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Antiepileptics
IUSM
16
Pharmacology
Professional
11/22/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
diazepam
Definition
Class: antiepileptic, benzodiaepine

Mechanism: enhance binding of GABA to receptors

Indications: status epilepticus, generalized epilepsies

Adverse effects: sedation, respiratory depression; tolerance, dependence and withdrawal
Term
lorazepam
Definition
Class: antiepileptics, benzodiazepine

Mechanism: enhances binding of GABA to receptors

Indication: status epilepticus, generalized epilepsies

Adverse effects: sedation, respiratory depression; tolerance, dependence, and withdrawal
Term
carbamazepine
Definition
Class: antiepileptic

Mechanism: stabilize VG sodium channels in (fast) inactivated conformation; decrease VG calcium conductance

Indication: localization-related epilepsies, trigeminal neuralgia

Adverse effects: double vision, dizziness, nausea, headache, hyponatremia, leukopenia, rash, fetal neural tube defects

Pharmacokinetics:
Metabolism - P450, active metabolite with more side effects
short half-life
Term
ethosuximide
Definition
Class: antiepileptic

Mechanism: blocks t-type calcium channels

Indication: absence epilepsy

Adverse effects: nause, hiccups, anorexia, rash, Lupus syndrome

Pharmacokinetics:
Metabolism - liver
Term
gabapentin
Definition
Class: antiepileptic

Mechanism: binds calcium channels (reduces expression through internalization); enhances GABA SYNTHESIS

Indication: adjuct therapy in localization-related therapy, post-herpetic neuralgia

Adverse effects: mild N, somnolence, lightheadedness

Pharmacokinetics:
Eliminatino - unchanged in urine
Term
pregabalin
Definition
Class: antiepileptics

Mechanism: bind calcium channels (reduce expression through internalization); enhances GABA TRANSPORT

Indication: adjuct therapy in localization-related epilepsies, post-herpetic neuralgia, DIABETIC NEUROPATHY PAIN, fibromyalgia

Adverse effects: mild N, somnolence, lightheadedness

Pharmacokinetics:
Excretion - unchanged in urine
Term
lacosamide
Definition
Class: antiepileptic

Mechanism: stabilizes VG sodium channels inactivated state; binds CRMPs that play a role in ion channel trafficking and neuronal sprouting

Indication: combo w/ other drugs for localization-related epilepsy

Adverse effects: prolong PR interval leading to atrial ventricular block (effect on cardiac Na channels), mild dizziness, ataxia, N/V, diplopia

Pharmacokinetics:
Metabolism - liver
Excretion - 40% unchanged in urine
Term
lamotrigine
Definition
Class: antiepileptics

Mechanism: stabilizes VG sodium channels inactivated state; inhibits glutamate release; affects t-type calcium channels

Indications: used alone or in combo for multiple types of epilepsy

Adverse effects: severe/life-threatening rash

Pharmacokinetics:
Metabolism - liver
Term
levetiracetam
Definition
Class: antiepileptics

Mechanism: inhibits calcium channels, interaction withh a unique synatpic vesicle protein (SV2A) --> reduces ability of vesicle to dock and release NT

Indication: adjuvant in tx of localization-related epilepsies

Adverse effects: somnolence, weakness, headache, behavioral difficulties

Pharmacokinetics:
Excretion - renal, unchanged
Term
phenobarbital
Definition
Class: antiepileptic

Mechanism: prolongs length of time GABA-activated Cl channel remain open, block VG calcium channels, direct inhibtion of NMDA-type glutamate receptors

Indication: multiple types of epilepsy, historical drug

Adverse effects: somnolence, depression, behavioral problems, hyperactivity, rash, Lupus syndrome

Pharmacokinetics:
Half-life - 60-110hr
Metabolism - enzyme inducer and inhibits metabolism of other drugs
Term
phenytoin
Definition
Class: antiepileptics

Mechanism: stabilizes VG sodium channels inactivated conformation, inhibits VG calcium channels, stimulates Na/K ATPase activity

Indication: localization-related epilepsies, status epilepticus

Adverse effects: nystagmus, ataxia, gingival hyperplasia, rash, blood sycrasias, skin necrosis, cardiac arrhythmias

Pharmacokinetics:
ZERO-ORDER, NON-LINEAR PHARMACOKINETICS
Metabolism - induces hepatic enzymes
Term
fosphenytoin
Definition
Class: antiepileptics

Mechanism: SOLUBLE PRO-DRUG OF PHENYTOIN; stabilizes VG sodium channels inactivated conformation, inhibits VG calcium channels, stimulates Na/K ATPase activity

Indication: localization-related epilepsies, status epilepticus; can be given faster than pheyntoin (IV or IM)

Adverse effects: fewer than penytoin, but same?

Pharmacokinetics:
ZERO-ORDER, NON-LINEAR PHARMACOKINETICS
Metabolism - induces hepatic enzymes
Term
tiagabine
Definition
Class: antiepileptic

Mechanism: inhibits reuptake of GABA

Indication: localization-related epilepsies

Adverse effects: tremor, dizziness, nervousness, difficulty concentrating, somnolence

Pharmacokinetics:
Metabolism - liver
Term
topiramate
Definition
Class: antiepileptic

Mechanism: direct potentiating actions on GABA receptor at unique site; inactivates VG sodium channels; prevents calcium influx

Indications: localization-related epilepsies, generalized epilepsies, migraine headache prevention

Adverse effects: psychomotor slowing, fatigue, N, parathesias, weight loss, kidney stones

Pharmacokinetics:
Elimination - renal
Term
valproate
Definition
Class: antiepileptics

Mechanism: inhibits metabolism and promotes synthesis of GABA; inactivates VG sodium channel in unique manner; blocks t-type calcium channels

Indications: localization-related epilepsies, generalized epilepsies, absence epilepsy, migraine headache prevention

Adverse effects: weight gain, hair loss, tremor, liver failure, pancreatitis, thrombocytopenia, neural tube defects

Pharmacokinetics:
Metabolism - liver, enzyme inhibitor
Term
zonisamide
Definition
Class: antiepileptics

Mechanism: direct potentiating actions on GABA receptor at unique site; inactivates VG sodium channels; prevents calcium influx

Indication: adjuvant for localization-related epilepsies

Adverse effects: psychomotor slowing, fatigue, N, parathesias, weight loss, kidney stones

Pharmacokinetics:
Elimination - renal
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