Karbamazepin sebagai Antiepileptic Agent
DOI:
https://doi.org/10.29313/jrf.v3i1.3165Keywords:
karbamazepin, sifat fisikokimia, mekanisme kerja, farmakokinetik.Abstract
Abstract. Epilepsy is a chronic neurological disorder that affects 65–70 million people globally. It occurs in all sexes and at all ages, especially in childhood and adolescence, and increases with age. Carbamazepine is a commonly prescribed antiepileptic drug which is a first-line drug for partial seizures, belonging to the Biopharmaceutical Classification System (BCS) class II, which means that carbamazepine has high membrane permeability (almost 90% of carbamazepine is absorbed in the gastrointestinal tract) and low water solubility. low (solubility practically insoluble in water, soluble in ethanol and in acetone). Carbamazepine has 3 forms of polymorphism. Carbamazepine is an antiepileptic that works on voltage-gated sodium channels, often referred to as sodium channel blockers, which play an important role in the initiation and propagation of neuronal action potentials. Carbamazepine is highly bound to plasma proteins ranging from 75-80% of the total plasma concentration. Bioavailability ranges from 75-85%. Carbamazepine induces its own metabolism, causing increased clearance, shortened serum half-life, and progressive decrease in serum levels.
Abstrak. Epilepsi merupakan gangguan neurologis kronis yang mempengaruhi 65–70 juta orang secara global. Itu terjadi pada semua jenis kelamin dan di segala usia, terutama di masa kanak-kanak, remaja,dan semakin meningkat seiring bertambahnya usia. Karbamazepin merupakan obat antiepilepsi yang biasa diresepkan yang merupakan obat lini pertama untuk kejang parsial, tergolong dalam Biopharmaceutical Classification System (BCS) kelas II yang artinya bahwa karbamazepin memiliki permeabilitas membran yang tinggi (hampir 90% karbamazepin diabsorbsi di saluran pencernaan) dan kelarutan dalam air yang rendah (Kelarutannya praktis tidak larut dalam air, larut dalam ethanol dan dalam aseton). Karbamazepin memiliki 3 bentuk polimorfisme. Karbamazepin merupakan antiepilepsi yang bekerja pada voltage-gated sodium channel sering disebut dengan sodium channel blockers berperan penting dalam inisiasi dan propagasi aksi potensial neuron. Karbamazepin sangat terikat dengan protein plasma berkisar antara 75-80% dari total konsentrasi plasma. Bioavailabilitas berkisar antara 75-85%. Karbamazepin menginduksi metabolismenya sendiri, menyebabkan peningkatan klirens, memperpendek waktu paruh serum, dan penurunan kadar serum secara progresif.
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