12 replies to this topic

[therapeuticbrigg84]

is there a difference between doxepin and elavil in terms of function. i know doxepin is an antagonist of alpha adrenergic 1 & 2. and elavil says it's a noradrenaline reuptake inhibitor and serotonin reuptake inhibitor. is noradrenaline reuptake inhibitor another word for antagonist of alpha adrenergic receptors? or are these totally different drugs in terms of mechanism?

Edited by therapeuticbrigg84, 24 August 2009 - 08:07 PM.

[Jerod Poore]

i know doxepin is an antagonist of alpha adrenergic 1 & 2.

The topical stuff is. I'm not having luck finding anything that will tell me one way or the other if the pills also do that.

and elavil says it's a noradrenaline reuptake inhibitor and serotonin reuptake inhibitor. is noradrenaline reuptake inhibitor another word for antagonist of alpha adrenergic receptors? or are these totally different drugs in terms of mechanism?

agonist: makes receptors more sensitive to a neurotransmitter
antagonist: makes receptors less sensitive to or blockades reception of a neurotransmitter
reuptake inhibitor: lets the receptors soak in the neurotransmitter longer

An antagonist is the opposite of a reuptake inhibitor. Several meds are both reuptake inhibitors and antagonists of the same neurotransmitters, because they act at different locations.

[therapeuticbrigg84]

so when it comes to elavil and doxepin...they both act upon different mechanims or what?

so since u said antagonist and reuptake inhibitor are opposites, then elavil is more like a long acting adrenergic agonist and doxepin is a blocker of those alpha adrenergic receptors.

here's doxepin

that shows exactly where it is in terms of blocking reuptake of noradrenaline, and at the same time, it mentions that it's an antagonist of the alpha adrenergic 1 & 2.

Edited by therapeuticbrigg84, 21 August 2009 - 09:40 PM.

[therapeuticbrigg84]

and also, altho i asked my pdoc to put me on elavil, he decided to give me a prescription for a low dose of doxepin for sleep. which one is better?

seroquel worked for me but had bad side effects. and doxepin is in that class of dibenzoxazepine along with clozaril and seroquel

bump

Edited by therapeuticbrigg84, 22 August 2009 - 11:31 AM.

[Jerod Poore]

I'm still not all that with it today, but on Friday I was working on the server all day long.

so when it comes to elavil and doxepin...they both act upon different mechanims or what

The short answer: doxepin does more serotonin reuptake inhibition and blockades H2 in addition to H1. Otherwise they're the same. Other than serotonin reuptake inhibition I don't have the numbers as to which is more potent where.

Doxepin is more likely to be better for sleep.

The long answer:

All TCAs are norepinephrine-selective reuptake inhibitors, antihistamines and anticholinergics. They are all serotonin-selective reuptake inhibitors, but impramine and desipramine barely do much in that department.

All TCAs also blockade some serotonin and the alpha adrenergic receptors. Again it's all a matter of potency.

so since u said antagonist and reuptake inhibitor are opposites, then elavil is more like a long acting adrenergic agonist and doxepin is a blocker of those alpha adrenergic receptors.

here's doxepin

that shows exactly where it is in terms of blocking reuptake of noradrenaline, and at the same time, it mentions that it's an antagonist of the alpha adrenergic 1 & 2.

I'm not a big fan of Wikipedia, but doxepin doesn't get much of a write-up in the books I have and I'm not finding much else online. So let's just take that article as a given. Anything described as "weak" means "The tests registered something. If it wasn't a false positive it's still not enough to matter." "Moderate" means "This may or may not make a difference to any random human taking it."

So the only thing that stands out with doxepin is being an antihistamine for both H1 and H2.

Like ipramine, Elavil (amtriptyline) doesn't do much in the way of selective serotonin reuptake inhibition. Doctor Preskorn considers both to have no appreciable serotonergic effect. Like all the other TCAs it blockades H1. Amtriptlyine isn't an agonist. It's an inverse agonist instead of antagonist at some of the receptors, and that's just getting extremely specific about how it keeps the receptor from soaking up the neurotransmitter goodness. The literature refers to inverse agonists and antagonists as being interchangeable all over the place. Right now I'm not sure I understand what the hell an inverse agonist actually does.

