21 Fall Pharm Final Oral Flashcards
Desflurane VP
669mmHg
Desflurane MAC
6%
Desflurane B:G
0.42
Desflurane O:G
19
volatile agents MOA
Unknown – likely involves NMDA receptors, tandem pore K+ channels, VG-Na+ channels, glycine receptors, and GABA receptors in the cerebral cortex, brain stem arousal centers, central thalamus, and spinal cord.
Isoflurane MAC
1.2%
Isoflurane VP
238mmHg
Isoflurane B:G
1.4
Isoflurane O:G
91
Sevoflurane MAC
2%
Sevoflurane B:G
0.68
sevolurane O:G
50
sevoflurane VP
157mmHg
Nitrous Oxide MAC
104%
Nitrous Oxide O:G
1.4
Nitrous Oxide B:G
0.47
Nitrous Oxide VP
38770
What is the MOA of magnesium?
Mag works in opposite direction of calcium, calcium excites, mag inhibits
The 3As in anesthesia and which location in the brain.
amnesia (brainstem), analgesia (thalamus), and areflexia (spinal cord) (no SNS/PSNS changes in V/S)
How to treat MH?
Na+ dantrolene 1.5 mg/kg or Ryanodex
Stages of anesthesia
Stage I – Amnesia & Anesthesia
Stage II – Delirium & Excitation
Stage III – Surgical Anesthesia
Stage IV – Anesthetic overdose
In what population should you avoid using desflurane?
Stinky bad boy!!! Avoid in patients with reactive airway disease
Which inhalational agent is best for inhalational induction
Sevoflurane
What complication can sevoflurane produce? How to mitigate? Surgery implication?
If used with Lyme, can create nephrotoxic compound A. Use lime can reduce risk. Give flow >2lpm
What is this?

desflurane
What is this

isoflurane
what is this?

Sevoflurane
Wha is special about Isoflurane?
Most potent, slowest. concern for coronary steal in HoTN
What are contraindications of nitrous oxide?
- methionine synthase pathway deficiency
- surgery involving gas filled spaces
- middle ear
- pneumothorax
- intraocular air bubble
- 1st tremester
- increased ICP
- long cases > 6hr
The ideal anesthetic agent
- Non-irritating to the respiratory tract
- Rapid induction and emergence
- Chemically stable (non-flammable)
- Produce amnesia, analgesia and areflexia
- Potent
- Not metabolized and excreted by respiratory tract
- Free of toxicity and allergic reactions
- Minimal systemic changes
- Uses a standardized vaporizer
- Affordable
Is propofol an acid or a base?
Acid
Propofol induction dose?
1.5mg/kg-2.5mg/kg
Propofol MAC (endoscopy) dose
25-100 mcg/kg/min
Propofol TIVA dose?
100mcg-300mcg/kg/min
Propofol antiemetic dose?
10mg IV
Propofol antipruritic dose?
10mg IV
Propofol anticonvulsive dose?
1mg/kg IV
Propofol MOA
GABA modulator (allosteric) – Cl- influx hyperpolarizes neuron (IPSP).
Propofol t1/2
30min - 1hr
Propofol Vd
2.5-3.5
Propofol active metabolites
4- hydroxypropofol
What’s propofol’s biggest advantage?
Rapid return to consciousness with minimal residual effect
Unique about propofol metabolism
Clearance exceeds hepatic blood flow (liver)
Tissue uptake in the lungs
Propofol context sensitive t1/2
<40 min
Factors that affectd FA/FI
Factors that affect the FA/FI ratio include:
- the delivered inspired anesthetic concentration,
- the blood-gas partition coefficient of the inhalation agent,
- alveolar ventilation (VA),
- cardiac output (Qt),
- and the distribution of Q to the vessel-rich organs (i.e., heart, brain, kidneys, and liver).

Etomidate MOA
GABA modulator
What does GABA stand for?
Gamma-aminobutyric acid
How long does propofol last?
