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192 Cards in this Set

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2 oxy barbs?
secobarbital
pentobarbital
methylated barb?
methohexital (brevital)
methohexital metabolism?
demethylation and oxidation at carbon-5 and ring hydrolysis occurs
barbs synthesized how?
by condensation of urea and malonic acid to form barbituric acid ring
thiopental is first metabolized to? then?
desulfuration to pentobarbital (hangover effect), then oxidation of carbon-5 radicals (ring hydrolysis also occurs)
no brevital with hx of?
seizures
what change gives the barbs a sedative hypnotic effect?
by replacing both hydrogen atoms at position 5 with alkyl or aryl group
what alterations give barbs increased potency?
longer side chain lengths
what # carbon for thio or oxy barbs?
replacementg of carbon 2 with sulfer or oxygen
what structural changes give barbs increased lipid solubility
sulfurization
methohexital is produced by?
methylation of phenobarbital at carbon-1
what changes give barbs a more rapid onset and shorer duration? (but also increased excitatory side effects)
methylation (methohexital)
barbs are weak ______?
acids
NMDA non-competitive antagonist?
ketamine
Structural similarities to phencyclidine?
ketamine
Ketamine lipid solubility?
more lipid soluble than thiopental (5 to 10 times)
Structure has imidazole,gives H2O solubility?
etomidate
Structure is alkylated phenol, insoluble in H2O?
propofol
Fentanyl and alfentanil increase concentrationon what agent?
propofol
which agent inhibits cortisol and aldosterol synthesis?
etomidate
barbiturate with incidence of hiccups and coughing?
methohexital
_______ compounds cause release of histamine from mast cells.
Thiol
Hyperanalgesic, increase reaction to painful stimuli at subanesthetic doses?
barbiturates
most lipophilic barbiturate?

which means that it distributes the _________?
secobarbital

fastest
least lipophilic barbiturate?


which means that it distributes the _________?
phenobarbital

slowest
barbiturates whose onset parallels the rate of absorption and duration parallels elimination.
Oxybarbiturates (secobarb, phenobarb)
barbiturates whose onset and duration are more closely related to the pattern of distribution.
Thiobarbiturates (thiopental)
barbiturates with 100% P450 Metabolism? (4)
Amobarbital
Butabarbital
Pentobarbital
Secobarbital
the more lipophilic a drug the higher/lower the rate of renal reaborption?
more lipophilic = more reabsorbed
only barbiturate that has any significant excretion without being unchanged?
Phenobarbital
barbiturates compared to benzodiazepines? [2]
more addicitve (intoxicated side effects)
smaller TI
ph of lipophilic midalolam form?
physiologic ph
benzodiazepines effect on adesosine receptor?
Agonist activity=increases effect because inhibits uptake of adenosine.
percent protien bound?

propofol
98
percent protien bound?

etomidate
75
percent protien bound?

ketamine
12
percent protien bound?

thiopental
80-85
percent protien bound?

methohexital
85
percent protien bound?

midazolam
94
percent protien bound?

diazepam
98
percent protien bound?

lorazepam
98
elimination t 1/2

thiopental
10-12 hr
elimination t 1/2

methohexital
2-4 hr
elimination t 1/2

etomidate
2-5 hr
elimination t 1/2

propofol
1-5 hr
elimination t 1/2

ketamine
2-3 hr
elimination t 1/2

midazolam
2-4 hr
elimination t 1/2

diazepam
20-50 hr
elimination t 1/2

lorazepam
10-20 hr
highest clearance-non barb
propofol
lowest clearance non barb
ketamine
highest clearance barb
methohexital
highest clearance benzo
midazolam
lowest clearance benzo
diazepam
highest HR increase barb
methohexital
most decrease in SVR barb
thiopental
highest HR incrase non barb
ketamine
most BP decrease of all IV agents?
propofol (decrease SVR)
most respiratory depressant?
propofol
what does etomidate decrease?
RR
HR -propofol?
no change or decreased
CBF with midazolam?
increase or decrease
how do NSAIDs work in general?
they inhibit formation of
algogenic substances
how do opiods work in general?
they inhibit neurotransmission of pain signals
Phenanthrenes?
OPIODS
Benzylisoquinolines?
Benzodiazepines
the 3 STRONG PO opiods?
Methadone (Dolophine)
Hydromorphone (Dilaudid)
Oxycodone (OxyContin) strongest
methadone uses...

