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Unit 7 Pharm - Epilepsy
Epilepsy drugs
14
Pharmacology
Graduate
04/04/2012

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Cards

Term
Phenytoin (Dilantin)
Definition

MECH: Stabilize inactive conformation of membrane Na+ channel inhibiting depolarization. Lengthens refractory state and slows rate of action potential firing.

USE: For acute seizures (Primary generalized epilepsy or partial onset and secondarily generalized epilepsy). Use IV preparation (beware of hypoT) for status epilepticus (persistent seizure).

AE: Hepatotoxicity, induces liver enzymes, contraceptive failure, myelosuppression, hirsutism, lupus-like. Long term use: cerebellar degeneration, peripheral neuropathy, osteoporosis.

TOX: Dizziness, Nystagmus (involuntary saccade), ataxia (lack of voluntary coordinated mvmnt), incoordination.

Term
Carbamazepine
Definition

MECH: Stabilize inactive conformation of membrane Na+ channel inhibiting depolarization. Lengthens refractory state and slows rate of action potential firing.

USE: For Complex partial epilepsy (both hemispheres--impaires awareness or responsiveness, loss of consciousness). Also used in Bipolar disorder and neuropathic pain.

AE: Heteroinduction and autoinduction, contraceptive failure, rash (rarely Stevens-Johnson).

TOX: Sedation, ataxia, diplopia (dizzy, drunk, double vision).

Term
Oxcarbazepine
Definition

Active metabolite of Carbamazepine (bypasses carbamazepine epoxide)

MECH: Stabilize inactive conformation of membrane Na+ channel inhibiting depolarization. Lengthens refractory state and slows rate of action potential firing.

USE: For Complex partial epilepsy (both hemispheres--impaires awareness or responsiveness, loss of consciousness). Also used in Bipolar disorder and neuropathic pain.

AE: LESS Heteroinduction and autoinduction, contraceptive failure, rash (rarely Stevens-Johnson).

TOX: LESS Sedation, ataxia, diplopia (dizzy, drunk, double vision).

Term
Lamotrigine
Definition

MECH: Blocks Na+ channel inhibiting depolarization. Lengthens refractory state and slows rate of action potential firing.

USE: Good for long-term use. Primary generalized epilepsy, partial complex epilepsy, secondary generalization, absence seizures. OK for kids. NOT okay for myoclonic seizures. Also used in Bipolar and neuropathic pain. Competes with valproate for excretion so when used together, less dose needed.

AE: Heteroinduction, contraceptive failure, rash (rarely Stevens-Johnson--slow initial titration).

TOX: Sedation, ataxia, diplopia (dizzy, drunk, double vision).

Term
Valproate
Definition

MECH: Mech unkown??? Probably involves Na+ channels and GABA.

USE: Broad spectrum use--Absence, myoclonic, tonic-clonic seizures of primary generalized, partial onset and secondarily generalized seizures. Also Bipolar and Migraine prophylaxis. IV route in Status Epilepticus.

AE: Nausea, wt. gain, hair loss, hyperammonemia, teratogen (4-8%) -- NO in child bearing age.

TOX: Sedation, tremor.

 

Term
Gabapentin
Definition

MECH: GABA analog--but really blocks Ca2+ currents.

USE: NOT powerful anti-epileptics but used as adjunct for partial complex epilepsy. More common use is neuropathic pain. Absorption limited at gut.

AE: Not metabolized in humans (pee it out). No side effects.

Tox: Sedation.

Term
Pregabalin
Definition

MECH: GABA analog--but really blocks Ca2+ currents.

USE: NOT powerful anti-epileptics but used as adjunct for partial complex epilepsy. More common use is neuropathic pain.

AE: Not metabolized in humans (pee it out). No side effects.

Tox: Sedation.

Term
Topiramate
Definition

MECH: AMPA and Kainate Ca channel blocker. Also Na+ channel and GABA receptors.

USE: Partial onset and secondarily generalized seizures and primary generalized epilepsy. Also migraine prophylaxis.

AE: Inhibits Carbonic Anhydrase--mild metabolic acidosis--respiratory compensation--mild alkalosis--changes Ca2+ ionization state leading to tingling of fingers. Counteract with vitamin C--organic acid. Some wt. loss, kidney stones, acute glaucoma.

TOX: sedation, cognitive "word finding".

Term
Levetiracetam (kepra)
Definition

MECH: Binds to vesicle protein inhibiting release of neurotransmitter.

USE: Partial onset and secondarily generalized seizures.

AE: Well-tolerated--Irritability, aphasia, thrombocytopenia.

Tox: Sedation.

Term
Felbamate
Definition

MECH: Blocks NMDA receptor.

USE: Anticonvulsant for partial onset seizures with or without secondary generalization. Due to potentially serious side effects--used in refractory epilepsy.

AE: Aplastic anemia (reason why it isn't used), hepatic failure.

Term
Ethosuximide
Definition

MECH: Blocks t-type Ca2+ channels influx reducing release of neurotransmitter.

USE: Absence epilepsy only.

Term
Lorazepam
Definition

MECH: Acts at GABA-A receptors.

USE: Status epilepticus. More potent and shorter half life than diazepam. Good for acute usage then get another drug ready.

AE: Sedation limits dosage.

 

Term
Diazepam
Definition

MECH: Acts at GABA-A receptors.

USE: Status epilepticus. Longer half-life than diazepam.

AE: Sedation limits dosage.

 

Term
Midazolam
Definition

MECH: GABA-A receptor enhances GABA effects.

USE: Anesthesia or refractory status epilepticus.

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