[therapeuticbrigg84]

i've recently been reading up on the TCAs and i found that anything that really antagonizes the histamine receptor or the 5HT1A or 5HT2, really causes a lot of side effects in me. I take buspar( which is a 5HT1A agonist, and it really helps me out.) so anything that antagonizes that receptor, does not agree with me. so my doc tries out doxepin, which out of all the TCAs antagonizes 5HT1A the most, and to a lesser extent 5HT2, and also histamine the most, it really affects me a lot. so that didn't really quite work out. So now I'm looking for a TCA that does not antagonize those receptors and does not have a lot of sedation in it(like seroquel did.)

So I looked into the other TCAs a lot to figure out which ones didn't antagonize H1 or 5HT1A as much as the others and i found that either Pamelor or desipramine would be the best candidates for me. they also don't affect dopamine(2) a lot either.

can anyone give me a comparison to trazodone, as to which receptors trazodone really hits??(numbers please) and also a comparison to wellbutrin as in what dopamine receptors it hits and what numbers, and how many norepinephrine(NET) receptors it hits?

Edited by therapeuticbrigg84, 24 August 2009 - 09:23 PM.

[therapeuticbrigg84]

the doc put me on 25 mg pamelor for migraine headaches/insomnia. because the doxepin wasn't really working out

update: so im now up to 50 mg pamelor, and it seems to be working or doing something at least. because otherwise, i'd probably be really depressed by now/ having bad headaches. as for whether i would, switch with elavil, i probably would, since it seems to be the 1-up version of pamelor. but the only thing preventing me from doing so is the effects i had from doxepin.

i would like to get the reference numbers for trazodone and wellbutrin XL also, but it seems like it's not really out there.

Edited by therapeuticbrigg84, 17 September 2009 - 05:10 PM.

[therapeuticbrigg84]

bump

[creepy]

I had awful headaches several hours after taking desipramine which were solved by taking it at night. No sleep issues since I have celexa putting me into the land of nod and snooze.
I still have some blood pressure weirdness in my head. I feel hot and may get a little headachey. But blood pressure reads normal when measured. pain relief isnt as strong as it was initially.
TCAs supposedly can weaken the resistance in the extremities and lower blood pressure, but as far as I know meds that are NRIs work a lot in the area of the brain that controls autonomic things like heartrate and blood pressure. Not sure how those two work out, they sound mutually exclusive. I have mild tachycardia (70 resting rate to 93 initially.. now 80) and normal pressure.
Im also finding out desipramine adds to my heartburn problem. I found a blurb in a psychopharm book that suggests TCAs can weaken the LES (lower esophageal sphincter). which might be related. Doc says I need to read books and not forums! Heh.. next time I quote sources
I think these side effects crop up at first then mostly go away.

Edited by creepy, 22 October 2009 - 12:18 PM.

[arcady59]

I took imipramine once and i seemed to work, but I had the worst dry mouth ever. I did not know i was possible to be that uncomfortable with dry mouth. Anyway I stopped that and went on a bunch of other unsuccessful meds, and now I find myself on nortriptyline. This compliments 45mg of Remeron, and 10mg of Suboxone, recently added because I developed an addiction to hydrocodone. I have not had any dry mouth so far on the nortriptyline.

[therapeuticbrigg84]

you may run into dry mouth with nortriptyline, but for me it wasnt bad enough to quit. i mean compared to imipramine, it mustnt be that bad. desipramine would also probably be a little more milder being that it's the metabolite of imipramine.

[DrSara]

I LOVED Nortriptyline, it was my magic drug. When I had to stop taking it (side effect), I tried desipramine and it made me ragefully manic...so there is a clinical difference even if theoretically there shouldn't be.

[arcady59]

Well the drymouth kicked in, but it is not nearly as bad as I remember it was with Imipramine. I just need a sip of water every now and then. I also feel a little more calm, almost sedate, but not in a bad way. I was on Wellbutrin and Remeron just before this and I was so jittery and anxious, it was horrible; I felt like I had reverted to how I was before all my treatments, like I haven't learned anything throughout the years. Almost like an uncontrollable anxiety. Anyway I like the Nortripyline so far, and I hope this one works. I will find out soon I hope!