Harm Reduction All Drugs - Short Half-Life vs. Long Half-Life Drugs

[Lorne???]

^ Its BA^ is also not dose dependent

It is a much better drug and hard to gey addicted to though YMMV

 

[Shant]

A much better drug than what? Gabapentin?

 

[Shant]

Pregabalin has much better bioavailability. It does also have side effects. The memory thing is well documented. When I was taking it I was forgetting so much, I literally felt my IQ had gone down. Tolerance builds super fast with it and then you’re just taking it to stop withdrawals which are fucking horrid. It was one of the worst drugs I’ve had to withdraw from.

However, it’s a brilliant drug as a comfort drug when withdrawing from opiates/opioids. It is brilliant if you have nerve pain and I’ve read a lot to say it is good for anxiety but at the lower doses like 150mg.

That’s great stuff friend, thank you. Can you explain bioavailability and why one should be concerned with it?

 

[Shant]

Btw the gabapentin also is affecting my memory. And I’m also starting to believe that my IQ has gone down. I’m constantly doing stupid shit. Certainly not as sharp or as quick as I used to be. Dunno if it’s all the years of opiate abuse or all the comfort meds I’ve been taking but I’ve definitely lost my fast ball. Hope it comes back...

 

[MsDiz]

Btw the gabapentin also is affecting my memory. And I’m also starting to believe that my IQ has gone down. I’m constantly doing stupid shit. Certainly not as sharp or as quick as I used to be. Dunno if it’s all the years of opiate abuse or all the comfort meds I’ve been taking but I’ve definitely lost my fast ball. Hope it comes back...

Yeah gabapentin affected me in the same way too.

Bioavailability is how much of the drug that enters the circulation after having taken it and is therefore what will have an actual effect on you.

Of 300mg of gabapentin taken orally about 62% of that will go on to have an effect. At 600mg it goes down to 40% and at 900mg it goes right down to around 30% ish.

So you’re gonna get more of the drug into your system by taking 300mg 45 mins apart than you are taking 600mg. Does that make sense?

 

[Shant]

Yes it does, thanks! So it basically means how much of the drug makes it through 1st pass?

 

[Lorne???]

^ Unless you are abusing the hell out of it should not effect memory and certainly not IQ.

I do believe 15 years of drug use/abuse has dropped my high IQ

 

[Lorne???]

Actually @PrincessDiz they did a study and at 1.2 grams bioavailability was hardly effected. At 1.8 grams however it was almost half

So I think 600-800mg spaced apart would be sufficient

 

[MsDiz]

I used gabapentin for 2 years and it affected my memory. I had a year out and started pregabalin which also affected my memory. There are Facebook groups called “lyrics survivors” etc that all have patients who talk about the awful side effects and even worse withdrawal. So it’s not just abuse. I was taking the max dose and never anymore. Not that anymore would be absorbed into the blood stream anyway.

Would love to see the study as I’ve not come across that yet. Do you have the link @Lorne???

 

[Shant]

I’ve been taking 1200 to 1800mg all at once. So does that mean I’m wasting it? But I only do it once or twice a week

 

[Lorne???]

Well I am glad it does not effect me like that

I will try later to find study I am out of opioids

(Although the BA% figures in the study were a little lower than you would expect IIRC which is why I recommend 600-800mg at a time. Taking 300mg, well remember it takes on Average ~4 hours to reach peak plasma levels so you would never feel anything or hardly!

And @Shant cut your dose in half, wait 45 minutes, take other half

 

[Shant]

@Shant cut your dose in half, wait 45 minutes, take other half

Gotcha, thanks Lorne. Why does bioavailability go down as dose goes up?

 

[Lorne???]

Because it relies upon transporters in your GI tract to be absorbed, oversaturate those and it gradually stops absorbing

Hope that helps!

 

[Lorne???]

Gabapentin bioavailability: effect of dose and frequency of administration in adult patients with epilepsy - PubMed

GBP F may be significantly increased by q.i.d. versus t.i.d. dosing, depending upon dose level. This increase in F however must be balanced against the inconvenience of more frequent dosing. Therapeutic drug level monitoring may aid in the evaluation of such pharmacokinetic maneuvers.

pubmed.ncbi.nlm.nih.gov

This is not the study I was talking about(which I cannot find) however interesting nonetheless.

