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    Gabapantin and Pregabalin

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    ayushi
    Gabapentin and pregabalin are structural analogues of the inhibitory neurotransmitter GABA. [1] Gabapentin was first approved as an anti-epileptic drug in 1994, while pregabalin was initially approved for treating neuropathic pain in 2005. [2] Both drugs bind to voltage-gated calcium channels and modulate calcium influx to reduce neurotransmitter release. They have higher bioavailability than gabapentin and are renally excreted without metabolic interactions. Key indications include postherpetic neuralgia, epilepsy, and fibromyalgia.

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    Gabapantin and Pregabalin

    Uploaded by

    ayushi
    21 views23 pages
    Gabapentin and pregabalin are structural analogues of the inhibitory neurotransmitter GABA. [1] Gabapentin was first approved as an anti-epileptic drug in 1994, while pregabalin was initially approved for treating neuropathic pain in 2005. [2] Both drugs bind to voltage-gated calcium channels and modulate calcium influx to reduce neurotransmitter release. They have higher bioavailability than gabapentin and are renally excreted without metabolic interactions. Key indications include postherpetic neuralgia, epilepsy, and fibromyalgia.

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    gabapantin and pregabalin

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    Gabapentin and pregabalin are structural analogues of the inhibitory neurotransmitter GABA. [1] Gabapentin was first approved as an anti-epileptic drug in 1994, while pregabalin was initially approved for treating neuropathic pain in 2005. [2] Both drugs bind to voltage-gated calcium channels and modulate calcium influx to reduce neurotransmitter release. They have higher bioavailability than gabapentin and are renally excreted without metabolic interactions. Key indications include postherpetic neuralgia, epilepsy, and fibromyalgia.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    21 views23 pages

    Gabapantin and Pregabalin

    Uploaded by

    ayushi
    Gabapentin and pregabalin are structural analogues of the inhibitory neurotransmitter GABA. [1] Gabapentin was first approved as an anti-epileptic drug in 1994, while pregabalin was initially approved for treating neuropathic pain in 2005. [2] Both drugs bind to voltage-gated calcium channels and modulate calcium influx to reduce neurotransmitter release. They have higher bioavailability than gabapentin and are renally excreted without metabolic interactions. Key indications include postherpetic neuralgia, epilepsy, and fibromyalgia.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 23

    GABAPENTIN AND

    PREGABALIN
    GABAPENTIN
    Introduction :

     Gabapentin is the structural analogue of the inhibitory neuro


    transmitter gamma-aminobutyric acid (GABA).
     Gabapentin,1-(aminomethyl)-cyclohexane acetic acid is a
    novel amino acid derived from adding a cyclohexyl group to
    GABA
    developed by Warner-
    Lambert, as an agent for the
    treatment of spasticity .
    First approved for use as an
    anti–epileptic drug by FDA in
    1994 by Parke-Davis.
    PHARMACOKINETICS
     Gabapentinis available in immediate release and sustained release
    formulations.
     Immediate release gabapentin show saturable kinetics due to
    saturable gastrointestinal absorption.
     Withoral bioavailability of 60% with 300 mg 3 times a day that
    decrease to 33% with 1200 mg two times a day.
     Less than 3 % plasma protein binding .
     Notmetabolized in liver eliminated unchanged
    by renal excretion.
     Gabapentin clearance correlates with that of
    creatinine clearance.
     Half lives when used as monotherapy – 6hrs.
    MODE OF ACTION
    The primary mode of action
    appears to be at the auxillary 2δ-
    1sub unit of voltage-gated calcium
    channel. Thus modulate calcium
    channels to reduce monoamine
    release.
     Have indirect GABAergic
    effects.
     Also have antigutaminergic
    action mediated by inhibition of
    glutamate synthesis
    T INDICATIONS :

     Postherpetic Neuralgia
     Adjunctive treatment of partial onset seizure
     Restless leg syndrome
    DOSAGE AND ADMINISTRATION
     Adult with epilepsy : Started as 300mg/day in three divided dose and can be increased upto
    1800mg/day in three divided dose.
     Pediatric with epilepsy : start with 10 mg/kg -15 mg/kg

    increased to 25 mg/kg – 40 mg/kg


     Post herpetic neuralgia : 300mg day -1

    600mg Day -2
    900mg day-3
    Maximum dose can be increased upto 1800 mg three divided dose.
    ADVERSE EFFECTS:
    PRECAUTIONS :

     classified
    as pregnancy category C drug as fetal loss and teratogenicity
    have been demonstrated in animals
    Gabapentin is classified as “probably safe” for lactation though it is
    excreted in breast milk. (prescribe only if potential benefit > risks).
    Do not discontinue the drug abruptly .
    DRUG INTERACTIONS :
     As Gabapentin is renally excreted it lack hepatic drug drug
    interaction .
     Gabapentin bioavailability decreases if administered at the same
    time as antacid . Should be taken 2 hours after taking antacid .
    PREGABALIN
    INTRODUCTION
     Pregabalin is a compound with structural similarity to the
    inhibitory neurotransmitter GABA that could easily cross
    the blood-brain barrier.

     Pregabalinwas initially used for the treatment of


    neuropathic pain associated with diabetic peripheral
    neuropathy by FDA in 2005
     Pregabalin, S-(+)-3-isobutylGABA , is a novel amino acid
    derived from GABA.
    PHARMACOKINETICS
     Pregabalin
    is not bound to plasma protein , has a moderate
    volume of distribution of 0.5L/kg.
     Half life of 6 hours.
     Notmetabolized in liver eliminated unchanged by renal
    excretion
     Hashigher bioavailability and absorption proportional to dose
    without GI saturation as seen with gabapentin .
    MODE OF ACTION
    Selective inhibitory effects on
    voltage-gated calcium channels
    containing the -2-δ-1subunit
    Reduced depolarizing calcium
    influx at the nerve terminal.
    Decreased release of glutamate and
    noradrenaline (excitatory
    neurotransmitters)
    Pregabalin lack direct GABAergic
    actions
    INDICATIONS :
     Adjunct for treatment of adults with partial onset seizure
     Post Herpetic Neuralgia
     Fibromyalgia
     Diabetic peripheral neuropathy .
     Neuropathic pain associated with spinal cord injury
    DOSE
     Dose of pregablin range from 150 mg / day to 600 mg/day
     Started as 150 mg / day in 2-3 divided dose and can be
    increased within 1 week to 300mg/day in 2-3 divided dose.
     Patient with insufficient efficacy the dose can be increased
    upto 600mg.
    ADVERSE EFFECTS

     Drowsiness
     Dry mouth
     Asthenia
     Headache
     Blurred vision
     Headache
     Peripheral edema
    PRECAUTIONS

     Pregablin is classified as pregnancy category C.


     It is classified as SAFETY UNKNOWN for lactation .
     Increased risk of suicidality in patient with epilepsy as well
    as psychiatric disorder

    .
    DRUG INTERACTIONS
     Pregablinhas no hepatic metabolism hence lack any metabolic
    drug interactions.
     Pregablin does not yield clinically significant changes with
    kinetics of harmonal contraceptives.
    REFERENCE

     Goodman and Gilman's The Pharmacological Basis of


    Therapeutics, 13th Edition

     Kaplan & Sadock's Comprehensive Textbook of Psychiatry.


    Thank you

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