BB2 Drugs Flashcards
Phenytoin
NA channel blocker
Stabilises inactivated state of channels; dose –dependent or zero order or saturation kinetics; liver enzyme induction; teratogenic effects; not used in absence seizures
Carbamazepine
NA channel blocker Stabilises the inactivated state of channels; liver enzyme induction; hypersensitivity reactions; not used in absence seizures
Sodium valproate
NA channel blocker
used in all
Not in pregnancy
Lamotrigine
Also activity at calcium channels; presynaptic inhibition of glutamate release – Favourable in pregnancy
Na channel blocker
Lacosamide
Binds to the inactivated state of channels
NA channel blocker
Zonisamide
Na + ca channel blocker
Ethosuximide
Calcium channel blocker
Used in absence seizures(Petit mal), blocks T-type calcium channels
Gabapentin (pregabalin)
Calcium channel blocker
Also increases GABA levels– Target the a2δ subunit
Benzodiazepines
Clonazepam
GABAA receptor positive allosteric modulators -
Sedation
Phenobarbitone
Barbiturate
GABAA receptor positive allosteric modulators
Levetiracetam
Neurotransmitter release
Binds to the synaptic protein SV2A; modulates neurotransmitter release
Tiagabine
Neurotransmitter uptake
Inhibits GAT-1 transporter for GABA
Vigabatrin
Neurotransmitter synthesis
Inhibition of GABA transaminase protection of GABA
Topiramate
Na channel blocker
also active at AMPA and kainite glutamate receptors
Acetylcholinesterase inhibitors
Rivastigmine
Donzepezil
Galantamine
= Used in Alzheimers
NMDA receptor antagonist
Memantine (used in Alzheimers)
Acute Migraine treatment + MoA
Sumatriptan
5HT1D/B Agonist
Prophylactic Migraine treatment + MoA
Methysergide
5HT2B Antagonist
Amitriptyline
Tricyclic AD
MoA of tricyclic antidepressants + SE
Inhibit reuptake of amines (5HT and NA)
Also act on H1 receptors, muscarinic, A1 +2 adrenoreceptors
SE - blurred vision, urinary retention, dry mouth, weigh gain,arrhythmias
Cardiotoxicity in overdose
Noritryptyline
Tricyclic AD
Clomipramine
Tricyclic AD
Imipramine
Tricyclic AD
Desipramine
Tricyclic AD