Today we’ll discuss the drug gabapentin which comes under the brand name like gabatar or gabapene 300mg so this gabapentine it’s a newer anti-epileptic which is introduced after 1990s which comes in 90s so this gabapentine originally it is developed as a spasmolytic and later on found to be effective as an anti-convulsant gabapentine which is a newer anti-epileptic
Introduced after 1990s originally it was developed as a spasmolytic anti-spasmodic and but later on it was found to be effective as a anti-convulsion drug so this gaba pentine by mechanism it’s a gaba analog so it increases gaba concentration by affecting the gaba metabolism its non-synaptic release and its reuptake by the gaba transporter there is a non-synaptic
Release and its reuptake by the or through gaba transporter but it does not act on the gaba a receptor though it is a gaba analog gabapentine that’s why the name is gabapentine gaba analog that’s why the name is gabapentine so it increases gaba concentration by affecting the gaba metabolism its non-synaptic release and its reuptake occurs through the gaba
Transporter but it does not act on the gaba receptor there is action on the calcium channels there is action on the calcium channel gabapentin binds with the alpha 2 receptor or alpha 2 subunit of the voltage-gated calcium channel where it binds it binds to the alpha to s subunit of the voltage-gated calcium channel that reduces the calcium entry and that’s
How it reduces the synaptic release that’s how it reduces the synaptic release of the glutamate which is a excitatory neurotransmitter and that’s how it exert its anticonvulsant action what is the action on the calcium channel gabapentin binds with the alpha 2 s sub unit of the voltage-gated calcium channel when it binds to this calcium channel it reduces the
Calcium entry and when it reduces the calcium entry it reduces the synaptic release of glutamate which is a excitatory neurotransmitter and that is the what we can say contribute for its anticonvulsant effect for megakinetic properties neither it is metabolized in the body and nor it is an enzyme inducer it is not metabolized in the body and it is not an enzyme
Inducer when it is given orally oral bioliability is 50 oral bioliability is 50 it does not bind to the plasma protein it will get excreted unchanged in the urine it does not bind to the plasma protein it will get excreted and change in the urine so it can safely combine with the enzyme inducers like antipilaptics enzyme inducer antipleftrics like phenytoin and
Phenobarbitom because it is not an enzyme inducer or it is not metabolized in the body so we can easily combine or safely combine with the other enzyme inducer and epileptics or phenytoin or phenobarbiton and it can be used in hepatic dysfunction or hepatic failure patients because it is not metabolized in the body and it will get excreted unchanged in the urine
Now where it is used this gabapentine is used for the partial scissors and generalized tony clonic scissor it is used for the partial scissors and generalized tonic lone scissor but as an adjuvant not as an drug of choice you can use as an adjuvant in case of partial scissors or generalized tonic lonic user it is also effective for the neuropathic pain it is
Also effective for the neuropathic pain and post herpetic neuralgia it relieves the acute muscle spasm because it was developed as a spasmolitic anti-spasmodic drug so you can use in cases of acute muscle spasm post herpetic neuralgia or in case of diabetic neuropathic pain but you can use as an adjuvant drug for the partial scissors or in case of generalized
Tonic lonic scissor adverse effects or side effects like sedation there is a headaches dizziness ataxia and tremors these are the side effects or adverse effect those those is very important 300 milligram od orally when it is started initially 300 milligram worry orally once daily or you can increase the dose up to 1800 milligram per day in three divided doses
You can increase up to 1 800 milligram per day but initially you have to start with the 300 milligram od brand names which comes under like gabapene gabatin gaba jasik pentanor pro gaba lara gab gabatar these are the various brand name which is present in the clinical market which is this cabba pin is available as a 100 milligram 300 milligram 400 milligram and
450 milligram slow release tablet or sustainably established these are the various brand name now there is one more container that is the pre-gabaline this pre-gabaline it’s a gaba analog or we can say it’s a gabapentine container what is pregabalin it’s a gaba analog or it’s a gabapentine container and it is most commonly used or drug of choice for the painful
Diabetic neuropathy pregabalin is a drug of choice for the painful diabetic neuropathy it will act similarly like gabapentine it acts by increasing the gaba concentration in the brain mechanism fraction is almost similar to the gaba pentene it acts by increasing the gaba concentration in the brain the dose is 150 to 600 milligram orally and it is very well
Absorbed when it is given orally overall bioavailability is almost 70 percent half life is 7 to 8 hours there is no plasma protein binding it is not metabolized in the body same like gabapentine right and it is used in cases as an adjuvant for partial scissors generalized honeyclonic scissor same like gabapentine it’s a gabapentine container newer drug it’s a
Gaba analog neurodrug and it’s a drug of choice for the painful diabetic neuropathy right and it is also used in case of the wrist leg restless leg syndrome spinal cord injury post herpetic neuralgia and neuropathic pain which is associated with the diabetic mellitus or you can say painful diabetic neuropathy it is most commonly used drug nowadays pregabalin
Which is a nothing but a gabapentine container or gaba analog mechanism faction is almost similar for magnetic properties like oral availability 70 percent half life is seven to eight hours it is not metabolized there is no plasma protein binding and uses almost similar like gaba pentene so this pre-gabaline and gabapentine these are the newer antipeleptic and
They are used in other cases like neuropathic pain post herpetic neuralgia and it also release the acute muscle spasm also so this is all about the gabapentin and pregabalin
Transcribed from video
Gabapentin & Pregabalin: Newer Antiepilectic Agents By Dr NITIN PURAM
