trazodone (Desyrel, Pragmazone, Oleptro)
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Introduction
Tradename: Desyrel. (trazodone HCl)
Indications
- depression
- sleep disorder*
- neurogenic pain
- especially useful in patients for which anticholinergic effects would be problematic:
- elderly
- patients with benign prostatic hypertrophy
* commonly used off-label to treat insomnia, but not much data to support use[10]
Contraindications
- Caution: cardiac disease or arrhythmias
- no evidence of cognitive benefit from trazodone vs other antidepressants in people with dementia[9]
Dosage
- hypnotic: 50-100 mg QHS
- start 50 mg PO TID
- increase in 50 mg/day increments every 3-4 days
- excessive sedation limits dose increase
- maximum dose: 600 mg/day
Tabs: 25, 50, 100, 150, 300 mg.
Oleptro 150, 300 mg (extended-release) for depression[7]
Pharmacokinetics
- oral bioavailability is 72-90%; take with snack to reduce nausea
- extensively metabolized by the liver by cyt P450 2D6
- active metabolite (1-m-chlorophenylpiperazine) is excreted in the urine
- elimination 1/2life is 5-9 hours
- maximal antidepressant effect occurs within 2-6 weeks
- onset of action: 7 days
elimination via liver
1/2life = 6-13 hours
protein binding = 89-95 %
elimination by hemodialysis = -
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- prolonged priapism (1/6000), hypotension, rash, tachycardia, bradycardia, agitation, seizures, extrapyramidal effects, hepatitis, urinary retention
- other
- sedation (frequent)
- postural hypotension (frequent)
- irregular heartbeat
- minimal anticholinergic effects
- photosensitivity
- in patients on hemodialysis, trazodone associated with higher risk of cardiovascular events[11]
Drug interactions
- other CNS depressants: increase CNS depression
- digoxin: increase in digoxin levels
- phenytoin: increase phenytoin levels
- MAO inhibitors: avoid combination
- trazodone may interfere with antihypertensive effects of clonidine & methyldopa
- trazodone may decrease effects of anticoagulants
- fluoxetine increases trazodone levels
- Ginkgo biloba in combination may cause CNS depression by overstimulation of GABA receptors[5]
- coadministration with selective serotonin reuptake inhibitors SSRI may result in serotonin syndrome
- any drug that inhibits cyt P450 2D6 may increase levels of trazodone
- drug interaction(s) of trazodone with SSRIs
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of NSAIDs with antidepressants
Laboratory
- specimen:
- methods:
Mechanism of action
- some effects similar to other antidepressants
- serotonin-2 receptor inhibition
- may inhibit reuptake of serotonin
- inhibition of alpha adrenergic receptors
More general terms
Additional terms
- 1-m-chlorophenylpiperazine (MCPP)
- cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 5.0 5.1 Prescriber's Letter 7(9):53 2000
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 7.0 7.1 Prescriber's Letter 17(10): 2010 COMMENTARY: Oleptro (Trazodone) and Silenor (Doxepin) CHART: Comparison of Insomnia Treatments Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=261005&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Paauw DS Dangerous and Deadly Drug Combinations Medscape. June 30, 2016 http://www.medscape.com/features/slideshow/dangerous-drug-combinations
- ↑ 9.0 9.1 Sommerlad A, Werbeloff N, Perera G et al. Effect of trazodone on cognitive decline in people with dementia: Cohort study using UK routinely collected data. Int J Geriatr Psychiatry, 2021. September 25. PMID: https://www.ncbi.nlm.nih.gov/pubmed/34564898 https://onlinelibrary.wiley.com/doi/abs/10.1002/gps.5625
- ↑ 10.0 10.1 Monaco K Trazodone Commonly Used Off-Label for Insomnia. Not much data to support efficacy or safety "as a surrogate hypnotic medication," researcher says. MedPage Today September 20, 2022 https://www.medpagetoday.com/meetingcoverage/psychcongress/100819
- ↑ 11.0 11.1 Mehrotra R et al Effectiveness of Existing Insomnia Therapies for Patients Undergoing Hemodialysis. A Randomized Clinical Trial. Ann Intern Med. 2024. Jan 16. PMID: https://www.ncbi.nlm.nih.gov/pubmed/38224591 https://www.acpjournals.org/doi/10.7326/M23-1794