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What is the mechanism of action for the drug phenytoin (dilantin)?
Inhibits neuronal sodium channels
Phenytoin (Dilantin) is highly protein-bound, what could result from a drug interaction that reduces the percentage of phenytoin binding to protein?
Toxicity of phenytoin due to more free drug circulating in the system
Note: renal failure and/or low albumin affects this
True or False: Phenytoin is a CYP3A inducer?
True
Name some side effects to phenytoin (Dilantin)?
Lethargy, blurred vision, Hirsutism, Gingival Hyperplasia, Vit D deficiency, and osteomalacia
Our patient needs phenytoin for a generalized seizure, but they do not have a central line or a decent IV, what and how should we administer?
We should administer Fosphenytoin IM
What can happen if we administer phenytoin IV in the hand but the IV blows and it leaks into the surrounding tissue?
Purple glove syndrome
What is the mechanism of action of the anti-seizure medication carbamazepine (Tegretol)?
Blocks sodium channels
How must we dose Carbamazepine (Tegretol) in order for the patient to receive the correct amount of drug?
We must constantly increase the dose due to a metabolism autoinduction
What adverse reaction are carbamazepine and Oxcarbazepine notable for?
Hyponatremia due to SIADH
Besides a sodium level, which lab value should we monitor for on a patient taking carbamazepine (Tegretol)?
Liver enzymes
Patient comes into the ED for seizures, the family states that the patient was started on a new seizure medication prior. Lab work comes back showing a low sodium level? Which two anti-seizure meds are known to cause a low sodium count (hyponatremia)?
Carbamazepine (Tegretol)
Oxcarbazepine (Trileptal) (MORE COMMON)
What three mechanism of actions does Valproic Acid (Depakote) have?
Inhibits Sodium Channels
Inhibits Calcium Channels
Increases/enhances GABA
Which notable adverse reactions is Valproic acid know for possibly causing?
HINT: 2 of them
Pancreatitis and hepatotoxicity
Which antiseizure medication can cause pancreatitis?
Valproic Acid (Depakote)
If we are treating a young female (24 yrs old) with Valproic Acid (Depakote), what must we counsel our patient on before prescribing it?
To not get pregnant and to use contraceptive measures because of the risk of neural tube defects
Patient is presenting to the office for a follow up after been on valproic acid (Depakote) for some time, we do a blood check and notice that the level of the anti-seizure drug is low. What is the patient at risk for?
Having a seizure
Note: Always do therapeutic drug monitoring for Valproic Acid
What is the mechanism of action for Benzodiazepines?
Enhances GABAA to increase Chloride influx
Which Benzodiazepine is notable for being used intranasally?
Midazolam (Versed)
Which benzodiazepine is used as an oral agent for pediatric kids having seizures?
Clonazepam (Klonopin)
Is it safe to discontinue Benzodiazepines OR Barbiturates abruptly?
NO!
What is the mechanism of action of Phenobarbital (Luminal)?
Activating and opening GABAA channels which increases chloride influx
Which antiseizure drug is better used for neonates?
HINT: specifically neonates, not just peds in general
Phenobarbital (Luminal)
-rarely used in adults do to ADRs
Which anti-seizure drug is mainly used for refractory status epilepticus?
Pentobarbital (nembutal)
Which antiseizure drug do we stay away from mainly because of its chances of causing fatal aplastic anemia?
Felbamate (Felbatol)
Which antiseizure drug is the drug of choice for Absence Seizures?
What is the mechanism of action of this drug?
Ethosuximide (Zarontin)
Inhibits neuronal calcium channels
How is Gabapentin (Neurontin) and Pregabalin (Lyrica) eliminated out of the body?
100% renally eliminated
What is the major adverse drug reaction that Gabapentin and/or Pregabalin can cause?
CNS depression
What three mechanism of actions does the anti-seizure medication lamotrigine (Lamictal) do?
Inhibits sodium channels
Inhibits glutamate release
Modulates calcium channels
What is a notable adverse reaction to lamotrigine (Lamictal)?
Why might we choose this anti-seizure medication over others?
Stevens-Johnson Syndrome
-this medication tends to have less sedative effects than others
Valproic acid is a CYP2C9 and UGT inhibitor, How can this affect Lamotrigine specifically?
This will change the way we dose lamotrigine (lower dose) because Valproic Acid is blocking Lamotrigine's pathway for excretion leading to abnormal higher levels in the blood.
Which common pediatric anti-seizure medication has unique adverse reactions of child aggression, psychosis, and suicide attempts?
Levetiracetam (Keppra)
NOTE: this drug is a common first line therapy for kids with seizures
Topiramate (Topamax) is considered a carbonic anhydrase inhibitor? Which type of patients should we be concerned with taking this medication?
Those with a history of kidney stones
What is a very notable adverse drug reaction that can occur when taking Topiramate (Topamax)?
Impaired concentration
If a child is presenting to the office with a history of previous seizures and is complaining of an inability to focus at school, which anti-seizure medication is this patient most likely on?
