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Pharmacology Exam III > Anti-Convulsants > Flashcards

Anti-Convulsants Flashcards

1
Q

Seizures defined

A

transient episodes of brain dysfunction and altered behavior due to ABNORMALLY EXCESSIVE, SYNCHRONOUS, AND RHYTHMIC FIRING of certain HYPEREXCITABLE NEURONS

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2
Q

Seizures Underlying Causes (3 primarily)

A

CNS injury

Congenital abnormalities

Genetic factors

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3
Q

Epilepsy defined

Two main subtypes?

A

CHRONIC NEUROLOGICAL DISORDER characterized by RECURRENT SEIZURES

Primary idiopathic
Secondary

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4
Q

Two main subtypes of Seizures?

A

PARTIAL - affect only parts of the brain

GENERALIZED - affect large areas and multiple areas of the brain

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5
Q

Partial Seizure IMPORTANT CHARACTERISTIC

A

ONLY PART OF THE BRAIN is involved

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6
Q

Partial Seizure Types (3)

A

Simple
Complex
Partial becoming generalized

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7
Q

Simple Partial Seizure

A

MINIMAL SPREAD OF ABNORMAL DISCHARGE

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8
Q

Complex Partial Seizure

A

STARTS IN SMALL BRIAN AREA but QUICKLY SPREADS TO OTHER AREAS

AUTOMATISMS

most common

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9
Q

Partial becoming generalized seizure

A

SPREAD THROUGHOUT BRAIN AND PROGRESS TO GENERALIZED

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10
Q

Generalized Seizures characteristic

two types?

A

involve THE ENTIRE BRAIN with global EEG change and BILATERAL MANIFESTATIONS

Petit mal (absence)
Grand mal (tonic clonic)
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11
Q

Petit mal seizures

A

sudden onset, abrupt cessation

BRIEF LOSS OF CONSCIOUSNESS

typically observed in CHILDREN

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12
Q

Grand mal seizures characteristics

A

TONIC SPASMS AND MAJOR CONVULSIONS OF ENTIRE BODY

LOSS OF CONSCIOUSNESS

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13
Q

Grand mal seizures four phases

A

Aura
Tonic
Clonic
Stuporous state and sleep

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14
Q

Status epilepticus

A

CONTINOUS OR VERY RAPID RECURRING SEIZURES

MEDICAL EMERGENCY REQUIRING IMMEDIATE THERAPY

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15
Q

3 Stages of Mechanisms Generating Epileptic Seizures

A

Initiation
Synchronization of surrounding
Propagation - recruitment of normal neurons

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16
Q

EPSP

A

excitatory post-synaptic potential

temporary depolarization and excitation of post-synaptic membranes caused by flow of positively charged ions into the cell

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17
Q

Epilepsy Treatment Options

A

Anti-epileptic meds
Surgery
Vagus nerve stimulation

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18
Q

Anti-epileptic medication goal

A

RESTORE NORMAL PATTERNS OF ELECTRICAL ACTIVITY

inhibit seizures

partially effective at prophylaxis

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19
Q

Cyclic Ureides (5)

A 
Phenytoin
Fosphenytoin
Primidone
Phenobarbital
Ethosuximide
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20
Q

Tricyclics (2)

A

Carbamazepine

Oxcarbazepine

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21
Q

Benzodiazepines (2)

A

Diazepam

Lorazepam

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22
Q

GABA Derivatives (2)

A

Gabapentin

Pregabalin

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23
Q

Other Anti-Seizure Drugs (5)

A 
Valproic acid
Lamotrigine
Acetazolamide
Tiagabine
Topiramate
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24
Q

Drugs for Partial Seizures with or without secondary generalized (3)

A

Carabamazepine
Phenytoin
Valproate

25
Q

Drugs for Tonic-clonic seizures (3)

A

Carbamazepine
Phenytoin
Valproate

26
Q

Drugs for Absence seizures (petit mal)

A

Ethosuximide

Valproate

27
Q

Drugs for myoclonic seizures (2)

A

Clonazepam

Valproate

28
Q

Drugs for Status Epilepticus (4)

A

Diazepam
Lorazepam
Phenytoin
Fosphenytoin

29
Q

Anti-Convulsant General MOA

3 options

A

INHIBIT FIRING

Decrease excitatory effects - BLOCK VOLTAGE GATED Na channels

Increase inhibitory effects of GABA

Alter neuronal activation by altering ion movement across membrane - INHIBITION OF VOLTAGE GATED Ca channels

