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Gabapentin
Class: Anticonvulsants, Miscellaneous
VA Class: CN400
Chemical Name: 1Aminomethylcyclohexaneacetic acid
Molecular Formula: C9H17NO2C16H27NO6
CAS Number: 60142963
Brands: Gralise, Horizant, Neurontin

Introduction
Anticonvulsant; structurally related to the inhibitory CNS neurotransmitter GABA; also possesses analgesic activity. 1 4 6 7 8 9
60 61 Gabapentin enacarbil is a prodrug of gabapentin. 61 76 83

Uses for Gabapentin

Seizure Disorders
Gabapentin as conventional [immediaterelease] preparations is used in combination with other anticonvulsant agents for
the management of partial seizures with or without secondary generalization in adults and children 3 years of age. 1 2 8 9

Safety and efficacy of gabapentin gastroretentive tablets Gralise and gabapentin enacarbil extendedrelease tablets
Horizant not established in patients with seizure disorders. 60 61

Neuropathic Pain
Gabapentin as conventional [immediaterelease] preparations or gastroretentive tablets and gabapentin enacarbil are
used for management of postherpetic neuralgia PHN in adults. 1 20 21 22 23 24 38 39 40 60 61 62 70

Gabapentin is considered one of several firstline therapies for PHN. 66 67

Gabapentin also has been used for management of pain associated with diabetic neuropathy. 20 21 22 23 24 25 40 41 42 43
44 45 70

Gabapentin also has demonstrated some evidence of benefit for the relief of chronic neurogenic pain in a variety of
conditions including trigeminal neuralgia, 20 21 46 47 pain and control of paroxysmal symptoms of multiple sclerosis
MS, 20 21 48 49 complex regional pain syndromes, 20 52 53 HIVrelated peripheral neuropathy, 20 21 50 and neuropathic
pain associated with cancer. 20 21 51 Additional study needed to further elucidate precise role in the management of these
conditions. 20 21 23

Restless Legs Syndrome

Gabapentin enacarbil is used for symptomatic treatment of moderatetosevere primary restless legs syndrome Ekbom
syndrome in adults. 61 71 74 78 79 80 81 82 Not recommended in patients who are required to sleep during the daytime and
remain awake at night. 61

Gabapentin also has been used for management of restless legs syndrome; however, the drug currently is not labeled by
FDA for this use. 26 27 28 71 72 73 78 81 82

Vasomotor Symptoms
Gabapentin has been used for the management of vasomotor symptoms e.g., hot flashes in women with breast
cancer. 30

Gabapentin has been used for the management of vasomotor symptoms e.g., hot flashes associated with menopause. 31
34 54

Gabapentin Dosage and Administration

General
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General
Closely monitor for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts
or behavior or depression. 55 56 57 59 60 61 See Suicidality Risk under Cautions.
If therapy is discontinued, gradually decrease dosage to avoid manifestations of abrupt withdrawal. 1 60 61 See Dosage
under Dosage and Administration, and also see Withdrawal Seizures under Cautions.

Administration
Oral Administration

Formulation Considerations
Gabapentin: Commercially available as conventional immediaterelease capsules, tablets, or oral solution. 1 Also available
as gastroretentive tablets Gralise; although not considered by FDA to be an extendedrelease formulation, the
gastroretentive tablets are sometimes referred to in this manner because of similar pharmacokinetics to an extended
release dosage form. 60 62 63 64 65 Because of differences in pharmacokinetics that affect frequency of administration,
gabapentin gastroretentive tablets are not interchangeable with other gabapentin preparations. 60 See Pharmacokinetics.

Gabapentin enacarbil: Commercially available as extendedrelease tablets Horizant. 61 Because of differences in

pharmacokinetics that affect frequency of administration, gabapentin enacarbil extendedrelease tablets are not
interchangeable with other gabapentin preparations. 61 See Pharmacokinetics.