Topiramate (Topamax)
Which anti-seizure medication can be notable for causing an increased PR interval?
Lacosamide (Vimpat)
Our patient is having status epilepticus, what is our initial first line of treatment?
Benzodiazepines (Diazepam, Lorazepam, Midazolam)
If our patient is having status epilepticus, we tried 2-3 doses of benzos but no response. What is our next course of action?
We can try Fosphenytoin, then Levetiracetam (Keppra), then Valproic acid
NOTE: Wood mentioned that after trying Benzos, you should probably consult with neurology to figure out which of these to try first
If our patient is having refractory status epilepticus with no improvement to any of our anti-seizure medications such as benzos and valproic acid, what should we consider next?
General anesthesia or Barbiturates such as Pentobarbital
Which two anti-seizure medications are notable for causing less drowsiness?
Lamotrigine and Valproic acid
Which two medications have black box warnings for life threatening rashes such as SJS/TEN?
Oxcarbazepine and Lamotrigine
Which 4 anti-seizure medications should we do therapeutic drug monitoring for?
Carbamazepine, phenobarbital, valproic acid, and phenytoin
Which neuro-protective medication (MAOI) for Parkinson's can show up as amphetamines on a urine drug screen?
Selegiline (Eldepryl, Zelapar)
Which two neuroprotective medications (MAOIs) for Parkinson's can potentially cause serotonin syndrome?
Selegiline and Rasagiline
Note: Rasagiline has fewer drug reactions and does not show up on a drug screen
Can we use MAO-B inhibitors as monotherapy for Parkinson's?
Yes
What is the theory behind how we can use MAOI's to help treat early signs of Parkinson's?
MAOI's help to prevent free radicals from damaging neurons in the brain
What type of foods should we tell our patient who is using MAOI's to stay away from due to possible serotonergic toxicity?
FANCY FOODS
Aged cheeses and meats
Fava beans
Red wine
Which specific types of drugs should we prescribe to a patient suffering from tremors secondary to Parkinsons?
Anticholinergics (Benztropine, Trihexyphenidyl, Diphenhydramine)
NOTE: These drugs can cause constipation, dry mouth, urinary retention, etc.... Use mnemonic for anti-cholinergics
Which drug can help manage levodopa induced dyskinesias?
Amantadine (Symmetrel)
What is the origin of Bromocriptine (Parlodel) in treating Parkinsons ?
What are the major side effects involved with this?
Infected rye
Think of his St. Anthony's fire reference
peripheral paresthesias, dyskinesias, and heart valve issues
Which non-ergot derivative can be used as a transdermal patch for the treatment of Parkinsons?
Rotigotine (Neupro)
What is our gold standard of treatment for Parkinsons?
Levodopa/Cardidopa (Sinemet)
Note: Not first line, try neuroprotective factors first
What is the main purpose of carbidopa?
To block enzymes in the blood stream (L-ADD) in order for levodopa to cross the BBB and get into the brain
Does levodopa have a dietary factor involved with taking the medication?
YES
Levodopa is absorbed by a saturable transporter in the small intestine
What kind of medications can we use in order to increase the half life of levodopa?
What is a unique side effects from these meds?
COMT inhibitors
Brown/Orange discoloration and enhanced dyskinesias
Which COMT inhibitor has a black box warning for hepatotoxicity?
Tolcapone (Tasmar)
NOTE: He said we never use this, use Entacapone instead
At what age would we consider sending patients straight to carbidopa/levodopa without trying other meds such as anticholinergics and dopamine agonists?
65 and above
What are some ways we can counteract dystonia and stiffness in patients on Levodopa/Carbidopa?
Bedtime dosing
Dopamine agonist
Rotigotine
Morning dosing
BOTOX*
How can we overall help treat Alzheimer's?
By enhancing acetylcholine and preventing the loss of cholinergic neurons
What are our three main cholinesterase inhibitors for the treatment of Alzheimer's?
Donepezil, Rivastigmine, and Galantamine
A patient presents to the office with Alzheimer's and is currently taking Tacrine for it. Your patient explains to you that she is very forgetful and sometimes has trouble taking it in time. Which cholinesterase medication could we switch her over to?
Donepezil (Aricept) because of the 70 hr half life
Why might we tend to use Rivastigmine over Donepezil and Galantamine when treating Alzheimer's?
Patient is taking ketoconazole, quinidine, or some sort of CYP 3A4 inhibitor/inducer
NOTE: Donepezil (Aricept) and Galantamine (Razadyne) is metabolized through CYP3A4
Which NMDA glutamate receptor antagonist is very well tolerated for the treatment of Alzheimer's?
Memantine (Namenda)
Which medication would we give to our patient who is undergoing a Multiple Sclerosis exacerbation?
IV methylprednisolone for 3-10 days
NOTE: Taper off after 1 week due to adrenal insufficiency
Which injectable multiple sclerosis agent can cause chest tightness, flushing, and dyspnea?
