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Dr. Bob is Robert Hsiung, MD,
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Posted by dbc on July 26, 2008, at 11:45:56
In reply to Like Trazodone for sleep but w/o heart problems, posted by David_Hi on July 26, 2008, at 10:51:29
Remeron?
Posted by Phillipa on July 26, 2008, at 12:18:27
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by dbc on July 26, 2008, at 11:45:56
I had no idea it had heart side effects thought it was safe. Thanks for educating me. Very thankful for that. Phillipa
Posted by Phillipa on July 26, 2008, at 12:30:45
In reply to Like Trazodone for sleep but w/o heart problems, posted by David_Hi on July 26, 2008, at 10:51:29
See you're new to babble let me welcome you. Lots of great knowledge here glad to meet you!!!! Love Phillipa
Posted by Phillipa on July 26, 2008, at 12:36:37
In reply to Re: Like Trazodone for sleep but w/o heart problems » David_Hi, posted by Phillipa on July 26, 2008, at 12:30:45
I never knew any of this here is the cardiac profile don't recall anyone before mentioning these side effects. Well this is Wike:
History
Trazodone was originally discovered and developed in Italy in the 1960s by Angelini research laboratories as a second-generation antidepressant. This agent was developed according to the mental pain hypothesis, which was postulated from studying patients and which proposes that clinical depression is associated with a decreased pain threshold.[2] Trazodone was patented and marketed in many countries all over the world. It was approved by the FDA at the end of 1981. It is closely related to Nefazodone.‎
[edit] Mechanism of action
Trazodone is not a serotonin reuptake inhibitor; in contrast to the selective serotonin reuptake inhibitors such as fluoxetine (trade name Prozac), trazodone's antidepressant effects may be due to its antagonistic effects at 5-HT2 receptors (PMID 1365657).
[edit] Pharmacokinetics
Trazodone is well absorbed after oral administration with mean peak blood levels obtained at approximately 1 hour after ingestion. Absorption is somewhat delayed and enhanced by food. The mean blood elimination half-life is biphasic: the first phase's half-life is 36 hours, and the following phase's half-life is 59 hours. The drug is extensively metabolized with 3 or 4 major metabolites having been identified in man, some of which such as mCPP[3] may contribute to the side effect profile of trazodone. Approximately 7075% of C14-labelled trazodone was found to be excreted in the urine within 72 hours (PMID 1037253). Trazodone is highly protein-bound.
[edit] Uses
Clinical depression with or without anxiety
Chronic insomnia[4][5][6] (in some countries, this is an off-label use)
Fibromyalgia, to control sleeping.
Control of nightmares or other disturbed sleep
A sleep aid (with a reduced risk of dependency)[edit] Other off-label and investigational uses
insomnia
panic disorder[7]
diabetic neuropathy[8]
bulimia nervosa[9]
obsessive-compulsive disorder[10][11]
alcohol withdrawal[12][13][14]
schizophrenia[15][16][edit] As an SSRI aid
Trazodone is often used in conjunction with selective serotonin reuptake inhibitor, like fluoxetine and has been noted to help with the anxiety that can result from beginning treatment with an SSRI anti-depressant. Trazodone has been prescribed to children as an aid to an SSRI.
[edit] Warnings
If the patient has a known hypersensitivity to trazodone.
If the patient is under 18 years of age. (Trazodone use in youth may increase the possibility of suicidal thoughts or actions.)[citation needed][edit] Precautions
Trazodone is metabolised by CYP3A4, a liver enzyme (PMID 9616194). Inhibition of this enzyme by various other substances may delay its degradation, leading to high blood levels of trazodone. CYP3A4 may be inhibited by many other medications, herbs, and foods, and as such, trazodone may interact with these substances. One drug-food interaction is grapefruit juice. Drinking grapefruit juice is discouraged in patients taking trazodone. One glass of grapefruit juice occasionally is not likely to have this effect on most people, but drinking large amounts, or drinking it regularly is proven to affect trazodone's clearance.The possibility of suicide in depressed patients remains during treatment and until significant remission occurs. Therefore, the number of tablets prescribed at any one time should take into account this possibility, and patients with suicidal ideation should never have access to large quantities of trazodone.