Gabapentin Conventional Immediaterelease Tablets, Capsules, or Oral Solution

Administer orally 3 times daily without regard to meals. 1 Interval between doses should not exceed 12 hours. 1

If filmcoated scored tablets containing 600 or 800 mg of gabapentin are divided to administer a 300 or 400mg dose,
use the remaining half tablet for the next dose. 1 Discard half tablets that are not used within 28 days. 1

Swallow capsules whole with water. 1

Gabapentin Gastroretentive Tablets Gralise

Administer orally once daily with the evening meal. 60 Swallow tablets whole; do not chew, crush, or split. 60

Gabapentin Enacarbil Extendedrelease Tablets Horizant

Administer orally once or twice daily depending on indication. 61

When used for restless legs syndrome, administer once daily at about 5 p.m.; if a dose is missed, take next dose the
following day as scheduled. 61

When used for PHN, administer orally twice daily; if a dose is missed, skip dose and take next dose at regularly scheduled
time. 61

Swallow tablets whole; do not crush, chew, or cut. 61

Dosage
Pediatric Patients

Seizure Disorders

Partial Seizures
Oral
Gabapentin conventional immediaterelease tablets, capsules, or oral solution in children 311 years of age: Initially, 10
15 mg/kg daily in 3 divided doses. 1 Interval between doses should not exceed 12 hours. 1 Titrate upward over a period of
approximately 3 days until an effective maintenance dosage is achieved. 1 Recommended maintenance dosage in children
34 years of age is 40 mg/kg daily in 3 divided doses; recommended maintenance dosage in children 511 years of age is
2535 mg/kg daily in 3 divided doses. 1 Dosages up to 50 mg/kg daily have been well tolerated in clinical studies. 1

Gabapentin conventional immediaterelease tablets, capsules, or oral solution in children 12 years of age: Initially, 300
mg 3 times daily. 1 Maintenance dosage of 300600 mg 3 times daily recommended. 1 Interval between doses should not

1
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exceed 12 hours. 1 Dosages up to 2.4 g daily have been well tolerated in longterm clinical studies, and a small number of
patients have tolerated dosages of 3.6 g daily for short periods. 1

If therapy is discontinued, dosage reduced, or an alternative drug substituted, such changes should be done gradually
over 1 week. 1

Adults

Seizure Disorders

Partial Seizures
Oral
Gabapentin conventional immediaterelease tablets, capsules, or oral solution: Initially, 300 mg 3 times daily. 1
Maintenance dosage of 300600 mg 3 times daily recommended. 1 Interval between doses should not exceed 12 hours. 1
Dosages up to 2.4 g daily have been well tolerated in longterm clinical studies, and a small number of patients have
tolerated dosages of 3.6 g daily for short periods. 1

If therapy is discontinued, dosage reduced, or an alternative drug substituted, such changes should be done gradually
over 1 week. 1

Neuropathic Pain

Postherpetic Neuralgia
Oral
Gabapentin conventional immediaterelease tablets, capsules, or oral solution: 300 mg on day 1, 300 mg twice daily on
day 2, and 300 mg 3 times daily on day 3. 1 Increase dosage as needed for relief of pain up to a total dosage of 1.8 g
daily in 3 divided doses. 1 No evidence of additional benefit with dosages >1.8 g daily. 1 If therapy is discontinued, dosage
reduced, or an alternative drug substituted, such changes should be done gradually over 1 week. 1

Gabapentin gastroretentive tablets Gralise: Titrate gradually over 2 weeks up to recommended maintenance dosage of
1.8 g once daily as follows: 300 mg once daily on day 1, 600 mg once daily on day 2, 900 mg once daily on days 36, 1.2 g
once daily on days 710, 1.5 g once daily on days 1114, and 1.8 g once daily on day 15. 60 If therapy is discontinued,
dosage reduced, or an alternative drug substituted, such changes should be done gradually over 1 week. 60

Gabapentin enacarbil extendedrelease tablets Horizant: Initially, 600 mg once daily in the morning for 3 days, then
increase to recommended maintenance dosage of 600 mg twice daily. 61 Dosages >1.2 g daily provide no additional
benefit and associated with an increased incidence of adverse effects. 61 When discontinuing therapy in patients receiving a
dosage of 600 mg twice daily, reduce to 600 mg once daily for 1 week prior to withdrawing therapy. 61

Diabetic Neuropathy
Oral
Dosages of gabapentin 900 mg to 3.6 g daily have been used; however, pain relief generally observed in patients
receiving dosages >1.8 g daily. 24 25

Restless Legs Syndrome

Oral
Gabapentin enacarbil extendedrelease tablets Horizant: 600 mg once daily at approximately 5 p.m. 61

