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Pharm 2 > Antiepiletics Test 1 > Flashcards

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
Q

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.

A

excitatory impulses, closed feedback pathway

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26
Q

Controls muscle movements, thinking, and judgment.

A

Frontal lobe-

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27
Q

Controls sense of touch, response to pain and temperature, and understanding of language.

A

Parietal lobe-

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28
Q

Controls vision.

A

Occipital lobe-

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29
Q

Controls hearing and memory

A

Temporal lobe-

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30
Q

Controls balance.

A

Cerebellum

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31
Q

Controls breathing and regulates heartbeat.

A

Brain stem-

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32
Q

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:

A 
Phenytoin
Carbamazepine
Primidone
Valproate
lamotrigine
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33
Q

Some drugs act at both sodium and calcium ion channels:

A

Phenytoin
Carbamazepine
Valproate
Lamotrigine

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34
Q

Other drugs act selectively on calcium ion channels:

A

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

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35
Q

Those drugs that alter synaptic function act primarily by enhancing GABA mediated neuronal inhibition:

A

Phenobarbital: And other Barbiturates increase the duration of ion channel openings
Benzodiazepines: increase frequency of GABA-mediated ion channel openings.

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36
Q

______ delays the reuptake of GABA from synaptic clefts, effectively enhancing GABA-mediated neuronal inhibition after synaptic release of the neurotransmitter.

A

Tiagabine

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37
Q

MOA and targeted seizures of Cabamazepine

A

Sodium channel blockade, Partial seizures

38
Q

MOA and targeted seizures of Gabapentin

A

Unknown (decrease gaba release), Partial and generalized seizures

39
Q

MOA and targeted seizures of Phenobarbital

A

Chloride ion channels, Partial and generalized seizures

40
Q

MOA and targeted seizures of Phenytoin

A

Sodium ion channels blockade, Calcium ion channel, NMDA receptors.
Partial and generalized seizures

41
Q

MOA and targeted seizures of Toprimate

A

Sodium ion channels blockade, enhanced GABA activity, Glutamate antagonism, Calcium ion channel blocker
Partial and generalized seizures

42
Q

MOA and targeted seizures of Valproate

A

Sodium ion channels blockade, Calcium ion channel

Partial and generalized seizures

43
Q

Recent benzo derivative. Unique because it does not cause significant sedation and can be used long-term d/t tolerance is relatively uncommon

A

Clobazam

44
Q

reserved for selected patients with uncontrolled seizures d/t its side effects

A

Felbamate

45
Q

patients develop a tolerance and sedation is a common side effects

A

Clonazepam

46
Q

Drugs used for partial seizures and has acceptable side effect profiles

A 
Carbamazepine
Lamotrigine
Oxcarbazepine
Topiramate
Zonisamide
phenytoin
47
Q

Drugs useful for treatment of generalized seizures:

A

Valproate
Lamotrigine
Topiramate

48
Q

Drugs effective in treatment of generalized nonconvulsive seizures and especially absence seizures

A

Ethosuximide
Lamotrigine
valproate

49
Q

Gabapentin MOA

A

Is an analog of GABA that increases synaptic GABA

50
Q

Gabapentin therapeutic dose

A

2- 20 mcg/mL

51
Q

Gabapentin elimination

A

Zero protein bound. Renal elimination

52
Q

Antiepileptic drugs can render PO birth control _____ effective

A

less

53
Q

Seizures during pregnancy = _______ morbidity and mortality for mother and fetus

A

increased

54
Q

for maternal epilepsy Goal:

A

Monotherapy with lowest dose to stop seizures

55
Q

Significant teratogenicity can happen if meds give in first____weeks

A

8

56
Q

________ and _______x2 risk of Neural tube defects such as spina bifida in preg women

A

Valproate and carbamazepine

57
Q

seizure medication for preg women

A

Lamotrigine

58
Q

Seizure medication for preg woman that can be added especially during labor.

A

Clobazam

59
Q

Used for patients with nonconvulsive and convulsive partial seizures. Useful in:
Trigeminal neuralgia
Glossopharyngeal neuralgia

A

CARBAMAZEPINE

60
Q

CARBAMAZEPINE _____ protein bound

A

70-80%

61
Q

CARBAMAZEPINE rapid absorption peak plasma concentrations in ____hours

A

2-6

62
Q

CARBAMAZEPINE Plasma elimination half time is ____hours

A

8-24

63
Q

CARBAMAZEPINE usual side effects

A

sedation, vertigo, diplopia, n/v and chronic diarrhea in some patients.

64
Q

Carbamazepine Rare side effects but can be life threatening:

A 
SIADH
Aplastic anemia
Thrombocytopenia
Hepatocellular and cholestatic jaundice
Oliguria
HPTN
Cardiac dysrhythmias
WBC suppression
65
Q

Carbamazepine High plasma concentration can have a arginine vasopressin hormone like actions resulting in _________.

A

hyponatremia

66
Q

Carbamazepine Accelerates metabolism of:

A 
Valproic acid
Ehtosuximide
Corticosteroids
Anticoagulants
Antipsychotics
67
Q

Carbamazepine Drugs that inhibit metabolism of carbamazepine sufficiently to cause toxic effects:

A 
Cimetidine
Propoxyphene
Diltiazem
Verapamil
Isoniazid
erythromycin
68
Q

Felbamate Pharmacokinetics:

A

Rapid PO absorption
Prolonged elimination half time
Excreted unchanged by kidneys

69
Q

Felbamet side effects

A

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
Q

PHENOBARBITAL _____ acting

A

long

71
Q

PHENOBARBITAL Effective against ALL seizure types EXCEPT _______________.

A

nonconvulsive primary generalized seizures

72
Q

PHENOBARBITAL Second-line drug treatment due to its side effects:

A

Cognitive

Behavioral

73
Q

PHENOBARBITAL peak concentration

A

12-18 hours

74
Q

Phenobarbital Plasma protein binding is

A

48% to 54%

75
Q

Phenobarbital Principle metabolite is an _______ parahydroxyphenyl derivative excreted in urine as a sulfate conjugate.

A

inactive

76
Q

Phenobarbital Plasma concentration of ________ are usually necessary for seizure control

A

10-40 mcg/ml

77
Q

Phenobarbital side effects

A

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
Q

Prototype of hydantoins

A

PHENYTOIN

79
Q

Phenytoin can be given acutely to achieve effective plasma concentrations within _____________

A

20 minutes

80
Q

Phenytoin Initial adult dose is________. Dose >______rarely tolerated

A

3-4 mg/kg. Does >500 mg

81
Q

Phenytoin IV should not exceed ________in adults

Should not exceed____________ (or 50 mg/min) whichever is slower in pediatrics

A

50 mg/min ,1-3 mg/kg

82
Q

Phenytoin____% to albumin

A

90

83
Q

_________ and ______are likely with concentrations of >20 mcg/ml (Phenytoin)

A

Nystagmus and ataxia

84
Q

(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

A

0.5-1.0 mg/kg

85
Q

Phenytoin side effects

A

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
Q

Valproic Acid is Effective in the treatment of ___________ epilepsies and __________.

A

all primary generalized and all convulsive epilepsies

87
Q

Valproic Acid Peak plasma concentrations in _____ hours

A

1-4

88
Q

Valproic Acid Plasma protein binding is ____

A

> 80%

89
Q

Valproic Acid Elimination half time is ____ hours

A

7-17

90
Q

Valproic Acid side effects

A

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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