Gabapentine
Brand names,
Gabapentine
Analogs
Gabapentine
Brand Names Mixture
Gabapentine
Chemical_Formula
C9H17NO2
Gabapentine
RX_link
http://www.rxlist.com/cgi/generic/gabapent.htm
Gabapentine
fda sheet
Gabapentine
msds (material safety sheet)
Gabapentine
Synthesis Reference
G Satzinger et al., U.S. Pat. 4,024,175 (1977).
Gabapentine
Molecular Weight
171.237 g/mol
Gabapentine
Melting Point
162-166 oC
Gabapentine
H2O Solubility
4490 mg/L
Gabapentine
State
Solid
Gabapentine
LogP
0.828
Gabapentine
Dosage Forms
Capsule; Tablet (oral); Solution (oral)
Gabapentine
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.
Gabapentine
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.
Gabapentine
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).
Gabapentine
side effects and Toxicity
Symptoms of overdose include ataxia, labored breathing, ptosis, sedation, hypoactivity, and excitation.
Gabapentine
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.
Gabapentine
Organisms Affected
Humans and other mammals