Pharmacology Flashcards
What is the AED that binds to a synaptic vesicle protein SV2A, which is involved in pre-synaptic neurotransmitter release?
Levetiracetam (broad spectrum)
What is the AED that blocks low-threshold T-type Ca2+ channels?
Ethosuximide (only for generalized onset seizures)
Which AED is an AMPA antagonist?
Perampanel
Which AEDs are broad spectrum and work in both focal or generalized onset seizures? (5)
- Phenobarbital
- Valproic acid
- Lamotrigine
- Topiramate
- Levetiracetam
Which AED only works in generalized onset seizures?
Ethosuximide
Which AEDs work only in focal onset seizures? (2)
- Carbamazepine
2. Oxcarbamazepine
Which AED is associated with highest rate of teratogenicity among antiepileptic medications?
Valproic acid (broad spectrum) Increases synaptic GABA
Also associated with weight gain
Which AED is associated with a hypersensitivity causing mild maculopapular or erythematous rash? What is this rash called?
Lamotrigine is the most likely AED to cause Stevens-Johnson syndrome
Lamotrigine is broad specturm Na+ channel blocker
Which AED is most likely to cause renal stones due to inhibition of carbonic anhydrase?
Topiramate (broad spectrum) Several MOA: Na+ channel blocker Glutamate receptor blocker Enhances GABA-A receptor activity Reduces L-type, high voltage activated Ca2+ channel activity
Which AED is associated with adverse side effects of behavior and mood changes such as agitation, anxiety, depression, and acute psychosis?
Levetiracetam (broad spectrum)
Binds to SV2A (synaptic vesicle protein) which is involved in presynaptic neurotransmitter reslease
With what drug does Valproic acid have a significant reaction with? What is the reaction?
Valproic acid (broad specturm, GABA) interacts with Lamotrigine (broad spectrum, Na+ channel) by increasing its metabolism and therefore increasing the amount of Lamotrigine in the blood. If patient is on both, need to watch levels of Lamotrigine b/c you might need to lower thier dosage
Which two AEDs have no significant drug interactions? What are their MOA?
Lacosamide (focal, Na+ channel)
Levetiracetam (broad spectrum, SV2A)-excreted renally, no hepatic metabolism
What is the MOA of ethosuximide?
blocks T-type Ca2+ channels in thalamo-cortical circuits
ONLY GENERALIZED ONSET AED
Which AED follows zero order kinetics, and why is that important?
Phenytoin (focal, prolongs inactivation of Na+ channels)
Zero order kinetics- non-linear pharmacokinetics meaning that at certain doses, a very small increase in dose may cause a very large increase in drug concentration in the blood, must be careful
What are the 4 direct acting muscarinic cholinomimetic drugs and the 1 direct acting nicotinic drug ?
Muscarinic
- Bethanechol
- Muscarine
- Pilocarpine
- Cevimeline
Nicotinic
1. Nicotine
Which direct acting muscarinic cholinomimetic drug is used for post-operative and neurogenic ileus and urinary retention?
Bethanechol-muscarinic
Recall that bowel and bladder smooth muscle is ACh-innervated
Remember that neostigmine is the indirect acting AChE inhibitor used for post op and neurogenic ileus and urinary retention
Side effects: SLUDGE
Which direct acting muscarinic cholinomimetic drug is used for glaucoma? Side effects?
Pilocarpine (muscarinic)
ACh activates sphincter and ciliary muscles of eye
Remember that physistigmine is the short acting and echothiophate is the long acting indirect acting AChE inhibitor used for glaucoma
Side effects: SLUDGE
Which direct acting muscarinic cholinomimetic drug is used for dry mouth (e.g. Sjogren’s) via increased salivation? Side effects?
Cevimeline (muscarinic)
Side effects: SLUDGE
Which direct acting nicotinic cholinomimetic drug is used for smoking cessation to reduce cravings?
Nicotine (nicotinic)
What side effects are included in SLUDGE?
S: salivation L: lacrimation U: Urination D: Defecation G: GI distress E: Emesis
All of these effects can be blocked by atropine
What are the 7 indirect acting AChE inhihbitors and 1 AChE regenerator?
AChE inhibitors
- Neostigmine
- Physostigmine
- Donepezil
- Edrophonium
- Echothiophate
- Sarin
- Parathion
AChE regenerator:
1. Pralidoxime