Posted by Stan on August 1, 2002, at 1:17:19
In reply to Shawn -- info on trazodone needed!, posted by turalizz on July 31, 2002, at 10:19:19
> Hi Shawn,
>
> Do you have any interesting information about trazodone? Where does its sedation come from? What affinities does it have for receptors (as agonist or antagonist)? What is its half-life and clearance time?
>
> It is the best sleep aid I've ever tired, and very interestingly I am not developing a tolerance against it. I am very curious why.
>
> thanks,
>
> cemhi cem -- i'm not shawn (obviously) but if you don't mind i'll take a shot at partially answering a couple of your queries -- perhaps shawn'll follow up with more detail and in a more technical fashion (i've come across a few of his posts since i starting checking out this board a week ago and they are very comprehensive!).
i took trazodone for about a year, up until such time that serzone became available in the usa (i think this was about 1995?). i had tried a couple of SSRIs (zoloft, paxil) for short trials before i started the trazodone (i suffer from "anxious depression") but they didn't improve my symptoms of restlessness and anxiety......in fact they made me feel a little "speedy" and "wired" -- so i discontinued them and decided that SSRIs in general weren't my bag. once i started the trazodone i noticed an almost immediate improvement in my symptoms of anxiety and restlessness -- but it was highly sedating, even at fairly low doses. trazodone is a weak reuptake inhibitor of serotonin and norepinephrine, but these mild effects are not its main mechanism of action. rather, the drug acts as a relatively potent antagonist at the group of 5HT2 serotonin receptors, and this activity is viewed as a major factor in relieving anxiety and helping to supress negative, intrusive thoughts. in addition, trazodone antagonizes alpha1-adrenergic receptors in similarly potent fashion, and therein lies the major reason for its prominent sedative qualities. by antagonizing this group of adrenoreceptors (i think that's a word), it acts a bit like certain blood pressure medications which work on the same receptor group in the same way -- the result can be drowsiness, fatigue, weakness,dry mouth, hypotension, etc.
however, on the plus side, trazodone can have additive anti-anxiety effects for certain individuals by antagonizing this receptor group, because the "activating" effects that the alpha1 group produces can heighten anxious feelings when left unchecked in a person sensitive to excess norepinephrine coursing through the body.i had difficulty tolerating trazodone because of the sedation and when serzone came out i made the switch and i still take serzone today (although i feel like it's "pooping-out" on me). serzone and trazodone are strikingly similar in many respects and it's been said that bristol-myers (manufacturer of both branded drugs) developed serzone as a response to complaints about trazodone's extreme sedation and occasional reports of priapism -- the main difference is that while serzone is also an antagonist at "alpha1," its effects there are so weak as to be nearly inconsequential, thus clearing up the two potential problems mentioned just above. the two drugs have a very similar chemical structure and serzone can almost be considered an "update" on desyrel (brand name for trazodone). for a time i combined them -- serzone in the morning, trazodone at night, but now i'm combining serzone with some other meds.
well, that was quite a ramble and i get the feeling that you're simply taking it as a sleep aid, cem, and one of your questions had to do with developing a tolerance to its effects - you may have to increase the dosage somewhat as time goes by -- if you keep antagonizing "alpha1," the receptor group may "fight back" and "up-regulate" for awhile.....the same phenomenon can be observed with some blood pressure meds that target this receptor group. you asked about half-life; i think it's about 7-8 hours.....if you take a decent dose you may have a bit of trouble dragging yourself out of bed in the morning. i'm guessing that you're taking about 50 mg before retiring. when used as an AD the range is more like 150-300 mg for most people, i believe.
hope that info helped a bit -- i think most of my statements are relatively accurate but i'm just an amateur :)
good luck,
Stan
poster:Stan
thread:114609
URL: http://www.dr-bob.org/babble/20020731/msgs/114736.html