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35 Cards in this Set
- Front
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Carbamazepine |
prototype of the antiseizure drugs used in the treatment of focal onset seizures, focal to-bilateral tonic-clonic seizure, trigeminal neuralgia, and bipolar disorder. |
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Oxcarbazepine |
• A 10-keto analog of carbamazepine. • Less potent than carbamazepine. • Fewer hypersensitivity reactions. • Hyponatremia may occur more commonly with oxcarbazepine than with carbamazepine, most adverse effects of oxcarbazepine are similar to those of carbamazepine |
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Eslicarbazepine |
• A prodrug of S(+)-licarbazepine, provides an alternative to oxcarbazepine, with some minor differences. • The side effect profile includes dizziness, somnolence, diplopia, and headache. Serious adverse reactions such as rash, psychiatric side effects, and hyponatremia occur rarely. |
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Lacosamide |
• A functionalized amino acid that demonstrates efficacy in epilepsy and in neuropathic and chronic pain. • MOA: Selectively enhances Na+ channel slow inactivation but has no effects of fact activation. • Bioavailability is nearly 100% • Approved for adjunctive treatment of focal seizures. • It is available in an injectable formulation. • The most common adverse events that limit treatment include dizziness, headache, and fatigue. |
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Phenytoin |
• The oldest nonsedating drug used in the treatment of epilepsy.
• Most effective against generalized tonic-clonic seizure and partial seizure.
• MOA: is a sodium channel-blocking antiseizure drug that acts in a similar fashion to carbamazepine and other agents in the class.
• Common adverse effects includes ataxia, gingival hyperplasisa, diplopia, hirsutism, neuropathy and megaloblastic anemia |
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Fosphenytoin |
•is a water-soluble prodrug of phenytoin and can be use intramuscularly • Contraindicated in primary generalized epilepsies, including absence epilepsy, juvenile myoclonic epilepsy, and Dravet’s syndrome |
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Gabapentin |
• Analogs of GABA which was design to cross the BBB. • Effective in the treatment of focal seizures • MOA: Do not act via GABA but its bind avidly to α2δ, a protein that serves as an auxiliary subunit of voltage-gated calcium channels. It also indirectly enhance the release of GABA • Contraindicated via absence seizures and myoclonic seizures. • Frequently used in the treatment of neuropathic pain conditions, including postherpetic neuralgia and painful diabetic neuropathy, and in the treatment of anxiety disorders. |
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Pregabalin |
• is also approved for the treatment of fibromyalgia. • Pregabalin is used at much lower doses than gabapentin since it exhibits linear absorption • The most common adverse effects are somnolence, dizziness, ataxia, headache, and tremor. • These adverse effects are most troublesome at initiation of therapy and often resolve with continued dosing. |
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Tiagabine |
• A GABA analogue, second-line treatment for focal seizures • MOA: A selective inhibitor of the GAT-1 GABA transporter. It blocks GABA uptake into presynaptic neurons permitting more GABA to be available for receptor binding, and therefore, it enhances inhibitory activity. • is effective as adjunctive treatment in partial-onset seizures. • In postmarketing surveillance, seizures have occurred in patients using tiagabine who did not have epilepsy. • should not be used for indications other than epilepsy. |
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RETIGABINE (EZOGABINE) |
• A 3rd -line treatment for focal seizures • Its use is limited to those who have failed to respond to other agents because it causes pigment discoloration of the retina and skin. • MOA: An allosteric opener of KCNQ2-5 voltage-gated potassium channels, which are localized, in part, in axons and nerve presynaptic terminals causing the inhibition of the release of various neurotransmitters, including glutamate, which may be responsible for the seizure protection. • Due to the ophthalmologic adverse reactions, regulatory agencies have recommended use of retigabine only in cases where other antiseizure drugs are not adequate or not tolerated ble for the seizure protection. |
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Lamotrigine |
• Used effectively for the treatment of focal, generalized, absence seizures, and LennoxGastaut syndrome and bipolar disorder.
• MOA: Blocks and prolongs the inactivation of Na+ channels and inhibits the release of glutamate.
• Adverse effects are similar to those of other sodium channel-blocking antiseizure drugs.
• is useful for monotherapy and add-on therapy of partial and secondarily generalized tonic-clonic seizures in adults and Lennox-Gastaut syndrome in both children and adults.
