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Gabapentin: Difference between revisions
>NaYeahMate m Added appetite enhancement effect. |
>Gabapentinoid m Altered and clarified description of pharmacological effects on GABA biosynthesis and Voltage-Gated Calcium Channels. |
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The bioavailability of gabapentin is relatively low and is inversely proportional to the dose. This means that higher doses have lower biovailability than lower doses. The bioavailability of gabapentin is approximately 60%, 47%, | The bioavailability of gabapentin is relatively low and is inversely proportional to the dose. This means that higher doses have lower biovailability than lower doses. The bioavailability of gabapentin is approximately 60%, 47%, | ||
34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day<ref>Neurontin Clinical Pharmacology Biopharmaceutics Review | http://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21-397.pdf_Neurontin_BioPharmr.pdf</ref> Eating a high fat meal substantially increases gabapentin's bioavailability.<ref> Gabapentin data sheet | http://reference.medscape.com/drug/neurontin-gralise-gabapentin-343011#showall</ref> | 34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day<ref>Neurontin Clinical Pharmacology Biopharmaceutics Review | http://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21-397.pdf_Neurontin_BioPharmr.pdf</ref> Eating a high fat meal substantially increases gabapentin's bioavailability.<ref>Gabapentin data sheet | http://reference.medscape.com/drug/neurontin-gralise-gabapentin-343011#showall</ref> | ||
==Chemistry== | ==Chemistry== | ||
Gabapentin, or 1-(aminomethyl)cyclohexanacetic acid, is an analogue of the neurotransmitter [[GABA]]. It contains a cyclohexane ring bound to a methylamino chain CH<sub>3</sub>NH<sub>2</sub>. At the same location, R<sub>1</sub>, 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 R<sub>3</sub> of the butanoic acid chain in GABA incorporated into an attached cyclohexane ring, converting it into a tertiary carbon while still maintaining the chain. | Gabapentin, or 1-(aminomethyl)cyclohexanacetic acid, is an analogue of the neurotransmitter [[GABA]]. It contains a cyclohexane ring bound to a methylamino chain CH<sub>3</sub>NH<sub>2</sub>. At the same location, R<sub>1</sub>, 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 R<sub>3</sub> 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== | ==Pharmacology== | ||
Gabapentin modulates the action of [[glutamate]] decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in [[GABA]] biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro.<ref>Mechanisms of action of gabapentin (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9686247</ref> As the GABA system is the most prolific inhibitory receptor set within the brain, its | Gabapentin modulates the action of [[glutamate]] decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in [[GABA]] biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro.<ref>Mechanisms of action of gabapentin (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9686247</ref> As the GABA system is the most prolific inhibitory receptor set within the brain, its increase in biosynthesis results in the [[sedating]] and anxiolytic (or [[Anxiety suppression|calming effects]]) of gabapentin on the nervous system. | ||
Gabapentin has also been shown to bind to the α2δ-1 | Gabapentin, as a gabapentinoid, has also been shown to bind to the α2δ-1 subunits of Voltage-Gated Calcium Channels to act as a VGCC blocker, which contributes to its inhibitory, analgesic, and anxiolytic effects. It is uncertain exactly how this method of action contributes to gabapentin's psychoactive effects. | ||
==Subjective effects== | ==Subjective effects== | ||
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*'''[[Effect::Dizziness]]''' - This effect is particularly prevalent at higher doses. It should be noted that the dizziness experienced on gabapentin is not always considered overly unpleasant and many users may not necessarily mind it. | *'''[[Effect::Dizziness]]''' - This effect is particularly prevalent at higher doses. It should be noted that the dizziness experienced on gabapentin is not always considered overly unpleasant and many users may not necessarily mind it. | ||
*'''[[Effect::Seizure suppression]]''' - Gabapentin is commonly used as an anticonvulsant. It is often combined with other anticonvulsants when used to treat epilepsy and other seizure disorders. | *'''[[Effect::Seizure suppression]]''' - Gabapentin is commonly used as an anticonvulsant. It is often combined with other anticonvulsants when used to treat epilepsy and other seizure disorders. | ||
*'''[[Effect::Pain relief]]''' - Gabapentin is used to control pain, particularly pain | *'''[[Effect::Pain relief]]''' - Gabapentin is used to control pain, particularly fibromyalgic/neuropathic pain (nerve pain) and [[restless leg syndrome]]. It is generally considered to be not very effective for the management of acute pain, such as [[opiates]]. | ||
*'''[[Effect::Muscle twitching]]''' | *'''[[Effect::Muscle twitching]]''' | ||
*'''[[Effect::Motor control loss]]''' | *'''[[Effect::Motor control loss]]''' | ||
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===Lethal dosage=== | ===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.<ref> 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.</ref> | 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.<ref>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.</ref> | ||
===Tolerance and addiction potential=== | ===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]]. | 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]]. | ||
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==References== | ==References== | ||
<references /> | <references /> | ||
[[Category:Psychoactive substance]][[Category:Substance]][[Category:Depressant]] | [[Category:Psychoactive substance]] | ||
[[Category:Substance]] | |||
[[Category:Depressant]] | |||
[[Category:Anxiolytics]] | [[Category:Anxiolytics]] | ||
[[Category:Gabapentinoid]] | [[Category:Gabapentinoid]] | ||