Antiepileptics Flashcards
First line drug for petit mal seizures
Second line
Valproate and ethosuximide- 1 st line
Clobazam (benzo) -2nd line
First line drug for tonic clonic seizures
Second line
Valproate - 1st line
Phenobarbitone- 2nd line
First and second line for complex partial seizures
Carbamazepine- 1st
Taigabine- 2nd
What are the 3ways GABA can be targeted? Give one drug as an example each.
- Inhibit GABA transaminase - valproate
- Block transporter for GABA reuptake - tiagabine
- Modulate GABA receptor activity via allosteric receptor - Benzo (midazolam) barbiturate (phenobarbitone)
Mx action valproate/ vigabatrin
Inhibit GABA transaminase (GABA-T) which metabolises GABA - valproate
Mx action of tiagabine
- Block transporter for GABA reuptake - tiagabine
Action of diazepam/ clonazepam/ clobazam/ midazolam.
Modulate GABA receptor activity via allosteric receptor - Benzo (midazolam) barbiturate (phenobarbitone)
Action of phenobarbitone and primidone
Modulate GABA receptor activity via GABA a allosteric receptor - Benzo (midazolam) barbiturate (phenobarbitone)
Carbamazepine, phenytoin and gabapentin act on:
Target Na channels of high frequency firing neurons- active in seizures - without interfering with low firing normal state neurons
Ca channel targets can be targeted dependent on voltage. What are two examples ?
Low voltage - T type (assoc. with petit mal) : ethosuximide High voltage (assoc. with partial) : levetiracetem
Phenytoin S/E
Gum hypertrophy
Acne
Hirsutism
Most anti epileptics: sedation and skin rashes
Most anti epileptics interfere with liver enzyme CYP450- promoting or inhibiting it’s ability to metabolise other drugs
Carbamazepine S/E:
Bone marrow depression
Most anti epileptics: sedation and skin rashes
Most anti epileptics interfere with liver enzyme CYP450- promoting or inhibiting it’s ability to metabolise other drugs
Valproate S/E:
Weight gain
Alopecia
Most anti epileptics: sedation and skin rashes.
Most anti epileptics interfere with liver enzyme CYP450- promoting or inhibiting it’s ability to metabolise other drugs
Most anti epileptics interfere with liver enzyme CYP450- promoting or inhibiting it’s ability to metabolise other drugs
Inducer of cyp450- phenobarbitone phenytoin carbamazepine
Inhibitor of cyp450- valproate
Pregnancy contraindications of phenytoin and valproate
Phenytoin- palate deformity, heart defects. (Folate/Vit K)
Valproate - spins bodies