• The drug is generally well tolerated; however, it can produce a potentially fatal rash (Stevens-Johnson syndrome) |
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LEVETIRACETAM |
• Approved for adjunctive therapy for myoclonic, partial-onset, and primary generalized tonic-clonic seizures in adults and children as young as 4 years old. • MOA: Its novel mechanism of action is modulation of synaptic neurotransmitter release through binding to the synaptic vesicle protein SV2A in the brain thereby reducing the release of the excitatory neurotransmitter glutamate during trains of high-frequency activity. • Adverse effects include somnolence, asthenia, ataxia, infection (colds), and dizziness. • Less common but more serious are behavioral and mood changes, such as irritability, aggression, agitation, anger, anxiety, apathy, depression, and emotional lability. |
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BRIVARACETAM |
• The 4-n-propyl analog of levetiracetam, is a high-affinity SV2A ligand recently approved for the treatment of focal (partial) onset seizures. • Contraindicated with carbamazepine and phenytoin. |
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PERAMPANEL |
• Approved for the treatment of focal seizures and primary generalized tonicclonic seizures in idiopathic generalized epilepsies. • MOA: A noncompetitive antagonist of the AMPA receptor, a subtype of the ionotropic glutamate receptor that is the main mediator of synaptic excitation in the central nervous system. • use is often associated with behavioral adverse reactions including aggression, hostility, irritability, and anger. • may decrease the effectiveness of levonorgestrel-containing hormonal contraceptives. |
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Phenobarbital |
• was introduced as a sleeping aid and later was serendipitously found to be useful in the treatment of epilepsy. • MOA: It act as positive allosteric modulators of GABAA receptors at low concentrations ; at higher concentrations, the drugs directly activate GABAA receptors causing an increase in mean open duration of the channel without altering either channel conductance or opening frequency. • is the oldest of the currently available antiseizure drugs. • It is still useful for neonatal (febrile) seizures. • The drug must be discontinued gradually over several weeks to avoid the occurrence of severe seizures or status epilepticus. |
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Primidone |
• A derivative of phenobarbital. • Clinically active in the treatment of epilepsy but was then largely abandoned because of its high incidence of adverse effects. • MOA: It alters sodium and calcium channel transport, reducing the frequency of nerve firing, which may be responsible for its effect on convulsions and essential tremor. It is effective for the treatment of essential tremor and is still used for this indication. •is metabolized to phenobarbital and phenylethylmalonamide • does not directly interact with GABA-A receptors or chloride |
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Felbamate |
•Used in the treatment of focal seizures and in the Lennox-Gastautsyndrome. • MOA: Unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors. • is generally well tolerated; some patients report improved alertness. • is used only for patients with refractory seizures who respond poorly to other medications because the drug can cause both aplastic anemia and severe hepatitis. |
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VALPROATE |
• A first-line broad-spectrum antiseizure drug used for myoclonic (such as in juvenile myoclonic epilepsy), atonic (as iLennox-Gastaut syndrome), and generalized onset tonic-clonic seizures.
• It is also effective in the treatment of generalized absence seizures and is often preferred to ethosuximide when the patient has concomitant generalized tonic-clonic seizures.
• Also used as a mood stabilizer in bipolar disorder and as prophylactic treatment for migraine.
• Intravenous formulations can be used to treat status epilepticus. |
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Divalproex |
•is a combination of valproic acid and sodium valproate. It has a better bioavailability and is better tolerated.
