Anesthesia Pharm Flashcards
1
Q
uptake = ?
A
uptake = solubility x CO x (PA-PV)
2
Q
2nd gas effect
A
- High volume uptake of 1 gas accelerates rate of increase of
PA of 2nd gas - N2O + sevo = faster increase of sevo concentration
- used for inhalational induction
3
Q
concentration effect
A
increasing the concentration of an agent increases the rate of rise of PA
4
Q
PA = ?
A
PA = Pi - uptake
5
Q
racemic mixtures
A
- 2 entantiomers present in equal proportions
- Etomidate and Thiopental
6
Q
division of CO
A
- VRG = 75% of CO and 10% of body mass
- muscle = 19% of CO and 50% of body mass
- fat = 6% of CO and 20% of body mass
- VPG = 0% CO and 20% body mass
7
Q
pKa
A
- pH at which 50% of a drug/molecule is ionized
- basic drugs ionize when pH < pK
- acidic drugs ionize when pH > pK
8
Q
pharmacokinetics
A
- what the body does to the drug
- absorption, distribution, elimination, metabolism
9
Q
pharmacodynamics
A
what the drug does to the body
10
Q
competitive antagonist
A
reversible – overcome by increasing the concentration of the agonist at the receptor site
11
Q
noncompetitive antagonist
A
irreversible
12
Q
Thiopental (Brevitol)
A
- barbituate
- contraindication: acute intermittent porphyria
- induction dose: 3-5 mg/kg
- supplied at 25 mg/ml
- onset: 30-40 s, peak: 1 min, duration: 5-8 mins
- protein binding: 80% Albumin
- great for burst suppression (dec. CMRO2 up to 55%)
- mechanism: dissociation of GABA from receptors leading
to chloride channel opening and hyperpolarization - decrease SBP, increase HR, vasodilates
- pH = 10.5 – bacteriostatic, thrombophlebitis
- hangover effect
- racemic mixture
13
Q
Etomidate (Amidate)
A
- water soluble in acid, lipid soluble in the body
- 35% glycerol – pain on injection
- racemic mixture
- 76% protein binding
- cardiovascular stability
- may induce seizures
- myoclonus, adrenocortical suppresion leading to
decreased cortisol levels, PONV, hiccups (rare) - induction dose: 0.2 - 0.6 mg/kg
- onset: 30 s, peak: 1 min, duration: 3-5 mins
14
Q
Propofol
A
- dose: MAC =
TIVA = 100-200 mcg/kg/min
induction = 1-2 mg/kg
- don't use > 3 days in ICU -- hyperlipidemia
- oil at room tempurature, aqueous insoluble
- 98% protein binding
- rapid redistribution
- contraindications: egg and soy allergy
- glycerol causes pain on injection
- preservative: disodium edetate
15
Q
Ketamine
A
- non GABA – NMDA
- PCP derivative
- low protein binding – 27%
- inc. ICP, inc. CMRO2, inc. CBF
- bronchodilation, increased secretions
- inc. BP, inc. HR, inc. CO, possible increase in release of
catecholamines leading to arrhythmias - Emergence Delerium (Tx = benzos)
- analgesic effects
16
Q
Midazolam (Versed)
A
- PO: 50% 1st pass metabolism
- potentiates opioid ventilatory depression
- dose: pediatric = 0.5 mg/kg PO (no grapefruit juice)
adult = - anticonvulsant
17
Q
Flumazenil
A
- benzo antagonist
- shorter half life than benzos
- metabolism: hepatic enzymes
18
Q
Solubility of inhaled anesthetics
A
halo > iso > sevo > N2O > des
19
Q
Desflurane
A
- 6.0% MAC
- needs a special vaporizer
- fast on/off
- B:G solubility: 0.42
- B:B solubility: 1.3
- tachycardia due to SNS stimulation
- apnea with 1.5-2 MAC
- airway irritant – avoid in asthmatics
- carbon monoxide formation from interaction with
absorbers
20
Q
Nitrous Oxide
A
- 105% MAC
- B:G solubility: 0.47 (highly insoluble)
- B:B solubility: 1.1
- increases CMRO2
- sympathomimetic
- increases PVR in patients with pulmonary HTN
- analgesic
- PONV
- diffusion hypoxia – Tx: supplemental oxygen
- bone marrow suppression
- drawn to air filled spaces – don’t use with middle ear,
eyes, laparoscopic, bowels, or insertion of a gas bubble
21
Q
Sevoflurane
A
- 2.0% MAC
- B:G solubility: 0.65
- B:B solubility: 1.7
- apnea with 1.5-2 MAC
