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Therapeutics Spring 2016 > Seizure Drugs > Flashcards

Seizure Drugs Flashcards

1
Q

What is the dosing schedule for Lamotrigine?

A 
No Concomitant therapy:
25mg QD for 14 days
50mg QD for 14 days
100mg QD for 7 days then 200mg QD
Concomitant Inducer(carbamazepine, phenytoin):
50mg daily for 14 days
100mg daily for 14 days
200mg daily for 7 days
400mg daily
With UGT inhibiter (Valproate)
25mg every other day for 14 days
25mg daily for 14 days
50mg daily for 7 days
100mg once daily
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2
Q

What are the adverse effects of Lamotragine?

A

Serious rash (Steven Johnsons syndrome BLACK BOX, toxic epidermal necrolysis), blurred double vision,

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3
Q

What is the pregnancy category for Lamotragine and how does it impact oral contraception?

A

Category C, OC’s may decrease serum concentrations of OC’s and vise versa

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4
Q

What is the initial dosing for Levetiracetam (Keppra) for non SE patients

A

IR or/IV: 500mg BID x 14 days, increase by 1000 mg every 14 days. MAX: 3000mg/day
XR: 1000 mg daily, increase by 1000mg every 14 days

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5
Q

How is Keppra dosed for decreased renal function?

A

CrCl 30-50mL/min: 250-750 mg PO BID

CrCl

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6
Q

How is Keppra dosed for SE?

A

1000 - 3000mg IV or 2-5mg/kg/min IV

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7
Q

What are the adverse effects of Keppra?

A

Behavioral abnormalities: psychosis, suicidal thoughts or behaviors, unusual mood changes or worsening depression, somnolence, asthenia, dizziness, fatigue, aggression, irritability, decreased appetite, SJS/TEN, leukopenia
PREG CATEGORY C

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8
Q

What is the initial dosing for Valproate (Depakote, depakene, Depacon)?

A

IV and all dosage forms except ER: 10-15mg/kg/day in divided doses, increase weekly by 5-10mg/kg/day
Usual initial dose: 250mg BID or 500mg QD

ER: 10-15 mg/kg/day (once a day dosing) increasing weekly by 5-10mg/kg/day. Usual initial dose: 500mg daily.

MAX: 60mg/kg/day

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9
Q

What is the target serum concentration for Valproate?

A

50-125 mcg/ml

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10
Q

What is the dose for Valproate for SE?

A

Initial: 20-40mg/kg IV, may give additional 20mg/kg; may use alternative dosing of 3-6mg/kg/min, may give additional dose 10 minutes after loading dose. IV is dosed Q 6 hours after load; IV to PO conversion is 1:1.

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11
Q

What are the warnings associated with Valproate?

A

Contraindicated in severe hepatic dysfunction
BOX WARNING: hepatic failure/pancreatitis
Warnings: CNS depression, HYPERAMMONEMIA, thrombocytopenia, increased risk of suicidal thoughts/behaviors
Adverse Effects: tremor, somnolence, nausea/vomiting, weight gain, alopecia, PCOS
Preg Category D (X for migraines)
Use with caution in traumatic head injury; preferred for glioblastoma multiforme,: CBC with platelets, LFTs, serum concentration

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12
Q

What is the dosing for Zonisamide (Zonegran)**

A

100mg once daily, increase by 100mg/day every 14 days.

Max: 3000mg/day

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13
Q

Zonisamide is contraindicated in what conditions?

A

Sulfa hypersensitivity; caution in hepatic disease

Warnings: Metabolic acidosis, renal caliculi, sulfonamide reactions

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14
Q

What are the adverse effects of Zonisamide (Zonegran)? **

A

Drowsiness, dizziness, confusion, tremor, nausea/vomiting, weight loss, paresthesias

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15
Q

How is Zonisamide metabolized and what percent is renally cleared?

A

Metablolized via glucuronidation (UDP-GT)

35% renally cleared

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16
Q

What are the monitoring paramaters for Zonisamide?

A

CBC, LFT’s, SCr, FDA evaluating risk of DRESS syndrome for possible inclusion in prescribing information

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17
Q

What is the dose for Clobazam (Onfi)C-IV? **

A

5mg BID daily, increase to 10mg BID daily at wk 1, increase to 20mg once daily at week 2.
Max: 40mg/day

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18
Q

What warnings and Adverse Effects are associated with Clobazam (Onfi)?

