Exam Three Flashcards
What is GHB metabolized to?
GABA
Which two benzoes yield inactive, water-soluble glucoronide metabolites?
Lorazepam and oxazepam
What drug is used to treat an OD of benzodiazepines?
flumazenil
Which benzo is an antispasmodic?
Diazepam
What is the exact MOA of benzodiazepines?
increase frequency of chloride channel opening of GABA-A receptor
What two subunits of the GABA receptor do benzodiazepines bind?
alpha1
gamma2
What effects do the α1 subunits of the GABA receptor mediate?
sedation/amnesia/ataxic
Which two benzos are weakly active and short lived?
Alprazolam and triazolam
Which two benzodiazepines undergo Phase I metabolism that yields two relatively long-lasting metabolic products?
diazepam and flurazepam
Which two benzos kinetics are not influenced by age? Which benzo is influenced by age?
lorazepam and oxazepam
diazepam
Flumazenil may induce seizures in patients taking what other three drugs?
TCA
alcohol
barbiturates
What are the two newer benzodiazepine hypnotics?
Eszopiclone
Zolpidem
The newer benzodiazepines used for sleep only interact with what subunit of the GABA receptor?
α1
What CYP enzyme metabolizes the newer benzodiazepines?
3A4
Name three barbiturates. What are their functions?
Pentobarbital = medically induced coma
Phenobarbital = anti-convulsant
Thiopental = anesthesia
What is the difference between benzos and barbs regarding their metabolsim?
barbs dont have active metabolites
Are barbiturates weak acids or weak bases?
weak acids
What is the specific MOA of barbiturates?
increases open time of GABA chloride channel
What is the function of MT1?
sleep onset
What is the melatonin receptor agonist?
Ramelteon
What is the function of MT2?
circadian pattern
Where in the brain does Ramelteon work?
suprachiasmatic nuclei
What two CYP enzymes degrade Ramelteon?
2C9
1A2
Does Ramelteon produce dependence?
no
What is the 5HT agonist Anxiolytic? Which specific isoform? Agonist or antagonist?
Buspirone
5HT1A
agonist
What is an advantage of buspirone compared to benzodiazepines for treating anxiety?
Buspirone is only an anxiolytic
Which specific serotnin receptor isoform is Buspirone known to activate? What does activation of this receptor do to serotonin release?
5HT1A
decrease serotonin release
What are the two anti-histamine hypnotics?
diphenhydramine and hydroxyzine
Does Buspirone potentiate the effects of other CNS depressants?
no
What is the function of BDNF? What disease state can a decrease in BDNF be seen?
promote neural growth and survival
depression
What is the main adverse effect of 5HTreuptake blockade?
GI disturbances
What are the two non-selective MAO-A and MAO-B inhibitors? Reversible or irreversible?
phenelzine and Tranylcypromine
irreversible
What is the selective MAO-B inhibitor? What disease is treated at low dose? What disease is treated by high dose?
Selegiline
LOW = parkinsons
high = depression
What does MAO-A degrade?
serotonin
norepinephrine
dopamine
What does MAO-B degrade?
dopamine
Which MAO is preferentially used to treat Parkinsons?
Selegiline
What are the three tricyclics?
Imipramine
Amitriptyline
Desipramine
What two compounds does Imipramine inhibit the reuptake of?
5HT and NE
Why can TCAs cause lethal cardic arrhythmias?
blockade of sodium and calcium channels
Withdrawl of what drug can cause Discontinuation Syndrome?
SSRIs
What are the two main symptoms of Discontinuation Syndrome?
dizziness and paresthesias
What two compounds do the SNRIs inhibit the re-uptake of?
5HT and NE
What is a non-depressive symptom that SNRIs are used to treat?
chronic pain
What is the main 5HT2 antagonist? Which other receptor can trazodone block?
Trazodone
H1
What is the most common use for trazodone?
insomnia
What two compounds does Bupropion inhibit the re-uptake of? What is bupropion used to treat?
DA and NE
smoking cessation
What receptor does Mirtazapine block?
α2 antagonist
What two compounds Mirtazapine increase the release of?
5HT and NE
Other than α2, what three receptors can Mirtazapine block?
5HT2 and 5HT3 and H1
What is the treatment of choice for Bipolar disorder?
Lithium
What severe condition are valproic acid and carbamazepine used to treat?
acute mania
What is the most common side effect of lithium?
tremor
Other than tremor, what are three side effects of lithium?
nephrogenic diabetis insipidus
hypothyroidism
skin issues
What two drugs are contraindicated in lithium use? Why?
loop and thiazide
increase lithium absorption
Where in the kidney is the primary site of lithium absorption?
PCT
What is the most common site for the origination of a seizure?
temporal lobe
What are the two MOAs of valproic acid?
blocks GABA transaminase
blocks Na+ channels
What is the MOA of vigabatrin?
blocks GABA-transaminase
What are the two MOAs of gabapentin?
block L-type
increase GABA release
What is the MOA of tiagabine?
blocks GABA re-uptake
What drug do most anti-seizure drugs interfere with the synthesis of? Why?
oral contraceptives
induction of p450
What neurotransmitter can phenytoin enhance the release of?