metab/solubility?

strength?
analgesia and addiction

not used for anesthesia

slow metabolism, high lipid solubility, t1/2 24-36 hours

STRONG
Hydromorphone strength?

dangers?

structure?
STRONG 8x MS

death with ETOH (facilitates absortption)

Hydrogenated ketone
Oxycodone (OxyContin) atregnth?

Why so desired?
STRONGEST

Oxycontin is SR

high bioavialibility via a number of routes
What are the 4 moderate PO opiods?
Codeine
Hydrocodone(Vicodin, Lorcet, Lortab,etc.)
Propoxyphene (Darvon, Darvocet)
Oxymorphone
Codeine strength?

dangers?

pro-drug of?
moderate

histamine release

morphine-demethylation
Hydrocodone strength?

special considerations?
moderate

NO MAOs
Propoxyphene strength?

special considerations?
moderate

can be used for withdrawal
low TI and efficacy
can be used and a local anesthetic
extensive 1st pass/toxic metabolites

does not use an opiod receptor
Oxymorphone strength?

special considerations?
moderate

OH grp added to hydromorphone

the 'blues'
Tramadol strength?

special considerations?
weak-10 time weaker than morphine

not related in structure to other opiods
can interact with coumadin/SSRI's(potentiate)
can cause sz'z
Loperamide strength?

special considerations?
weak

for diarrhea
diphenoxlate? (Lomotil) strength?

special considerations?
weak

for diarrhea
with atropine
dextromethorphan strength?

special considerations?
weak

antitussive
How do the opioid agonist-antagonists work?
Lack complete agonist effect at mu receptors so less respiratory depression and lower chance fro drug dependence than the complete opioid agonists. Also less constipation
side effects of opiod agonist/antagonist?
Side effects are anxiety, nightmares, psychotomimetic effects such as hallucinations because of kappa agonist activity. If patient is on a full agonist, can cause withdrawal.
4 opioid agonist-antagonists?
Pentazocine (Talwin)
Nalbuphin (Nubaine)
Butorphanol (Butorfanol)
Buprenorphrine (Buprenex)
Pentazocine (Talwin)?

special considerations?
opiod agonist/antagonist

Kappa and sigma receptor agonist
Supplement to anesthesia
Paraenteral use can cause severe condiopulmonary reactions
Butorphanol (Butorfanol)

special considerations?
opiod agonist/antagonist

Kappa receptor agonist
Partial agonist/antagonist at mu receptor
Paraenteral
Supplement to anesthesia
Relief of pain during labor
Nalbuphine (Nubain)

special considerations?
opiod agonist/antagonist

Kappa receptor agonist
Partial agonist/antagonist at mu receptor
Paraenteral
Supplement to anesthesia
Nalorphine (not used)special considerations?
opiod agonist/antagonist

has analgesic properties, antagonist activity is that it displaces opioid agonists – precipitates withdrawal
high incidence of dysphoria
impending death which is probably sigma agonism)
Buprenorphine(Buprenex)

special considerations?
opiod agonist/antagonist

Partial mu agonist
Slow dissociation so longer activng
IM, IV, oral sublingual
Approved for treatment of opioid dependence
Formulated with Naloxone to lower abuse
2 opioid antagonists
naloxone

naltrexone (cepulan)
naloxone considerations?
IV for rapid termination of opioid respiratory depression (poor oral bioavailability
Short half-life
May need repeated dosing
naltrexone considerations?
Oral and transdermal
High oral bioavailability
Can be used long term
Also for alcohol dependence
duration of action depends on? [3}
lipophilicity

volume of destribution

metabolism clearance
what 2 agents have some degree of extra-hepatic metabolism?
etomidate
propofol
what 2 agents can cause enzyme induction?

