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Trazodone (Desyrel) Facts
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Basic information
- Generic name: trazodone hydrochloride
- Brand/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
- Habit forming? No
- Pregnancy risk factor: C
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| Dosage |
Quantity |
Price |
Pharmacy |
| 100 mg |
30 tablets |
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| 100 mg |
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| 100 mg |
90tablets |
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| 150 mg |
30 tablets |
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| 150 mg |
60 tablets |
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| 150 mg |
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Basic information
- Generic name: trazodone hydrochloride
- Brand/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
- Habit forming? No
- Pregnancy risk factor: C
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Medical uses
Trazodone is an antidepressant medication. It was discovered
in Italy by the Angelini research laboratories.
Trazodone is a psychoactive compound with sedative, anxiolytic,
and antidepressant properties. Trazodone has less prominent anticholinergic
(dry mouth, constipation, tachycardia) and adrenolytic (hypotension,
male sexual problems) side effects than most tricyclic antidepressants.
The incidence of nausea and vomiting observed with Trazodone is
relatively low compared to SSRIs.
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Trazodone for insomnia
Trazodone is a sedating antidepressant, widely used for insomnia.
It is especially effective for the treatment of insomnia caused
by other antidepressants [1]. However, Trazodone is used for the
treatment of insomnia even in the absence of a depressive disorder.
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) sleep [11, 12].
Usually, the starting dose for insomnia is 25 mg or 50 mg at
bedtime. The dose can be increased if necessary up to 100 mg.
There is little need to increase the dose above 100 mg for this
indication. It's sleep aid effect starts within 1-2 hours and
usually lasts about 8 hours.
Important facts:
- Take trazodone with food. Total tazodone absorption 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
of about 1-1.5 hour, within which you should go to bed. If you
miss that window, you may feel very sleepy but unable fall asleep.
Trazodone may cause congested nose, feelings of tiredness and
grogginess (frequently described as hangover) on the next morning.
However it's advantage is that unlike most sleeping pills, it
is not addictive and not habit forming.
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Pharmacological characteristics
- Elimination half-life: 3-6 hours
- Metabolism: Hepatic via CYP3A4 to an active metabolite
(mCPP)
- Excretion: Primarily urine (80%); secondarily feces
(20%)
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Benefits
- Effective antidepressant in treating major depressive disorder
- Has no risk of addiction
- Has a long safety record
- Safe in overdose
- Low levels of anticholinergic effects, such as dry mouth,
blurred vision, bowel movement disturbance, and delayed urine
flow [9]
- Low cost
- Equal antidepressant efficacy with amitriptyline, imipramine,
and fluoxetine
- Increased pain threshold [5]
- Can be safely used in combination with SSRIs [8]
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Concerns
- potential for drug interactions with inducers and/or inhibitors
of CYP3A4 [7]
- risk of drug-induced priapism due to alpha-adrenergic antagonist
properties [10]
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Unlabeled uses
Whereas trazodone is not approved to treat insomnia, relatively
few studies actually support its efficacy and safety. Trazodone
may be of advantage in depressed patients with sleep difficulties.
Trazodone is effective in the treatment of antidepressant-associated
insomnia.
- Panic/Anxiety [2]
- Insomnia [1]
- Bipolar depression
- Chronic fatigue
- Fibromyalgia
- Eating disorders
- Alcohol withdrawal [3]
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Mechanism of action
Trazodone is a serotonin reuptake inhibitor and is also a 5-HT2
receptor antagonist. However, in contrast to the selective serotonin
reuptake inhibitors, trazodone's antidepressant effects may be
due to its antagonistic effect 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.
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Trazodone Discussion Boards & Forums
- Trazodone discussion: http://www.drugs.com/forum/featured-drugs/trazodone-21084.html
- Trazodone discussion: http://www.drugs.com/forum/featured-drugs/trazadone-41290.html
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References
- 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. Roccatagliata G, Albano C, Maffini M, Farelli S. Alcohol
withdrawal syndrome: treatment with trazodone. Int Pharmacopsychiatry.
1980;15(2):105-10. PubMed
- 4. Haria M, Fitton A, McTavish D. Trazodone. A review of its
pharmacology, therapeutic use in depression and therapeutic
potential in other disorders. Drugs Aging. 1994 Apr;4(4):331-55.
PubMed
- 5. Silvestrini B. Trazodone: from the mental pain to the "dys-stress"
hypothesis of depression. Clin Neuropharmacol. 1989;12 Suppl
1:S4-10. PubMed
- 6. Dossier Trazodone. 15/03/2007 . Available at: Angelini.it
- 7. Rotzinger S, Fang J, Baker GB. Trazodone is metabolized
to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug
Metab Dispos. 1998 Jun;26(6):572-5. PubMed
- 8. Prapotnik M, Waschgler R, Ko"nig P, Moll W, Conca A. Therapeutic
drug monitoring of trazodone: are there pharmacokinetic interactions
involving citalopram and fluoxetine? Int J Clin Pharmacol Ther.
2004 Feb;42(2):120-4. PubMed
- 9. Gershon S, Newton R. Lack of anticholinergic side effects
with a new antidepressent--trazodone. J Clin Psychiatry. 1980
Mar;41(3):100-4. PubMed
- 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. PubMed
- 11. Parrino L, et al. Clinical and polysomnographic effects
of trazodone CR in chronic insomnia associated with dysthymia.
Psychopharmacology (Berl) 1994;116:389-395. PubMed
- 12. Montgomery I, et al. Trazodone enhances sleep in subjective
quality but not in objective duration. Br J Clin Pharmacol 1983;16:139-144.
PubMed
- U.S. Food and Drug Administration. Trazodone U.S. Prescribing
Information. Available at (PDF format): Prescribing
Information
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Interesting Trazodone facts
- Trazodone is a triazolopyridine derivative, chemically and pharmacologically
unrelated to other currently available antidepressants.
- Trazodone is the most sedating, and least anticholinergic, of
all the currently marketed antidepressants.
- Trazodone is currently the second most commonly prescribed treatment
for insomnia because of its sedative properties, perceived lack
of risk, generic availability, and lack of duration-of-use restrictions.
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