When discontinuing therapy, gradual withdrawal only necessary in patients receiving higher than recommended dosages;
in such cases, reduce dosage to 600 mg once daily for 1 week prior to withdrawing therapy. 61

Vasomotor Symptoms

Oral
300 mg 3 times daily as gabapentin conventional immediaterelease preparations has been effective; higher dosages
may provide additional benefit. 30 31 37

Special Populations
Renal Impairment
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Adjust dosage of gabapentin or gabapentin enacarbil in patients with renal impairment based on Clcr see Tables 14. 1 60
61

Table 1. Dosage Adjustments for Renal Impairment in Adults and Children 12 Years of Age Receiving Conventional
Immediaterelease Gabapentin 1
Clcr mL/minute Adjusted Dosage Regimen

>30 to 59 200700 mg twice daily i.e., up to a total dosage of 1.4 g daily

>15 to 29 200700 mg once daily

15 100300 mg once daily

<15 Reduce dosage in proportion to Clcr e.g., a patient with a Clcr of 7.5 mL/minute should receive one
half the dosage that a patient with a Clcr of 15 mL/minute should receive

Patients In addition to the renally adjusted maintenance dosage, administer supplemental dose of 125350
undergoing mg following each 4hour hemodialysis session
hemodialysis

Table 2. Dosage Adjustments for Renal Impairment in Adults Receiving Gabapentin Gastroretentive Tablets60
Clcr
Adjusted Dosage Regimen
mL/minute

3060 600 mg to 1.8 g once daily; initiate at 300 mg once daily and may titrate according to same schedule
recommended for those with normal renal function based on individual patient response and
tolerability

<30 Do not use

Patients Do not use

undergoing
hemodialysis

Table 3. Dosage Adjustments for Renal Impairment in Adults Receiving Gabapentin Enacarbil for PHN61
Clcr Titration
Maintenance Dosage Tapering Schedule
mL/minute Schedule

3059 300 mg 300 mg twice daily; increase to Reduce frequency of maintenance dosage to once daily
once daily 600 mg twice daily as in the morning for 1 week
in the necessary based on patient
morning response and tolerability
for 3 days

1529 300 mg 300 mg once daily in the In patients currently receiving a maintenance dosage of
once daily morning; increase to 300 mg 300 mg twice daily, reduce to 300 mg once daily in the
in the twice daily if necessary based morning for 1 week; in patients currently receiving a
morning on on patient response and maintenance dosage of 300 mg once daily, no taper
days 1 and tolerability needed
3

<15 not on None 300 mg every other day in the None

hemodialysis morning; increase to 300 mg
once daily if necessary based

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on patient response and

tolerability

<15 on None 300 mg following each None

hemodialysis hemodialysis session; increase
to 600 mg if necessary based
on patient response and
tolerability

Table 4. Dosage Adjustments for Renal Impairment in Adults Receiving Gabapentin Enacarbil for Restless Legs
Syndrome61
Clcr mL/minute Target Dosage

3059 Initiate at 300 mg once daily, then increase to 600 mg once daily as needed

1529 300 mg once daily

<15 not on hemodialysis 300 mg every other day

<15 on hemodialysis Use not recommended

Geriatric Patients
Select dosage carefully, usually initiating therapy at the low end of the dosage range. 1 Adjust dosage based on Clcr. 1 See
Renal Impairment under Dosage and Administration.

Cautions for Gabapentin

Contraindications
Gabapentin: Known hypersensitivity to gabapentin or any ingredient in the formulation. 1 60
Gabapentin enacarbil: Manufacturer states none known. 61

Warnings/Precautions
Warnings

Suicidality Risk
Increased risk of suicidality suicidal ideation or behavior observed in an analysis of studies using various anticonvulsants
in patients with epilepsy, psychiatric disorders e.g., bipolar disorder, depression, anxiety, and other conditions e.g.,
migraine, neuropathic pain; risk in patients receiving anticonvulsants 0.43% was approximately twice that in patients
receiving placebo 0.24%. 1 55 56 57 60 61 Increased suicidality risk was observed 1 week after initiation of anticonvulsant
therapy and continued through 24 weeks. 1 55 56 57 60 61 Risk was higher for patients with epilepsy compared with those
receiving anticonvulsants for other conditions. 1 55 56 57 60 61