what does this cause?
ketamine
barbiturates

increased metabolism
how does a large Vd affect elimination?
it prolongs it
if drug-drug interactions occur in the liver, what is the effect?
usually slows metabolism of the drug you are giving or slows the metabolism of other drugs. There is competition for the enzymes. This can produce prolonged drug effects of the main drug of interest usually
a steep slope on the dose-response curve indicates what?
high potency
all barbiturates have a _______ TI.
low
With barbiturates, the R3 position has N and can be substituted. T/F
True
a low TI has what type of curve?
steep curve
isomerism is at postion #?
1 for brevital plus #5 for all of the others.
With Barb's, N can be substituted at position #?
3
Glutamate receptors are inhibitory or excitatory?
excitatory
How do we inhibit the glutamate receptor?
steric hindrance....we keep the Na+ from coming in
Do we want agonism or antagosism of the glutamate receptor?
antagonism
What does serotonin do?
promotes sleepiness
Do we want antagonism or agonism of the adenosine receptor?
we wnat agonism-we inhibit the uptake of adenosine
What does caffiene do?
it is an adenosine pathway antagonist
How do barbiturate act on the nicotinic cholinergic (ionotropic) receptor?
the lodge in the pore (steric hindrance) to keep the Na+ out.
What receptors do the barbiturates antagonize?
Ach
Nicotinic
muscarinic
barbs with 100% p450 metabolism
amobarbital
butabarbital
secobarbital
barbs with 75% p450 metabolism
phenobarbita
pentobarbital
barbiturate induction of microsomal enzymes (liver) leads to high clearance of what other drugs?
TCAs
ICS
coumadin
estrogen/progesterone
digoxin
what interaction with MAO's?
inhibit p450
benzo?
7 figured ring?
diaza?
benzine ring
-epine
2 nitrogens
triazo groups are more?
more potent, less metabolized
Adenosine receptors contribute to?

do we want antag/agonism?
sleepiness

agonize
benzo's work on what GABA subunit?
gamma
lowest Vd benzo?
lorazepam
why do we use propylen glycol as a solvent?
slight h20 solubility secondary to OH groups
brings drug into solution
onset depends on distribution to__________ which is dependent on ____________.
brain

lipophilic character
benzo drug-drug interactions that slow metabolism (Cyp3A)
cimetidine
e-mycin,antifungals
Ca+ channel blockers
fentanil
grapefruit juice
benzo with only phase 2?
lorazepam
benzo that undergoes phase once twice?
diazepam
benzo with no phase 2?
midazolam
benzo with active metabolite?
diazepam
benzo where elimination does paralled duration?
diazepam d/t active metabolites
elimination/duration is ussally _______ with drugs with INactive metabolites?
paired/parrallel
benzo same site antagonist?
flumazenil
benzo different site antagonist?
physostigmine/aminophyline
benzo antagonist that is a CNS stimulant?
physostigmine/aminophyline
benzo metabolized solely by conjugation?
lorazepam
Ketamine Pka?

therefore?
7.5

50/50 ionized at phys pH.
never mix ketamine with a ?
base
Ketamine suppresses neutrophi production of inflammatory mediators which does what?
improves blood flow
inhibits cytokines
ketamine is formulated at a pH of 3-5, why?
acidic to form a water soluble salt/conjugate acid form.
ketamine is a NMDA?
non-competitive antagosist

poss opiod (kappa)
ketamine hepatic Cl, ER?
high, high
ketamine metabolite activity?
some active, some not
ketamine metabolism?
dealkylation
ketamine S/A's
sympathetic stim
nystagmus
hypertonus
increased AW secretions
no ketamine with?
theophylline
ketamine effects on librium?
increased duration
diazepam effect on ketamine?
increased CV stimulation and increased elim t1/2
No ketamine with what patient?
HTN, CAD, CHF, aneurysms
increased ICP
glaucoma
Etomidate acid/base? pKa?
weakly basic
4.2
Etomidate formulation?
pH 7. base in base
highly non-ionized
etomidate GABA effect?
modulator only

