When used as sleep aid, the usual starting dose is 25-50 mg of Trazodone at bedtime. The dose can be increased if necessary up to 100 mg. There is little need to increase the maximum dose for this indication. Its sleep promoting effect starts within 1-2 hours and usually lasts about 8 hours.

Important notes:

• Take trazodone with food. The absorption of the drug may be up to 20% higher when it is taken with food rather than on an empty stomach.
• Trazodone has a narrow "window" of hypnotic effect. You should go to bed within 60-90 minutes after taking it. If you miss that window, you may feel very sleepy but unable fall asleep.

Trazodone may cause feelings of tiredness and grogginess ("hangover") on the next morning. However its advantage is that unlike most sleeping pills, it is not addictive and not habit forming.

• Elimination half-life: 3-6 hours
• Metabolism: Hepatic via CYP3A4 to an active metabolite (mCPP)
• Excretion: Primarily urine (80%); secondarily feces (20%)

• Effective antidepressant in treating major depressive disorder.
• Has no risk of addiction and dependence.
• Has a long safety record, and is relatively safe in overdose.
• Low risk of anticholinergic effects, such as dry mouth, blurred vision, bowel movement disturbance, and delayed urine flow9.
• Low cost - trazodone is one of the most inexpensive antidepressants for people without insurance.
• Equal antidepressant efficacy with amitriptyline, imipramine, and fluoxetine
• Can be safely used in combination with SSRIs8.

• Potential for drug interactions with inducers and/or inhibitors of CYP3A47.
• Risk of drug-induced priapism due to alpha-adrenergic antagonist properties10.

Whereas trazodone is not approved to treat insomnia, relatively few studies actually support its efficacy and safety. The medicine may be of advantage in depressed people with sleep difficulties. Trazodone is effective in the treatment of insomnia caused by other drugs.

• Panic, anxiety2
• Insomnia1
• Bipolar depression
• Chronic fatigue
• Eating disorders
• Alcohol withdrawal

Trazodone is a serotonin reuptake inhibitor and is also a 5-HT2 receptor antagonist. However, in contrast to the SSRIs, trazodone's antidepressant effects may be due to its antagonistic action at the 5-HT2 receptor site. It causes adrenoreceptor subsensitivity, and induces significant changes in 5-HT presynaptic receptor adrenoreceptors. This agent also blocks histamine (H1) and alpha1-adrenergic receptors.

• Trazodone Ratings on DrugLib.com
• Desyrel Reviews on Psych Central
• Trazodone User Success Rate Reviews on DailyStrength.org
• User Reviews for Trazodone on Drugs.com
• Trazodone User Ratings - on WebMD

• 1. Nierenberg AA, Adler LA, Peselow E, Zornberg G, Rosenthal M. Trazodone for antidepressant-associated insomnia. Am J Psychiatry. 1994 Jul;151(7):1069-72.
• 2. Mavissakalian M, Perel J, Bowler K, Dealy R. Trazodone in the treatment of panic disorder and agoraphobia with panic attacks. Am J Psychiatry. 1987 Jun;144(6):785-7.
• 4. Haria M, Fitton A, McTavish D. Trazodone. A review of its pharmacology, therapeutic use in depression and therapeutic potential in other disorders. 1994 Apr;4(4):331-55. PubMed
• 6. Dossier Trazodone. 15/03/2007: Angelini.it
• 7. Rotzinger S, Fang J, Baker GB. Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug Metabolism Disposition 1998 Jun;26(6):572-5.
• 8. Prapotnik M, Waschgler R, Konig P, Moll W, Conca A. Are there pharmacokinetic interactions involving trazodone and SSRIs? Int J Clin Pharmacol Ther. 2004 Feb;42(2):120-4.
• 9. Gershon S, Newton R. Lack of anticholinergic side effects with trazodone. J Clin Psychiatry. 1980 Mar.
• 10. Abber JC, Lue TF, Luo JA, Juenemann KP, Tanagho EA. Priapism induced by chlorpromazine and trazodone: mechanism of action. J Urol. 1987 May;137(5):1039-42.
• 11. Parrino L, et al. Trazodone in chronic insomnia associated with dysthymia: polysomnographic variables and sleep quality. Psychopharmacology 1994;116:389-395.
• 12. Montgomery I, et al. Trazodone enhances sleep in subjective quality but not in objective duration. Br J Clin Pharmacol 1983;16:139-144. PubMedCentral

Written for HealthyStock.net, October 2009.
Last modified: August, 2011