A

Somnolence/sedation, withdrawal symptoms, SJS, TEN, drug dependence, suicidal thoughts/behaviors
Adverse Effects: constipation, somnolence, sedation, increased body temperature, lethargy, drooling

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19
Q

True or False: Clobazam may decrease the effectiveness of oral contraceptives.

A

True

Pregnancy Category C

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20
Q

What is the dose for Clonazepam (Klonopin)?**

A

1.5mg/day in 3 divided doses, increase by 0.5-1mg every 3 days. Max of 20mg/day

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21
Q

What conditions are contraindicated for the use of Clonazepam? What warnings are associated with this med?

A

Severe hepatic Disease

CNS depression, respiratory depression, anterograde amnesia, paradoxical reactions, withdrawal symptoms

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22
Q

What Adverse Effects are associated with Clonazepam?

A

Ataxia, confusion, drowsiness, slurred speech

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23
Q

What are P450 interactions of Clonazepam, Preg category and monitoring parameters?

A

P4503A4 substrate Major
Preg Category D
Monitoring Parameters: CBC and LFTs

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24
Q

What is the dosing for Carbamazepine ***(Tegretol, Tegretol XR, Carbatrol, Epitol)

A

IR or ER
200mg BID, increase by 200mg/day once weekly
Suspension: 100mg (5mL) four times daily, increase by 200mg/day once weekly
Max: 1600mg/day
Monitor serum concentrations: 4-12mcg/ml (>12 = toxicity)
Usually just for kids, a lot of dosing challenges with this.

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25
Q

What are the contraindications of Carbamazepine?

A

Concurrent use with TCA, carbamazepine sensitivity

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26
Q

What are the boxed warnings of Carbamazepine?

A

SJS/TEN (most likely in patients of Asian descent who are + for HLA-B1502; Drug reactionwith Eosinophilia and Systemic Symptoms (DRESS) hypersensitivity reaction if positive for HLA-A3101 (Northern European descent); aplastic anemia, agranulocytosis

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27
Q

What are the Adverse effects of Carbamazepine?

A

drowsiness, dizziness, HA, fatigue, nausea/vomiting Vitamin D/ Calcium deficiency, double vision, sedation, leukopenia, syndrome of inappropriate antidiuretic hormone (SIADH), hyponatremia

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28
Q

What is the P450 influence and Pregnancy category for Carbamazepine?

A

P450 3A4 Substrate major, P450 2C8 minor

Preg Category D

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29
Q

What is the UGT substrate influence of Carbamazepine?

A

UGT strong inducer: 1A3, 2B6, 2C8, 2C9, 2C19, 3A4

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30
Q

What are the monitoring parameters for Carbamazepine?

A

LFTs, CBC with platelets, electrolytes, BUN/SCr

May autoinduce own metabolism for several weeks after initiation and dose increase.

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31
Q

Eslicarbazepine Acetate (Aptiom) dosing?**

A

400mg once daily for 1 week, increase to 800 mg once daily.
MAX: 1200mg once daily (after a min of 800mg once daily)
Moderate to severe renal impairment: 600mg once daily

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32
Q

What warning is associated with Eslicarbazepine Acetate>

A 
Dermatologic reaction (SJS/TEN), hyponatremia,
Same Box warning as Carbamazepine
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33
Q

What active metabolite comes from Eslicarbazepine and what is it’s impact on P450?

A

Eslicarbazepine, active metabolite of oxcarbzepine P450 2C19 inhibitor Moderate
Same HLA effects as Carbamazepine
MONITOR electrolytes!!

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34
Q

What is the dose of Exobagine (Potiga) C-V?

Include renal dosing and max dosing.

A

100mg three imes daily, increase by up to 50mg TID once a wk.
Max: 1200mg
Renal Dosing: CrCl

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35
Q

What is the Box warning and other warnings for Exobagine?

A

Boxed: Retinal abnormalities - may progress to vision loss
Warnings: urinary retention, grey-blue/brown skin discoloration (sign of toxicity) QTc prolongation, memory impairment, hallucinations, double vision

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36
Q

What are the important monitoring parameters for Ezobagine (Potiga)?

A

Baseline ophthalmic exam, repeat every 6 months

Extensive metabolism via UGT

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37
Q

Felmbamate (Felbatol) dosing?

A

1200mg/day in 3 to 4 didvided doses, increase every 2 wks by 600mg/day. Max: 3600mg/day
RENAL: CrCl

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38
Q

What is the Box warning for Felbamate?

