Neuro-Epileptic Drugs Flashcards
What is the definition of a seizure
Transient alteration of behavior due to disordered synchronous and rhythmic firing of brain neurons
What class of drug is Oxcarbazepine
Prolonged fast inactivation voltage gated sodium channel
What is the correlation between barbituates and needed levels of GABA
GABA independent
Which class is gabapentin
Alpha calcium channel
Which type of conditions can Calcium the T channels AEDs be used to treat
Petit mal aka absence seizures
What is the mechanism of Vigabatrin
Blocks metabolism of GABA-T
What is the general psychological risk associated with all AED
Depression and suicidal thoughts
What are the AED indications for primidone
Tonic/colon seizures
What are the sedating drugs given for treatment of nonconvulsive state epilepticus
- Lorazepam
- Diazepam
- midazolam
- Clonazepam
Which class is ethosuximide
T type Calcium Channel inhibitor
What drug class if Topiramate
AMPA receptor antagonist
What is the mechanism of action for Tiagabine
Blocks the reuptake of GABA via GAT1, leading to increased concentration in the cleft
What type of channel mediates the absence (petit mal) seizure
T type calcium channels
What are the AED indications for phenobarbital
Broad spectrum
-Epilepsy
What is the result of AED inducers taken with anticoagulants
Increase the clearance of warfarin, resulting in the increased risk for clots and thrombosis `
Which class is levitiracetams (and all -racetams)
Synaptic vesicles 2A proteins which loads Glutamate into vesicles
What are the AED indications for perampanel
Simple and complex seizures
What is the side effect of giving valproic acid or lamotrigine
-Inhibits conjugation of grubs by UGT, resulting in the accumulation of parent drug
What class of drug is lamotrigine
Prolonged fast inactivation voltage gated sodium channel
How do AMPA receptors function
Ligands bind to the AMPA receptor and allow depolarization
Which class is pregabalin
Alpha calcium channel
Which class is clonazepam
Benzodiazepine (aka post synaptic GABAreceptor)
What are the AED indications for lacosamide
Simple and complex seizures
What is the mechanism of valproic acid
Blocks metabolism of GABA via GABA-T
If a patients comes into the hospital with status epilepticus, what are the drugs given via the second IV
Fosphenyoin
Phenytoin
Valproic acid
Levetiracetam
What is the correlation between benzodiazapines and needed levels of GABA
Benzodiazepines are GABA dependent
What is the result of AED inducers taken with HIV medications
Increases the clearance and increased risk of HIV replication
What are the side effects of vigabatrin
Progressive, permanent, bilateral concentric vision loss
What are the AED indications for diazepam
Epilepsy
What is the mechanism of action for benzodiazepines
-Bind to an allosteric GABA receptor binding site that potentiates GABA binding and hyperpolarization
What is unique about carbamazepine and its metabolism
Induces CYP450, which subsequently increases its own metabolism, so there is a drop in efficacy of the drug, leading to recurrent seizures
What are the AED indications for valproic acid
- Absence seizure
- Broad spectrum seizure
- Epilepsy
What are the AED indications for lamotrigine
Simple and complex Parital seizures
Which class is primidone
Barbituate (aka post synaptic GABAreceptor)
What drug class is perampanel
AMPA-receptor antagonist
What are the three general classes of AED that inhibit the post synaptic GABA receptors
- Barbituates
- Benzodiazapines
- Topiramate
Which class of drug is Tiagabine
Presynaptic GAT-1 inhibitor
What are the AED indications for Ethosuzimide
Absence seizures
What class if felbamate
NMDA receptor antagonist
What is the mechanism that some AED can cause osteoporosis
They induce CYP450, which causes vitamin D catabolism, resulting in lower circulating levels. This decreases absorption of Calcium in the intestine and subsequent increased PTH secretion and demineralization from bone
What are the AED indications for lorazepam
Epilepsy
What are the steps in the activation and depolarization of sodium voltage gated channels
1) Resting state (activation gate closed)
2) Open state (both open)
3) Fast-Inactivated (inactivation gate closed)
4) Inactivated closed (both gates closed)
Which class of drug is lacosamide
Prolonged fast inactivation voltage gated sodium channel
What class of drug is vigabatrin
Presynaptic GABA-T inhibitor
What are the side effects of carbamazepine
- Inducer of CYP-450
- Leukopenia/neutropenia/thrombocytopenia
- Osteoporosis
