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Trazodone (Desyrel) Prescription
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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
- Pregnancy risk factor: C
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What is Trazodone?
Trazodone hydrochloride is a prescription antidepressant medication. It was discovered
in Italy by the Angelini research laboratories. In the US the drug was sold under the brand name Desyrel by Bristol-Myers Squibb. After drug's patent expiration generic version of Trazodone became widely available and the brand Desyrel is no longer manufactured.
Trazodone hcl is a medicine with sedative, anxiolytic,
and antidepressant properties. It has less prominent anticholinergic
(dry mouth, constipation, increased heart rate, visual disturbances) and adrenolytic (hypotension,
sexual problems) side effects than most tricyclic antidepressants.
The incidence of nausea and vomiting observed with Trazodone is
relatively low compared to SSRIs. Unlike most new and old antidepressants, it is generally weight neutral, causing neither weight gain nor weight loss. |
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Trazodone for insomnia
Trazodone is a sedating antidepressant, widely used for insomnia.
It is especially effective prescription for the treatment of 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 mg or 50 mg of Trazodone 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. Its sleep promoting effect starts within 1-2 hours and
usually lasts about 8 hours.
Important facts:
- Take the medication 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 the medication. 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. |
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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 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
- Increased pain threshold5.
- Can be safely used in combination with SSRIs8.
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Concerns
- Potential for drug interactions with inducers and/or inhibitors
of CYP3A47.
- Risk of drug-induced priapism due to alpha-adrenergic antagonist
properties10.
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Unlabeled uses
Whereas trazodone is not approved to treat insomnia, relatively
few studies actually support its efficacy and safety. The medication may be of advantage in depressed people with sleep difficulties.
Trazodone is effective in the treatment of
insomnia caused by use of other prescription medications.
- Panic, anxiety2
- Insomnia1
- Bipolar depression
- Chronic fatigue
- Fibromyalgia
- Eating disorders
- Alcohol withdrawal
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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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User Reviews & Discussions
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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.
- 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.
- 3. Trazodone (Desyrel) Prescription
Information on RXList
- 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 Metabolism Disposition 1998 Jun;26(6):572-5.
- 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.
- 9. Gershon S, Newton R. Lack of anticholinergic side effects
with a new antidepressent trazodone. J Clin Psychiatry. 1980
Mar;41(3):100-4.
- 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. Clinical and polysomnographic effects
of trazodone CR in chronic insomnia associated with dysthymia.
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 Updated: February 2010 |
Interesting Trazodone facts
- Trazodone hydrochloride, a triazolopyridine derivative, is the most sedating, and least anticholinergic, of
all the currently available antidepressants.
- Trazodone is one most commonly prescribed treatments
for insomnia because of its sedative properties, low risk for serious side effects, perceived lack
of risk, generic availability, and lack of restrictions for long-term use.
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