in and pregablin[1]
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Pharmacologic classification:1-amino-methyl
cyclohexoneaceticacid
Therapeutic classification: anticonvulsant
Pregnancy risk : category C
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Tablet:600 mg,800 mg
Capsule:100mg,300mg,400mg
Or al solution 250 mg per 5 mL
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-Gabapentin was initially synthesized of chemical str uctur eto mimic the
-gammaneur otr ansmitter the
aminobutyr ic acid (GABA), but is
not believed to act on the same
br ain r eceptor s.Its exact is unknown,mechanism of action
but its therapeutic action on
is thought to neuropathic pain
type - Ngated-voltageinvolve
. It is thought ion channelscalcium
to bind to the 2 subunit of the dependent calcium-voltage
in the C NS ,modulate channel
calcium influx in hyper excited
neur on ,r educe neur otr ansmitter
r elease«
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Adjunctive ther apy in tr eatment of par tial seizur es with or without secondar y gener alization in patients older than 12 yr of age with epilepsy; adjunctive ther apy for par tial seizur es in childr en 3 to 12 yr of age; management of posther petic
neur algia in adults.Unlabeled Uses
Agitation in dementia; alcohol withdr awal; bipolar disor der ; cocaine withdr awal; diabetic neur opathy; fibr omyalgia; headaches; hiccups (singultus); hot flashes (cancer - and/or postmenopausal-r elated); hyper hidr osis; nausea (cancer -r elated); neur algia/neur opathy/chr onic pain; pr evention of migr aine; pr ur itus ( br achior adial/cholestatic/ur emic); r ectal administr ation; r estless leg syndr ome; tr emor s in multiple scler osis.
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3 hr in24mg/kg/35 ± 15:yr12 ± 2Children
divided doses (max: 50mg/kg/24hr).
mg300Start:yr and adults12Children >
daily, then daily increase by 300mg to 900±
3,600mg/24hr in 3 divided doses.
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mg400ml/minute give60is more thanIf Cr ClP.O t.i.d.daily
ml/minute give30to15isIf Cr Cl300mgP.O.t.i.d daily
mg300ml/minute give15is less thanIf Cr ClP.O other day.
Patients on haemodialysis should receive amgP.O,then400-mg300loading dose of
h of4mg P.O. after q300mg to200haemodialysis
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Gabapenten bioavailability is not dose:Absorptionproportional.A400mg dose, for example is about 25% lessbioavailable than 100mg dose. Over the recommended doserange of 300 to 600mg t.i.d, however differences inbioavailability are not large and bioavailability is about60%.Food has not effect on the rate or extent of absorption..
Gabapentin circulate largely unbound (lessDistribution:
than3%) to plasma protein.Cross BBB with approximately20% of the corresponding plasma conc. Found in CSF.
.
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is not appreciably metabolized in:Metabolism
human.
:is eliminated from the systemicExcretion
circulation by renal excretion as unchanged drug,
,gabapentin can removedhr7-5is2/1tit elimination
from plasma by haemodialysis
contraindicate in patients:Contraindicationhypersensitive to the drug
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Antacid decr eases the absor ption of Interaction:gabapentin .Administr ation of the two dr ugs should be separ ate by at least 2 hr .
Laboratory Test Interactions
False- positive r eadings for Ames N-Multistix SG dipstick test when gabapentin is added to other
antiepileptic dr ugs. Sulfosalicylic acid pr ecipitation pr ocedur e is r ecommended
to determine the pr esence of ur ine pr otein.
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fatigue, somnolence ,dizziness ,ataxia ,nystagmus,CNS:tremor ,nervousness ,dysarthria ,amnesia , depression ,abnormal thinking ,twitching , incordoration
peripheral odema , vasodilation.CV:
diplopia, rhinitis, phyringitis, dry throat ,coughingEENT:,amblyopia.
impotence.GU:
leukopenia ,decrease WBC countHaematologic:
: pruritis ,abrasionSkindental abnormalities , increased appetite,Other:
weight gain , back pain , myalgia, fracture
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Acute over dose of gabapentin may cause double
vision, slurr ed speech , dr owsiness ,lethargy
and diarr hea.
Suppor tive car e is r ecommended. In addition
gabapentin can r emoved by haemodialysis and
may be indicated by the patient¶s clinical state
or in plasma with significant r enal im pairment.
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If gabapentin ther apy is discontented or alter native medication is substituted ,do so gr adually over at least 1 week to minimize the r isk of pr ecipitating seizur e.
Do not suddenly withdr aw other anticonvulsant dr ugs in patients star ting gabapentin ther apy
Breast feeding
It is not known if gabapentin excr eted in human milk.
Because many dr ug ar e excr eted in human milk. Gabapentin should be used in br east feeding patient only if the benefit clear ly out-weight the r isks.
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to avoid dr iving or oper ating*Warn patient
heavy machiner y until adver se C NS effects of
the dr ug ar e known.
to take fir st dose at bed time *Instruct patient
to minimize dr owsiness , dizziness, fatigue ,
and ataxia.
that he can take gabapentin *Inform patient
without r egar d to meal
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Pregablin(lyrica)
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Clinical study
Objective: To com par e the dose-r esponse (seizur e f r equency) r elationship of pr egabalin and gabapentin add-on tr eatment in patients with r ef r actor y par tial epilepsy.Background: Pr egabalin (Lyr ica®) and gabapentin ( Neur ontin®) ar e antiepilepticdr ugs that appear to have a similar mechanism of action thr ough binding to the 2-subunit of voltage-gated calcium channels. Pr eclinical studies with pr egabalin and gabapentin indicate similar anticonvulsant pharmacological pr ofiles; however,
pr egabalin shows 3- to 6-fold gr eater potency. Pr egabalin, unlike gabapentin,exhibits linear absor ption , incr easing pr opor tionally with dose. In contr ast, the
extent of gabapentin absor ption decr eases with incr easing dose.
Results: Pr egabalin (50±600 mg/d) and gabapentin (600±1800 mg/d) showed an asym ptotic dose-r elated decr ease in seizur e f r equency. Both pr egabalin- and gabapentin-tr eated patients demonstr ated a dose-r esponse r elationship; however,the maximal decr ease in seizur e f r equency f r om baseline with pr egabalin was 100%, while the maximal decr ease with gabapentin ther apy was 24.5%. Based on
this information, pr egabalin was estimated to be 4 times mor e effective than gabapentin in patients who r esponded to tr eatment. Pr egabalin was also 2.5 times mor e potent than gabapentin in r esponding patients, as measur ed by the dose that r educed seizur e f r equency by 50%.
Conclusions: The obser ved im pr ovement in potency and effectiveness com bined with the pharmacokinetic- pharmacodynamic pr oper ties of pr egabalin r elative to gabapentin offer distinct advantages over standar d gabapentin ther apy for the tr eatment of r ef r actor y par tial seizur es.
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