How does the action of binding for the AED on voltage gated sodium channels effect when the AED can actually bind
AEDs can only bind to the pore when the activation gate is open, whcih is in the open state or the fast-Inactivated state
What are the AED indications for clonazepam
- Absence seizure
- Myoclonic seizure
What class of drug is valproic acid
Presynaptic GABA-T inhibitor
What is the effect of the the newer AEDs that are eliminated by the kidneys, rather than the liver
Patients with renal insufficiency must have their dose levels adjusted
Which drug class is Lacosamine
Enhanced slow inactivation voltage gated sodium channel
What class of drug is Carbamazepine
Prolonged fast inactivation voltage gated sodium channel
What is the definition of epilepsy
Acquired or inherited malformation of neuronal ion channels or NT systems that disrupt the electrical activity of the brain
Which class is phenobarbital
Barbituate (aka post synaptic GABAreceptor)
Which class of drug is valproic acid
Prolonged fast inactivation voltage gated sodium channel
What is the mechanism of an enhanced slow inactivation of sodium channels
Prolonged depolarized stimuli, the drug will reduce the amplitude and frequency of the sustained repetitive firing spikes
What are the AED indications for levetiracetam
Epilepsy
What are the AED indications for primidone
Simple and complex partial seizures
If a patients comes into the hospital with status epilepticus, what is the first drug given if IV is not available
Midazolam
What are the side effects associated with Phenytoin
- Inducer of CYP450
- gingival hyperplasia
- hypothyroidism
- CV risk
- Hypocalcemia/Osteoporosis
What are the nonsedating drugs given for treatment of nonconvulsive state epilepticus
- Phenytoin
- Fosphenytoin
- Valproate
- Levetiracetam
- Lacosamide
Which AED drugs are associated with osteoporosis during chronic use
- Cabamazepine
- Phenytoin
- Phenobarbital
- Valproic acid
What are the AED indications for phenytoin
Tonic/clinic seizures
-Epilepsy
What are the side effects of phenobarbital
- Inducer of CYP450
- CNS depression
- Osteoporosis
Which class of drug is topirimate
Prolonged fast inactivation voltage gated sodium channel
What is the result of AED induces while taking OCs
Increases the clearance of the OC, resulting in increased risk of pregnancy
What are the AED indications for topiramate
Broad spectrum
Which class of drug is zonisamide
Prolonged fast inactivation voltage gated sodium channel
What is a generalized seizure
Seizure that involves both hemispheres
What is the binding site of AEDs with regards to those that bind to the voltage gated sodium channels
Binding site is in the interior of the sodium channel
Which class of drug is phenytoin
Prolonged fast inactivation voltage gated sodium channel
What allergic reaction is possible with the drug zonisamide
Allergic reaction to a sulfonamide
Which class is diazepam
Benzodiazepine (aka post synaptic GABAreceptor)
What are the AED indications for oxcarbazepine
Simple and complex partial seizures
What is meant when they say that sodium voltage gated AED are use dependent
Because they bind to the inside of the pore, they can only bind when the pore is open. Therefore, the amount of binding is proportional to the frequency that the channel is open
Which class of drug is Rufinamide
Prolonged fast inactivation voltage gated sodium channel
Which class is lorazepam
Benzodiazepine (aka post synaptic GABAreceptor)
What is a complex partial seizure
Starts in a localized cortical site and includes impairment of consciousness
What is the mechanism of action for Barbiturates
Bind to an allosteric binding site on GABA receptor and increased Chloride channel opening
Which class is Topiramate
GABA agonist
- Sodium fast inactivator
- AMPA receptor blocker
What is a simple partial seizure
Starts in a localized cortical region and included the Preservation of consciousness
What is the side effect of giving phenytoin, carbamazepine, or phenobarbital
Inducers of CYP 450
Induces conjugation of drugs by UGT, resulting in the reduction of the parent drug
If a patients comes into the hospital with status epilepticus, what is the first drug given via IV
Lorazepam or diazepam
Which class is clobazam
Benzodiazepine (aka post synaptic GABAreceptor)
What are the characteristics of a sodium channel when it is in the inactivated state
Aka fast inactivated state
-Can not be deactivated directly or instantly because it is closed from the inside
What are the AED indications for carbamazepine
Broad spectrum
What are the kinetics associated with Phenyoin
Zero order
