MAOI injections?

[Eric01]

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N/a

 

[firedoor]

Even with the minimization of dietary-drug interactions, drug-drug interactions remain the achilles heel of parenteral MAOI's. Perhaps a parenteral RIMA (reversible inhibitor of monamine oxidase) would minimize DDI's even further.

 

[billypilgrim37]

Why bother with a patch in the first place?

Because you can take a patch off.

If you put a mouse into hypertensive crisis, you just get another mouse.

 

[Eric01]

N/a

 

[billypilgrim37]

But it doesn't matter if you stop oral medication in drugs like Nardil, the inhibition is permanent anyways, until new MAO enzymes get produced.

Right, but if I stop PO nardil today, then MAOs will start replenishing, albeit slowly, in a few days. If I stop Nardil Consta, they may not start for weeks to months. If you have someone on Risperdal Consta at steady state, and they stop it tomorrow, they will still have detectable serum levels of risperidone two months from now, and they will still have observable receptor occupancy for much longer than that (CNS levels will deplete much more slowly than serum levels).

Even the patch still does not completely eradicate the theoretical risk of disrupting MAO in the gut epithelia, and parenteral administration wouldn't either. While the concentration of drug that reaches the gut epithelia will be much lower than in a PO route, there is still going to be exposure, and even at higher dose selegiline there is concern that if you ate enough stinky cheese and german beer you could still be at pretty high risk.

I'm not sure what the pressing need for a depot MAOi would be, either.

 

[whopper]

I heard, via word-of-mouth, that Ensam patches didn't sell too well. I could be wrong, and someone correct me if I am.

If I am correct, this would lead me to believe that no company would want to market an injectable MAO-I.

It might not be possible to make an injectable MAO-I given our current level of knowledge. I know that some antipsychotics, given the current technology, cannot be easily converted to that format. It depends on the molecular structure. While I am a psychiatrist, my knowledge of that aspect is limited, so I cannot state if the possibilities in that respect, but can state that not all psychotropics can be turned into an injectable format simply because the idea sounds like a good one.

Antipsychotics are a different game vs. antidepressants. There is a large demographic of patients that are manic or psychotic that do not want an antipsychotic due to poor insight. While this does exist for the depressed and anxious, it's not the same thing. Someone manic often enjoys their mania. Someone psychotic often doesn't realize they are that, and when you treat them it feeds into their delusions that someone in the government is trying to control them. Someone with depression or anxiety usually realized they got a problem and want treatment for it.

 

[OldPsychDoc]

I heard, via word-of-mouth, that Ensam patches didn't sell too well. .

That would be a significant understatement.
They didn't work too well, either, though whether that's correlated to your statement is a matter for debate, I guess. 🙄

 

[billypilgrim37]

That would be a significant understatement.
They didn't work too well, either, though whether that's correlated to your statement is a matter for debate, I guess. 🙄

I've never started it, but the one case I was around most was a woman with MDD, PTSD, ACT-team requiring borderline pd whose life was completely turned around with Emsam. It was amazing. I speculate it worked just well enough to get her to be able to engage her DBT groups, which was probably then responsible for most of her recovery, but little else had been helpful up to that point.

Of course, maybe the turning point was the prazosin I gave her on her nth admission 😀

 

[jamesearlejones]

If we're talking about developing useful depot medications, we should focus on mood stabilizers. Wow, it would be truly phenomenal if depot lithium or VPA existed for some of my patients.

 

[Mattchiavelli]

Just a point to note, removing a patch doesn't stop administration of a drug since the drug first re-distributes to the skin and administers from there.

My main experience with MAOIs is in Parkinson's patients. There was an article recently showing a weak neuroprotective effect with MAOIs, and even then the general consensus was that it wouldn't change practice b/c of the many side effects and drug interactions seen with MAOIs, granted that patient population tends to be older with other medical comorbidities thus requiring more medications.

My thing I wonder about is why don't more meds work on the levodopa/carbidopa model of an active drug + competitive inhibitor that doesn't penetrate the blood/brain barrier in order to avoid systemic side effects while getting good CNS activity.

 

[billypilgrim37]

Just a point to note, removing a patch doesn't stop administration of a drug since the drug first re-distributes to the skin and administers from there.

Hours to days. Not weeks to months.