Closely monitor all patients currently receiving or beginning anticonvulsant therapy for changes in behavior that may
indicate emergence or worsening of suicidal thoughts or behavior or depression. 55 56 57 Anxiety, agitation, hostility,
hypomania, and mania may be precursors to emerging suicidality. 55

Balance risk of suicidality with the risk of untreated illness. 55 Epilepsy and other illnesses treated with anticonvulsants are
themselves associated with morbidity and mortality and an increased risk of suicidality. 1 60 61 If suicidal thoughts or
behavior emerge during anticonvulsant therapy, consider whether these symptoms may be related to the illness itself. 1 60
61 See Advice to Patients.

Cognitive/Neuropsychiatric Effects

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Emotional lability primarily behavioral problems, hostility including aggressive behaviors, thought disorders including
concentration and school performance changes, and hyperkinesia primarily restlessness and hyperactivity associated
with use in children 312 years of age with epilepsy. 1

Dizziness and Somnolence

Risk of somnolence, sedation, and dizziness. 1 60 61 See Advice to Patients. Avoid concomitant use of alcohol or other
drugs that can potentiate these effects. 1 60 61 See Specific Drugs under Interactions.

Effects on Driving and Operating Heavy Machinery

Risk of substantial driving impairment; may be related to somnolence or other CNS effects of the drug. 1 61 72 See
Dizziness and Somnolence under Cautions. Duration of such impairment not known. 1 61

Patients should not drive or operate other complex machinery until they have gained sufficient experience with the drug. 1
61

Withdrawal Seizures
Abrupt withdrawal may result in increased seizure frequency and other withdrawal symptoms e.g., anxiety, insomnia,
nausea, pain; withdraw therapy gradually. 1 60 61 See Dosage under Dosage and Administration.

Tumorigenic Potential
Increased incidence of pancreatic acinar adenocarcinomas observed in rat carcinogenicity studies with gabapentin and
gabapentin enacarbil. 1 61 Clinical relevance of these findings to humans unknown. 1 60 61 72

New tumors or worsening of preexisting tumors reported in some patients receiving gabapentin; however, causal
relationship not established. 60 61

Sudden, Unexplained Deaths in Epilepsy

Higher incidence of sudden and unexplained deaths than would be expected in a healthy nonepileptic population;
however, incidence is within range of estimates for patients with epilepsy or refractory epilepsy. 1

Lack of Interchangeability
Different formulations of gabapentin e.g., conventional [immediaterelease] gabapentin preparations, gabapentin
gastroretentive tablets, gabapentin enacarbil extendedrelease tablets not interchangeable because of differences in
pharmacokinetics that affect frequency of administration. 60 61

Sensitivity Reactions

Multiorgan Hypersensitivity Reactions

Multiorgan hypersensitivity reactions also known as drug reaction with eosinophilia and systemic symptoms or DRESS
reported with anticonvulsants, including gabapentin; clinical presentation is variable but typically includes fever, rash,
eosinophilia, and/or lymphadenopathy associated with other organ system involvement e.g., hepatitis, nephritis,
hematologic abnormalities, myositis, myocarditis. 1 60 61 Potentially fatal or lifethreatening. 1 60 61

If manifestations of DRESS occur, evaluate patient immediately; discontinue gabapentin if an alternative etiology cannot be
identified. 1 60 61

Specific Populations
Pregnancy
Category C. 1

No adequate and wellcontrolled studies to date in pregnant women; developmental toxicity e.g., skeletal abnormalities,
hydroureter and hydronephrosis, increased embryofetal mortality demonstrated in animals. 1 16 60

North American Antiepileptic Drug NAAED Pregnancy Registry at 8882332334 for patients; NAAED registry information
also available on the website . 1

Lactation

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Distributed into milk; use only if potential benefits outweigh risks. 1 60 The manufacturer of gabapentin enacarbil states to
discontinue nursing or the drug. 61

Pediatric Use
Safety and efficacy of conventional immediaterelease gabapentin as adjunctive therapy for management of partial
seizures not established in children <3 years of age. 1

Safety and efficacy of conventional immediaterelease gabapentin for management of PHN not established in children. 1

Safety and efficacy of gabapentin gastroretentive tablets not established in children. 60

Safety and efficacy of gabapentin enacarbil not established in children. 61

Geriatric Use
Insufficient experience with conventional immediaterelease gabapentin for the management of partial seizures in patients
65 years of age to determine whether they respond differently than younger adults. 1 Select dosage carefully. 1 See
Geriatric Patients under Dosage and Administration.