Episodes of complex partial seizures have been reported in a small number of patients.[citation needed] The majority of these patients were already receiving anticonvulsant therapy for a previously diagnosed seizure disorder.[citation needed]
While trazodone is not a true member of the SSRI class of antidepressants, it does still share many properties of the SSRIs, especially the possibility of discontinuation syndrome if the medication is stopped too quickly. [17] Care must therefore be taken when coming off the medication, usually by a gradual process of tapering down the dose over a period of time.
A person who abruptly stops taking Trazodone, even in doses as low as 25mg (common for use as a sleep aid for people with anxiety disorders), may experience adverse mental reactions such as emotional instability, depressed mood, and suicidal thoughts. Although such warnings may be included in printed materials supplied with the drug, physicians prescribing Trazodone, particularly those who are not psychiatrists, might not give oral warnings.
[edit] Pregnancy and lactation
Pregnancy : Sufficient data in humans is lacking. The use should be justified by the severity of the condition to be treated.
Lactation : Sufficient data in humans is also lacking. Additionally, trazodone may be found in the maternal milk in significant concentrations. Women should not breastfeed while taking Trazodone.[edit] Side effects
The most common adverse reactions encountered are drowsiness, nausea/vomiting, headache and dry mouth. Adverse reactions reported include the following:[citation needed]
[edit] Behavioral
Drowsiness, fatigue, lethargy, psychomotor retardation, lightheadedness, dizziness, difficulty in concentration, confusion, uncontrollable laughter, sex drive increase. (Trazodone is also known to cause a "hangover effect" in patients prescribed the drug as a sleep aid: the "Trazodone hangover" generally ceases with regular use after three or four days.)
[edit] Neurological
Tremor, headache, ataxia, migraine, akathisia, muscle stiffness, slurred speech, slowed speech, vertigo, tinnitus, tingling of extremities, paresthesia, weakness, complex partial seizures, and rarely, impaired speech, muscle twitching, numbness, dystonia, euphoria, and involuntary movements.
[edit] Autonomic
Dry or numb mouth, blurred vision, priapism, diplopia, miosis, nasal congestion, constipation, sweating, urinary retention, increased urinary frequency and incontinence.
[edit] Cardiovascular
hypotension, tachycardia, palpitations, shortness of breath, apnea, syncope, arrhythmias, prolonged P-R interval, atrial fibrillation, bradycardia, ventricular ectopic activity (including ventricular tachycardia), myocardial infarction and cardiac arrest.
[edit] Rare side effects
Recent clinical studies in patients with pre-existing cardiac disease indicate that trazodone may be arrhythmogenic in some patients in that population. Arrhythmias identified include isolated PVC's, ventricular couplets, and in 2 patients short episodes (3 to 4 beats) of ventricular tachycardia. There have also been several post-marketing reports of arrhythmias in trazodone-treated patients who have pre-existing cardiac disease and in some patients who did not have pre-existing cardiac disease. Until the results of prospective studies are available, patients with pre-existing cardiac disease should be closely monitored, particularly for cardiac arrhythmias. Trazodone is not recommended for use during the initial recovery phase of myocardial infarction.
[edit] Priapism
Priapism is a potentially harmful medical condition in which the erect penis does not return to its flaccid state (despite the absence of both physical and psychological stimulation) within about four hours. It is often painful. Priapism is considered a medical emergency, which should receive proper treatment by a qualified medical practitioner.
[edit] Gastrointestinal
Nausea, vomiting, diarrhea, gastrointestinal discomfort, anorexia, increased appetite.
[edit] Liver
Rare cases of idiosyncratic hepatotoxicity have been observed, possibly due to the formation of reactive metabolites (PMID 15978881).