A

Aplastic Anemia, hepatic failure

39
Q

What are Important monitoring parameters for Felbamate?

A

LFTs at baselihne and frequently thereafter; discontinue if evidence of bone marrow suppression. Monitor CBC with differential/platelets, LFTs at least every 3 months

40
Q

Gabapentin Dosing? Renal adjustment?

A

300mg TID, increase every 1-3 days by 300-800mg/day
Max: 3600mg/day
Renal: CrCl 30-60ml/min: 600 - 1800mg/day
Not rec for CrCl

41
Q

Gabapentin adverse effects?

A

Somnolence, Peripheral edema,

100% renal clearance, monitor baseline then routinely!

42
Q

What unique dosage form does Gabapentin come in?

A

Compounding powder for oral suspension: 2500mg/420ml

43
Q

What is Lacosamide (Vimpar) dosing?

A

Comes in IR and Oral solt.
50mg BID daily, increase by 100mg/day each week.
Max: 400mg/day

44
Q

What is Lacosamide dosing for SE?

A

200-400mg IV, infuse 200mg IV over 5 minutes

45
Q

What warnings are associated with Lacosamide?

A

Caution in patients with cardiac conduction abnormalities, prolongs PR interval, Dermatological reactions, visual disturbances

46
Q

What major adverse effects are associated with Lacosamide?

A

Idiosyncratic reactions: hepatic impairment, 1st degree AV block

47
Q

What is the P450 reaction of Lacosamide?

A

p450 2C19 substrate and inhibitor: MAJOR

48
Q

What is the dose conversion of Oxcarbazepine when switching from Carbamazepine?

A

Oxcarbazepine is 1.5X the dose of carbamazepine

49
Q

What are the major Warnings associated with Oxcarbazepine?

A

Derm reactions (HLA-B1502 and HLA - A3101 - SJS/TEN/DRESS), hyponatremia (

50
Q

What P450 interaction does Oxcarbazepine have?

A

Major/Strong P450 3A4/5 substrate/inducer
P450 2C19 inhibitor: Moderate
MONITOR ELECTROLYTES

51
Q

What is the major boxed warning for Perampanel (Fycompa) C-III

A

Dose related serious and /or life threatening neuropsychiatric events!!
NOT for psych patients!!

52
Q

What are adverse affects of Perampanel?

A

gait disturbances and somnolence

53
Q

What is the SE dose for Phenobarbital?

A

Loading dose: 15-18 mg/kg IV (ventilated)

10mg/kg IV (non-ventilated) Increased by 5mg/kg IV infused over 30-60minutes

54
Q

What is the SE max dose and goal serum concentration for phenobarbital?

A

25-30mg/kg IV (SE), 50-100mg/min IV

Serum concentration: 15-40mcg/ml

55
Q

What are the adverse effects of Phenobarbital?

A

Somnolence, confusion, cognitive impairment, impaired calcium metabolism

56
Q

What is the pregnancy category and P450 metabolism of phenobarb?

A

Category D
P450 2C9 substrate major
P450 1A2,2C,3A and UGT inducer: strong

57
Q

What is phenytoin dose for SE?

A

15-20mg/kg IV, may give additional 5-10mg/kg
Max 50mg/minute loading dose
May give additional dose 10mins after load.

58
Q

What is loading dose of Fosphenytoin for SE?

A

20mg phenytoin equivalent/kg IV or IM
May give an additional 5mg/kg; may give an additional dose 10mins after load.
Max: 150mg PE/minute loading dose

59
Q

What is the goal for serum concentrations of phenytoin?

A

10-20 mcg/ml

Fosphenytoin to phenytoin conversion occurs in 0.5-1 hour post dose.

60
Q

What are the adverse effects of fosphenytoin (IV)?

A

hypotension, arrhythmias

61
Q

What are the adverse effects of phenytoin (IV)?

A

Arrythmias, hypotension, purple glove syndrome (local reaction)

62
Q

What are the contraindications of phenytoin?

A

sinus bradycardia or 2cnd/3rd degree heart block

63
Q

What is the pregnancy category and P450 metabolizer?

A

Preg category D, P450 2C9/2C19 substrate: major

P450 1A2, 2C19, 3A4 and UGT inducer strong

64
Q

What are the monitoring parameters for Phenytoin?

A

Serum concentration and serum albumin

65
Q

What are the phenytoin warnings?

