Gabapentin

Gabapentin is an anti-epileptic medication, also called an anticonvulsant. It affects chemicals and nerves in the body that are involved in the cause of seizures and some types of pain. Gabapentin is used in adults to treat nerve pain caused by the herpes virus or shingles, to treat restless leg syndrome, and to treat seizures. In some cases it can be used as an alternative anti-anxiety medication and is often used to relieve some symptoms of opiate withdrawal.

Introduction to Gabapentin

Gabapentin (brand names Fanatrex, Gabarone, Gralise, Neurontin, Nupentin) is a pharmaceutical drug, specifically a GABA analogue. It was originally developed for the treatment of epilepsy, and currently is also used to relieve neuropathic pain. Gabapentin capsules, tablets, and oral solution are used to help control certain types of seizures in people who have epilepsy. Gabapentin capsules, tablets, and oral solution are also used to relieve the pain of postherpetic neuralgia (PHN; the burning, stabbing pain or aches that may last for months or years after an attack of shingles). Gabapentin extended-release tablets (Horizant) are used to treat restless legs syndrome (RLS; a condition that causes discomfort in the legs and a strong urge to move the legs, especially at night and when sitting or lying down). Gabapentin is in a class of medications called anticonvulsants. Gabapentin treats seizures by decreasing abnormal excitement in the brain. Gabapentin relieves the pain of PHN by changing the way the body senses pain.

Using Gabapentin

Ways of Administration

Neurontin® (gabapentin) Capsules, Neurontin (gabapentin) Tablets, and Neurontin (gabapentin) Oral Solution are supplied as imprinted hard shell capsules containing 100 mg, 300 mg, and 400 mg of gabapentin, elliptical film-coated tablets containing 600 mg and 800 mg of gabapentin or an oral solution containing 250 mg/5 mL of gabapentin

Effects of Gabapentin

Combinations with Gabapentin

Different Uses for Gabapentin

Though not controlled gabapentin does have psychoactive properties that give it the potential at least for recreational use, even at low doses, gabapentin has been known to reduce acute pain and create a calming effect reducing anxiety and even making one overly social and talkative. Tolerance to gabapentin happens extremely rapidly with recreational use. Recreational users have been known to have needed to double their dosage within a couple of days of misuse.
Due to a perceived low bioavailability, there is a commonly reported method of Gabapentin usage known as “Staggering”, this from drug experience sharing websites on the internet. This form of Gabapentin abuse involves taking more than the prescribed daily amount of the drug, often over intervals of half hours or longer. The users have feelings ranging from euphoria to nausea and chest tension. There is also a risk of gastrointestinal side effects when extremely high doses are ingested, causing severe diarrhea, with doses in excess of 4800 mg or more over the course of one day. This some believe could be due to the large quantities of binders and fillers in the gabapentin. Though there is a good possibility that the sheer volume of the alkaloid itself that is needed to achieve recreational effects may be the cause of this gastrointestinal side effect. The reason for the staggering is to maximize the saturation along gabapentin’s main transporter. Due to the fact that gabapentin’s mechanism for action remains relatively unknown, especially on its effects on bipolar and other psychological disorders, the tendency of users to experiment and self-regulate the drug should be considered when examining its adverse effects. Other reported experimental methods of recreational abuse are chewing the time released pills and swallowing or letting it be absorbed by the lining of the mouth. There have been incidents reported of abusers snorting the removed powdery substance also. This type of ingestion is highly ill-advised and abuses such as this led to the removal gabapentin from some of California’s State Prisons.

Pharmacology of Gabapentin


The inactive ingredients for the tabletswhich ones? are poloxamer 407, copolyvidonum, cornstarch, magnesium stearate, hydroxypropyl cellulose, talc, candelilla wax and purified water.
The inactive ingredients for the oral solutionwhich one? are glycerin, xylitol, purified water and artificial cool strawberry anise flavor.

Chemistry of Gabapentin

Column 1 Column 2
Systematic(IUPAC) name: 1-(aminomethyl)cyclohexaneacetic acid
Synonyms: CI-945, Gö-3450, GOE-3450, Gralise, Neurontin
Molecular Formula: C9H17NO2
Molar mass: 171.24 g/mol [1]
CAS Registry Number: 60142-96-3
Melting Point: 162-166°C[2], also reported 165-167°C[2]
Boiling Point: no data
Flash Point: no data
Solubility: Freely soluble in water and in alkaline and acidic solutions[2]
Additionnal data: pKa1 3.68[2], pKa2 10.70 @ 25°C[2]; Isoeletric point 7.14[2]; Partition coefficient (octanol/buffer) 0.075 @ pH 7.4[2]
Notes: Aspect: white to off-white crystalline solid[2]; bitter taste[2]; crystallized from ethanol/ether[2]

The Dangers of Gabapentin

Producing Gabapentin

Forms of Gabapentin

Gabapentin is typically given in capsule form, most often in 100, 200, 300 and 400mg sizes. Although tablets up to 600mg are available.

Legal Status of Gabapentin

United Nations

USA

Gabapentin (Neurontin) is not a scheduled drug in the U.S. However it is only available by prescription meaning that the distribution and sales are allowed only by those with a license and only to those with a prescription, this according to FDA regulations. It should be said also that Possession is not illegal even without a prescription.

EU

References

  1. ^Calculated from Atomic Weights of the Elements, 2007
  2. ^ a b c d e f g h i jMerck Index, fifteenth edition (2013)

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