HINT: this agent mimics antigenic properties of myelin protein
Glatiramer Acetate (Copaxone)
Which monoclonal antibody prevents lymphocytes from crossing the BBB and is used to treat MS?
What is the black box warning associated with this?
Natalizumab (Tysabri)
--> Progressive multifocal leukoencephalopathy
Which oral MS medication should we monitor for bradycardia after the first dose?
Fingolimod (Gilenya)
Why would a patient who is taking Fingolimod (Gilenya) be at risk for reversible Lymphoma?
Because the drug is moving lymphocytes into lymphoid organs as apart of the mechanism of action.
Which oral MS medication has black box warnings for both hepatotoxicity and teratogenicity?
Teriflunomide (Aubagio)
25 y/o female presents to the office who has been on Teriflunomide for MS, she is looking to get pregnant this year. How would we make sure all of the medication is out of her system in order to prevent pregnancy issues?
We give a cholestyramine washout!
What should we test the patient for before giving Teriflunomide (Aubagio)?
Hint: other than liver enzymes and a pregnancy test
Tuberculosis!!
How can we pretreat a patient using Alemtuzumab (Lemtrada) for MS in order to prevent infusion associated reactions?
Tylenol, Benadryl, or corticosteroids
Which class of medications can be used for nausea/vomiting due to a migraine, but are very sedating?
Phenothiazines
(Promethazine, Metoclopramide, Prochlorperazine)
For mild/moderate migraines, what kinds of treatment should we use?
NSAIDS and simple analgesics
How can ergots treat moderate/severe migraines?
activates 5HT1D/1B receptors to vasoconstrict vessels
Which major side effect can occur from using ergots for migraines?
Ergotism
--> peripheral ischemia, cold extremities, paresthesias
What major contraindications are associated with using Ergots for migraines?
Coronary dx, hypertension, renal failure, and PREGNANCY
How long should we wait before taking ergots if we were taking triptans for migraines in the past?
24 hours (can cause vasospasms)
Can we give a patient with coronary artery dx triptans for their severe headache?
absolutely not
What is our gold standard first line triptan that we use in order to treat a moderate to severe migraine?
Sumatriptan (Imitrex)
Which triptans can we use to lower the recurrence and have a long half-life?
What is the downside?
Naratriptan (Amerge) and Frovatriptan (Frova)
--> The onset of action is very long (up to 4 hours)
Which notable triptan drug has an interaction with propranolol?
Rizatriptan (Maxalt)
Which triptan could we use if our patient cant tolerate sumatriptan and is considered the next best option?
Almotriptan (Axert)
If we have a patient who has HTN and angina symptoms, but has a severe headache. Which medications could we consider giving them?
Lasmiditan (Reyvow)
CGRP antagonists (gepants)
When would we absolutely taper off analgesic medication for those experiencing medication overuse headaches?
Those who have been taking the medication >12 days and for those who are pregnant
If a patient wants to prevent migraines but they also have asthma? what kind of medication should we prescribe them?
HINT: he said this will be a test question most likely
low dose selective beta blockers like atenolol
What kind of therapy would be best for a 18 year old kid who is currently on his way to a state baseball championship this year and wants to prevent his migraines that he has been experiencing?
Anticonvulsants such as topiramate or valproic acid
NOTE: topiramate can inhibit concentration so he'll stink at math
What kind of therapy would be best for a woman who is pregnant and cannot use beta blockers but wants to prevent migraines from happening?
Calcium channel blockers such as verapamil
Which medication is the ONLY one that can treat and prevent migraines?
HINT: going to be a test question, know it!
Rimegepant (Nurtec)
What is the drug of choice for migraines during pregnancy?
Acetaminophen
What is the best prophylactic therapy for cluster headaches?
Verapamil (calcium channel blocker)
Will gastric emptying time be faster or slower in infants less than 6 months of age?
Faster
Do we see alot of extended release drugs being used in pediatrics?
No, because their gastric emptying time is increased and so the drug will be excreted rapidly
How do neonates and infants differ from older kids and adults as far as blood flow to muscles and percent of water in the muscles?
Neonates and Infants have decreased blood flow and increased percent of water in the muscles
Do neonates/infants have good rectal absorption?
yes
What type of route should we use for medicine in neonates for emergent situations?
Intraosseous (IO)
What is the concern with using topical/patch drugs on neonates and infants?
Toxicity due to an underdeveloped stratum corneum
How does an increased amount of body water content (as seen in infants) affect the volume of distribution for hydrophilic medications?
Increases the volume of distribution for hydrophilic meds
If we have a higher amount of volume of distribution for hydrophilic meds, what do we need to do to adjust the dosing concentration on medications?
Increase the dose concentration
Can infants tolerate acetaminophen better than adults?
Yes!
For infants receiving aminoglycosides such as gentamicin, the half life is much longer than adults, how would this affect the way we do our dosing interval?
the dosing interval will be much longer
--> example: adult gets meds every 8 hours
Kid gets meds every 24 hours