Pharm
Gabapentin
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Gabapentin
, Neurontin
Precautions
Risk of Abuse
Gabapentin and
Pregabalin
(
Lyrica
) are abused by patients on
Opiate
s to potentiate CNS
Opiate
effects
More than one quarter of
Opiate
patients have abused Gabapentin
Pregabalin
(
Lyrica
) is more potent with faster onset and has higher abuse potential than Gabapentin
Lyrica
is categorized as
DEA Controlled Substance
Class V (and Gabapentin in several states)
Smith (2012) Br J Gen Pract 62(601):406-7 +PMID:22867659 [PubMed]
Indications
Neuropathic pain (peripheral nerve syndromes)
Diabetic Neuropathy
Postherpetic Neuralgia
Trigeminal Neuralgia
Cancer Pain Management
Multiple Sclerosis
Parkinson's Disease
Restless Legs Syndrome
Effective in idiopathic RLS
Happer (2001) Neurology 57(9):1717-9 [PubMed]
Effective in RLS among
Hemodialysis
patients
Thorp (2001) Am J Kidney Dis 38(1):104-108 [PubMed]
Epilepsy
Generalized Tonic Clonic Seizure
s (rarely used)
Partial Seizure
s (adjunctive agent)
Bipolar Disorder
Anxiety Disorder
Post-Traumatic Stress Disorder
(
PTSD
)
Social Phobia
Generalized Anxiety Disorder
Alcohol Dependence
Doses of 600 mg orally three times daily appear to decrease
Alcohol
cravings
Safety
Pregnancy Category C
Excreted in
Breast Milk
Mechanism
GABA amino acid derivative (does not bind GABA-A or GABA-B receptors)
Binds alpha2-delta1 subunit of
Central Nervous System
voltage-gated
Calcium
channels
Decreases excitatory neurotransmitter release and activity
Metabolism
Primarily renal excretion
Half-life: 5 to 7 hours
Therapeutic Dose: 4-8 ug/ml
Adverse Effects
Most common
Sedation
Dizziness
Ataxia
Other adverse effects
Weight gain
Nausea
Fatigue
Nystagmus
Preparations
Newer related agents
Pregabalin
(
Lyrica
)
Indicated in
Neuropathy
More potent than Gabapentin, and possibly less
Fatigue
Dosing
Neuropathy
in Adults
Starting Dose
Start at 300 mg orally at bedtime
Advance to 300 mg orally three times daily (over 4-7 days)
Plan to ultimately increase to 600 mg three times daily
Patients tolerate starting 300 three times daily without titrating
Fisher (2001) Neurology 56(6):743-8 [PubMed]
Average Dose: 600 mg orally three times daily
Maximum Dose: 1200 mg orally three times daily
No increase in bioavailability above 1200 mg orally three times daily
Minimal pain benefit above 1800 mg/day in most conditions studied
Stopping (similar to
Pregabalin
)
Taper off agent over 1 week or more
Avoid stopping abruptly due to withdrawal symptoms
Dosing
Seizure Prophylaxis
Age 3-12 years old
Gabapentin 10-15 mg/kg (max 40 mg/kg) daily divided three times daily
Age >12 years old
Gabapentin 300-900 mg (max 1800) daily divided three times daily
Drug Interactions
No significant
Drug Interaction
s
Disadvantages
Low potency as antiepileptic
References
(2016) Crit Dec Emerg Med 30(9):24
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