- compound A: interaction with CO2 absorbers that can
be overcome with flows of > 2L/min, worse with baralyme - least AW irritant – good for inhalational inductions
- low flow for 2 MAC hours
22
Q
Isoflurane
A
- 1.1% MAC
- B:G solubility: 1.4
- B:B solubility: 2.6
- barely affects CBF – great for neurosurgery
- burst suppression with 1.5 MAC
- coronary steal
23
Q
Halothane
A
- 0.75% MAC
- B:G solubility: 2.4
- B:B solubility: 2.9
- increases CBF 200%
- decreases myocardial contractility – decrease CO
- most potent trigger of MH
- nephrotoxicity – 20% liver metabolism
- thymol preservative
- great for inhalational inductions
- high potency
- bronchodilation
24
Q
metabolism and elimination of inhaled anesthetics
A
- biotranformation, transQ loss, and exhalation (major)
- Halothane is most metabolized
- Nitrous is least metabolized
25
MAC
- MACbar = 1.3 - 1.5
- 1.3 MAC prevents movement in 95% of patients
- MAC awake = 0.1-0.3 MAC
- MAC intubation = 2 MAC
- MAC amnestic = 0.25 MAC
- MAC decreases 6% per decade
- avoid more than 0.5 MAC with motor potential monitoring
26
factors increasing MAC requirement
hyperthermia, drug-induced increase in catecholamines, hypernatremia
27
factors decreasing MACrequirement
hypothermia, increased age, preop meds, hyponatremia, alpha-2 agonists, acute EtOH intoxication, pregnancy, immediate post-partum, lithium, lidocaine, neuraxial opioids, PaO2 < 38, BP < 40, CPB, opioids
28
potency of inhaled anesthetics
halo > iso > sevo > des > N2O
29
local anesthetic loss of sensation
autonomic > sensory > motor
30
resting membrane potential
~ -70 mV
31
membrane potentials
maintained by Na-K pump
32
local anesthetics mechanism of action
bind Na channels in the activated state to decrease the rate of depolarization and therefore prevent action potential propagation
33
easiest nerves to block
small diameter with greater myelination, sensory, basic environment, rapidly firing, decreased K and increased Ca
34
metabolism of amides
CYP 450 (hepatic)
35
metabolism of esters
- plasma cholinesterase hydrolysis
- metabolite PABA can cause allergic reactions
- exception: cocaine is metabolized in the liver
36
methemoglobinemia
- caused by metabolite in prilocaine and benzocaine
- infants at greatest risk
- spO2 will read 85%, dark/chocolatey blood
- treatment: methylene blue
37
epinephrine and LA
- limits systemic absorption and maintains concentration
of drug at the site
- helps prevent toxicity
- does not affect onset
- 1:200,000 (5 mcg/ml)
- epi has a lesser effect on Bupivicaine because it has an
longer duration
- contra: end arterial supply (Tx: nitroglycerin paste)
38
systemic toxicity from LA
- causes: accidental IV injection, absorption from the
injection site (dose, vascularity, epi, drug itself)
- symptoms: circumoral numbness, tinnitus,
lightheadedness, visual disturbances, muscle twitching,
unconsciousness, convulsions, respiratory depression,
cardiovascular collapse
- signs: hypotension, decreased cardiac conduction, vent
arrhythmias
39
Bupivicaine
- long duration
- highly toxic to CV system, especially in pregnant
patients and potentiated with hypoxia and acidosis
- don't use in upper extremity
40
vascularity of injection sites
IV > tracheal > intercostal > caudal > paracervical > epidural > brachial plexus > sciatic > subQ
41
maximum toxic dose
Lidocaine: 5 mg/kg
7.5 mg/kg with epi
Bupivicaine: 2.5 mg/kg
42
Cocaine
- hepatic metabolism
- vasoconstriction and LA of mucosal membrane (ENT)
- intranasal onset: 30 mins
- IV/smoked onset: < 5 mins
- prevents reuptake of NE dopamine causing HTN, vent
arrhythmias, increased O2 demands of heart, coronary
vasospasm, decreased uterine blood flow, and seizures
- no OD treatment, treat symptoms -- NTG, benzos, etc.