Appeared to be more effective for the management of PHN in patients >75 years of age than in younger patients;
apparent difference in efficacy may be related to decreased renal function in older patients. 1 Adverse effects in older
patients with PHN generally similar to those in younger adults; however, the incidence of peripheral edema and ataxia
appears to increase with age. 1

Adverse effects reported with gabapentin as gastroretentive tablets generally similar across all age groups except for
peripheral edema, which tended to increase with age. 60

Insufficient experience with gabapentin enacarbil in patients 65 years of age to determine whether they respond
differently than younger patients. 61 No overall differences in safety and efficacy observed between geriatric and younger
patients receiving the drug. 61

Geriatric patients may have decreased hepatic, renal, or cardiac function, with increased risk of adverse effects. 1 16 60 61
Use with caution; dosage reductions may be necessary in those with renal impairment. 1 See Renal Impairment under
Dosage and Administration.

Renal Impairment
Eliminated renally; dosage adjustments may be necessary in patients with renal impairment. 1 60 61 See Renal Impairment
under Dosage and Administration.

Common Adverse Effects

Children 312 years of age receiving conventional immediaterelease gabapentin as adjunctive therapy for partial
seizures: viral infection, fever, nausea and/or vomiting, somnolence, hostility. 1

Adults and children >12 years of age receiving conventional immediaterelease gabapentin as adjunctive therapy for
partial seizures: somnolence, dizziness, ataxia, fatigue, nystagmus. 1

Adults receiving conventional immediaterelease gabapentin for management of PHN: dizziness, somnolence, peripheral
edema. 1

Adults receiving gabapentin gastroretentive tablets for PHN: dizziness. 60

Adults receiving gabapentin enacarbil for PHN: dizziness, somnolence, headache. 61

Adults receiving gabapentin enacarbil for restless legs syndrome: somnolence/sedation, dizziness. 61

Interactions for Gabapentin

Not metabolized by CYP isoenzymes. 1 Does not inhibit CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4 in vitro; causes
slight inhibition of CYP2A6 at high concentrations. 1

Specific Drugs

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Drug Interaction Comments

Alcohol Increases risk of sedation/somnolence, dizziness 1 60 61 Avoid concomitant use 1 60 61

Causes rapid release of drug from gabapentin enacarbil
extendedrelease tablets 61

Antacids Reduced bioavailability of gabapentin, but to a smaller extent Administer gabapentin at least 2
when gabapentin administered 2 hours after antacid 1 60 hours after antacid 1 60

Anticonvulsants Plasma concentrations of carbamazepine, phenytoin, valproic May be used concomitantly without
acid, phenobarbital, and diazepam in existing treatment regimens concern about alterations in
not affected by gabapentin; 1 3 12 13 14 60 pharmacokinetics of plasma concentrations of
gabapentin not affected by these drugs 1 6 12 15 60 gabapentin or other anticonvulsant
drugs 1

Cimetidine Possible decrease in gabapentin clearance 1 60 Not likely to be clinically important 1

60

Naproxen Increased bioavailability of gabapentin at subtherapeutic dosages Extent of interaction at usual

of both drugs 1 60 therapeutic dosages is unknown 1
60

Opiate Possible increased gabapentin concentrations and increased risk Carefully observe for signs of CNS
analgesics of adverse effects e.g., somnolence, dizziness, nausea 1 or respiratory depression and
e.g., Hydrocodone: Possible decrease in plasma concentrations of reduce dosage of gabapentin or
hydrocodone, hydrocodone 1 60 the opiate analgesic if indicated 1
morphine Morphine: Morphine pharmacokinetics based on a controlled
release preparation not affected by gabapentin when
administered 2 hours after the morphine dose 1

Oral Possible increase in peak plasma concentrations of Not likely to be clinically important 1
contraceptives norethindrone 1 60

