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Drug Study

1. Gabapentin is used to treat partial seizures, postherpetic neuralgia, and restless leg syndrome. 2. Its mechanism of action involves interacting with voltage-sensitive calcium channels in cortical neurons to increase GABA concentrations and responses, and reduce monoamine neurotransmitter release. 3. It has rapid absorption via an amino acid transport system, with a bioavailability ranging from 60% for lower doses to 27% for higher doses.
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0% found this document useful (0 votes)
140 views3 pages

Drug Study

1. Gabapentin is used to treat partial seizures, postherpetic neuralgia, and restless leg syndrome. 2. Its mechanism of action involves interacting with voltage-sensitive calcium channels in cortical neurons to increase GABA concentrations and responses, and reduce monoamine neurotransmitter release. 3. It has rapid absorption via an amino acid transport system, with a bioavailability ranging from 60% for lower doses to 27% for higher doses.
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Generic Trade Name Classification Dose Route Time/frequency

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

Mechanism of action and indications: Nursing Implications (what to focus on)


(Why med ordered) Contraindications/warnings/interactions- Hypersensitivity,
Use cautiously in geriatric pt. because of age-related
Mechanism of action is unknown. May affect transport decrease in renal function.
of amino acids across and stabilize neuronal
membranes. Therapeutic effects: decreased incidence Common side effects: CNS: confusion, depression,
of seizures. (Tics) drowsiness, sedation, anxiety, dizziness, hostility, malaise,
vertigo, weakness. EENT: abnormal vision, nystagmus.
For Tic disorder CV: hypertension. GI: wt. gain, anorexia, flatulence,
gingivitis. MS: arthralgia. Neuro: ataxia, altered reflexes,
hyperkinesia, paresthesia. Misc: facial edema.

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.

Nursing Process- Assessment Assessment Evaluation


(Pre-administration assessment) Why would you hold or not give this Check after giving
med?
Vital signs, especially BP. Hypersensitivity. Decreased frequency or
Assess location, duration, and Severe agitation or hostility. cessation of Tics.
characteristics of Tics. Severe exacerbation of side effects. Monitor for side effects.
Signs of renal failure. Would contact
PCP.

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 is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of


Decreased Central Nervous System Disorganized Electrical Activity.

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)

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