Exam 2 Review sheet Flashcards
Antiepileptics
Hydantoins Succinimides Barbiturates Adjunct Therapy Benzodiazepines
Hydrantoins Prototype
phenytoin (Dilantin)
Other drugs in the same class as phenytoin (Dliantin)
ethotoin
fosphenytoin
mephytoin
Indications for phenytoin (Dilantin)
Treats tonic-chronic (grand-mal) & complete-partial seizures
Mechanism of action of phenytoin (Dilantin)
- enhancement of GABA
- inhibition of glutamate
- prolonging inactiveation period of Na Channels (Slows channels down)
- inactivation of Ca channels
Absorption of phenytoin (Dilantin)
slow with PO and IM
Distribution of phenytoin (Dliantin)
Highly protein bound
T1/2 increases as dose increases
Low dose = 6-24 hours T 1/2
Thera peutic dose = 20-60 hr T 1/2
Metabolism of phenytoin (Dilantin)
Liver
Elimination of phenytoin (Dilantin)
Kidney
Therapeutic level of phenytoin (Dilantin)
10-20 mcg/mL (narrow therapeutic range)
Steady state at 7-10 days
Drug interactions with phenytoin (Dilantin)
CYP450 inducer = increase metabolism of other meds
Adverse effects of phenytoin (Dilantin)
CNS: dizziness, ataxia, blurred vision, slurred speech, tremor, confusion
Nausea
gingival hyperplasia
derm reaction (infiltrate steven johnson syndrome)
Liver damage
CV collapse (IVP slow)
hypotension
Contraindications of phenytoin (Dilantin)
CV: sinus bradycardia, sinoatrial block, 2nd and 3rd degree heart block
DM: Increase blood sugars
PG: class D
co-admin with tube feedings (Increase protein levels)
ETOH use & other drug interactions
Education of phenytoin (Dilantin)
Do not stop suddenly (will cause seizures)
Monitor levels (small change in dose = large change in serum level
must shake thoroughly
Good dental hygiene
take with food
DM: Check blood sugar
May decrease effectiveness of birth control
True or false: Always dilute in NS
True
True or false: Compatible w/ D5W (will cause precipitate)
False: NOT compatible with D5W
True or false: Can increase BS
True
What is the prototype of Succinimides?
ethosuximide (Zarontin)
Indications for ethosuximide (Zarontin)
Treat absence (petite mal seizures)
Mechanism of action of ethosuximide (Zarontin)
Delays influx of Ca ions
1 week to see results
Absorption of ethosuximde (Zarontin)
Only oral admin
Distribution of ethosuximide (Zarontin)
Peak: 3-7 hours
Half life: 30-60 hours
Metabolism of ethosuximide (Zarontin)
Liver
Elimination of ethosuximide (Zarontin)
Kidneys
Drug interactions with ethosuximide (Zarontin)
interacts with some other anti-epileptic drugs
Adverse effect of ethosuximide (Zarontin)
Increased suicidal thoughts Drowsiness lethargy nausea blood dyscrasias rash, joint pain, fever, sore throat, blurred vision, PG Unusual bleeding or bruising Notify MD
What is dyscrasias?
Any disease condition, especially in hematology, as in “blood dyscrasias.” The term “dyscrasia” was borrowed from the Greek meaning “a bad mixture” referring to the ancient belief that an imbalance between the four humors - blood, phlegm, yellow bile, and black bile- which caused disease.
Education of ethosuximide (Zarontin)
Monitor levels at the start and when changing doses Assess CBC, UA, and LFT Taper gradually to discontinue Take with milk or food if GI upset Use birth control beyond the pill Urine may change color (pinkish) NO ETOH due to drowsiness
Drug prototype for barbituates
phenobarbital
Indications for phenobarbital
Last resort for extended seizures
Tonic clonic and focus seizure treatment
Mechanism of Action of phenobarbital
Stimulates GABA receptors
What is GABA again??