[edit] Endocrine
Decrease and, more rarely, increase in libido, weight gain and loss, and rarely, menstrual irregularities, retrograde ejaculation and inhibition of ejaculation.Elevated prolactin concentrations have been observed in patients taking trazodone (PMID 7673654).
Trazodone has been associated with the occurrence of priapism. In approximately 33% of the cases reported, surgical intervention was required and, in a portion of these cases, permanent impairment of erectile function or impotence resulted. Male patients with prolonged or inappropriate erections should immediately discontinue the drug and consult their physician. If the condition persists for more than 24 hours, it would be advisable for the treating physician to consult a urologist or appropriate specialist in order to decide on a management approach.
[edit] Allergic or toxic
Skin rash, itching, edema, and, rarely, hemolytic anemia, methemoglobinemia, liver enzyme alterations, obstructive jaundice, leukocytoclastic vasculitis, purpuric maculopapular eruptions, photosensitivity and fever.
[edit] Miscellaneous
Aching joints and muscles, hypersalivation, chest pain, hematuria, red, tired and itchy eyes.[citation needed] muscle twitches[citation needed]
[edit] Occupational hazards
Since trazodone may impair the mental and/or physical abilities required for performance of potentially hazardous tasks, such as operating an automobile or machinery, the patient should be cautioned not to engage in such activities while impaired.
[edit] Laboratory tests
It is recommended that white blood cell and differential counts should be performed in patients who develop sore throat, fever, or other signs of infection or blood dyscrasia and trazodone should be discontinued if the white blood cell or absolute neutrophil count falls below normal.
[edit] Drug interactions
Trazodone may enhance the effects of alcohol, barbiturates and other CNS depressants; patients should be cautioned accordingly as trazodone with the combination of another CNS depressant, can result in extreme tiredness and dizziness.Increased serum digoxin and phenytoin levels have been reported to occur in patients receiving trazodone concurrently with either of those 2 drugs. Little is known about the interaction between trazodone and general anesthetics; therefore, prior to elective surgery, trazodone should be discontinued for as long as clinically feasible.
Because it is not known whether an interaction will occur between trazodone and MAO inhibitors, administration of trazodone should be initiated very cautiously with gradual increase in dosage as required, if an MAO inhibitor is given concomitantly or has been discontinued shortly before medication with trazodone is instituted.
Because of the absence of experience, concurrent administration of electroconvulsive therapy should be avoided.
[edit] Dosage
Treatment should be started with low initial doses of 25 to 50 mg daily in divided doses or in an evening single dose. The dose may be increased slowly to a maximum of 300 mg daily in ambulatory patients and to 600 mg daily in hospitalized patients. Geriatric and emaciated patients should begin with 100 mg daily; this dose may be slowly increased to 300 mg. The duration of treatment should be at least one month. A 50 mg dose is recommended when using Trazodone as a sleep aid.
[edit] Overdose[edit] Symptoms
Overdosage of trazodone may cause an increase in incidence or severity of any of the reported adverse reactions, e.g. excessive sedation. Death by deliberate or accidental overdosage has been reported (PMID 15975258, PMID 11603256). However, trazodone is often used instead of tricyclic antidepressants because it is very rarely lethal in overdose. Depressed patients are therefore unlikely to successfully commit suicide with trazodone. [18]
[edit] Treatment
There is no specific antidote for trazodone. Management of overdosage should, therefore, be symptomatic and supportive. Any patient suspected of having taken an overdosage should be admitted to hospital as soon as possible and the stomach emptied by gastric lavage. Forced diuresis may be useful in facilitating elimination of the drug.
Posted by David_Hi on July 26, 2008, at 13:22:25
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by Phillipa on July 26, 2008, at 12:36:37
Myocardial infarction listed as a side-effect looks pretty scary to me. Also one review on askapatient.com:
http://www.askapatient.com/viewrating.asp?drug=70857&name=TRAZODONE%20HCL
mentioned developing a heart disease.
