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Pharmacology > !Neuropharm Antiepileptics > Flashcards

!Neuropharm Antiepileptics Flashcards

1
Q

Benzodiazepines first line

A

Acute status epilepticus

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2
Q

Benzodiazepines second line indications

A

Eclampsia seizures

Can also be used for alcohol detoxification

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3
Q

Suffix of benzodiazepines

A

Pam

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4
Q

Examples of benzodiazepines

A

Diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, and chlordiazepoxide

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5
Q

How do benzodiazepines work

A

Bind to the BZd site not he GABAa Cl channels, leading to increased frequency of the Cl channel opening . Leading to neuronal membrane hyperpolarization and decrease in CNS excitability

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6
Q

Side effects of benzodiazepines

A

Decreased REM sleep
CNS depression
Dependence

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7
Q

How do you treat a benzodiazepine overdose

A

Flumazenil

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8
Q

Why do benzodiazepines treat status epilepticus first line

A

Fast acting , strong, and potent anticonvulsant drugs

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9
Q

Midazolam

A

IV used to induce anesthesia
Also cause relaxation
Causes anterograde amnesia

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10
Q

Benzodiazepine and anxiety

A

Acute use as anxiolytics

Not used one term due to risk of dependence

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11
Q

Benzodiazepines and eclampsia

A

Second line if magnesium sulfate is contraindicated.

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12
Q

Benzodiazepines and detoxification

A

Treat alcohol detox to prevent withdrawal symptoms

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13
Q

What benzodiazepines treat alcohol detox

A

Diazepam and chlorodiazepoxide

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14
Q

What are the two suffix of benzodiazepine

A

Zelma Zola’s

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15
Q

Name a benzodiazepine without the usual suffix

A

Chlorodiazepexide

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16
Q

How do diazepine work

A

Bind GABAA Cl receptor complex
Leads to Cl channel opening and increased frequency, yielding a higher chloride conductance
Causes neuronal membrane hyperpolarization and decreased CNS excitation

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17
Q

Sleep and benzodiazepines

A

Decrease REM but also sleep more

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18
Q

Benzodiazepine and CNS depression

A

ESP when combined with alcohol and other drugs

Alcohol binds GABAA like benzodiazepines

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19
Q

Benzodiazepine overdose

A

Dangerous

Espicially in combination with alcohol, barbiturates, opioids or tricyclics antidepressants

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20
Q

Symptoms of benzodiazepine overdose

A

CNS depression and intoxication with impaired balance, ataxia,and slurred speech
Respiratory distress, coma

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21
Q

Treat benzodiazepine overdose

A

Supportive care and flumazenil

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22
Q

How does flumazenil work

A

Benzodiazepine receptor antagonist which reverses the effects of benzodiazepine by competitive inhibition at the benzodiazepine binding site on the GABA receptor

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23
Q

Barbiturates

A

Barb in name

Wide range of uses and side effects

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24
Q

Indication for barbiturates

A

Seizure (simple and complex partial seizures as well), generalized tonic-clonic seizures

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25
Q

Thiopental barbiturate

A

Fast acting medication used for anesthesia induction

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26
Q

How do barbituates work

A

Potentiating GABAa, leading to increased chloride channel opening duration.leading to decreased neuronal firing.

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27
Q

Barbiturates increase the ____of chloride channel opening, whereas benzodiazepines increase __ of chloride channel opening

A

Duration

Frequency

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28
Q

Side effects of barbiturates

A

Sedation, grogginess
Respiratory and cardiac depression, which can progress to respiratory arrest and low blood pressure in patients who overdose or recreationally use barbiturates
CNS depression
If take with ethanol-additive adverse effects
Induce cytochrome P450 enzyme complex and may affect the metabolism of other medications

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29
Q

Examples of barbiturates

A 
Barb
Phenobarbital
Pentobarbital
Secobarbital
Anesthetic thiopental
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30
Q

Exception to barb name barbiturate

A

Thiopental-an anesthetic

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31
Q

Indications for barbiturate

A

Seizure control and anesthesia induction

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32
Q

What barbiturate use for seizure treatment -epilepsy, simple and complex seizures and generalized tonic-clonic seizures

A

Phenobarbital

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33
Q

Nick name of IV injected thiopental

A

Truth serum bc patients divulge sensitive information

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34
Q

Barbiturates : by increasing CL channel opening duration, __ __ is decreased

A

Neuronal firing

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35
Q

Barbiturates often mimic __

A

Ethanol
Can lead to severe cardiovascular depression
(Respiratory arrest and low bp in patients who abuse these drugs)