43
spinal anesthesia
- inject LA into subarachnoid space
- works on preganglionic fibers
- dose depends on patient height, segments of anesthesia
needed, and duration of action
- dependent on concentration not volume
- faster onset than epidurals
- duration
lidocaine: < 1.5 hours
bupivicaine: 2-2.5 hours
tetracaine: 2-3 hours or 5 with epi
- chloroprocaine is contraindicated because it is
neurotoxic
44
Lidocaine
- add dextrose to a spinal to make it hyperbaric
- transient neurologic symptoms
- crosses dura mater quickly in epidural
45
epidural anesthesia
- mechanisms of action: diffuse across dura mater and
absorbed intravenously
- dependent on volume not concentration
- onset: 15-30 mins
- fetal effects: none unless baby is acidotic which could
create ion trapping and toxicity
- typical volume used: 15-30 ml
46
Bier block
- regional hand block
- duration of action is indicated by tourniquet time
- tourniquet must be let down slowly
- don't use bupivicaine
- 50 ml of lidocaine or prilocaine
47
peripheral nerve blocks
- diffusion occurs on a concentration gradient
- onsets and durations
Lidocaine: 3 mins, 1-2 hours or 2-3 hours with epi
Bupivicaine: 15 mins, 3-6 hours or 4-8 hours with epi
48
topical anesthesia
- drugs used: tetracaine, cocaine, lidocaine, benzocaine
| in hurricaine spray
49
EMLA
- eutectic mixture of LA
- lidocaine 5% and priolocaine 5%
- local anesthetic absorbed through the skin
50
cauda equina syndrome
- lumbar plexus block
- risk greatest with 5% lidocaine via catheter
- spinal anesthesia
51
mechanism of action of opioids
- agonist at the opioid receptors and mimic the effects of
endogenous ligands
- decrease neurotransmitter release
- location of action: pariaqueductal gray matter of brain
stem, amygdala, corpus stiatum, hypothalamus, spinal
cord
52
mu 1 receptors
- supraspinal and spinal
- analgesia*, euphoria, N/V, pruritis, low abuse potential,
bradycardia
- binds endorphins
53
mu 2 receptors
- predominantly in spinal cord
- hypoventilation*, analgesia, euphoria, sedation, physical
dependence, constipation
- binds endorphins
54
kappa receptors
- supraspinal and spinal
- analgesia, respiratory depression (less than mu 2),
dysphoria, diuresis
- binds dynorphins
- agonist-antagonists typically work here (Nalbuphine),
used in abuse potential patients
- resistant to high intensity pain
55
delta receptors
- supraspinal and spinal
- analgesia, respiratory depression, physical dependence,
urinary retention
- enkephalins bind here
56
neuraxial analgesia
- acts on mu receptors in the spinal cord
- some systemic absorption
- dose related analgesia and specific for visceral pain
- side effects: pruritis, N/V, urinary retention, ventilatory
depression
- CV effects: decrease HR, BP, and sympathetic tone and
minimal contractility effects
- increased apneic theshold, decreased RR and increase
tidal volume, decreased minute ventilation, cough
suppression
- seizures with Meperidine use -- normeperidine metabolite
- sphincter of oddi spasms -- Tx: Glucagon 2 mg IV
- OD: miosis, ventilatory depression, coma
57
potency of opioids
Meperidine: 0.1
Morphine: 1
Hydromorphone: 8
Alfentanil: 10-20 (1/5-1/10 more than fentanyl)
Fentanyl: 75-125
Remifentanil: 100 (similar to fentanyl)
Sufentanil: 1000 (5-125 more than fentanyl)
58
Morphine