So if you know any other sedating anti-depressants that might help with sleep please do tell.
Thanks,
David
Posted by dbc on July 26, 2008, at 14:01:49
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by David_Hi on July 26, 2008, at 13:22:25
I did and its remeron.
Posted by David_Hi on July 26, 2008, at 14:24:34
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by dbc on July 26, 2008, at 14:01:49
dbc: What dosage of Remeron do you take for sleep? I know that at higher doses it won't help with sleep anymore. Do you know of any other sedating anti-depressants?
Thanks
Posted by dbc on July 26, 2008, at 15:40:48
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by David_Hi on July 26, 2008, at 14:24:34
Below 30mg has the most sedating effect without actually activating the drug. It and trazadone are really the only ones that are used off label for sleep issues.
Seroquel is used a lot these days but its an anti psychotic and you know the story with them.
Posted by David_Hi on July 26, 2008, at 16:29:46
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by dbc on July 26, 2008, at 15:40:48
Thanks dbc; I'll try Remeron too.
The only drawback is that quite a few people say it stops working after a while for insomnia:
http://www.askapatient.com/viewrating.asp?drug=20415&name=REMERON
Perhaps they should have lowered the dose?
Posted by dbc on July 26, 2008, at 17:41:55
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by David_Hi on July 26, 2008, at 16:29:46
Every sleep med eventually stops working. Just the nature of the beast i suppose.
I looked up some of the drugs im taking on that site and the amount of complaining and totally insane obscure side effects was kind of funny. Im not sure if i would rely on that site.
I think the problem with those types of sites is people arent compelled to post about meds unless they're having side effects. Im pretty sure lamictal wont kill me or cause me to kill other people or make me think my dog is satan despite what some posters on that site may think.
Posted by Larry Hoover on July 26, 2008, at 21:52:00
In reply to Like Trazodone for sleep but w/o heart problems, posted by David_Hi on July 26, 2008, at 10:51:29
> So basically I'm looking for an anti-depressant with sedating properties like Trazodone but with no heart-related side-effects.
>
> ThanksThe tricyclics doxepin, trimipramine, and amitriptyline are all used to promote sleep.
Lar
Posted by jrbecker76 on July 26, 2008, at 23:51:36
In reply to Re: Like Trazodone for sleep but w/o heart problems » David_Hi, posted by Larry Hoover on July 26, 2008, at 21:52:00
> > So basically I'm looking for an anti-depressant with sedating properties like Trazodone but with no heart-related side-effects.
> >
> > Thanks
>
> The tricyclics doxepin, trimipramine, and amitriptyline are all used to promote sleep.
>
> Lar
>
>Nefazadone (Serzone) and Trazadone both metabolize into m-CPP, a serotonin agonist that causes a host of side effects, including chest pressure and heart palpitations. For most, the adverse events typically subside after initial titration and/or can be controlled by reducing your daily dosage. However, they can be a continual problem for some.
There is a new hypnotic class of 5-HT2 antagonists that will be on the market soon that will provide many of the benefits of nefazodone and trazadone, but with less of a side effect profile. Eplivanserin, which is a drug candidate from Sanofi-Aventis, should reach the market sometime next year. In the meantime, I would add to the other posters' recommendations by also throwing out there Rozerem (ramelteon). Some people find it does nothing, but many others report it gives them a great night's sleep with little residual effects in comparison to the GABA-A class of hypnotics (Ambien, Sonata, Lunesta). I take Rozerem in combination with a very low-dose of Nefazadone nightly.
JB
Posted by Phillipa on July 27, 2008, at 0:46:29
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by jrbecker76 on July 26, 2008, at 23:51:36
You take serzone? Aren't you afraid of liver damage. If I hadn't been it might have worked as it was sedating. So this new med next year is that the tradename? Thanks compulsive poster Phillipa
Posted by Amigan on July 27, 2008, at 14:39:31
In reply to Like Trazodone for sleep but w/o heart problems, posted by David_Hi on July 26, 2008, at 10:51:29
I'm surprised that nobody mentioned of Clonidine yet... It's the PERFECT thing to add to Trazodone if you take it as a sleeping pill and either you don't find it sedating enough or it gives you palpitations. Not so good if you take it as an AD, though.
