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Pharmacology II > Exam 1 - Neurology Meds > Flashcards

Exam 1 - Neurology Meds Flashcards

1
Q

What drugs cause seizures?

A 
Theophylline
Alcohol
Phenothiazine antipsychotics
Antidepressants (Buproprion)
AEDs
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2
Q

GABA

A

Inhibitory neurotransmitter

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3
Q

Glutamate

A

Excitatory neurotransmitter

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4
Q

What drug causes glutamate to be converted into GABA? Why is this bad?

A

Glutamate is converted into GABA.
INH: inhibits enzyme that makes GABA > glutamate.

Patients develop seizures from too much glutamate activity.

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5
Q

Toxin Induced Seizures
What causes them?

OTIS CAMPBELL

A

OTIS CAMPBELL

Oral hypoglycemics and organophosphates
Theophilline/TCA
Isoniazid/Insulin
Salicylates
Camphor, cocaine, carbon monoxide
Amphetamines, anticholinergics
Methylxanthines
PCP 
Ethanol withdrawal
Lidocaine/Lead
Lindane/Lithium
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6
Q

Phenytoin

A
  • Treats seizures
  • Dose depends on age of patient, maturation of liver, and pharmacokinetics

Children 6m-3y metabolize at an increased patient 8-10mg/kg/day, while a 16y can only metabolize 6mg/kg/day.

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7
Q

Treatment options

A

Anti-epileptic drugs

Surgery to remove hyperactive parts of the brain

Ketogenic diet - puts patient in ketoacidosis. Acidifying blood increases seizure threshold.

Issue for peds - drugs come in suspensions that include sugar to make it taste better. Hard to manage patient on a ketogenic diet; check their food, meds.

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8
Q

AED therapy -

  • What do you start with?
  • What if you’ve failed multiple drug attempts?
A

Monotherapy should be tried first; add on additional agents if seizures are not controlled.

When multiple drug attempts are failed, may try nerve stimulator, ketogenic diet, and surgery. Charlotte’s web.

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9
Q

What is the drug of choice for absense seizures?

How does it work?

A

Ethosuximide

  • Blocks T channels (Calcium)
  • Only used for absence seizures
  • Valproate also works on calcium channels to help limit depolarization of neuron
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10
Q

GABA A receptor

A

GABA binds to GABA A receptor:

  • Opens channel and allows chloride to flow in
  • Hyperpolarizes cell to prevent it from firing off

GABA A: Target for seizures

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11
Q

What drug will modulate GAD, which is responsible for metabolizing glutamate into GABA?

A

Isoniazid

-Increasing glutamate metabolism, produces more GABA to be released and stop APs.

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12
Q

What drug blocks the reuptake of GABA?

A

Tiagabine

-More GABA in synapse will inhibit neuron from firing off.

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13
Q

What drug inhibits GABA metabolism by turning off the enzyme GABA transaminase?

A

Vigabatrin

-Stops the metabolism in the neuron to keep GABA there.

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14
Q

What drug allosterically causes GABA to be more effective in enhancing movement of chloride ions through the channels?

A 
Phenoarbital
Benzodiazepines
-Make GABA work better
-Hyperpolarize, calcium influx
-Good for status epilepticus and acute seizures
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15
Q

GAD role

A

Increases amounts of GABA being made

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16
Q

Glutamate receptors

A

Excitation

  • AMPA site
  • NMDA site
  • Kainate site
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17
Q

What drugs work to block glutamate from binding to receptors?

A

NMDA: Felbamate and Levetiracetam

AMPA/Kainate: Topiramate

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18
Q

What hormones have seizure inhibiting effects?

A

Progesterone prevents seizures, while estrogen may cause seizures.

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19
Q

Carbonic anhydrase inhibitors

-Acetazolamide

A

Drugs increase hydrogen ions intracellularly; makes blood acidic so seizure threshold is increased.

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20
Q

Phenytoin (Dilantin)

A
  • Treats generalized and partial seizures
  • Blocks sodium channels, so less firing of APs.
  • Protein bound.
  • Metabolized by CYP2C9 and CYP219
  • Induces CYP3A, 2C, and PGP
  • Michealis Menten kinetics put you at risk for toxicity with higher doses (0 order) - hepatocytes are oversaturated.
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21
Q

Phenytoin (Dilantin) ADR

A
  • Lethargy, blurred vision, nystagmus, ataxia, fall risk
  • SJS
  • Gingival hyperplasia, hirsutism
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22
Q

Why do we prefer Fosphenytoin over Phenytoin?

A

Phenytoin

  • Formulated with alcohol, propylene glycol - hard on the veins!!!
  • Can cause purple glove syndrome; tissue starts to become necrotic.