- onset: 15-30 mins, duration: 3-4 hours
- dose: 2-10 mg
- hepatic, extrahepatic, and renal metabolism
- metabolite morphine-6-glucaronic-- allergic reaction
59
Meperidine (Demerol)
- potency: 0.1
- IV, IM, PO
- peak: 5-7 mins, duration: 2-3 hours
- local/atropine like side effects
- 90% hepatic metabolism and renal elimination
- seizures in renal patients
- treatment for post op shivering: 12.5 mg
60
Fentanyl
- IV, transdermal, PO, intranasal
- potency: 75-125
- peak: 3-5 mins, duration: 30-60 mins
- 75% fist pass pulmonary uptake
- highly lipid soluble and protein bound, cross BBB fast
- hemodynamically stable
- induction dose: 2-6 mcg/kg with sedative hypnotic
- additional dose: 25-50 mcg every 15-30 minutes
- infusion rate: 0.5-5 mcg/kg/hr
61
Sufentanil
- potency: 1000 (5-10x more than fentanyl)
- peak: 3-5 mins, duration: 30-60 mins
- dose: induction: 0.3-1 mcg/kg 1-3 mins before induction
additional: 0.5 mcg/kg
infusion: 0.5 mcg/kg/hr
- good for neuro cases, no HTN from intubation, helps
with Mayfield stimulation
62
Alfentanil
- potency: 10-20 (1/5-1/10x more than fentanyl)
- peak: 1.5-2 mins, duration: 10-20 mins
- renal failure doesn't alter clearance
- rapid on/off of intense analgesia
- great for retrobulbar block and DL
- dose: 5-10 mcg/kg
63
Remifentanil
- potency: 100 (similar to fentanyl)
- peak: 1.5-2 mins, duration: 6-12 mins
- metabolism: plasma and tissue esterases
- dose: 0.5-1 mcg/kg (+propofol) for DL
0. 25-0.5 mcg/kg/min following
- caution: patient won't breathe on remi infusion
64
Codeine
antitussive, analgesia for mild to moderate pain
65
Methadone
long term relief from chronic pain and opioid withdrawal
66
Hydromorphone (Dilaudid)
- potency: 8
| - shorter acting than morphine
67
Percodan
aspirin and oxycodone
68
agonist/antagonists
- pentazocine, butorphanol, nalbuphine
- produce analgesia with minimal respiratory depression
- ceiling effect
69
Naloxone (Narcan)
- opioid antagonist
- pure mu antagonist
- treats overdose and respiratory depression
- duration: 30-45 mins
- dose: 1-4 mcg/kg
- side effects: N/V, pain, tachycardia, increase SNS activity
- dilute the 400 mcg vial into 10 ml and give 1-2 ml every
2-3 mins
70
Succinylcholine
- 2 ACh molecules bound together
- dose: 1-2 mg/kg
- onset: 30-60 seconds, duration: 3-5 mins
- laryngospasm dose: 0.1 mg/kg IV
- mechanism of action: binds to and activates receptors
- fasiculations
- metabolism: plasma cholinesterases
- decreased metabolism: hypothermia, hypthyroidism,
high estrogen mom at term, liver failure
- phase I blockade: decreased single twitch response,
decreased amplitude with tetany without fade (box-like
appearance), enhanced with Neostigmine
- phase II blockade: resembles NDNMBD (stair-case), fade,
post-tetanic potentiation, antagonized by Neostigmine
- side effects: brady/tachycardia, hyperkalemia*, increased
IOP/ICP, MH trigger, increased intragastric pressure,
myoglobinuria
- hyperkalemic conditions: 3rd degree burns, trauma,
severe intraabdominal infection, spinal cord injury,
encephalitis, Guillan-Barre, Parkinson's, tetanus, prolonged
total body immobilization, ruptured cerebral aneurysm,
polyneuropathy, closed head injury, hemorrhagic shock,
metabolic acidosis
71
characteristics of muscle relaxants
- small, rapidly moving muscles are the first to go