Also found this supposed data:




The oral bioavailability of gabapentin is approximately 80% at 100 mg administered three times daily once every 8 hours, but decreases to 60% at 300 mg, 47% at 400 mg, 34% at 800 mg, 33% at 1,200 mg, and 27% at 1,600 mg, all with the same dosing schedule.

Which does not agree with the study I read and am trying to find
Peace out for now

 

[Lorne???]

Hey everybody read this abstract
Increase

Drugs that increase the transit time of gabapentin in the small intestine can increase its oral bioavailability; when gabapentin was co-administered with oral morphine (which slows intestinal peristalsis), the oral bioavailability of a 600 mg dose of gabapentin increasedby 50%.

So opioid addicts can get more out of gabapentin, @Shant and @PrincessDiz

 

[Deru]

Yeah gabapentin affected me in the same way too.

I was on 600 mg of gabapentin per day after my first heart surgery in combination with all the other pain management, and when I stopped taking gabapentin, I had the most intense suicidal ideations ever. I’ve never once in my life been actually suicidal, it was an incredible experience, to say the least.

So it basically means how much of the drug makes it through 1st pass?

It’s what percentage of the absolute amount of the substance you take that makes it to arterial blood (from the heart’s left ventricle to the aorta and the vast network of arterial vessels that follows.). If you take the drug orally, then yes, after it‘s absorbed into the blood through the stomach and intestinal walls (almost all blood absorbed through intestinal walls is routed through portal system, to the hepatic portal vein to the liver (where first pass occurs), then through the inferior vena cava to the right side of the heart, through the pulmonary circulation (lungs), to the left side of heart and ultimately to arterial blood is where the absolute bioavailability percentage is calculated. Intravenous administration isn’t even always a guaranteed 100% bioavailability because there is sometimes loss in the pulmonary circulation, prior to reaching arterial blood, although for most drugs discussed it is minimal or irrelevant.

 

[Shant]

Hey everybody read this abstract
Increase

Drugs that increase the transit time of gabapentin in the small intestine can increase its oral bioavailability; when gabapentin was co-administered with oral morphine (which slows intestinal peristalsis), the oral bioavailability of a 600 mg dose of gabapentin increasedby 50%.

So opioid addicts can get more out of gabapentin, @Shant and @PrincessDiz

I was just about to ask about that. Makes perfect sense. Thanks for this

 

[Shant]

I was on 600 mg of gabapentin per day after my first heart surgery in combination with all the other pain management, and when I stopped taking gabapentin, I had the most intense suicidal ideations ever. I’ve never once in my life been actually suicidal, it was an incredible experience, to say the least.



It’s what percentage of the absolute amount of the substance you take that makes it to arterial blood (from the heart’s left ventricle to the aorta and the vast network of arterial vessels that follows.). If you take the drug orally, then yes, after it‘s absorbed into the blood through the stomach and intestinal walls (almost all blood absorbed through intestinal walls is routed through portal system, to the hepatic portal vein to the liver (where first pass occurs), then through the inferior vena cava to the right side of the heart, through the pulmonary circulation (lungs), to the left side of heart and ultimately to arterial blood is where the absolute bioavailability percentage is calculated. Intravenous administration isn’t even always a guaranteed 100% bioavailability because there is sometimes loss in the pulmonary circulation, prior to reaching arterial blood, although for most drugs discussed it is minimal or irrelevant.

Great insights. You wouldn’t expect a drug that works on gaba to cause suicidal feelings. I think I’m gonna stop taking it. At the dosages I need it’s just not worth it. Suboxone, ambien, & weed oughta be enough. Appreciate that Deru

 

[Shant]

And if I understand this correctly, wouldn’t that mean that drugs which are smaller physically, like say fentanyl which is measured in mcg, that in itself would increase the bioavailability. Right or wrong?

 

[Lorne???]

Is flubromazolam fast acting?

Great insights. You wouldn’t expect a drug that works on gaba to cause suicidal feelings. I think I’m gonna stop taking it. At the dosages I need it’s just not worth it. Suboxone, ambien, & weed oughta be enough. Appreciate that Deru

Actually Benzodiazepines cause suicidal ideation sometimes.
RIP Chris Cornell

Kurt Cobain also downed a bottle of Valium before he shot himself
(And YES, it was suicide, live with it )