Gamma-Amino Butyric acid (GABA) is an amino acid which acts as a neurotransmitter in the central nervous system. It inhibits nerve transmission in the brain, calming nervous activity
Therapeutic level of phenobarbital
20-40 mcg/mL (narrow therapeutic range)
Drug interaction with phenobarbital
Interacts with many different drugs
Adverse effects of phenobarbital
CNS, respiratory depressant
Sedation
Increased potential for abuse/addiction
Increase tolerance (sedative) with/LT use and dependence
Contraindications with phenobarbital
PG: Class D
Education for phenobarbital
Wean slowly
True or false: phenobarbital is used mostly after other seizure meds have failed
True
Drug prototype for Adjunct therapy
levetiracetam (Keppra)
Indications for use of levetiracetam (Keppra)
Used more now as primary drug for seizure treatment than Dilantin due to less side effects
Mechanism of action of levetiracetam (Keppra)
Unknown
Metabolism of levetiracetam (Keppra)
1/3 in liver (ok for liver patients)
Elimination of levetiracetam (Keppra)
Kidneys (unchanged)
Drug interactions with levetiracetam (Keppra)
no significant
Adverse effects with levetiracetam (Keppra)
Drowsiness, dizziness, headache, infection
Education for levetiracetam (Keppra)
- caution d/t ↑ accidental injuries
- PEDS = ↑ behavioral changes (nervous, hostile, agitated, depressed)
Prototype for Benzodiazepines
lorazepam
Other drugs in the same class as lorazepam
clonazepam
diazepam
midazolam
carbamazepine (Tegretol)
- partial seizure tx
- off label uses for psych disorders
- Decrease sodium into cells
- Do not give with other drugs
- Black box warning - anemia
- IVP = Steven Johnson syndrome (Asians)
valproic acids (Depakote)
- most used world wide
- block influx of sodium and stim GABA
- hard on liver (monitor LFT’s)
- caution with PEDS
- off-label use for psych (migraines)
gabapentin (Neurontin)
- originally neuropathy treatment
- used in PEDS for seizure tx
- unknown MOA
- Not metabolized in liver (ok for liver patients)
- No drug interactions
Anxiety/Sleep meds
Benzodiazepines Barbituates Non-Benzodiazepam hypnotic Melatonin receptor agonist Hypnotic
What is the prototype for Benzodiazepine as an anxiety/sleep med?
lorazepam (Ativan)
Other drugs in the same class as lorazepam (Ativan) that are considered anxiety/sleep meds?
alprazolam (Xanax) chlordiazepoxide (Librium) chlorazepate (Traxene) diazepam (Valium) midazolam (Versed)
Hypnotic drugs that are under the same class as lorazepam (Ativan)?
flurazepam (Dalmane)
temazepam (Restoril)
triazolam (Halcion)
Indications for use of lorazepam (Ativan)
anxiety sleep antiepileptic ETOH withdrawl induction of gen. antesthesia pre-op sedation continuous sedation
Mechanism of action lorazepam (Ativan)
bind to BZ1 (sleep) and BZ2 (memory, motor, sensory, cognitive) receptors
Increase effects of GABA
Distribution of lorazepam (Ativan)
highly protein bound
Onset: fast/medium
Absorption of lorazepam (Ativan)
easliy absorbed from GI tract
some readily absorbed when given IM
Metabolism of lorazepam (Ativan)
Liver
lorazepam and oxazepam metab to inactive substances (ok for liver patients)
Excretion of lorazepam (Ativan)
Kidneys
Contraindications of lorazepam (Ativan)
Resp depression or with other CNS depressants acute angle glaucoma psychoses ETOH, narcotics, barbituates PG: Class X
Adverse effects of lorazepam (Ativan)
well tolerated
mild drowsiness
ataxia and confusion (esp elderly)
rare: CNS depression
Education with lorazepam (Ativan)
do not stop abruptly (esp for seizure management)
elderly may need half dose due to toxicity
Other drugs in the same class at phenobarbital used for anxiety/sleep meds
chloral hydrate mephobarbital phenobarbital secobarbital tuinal thiopental
Adverse effects of phenobarbital
low safety CNS depressant resp depressant suicidal potential physical dependence tolerance abuse potential induce hepatic drug metabolism
What is the prototype of a barbituate?
phenobarbital
What is the prototype of a non-benzodiazepam hypnotic?
eszopiclone (Lunesta)
Indications for use of eszopiclone (Lunesta)
induce sleep
ok for LT use
Mechanism of action of eszopiclone (Lunesta)
induces sleep quickly
prevents waking up in the middle of the night
Distribution of eszopiclone (Lunesta)
long half life
rapid onset: 1 hr
Adverse effects of eszopiclone (Lunesta)
AM headache
Prolonged drowsiness
Bitter aftertaste
What is the prototype for Melatonin receptor agonist
ramelteon (Rozerem)
Indications for ramelteon (Rozerem)
Induces sleep
Mechanism of action of ramelteon (Rozerem)
high affinity for melatonin receptors
no effect on GABA
Contraindications for ramelteon (Rozerem)
Pregnancy: Category X
Education of ramelteon (Rozerem)
No risk of abuse or tolerance
True or false: ramelteon (Rozerem) is a controlled substance?
False: It is not a controlled substance
What is the prototype for Hypnotics?
zolpidem (Ambien)
Indications for use of zolpidem (Ambien)
Insomnia
Short term use: 7-10 days only
Adverse effects of zolpidem (Ambiem)
Tolerance possible
Education on zolpidem (Ambiem)
no residual effects next day
no insomnia rebound effects when discontinued