A

Decreased bone mineral density, dermatological reactions, blood dyscarias

66
Q

What are the Adverse effects of Phenytoin?

A

Nystagmus, ataxia, double vision, hepatotoxicity, hisuitism, gingival hyperplasia, cardiac arrhythmias, SJS, alteration of vitamin D metabolism, osteoporosis

67
Q

What is the renal dosing for Pregabalin (Lyrica)

A

Renal Dosing: CrCl 30-60mL/min: 300mg
CrCl 15-30 mL/min: 150mg
CrCl

68
Q

What are the warnings with Pregabalin?

A

Angioedema and Peripheral edema

69
Q

Primidone (mysoline) is metabolized to what drug?

A

Phenobarbital

70
Q

What pregnancy category is Primidone?

A

D

71
Q

What unique seizure disorder is Rufinamide (Banzel) indicated for?

A

Lennox-Gastaut/ Refactory seizures

72
Q

What are the contraindications and warnings of Rufinamide?

A

Familial short QT syndrome

Warning: Multiorgan sensitivity reactions (DRESS), SJS, TEN

73
Q

Tiagabine (Gabitril) dosing needs to be adjusted when taken with certain drugs. How is it dosed for enzyme inducing drugs?
Valproate therapy?

A

Concomitant enzyme inducing drugs: 4mg once daily, increase by 4-8mg/day once weekly
Concomitant valproate therapy: 4mg every other day increase by 4-8mg / day every 2 wks.

74
Q

What are the goal serum concentrations for Tiagabine?

A

0.02 -0.2mcg/mL

75
Q

What patients should Tiagabine be used in caution with?

A

For patients without seizure disorder and with hepatic disease, may trigger seizures.

76
Q

What is a major Adverse effect of Tiagabine?

A

Cognitive impairement

77
Q

What is the P450 impact of Tiagabine?

A

P450 3A4 substrate: major

78
Q

What is the dose for Topiramate (Topamax)?

A

25-50mg/day, increase by 25-50mg/day once weekly

79
Q

What is the renal dosing for Topiramate?

A

CrCl

80
Q

What is the dosing for SE for Topiramate?

A

200-400mg per nasogastric tube or PO: 300 - 1600mg/day orally in 2-4 divided doses

81
Q

What patients do you use Topiramate with caution in?

A

nephrolithiasis, renal impairment, hepatic disease

82
Q

What are the warnings for Topiramate?

A

CNS depression, metabolic acidosis, oligohydrosis/hyperthermia, acute mhopia, secondary angle-closure glaucoma, nephrolithiasis, visual field defects, cognitive impairment, hyperchloremic non anion,gap metabolic acidosis

83
Q

What is the preg category and metabolism of P450 enzymes?

A

Category D
P450 2C19 inhibitor moderate
P450 3A4 substrate/inducer; moderate-strong (dose dependant)

84
Q

What are monitoring parameters for Topiramate?

A

Basic metabolic profile, urinalysis every 3-6 months

85
Q

What type of seizures is Vigabatrin (Sabril) used for and what is the dose?

A

Refactory seizures:

500mg BID, increase by 500mg daily

86
Q

What is the renal dosing for Vigabatrin?

A

CrCl 50 - 80ml/min: reduce dose by 25%
CrCl 30 -50: reduce by 50%
CrCl 10 - 30: reduce dose by 75%

87
Q

Vigabatrin is contraindicated in which patients?

A

BLACK BOX for VISION LOSS. So don’t use if patient has other risk factors for irreversible vision loss

88
Q

What are the adverse effects of Vigabatrin?

A

Depression, weight gain, insomnia, permanent loss of peripheral vision

89
Q

What are the monitoring parameters for Vigabatrin?

A

SCr, vision assessment at baseline and every 3-6 months

90
Q

What type of seizures is Ethosuximide (Zarontin) used to treat?

A

Absence

91
Q

What are the contraindications and warnings with Ethosuximide?

A

Avoid in renal/hepatic dysfunction

Warnings: Systemic Lupus Erythematosus, SJS/TEN

92
Q

What are the adverse effects associated with Ethosuximide?

A

Leukopenia, eosinophilia, psychiatric and sleep disturbances, aggression, hiccups

93
Q

What are the monitoring parameters and P450 metabolism?

A

P450 3A4 Substrate: major

CBC with differential and platelets, basic metabolic profile baseline and every 3 months

Therapeutics Spring 2016 (6 decks)

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