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
Phenelzine
Monoamine Oxidase Inhibitors
TYRAMINE cheese effect
Tranylcycpromine
Monoamine Oxidase Inhibitors
Tyramine cheese effect
Iproniazid
Monoamine Oxidase Inhibitors
CHEESE EFFECT with tyramine
Citalopram
SSRI
Fluexitine
SSRI
Paraoxetine
SSRI
SE of SSRI
Nausea, Insomnia, Anxiety
Reversible monoamine oxidase inhibitor
Moclobemide
SNRI
Venlafaxine
NARI
Reboxetine