GABA
What are the two main side effects of phenytoin?
nystagmus
gingival hyperplasia
Why can phenytoin cause anemic issues?
decreases folate levels
What is the drug of choice for trigeminal neuralgia?
carbamazepine
What are the two major side effects of carbamazepine?
leukopenia
SIADH
What is the drug of choice for seizures in infants?
phenobarbital
Other than treating seizures in infants, what condition is phenobarbital used to treat?
status epilepticus
Primodine is similar to what drug? What does primodine get converted into?
phenytoin
phenobarbital
What is the drug of choice for petit mal seizures? What patient population are petit mal seizures most often seen?
ethosuximide
children
What are the two MOAs of valproic acid?
inhibits Ca2+ influx
blocks GABA-T
What type of seizure is valproic acid used to treat?
petit mal
According to Duric, what are the two toxicities of valproic acid?
hepatotoxic
teratogenic
What is the preferred initial drug for status epilepticus?
Diazepam
What are the two MOAs of lamotrigine?
block Na+ and Ca2+ channels
What specific antiseizure drug does Duric say can cause Steven-Johnson Syndrome?
Lamotrigine
What is the MOA of tigabine?
block reuptake of GABA
What are the two MOAs of topiramate?
block AMPA
What is the MOA of baclophen?
GABA-B agonist
What is the BG Coefficient?
a measure of a drugs solubility in blood
What is anesthetic potentcy correlated to?
fat solubility
Will increased cardiac output increase or decrease the induction of anesthesia?
decrease
What is the MAC?
[anethetic] in the inspired air at equilibrium when 50% of patients do not sense noxious stimuli
What is the most adverse side effect of halothane during anesthesia?
malignant hyperthermia
What is the most adverse side effect of halothane during postop?
hepatitis
What is the most adverse effect of enflurane?
CNS induced seizuring
What are the two constituents of the diencephalon?
thalamus and hypothalamus
What are the three monoamines in the brain?
NE, 5HT, dopamine
Which benzo can be used as a date drug? Why?
flunitrazepam
induction of amnesia
Is selegilie reversible or irreversible?
irreversible
What condition is high dose selegiline used to treat?
depression
What are the two main side effects of all MAOIs? Antagonization of which receptor mediates these effects?
orthostatic hypotension and weight gain
H1
Which class of drug can be used to treat neuropathic pain?
TCAs
What two transporters do TCAs block?
SERT and NET
What three receptors can TCAs directly antagonize?
cholineric, histaminergic and α-adrenergic
What is Imipramine used to treat? Why?
enuresis
Imipramine is anti-cholinergic
What is the result of TCAs antagonizing cholinergic receptors?
GI issues
What is the result of TCAs antagonizing histamine receptors?
sedation
What is the result of TCAs antagonizing α1-adrenergic receptors?
orthostatic hypotension
What can TCAs produce in elderly patients?
delirium
What ion channels can TCAs effect? What can this lead to?
Na/K ATPase
arrhythmias
What are the three C’s of TCAs?
coma
convulsion
cardiac arrhythmias
What is the short term side effect of SSRIs?
GI disturbances
What is the long-term effect of SSRIs?
sexual dysfunction
Which SSRI is most likely to produce Serotonin Syndrome?
Fluoxetine
What are the two SNRIs?
venlafaxine and duloxetine
What other drug is the side effect profile of SNRIs similar to? What is the difference
TCAs
not as severe
What is the side effect profile of 5HT2?
GI disturbances
Which two classes of anti-depressants should never be combined?
TCAs and SSRI
Which two drugs can be added to lithium to treat Bipolar Disorder?
valproic acid
carbamazepine
Which lobe of the brain is most susceptible to developing a seizure?
temporal lobe
What three drugs are used for partial seizures?
Carbamazepine, Phenytoin, Valproate
What three drugs are used to treat tonic clonic seizures?
carbamazepine, phenytoin, valproate
What two drugs are used to treat Petit Mal seizures?
Ethosuximide and valproate
What two drugs are used to treat myoclonic seizures?
Clonazepam and valproate
What four drugs are used to treat status epilepticus?
lorazepam, diazepam, phenytoin, fosphenytoin
Which anti-epileptic is considered safest during pregnancy?
Phenobarbital
What is the difference between phenytoin and fosphenytoin?
fosphenytoin is more water soluble
Which antiepileptic possesses zero order elimination kinetics?
Phenytoin
What neurotransmitter does phenytoin promote the secretion of? Decrease the release of?
GABA
glutamate
What are the CNS defects in phenytoin?
ataxia and nystagmus
Which anti-epileptic is a teratogen?
Phenytoin
What are the two MOAs of carbamazepine?
sodium channel blocker
GABA receptor agonist
What is the new metabolite of carbamazepine?
Oxacarbazepine
What is the drug of choice for trigeminal neuralgia?
carbamazepine
What drug can cause SIADH?
carbamazepine
What three drugs can carbamazepine have potential interactions with?
Phenytoin,
valproate
phenobarbital
What drug is metabolized into phenobarbital?
Primidone