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Antiepiletics Test 1 Flashcards

1
Q

Collective term used to designate a group of chronic CNS disorders characterized by the onset of sudden disturbances of sensory, motor, autonomic, or psychic origin.

A

EPILEPSY

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2
Q

Epilepsy generally transient with the exception of _____ ________.

A

status epilepticus

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3
Q

Protein binding greatly varies: _______0% to ______> 90%

A

gabapentin, phenytoin

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4
Q

GI absorption is _____ over hours and may be incomplete (ESPECIALLY gabapentin)

A

slow

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5
Q

Medications relying on renal excretion and may need adjusting according to renal function: (5)

Remaining drugs should be dosed according to patient’s liver dysfunction

A 
Gabapentin
Pregabalin
Levetitracetam
Vigabatrin
Zonisamide
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6
Q

Drug clearance and Elimination half-time range from:
Hours: (4 drugs)
TO
Days: (4 drugs)

A

carbamazepine, valproate, primidone, gabapentin

to
phenytoin, lamotrigine, phenobarbital, zonisamide

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7
Q

Because of their ability to induce or inhibit drug metabolism ALL antiepileptic drugs may be associated with drug interactions resulting interactions of plasma drug concentrations EXCEPT

A

Gabapentin
Levetiracetam
vigabatrin

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8
Q

Examples of highly bound protein drugs:

A

Phenytoin
Valproate
Carbamazepine

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9
Q

________ is principle binding protein for antiepileptic drugs

A

Albumin

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10
Q

Medication ineffectiveness is failure to achieve sufficient ___________.

A

high plasma concentrations

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11
Q

Noncompliance is high in _______ and _______.

A

elderly and adolescents

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12
Q

Dosing at ½ the drug’s elimination half-time ensures :

A

that a single dose missed will not result in sub-therapeutic plasma concentrations

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13
Q

Carbamazepine dosing

A

10-40 mg/kg/day in 2-3 doses

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14
Q

Gabapentin dosing

A

10-60mg/kg/day

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15
Q

Phenobarbital dosing

A

2-5mg/kg/day could divide x2 a day

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16
Q

Phenytoin dosing

A

3-7mg/kg/day divided x3

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17
Q

Toprimate dosing

A

500-3000mg/day in 2-4 doses.

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18
Q

Valproate dosing

A

500-3000mg/day in 2-4 doses.

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19
Q

_______ is the ONLY agent requiring routine monitoring

A

Phenytoin

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20
Q

_______ seizure activity has a localized or focal origin in most patients.

A

Epileptic

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21
Q

________ and ________ firing in a seizure focus is usually unknown.

A

High frequency and synchronous

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22
Q

Factors that my facilitate the spread of a seizure focus into areas of the normal brain:

A 
Blood glucose concentrations
PaO2
PaCO2
pH
Endocrine function
Stress
fatigue
Electrolyte balance
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23
Q

Neurons of chronic seizure focus exhibit a type of _______ ______ with regard to excitatory stimuli

A

denervation hypersensitivity

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24
Q

If the spread of a seizure focus is extensive enough the entire brain is activated and a ______ ______seizure with unconsciousness ensues

