Gabapentin
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Gabapentin
The skeletal formula of gabapentin
Gabapentin1.png
Gabapentin 3D.png
Chemical Nomenclature
Common names GABApentin, Neurontin, Gabarone, Gralise
Substitutive name 1-(aminomethyl)cyclohexaneacetic acid
Class Membership
Psychoactive class Depressant
Chemical class GABAergic
Routes of Administration



Oral
Dosage
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is a summary of data gathered from users and resources. It is not a recommendation and should be verified with other sources for accuracy.
Common 50 - 300 mg
Duration
Total 5 - 7 hours









Summary sheet: Gabapentin
A capsule of Gabapentin

Gabapentin (marketed under the brand name Neurontin) is a medication used as an anticonvulsant, analgesic and anxiolytic. It was originally developed to treat epilepsy and is currently used to relieve neuropathic pain and restless leg syndrome.[1] It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.[2]

Gabapentin is also an effective tool for treating social anxiety disorder, panic disorder[3][4] and generalized anxiety disorder.[5][6] It is these effects which provide gabapentin with some recreational potential in a manner that can be accurately compared to a mild benzodiazepine. However, these recreational effects diminish with repeated usage and are most commonly reported by those who try this compound who do not have a tolerance.

Chemistry

Gabapentin, or 1-(aminomethyl)cyclohexanacetic acid, is an analogue of the neurotransmitter GABA. It contains a cyclohexane ring bound to a methylamino chain CH3-NH<2. At the same location, R1, the cyclohexane ring is also substituted with an acetic acid group. Gabapentin is structurally analagous to GABA. GABA contains an amino group bound to the terminal carbon of a butanoic acid chain. The structure of gabapentin contains the secondary carbon 3 of the butanoic acid chain in GABA incorporated into an attached cyclohexane ring, converting it into a tertiary carbon while still maintaining the chain.

Pharmacology

The mechanism of action of gabapentin is not fully understood and continues to remain elusive. It was initially created to mimic the structure of the neurotransmitter GABA, but gabapentin has no effect on GABA binding, uptake, or degradation. In contrast to other anticonvulsant drugs, gabapentin has not been shown to interact with L-type calcium ion channels. Additionally, gabapentin does not interact with glutamate, NDMA, or glycine receptors.

One possible mechanism for action of gabapentin is its interaction with voltage gated calcium channels. Gabapentin binds to the α2δ subunit (1 and 2) and has been found to reduce calcium currents after chronic (but not acute) application via an effect on trafficking of voltage-dependent calcium channels in the central nervous system.

Gabapentin also modulates the enzymes glutamate decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in GABA synthesis. This suggests a potential mechanism of action that is not fully discovered yet.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Cognitive effects

Physical effects

Toxicity and harm potential

The most common side effects of gabapentin in adult patients include dizziness, fatigue, drowsiness, weight gain, and peripheral edema (swelling of extremities).[7] Gabapentin may also produce sexual dysfunction in some patients whose symptoms of which may include loss of libido, inability to reach orgasm, and erectile dysfunction.[8][9] Gabapentin should be used carefully in patients with renal impairment due to possible accumulation and toxicity.[10]

Suicide

In 2009, the U.S. Food and Drug Administration issued a warning of an increased risk of depression and suicidal thoughts and behaviors in patients taking gabapentin (along with other anticonvulsant drugs),[11] modifying the packaging insert to reflect this. A 2010 meta analysis confirmed the increased risk of suicide associated with gabapentin use.[12]

Lethal dosage

People who accidentally or intentionally overdose may experience drowsiness, sedation, blurred vision, slurred speech, somnolence and possibly death (if a very high amount was taken and particularly if combined with alcohol). Serum gabapentin concentrations may be measured to confirm diagnosis.[13]

Tolerance and addiction potential

Gabapentin is not considered psychologically addictive. However, it is possible to develop a physical dependence on the drug. In fact, people can experience withdrawal symptoms for up to 45 days after they stop taking gabapentin. Although gabapentin does give some people a euphoric “high” which can cause abuse, gabapentin abusers do not present with the kind of compulsive, drug-seeking behavior or strong cravings associated with other more common depressants such as opioids, alcohol or benzodiazepines.

Dangerous combinations

Gabapentin significantly potentates the effects of alcohol and benzodiazepines, which may lead to blackouts.

Legal issues

Gabapentin is a prescription only medicine and can only be prescribed following a consultation with a doctor. It is therefore illegal to possess or sell in most parts of the world.

See also

External links

References

  1. ↑ Restless legs syndrome: clinical presentation diagnosis and treatment | http://www.sleep-journal.com/article/S1389-9457(15)00647-4/abstract
  2. ↑ EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision | https://www.ncbi.nlm.nih.gov/pubmed/20402746
  3. ↑ The role of anticonvulsant drugs in anxiety disorders: a critical review of the evidence | https://www.ncbi.nlm.nih.gov/pubmed/17502773
  4. ↑ Manual of Clinical Psychopharmacology | https://books.google.co.uk/books?id=D3zz1NCm3qcC&pg=PA345&hl=en
  5. ↑ Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | https://books.google.co.uk/books?id=dnAlO_Veu2QC&pg=PA124&hl=en
  6. ↑ https://books.google.co.uk/books?id=82oiYYHGNTQC&pg=PA765&hl=en
  7. ↑ http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020235s041,020882s028,021129s027lbl.pdf
  8. ↑ https://books.google.co.uk/books?id=jTc3AAAAQBAJ&pg=PA137&hl=en
  9. ↑ https://books.google.co.uk/books?id=_VzzAgAAQBAJ&pg=PT482&hl=en
  10. ↑ http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020235s057,020882s041,021129s039lbl.pdf
  11. ↑ http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm100190.htm
  12. ↑ https://www.ncbi.nlm.nih.gov/pubmed/20388896
  13. ↑ R.C. Baselt, Disposition of Toxic Drugs and Chemicals in Man, 8th edition, Biomedical Publications, Foster City, CA, 2008, pp. 677–8. ISBN 978-0-9626523-7-0.
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