Trazodone HCl (Desyrel)
- Generic name: Trazodone hydrochloride
- Trade names: Desyrel, Trazon, Trialodine
- Dosages: Tablets 50 mg, 100 mg, 150 mg
- Pharmacologic category: antidepressant, triazolopyridine
derivative, 5-HT(2) antagonist and 5-HT reuptake inhibitor
- FDA approved: December 24, 1981
- Pregnancy risk factor: C
What is Trazodone?
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 100 mg
Trazodone for sleep
Trazodone is a sedating antidepressant, widely used to treat insomnia. It is especially effective for insomnia caused
by other antidepressants1. However, Trazodone is used for the
treatment of sleep difficulties 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 deep slow-wave (stages 3 and 4) sleep11,12, which is is important to restorative rest.
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.
- 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.
Trazodone and Sleep Apnea
Trazodone may reduce apnea severity in some people with obstructive sleep apnoea (with a mildly compromised upper airway)3. It has been shown to increases the arousal threshold and to be a stimulant of upper airway muscle activity.
- 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.
- 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
- 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
- Risk of drug-induced priapism due to alpha-adrenergic antagonist
Whereas trazodone is not FDA-approved to treat insomnia, several clinical studies and practical experience support its
efficacy and safety. This medicine may be of advantage in depressed people
with sleep difficulties and for treating insomnia caused by other drugs.
- Panic, anxiety2
- Bipolar depression
- Chronic fatigue
- Eating disorders
- Alcohol withdrawal
- Antidepressant-induced sexual dysfunction
Mechanism of action
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.
User Reviews & Discussions
- 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. PubMed
- 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. PubMed
- 3. Heinzer RC, White DP, Jordan AS, Lo YL, Dover L, Stevenson K, Malhotra A. Trazodone increases arousal threshold in obstructive sleep apnoea. Eur Respir J. 2008 Jun;31(6):1308-12 PubMed
- 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.
- 5. Mendelson WB. A review of the evidence for the efficacy and safety of trazodone in insomnia. J Clin Psychiatry. 2005 Apr;66(4):469-76. 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.
Written for HealthyStock.net, October 2009.
Last modified: May, 2013
- Trazodone hydrochloride, a triazolopyridine derivative, is the most sedating, and least anticholinergic, of
all the currently available antidepressants.
- Lately, trazodone is the second most commonly prescribed treatment
for insomnia5 because of its effectiveness, sedative properties, perceived lack
of hazards and serious problems, generic availability, and lack of restrictions for long-term use.