8-10 min
How long does etomidate last?
5-15 min
Contraindication of etomidate
Porphyria, septic shock (etomidate causes suppressed 11-betahyroxylase for 8 hrs, low cortisol)
How is etomidate metabolized?
hydrolysis, plasma esterase and microsomal enzymes in the liver.
Etomidate induction dose
0.2-0.4mg/kg IV
Is Etomidate an acid or base?
It’s a base.
Etomidate t1/2
2-5 hrs
Ketamine induction dose
1-2.5mg/kg
ketamine t1/2
2-3 hrs
Etomidate VD
2.2-4.5
Ketamine Vd
3.5-4.5
Ketamine MOA
NMDA (N-methyl-D-aspartate) non-competetive antagonist ==> dissociative amnesia
Ketamine dart dose, onset time
Ketamine PO dose, onset time
dart 4-8mg/kg, <10 min onset
PO 10 mg, 10-20 min onset
Ketamine active metabolite
metabolized by liver, norketamine
ketamine contraindication
increased ICP
eye procedures
eye trauma
high emergence delirium risk
benzodiazepine MOA
allosteric agonist on GABA
benzodiazepine effects
anxiolytic
muscle relaxant
anticonvulsant
anterograde amnesia
What are side effect of benzodiazepine?
STRONG synergistic effect with opioids (RESPIRATORY DEPRESSION)!!!
midazolam induction dose
0.02-0.04mg/kg
midazolam Vd
High
How is midazolam metabolized? active metabolite?
rapid metabolism in liver d/t imidazole ring.
active metabolite:
- 1-hydroxymidazolam, which has half the activity
- 4- hydroxymidazolam, nondetectable amount
midazolam t1/2
2 hrs
Is midazolam injection painful? why?
water soluble with imidazole ring. only benzo with painless injection
Is midazolam an acid or base?
Base
Is diazepam Vd?
High
diazepam t1/2
>40 hrs
How is diazepam metabolized? Active metabolites?
Liver I (oxidative)
Active metabolites:
- desmethyl diazepam (responsible for long t1/2)
- Oxazepam
- temazepam
diazepam contraindication
don’t give to pt with porphyria
t1/2 is pt’s age, careful with old pt.
what can diazepam be used for?
DT, anticonvulsant, pt with tetany, lumbar disc disease.
Lorazepam t1/2
14 hrs
What is special about lorazepam’s PK?
Slowest onset (1-2 min) but most potent
What do you use to reverse benzodiazepine?
flumazenil
dosage of flumazenil
give 0.2mg initially, usually have effect in 2 min.
then give 0.1mg every 60 seconds. 0.5-1mg should completely reverse. if given 5mg and pt still not responsive, something else is going on.
Barbiturates MOA
GABA agonist,
also works on adenosine, nAchR, glutamate
barbiturates contraindication
Do not give pt with porphyria
What drug should not given to pt with porphyria?
Barbiturates
Diazepam
Etomidate
If barbiturates are infused arterially, what to do?
papaverine, heparinization, arteriodilate with regional anesthesia
Thiopental induction dose?
2.5-5mg/kg
how is Thiopental metabolized? Acftive metabolite?
Liver I phase I
Active metabolite: pentobarbital
Thiopental Vd?
Large
What is methohexital induction dose?
What is methohexital pediatric dose?
1-2mg/kg
25mg/kg
what is methohexital used for?
ECT to lower seizure threshold
Opioid MOA
- Pre synaptic – inhibit release of acetylcholine, dopamine, norepinephrine and Substance P
- Post synaptic – increased K+ conductance = decreased function
opioids major side effects
- CV – bradycardia, impaired SNS response, orthostatic hypotension, SYNERGISM ↓↓ BP with benzos and nitrous oxide!!!
- Resp – ↓↓ responsiveness to CO2, deep, slow breaths. ↑↑ airway resistance.