- diaphragm is one of the last to relax
- onset depends on fiber type and ACh receptor density
- adductor pollicis can be blocked before larynx
- orbicularis occuli correlates most with VC and
diaphragm
- limited volume of distribution similar to extracellular
fluid
- can't cross lipid membranes -- no CNS effects, minimal
renal absoprtion, PO is ineffective, no fetal effect
- decreased clearance with age, volatiles, and disease
72
Pancuronium
- long acting
- dose: 0.08-1.2 mg/kg
0. 01 mg/kg maintenance
- onset: 3-5 mins, duration: 60-90 mins
- 80% renal excretion -- bad for renal patients
- ED95 = dose for CV effects
73
Benzylisoquinoliniuma
-curiums
74
Aminosteroids
-roniums
75
ACh
- binds to cholinergic receptors (nicotinic and muscarinic)
- postynaptic membrane receptors
- metabolized by anticholinesterase into acetic acid and
choline
76
Dibucaine
- LA that decreases function of plasma cholinesterase and
prolongs Succ duration
- #80
77
NDNMB characteristics
- compete with ACh at alpha subunits
- decreased single twich, fade, TOF ratio < 0.7,
posttetanic potentiation,antagonized with Neostigmine
- rare histamine release (curiums)
- large margin of safety
- prolonged block with volatiles, aminoglycosides (AB),
and high doses of LA, anti-dysrhthmics, diuretics,
ganglionic blockers (trimethaphan), hypothermia,
increased Mg
- shortened block with seizure meds (Phenytoin)
78
Atracurium
- intermediate acting
- onset: 3-5 mins, duration: 20-35 mins
- good for renal failure patients -- Hoffmann degradation
- will form crystals when used with Thiopental
- pH: 3.2
- dose: 0.5 mg/kg (over 30-60 seconds)
- increased degredation with alkalosis
- side effects: histamine release
- decrease pediatric dose 50%
- laudanosine metabolite can cause seizures from
continuous use
79
Cisatracurium
- dose: 0.1-0.15 mg/kg, infusion: 1-2 mcg/kg/min
- Hoffman degradation
- intermediate acting
- onset: 2-3 mins, duration: 20-45 mins
- no histamine release or metabolite
80
Rocuronium
- can mimic the onset of SCh if you use 1.2 mg/kg
- dose: 0.6-1.2 mg/kg, 5-12 mcg/kg/min
- intermediate acting
- onset: 2.5 mins, duration: 20-45 mins
- cleared unchanged by liver and kidneys -- no metabolites
81
Vecuronium
- 10 mg poweder reconstituted to 1 mg/ml
- dose: 0.08-0.12 mg/kg
0.01 mg/kg q 15-20 mins maintenance
1-2 mcg/kg/min infusion
- intermediate acting
- onset: 2-3 mins, duration: 20-45 mins
- liver and kidney clearance
- faster onset with pediatrics and longer duration
- longer duration in elderly
82
Mivacurium
- short-acting
- used to be used for pediatric intubations
- dose: 0.15-0.2 mg/kg, 4-10 mcg/kg/min
- onset: 2-3 mins, duration: 10 mins
- plasma cholinesterase clearance
- no longer made
83
Anticholinesterase drugs
- reverse muscle relaxants
- antagonism of CNS effects of other drugs (atropine
overdose) , treatment of MG or glaucoma
- increase ACh in the NMJ and everywhere else
- renal clearance is 50-70% of elimination
- lower dose and faster onset with kids
- increased duration with elderly
- BBLUDS
84
Edrophonium
- reversible inhibition
- short onset, quaternary amine
- onset: 1-2 mins
- shortest duration
- Mysathenia Gravis test
85
Neostigmine
- intermediate onset, 7 mins
- formation of carbamyl esters
- quaternary amine
- duration: 80 mins
- dose: 0.04-0.07 mg/kg