A

tonic-clonic

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25
Once a seizure is initiated it is likely to be maintained by reentry of _____ _____ in a _____ ____ _____ that my not even include the original seizure focus.
excitatory impulses, closed feedback pathway
26
Controls muscle movements, thinking, and judgment.
Frontal lobe- 
27
Controls sense of touch, response to pain and temperature, and understanding of language.
Parietal lobe- 
28
Controls vision.
Occipital lobe- 
29
Controls hearing and memory
Temporal lobe- 
30
Controls balance.
Cerebellum
31
Controls breathing and regulates heartbeat.
Brain stem- 
32
Drugs that delay reactivation of sodium channels during high frequency neuronal firing produce an inhibitory effect on creation of action potentials until neuronal discharge is blocked:
``` Phenytoin Carbamazepine Primidone Valproate lamotrigine ```
33
Some drugs act at both sodium and calcium ion channels:
Phenytoin Carbamazepine Valproate Lamotrigine
34
Other drugs act selectively on calcium ion channels:
Ethosuximide: Selectively blocks the T-type calcium ion current which is thought to act as a pacemaker for the thalamic neurons and may be important in absence seizures Phenobarbital
35
Those drugs that alter synaptic function act primarily by enhancing GABA mediated neuronal inhibition:
Phenobarbital: And other Barbiturates increase the duration of ion channel openings Benzodiazepines: increase frequency of GABA-mediated ion channel openings.
36
______ delays the reuptake of GABA from synaptic clefts, effectively enhancing GABA-mediated neuronal inhibition after synaptic release of the neurotransmitter.
Tiagabine
37
MOA and targeted seizures of Cabamazepine
Sodium channel blockade, Partial seizures
38
MOA and targeted seizures of Gabapentin
Unknown (decrease gaba release), Partial and generalized seizures
39
MOA and targeted seizures of Phenobarbital
Chloride ion channels, Partial and generalized seizures
40
MOA and targeted seizures of Phenytoin
Sodium ion channels blockade, Calcium ion channel, NMDA receptors. Partial and generalized seizures
41
MOA and targeted seizures of Toprimate
Sodium ion channels blockade, enhanced GABA activity, Glutamate antagonism, Calcium ion channel blocker Partial and generalized seizures
42
MOA and targeted seizures of Valproate
Sodium ion channels blockade, Calcium ion channel | Partial and generalized seizures
43
Recent benzo derivative. Unique because it does not cause significant sedation and can be used long-term d/t tolerance is relatively uncommon
Clobazam
44
reserved for selected patients with uncontrolled seizures d/t its side effects
Felbamate
45
patients develop a tolerance and sedation is a common side effects
Clonazepam
46
Drugs used for partial seizures and has acceptable side effect profiles
``` Carbamazepine Lamotrigine Oxcarbazepine Topiramate Zonisamide phenytoin ```
47
Drugs useful for treatment of generalized seizures:
Valproate Lamotrigine Topiramate
48
Drugs effective in treatment of generalized nonconvulsive seizures and especially absence seizures
Ethosuximide Lamotrigine valproate
49
Gabapentin MOA
Is an analog of GABA that increases synaptic GABA
50
Gabapentin therapeutic dose
2- 20 mcg/mL
51
Gabapentin elimination
Zero protein bound. Renal elimination
52
Antiepileptic drugs can render PO birth control _____ effective
less
53
Seizures during pregnancy = _______ morbidity and mortality for mother and fetus
increased
54
for maternal epilepsy Goal:
Monotherapy with lowest dose to stop seizures
55
Significant teratogenicity can happen if meds give in first____weeks
8
56
________ and _______x2 risk of Neural tube defects such as spina bifida in preg women
Valproate and carbamazepine
57
seizure medication for preg women
Lamotrigine
58
Seizure medication for preg woman that can be added especially during labor.
Clobazam
59
Used for patients with nonconvulsive and convulsive partial seizures. Useful in: Trigeminal neuralgia Glossopharyngeal neuralgia
CARBAMAZEPINE
60
CARBAMAZEPINE _____ protein bound
70-80%
61
CARBAMAZEPINE rapid absorption peak plasma concentrations in ____hours
2-6
62
CARBAMAZEPINE Plasma elimination half time is ____hours
8-24
63
CARBAMAZEPINE usual side effects
sedation, vertigo, diplopia, n/v and chronic diarrhea in some patients.
64
Carbamazepine Rare side effects but can be life threatening:
``` SIADH Aplastic anemia Thrombocytopenia Hepatocellular and cholestatic jaundice Oliguria HPTN Cardiac dysrhythmias WBC suppression ```
