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GabapentinAka: Neurontin

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  1. Indications
    1. Neuropathic pain (peripheral nerve syndromes)
      1. Diabetic Neuropathy
      2. Postherpetic Neuralgia
      3. Trigeminal Neuralgia
      4. Cancer Pain Management
    2. Multiple Sclerosis
    3. Parkinson's Disease
    4. Restless Legs Syndrome
      1. Effective in idiopathic RLS
        1. Happer (2001) Neurology 57(9):1717
      2. Effective in RLS among Hemodialysis patients
        1. Thorp (2001) Am J Kidney Dis 38(1):104
    5. Epilepsy
      1. Generalized Tonic Clonic Seizures (rarely used)
      2. Partial Seizures (adjunctive agent)
    6. Bipolar Disorder
    7. Anxiety Disorder
      1. Post-Traumatic Stress Disorder (PTSD)
      2. Social Phobia
      3. Generalized Anxiety Disorder
  2. Mechanism
    1. GABA amino acid derivative
  3. Metabolism
    1. Primarily renal excretion
    2. Half-life: 5 to 7 hours
    3. Therapeutic Dose: 4-8 ug/ml
  4. Adverse Effects
    1. Sedation
    2. Weight gain
    3. Nausea
    4. Dizziness
    5. Ataxia
    6. Fatigue
    7. Nystagmus
  5. Newer related agents: Pregabalin (Lyrica)
    1. Indicated in Neuropathy
    2. More potent than Gabapentin, and possibly less Fatigue
  6. Dosing: Adults
    1. Starting Dose: 300 mg PO qhs or 300 mg PO tid
      1. Patients tolerate starting 300 tid without titrating
      2. Fisher (2001) Neurology 56(6):743
    2. Average Dose: 600 mg PO tid
    3. Maximum Dose: 1200 mg PO tid
      1. No increase in bioavailability above 1200 mg tid
  7. Drug Interactions
    1. No significant drug interactions
  8. Disadvantages
    1. Expensive
    2. Low potency as antiepileptic

gabapentin (C0060926)

Definition (NCI)A substance that is being studied as a treatment for relieving hot flashes in women with breast cancer. It belongs to the family of drugs called anticonvulsants.
Definition (PDQ)A synthetic analogue of the neurotransmitter gamma-aminobutyric acid with anticonvulsant activity. Although its exact mechanism of action is unknown, gabapentin appears to inhibit excitatory neuron activity. This agent also exhibits analgesic properties. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=38402&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=38402&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1108" NCI Thesaurus)
Definition (CSP)cyclohexananeacetic acid originally used as an anticonvulsant, found to have diverse CNS depressant actions.
Definition (NCI)A synthetic analogue of the neurotransmitter gamma-aminobutyric acid with anticonvulsant activity. Although its exact mechanism of action is unknown, gabapentin appears to inhibit excitatory neuron activity. This agent also exhibits analgesic properties. (NCI04)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
Englishgabapentin, GABAPENTIN PREPARATION
Spanishgabapentina
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Neurontin (C0678176)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishAventis brand of gabapentin, Neurontin, Parke Davis brand of gabapentin, Pfizer brand of gabapentin
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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