Probenecid No pharmacokinetic interaction observed 1

Gabapentin Pharmacokinetics
Absorption
Bioavailability
Conventional immediaterelease gabapentin: Following oral administration, absorbed principally in the proximal small
intestine via a saturable Lamino acid transport system; bioavailability is not dose proportional and decreases as dose
increases. 1 60 63 83 84 Bioavailability is 60 to 27% for doses ranging from 900 mg to 4.8 g daily. 1

Gabapentin gastroretentive tablets: In healthy individuals, time to peak plasma concentrations is prolonged about 46
hours longer, peak plasma concentrations are higher, and systemic exposure is lower relative to immediaterelease
formulations. 60

Gabapentin enacarbil extendedrelease tablets: Absorbed by highcapacity transporters throughout the GI tract and not
affected by saturable absorption; this improves bioavailability and allows for doseproportional exposure. 61 72 74 78 80 83
Mean bioavailability in the fed state is about 75% and in the fasted state is about 4265%. 61 Steadystate achieved in
about 2 days with daily administration. 61

Food
Conventional immediaterelease gabapentin: Food does not substantially affect bioavailability. 1 60 64

Gabapentin gastroretentive tablets: Food increases absorption of the drug formulation; tablets swell upon contact with
gastric fluid to a size that promotes gastric retention for approximately 810 hours when taken with a meal. 60 63 64 65

Gabapentin enacarbil extendedrelease tablets: Food increases systemic exposure. 61 76

Distribution
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Distribution
Extent
Readily crosses the bloodbrain barrier and concentrates in brain tissue. 29 Distributed into breast milk. 1 Not known
whether gabapentin crosses the placenta. 1

Plasma Protein Binding

<3%. 1

Elimination
Metabolism
Gabapentin is not appreciably metabolized. 1 61

Gabapentin enacarbil, the prodrug of gabapentin, is rapidly and efficiently converted to gabapentin by firstpass
hydrolysis following oral administration. 61 74

Elimination Route
Excreted renally as unchanged drug. 1 61

Halflife
Approximately 57 hours. 1 60 61

Special Populations
In children <5 years of age, clearance normalized for weight is higher than in adults and children 5 years of age. 1

In patients with renal impairment, plasma clearance is decreased and halflife is prolonged. 1 In patients with Clcr <30
mL/minute, halflife of 52 hours reported with conventional immediaterelease gabapentin; in anuric patients, halflife
reported to be 132 hours on nondialysis days and 3.8 hours during hemodialysis. 1

Stability
Storage
Oral
Gabapentin Conventional immediaterelease Capsules and Tablets
25C may be exposed to 1530C. 1

Gabapentin Conventional immediaterelease Oral Solution

28C. 1

Gabapentin Gastroretentive Tablets Gralise

25C may be exposed to 1530C. 60

Gabapentin Enacarbil Extendedrelease Tablets Horizant

25C may be exposed to 1530C. 61

Actions
Mechanism of anticonvulsant action is unknown. 1 4 5 7 8 9 Does not bind to GABA receptors, 1 4 5 6 7 17 affect GABA
reuptake or metabolism, 1 6 7 17 or act as a precursor of GABA or other substances active at GABA receptors. 1 17

Mechanism of analgesic action is unknown. 1 20 21 22 23 Prevents allodynia painrelated behavior in response to

normally innocuous stimuli and hyperalgesia exaggerated response to painful stimuli in several animal models of
neuropathic pain. 1 20 Decreases painrelated responses after peripheral inflammation in animals; however, has not

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altered immediate painrelated behaviors, and clinical relevance is not known. 1 In vitro studies demonstrate that the
drug binds with high affinity to the 2 subunit of voltageactivated calcium channels; however, clinical relevance not
known. 1 66 69

Advice to Patients
Importance of advising patient to read the manufacturers medication guide before initiating therapy and each time the
prescription is refilled. 1
Importance of taking gabapentin exactly as prescribed. 1 Importance of not abruptly discontinuing therapy. 1
Risk of suicidality. 1 55 56 57 59 Importance of patients, family, and caregivers being alert to daytoday changes in
mood, behavior, and actions and immediately informing clinician of any new or worrisome behaviors e.g., talking or
thinking about wanting to hurt oneself or end ones life, withdrawing from friends and family, becoming depressed or
experiencing worsening of existing depression, becoming preoccupied with death and dying, giving away prized
possessions. 1 55
Potential for drug to impair mental alertness or physical coordination; avoid driving or operating machinery until
effects on individual are known. 1
Risk of serious hypersensitivity reactions affecting multiple organ systems e.g., liver, kidney. 1 Importance of informing
patients to contact their clinician immediately if a rash or other manifestations of hypersensitivity e.g., fever,
lymphadenopathy occur. 1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breastfeed. 1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC
drugs. 1
Importance of informing patients of other important precautionary information. 1 See Cautions.

Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific
product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic nonproprietary name

Gabapentin
Routes Dosage Forms Strengths Brand Names Manufacturer

Oral Capsules 100 mg* Gabapentin Capsules

Neurontin Pfizer

300 mg* Gabapentin Capsules

Neurontin Pfizer

400 mg* Gabapentin Capsules

Neurontin Pfizer

Solution 250 mg/5 mL* Neurontin Pfizer

Tablets 100 mg* Gabapentin Tablets

300 mg* Gabapentin Tablets

Gralise Depomed

400 mg* Gabapentin Tablets

600 mg* Gabapentin Tablets

Gralise Depomed
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800 mg* Gabapentin Tablets

Tablets, filmcoated 600 mg* Gabapentin Tablets

Neurontin Pfizer

800 mg* Gabapentin Tablets

Neurontin Pfizer

Gabapentin Enacarbil
Routes Dosage Forms Strengths Brand Names Manufacturer

Oral Tablets, extendedrelease 300 mg Horizant XenoPort

600 mg Horizant XenoPort

AHFS DI Essentials. Copyright 2017, Selected Revisions November 23, 2015. American Society of HealthSystem Pharmacists, Inc., 4500
EastWest Highw ay, Suite 900, Bethesda, Maryland 20814.
Use is not currently included in the labeling approved by the US Food and Drug Administration.

References
1. Pfizer. Neurontin gabapentin capsules, tablets, and oral solution prescribing information. New York, NY; April 2015.
2. Anon. ParkeDavis Neurontin recommended for approval as add on therapy for refractory seizures in epilepsy; gabapentin
monotherapy trials under w ay. FDC Rep. 1992 Dec:78.
3. Anon. Warner Lamberts Neurontin approved for adjunctive therapy in epilepsy patients Dec 30; 1P drug does not interact w ith other
anticonvulsants. FDC Rep. 1994 Jan:11.
4. Ramsay ER. Advances in the pharmacotherapy of epilepsy. Epilepsia. 1993; 34Suppl 5:S916. [PubMed 8339715]
5. MacDonald RL, Kelly KM. Antiepileptic drug mechanisms of action. Epilepsia. 1993; 34Suppl 5:S18. [PubMed 7687957]
6. Goa KL, Sorkin EM. Gabapentin: a review of its pharmacological properties and clinical potential in epilepsy. Drugs. 1993; 46:40927.
[PubMed 7693432]
7. Graves NM, Leppik IE. Antiepileptic medications in development. DICP Ann Pharmacother. 1991; 25:97886. [PubMed 1949977]
8. UK Gabapentin Study Group. Gabapentin in partial epilepsy. Lancet. 1990; 335:11147. [PubMed 1971862]
9. US Gabapentin Study Group. Gabapentin as addon therapy in refractory partial epilepsy: a double blind, placebocontrolled, parallel
group study. Neurology. 1993; 43:22928. IDIS 321974 [PubMed 8232945]
10. SumanChauhan N, Webdale L, Hill DR et al. Characterisation of [ 3H] gabapentin binding to a novel site in rat brain: homogenate
binding studies. Eur J Pharmacol. 1993; 244:293301.
11. Hill DR, SumanChauhan N, Woodruff GN. Localization of [ 3H] gabapentin to a novel site in rat brain: autoradiogaphic studies. Eur J
Pharmacol. 1993; 244: 3039. [PubMed 8384571]
12. Anhut H, Leppik I, Schmidt B et al. Drug interaction study of the new anticonvulsant gabapentin w ith phenytoin in epileptic patients.
Naunyn Schmiedeberg Arch Pharmacol. 1988; 337Suppl:R127. Abstract No. 507.
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