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new uses for L type calcium blockers

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Neuroprotection

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Apr 18, 2015
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L type calcium channel blockers are widely used to treat high blood pressure and chest pain/angina pectoris. They include drugs like nimodipine, isaradipine and vyrapamol. However, these substances also block calcium channels in neurons of the CNS and brain, but without significantly altering consciousness at therapeutic levels. They have been shown to have potent neuroprotective affects by blocking excess calcium influx induced by trormer or excitatory amino acids. They also slow or inhibit opioid tolerance in animals.
What are your views?
How about using calcium channel blockers to treat opioid or benzodiazepine withdrawal/addiction, providing you use ones that can cross the blood brain barrier.
I’ve also heard they can enhance memory of a ketamine trip, not sure how that one works, but they are given just before administration of ketamine in hallucinogen assisted psychotherapy.
 
I too have wondered about the mental / neuronal effects of calcium channel blockers, seeing that acting on a sub unit (a2d with the gabapentinoids) has such profound effects. Maybe they are too inselective and would have harmful side effects before relevant effects set in - or are they just not yet documented and these Ca blockers could be potential mood-stabilizers etc..or general anti-excitatory drugs as you suggest for withdrawal?

The point about enhancing memory of dissociatives is interesting. Do you know more about this or have a source?
 
Neuroprotection said:
L type calcium channel blockers are widely used to treat high blood pressure and chest pain/angina pectoris. They include drugs like nimodipine, isaradipine and vyrapamol. However, these substances also block calcium channels in neurons of the CNS and brain, but without significantly altering consciousness at therapeutic levels. They have been shown to have potent neuroprotective affects by blocking excess calcium influx induced by trormer or excitatory amino acids. They also slow or inhibit opioid tolerance in animals.
What are your views?
How about using calcium channel blockers to treat opioid or benzodiazepine withdrawal/addiction, providing you use ones that can cross the blood brain barrier.
I’ve also heard they can enhance memory of a ketamine trip, not sure how that one works, but they are given just before administration of ketamine in hallucinogen assisted psychotherapy.
Click to expand...
The use of L-type Ca channel blockers with ketamine is experimental. Many adjunctive agents have been used in combination with ketamine to try to reduce side effects or make the experience more manageable. Benzodiazepines are commonly used to reduce "emergence reactions".
 
http://www.ncbi.nlm.nih.gov/pubmed/26039257

This paper basically reviews the possible answers to your question. I am not at a computer with access to this journal but, it is very recent and published in a journal dedicated to ion channels and other membrane dynamic thoroughfares.

Based on the text I was able to read it would have more therapeutic use in convulsive, hyper-excitability type disorders. They even propose them (l-type calcium channels) as therapeutic targets for parkinsonism.
 
has anyone used a calcium channel blocker such as vyrapamol, isaradapine etc. more importantly have you taken them along side recreational addictive drugs such as cocaine alcohol, amphetamine and opioids.
If so, how was your experience affected
 
FWIW, the only calcium channel that I know of which is implicated in addiction (specifically, amphetamine) is Cav1.2, which happens to be an L-type calcium channel.
 
Seppi said:
FWIW, the only calcium channel that I know of which is implicated in addiction (specifically, amphetamine) is Cav1.2, which happens to be an L-type calcium channel.
Click to expand...

Is that channel somehow linked to glutamate signalling By the NMDA receptors.
The reason I am interested in L type calcium channel blockers is because they are not psychoactive where as NMDA antagonists are.
Also have you tried any L type calcium channel blocker
 
im curious about these for alcohol addiction. whats the prognosis?
 
Neuroprotection said:
Is that channel somehow linked to glutamate signalling By the NMDA receptors.
The reason I am interested in L type calcium channel blockers is because they are not psychoactive where as NMDA antagonists are.
Also have you tried any L type calcium channel blocker
Click to expand...

These two entities -- NMDA receptors and L-type Ca channels -- have very different functions. L-Type Ca channels are voltage-gated, whereas NMDA receptors are gated by glutamate and glycine. The NMDA receptor can pass calcium but it is not exclusively a calcium channel -- it is also permeable to sodium and potassium.
 
asecin said:
here is a natural source that i have found; https://en.wikipedia.org/wiki/Tetrahydropalmatine which claims ability to help addictive behavior
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Interesting. THP, particularly the L form is thought to act as a sedative by blocking dopamine neurotransmission, and by the same mechanism help reduce drug cravings. However I find one thing about this substance surprising, that is it does not appear to have the same side effects as dopamine antagonist antipsychotics, even though both block dopamine receptors. Does anyone know why this is?
 
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