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Advanced Pharm. > Advanced Pharm > Flashcards

Advanced Pharm Flashcards

1
Q

What is carbamazepine used for?

A

Generalized tonic clonic, partial

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2
Q

What is carbamazepine a substrate of and what does it induce?

A

CYP 3A4

It’s an autoinducer. It induces it’s own metabolism.

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3
Q

What are some of the adverse effects of carbamazepine?

A

CNS: Blurred vision, unsteadiness, headache, nausea

Black box warnings: Derm reactions, Blood dyscrasias, anticonvulsant hypersensitivity syndrome.

Hyponatremia

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4
Q

What is the target concentration of carbamazepine?

A

6-8 mcg/mL

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5
Q

When does anticonvulsant hypersensitivity syndrome usually occur?

A

1-8 weeks after exposure

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6
Q

What are partial seizures?

A

Limited to one hemisphere. Simple partial (no impaired consciousness). Complex partial (impaired consciousness)

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7
Q

What are the types of Antiepileptic Agents?

A

Sodium channel blockers
GABAERGIC
Calcium channel blockers
Glutamate blockers

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8
Q

What do sodium channel blockers do?

A

Reduce sodium influx which slows depolarization. It reduces the ability of neurons to fire at a rapid rate.

By blocking the voltage sensitive sodium channels the inactivation state of the channels is prolonged.

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9
Q

Sodium channel blockers inhibit the release of what?

A

Excitatory amino acids

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10
Q

What are the black box warnings of carbamazepine?

A

Dermatologic reactions. Blood dyscrasia. Anticonvulsant hypersensitivity syndrome. Hyponatremia.

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11
Q

What is the patho physiology of anticonvulsant hypersensitivity syndrome?

A

T-cell activation

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12
Q

What are the symptoms of anticonvulsant hypersensitivity syndrome?

A
  1. Fever, malaise
  2. Rash/skin eruption
  3. Systemic organ involvement
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13
Q

What is oxcarbazinepine an analog of?

A

Carbamazepine

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14
Q

How is oxcarbazinepine metabolized and excreted?

A

MHD is inactivated by glucuronide conjugation and eliminated by kidneys

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15
Q

What is the conversion of carbamazepine to oxcarbazinepine?

A

Initiate dose 1.5x higher than the carbamazepine dose.

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16
Q

What are the significant adverse effects of oxcarbazinepine?

A

NO black box warnings

Generally less than carbamazepine

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17
Q

What are the drug interactions of oxcarbazinepine?

A

Induces 3A4

Reduces oral contraceptive levels

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18
Q

What is eslicarbazepine used for?

A

Partial onset seizures

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19
Q

What is the metabolism and elimination of eslicarbazepine?

A

Partial onset seizures.

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20
Q

What is the metabolism and elimination of eslicarbazepine?

A

Adjust for renal dysfunction

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21
Q

What does the eslicarbazepine induce and what does it inhibit?

A

Induces CYP 3A4

Inhibits CYP 2C19

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22
Q

Eslicarbazepine decreases concentrations of what?

A

Oral contraceptives

23
Q

What are the types of phenytoin?

A

Phenytoin acid and phenytoin sodium

24
Q

Phenytoin sodium has how much less than phenytoin?

A

8% less

25
Q

What is the dose dependent metabolism of phenytoin?

A

Michaelis-Mentin or capacity limited

Enzyme system saturable

26
Q

For phenytoin below the enzyme system saturability, what are the kinetics like?

A

Linear

27
Q

For phenytoin, what can small dose increase result in?

A

Large increase in levels

28
Q

What is the half life of phenytoin?

A

7-24 hours

29
Q

How is the clearance for the elderly with phenytoin?

A

20% less

30
Q

What is the target concentration and free concentration of Phenytoin?

A

Total concentration is 10-20 micrograms

Free concentration is 1-2 micrograms

31
Q

What are the adverse effects of phenytoin?

A 
Phenytoin hypersensitivity syndrome
Nausea, vomiting, constipation 
Gingival hyperplasia
Hirsutism
Hypotension 
Bradycardia 
QRS prolongation 
Decreased cognitive ability
Leukopenia, thrombocytopenia, anemia
32
Q

Phenytoin is an inducer of what?

A

CYP 3A4

33
Q

What is phenytoin metabolized by?

A

2C9 and 2C19

34
Q

What do you have to remember with protein binding when it comes to phenytoin?

A

There are displacement interactions with other drugs that are highly protein bound.

35
Q

What must you remember about phenytoin and tube feeding and antacids?

A

There is a significant reduction in bioavailability

Space dosing by 2 hours

36
Q

What is the loading and maintenance dose for phenytoin?

A

Loading is 10-20mg/kg

Maintenance is 4-7 mg/kg/day

37
Q

What is the maximum infusion rate for phenytoin?

A

50mg/min

25mg/min in the elderly

38
Q

What are the pharmacokinetics of zonisamide?

A

Low protein binding

No active metabolite

39
Q

How is zonisamide metabolized?

A

It is hepatically metabolized by carbyoxylestrase.

40
Q

How is zonisamide excreted?

A

It is excreted by the kidneys unchanged.

41
Q

What are some of the adverse effects of zonisamide?

A

CNS (somnolence, agitation, cognitive impairment)

Renal stones

42
Q

What are some of the contraindications of zonisamide?

A

Sulfa allergy

Not recommended inpatients with CLcr of less than 50

43
Q

How is lamotrigine metabolized?

A

It is hepatically metabolized through glucoronidation

44
Q

What are the significant adverse effects of lamotrigine?

A

Dizziness, blurred vision, headaches

45
Q

What is the black box warning for lamotrigine?

A

Skin reactions
Hypersensitivity Syndrome
D/C at first sign

46
Q

How does oral contraceptives and phenytoin affect lamotrigine?

A

It induces it thereby decreasing the serum concentration

47
Q

How much valproic acid is needed to inhibit lamotrigine?

A

500 mg

48
Q

Rufinamide is an adjunctive for what?

A

Lennox-Gastaut

49
Q

What is the pharmacokinetics of Rufinamade?

A

Slow absorption

(4-6 hours to peak), increased with food.

50
Q

How is Rudinamide metabolized?

A

It is hepatically metabolized to inactive metabolite.

51
Q

What is the pharmacokinetics of lacosamide?

A

It is 100% bioavailable

52
Q

How is lacosamide eliminated?

A

Eliminated by renal excretion and biotransformation.

53
Q

What are significant adverse effects of lacosamide?

A

Prolong PR Interval, heart block

Advanced Pharm. (1 decks)

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