Neuro Toxicity of 5ar Inhibitors

HairlossTalk

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"CNS Toxicity: At 425 and 315 fold the expected clinical drug some rats and dogs exhibited signs of non-specific, reversible, centrally-mediated toxicity without associated histopathological changes.

Note that only 'some' and not all rats and dogs had signs of neural toxicity. I think if you ate 300 times the table salt you normally now do, you would probably have "non-specific, reversible, centrally-mediated [CNS] toxicity". Actually, you would probably wouldn't survive very long.

Also, does dutasteride cross the blood-brain barrier readily and enough quantity when taken at 0.5 mg/day to reduce 5AR-1 activity in the brain? The blood-brain barrier is a formidable deterrent against relatively small concentrations of substances entering the brain. Testosterone, which is chemically similar to dutasteride, does cross the blood-brain barrier, but dutasteride has many modifications in it's chemical structure (it's quite electronegative) that may prohibit it's crossing that barrier except at high does (for example, 300 times the normal dose).

5AR-1 does play a role in the CNS - it's thought to prevent neurological toxicity by catabolism of neurotoxic steriods. It also functions to convert progesterone to dihydroprogesterone (DHP) in the brain - a beneficial neurosteroid. 3-alpha-HSD (another enzyme in the brain) converts DHP to allopregnanolone. Allopregnanolone is a neurosteroid which exhibits anxiolytic (anti-anxiety) and anticonvulsant activities through potentiation of the GABA(A) receptor. So if you start feeling more anxiety or have seizures, stop taking dutasteride and tell your doctor (and Glaxo)."
 

Cassin

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I am not up to snuff as some of the people on this board when it comes to stuff like this, so could you give us a basic run down of what this means HairLossTalk.com, or anyone else?
 
G

Guest

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I think the points made are.


1. some 5AR-1 is needed for a healthy Central Nervous System, in particular it appears to be involved in anti-convulsant and anti-anxiety processes.


2. because of it's chemical structure dutasteride is unlikley to cross the blood-brain barrier (at common dosage) and lead to brain toxicity.


4. what happened to 3


5. take 300/400 X the clinical dose of dutasteride and some rats and dogs (and possibly Cal Que Later) will experience non-specific reversible brain toxicity.


3. oh there you are.


6. lots of salt is bad for you.



Ty
 

Cassin

Senior Member
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tynanW said:
I think the points made are.

1. some 5AR-1 is needed for healthy brain function, in particular it appears to be involved in anti-convulsant and anti-anxiety processes.


2. because of it's chemical structure dutasteride is unlikley to cross the blood-brain barrier (at common dosage) and lead to brain toxicity.


4. what happened to 3


5. take 300/400 X the clinical dose of dutasteride and some rats and dogs (and possibly Cal Que Later) will experience non-specific reversible brain toxicity.


3. oh there you are.


6. lots of salt is bad for you.



Ty

So...........

#1. Taking dutasteride could possible lead to paranoia?

#3. is a naughty fella isn't he?
 
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