Gabapentin
Brand names,
Gabapentin
Analogs
Gabapentin
Brand Names Mixture
Gabapentin
Chemical_Formula
C9H17NO2
Gabapentin
RX_link
http://www.rxlist.com/cgi/generic/gabapent.htm
Gabapentin
fda sheet
Gabapentin
msds (material safety sheet)
Gabapentin
Synthesis Reference
G Satzinger et al., U.S. Pat. 4,024,175 (1977).
Gabapentin
Molecular Weight
171.237 g/mol
Gabapentin
Melting Point
162-166 oC
Gabapentin
H2O Solubility
4490 mg/L
Gabapentin
State
Solid
Gabapentin
LogP
0.828
Gabapentin
Dosage Forms
Capsule; Tablet (oral); Solution (oral)
Gabapentin
Indication
For the management of postherpetic neuralgia in adults and as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in patients over 12 years of age with epilepsy.
Gabapentin
Pharmacology
Gabapentin, an analog of GABA, is used as an anticonvulsant to treat partial seizures, amyotrophic lateral sclerosis (ALS), and painful neuropathies. Potential uses include monotherapy of refractory partial seizure disorders, and treatment of spasticity in multiple sclerosis, tremor. mood disorders, and attenuation of disruptive behaviors in dementia. Gabapentin has high lipid solubility, is not metabolized by the liver, has no protein binding, and doesn't possess the usual drug interactions.
Gabapentin
Absorption
Rapid. Absorbed in part by the L-amino acid transport system, which is a carrier-mediated, saturable transport system; as the dose increases, bioavailability decreases. Bioavailability ranges from approximately 60% for a 900 mg dose per day to approximately 27% for a 4800 milligram dose per day. Food has a slight effect on the rate and extent of absorption of gabapentin (14% increase in AUC).
Gabapentin
side effects and Toxicity
Symptoms of overdose include ataxia, labored breathing, ptosis, sedation, hypoactivity, and excitation.
Gabapentin
Patient Information
Patients should be instructed to take Neurontin only as prescribed.
Patients should be advised that Neurontin may cause dizziness, somnolence and other symptoms and signs of CNS
depression. Accordingly, they should be advised neither to drive a car nor to operate other complex machinery until
they have gained sufficient experience on Neurontin to gauge whether or not it affects their mental and/or motor
performance adversely. Patients who require concomitant treatment with morphine may experience increases in
gabapentin concentrations. Patients should be carefully observed for signs of CNS depression, such as somnolence, and
the dose of Neurontin or morphine should be reduced appropriately.
Gabapentin
Organisms Affected
Humans and other mammals