Drug info - Gabapentin (Neurontin)

[Nicaine]

Got a bunch of Neurontin (gabapentin) from an older prescription I never used much of. Mostly been using it as an occasional sleep aid, but it's an interesting buzz in itself... mostly drowsiness & cottonmouth, but some alcohol-like impairment as well, along with benzo-like relaxation. A kind of heavy feeling in the head & limbs. Dizziness is apparently a common side effect, but I never get that.

Worth a try if anyone has some around, 600mg to 900mg is a good dosage.

Definitely helps with sleep, if nothing else.Edited by: Nicaine

[thechimpo]

SWIMhas this stuff called neurontin/gabapentin (i think its the same thing)


SWIM is wondering if SWIM takes like a bunch of them while on 1.25mg of Klonopin if it will fuck SWIM up?

[allyourbase]

neurontin causes hepatic cancer

[tinogsx]

I'm pretty sure if you mix those to that they will fuck you up. Be careful when doing this experiment. They both can make you very drowsy.

[Nicaine]

Originally Posted by thechimpo

SWIM*has this stuff called neurontin/gabapentin (i think its the same thing)


SWIM is wondering if SWIM takes like a bunch of them while on 1.25mg of Klonopin if it will fuck SWIM up?

Not really. I have a script for Klonopin, and have taken Neurontin with it. The "high" rather sux, makes you drowsy, heavy feeling, etc. with no real pleasure to speak of (YMMV).

BTW it's very difficult to overdose on Neurontin, the toxic dosage is some ridiculously high figure. You'd probably choke to death on the pills first. Edited by: Nicaine

[bandito]

Originally Posted by allyourbase

neurontin causes hepatic cancer

Where did you hear/read this? Can you post any links please?

Bandito.

[Fantasian]

SWIF will recently be prescribed Gabapentin for pain, he intends to use it legitimately for this use. He has however come aware that there are apparent recreational uses but isnt sure what they are. Here is something he pulled of WIkipedia could anyone further expand on this.

Abuse Potential
Though Gabapentin is not a controlled substance, it does produce psychoactive effects that could lead to abuse of the drug. However, it is widely regarded as having little or no abuse potential. As to why, it is unknown. Pregabalin, a Gabapentinoid with higher potency marketed for neuropathic pain, is a controlled substance, under the DEA schedule 5; akin to codeine-based cough syrup

[old hippie 56]

Wife takes them for her MS, they are linked to suicide and depression.

[Forthesevenlakes]

swim has found that gabapentin has had some use for dealing with social anxiety. many of the recreational users who report on erowid say that it makes them socially outgoing, act silly, makes movements uncooridinated, etc. to swim these sound like they are due to some action at the gaba receptor; even though its not a benzo, their trip reports remind swim somewhat of a person who has taken a low dose of a benzo or drank a bit. the synergism with alcohol would lend some support to the gaba agonist idea.

interestingly the manufacturer of gabapentin, parke-davis, got into a lot of trouble reccomending that the drug be prescribed for many things that it had not been proven to treat! its a shocking display of callous greed on the part of the pharmaceutical industry, and is worth reading, so here's the link!

[BUZZFACTOR]

Swim's friend was diagnosed with bipolar disorder and he reports that it greatly helps the anxiety and keeps manic episodes to a minimum, along with controlling depression. Swim would like to hear from others who are taking neurontin, their daily dosages and experience with it. Friend's daily dose is 800 mg. three times daily.

[Broshious]

Swim originally ordered Gabapentin online to try for social anxiety. Swim took 600mg didn't feel much. Swim took 1.2g didn't feel much. Swim too 1.8g and Swim felt WONDERFUL. Not only does it make you kinda drunk, but even after it has worn off Swim feels good. Swim then got a prescription for 600mg twice daily. Swim tried just taking 600mg again and Swim noticed that in situations that would normally make him very anxious Swim didn't feel the anxiety. So taking a normal does seems to be a more subtle treatment for social anxiety while taking large doses(Swim is up to using around 3.6g now) have very obvious effects.

[monkeygone2heaven]

it's a anticonvulsant (anti-epileptic, ie, seizure) drug sometimes used also for pain and psychiatric conditions, largely due to aggressive marketing on the pharmacologic company's part no necessarily because it is the best treatment...

do you really want to experiment?? well you can go ahead take a few althoug i don't recomment... it's not fun!! it has serious side effects - kidney, liver issues as well as serious weight gain.. as for its menta; effects... it's trade name is "neurontin" and doctors lovingly call it "morontin"... guess why?

this is one drug which has little recreational enjoyment. i am shocked to hear that young people are talking about taking it recreationally. hey i believe in freedom. go fo it!! if you enjoy not getting high but ruining your interna organs whilst being mentally slow and also want to put on weight...

all this info is freely available online people!! read about what you put into your body!

jeeez

Dr Monkey, PhD.