Try it and see. Start with half a pill and remember that it has much longer half-life. Thus, you may feel groggy the other day.
It also decreases the blood pressure and may cause orthostatic hypotension.You will likely get palpitations from Remeron as well.
Posted by dbc on July 27, 2008, at 15:57:37
In reply to Re: Like Trazodone for sleep but w/o heart problem » David_Hi, posted by Amigan on July 27, 2008, at 14:39:31
> You will likely get palpitations from Remeron as well.
Cite a source or this is simply a biased statement.
Posted by Amigan on July 27, 2008, at 16:03:05
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by dbc on July 27, 2008, at 15:57:37
> > You will likely get palpitations from Remeron as well.
>
> Cite a source or this is simply a biased statement.Although i don't like this attitute, it shares the same noradrenergic mode of action which causes the palpitations with Trazodone.
Posted by dbc on July 27, 2008, at 18:16:45
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by Amigan on July 27, 2008, at 16:03:05
I got the impression he wanted to take sub therapeutic doses. Of course taking 30mg of remeron is pointless because the NRI effect impacts its sedating properties.
Posted by jrbecker76 on July 27, 2008, at 18:21:53
In reply to Re: Like Trazodone for sleep but w/o heart problems » jrbecker76, posted by Phillipa on July 27, 2008, at 0:46:29
> You take serzone? Aren't you afraid of liver damage. If I hadn't been it might have worked as it was sedating. So this new med next year is that the tradename? Thanks compulsive poster Phillipa
I consider the risks extremely minimal, especially considering I typically take a micro-dose of 12.5-25mg nightly. My doctor concurs. I have taken nefazadone on and off for 5 years at a low-dose. It is somewhat sedating (due not just to the 5-HT2 antagonism, but the alpha-1 adrenoreceptor affinity). But overall, it's a great augmentor for sleep as well for individuals who don't fully respond to SSRI/SNRIs.
As for eplivanserin, that's the compound name, not the tradename. Sanofi plans to submit to the FDA sometime later this year.
JB
Posted by dbc on July 27, 2008, at 18:25:07
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by jrbecker76 on July 27, 2008, at 18:21:53
To make my post more clear if you're not familiar with how remeron works. Its kind of strange, the lower the dose the more sedating it is. I know that sounds incredibly strange but its true.
When i was on a trial for it i literally slept the entire first month from the non therapeutic level doses. It has a really potent antihistamine effect that rivals even seroquel.
Posted by Phillipa on July 27, 2008, at 19:19:15
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by jrbecker76 on July 27, 2008, at 18:21:53
Thanks JR fits my profile. And I know you know your stuff. Love Phillipa
Posted by johnj on July 27, 2008, at 19:49:10
In reply to Re: Like Trazodone for sleep but w/o heart problem, posted by dbc on July 27, 2008, at 15:57:37
I also get internal anxiety for remeron. I can't say it is only heart palps but it is very unpleasant and continued even and small doses that I was using for sleep. It also made me very depressed at lower doses. I guess this is probably from the histamine but I think something else is going on as antihistamines don't do the same thing. Anti-h just make me feel cruddy the next day.
Posted by johnj on July 27, 2008, at 19:52:31
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by jrbecker76 on July 27, 2008, at 18:21:53
Thank you for sharing this info. I know you mentioned before about low doses as you are med sensitive. I am the same. I did try trazodone at 25 mg and slept well but was very hung over the next day. I get the same from remeron except the low doses also make me feel very depressed and I didn't get that from trazodone.