30
Q

Inactivation of Na Channels causes

A

DECREASE IN SUSTAINED, HIGH FREQUENCY, REPETITIVE DISCHARGE

prolongs inactivation

31
Q

Reduced calcium influx causes

A

DECREASED NEUROTRANSMITTER RELEASE

prevent neuronal excitability

32
Q

Anti-convulsant side effects

A 
Sedation
Diplopia
Nystagmus
Ataxia
GI Upset
33
Q

Anti-convulsant important considerations

A

AVOID ABRUPT WITHDRAWAL

DECREASE EFFICACY OF ORAL CONTRACEPTIVES

TERATOGENIC

PHENOBARBITAL - safest during pregnancy

34
Q

Fosphenytoin unique

A

newer, more soluble PRODRUG OF PHENYTOIN

used for parenteral routes**

35
Q

Phenytoin absorption

A

VARIABLE

FORMULATION DEPENDENT

36
Q

Phenytoin pharmacokinetics

A

Metabolized in LIVER

DOSE-DEPENDENT - ZERO ORDER elimination

CAN BE SATURATED

37
Q

Phenytoin MOA

A

blocks and prolongs INACTIVATED STATE OF Na Channels

Enhances GABA release

Prevents seizure PROPAGATION

38
Q

Phenytoin clinical uses (3)

A

Generalized tonic-clonic
Partial seizures
Status epilepticus

39
Q

Phenytoin Idiosyncratic Side Effects

A 
Hirsutism
GINGIVAL HYPERPLASIA
Osteomalacia
Megaloblastic Anemia
Fetal hydantoin syndrome
40
Q

Carbamazepine MOA

A

INHIBITION OF VOLTAGE GATED Na Channels

blocks high frequency firing
decreases glutamate release

41
Q

Carbamazepine Metabolism

A

INDUCES P450 enzymes

induces it’s own metabolism

42
Q

Oxacarbazepine

A

NEWER drug similar to carbamazepine

ACTIVE METABOLITE HAS LONGER DURATION, fewer drug interactions

43
Q

Carbamazepine clinical uses

A

TONIC CLONIC SEIZURES
PARTIAL SEIZURES

drug of choice for TRIGEMINAL NEURALGIA

44
Q

Carbamazepine Important Side effects (2)

A

SIADH - syndrome of inappropriate ADH secretion

teratogenic –> SPINA BIFIDA

45
Q

Barbiturates (phenobarbital) MOA

Important clinical use?

A

Enhances GABA-A RECEPTOR RESPONSES

increases opening time of Cl- channel

STATUS EPILEPTICUS

46
Q

Primidone

A

metabolized by LIVER to PHENOBARBITAL and PEMA

47
Q

Ethosuximide MOA

Primary clinical use?

A

BLOCKS PRE-SYNAPTIC Ca Channels

ABSENCE SEIZURES - drug of choice***

48
Q

Valproic acid MOA

A

INHIBITION OF Ca Channels

Inhibition of GABA transaminase

Absence Seizures - drug of choice***

bipolar disorder as well

49
Q

Valproic acid adverse effects

A

HEPATOTOXIC SYNDROME - d/t toxic metabolite

TERATOGENIC - spina bifida

50
Q

Diazepam MOA

Great choice clinically for?

A

POTENTIATES GABA-A RESPONSE

increases Cl- channel opening

STATUS EPILEPTICUS

51
Q

Diazepam vs Lorazepam

A

Diazepam effects are MUCH SHORTER - cannot be used by itself

Lorazepam has LONGER DURATION OF ACTION - can be used by itself

52
Q

Gabapentin MOA

Clinical uses (2)

A

GABA analog

BLOCKS PRE-SYNAPTIC Ca Channels

PARTIAL SEIZURES
TONIC-CLONIC SEIZURES

NEUROPATHIC PAIN***

53
Q

Pregabalin

A

similar to gabapentin

GABA Analog

54
Q

Lamotrigine MOA

Important side effect?

A

BLOCKS PRE-SYNAPTIC VOLTAGE GATED Na and Ca channels

Stevens-Johnson Syndrome

55
Q

Felbamate MOA

A

BLOCKS Na Channels and GLUTAMATE RECEPTORS

56
Q

Tiagabine MOA

A

specifically designed as GABA UPTAKE INHIBITOR

57
Q

Centrally Acting Muscle Relaxants (2)

A

Baclofen

Benzodiazepine

58
Q

Baclofen MOA

A

GABA-B AGONIST

increased K conduction, decrease Ca influx

results in HYPERPOLARIZATION

Reduction in excitatory transmitter release

Pharmacology Exam III (11 decks)

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