[BobTheGreat]

Swim was recently prescribed gababpentin for anxiety problems. He has seached the forums and found no real information on gabapentin. There were some mentions of it in the lyrica thread but no real solid information.

Gabapentin is described as 1-(aminomethyl)cyclohexaneacetic acid with a molecular formula of
C9H17NO2 and a molecular weight of 171.24. Gabapentin is a white to off-white crystalline solid with a pKa1 of 3.7 and a pKa2 of 10.7. It is
freely soluble in water and both basic and acidic aqueous solutions. The log of the partition
coefficient (n-octanol/0.05M phosphate buffer) at pH 7.4 is –1.25.

CLINICAL PHARMACOLOGY

Mechanism of Action

Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but
it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into
GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation.
Gabapentin was tested in radioligand binding assays at concentrations up to 100 μM and did not
exhibit affinity for a number of other common receptor sites, including benzodiazepine,
glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or
strychnine-sensitive glycine, alpha 1, alpha 2, or beta adrenergic, adenosine A1 or A2,
cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, serotonin S1 or S2,
opiate mu, delta or kappa, cannabinoid 1, voltage-sensitive calcium channel sites labeled with
nitrendipine or diltiazem, or at voltage-sensitive sodium channel sites labeled with
batrachotoxinin A 20-alpha-benzoate. Furthermore, gabapentin did not alter the cellular uptake
of dopamine, noradrenaline, or serotonin.
In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of
rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain
tissue has been identified as an auxiliary subunit of voltage-activated calcium channels.
However, functional correlates of gabapentin binding, if any, remain to be elucidated.

Pharmacokinetics and Drug Metabolism

All pharmacological actions following gabapentin administration are due to the activity of the
parent compound; gabapentin is not appreciably metabolized in humans.

Oral Bioavailability: Gabapentin bioavailability is not dose proportional; i.e., as dose is
increased, bioavailability decreases. Bioavailability of gabapentin is approximately 60%, 47%,
34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day given in 3 divided
doses, respectively. Food has only a slight effect on the rate and extent of absorption of
gabapentin (14% increase in AUC and Cmax).
Distribution: Less than 3% of gabapentin circulates bound to plasma protein. The apparent
volume of distribution of gabapentin after 150 mg intravenous administration is 58±6 L (Mean
±SD). In patients with epilepsy, steady-state predose (Cmin) concentrations of gabapentin in
cerebrospinal fluid were approximately 20% of the corresponding plasma concentrations.

Elimination:
Gabapentin is eliminated from the systemic circulation by renal excretion as
unchanged drug. Gabapentin is not appreciably metabolized in humans.
Gabapentin elimination half-life is 5 to 7 hours and is unaltered by dose or following multiple
dosing. Gabapentin elimination rate constant, plasma clearance, and renal clearance are directly
proportional to creatinine clearance. In elderly patients, and in patients with impaired renal function, gabapentin plasma
clearance is reduced. Gabapentin can be removed from plasma by hemodialysis.
Dosage adjustment in patients with compromised renal function or undergoing hemodialysis is
recommended.
Age: The effect of age was studied in subjects 20-80 years of age. Apparent oral clearance
(CL/F) of gabapentin decreased as age increased, from about 225 mL/min in those under 30
years of age to about 125 mL/min in those over 70 years of age. Renal clearance (CLr) and CLr
adjusted for body surface area also declined with age; however, the decline in the renal clearance
of gabapentin with age can largely be explained by the decline in renal function. Reduction of
gabapentin dose may be required in patients who have age related compromised renal function.


Drug Interactions

In vitro studies were conducted to investigate the potential of gabapentin to inhibit the major
cytochrome P450 enzymes (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and
CYP3A4) that mediate drug and xenobiotic metabolism using isoform selective marker
substrates and human liver microsomal preparations. Only at the highest concentration tested
(171 μg/mL; 1 mM) was a slight degree of inhibition (14%-30%) of isoform CYP2A6 observed.
No inhibition of any of the other isoforms tested was observed at gabapentin concentrations up to
171 μg/mL (approximately 15 times the Cmax at 3600 mg/day).
Gabapentin is not appreciably metabolized nor does it interfere with the metabolism of
commonly coadministered antiepileptic drugs.
The drug interaction data described in this section were obtained from studies involving healthy
adults and adult patients with epilepsy.

Phenytoin: In a single (400 mg) and multiple dose (400 mg TID) study of Neurontin in epileptic
patients (N=8) maintained on phenytoin monotherapy for at least 2 months, gabapentin had no
effect on the steady-state trough plasma concentrations of phenytoin and phenytoin had no effect
on gabapentin pharmacokinetics.