I really just need something to take the edge off and help me sleep somewhat well as this really makes me feel so much better. I was thinking of a small dose nortryptline and maybe serzone.
johnj
Posted by jrbecker76 on July 29, 2008, at 23:25:35
In reply to Re: Like Trazodone for sleep but w/o heart problems » jrbecker76, posted by johnj on July 27, 2008, at 19:52:31
> Thank you for sharing this info. I know you mentioned before about low doses as you are med sensitive. I am the same. I did try trazodone at 25 mg and slept well but was very hung over the next day. I get the same from remeron except the low doses also make me feel very depressed and I didn't get that from trazodone.
>
> I really just need something to take the edge off and help me sleep somewhat well as this really makes me feel so much better. I was thinking of a small dose nortryptline and maybe serzone.
>
> johnjHi John,
I'd recommend a go of nefazadone first. I'd try out a low-dose of 12.5-50mg. Give it about 1 week to settle into a dose. Despite the fact that nefazadone's half-life is just slightly longer than trazadone's, there is an active metabolite that mimics the parent compound's hypnotic/anxiolytic quality. So, don't up the dose too early. On the other end, for some individuals - despite being sedating for the first half of the night - it can actually cause early awakening. This is most likely due to the m-CPP metabolite. Typically, the activation from m-CPP fades after a week or so of titration for most individuals, but may continue to be a nuisance for some.
My ideal dose was 25mg for quite a few years, but I recently traded that in for the lower dose of 12.5mg in combo with 8 mg of Rozerem. I still sleep soundly, but perhaps not as soundly as I did at the higher dosage level of nefazadone. Given that I'm quite med-sensitive though, I have found that the lower dose gives me less side effects (but now also with less efficacy on antidepressant/anxiolytic effects though).
JB
Posted by yxibow on July 31, 2008, at 1:56:30
In reply to Re: Like Trazodone for sleep but w/o heart problems » David_Hi, posted by Larry Hoover on July 26, 2008, at 21:52:00
> > So basically I'm looking for an anti-depressant with sedating properties like Trazodone but with no heart-related side-effects.
> >
> > Thanks
>
> The tricyclics doxepin, trimipramine, and amitriptyline are all used to promote sleep.
>
> Lar
>
>I take amitriptyline -- for some though, tricyclics can present heart problems, generally in the older population.
Posted by yxibow on July 31, 2008, at 2:00:19
In reply to Re: Like Trazodone for sleep but w/o heart problems, posted by jrbecker76 on July 26, 2008, at 23:51:36
> > > So basically I'm looking for an anti-depressant with sedating properties like Trazodone but with no heart-related side-effects.
> > >
> > > Thanks
> >
> > The tricyclics doxepin, trimipramine, and amitriptyline are all used to promote sleep.
> >
> > Lar
> >
> >
>
> Nefazadone (Serzone) and Trazadone both metabolize into m-CPP, a serotonin agonist that causes a host of side effects, including chest pressure and heart palpitations. For most, the adverse events typically subside after initial titration and/or can be controlled by reducing your daily dosage. However, they can be a continual problem for some.
>
> There is a new hypnotic class of 5-HT2 antagonists that will be on the market soon that will provide many of the benefits of nefazodone and trazadone, but with less of a side effect profile. Eplivanserin, which is a drug candidate from Sanofi-Aventis, should reach the market sometime next year. In the meantime, I would add to the other posters' recommendations by also throwing out there Rozerem (ramelteon). Some people find it does nothing, but many others report it gives them a great night's sleep with little residual effects in comparison to the GABA-A class of hypnotics (Ambien, Sonata, Lunesta). I take Rozerem in combination with a very low-dose of Nefazadone nightly.
>
> JB
As for whether anything from France politically ever makes it past the FDA, we shall see -- there have been diminishing returns from companies like Servier (just an observation).m-CPP can cause those effects I suppose, yes, I did have an idosyncratic but self-limiting palpitation with Trazodone. But primarily m-CPP presents a problem with people prone to its effects on psychosis. Its not the best choice.
This is the end of the thread.
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Dr. Bob is Robert Hsiung, MD,
[email protected]
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