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36
Q

What happens when barbiturates increase p450

A

Clearance of such drugs from blood also increased. Therefore barbiturates can shorten the effects of other administered drugs making them less effective

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37
Q

Phenobarbital

A

Treat seizures acting onGABA receptors to inhibit excitatory neuronal firing

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38
Q

Side effect phenobarbital

A

CNS depression , drowsiness, fatigue, ataxia , paradoxical excitement

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39
Q

Why should you check blood levels of the drug

A

To avoid overdose

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40
Q

Huge concern with phenobarbital

A

High potential for recreational abuse with phenobarbital

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41
Q

Other use for phenobarbital

A

CNS depression is what it does

Daytime sedation and induction of sleep and anesthesia

42
Q

Ataxia from phenobarbital

A

High doses

Also show nystagmus

43
Q

Paradoxical excitement with phenobarbital

A

Espicially kids
Can get hyperactivity or “paradoxical excitement”

Important to ensure a calm environment

44
Q

Phenytoin

A

Antiepileptic medication used to treat generalized tonic clonic (grand mal) seizures and during status epilepticus.

45
Q

How does phenytoin work

A

Blocking sodium channel activation in neuronal membranes leading to an inhibition of glutamate release and resultingly, enhanced GABA release

46
Q

Phenytoin is categorized as and also has use as a class IB ___ medication

A

Antiarrhythmic

47
Q

Side effects phenytoin

A 
Teratogenic-fetal hydantoin syndrome
Induces cytochrome p45-
Decreases folate levels-megaloblastic anemia 
Drug induced lupus
Neurological symptoms 
Hirsutism-women who use it one term 
Gingival hyperplasia
48
Q

Indications for phenytoin

A

2nd line-status epilepticus (when benzodiazepines fail)

1st line-generalized tonic-clonic (grand mal) seizures

49
Q

MOA phenytoin

A

Blocks Na channel activation on neuronal cell membrane
Increases sodium channel inactivation
Decreasing lux of sodium ions across the Neuronal membrane
Limits spread of seizure activity and reducing propagation
Also stabilizes the threshold against hyperexcitability caused by excessive stimulation or environmental changes

50
Q

As a consequence of blocking na channel activation, phenytoin inhibits ___ release from excitatory presynaptic neurons and enhances __ release

A

Glutamate

GABA

51
Q

Teratogen effects of phenytoin

A

Fetal hydantoin syndrome

52
Q

What is fetal hydantoin syndrome

A

Intrauterine growth restriction, microcephalic, craniofacial deformities, developmental delay

53
Q

How does phenytoin cause microcytic megaloblastic anemia

A

Decreases folate levels

54
Q

What do patients with drug induced lupus from phenytoin have

A

Anti histone antibodies

55
Q

__ use of phenytoin can lead to peripheral neuropathy whale ataxia and diplopia can be seen with __ use of phenytoin

A

Chronic

Acute

56
Q

Long term use of phenytoin may lead to women with facial hair, ___

A

Hirsutism

57
Q

What percent of patients taking phenytoin have gingival hyperplasia

A

50

58
Q

Valproic acid (valproate)

A

Anticonvulsant and mood stabilizing drug that works by increasing GABA concentration and blocking Na channels

59
Q

Indications for valproic acid

A

Epilepsy, bipolar, migraine prophylaxis

60
Q

How does valproic acid work

A

Increases GABA by inhibiting the enzyme GABA transaminase, which acts to break down GABA

61
Q

Also valproic acid decreases repetitive neuronal firing by blocking what

A

Voltage gated Na channels

62
Q

Side effects valproic acid

A

GI distress
Hepatotoxic
Pancreatitis

63
Q

Who should not have valproic acid

A

Pregnant women-teratogenic and a folate antagonist and can lead to neural tube defects

64
Q

First line valproic acid

A

Tonic-clonic seizures and can also be used for absence, myoclonic and partial seizure treatment

65
Q

Bipolar and valproic acid

A

Totally

66
Q

Migraine prophylaxis and valproic acid

A

Totally

67
Q

Valproic acid MOA

A

Increases GABA concentration by inhibiting GABA transaminase, an enzyme which acts to break down GABA

Blocks voltage gated Na channels
Suppressing repetitive neuronal activity preventing Na influx though fast channels

68
Q

Side effects valproic acid

A 
VALPROATE
Vomiting
Alopecia
Liver toxicity
Pancreatitis/pancytopenia
Retain fat (weight gain
Oedema (edema) 
Appetite increase 
Tremor 
Enzyme inhibitor (P450)
69
Q