- maximum dose is not 5 mg
86
Physostigmine
- formation of carbamyl esters
- tertiary amine, crosses BBB
- treatment of anticholinergic OD
87
Pyridostigmine
- formation of carbamul esters
- intermediate onset, 12 mins
- duration: 2 hours
88
Echothiophate
- irreversible inactivation of ACh
- pesticides/insecticides form irreversible covalent bonds
with enzymes
89
Anticholinesterase overdose
- effects are BBLUDS and wek muscles
| - Tx: atropine and pralidoxime*
90
Antichoinergics
- prevent ACh binding at the muscarinic receptors,
reversible, can be overcome with increased ACh
- effects: sedation, antisialagogue, increased HR, smooth
muscle relaxation, mydriasis, prevention of motion
sickness, decreased gastric ion secretion
- renal clearance but renal disease is not a contraindication
- uses: premed sedation, bradycardia Tx, reversal of
NDNMB, antisialagogue
91
Atropine
- naturally occurring
- tertiary amine, crosses BBB
- onset: 1-2 mins
- duration: 30-60 mins
- mild sedative
92
Glycopyrrolate
- quarternary amine, doesn't cross BBB
- synthetic
- onset: 2.3 mins
- duration: 30-60 mins
-fastest clearance
- 0.2 mg IM is more potent antsaiagogue effect than IV
and won't increase the heart rate as much, 2x more
potent than atropine
- slower onset than atropine for the treatment of
bradycardia
- good for oculocardiac reflex and colon resections
93
Scopolamine
- tertiatry amine, crosses BBB
- naturally occuring
- powerful sedative and antisialagogue (3x more potent
than atropine)
- dose: 0.4mg IV
- amnesia
- reticular activating system in the braine
94
Ipatropium (Atrovent)
- inhaled anticholinergic
- works on muscarinic receptors on smooth muscles of
medium and large airways
95
Combivent
- Albuterol + Ipratropium
96
central anticholinergic syndrome
- too much anticholinergic
- symptoms: restlessness, hallucinations, somnolence
- treatment: physostigmine
- children and elderly most susceptible
- rapid onset of dry mouth, blurred vision, tachycardia,
increased temp, flushing, and irritability
- effect: seizures, coma, ventilatory paralysis
97
reversal criteria for extubation
- TOF ratio > 0.7
- tetanus with 100 Hz (50% can still be blocked)
- grip strength
- negative inspired pressure > 20 cmH2O
- sustained head lift for 5 seconds* (33% can still be
blocked)
98
NDNMBD monitor
- ulnar nerve -- adduct thumb
- posterior tibial nerve -- plantar flex big toe
- peroneal nerve -- dorsiflex foot
- facial nerve -- most cloesly corresponds to the vocal cords
99
Sugammadex
- binds to actual muscle relaxant
- can reverse with no twitches
- independent of ACh level in the NMJ
- cleared renally but speed of reversal is independent of
renal function
- no need for anticholinergic
100
Cephalosporins
- 1st generation: gram + (Cefazolin)
- 2nd generation: gram - (Cefoxitin, Cefuroxoime,
Cefaclor)
- 3rd generation: Ceftriaxone and Ceptizoxime
- 4th: gram + and - (Maxiprime and Cefelidine)
101
Antimicrobial prophylaxis, head and neck surgery, cephalosporin allergy
- Clindamycin (gram +) + Gentamycin (gram -)
102
Antimicrobial prophylaxis, knee replacement, PCN allergy
Vancomycin 1 g
103
Antimicrobial prophylaxis, clean ortho procedure
none
104
antimicrobial prophylaxis, bowel procedure
- Cefoxitin
- Cefazolin + Metronidazole
- Ampicillin + Sublactam 3 g
105
AB for C section