Water soluble form: Fosphenytoin

  • SAFER administration
  • First line for generalized and partial seizures.
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23
Q

Phenytoin Dosing Levels

A
  • Phenytoin is 90% protein bound.
  • Two levels: Free/Total
  • Free - in blood
  • Total - in blood/bound to proteins

Those with liver problems who don’t produce enough albumin, will have a higher free level.

Breakthrough seizures and increased toxicity – check the free level!

Altered binding:

  • Hypoalbuminemia
  • Renal failure
  • Multi-antiepileptic drug therapy
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24
Q

What happens if you administer over 50mg/min of Phenytoin?

A

Phlebitis and cardiovascular complications

Fosphenytoin - less pain and phlebitis, can do 150mg/min. Needs to be converted, though.

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25
Q

PE

A

phenytoin equivalence

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26
Q

Carbamazepine (Tegretol)

A
  • Treats seizures, mood stabilizer, and bipolar disorder
  • Sodium channel blocker
  • Induces CYP3A4, 2C9, 2C19

Autoinduction: metabolizes itself, dose has to increase over first few weeks until its stable. Otherwise, blood levels will drop

ADR: Bone marrow suppression, thrombocytopenia, leukopenia

SIADH - syndrome of inapropriate antidurietic hormone!!!!!!!!!!!!!!!!!

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27
Q

Oxcarbazepine (Trileptal)

A

Less enzyme induction, causes more SIADH. Hyponatremia.

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28
Q

Valproic acid (Depakote)

A

Blocks sodium, calcium chennels and enhances GABA
Used for bipolar and mood stabilizer
High protein binding

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29
Q

Valproic Acid ADR

A

Sedation, ataxia, tremor
Drug induced pancreatitis
Hepatotoxicity

30
Q

Valproic Acid DI

A

Use caution with drugs that inhibit PLT function, can see thrombocytopenia

Inhibit CYP2C9 and UGT (affect iamotrigene, lorazepam)

31
Q

Benzodiazepines

  • Diazepam (Diastat)
  • Lorazepam (Ativan)
  • Midazolam (Versed)
  • Clonazepam (Klonoprin)
  • Clobazam (Onfi)
A

Diazepam - rectal gel (used for acute seizures)

Midazolam - intranasal; used for kids without IV access

MOA: Bind to GABA A and allosterically make GABA work better

Abuse potential

32
Q

Fat soluble vs. water soluble drugs

A

Fat soluble = Benzodiazepines, fast onset for seizures, crosses BBB fast; but leaves quick.

Water soluble = Lorazepam; takes longer to cross BBB but stays there longer.

33
Q

What’s the go to for acute seizures?

A

Lorazepam

  • Rectal dose of diazepam
  • IV dose Lorazepam

-Takes longer to cross BBB but stays there longer.

34
Q

Phenobarbital (Luminal)

A
  • Opens up GABA A channels
  • Drug of choice for neonatal seizures; can be used if patient fails a benzodiazepine (2nd line)
  • Good for status epilepticus
  • CNS depression, respiratory depression, hypotension
  • Directly open channel, so more depressive effects.
  • Metabolized by CYP2C19, Induces 2C9 and 3A4

C4

35
Q

Pentobarbital (Nembutal)

A
  • Similar to phenobarbitol in MOA/ADR
  • IV for status epilepticus
  • “Pentobarb coma”
36
Q

Felbamate (Felbatol)

A
  • Enhance GABA and inhibit NMDA glutamate receptors

- Risk for aplastic anemia, hepatotoxicity, drug interactions

37
Q

Ethosuximide

A
  • Blocks calcium channels

- DOC for absence seizures.

38
Q

Gabapentin (Neurontin)

Pregabalin (Lyrica)

A

May interact with calcium channels and enhance GABA synthesis

  • Renal excretion, DOSE RENALLY
  • CNS depression
39
Q

Lamotrigene (Lamictal)

A
  • Inhibits sodium channels, inhibits glutamate release
  • Inhibited by VPA, need to use 50% less of Lamotrigene so you don’t get toxicity!!!!!!!!

Black boxed: D/C at any sign of a rash.

  • Rash, prevent by using low dose
  • SJS
  • Dizziness, ataxia, N/V
40
Q

Patient on VPA still hving breakthrough seizures, want to add on Lamotrigene? How would you dose?

A

Use half of Lamotrigene to prevent toxicity.

