10 keto analog of carbamazepine Dose 300 mg PO BID titrated gday MOA

10 keto analog of carbamazepine dose 300 mg po bid

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10-keto analog of carbamazepine Dose: 300 mg PO BID (titrated upto 1.2 – 2.4 g/day) MOA : use-dependent blockade of Ѵ-gated Na + channels 10-Hydroxycarbazepine is active metabolite Eslicarbazepine acetate (Aptiom®) (prodrug; 10-hydroxycarbazepine) Pharmacokinetics: t 1/2 = 2 hrs (parent); ~ 9hrs (active metabolite) Mild inducer of CYP3A4/5 Adverse Effects : (dose-related) Hyponatremia is more common than w/carbamazepine Sedation, dizziness, ataxia, nausea Drug-drug interactions: doses Trileptal may plasma [oral contraceptives] Strong hepatic inducers / inhibitors can impact trileptal levels? oxcarbazepine (Trileptal ® ) *
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topiramate (Topamax ® ) Sulfamate-substituted monosaccharide Broad-spectrum AED activity Approved monotherapy : partial & generalized seizures Also approved for migraine prophylaxis; weight control Dose: (AED-mono) 200 mg PO, BID (IR) or 400 mg PO/day (ER) (AED – adj) 100 – 200 PO, BID (IR) or 200 – 400 PO/day (ER) No contraindication with sulfonamide allergy Multiple mechanisms of action (MOA): 1. Blocks Ѵ -gated Na + channels (similar to phenytoin) Also activates hyper-polarizing K + channels 2. Antagonist at AMPA / kainate glutamate receptors 3. Enhance GABA A -channel activity 4. Weak inhibitor of carbonic anhydrase what side effect concern?
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topiramate (Topamax ® ) Pharmacokinetics: linear PK ~20% plasma protein binding; t ½ = ~ 24 hrs Undergoes metabolic oxidation and hydroylsis Eliminated unchanged in urine; dose adjust w/ impairment Adverse effects: cognitive impairment @ high dose or fast titration drowsiness, fatigue, memory impairment, weight loss Chronic use: nephrolithiasis / vision changes may also occur Due to inhibition of carbonic anhydrase Drug-drug Interactions: TOPiramate inhibits CYP2C19 / mild inducer of CYP3A4 Variable effects on [ phenytoin ] plasma levels Topiramate (200mg) metabolism oral contraceptives Trokendi XR ®
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lamotrigine (Lamictal ® ) Dose: 25-50 mg/day PO; titrate upto 100-200 mg/day MOA: Ѵ -gated Na + channel (like PHT / CBZ) Inhibits propagating neuronal action potential Pharmacokinetics: Ph-2 metabolism via UGT N-glucuronidation; t 1/2 = 24-35 hr Adverse effects : N/V, drowsiness, dizziness, ataxia, diplopia, alopecia Dose adjust with hepatic impairment Boxed-warning : serious skin reactions (SJS / TEN); rate in pediatrics >> adults; Rash when combined w/ valproic acid (life-threatening!) DDIs : Valproate inhibits UGT; [LMT] plasma and t 1/2 CBZ, PHT, PHB induces UGT; [LMT] plasma and t 1/2 ritonavir, rifampin, oral E 2 contraceptives [LMT] plasma
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levetiracetam (Keppra ® ) Broad spectrum AED
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