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48 Cards in this Set

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Anticonvulsant drugs prolong what state of the Na channel?
Inactivated state.
Loss of the inhibitory actions of what molecule lead to propagation of seizure activity?
GABA
These seizures have an inhibitory focus and limited spread that may have one particular function.
Partial Seizures
These seizures affect the thalamus, which initiates widespread generalization.
Secondary Generalized Seizure
This seizure originates in the thalamus.
Primary Generalized Seizure, Absence or Petimal Seizure
What channel found in the thalamus is involved in Ca++ influx?
T channel
Inhibited Na+ or Ca++ influx results in prolongation of what channel phase?
Reactivation phase
1.GABA effects are facilitated through what channel?
2.What is the result of this?
1.GABAa channel, GABA chloride complex.
2.hyperpolarization
What 2 classes of drugs bind allosterically to the GABAa channel?
Barbiturates and Benzodiazepines
Pharmacokinetics:
1.slow & variable absorption (PO)
2.Fosphenytoin is more water soluble (IV)
3.Dose dependent hepatic metabolism (P450)
4.Induces CYP3A4
5.90% bound to albumin in plasma
6.Half life=24 hrs
Phenytoin
Mechanism:
-Blocks voltage-sensitive sodium channels by prolonging their inactivation state
Phenytoin
Excessive alcohol consumption causes a decrease in what protein produced by the liver?
Albumin
Adverse Effects:
1.Dose dependent cerebellar effects=ataxia & nystagmus
2.Cognitive impairment (at high doses)
3.Gastric Irritation
4.Hirsutism=abnormal hair growth
5.Gingival hyperplasia
6.Peripheral neuropathy
7.Osteomalacia
8.Hypothrombinemia (liver effect) and hemorrhage
9.Teratogenic=birth defects
Phenytoin
Women low in what enzyme activity will get hepatic toxicity and teratogenic effects from phenytoin?
Epoxide Hydrolase
Clinical Uses:
1.Major motor seizures
2.Partial seizures
3.Cardiac dysrhythemias
4.Chronic pain states
Phenytoin
Mechanism:
1.Blocks reactivation of voltage-gated sodium channels in neuronal cell membranes
2.Blocks NE reuptake
Carbamazepine
Pharmacokinetics:
1.Hepatic meatbolism to an active epoxide
2.Induces CYP450 and it's OWN METABOLISM (1A2, 2C19, 3A)
3.Half Life=10-20 hours
Carbamazepine
Adverse Effects:
1.Cerebellar effects=nausea, dizziness, nystagmus & ataxia
2.Mild, transient neutropenia
3.Aplastic anemia (1/200,000) so monitor CBC
4.SIADH-Syndrome of inappropriate ADH secretion=retain too much water, causes low serum Na+
5.Paradoxical excitation=more in kids
6.Hepatitis=b/c of liver metabolism
Carbamazepine
Clinical Uses:
1.Cranial Nerve V (trigeminal) Neuralgia
2.Bipolar Disorder
3.(Z)Seizures-partial seizures, generalized tonic-clonic seizures
Carbamazepine
CBZ
Mechanism:
Inhibits reactivation of voltage-gated sodium channels
Lamotrigine (Lamictal)
Adverse Effects:
-May cause dizziness, nausea, blurred vision, ataxia, and rash including Steven-Johnson Syndrome=severe skin condition (can shed skin)
Lamotrigine (Lamcital)
Clinical Uses:
-Refractory Seizures
-Generalized Seizures
-Chronic Pain Syndromes
Lamotrigine (Lamcital)
Taking what 2 drugs together is NOT a good combination b/c one inhibits the metabolism of the other?
Valproate inhibits the metabolism of Lamotrigine.
Mechanism:
1.Inhibition of voltage gated sodium channels
2.Inhibits T-type calcium channels in thalamus
3.May increase GABA synthesis and decrease GABA degradation
Valproate
Pharmacokinetics:
1.
-Low MW branched fatty acid
-Not tolerated well in GI
2.
-1:1 molar stable coordination compound of sodium valproate and valproic acid
1.valproic acid (depakene)
2.divalroex sodium (depakote)
Adverse Effects:
1.Anorexia, nausea, vomiting and diarrhea
2.Sedation (relatively little)
3.Menstrual irregularities--ammenorhea or become irregular
4.Weight gain
5.Elevated Liver Transaminases--ACT/AST (mild and transient)
6.Risk of fatal hepatitis (1/50,000)=especially in kids when given with cyclosporine
7.Pancreatitis and thrombocytopenia
Valproate
Clincial Uses:
1.Generalized Seizures
2.Partial Seizures
3.Absence Seizures
4.Bipolar Disorder
5.Chronic Pain States
Valproate
Mechanism:
Inhibits T-type Ca channels and prolongs the inactivation state of voltage-gated Na+ channels
Zonisamide (Zonegram)
Pharmocokinetics:
1.NOT metabolized in the liver
2.83% excreted by the KIDNEYs unchanged or as glucuronide
3.Half Life=63 hours
Zonisamide
Mechanism:
GABA analog (It may act on alpha2delta subunit of Ca channels)
Gabapentin (Neurontin)
Pharmacokinetics:
-excreted unchanged in urine
(NOT metabolized in liver)
-Half life=5-9 hours
Gabapentin
Adverse Effects:
1.Transient drowsiness (usually goes away)
2.Dizziness,ataxia, and fatigue
Gabapentin
Aunt Gab likes to put you to sleep.
Clinical Uses:
1.Partial Seizures
2.Chronic Pain
3.Bipolar
Gabapentin
Mechanism:
Blocks voltage-gated Ca++ channels (like Gabapentin)
Pregabalin (Lyrica)
Pharmocokinetics:
1.Structural analog of GABA
2.90% excreted unchanged by kidneys
Pregabalin (Lyrica)
Adverse Effects:
Weight gain, fluid retention, drowsiness, & cognitive f(x) including hallucinations
Pregabalin (Lyrica)
Clinical Uses:
-Approved for neuropathic pain associated with diabetic neuropathy and postherpetic neuralgia
-Adjunctive treatment for partial seizures in adults
Pregabalin (Lyrica)
Multiple mechanisms:
1.Decreases glutamate receptor activity
2.Potentiates GABA response
3.Blocks voltage gated sodium channels
Topiramate (Topamax)
Clinical Uses:
Broad Spectrum-
1.Used for multiple types of seizures
2.Migraines
3.Chronic Pain
4.Bipolar Disorder
Topiramate (Topamax)
Mechanism:
Facilitation of effects of GABA (through an allosteric interaction)
Phenobarbital
Pharmacokinetics:
1.Elimination 75% hepatic (P450)
2.Half life=100 hours
Phenobarbital
Adverse Effects:
1.SEDATION
2.Impaired cognitive function (so bad for kids)
Phenobarbital
Clinical Uses:
Second line drug for partial and generalized seizures
Phenobarbital
Mechanism:
Facilitation of effects of GABA through Phenobarbital metabolite
Primidone
What are the anti-seizure drugs with NO interactions with hepatic microsomal enzymes?
1.Ethosuximide
2.Gabapentin
3.Pregabalin
Eric Sucks GABA
What are the anti-seizure drugs that INDUCE CYP450 Enzymes?
1.Carbamazepine
2.Phenobarbital
3.Phenytoin
4.Primidone
Pheny's primitive car with phenol.
Mechanism:
Inhibits T-type Ca channels in thalamic neurons
Ethosuximide
Clinical Use:
Absence seizures in children
Ethosuximide