• The most common dose-related adverse effects of valproate are nausea, vomiting, and other gastrointestinal complaints such as abdominal pain and heartburn. It is also teratogenic. |
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Topiramate |
A broad-spectrum antiseizure drug used in the treatment of focal seizures, primary generalized seizures, and seizures in the Lennox-Gastaut syndrome. • is also commonly used for migraine headache prophylaxis. • MOA: It acts by (1) blocking voltage-gated sodium channels; (2) enhances GABAA receptor subtypes; and (3) blocks AMPA or kainate receptors. • The drug is approved for the Lennox-Gastaut syndrome and may be effective in juvenile myoclonic epilepsy, infantile spasms, Dravet’s syndrome (severe myoclonic epilepsy in infancy), and even childhood absence seizures. •Dose-related adverse effects that occur frequently in the first 4 weeks of topiramate therapy are somnolence, fatigue, dizziness, nervousness, and confusion. |
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Urolithiasis |
occurs in 0.5–1.5% of patients on long-term therapy and is more common in men. |
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Zonisamide |
• A broad-spectrum antiseizure drug that is effective for focal and generalized tonicclonic seizures in adults and children and may also be effective in some myoclonic epilepsies and in infantile spasms. • MOA: Acts by inhibiting T type Ca2+ currents and also by blocking Na+ channels. • has no clinically significant effects on the pharmacokinetics of other antiseizure drugs. • Both are associated with weight loss. They also both (rarely) cause kidney stones and oligohydrosis. • has high bioavailability and a long half-life of 1–3 days |
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Ethosuximide |
• A first-line drug of choice for the treatment of generalized absence seizures. • It can be used as monotherapy unless generalized tonic-clonic seizures are also present, in which case valproate is preferred or ethosuximide can be combined with another drug effective against generalized tonic-clonicseizures. • MOA: It acts by inhibition of low-voltage-activated T-type calcium channels in thalamocortical neurons that underlie the 3-Hz spikewave discharges of generalized absence seizures. • The most common dose-related adverse effect of ethosuximide is gastric distress, including pain, nausea, and vomiting. When an adverse effect does occur, temporary dosage reductions may allow adaptation. |
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Trimethadione |
It is effective in the treatment of generalized absence seizures. • MOA: Inhibits generation of T-type calcium currents in thalamic neurons, thereby stabilizing neuronal membranes, raising the threshold for repetitive activities in the thalamus • has numerous dose-related and idiosyncratic side effects, including hemeralopia (day blindness) • Because of many side effects, trimethadione and the related oxazolidinedionesparamethadione and dimethadione, the major metabolite of trimethadione, are now rarely used. |
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Topiramate, felbamate, and lamotrigine |
also used in the treatment of Lennox- Gastaut syndrome. |
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Phenobarbital and Vigabatrin |
should be used with caution because they may worsen atonic seizures. |
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Clobazam and rufinamide |
are also used in the treatment of seizures associated Lennox-Gastaut syndrome. |
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Clobazam |
•Its only approved use in the US is for treatment of seizures associated with LennoxGastaut syndrome in patients 2 years of age or older • MOA: A positive allosteric modulator of GABAA receptors and has similar pharmacologic activities and adverse effects. • Side effects that occur in a dose-dependent fashion include somnolence and sedation, dysarthria, drooling, and behavioral changes, including aggression. Withdrawal symptoms may occur with abrupt discontinuation. |
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Rufinamide |
• In the USA and Europe, is only approved for treatment of seizures associated with the Lennox-Gastaut syndrome.
• MOA: A blocker of voltage-gated sodium channels
• is effective against all seizure types but especially against atonic seizures. Some clinical data suggest it may be effective against focal seizures.
• The drug should be given with food. The most common adverse events are somnolence and vomiting. |
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Stiripentol |
An aromatic allylic alcohol that has activity in the treatment of Dravet’s syndrome. • is often used in conjunction with clobazam or valproate. • MOA: Enhances inhibitory neurotransmission by reducing synaptosomal uptake of GABA, and inhibiting GABA transaminase-mediated breakdown of GABA.• •The most frequent adverse effects are sedation/drowsiness, reduced appetite, slowing of mental function, ataxia, diplopia, nausea, and abdominal pain. • exhibits nonlinear pharmacokinetics, decreasing in clearance as the dose increases. |
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vigabatrin |
An analog of GABA effective in the treatment of focal seizures and in the treatment of infantile spasms • MOA: A specific, irreversible inhibitor of GABA-T, producing a sustained increase in the extracellular concentrations of GABA in the brain which leads to inhibition of synaptic GABAA receptor responses, but also prolongs the activation of extrasynaptic GABAA receptors that mediate tonic inhibition. • The most important adverse effect is irreversible retinal dysfunction. Patients may develop permanent bilateral concentric visual field constriction that is often asymptomatic but can be disabling. |
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Benzodiazepines |
Seven play roles in the treatment of seizures and epilepsy
• MOA: Act as a positive allosteric modulation of GABAA receptors.
• Diazepam, Lorazepam, Midazolam, Clonazepam, Nitrazepam, Clorazepate and Clobazam. |
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Valproate |
known human teratogen |
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Phenobarbital |
use during pregnancy is also associated with an elevated risk of major congenital malformation, most often cardiac defects. |
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Valproate, phenobarbital, topiramate |
should be avoided in women of childbearing potential, and if the drugs cannot be eliminated, they should be used at the lowest dose possible because the risk. |