41
Q

Levetireacetam (Keppra)

A

Mechanism unknown
Quickly becoming a first line therapy
Adjunct for patrial seizures
Few drug interactions adn ADRs

Can increase aggression in children

42
Q

Tiagabine (Gabitril)

A
  • Inhibits reuptake of GABA
  • Used as second line therapy when others failed by themselves
  • Can cause psychosis
  • Prevent toxic levels by taking it wtih food to slow rise in blood levels
43
Q

Topiramate (Topamax)

A
  • Sodium, gaba, and antiglutamate
  • RENAL DOSING due to renal elimination
  • Carbonic anhydrase activity
  • Renal calculi and metabolic acidosis, esp with overdose

Also used for weight loss and migraines

44
Q

Zonisamide (Zonegran)

A

Inhibits T calcium channels
Adjunct therapy, not used alone
Sulfonamide structure, so don’t give to those with SULFA allergy!!!!
Renal calculi

45
Q

START OF NEWER DRUGS

Lacosamide (Vimpat)

A

Targets sodium and binds to collapsin response mediator protein

C5

46
Q

Rufinamide (Banzel)

A

Triazole derivative
Modulate sodium channels
Somnolence, SUICIDE BEHAVIOR, QT shortening, STATUS EPILEPTICUS

47
Q

Ezogabine (Potiga)

A
  • Potassium channels

- QT prolongation, dysrythmias, aggressiveness

48
Q

Perampanel (Fycompa)

A
  • AMPA antagonist

- Aggression, hostility, homocidal ideation

49
Q

TEST

A

Newer agents are less likely to be asked.

Phenytoin, carbamazepine, valproic acid = frequently used

50
Q

Status epilepticus

A
  • Airway and circulation under control first.
  • 1st line: Lorazepam, diazapem per rectum, medazolam intransal.
  • 2nd line: If unresponsive, phenytoin or fosphenytoin.
  • 3rd line: If unresponsive, Levetireacetam or phenobarbital.
  • 4th line: If unresponsive, valproic acid or phenobaritol.
  • If unresponsive, general anesthesia or coma.
51
Q

When do you stop AED therapy?

A
  • Seizure free for 2 to 5 years.
  • Single seizure type.
  • Normal neuro exam.
  • EEG normalized with treatment.

Can titrate off and see how they respond.

52
Q

Drug Levels…..

A

….

53
Q

What drugs cause less drowsiness?

A

Lamotrigene and valproic acid

54
Q

What drugs are not used for school aged children due to their interference with learning?

A

Phenobarbital

55
Q

What causes SJS?

A

Lamotrigene, carbamazepine, phenytoin, ethosuximide, phenobarbital

56
Q

What caues life threatening rashes?

A

Oxcarbazepine, Lamotrigene

57
Q

Aplasia anemia?

A

Felbamate

Use if they fail all the other treatmetns

58
Q

Thrombocytopenia?

A

Carbamazepine, valproic acid, and phenytoin

59
Q

Mouth ulcers, unusual bruising or bleeding

A

signs of blood dyscrasia

60
Q

Hepatic failure?

A

Valproic acid

61
Q

What drugs need TDM?

A

carbamazepine, phenobarb, valproic acid, phenytoin

62
Q

What decrease effectiveness of oral contraceptives?

A

Phenytoin, phenobarb, carbamazepine, oxcarbazepine, felbamate

INDUCE CYP3A4 so metabolize it more quickly

63
Q

Cholinergic toxidrome

A

Increasing levels of Ach, run risk of having muscarinic excess.

Defecation
Urination
Miosis
Bradycardia
Bronchorrhea and spasm
emesis
Lacrimation
Salivation

leaking fluids from everywhere, pulmonary secretions are bad.

64
Q

Cholinesterase inhibitors

  • Tacrine
  • Donepezil
  • Rivastigmine
  • Galantamine
A
  • centrally acting, used to treat mild to moderate alzheimer’s disease.
  • Improve memory/cognition
  • Don’t affect course of continuing neurodegeneration, just extends life of Ach release.

-Does not stop disease progression.

65
Q

G1 form

A

acetyl cholinesterase in the brain

66
Q

Tacrine

A

Not used, because hepatotoxicity

67
Q

Donepezil (Aricept)

A

Specific for acetyl cholesterase, no heptotoxicity or mild peripheral cholinergic affects.

metabolized by CYP2D6 and 3A4.

68
Q

Rivastigmine (Exelon)

A

Inhibits acetylcholinesterase and BuChE
Dissocation or half life is 9 hours, longer duration of action and requires twice daily dosing

no cyp interactions
slow reversability

69
Q

Galantamine (Razadyne)

A

Specific for AChE
Twice daily dosing
Have rapid reversability, may see reduced response over time.
Metabolized by CYP2D6 and 3A4.

70
Q

Glutamate neurotoxicity drug therapy

A

Excitatory - destruction of neurons occurs from over excitatory or excess glutamtate activity - puts stress on neurons leading to neuronal loss.

Glutamate is responsible for it, so to slow progession of disease, can inbhit glutamate

71
Q

Mamantine (Namenda)

A

moderate to severe alzheimers
well tolerated
glutamate antagonist - binds to receptor to change receptor so glutamate can’t bind.

Neuroprotective effects - able to slow down or stop neurodegeneration

Pharmacology II (10 decks)

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