Advanced Pharm

Question 1

What is carbamazepine used for?

Answer 1

Generalized tonic clonic, partial

Question 2

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

Answer 2

CYP 3A4

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

Question 3

What are some of the adverse effects of carbamazepine?

Answer 3

CNS: Blurred vision, unsteadiness, headache, nausea

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

Hyponatremia

Question 4

What is the target concentration of carbamazepine?

Answer 4

6-8 mcg/mL

Question 5

When does anticonvulsant hypersensitivity syndrome usually occur?

Answer 5

1-8 weeks after exposure

Question 6

What are partial seizures?

Answer 6

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

Question 7

What are the types of Antiepileptic Agents?

Answer 7

Sodium channel blockers
GABAERGIC
Calcium channel blockers
Glutamate blockers

Question 8

What do sodium channel blockers do?

Answer 8

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.

Question 9

Sodium channel blockers inhibit the release of what?

Answer 9

Excitatory amino acids

Question 10

What are the black box warnings of carbamazepine?

Answer 10

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

Question 11

What is the patho physiology of anticonvulsant hypersensitivity syndrome?

Answer 11

T-cell activation

Question 12

What are the symptoms of anticonvulsant hypersensitivity syndrome?

Answer 12

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

Question 13

What is oxcarbazinepine an analog of?

Answer 13

Carbamazepine

Question 14

How is oxcarbazinepine metabolized and excreted?

Answer 14

MHD is inactivated by glucuronide conjugation and eliminated by kidneys

Question 15

What is the conversion of carbamazepine to oxcarbazinepine?

Answer 15

Initiate dose 1.5x higher than the carbamazepine dose.

Question 16

What are the significant adverse effects of oxcarbazinepine?

Answer 16

NO black box warnings

Generally less than carbamazepine

Question 17

What are the drug interactions of oxcarbazinepine?

Answer 17

Induces 3A4

Reduces oral contraceptive levels

Question 18

What is eslicarbazepine used for?

Answer 18

Partial onset seizures

Question 19

What is the metabolism and elimination of eslicarbazepine?

Answer 19

Partial onset seizures.

Question 20

What is the metabolism and elimination of eslicarbazepine?

Answer 20

Adjust for renal dysfunction

Question 21

What does the eslicarbazepine induce and what does it inhibit?

Answer 21

Induces CYP 3A4

Inhibits CYP 2C19

Question 22

Eslicarbazepine decreases concentrations of what?

Answer 22

Oral contraceptives

Question 23

What are the types of phenytoin?

Answer 23

Phenytoin acid and phenytoin sodium

Question 24

Phenytoin sodium has how much less than phenytoin?

Answer 24

8% less

Question 25

What is the dose dependent metabolism of phenytoin?

Answer 25

Michaelis-Mentin or capacity limited Enzyme system saturable

Question 26

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

Answer 26

Linear

Question 27

For phenytoin, what can small dose increase result in?

Answer 27

Large increase in levels

Question 28

What is the half life of phenytoin?

Answer 28

7-24 hours

Question 29

How is the clearance for the elderly with phenytoin?

Answer 29

20% less

Question 30

What is the target concentration and free concentration of Phenytoin?

Answer 30

Total concentration is 10-20 micrograms Free concentration is 1-2 micrograms

Question 31

What are the adverse effects of phenytoin?

Answer 31

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

Question 32

Phenytoin is an inducer of what?

Answer 32

CYP 3A4

Question 33

What is phenytoin metabolized by?

Answer 33

2C9 and 2C19

Question 34

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

Answer 34

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

Question 35

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

Answer 35

There is a significant reduction in bioavailability Space dosing by 2 hours

Question 36

What is the loading and maintenance dose for phenytoin?

Answer 36

Loading is 10-20mg/kg Maintenance is 4-7 mg/kg/day

Question 37

What is the maximum infusion rate for phenytoin?

Answer 37

50mg/min | 25mg/min in the elderly

Question 38

What are the pharmacokinetics of zonisamide?

Answer 38

Low protein binding | No active metabolite

Question 39

How is zonisamide metabolized?

Answer 39

It is hepatically metabolized by carbyoxylestrase.

Question 40

How is zonisamide excreted?

Answer 40

It is excreted by the kidneys unchanged.

Question 41

What are some of the adverse effects of zonisamide?

Answer 41

CNS (somnolence, agitation, cognitive impairment) Renal stones

Question 42

What are some of the contraindications of zonisamide?

Answer 42

Sulfa allergy Not recommended inpatients with CLcr of less than 50

Question 43

How is lamotrigine metabolized?

Answer 43

It is hepatically metabolized through glucoronidation

Question 44

What are the significant adverse effects of lamotrigine?

Answer 44

Dizziness, blurred vision, headaches

Question 45

What is the black box warning for lamotrigine?

Answer 45

Skin reactions Hypersensitivity Syndrome D/C at first sign

Question 46

How does oral contraceptives and phenytoin affect lamotrigine?

Answer 46

It induces it thereby decreasing the serum concentration

Question 47

How much valproic acid is needed to inhibit lamotrigine?

Answer 47

500 mg

Question 48

Rufinamide is an adjunctive for what?

Answer 48

Lennox-Gastaut

Question 49

What is the pharmacokinetics of Rufinamade?

Answer 49

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

Question 50

How is Rudinamide metabolized?

Answer 50

It is hepatically metabolized to inactive metabolite.

Question 51

What is the pharmacokinetics of lacosamide?

Answer 51

It is 100% bioavailable

Question 52

How is lacosamide eliminated?

Answer 52

Eliminated by renal excretion and biotransformation.

Question 53

What are significant adverse effects of lacosamide?

Answer 53

Prolong PR Interval, heart block