8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 1/19

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 2/19

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 3/19

Pharmacologic classification:1-amino-methyl

cyclohexoneaceticacid

Therapeutic classification: anticonvulsant

Pregnancy risk : category C

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 4/19

Tablet:600 mg,800 mg

Capsule:100mg,300mg,400mg

Or al solution 250 mg  per 5 mL

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 5/19

-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«

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 6/19

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.

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 7/19

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.

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 8/19

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

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 9/19

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.

.

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 10/19

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

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 11/19

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.

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 12/19

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

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 13/19

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.

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 14/19

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.

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 15/19

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

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 16/19

Pregablin(lyrica)

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 17/19

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 18/19

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. 

8/9/2019 in and Pregablin[1]

http://slidepdf.com/reader/full/in-and-pregablin1 19/19