Cefazolin 2 g after clamping of the cord
106
AB prophylaxis timing
within 60 minutes of incision
107
VRE
vancomycin resistant enterococci
108
MRSA
methocillin resistant staphylococcus areus
109
surgical site infection prevention, hypothermia and tissue perfusion
mild hypothermia (34-36*C) increases infection because of decreased tissue perfusion, decreased super oxide radicals, induced anti-inflammatory profile, decreased collagen production
110
surgical site infection and blood glucose
hyperglycemia increases morbidity and mortality
111
subacute bacterial endocarditis prophylaxis
- high risk: prosthetic heart valves, previous IE, complex
cyanotic congenital heart disease, surgically constructed
systemic and pulmonary codiuts
- Ampicillin 2 g or Gentamycin 1.5 mg/kg, 120 mg max
- PCN allergy: Clindamycin 600 mg or Cefazolin 1 g or
Vancomycin 1 g
112
Humalog (Lispro)
- rapid or fast insulin
| - better covers patients meals than regular Insulin
113
IV insulin infusion protocol
begin regular insulin at 0.5-1 unit/hour (25 units/25 ml saline)
114
Omeprazole
- proton pump inhibitor
- decreases gastric acid secretion and daily H+ production
- uses: GERD and ulcers
115
Carvedilol (Coreg)
- beta receptor antagonist
| - a:B = 1:10
116
portal vein thrombosis
- obstruction due to a clot or narrowing of the portal vein,
which brings blood to the liver from the intestines
- portal vein pressure increases -- portal HTN
- portal HTN can lead to ascites, splenomegaly, and
esophageal varices
- 25% of adults with cirrhosis have portal HTN
- diagnosed with doppler ultrasonography, bleeding of
esophageal or gastric varices, or splenomegaly
117
fundoplication
- treatment of GERD or hiatal hernia
- fundus is wrapped around the esophagus to strengthen
the LES and stop acid from backing up easily
118
Clevidipine (Cleviprex)
- CCB
- IV administration and titrated to effect with 25%
reduction in baseline SBP
- starting dose: 1-2 mg/hour up to 16 mg/hour
- looks like propofol
- use within 4 hours
- very little reflex tachycardia
119
ASA drug interactions
Warfarin and bleeding
120
CCB
- selectively inhibit L-type calcium channels in the heart
- 3 types: phenylalkymines (intracellular pore blocking -
Verapamil), dihydropropyridines (extracellular allosteric
modulation - Nicardipine), benzothiazepines (unknown -
Diltiazem)
- effects: decrease contractility, HR, SA node activity, AV
node conduction, BP
- clinical uses: coronary artery spasm, HTN (usually with BB
or nitrates)
- exaggerated response to volatiles, impaired NMB
reversal, increased risk of LA toxicity, decreased platelet
function, increased concentration of digoxin
121
Nicardipine
- CCB
- most vasodilation activity
- no SA/AV node effect or myocardial depression
122
Nimodipine
- CCB
- crosses the BBB and is used to treat cerebral artery
vasospasm
123
Verapimil
- CCB
- used intraop to correct cerebral artery vasospasm
- can prolong LA
- AV node depression, SA node negative chronotrope,
negative inotrope, slight vasodilator
124
Histamine
- autocoid, naturally occurring endogenous amine
- chemical mediator of inflammation and increases acid
production
- doesn't cross the BBB
- metabolism: 2 pathways -- methylation* and oxidative
deamination
- effects: dilation of arterioles and capillaries, flushing