Manage liver with valproic acid

A

Check AST/ALT before and during treatment

70
Q

Pancytopenia valproic acid

A

Blood dyscrasias like anemia, leukopenia, and thrombocytopenia
Do a CBC found regularly

71
Q

Valproic acid and p450 inhibitor

A

Increase circulating amounts of other medications that would normally be metabolized
Liver disease patients-dosage decrease

72
Q

Topiramate

A

Epilepsy drug used in the treatment of partial seizures, and generalized tonic-clonic seizures

73
Q

What is the most common cause to prescribe topiramate

A

Migraine prophylactic

74
Q

Topiramate potentials __. What does this do

A

GABA, augmenting its Action on the GABAa receptor.

75
Q

Topiramate also induces a block of _ channel

A

Coltage gated Na

76
Q

Side effects topiramate

A

Kidney stones, weight loss and sedation

77
Q

Indications for topiramate

A

Seizure control

Migraine prophylaxis

78
Q

Can topiramate be used for weight loss

A

Yup and its FDA approved when combined with phentermine

79
Q

Carbamazepine

A

Anticonvulsant drug used as a first line agent against seizure and trigeminal neuralgia
Also a mood stabilizer in bipolar

80
Q

How does carbamazepine work

A

Blocking Na channel activation, stabilizing channels in an inactivated state, in a mechanism similar to phenytoin

81
Q

Side effects carbamazepine

A

SJS-dangerous hypersensitivity reaction affecting skin and mucous membranes
Hepatotoxicity-affecting the glutathione pathway
Blood dsycrasias-anemia and agranulocytosis
Inducer of cytochrome p450
Teratogen -neural tube defects /other birth defects

82
Q

First line indications for carbamazepine

A

Simple and complex partial seizures

Trigeminal neuralgia

83
Q

Second line carbamazepine

A

Neuropathic pain syndromes
Tonic-clonic generalized seizures
Mood stabilizer

84
Q

How does carbamazepine work

A

Stabilizing the inactivated state of voltage gated sodium channels, leaving cells less excitable and decreasing conductance.
Similar mechanism to phenytoin

85
Q

SJS

A

Hypersensitivity complex involving the skin and mucous membranes

86
Q

Carbamazepine and cytochrome p450

A

Increasing metabolism and reducing half life

May also accelerate clearance of other drugs

87
Q

Teratogen carbamazepine

A

Spina bifida, craniofacial abnormalities, Cardiovascular and urinary tract anomalies

88
Q

Carbamazepine and hepatotoxicity

A

Bc causes disturbance in glutathione metabolism which may occur as a result of accumulated toxic metabolites
Can be fatal , but rapidly reversed by stopping therapy

89
Q

Carbamazepine and blood dyscrasias

A

Rare side effect of carbamazepine includes blood dyscrasias such as agranulocytosis and aplastic anemia

90
Q

Lamotrigine

A 
Anticonvulsant medication used to treat simple ad complex partial seizures, as well as generalized tonic-clonic seizures 
Mood stabilizing (bipolar type I)
91
Q

Off label indications for lamotrigine

A

Neuropathic, migraine and personality disorders

92
Q

How does lamotrigine work

A

Block voltage sensitive Na channels, thereby stabilizing neuronal membranes and consequently modulating presynaptic transmitter release of glutamate and aspartate , which are excitatory aa (glutamate is a precursor to GABA)

93
Q

Side effects lamotrigine

A

SJS

94
Q

What is the effect of lamotrigine blocking voltage gated Na channels

A

Modulated presynaptic transmitter release of glutamate and aspartate, which are excitatory aa

95
Q

Ethosuximide

A

Anticonvulsant medication used to treat absence seizures, or petit mal seizures, which are mostly seen in school age kids

96
Q

First line indication for ethosuximide

A

Neurological disorder, and is preferred over similar drugs bc it does not cause hepatotoxicity

97
Q

MOD ethosuximide

A

Blocking thalmic t type ca channels leading to decreased neuronal transmission

98
Q

Side effects ethosuximide

A

SJS

99
Q

First line ethosuximide

A

Absence seizure treatment (petit mal seizures) and is preferred over other agents bc it does not cause hepatotoxicity

100
Q

T type channels

A

Blocked by ethosuximide
They serve peacemaking functions in both central neurons and support calcium signaling and are also involved int he modulation of firing patterns of neurons

101
Q

Side effects ethosuximide

A

SJS
Fatigue
Diarrhea

Pharmacology (52 decks)

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