Carbamazepine: Steady-state trough plasma carbamazepine and carbamazepine 10, 11 epoxide
concentrations were not affected by concomitant gabapentin (400 mg TID; N=12)
administration. Likewise, gabapentin pharmacokinetics were unaltered by carbamazepine
administration.

Valproic Acid: The mean steady-state trough serum valproic acid concentrations prior to and
during concomitant gabapentin administration (400 mg TID; N=17) were not different and
neither were gabapentin pharmacokinetic parameters affected by valproic acid.

Phenobarbital: Estimates of steady-state pharmacokinetic parameters for phenobarbital or
gabapentin (300 mg TID; N=12) are identical whether the drugs are administered alone or
together.

Naproxen: Coadministration (N=18) of naproxen sodium capsules (250 mg) with Neurontin
(125 mg) appears to increase the amount of gabapentin absorbed by 12% to 15%. Gabapentin
had no effect on naproxen pharmacokinetic parameters. These doses are lower than the
therapeutic doses for both drugs. The magnitude of interaction within the recommended dose
ranges of either drug is not known.

Hydrocodone: Coadministration of Neurontin (125 to 500 mg; N=48) decreases hydrocodone
(10 mg; N=50) Cmax and AUC values in a dose-dependent manner relative to administration of
hydrocodone alone; Cmax and AUC values are 3% to 4% lower, respectively, after administration
of 125 mg Neurontin and 21% to 22% lower, respectively, after administration of 500 mg
Neurontin. The mechanism for this interaction is unknown. Hydrocodone increases gabapentin
AUC values by 14%. The magnitude of interaction at other doses is not known.

Morphine: A literature article reported that when a 60-mg controlled-release morphine capsule
was administered 2 hours prior to a 600-mg Neurontin capsule (N=12), mean gabapentin AUC
increased by 44% compared to gabapentin administered without morphine. Morphine pharmacokinetic parameter values were not affected by administration of Neurontin 2 hours after morphine. The magnitude of interaction at other doses
is not known.

Cimetidine: In the presence of cimetidine at 300 mg QID (N=12) the mean apparent oral
clearance of gabapentin fell by 14% and creatinine clearance fell by 10%. Thus cimetidine
appeared to alter the renal excretion of both gabapentin and creatinine, an endogenous marker of
renal function. This small decrease in excretion of gabapentin by cimetidine is not expected to be
of clinical importance. The effect of gabapentin on cimetidine was not evaluated.

Oral Contraceptive: Based on AUC and half-life, multiple-dose pharmacokinetic profiles of
norethindrone and ethinyl estradiol following administration of tablets containing 2.5 mg of
norethindrone acetate and 50 mcg of ethinyl estradiol were similar with and without
coadministration of gabapentin (400 mg TID; N=13). The Cmax of norethindrone was 13%
higher when it was coadministered with gabapentin; this interaction is not expected to be of
clinical importance.

Antacid (Maalox®): Maalox reduced the bioavailability of gabapentin (N=16) by about 20%.
This decrease in bioavailability was about 5% when gabapentin was administered 2 hours after
Maalox. It is recommended that gabapentin be taken at least 2 hours following Maalox
administration.

Effect of Probenecid: Probenecid is a blocker of renal tubular secretion. Gabapentin
pharmacokinetic parameters without and with probenecid were comparable. This indicates that
gabapentin does not undergo renal tubular secretion by the pathway that is blocked by
probenecid.

Drug/Laboratory Tests Interactions

Because false positive readings were reported with the Ames N-Multistix SG® dipstick test for
urinary protein when gabapentin was added to other antiepileptic drugs, the more specific
sulfosalicylic acid precipitation procedure is recommended to determine the presence of urine
protein.

Carcinogenesis, Mutagenesis, Impairment of Fertility
Gabapentin was given in the diet to mice at 200, 600, and 2000 mg/kg/day and to rats at 250,
1000, and 2000 mg/kg/day for 2 years. A statistically significant increase in the incidence of
pancreatic acinar cell adenomas and carcinomas was found in male rats receiving the high dose;
the no-effect dose for the occurrence of carcinomas was 1000 mg/kg/day. Peak plasma
concentrations of gabapentin in rats receiving the high dose of 2000 mg/kg were 10 times higher
than plasma concentrations in humans receiving 3600 mg per day, and in rats receiving
1000 mg/kg/day peak plasma concentrations were 6.5 times higher than in humans receiving
3600 mg/day. The pancreatic acinar cell carcinomas did not affect survival, did not metastasize
and were not locally invasive. The relevance of this finding to carcinogenic risk in humans is
unclear.
Studies designed to investigate the mechanism of gabapentin-induced pancreatic carcinogenesis
in rats indicate that gabapentin stimulates DNA synthesis in rat pancreatic acinar cells in vitro
and, thus, may be acting as a tumor promoter by enhancing mitogenic activity. It is not known
whether gabapentin has the ability to increase cell proliferation in other cell types or in other
species, including humans.
Gabapentin did not demonstrate mutagenic or genotoxic potential in three in vitro and four in
vivo assays. It was negative in the Ames test and the in vitro HGPRT forward mutation assay in
Chinese hamster lung cells; it did not produce significant increases in chromosomal aberrations
in the in vitro Chinese hamster lung cell assay; it was negative in the in vivo chromosomal
aberration assay and in the in vivo micronucleus test in Chinese hamster bone marrow; it was
negative in the in vivo mouse micronucleus assay; and it did not induce unscheduled DNA
synthesis in hepatocytes from rats given gabapentin.
No adverse effects on fertility or reproduction were observed in rats at doses up to 2000 mg/kg
(approximately 5 times the maximum recommended human dose on a mg/m2 basis).