Signs of opioid OD
miosis+hypoventilation+coma
How do you reverse opioid? dose? what’s its t 1/2?
naloxone, 1-4ug/kg IV, 30-45 min
Morphine active metabolite. DOA and potency?
morphine-6-glucorinide, longer DOA, 65X potency than morphine
What organ dysfunction can cause respiratory depression when morphine is given?
renal dysfunction
Meperidine (Demerol) mainly used for?
Anti-shivering postoperatively
• Stimulation of kappa receptors
Meperidine potency compared to morphine
1/10
meperidine active metabolite
normeperidine
normeperidine elimination t1/2
15 hrs, >30 hrs in renal failure, accumulation can lead to meperidine delirium, seizures
Meperidine Vd
High
fentanyl induction dose. why use it?
1-3 ug/kg
Blunt sympathetic stimulation to intubation
are all IV opioids acids or bases?
They are bases
fentanyl Vd
High
How is fentanyl metabolized
Liver, phase 1
Fentanyl context sensitive t1/2 increases after infusion for how long?
After 2 hrs. It keeps growing
what is responsible for fentanyl’s large first pass uptake?
Lungs
fentanyl’s potency compared to morphine
100x
Sufentanyl dose
0.1-0.4 u/kg
sufentanyl Vd
high
How is sufentanil metabolized
Liver phase I
Sufentanil active metabolite
desmethyl sufentail
Does fentanil release histamine?
No
What is a big complaint about morphine?
Morphine spinals cause crazy itchiness, can cause delayed ventilatory depression
Sufentanil potency
5-10 x than fentanyl
What patient should avoid sufentanil?
Renal, accumulation issue
What intubation issue can sufentanil cause?
Chest wall rigidity
Alfentanil dose
15mcg/kg
What is the biggest advantage of alfentanil
fast onset
what pt population should avoid alfentanil
Avoid in untreated parkinson pt, it causes acute dystonia
Remifentanil context sensitive t1/2
4 minutes
Remifentanil Vd
small
Remifentanil TIVA dose
1-3 ug/kg
How is remifentanil metabolized?
non specific plasma esterease hydrolysis
What do you need to consider when using remifentanil? What do drug could you use?
Long acting opioid for postop analgesia. Ketamine (0.5-1mg/kg) and magnesium (1g over 2 hrs) can help
What is ketamine mostly used for?
Trauma
Opioid agonist-antagonist MOA
Bind to mu receptors with minimal activation (antagonism) and then bind to kappa/delta for other effects (agonism) àlower efficacy
What is butorphanol used for?
Good for analgesia, anti-shivering (kappa). Can limit effectiveness of pure opioid agonists though!
butorphanol unique side effect
dysphoria, hyperdynamic CV (catecholamines)
What’s unique about Nalbuphine’s structure?
Chemically related to oxymorphone and naloxone; analgesic properties of morphine, 1/4 antagonist of nalorphine
how does Nalbuphine’s antagonist effect related to timing?
If given before opioid, opioid does not work very well; if given after opioid given, can reverse resp depression for 2-3 hrs but maintain analgesisa
Nalbuphine side effects compared with butorphanol
compared with Butorphanol less dysphoria, and LIMITED catecholamine stimulation, good for CV patients
How does NSAIDS work
Damaged cells releases COX and prastaglandins, NSAIDS has anti-inflammatory effect on the damaged nerve endings and reduce inflmmatory response
COX-1 fxn
maintain renal, GI and thromboxane (PLT aggregation)
COX-2 fxn
fever, pain, inflammation
what type of NSAID is Toradol (Ketorolac)
non selective NSAID
Ketorolac (Toradol) dose
15mg q6h
What type of NSAID is Celecoxib?
selective Cox-2 inhibitor
Benefit and risk fo Celecoxib (Celebrex)
less GI toxicity, but increases CV risk
Celecoxicb(Celebrex) dose
400mg preop, 200mg BID x 5 days postop
Are all NSAIDS acids or bases?