GABA must be present
Etomidate GABAa subunit receptor?
alpha, increases affinity for GABA ligand
Etomidate mech of action?
depresses RAS
rational for Etomidate myoclonus?
disinhibition of extrapyramidal motor activity
Etomidate ionization?

protien binding?
highly non-ionized

75% bound
Etomidate context sensitive 1/2 time versus thiopental?
etomidate has shorter 1/2 life
Etomidate S/A's
N/V
adrenocortical suppresion
immune depression (decrese stress response)
fentanil/alfentanil effects of etomidate?
increase plasma levels and decrease elim t1/2
opiod effects on etomidate?
decrese myoclonus
propofol structure?
alkylated phenol
propofol mech of action?
GABA modulator

decreases the rate of release of GABA
propofol++'s
antiemetic
anticonvulsant
antipruritic
propofol Vd?
LARGE (lungs, too)
Propofol hepatic metab?
clearance exceeds hepatic blood flow.

has a weak metabolite
propofol HR response
impairs baroreflexes

ussually no change in HR
Vd effect on propofol dosing?
increased dosage needed with lower Vd (elderly, neonates)

increased dosage for women
fentanil/alfentanil effect on propofol?
they increase serum concentration
Ketamine may result in decreased CO and MAP if.....
cathecholimine stores are exhausted
drugs that increase HR?
barbs
benzo's(possibly)
meperidine
ketamine
droperidol
drugs that decrease HR?
opiods except meperidine
drugs that decrease BP/MAP?
barbs
benzos(depends)
opiods (a little)
etomidate (a little)
propofol the most
inactivated barbs don't have ______?
carbon chains at the 5th position
What change in barb SAR leads to a more rapid onset and shorter duration?
sulfer-incrased lipophilicity
2 5-sustituents required for _______
GABA activity with barbs
barbs are acid/base?
acidic secondary to amide group
hypnotic activity is increased with what barb SAR change?
side chains at postion 5, especially if branched
barb acid+acid='s
non-ionized
lipophilic
fast absrption
if the patient becomes more acidotic, how does this affect the ionization with barbs?
more unionized=more drug available
muscarinic receptors are?

where?
Ach g-coupled

only parasympathetic at the effector organ
antimuscarinics? [2]
atropine
scoplamine
barbiturates at pharmacologic concentrations allosterically increase binding of _________ to thier respective binding sites.
benzodiazepines
pain causing substances? [2]
interluekins
prostaglandins
which Cox activity for analgesia?
cox-2 (we inhibit)
# rings-phenanthrine?
3-morphine
the 'coming out' ring on a phenanthrine?
piperdine ring
benzoisoquinolones?
fentanil
sufenanil
remifentanil
alfentanil
methadone solubility, metabolism rate?
high lipid solubility
slow metabolism
not as potent as MS
not a phenanthrine
oxycodone++'s
selective for Mu
high bioavailability
CYP2D6 deficiency?
incrased codiene-toxicity
cannot be mixed with MAO's
hydrocodone

vicodin, lortab
unique property of propoxyphene?
can be used as a local
does not use an opiod receptor
PO med that does not ustilize an opiod receptor\?
propoxyphene
propoxyphene negatives
addicitive
low TI
extensive 1st pass effect
toxic byproducts
Tramodol's unique mech of action?
descending pathway (serotonin)

inhibit the uptake of nor-epi
stadol is?
butrophanol
buprenophine specifically approved for?
treatment of opiod dependence