Pregnancy
Pregnancy Category C: Gabapentin has been shown to be fetotoxic in rodents, causing delayed
ossification of several bones in the skull, vertebrae, forelimbs, and hindlimbs. These effects
occurred when pregnant mice received oral doses of 1000 or 3000 mg/kg/day during the period
of organogenesis, or approximately 1 to 4 times the maximum dose of 3600 mg/day given to
epileptic patients on a mg/m2 basis. The no-effect level was 500 mg/kg/day or approximately ½
of the human dose on a mg/m2 basis.
When rats were dosed prior to and during mating, and throughout gestation, pups from all dose
groups (500, 1000 and 2000 mg/kg/day) were affected. These doses are equivalent to less than
approximately 1 to 5 times the maximum human dose on a mg/m2 basis. There was an increased
incidence of hydroureter and/or hydronephrosis in rats in a study of fertility and general
reproductive performance at 2000 mg/kg/day with no effect at 1000 mg/kg/day, in a teratology
study at 1500 mg/kg/day with no effect at 300 mg/kg/day, and in a perinatal and postnatal study
at all doses studied (500, 1000 and 2000 mg/kg/day). The doses at which the effects occurred are
approximately 1 to 5 times the maximum human dose of 3600 mg/day on a mg/m2 basis; the noeffect
doses were approximately 3 times (Fertility and General Reproductive Performance study)
and approximately equal to (Teratogenicity study) the maximum human dose on a mg/m2 basis.
Other than hydroureter and hydronephrosis, the etiologies of which are unclear, the incidence of
malformations was not increased compared to controls in offspring of mice, rats, or rabbits given
doses up to 50 times (mice), 30 times (rats), and 25 times (rabbits) the human daily dose on a
mg/kg basis, or 4 times (mice), 5 times (rats), or 8 times (rabbits) the human daily dose on a
mg/m2 basis.
In a teratology study in rabbits, an increased incidence of postimplantation fetal loss occurred in
dams exposed to 60, 300, and 1500 mg/kg/day, or less than approximately ¼ to 8 times the
maximum human dose on a mg/m2 basis. There are no adequate and well-controlled studies in
pregnant women. This drug should be used during pregnancy only if the potential benefit
justifies the potential risk to the fetus.

Use in Nursing Mothers
Gabapentin is secreted into human milk following oral administration. A nursed infant could be
exposed to a maximum dose of approximately 1 mg/kg/day of gabapentin. Because the effect on
the nursing infant is unknown, Neurontin should be used in women who are nursing only if the
benefits clearly outweigh the risks.

DRUG ABUSE AND DEPENDENCE

The abuse and dependence potential of Neurontin has not been evaluated in human studies.

OVERDOSAGE
A lethal dose of gabapentin was not identified in mice and rats receiving single oral doses as
high as 8000 mg/kg. Signs of acute toxicity in animals included ataxia, labored breathing, ptosis,
sedation, hypoactivity, or excitation.
Acute oral overdoses of Neurontin up to 49 grams have been reported. In these cases, double
vision, slurred speech, drowsiness, lethargy and diarrhea were observed. All patients recovered
with supportive care.
Gabapentin can be removed by hemodialysis. Although hemodialysis has not been performed in
the few overdose cases reported, it may be indicated by the patient’s clinical state or in patients
with significant renal impairment.



Swim will write his experiences with the drug tommorrow after some rest.

[Laudaphun]

Ok, once a crackhead tried to give SWIM a bottle of these things knowing SWIM liked pills... SWIM said he didn't want them, but neither did the crackhead so she just gave them to SWIM for free. SWIM would take a couple of them at a time here and there when he was without anything else... The only effects SWIM noted were sleep and strange dreams... always strange dreams. Not really pleasant, not really unpleasant... just weird. Definitely no euphoria or buzz. SWIM supposes that used for an actual medical purpose they might be ok. SWIM would not recommend trying to abuse these.

[Ontherooftops]

GP is one of SWIM's favorite pharms, however SWIY should use much more than they expect. A close friend of SWIM's has shared his script of GP many times with SWIM. The ex