Acids
Do NSAIDS have high Vd or low Vd
low Vd
NSAIDS are metabolized and eliminated by what?
metabolized in liver and eliminated by renal and biliary
What can cause hypersensitivity to NSAIDS?
nasal polyps + rhinitic allergy + asthma = Risk of anaphylaxis
Acetaminophen MOA
centrally activate serotonergic pathway, antagonism of NMDA, sub P and nitric oxide pathways
Does acetaminophen have anti-inflmmatory effect?
No
Acetaminophne dosage
325-650mg Q4-6h, do not exceed 4000 mg q24h, <2g for chronic alcoholics;
1000mg IV q6h, do not exceed 4000mg/24h
What is the NSAID to use in CV patients?
Naproxen
How does acetaminophen damage liver? How to treat OD?
It depletes glutathione.
Charcoal or infusing acytylcisteine
Ibuprophen type of NSAID and dose
non selective
400-800 mg q6-8h
Succynocholine dose
1mg/kg
How is succinylcholine metabolized
PchE
Succinylcholine onset
60 seconds
Succinylcholine DOA
9-13 min
Atracurium dose
0.5 mg/kg
Atracurium metabolized
Ester hydrolysis and Hoffman
Does atracurium have active metabolite?
Laudanosine can cause convulsions
cisatracurium dose
0.1mg/kg
cisatracurium metabolized
hoffman
Explain Succinylcholnine MOA
Chemical structure is two Ach molecules connected together, binds to nAchR, cannot be hydrolyzed by AchE, has to drift off into blood stream and metabolized by PchE
What populatin is contraindicated for Succinylcholine?
Pediatric pt <5 yrs old; hyperkalmelia (will increase K by 0.5); Pt with MH history; ICP issue; eye surgery
What is the biggest unfavorable feature of Atracurium? How to treat?
Histamine? H1 and H2 blocker.
Rocuronium dose
0.6mg/kg
Rocuronium metabolized
Liver and Kidney
Rocuronium onset time
1.7 min
Vecuronium dose
0.1 mg/kg
Vecuronium metabolized
mostly liver, some kidney
Vecuronium onset
2.4 min
Vecuronium active metabolite
3-OH (80% potency)
pancuroium dose
0.08mg/kg
pancuronium onset
2.9 min
pancuronium metabolized
major kidney, some liver.
What is pancuronium good for?
has vagolytic effect, good for CV patient
Sugammadex dose
>2 twitches 2mg
1-2 twitches 4mg
0 twitches 8-16mg
Sugammadex MOA
gamma-cyclodextrin encapsulates NMBD (rocuronium)
dexmedetomidine dose
Preop: 4mcg, up to 20 mcg, monitor for bradycardia
[0.5-1 ug/kg] bolus over 15 minutes, then [0.2-0.7 mcg/kg/hr]; monitor for severe bradycardia (and hypotension)
What do you monitor when giving dexmedetomidine
bradycardia
dexmedetomidine MOA
Alpha 2 agonist, inhibits SNS
cholinesterase inhibitor MOA
inhibit the breakdown of Ach hence increase the concentration of Ach, so they have higher chance of binding to nAchR
What is the side effect of cholinesterase inhibitor?
muscarinic effect: salvalation, lacrimination, bronchoconstriction, increased bowel motility
Edrophonium dose
1-1.5 mg/kg
What do you pair edrophonium with? Dose?
Atropine. 15mcg/kg
Neostigmine dose
0.06mg-0.08mg/kg
What do you pair neostigmine with? Dose?
glycopyrrolate, 10-20mcg/kg
Scopolamine dose, onset
1.5mg behind ears, onset 2-4hrs
How to reverse scopolamine? dose and timing?
physostigmine, 0.01-0.03mg/kg IV, repeat in 15-30 minutes.
Contraindication for scopolamine
closed angle glaucoma
What are SE of scopolamine?
Passes BBB, risk for restless, hallucination->unconsciousness
What patient population has highest risk for PONV?