65
Carbamazepine High plasma concentration can have a arginine vasopressin hormone like actions resulting in _________.
hyponatremia
66
Carbamazepine Accelerates metabolism of:
``` Valproic acid Ehtosuximide Corticosteroids Anticoagulants Antipsychotics ```
67
Carbamazepine Drugs that inhibit metabolism of carbamazepine sufficiently to cause toxic effects:
``` Cimetidine Propoxyphene Diltiazem Verapamil Isoniazid erythromycin ```
68
Felbamate Pharmacokinetics:
Rapid PO absorption Prolonged elimination half time Excreted unchanged by kidneys
69
Felbamet side effects
Hepatotoxicity Monitor CPC, Liver Functions indicated Metabolized by liver cytochrome P 450 so effected by concurrent meds metabolized by cytochrome P 450 Concomitant administration of carbamazepine or phenytoin may decrease plasma concentrations of Felbamate Since Felbamate is a potent inhibitor of P 450 enzymes, it can slow metabolism of phenytoin, phenobarbital and Valproic acid If receiving Felbamate, carbamazepine, phenytoin, and Valproic, dose should be decreased by 20-30% to prevent toxicity
70
PHENOBARBITAL _____ acting
long
71
PHENOBARBITAL Effective against ALL seizure types EXCEPT _______________.
nonconvulsive primary generalized seizures
72
PHENOBARBITAL Second-line drug treatment due to its side effects:
Cognitive | Behavioral
73
PHENOBARBITAL peak concentration
12-18 hours
74
Phenobarbital Plasma protein binding is
48% to 54%
75
Phenobarbital Principle metabolite is an _______ parahydroxyphenyl derivative excreted in urine as a sulfate conjugate.
inactive
76
Phenobarbital Plasma concentration of ________ are usually necessary for seizure control
10-40 mcg/ml
77
Phenobarbital side effects
Sedation, irritability, hyperactivity most troublesome side effects Tolerance to sedation with chronic therapy Depression in adults, and confusion in elderly Megaloblastic anemia that responds to folic acid Osteomalacia that responds to vitamin D Nystagmus and ataxia with concentrations > 40 mcg/ml Abnormal collagen deposition causing Dupuytren (du-pew-TRNAZ) contracture may occur (mainly ring and pinky) Classic example of a hepatic microsomal enzyme inducer that can accelerate the metabolism of many lipid soluble drugs.
78
Prototype of hydantoins
PHENYTOIN
79
Phenytoin can be given acutely to achieve effective plasma concentrations within _____________
20 minutes
80
Phenytoin Initial adult dose is________. Dose >______rarely tolerated
3-4 mg/kg. Does >500 mg
81
Phenytoin IV should not exceed ________in adults | Should not exceed____________ (or 50 mg/min) whichever is slower in pediatrics
50 mg/min ,1-3 mg/kg
82
Phenytoin____% to albumin
90
83
_________ and ______are likely with concentrations of >20 mcg/ml (Phenytoin)
Nystagmus and ataxia
84
(Phenytoin) For control of digitalis-induced cardiac dysrhythmias _________ IV is given every 15-30 minutes until a satisfactory response or a max dose of 15 mg/kg is given
0.5-1.0 mg/kg
85
Phenytoin side effects
CNS toxicity manifesting as: (> 20 mcg/ml) Nystagmus Ataxia Diplopia Vertigo (cerebellar-vestibular dysfunction Peripheral neuropathy in 30% of pts Gingival hyperplasia in 20% pts and is probably the most common manifestation
86
Valproic Acid is Effective in the treatment of ___________ epilepsies and __________.
all primary generalized and all convulsive epilepsies
87
Valproic Acid Peak plasma concentrations in _____ hours
1-4
88
Valproic Acid Plasma protein binding is ____
> 80%
89
Valproic Acid Elimination half time is ____ hours
7-17
90
Valproic Acid side effects
Anorexia n/v Weight gain is common Fine distal tremor with higher doses Thrombocytopenia seen frequently at higher doses Most serious side effect is hepatotoxicity occurring in ~ 0.2% of children under 2 years old who are treated chronically. This is potential fatal. Hepatic necrosis decreases dramatically after 2 years of age 20% treated pts have hyperammonemia without hepatic damage Sedation and ataxia are INFREQUENT side effects. Partly eliminated as a ketone containing metabolite, may have false positive results Can displace phenytoin and diazepam from protein binding sites resulting in increased pharmacologic effects produced by displaced drug Enzyme inhibitor and may slow metabolism of phenytoin Causes plasma concentration of phenobarbital to increase ~ 50% DOES NOT INTERFERE with action of oral contraceptives

Pharm 2 (13 decks)

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