March 28, 2023

Gabapentin is a GABA-like drug that has been used medically in the treatment of epilepsy, neuropathic pain, and other conditions.

Gabapentin is a gaba like drug which has been used medically in the treatment of epilepsy and neuropathic pain some people also find the drug offers recreational effects like anxiety reduction sedation in some euphoria it has a complex from ecology that is still not fully understood among its positive effects are anxiety reduction euphoria muscle relaxation sedation

And pain reduction its negative effects include dizziness memory loss erectile dysfunction fatigue drowsiness and reduced control of muscles the substance has primarily been used to reduce seizures in neuropathic pain but it’s sometimes prescribed for insomnia anxiety bipolar disorder and panic disorder some users find it’s difficult to attain any non-medical

Effects from the drug without taking it every so often for a couple hours others however find just taking a relatively large initial dose is adequate to attain effects i’ve seen some reports claiming it offers minor closed or open eye visual distortions which may be true for some users at certain doses but it’s not a core effect of the drug orally gabapentin lasts

For five to eight hours and begins working in thirty to ninety minutes gabapentin is similar in structure to gaba and it’s a member of the gabapentin oi class which is made up of gaba derivatives that share a similar pharmacology the drugs from ecology still isn’t fully understood and different actions could be responsible for different effects and depending on

The effect you’re looking for peripheral rather than central actions may be responsible one possibility is that it increases glutamic acid decarboxylase activity which boosts the conversion of glutamate to gaba concentration is an issue with this mechanism but studies have noted both an increase in gaba and a decrease in glutamate it is known that gabapentin does

Not directly modulate gaba receptor function like benzodiazepines and it’s not a gaba agonist this leaves us with what seems to be a key part of gabapentin activity which is calcium channel block the drug operates at the one in two isoforms of the v dc c alpha 2 delta subunit this action particularly alpha 2 delta 1 appears to be connected to anxiety reduction

Pain relief and anticonvulsant activity it’s important to note that gabapentin s bioavailability significantly declines as the dose increases the drug is dependent on an ella me no acid transport system to absorb through the gi tract as the transporter is saturated less gabapentin can reach its target thereby effectively reducing the dose go deki a german company

Established a program to look for active gaba like drugs in the early 1970s researchers at the company hoped to find a substance that could cross the blood-brain barrier and prove efficacious for conditions like epilepsy and multiple sclerosis a team at go deki led by ger hearts at sanger envisioned a set of 25 gavel like substances in 1973 and then synthesized

Them gabapentin preparation was described in 1975 in its activity in animal models of epilepsy was reported shortly thereafter early studies showed gabapentin was the best drug out of the 25 envisioned by satsanga and the research grew from there eventually the alpha 2 delta subunit was discovered as a target for gabapentin opening up a new area of research it

Was approved in the united states as an add-on seizure treatment in 1993 while it was originally only used for seizures it’s applications have grown since then more recently recreational use has reportedly increased leading some to believe it should be more carefully prescribed and controlled a light oral dose is 300 to 600 milligrams a common dose is 600 to 900

Milligrams and a strong dose is 900 to 1200 milligrams or more some anecdotal reports claim the drug should be administered over a period of one to two hours in order for to provide recreational effects for example using around 300 milligrams every 30 minutes with two to four applications has been recommended by some in the us gabapentin is prescription-only

Meaning its sale is controlled elsewhere it’s usually prescription only or not controlled at all gabapentin is quite safe even insignificant overdoses but there are factors that increase the chance of harm and it can even be deadly it’s not wise to combine the drug with other depressants like alcohol or benzodiazepines also because gabapentin is reliant on the

Kidneys for elimination renal impairment can make common dosas potentially dangerous there are reports of renal impairment and gabapentin use leading to more drowsiness negative changes in mental status and coma few deaths have been reported but there are a number of overdoses that could have been fatal if not for medical attention likely because of the reduced

Bioavailability at higher doses as much as 49 grams has been taken without a fatal response this should not be taken to mean anywhere near 49 grams can be viewed as safe overdoses featuring significant sedation blurred vision slurred speech and death are possible withdrawal does exist with chronic use if you have any questions about gabapentin feel free to leave

Them in the comment section support on patreon is greatly appreciated so if you’d like to contribute you can head to drug classroom you can also contribute through youtube paypal or bitcoin using the addresses and links in the description you can connect me on twitter i set a fitzgerald and via email at seth at the drug classroom comm more

Information and links to references can be found on the tdc website using the link below

Transcribed from video
Gabapentin: What You Need To Know By The Drug Classroom