Drug Study
Drug Study
Name Anticonvulsant,
Gabapentin Neurontin mood stabilizer 100 mg PO BID
Peak Onset Duration For IV meds, compatibility with IV drips and /or solutions
2-4 hr rapid 8 hr N/A
Interactions with other patient drugs, OTC or Lab value alterations caused by medicine: May cause
herbal medicines (ask patient specifically) Leukopenia. May cause false-positive readings when
testing for urinary protein with Ames N-Multistix SG
Dilantin (phenytoin)—Neurontin may increase drug dipstick test; use sulfosalicylic acid precipitation
levels of dilantin. procedure.
Zoloft- may cause additive CNS depression effects. Be sure to teach the patient the following about this
medication:
INDICATION: Gabapentin is a cyclohexane-gamma- May cause dizziness and drowsiness. Do not take within 2
aminobutyric acid derivative that is used for the hrs of antacid.
treatment of PARTIAL SEIZURES; NEURALGIA; and
RESTLESS LEGS SYNDROME.
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.
Pharmacodynamics
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.
Mechanism of action
Gabapentin interacts with cortical neurons at auxillary subunits of voltage-sensitive
calcium channels. Gabapentin increases the synaptic concentration of GABA, enhances
GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of
mono-amine neurotransmitters. One of the mechanisms implicated in this effect of
gabapentin is the reduction of the axon excitability measured as an amplitude change of
the presynaptic fibre volley (FV) in the CA1 area of the hippocampus. This is mediated
through its binding to presynaptic NMDA receptors. Other studies have shown that the
antihyperalgesic and antialldynic effects of gabapentin are mediated by the descending
noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Gabapentin has also been shown to bind and activate the adenosine A1 receptor.
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)