Young female, non-smoker, hx of NV, used opioid, motion sickness,
Ondasetron MOA. Which area does it work on?
5-HT 3 inhibitor, works on chemoreceptor trigger zone.
ondansetron dose
4mg IV
ondansetron which population to adjust dose?
hepatic dysfunctional population do not give more than 8mg
ondansetron when do you give?
30 minutes before end of surgery
Major side effect of ondansetron
Headache dizziness, prolonged QT
Promethazine (Phenergan) dose, preffered route, why?
Onset?
12.5-25 IM preffered dt leaking out of vascular space.
onset 5 min IV, 20 min IM
promethazine contraindications
Older pt>65, causes confusion, give with opioid will cause sedation with opioids
Metoclopramide dose
10mg
metochlopramide MOA
dopamine D2 hibitor.
metochlopramide dosing adjustment
adjust for renal patients.
What do you need to be aware of when giving metoclopramide?
Slow push, otherwise abd cramping, anxiety
metoclopramide contraindication
pheochromocytoma, HTN crisis
Don’t give to Parkinson pt d/t EP effects, GI obstruction, seizure
what is metoclopramide good for?
GI prokinetic
What pt population should get corticosteroids
- daily taking >5mg for 2-3 weeks
- have been on treatment for the last 12 months
What can corticosteroids do?
anti-inflammatory, immunosuppressant.
What do you give during adrenal crisis?
Hang fluid NS 1-3L over 1hr, give 100mg hydrocortisone, then 50mg q6h
Dexamethasone dose
4-10mg IV
Contraindication of dexamethasone
active infection,
What is MAC
the minimum alveolar concentration to produce lack of movement in surgery in 50% of populations
Factors increasing MAC
hyperthermia, alcohol abuse, hypernatremia, increased CNS activity
Factors decreasing MAC
hypothermia, increased age, pregnancy, alpha 2 agonist, hyponatremia
Explain blood gas efficiency
the amount of drug that binds to drug(inactive), VS the amount of drug that will diffuse into tissues that has anesthetic effect
What is uncoupling effect?
CMRO2 decrease, CBF increase
why are we using NMBD?
- optimal condition for surgery
- optimal condition for intubation
- ventilator synchronization
Midazolam pediatric oral dose
0.4-0.8 mg/kg
Gabapentin preop multimodal pain mgnt dose
Gabapentin postop dose
1200mg one time
600mg Q8h x 14 days
Lidocaine induction dose. why use it?
Intra op multimodal dose?
1mg/kg: to blunt sympathetic stimulation to intubation
1-2 mg/kg/hr
Propofol age consideration
Decrease dose in elderly; increase in children and young adults
When to give dexamethasone
give shortly after induction
What pt population is contraindicated for ketorolac?
avoid renal compromised pt.
meperidine antishivering dose?
12.5 mg
midazolam postop sedation dose? gtt dose
0.5-4mg; 1-7mg/hr
What mechanism causes miosis?
Edinger-westphal nucleus on oculomotor nerve (cranial nerve III)
After opioid administration, GI spasm happens at?
Sphincgter of oddi
What do you do in opioid overdose?
reversal dosage?
- Antagonist
- Give oxygen
- mechanical ventilation
Narcan: 1-4 ug/kg IV 5 ug/kg/hr can fix depression of ventilation without affecting analgesia
Which pt population should not get atracurium?
asthma
What is pancuronium not good for?
Rapid sequence intubation, due to its slow onset
what class of antiemetic is promethazine?
Antihistamine
What PK property of thiopental makes it different from propofol.
10x long elimination t1/2
In a perfect world, an indution drug should be:
- rapid smooth onset and recovery
- analgesia
- minimal cardiac and respiratory depression
- antiemetic
- bronchodilation
- lack of toxicity and histamine release
- advantageous pharmocokinetics and pharmaceutics
drug doses related to 15
ketorolac - 15mg q6h
Alfentanil - 15mcg/kg
Atropine -15mcg/kg