(red/hives), decreased SVR, decrease BP, increased
capillary perfusion
125
histamine receptors
- H1: respiratory and GI smooth muscle contraction,
pruritis and sneezing, NO release, vasodilation,
hypotension
activation: decreased AV node conduction, coronary
artery vasoconstriction, bronchiole constriction
- H2: increased GI secretion of H+, increased
HR/contractility
activation: CV effects, catecholamine release,
coronary artery vasodilation, increase gastric H+
secretion
- H3: presynaptic receptors, decreased histamine
synthesis and release
126
1st generation H1 blockers
- cause significant sedation and are not very specific
- effects: somnolence, decreased alertness, dry mouth,
blurred vision, urinary retention, impotence, tachycardia,
dysrhythmias
127
2nd generation H1 blockers
- only bind H1 receptors and are non-competitive
| - effects: QT prolongation at high doses
128
Diphenhydramine (Benadryl)
- 1st generation H1 blocker
| - inhibits alcohol dehydrogenase
129
Loratadine (Claritin)
- 2nd generation H1 blocker
130
Fexofenadine (Allegra)
- 2nd generation H1 blocker
131
H2 blocker potency
Famotidine (Pepcid) > Ranitidine (Zantac) = Nizaditine (Axid) > Cimetidine (Tagamet)
132
H2 blockers
- rapid PO absorption, extensive 1st pass metabolism,
cross BBB and placenta, avoid with renal dysfunction or
increased age or decrease dose
- uses: treatment of ulcers, GERD, allergy prophylaxis,
preop med (decrease secretion but no effect on current
H+ in gut)
- take the morning of surgery
- effects: diarrhea, headaches, may weaken the barrier to
bacteria with prolonged use
- Cimetidine inhibits cytochrome P450
133
Famotidine (Pepcid)
- pre med: 20 mg IV 30 minutes prior
| - won't change current H+ but will cause less secretion later
134
proton pump inhibitors
- ...prazoles
- longer durations than H2 blockers
- prolong inhibition of gastric acid secretion up to 24
hours
- increase gastric pH and emptying
- consider patients taking these an aspiration risk
- Prilosec, Protonix, Prevacid
- pre med: can increase gastric fluid pH if given > 3 hours
before surgery and can decrease gastric contents
135
Cromolyn
```
- inhibits antigen-induced release of histamine from mast
cells
- inhalational
- used as prophylaxis for asthma
- patients can become allergic to it
```
136
serotonin 5-HT3 receptor antagonists
- autocoid, cerebral/coronary/pulmonary vasoconstriction
- oxidized by liver and lungs and taken up by platelets
- 90% found in enterochromaffin cells of GI tract
- sites of action: GI tract, platelets, vascular system, CNS
137
5-HT1
- cerebral vasoconstriction
- agonist: Sumatriptan (Imitrex) reverses middle cerebral
artery vasodilation for treatment of migraines
138
5-HT2
- coronary artery and pulmonary vessels
- antagonist: Ketanserin attenuates vasoconstriction,
bronchoconstriction, platelet aggregation, and acts as an
alpha blocker
139
5-HT3
- nausea and vomiting, appetite, addiction, pain and
anxiety
- antagonists: Zofran, Tropisetron, Dolasetron ( 12.5 mg,
0.035 mg/kg), granisetron (0.01 mg/kg)
140
Sumatriptan
- 5-HT1 agonist
| - causes cerebral artery vasoconstriction
141
Ondansetron (Zofran)
- 5-HT3 antagonist
- related to serotonin
- decreased PONV
- effects: headache, diarrhea, increased liver enzymes
with chronic use
- pediatric dose: 0.1 mg/kg
- adult dose: 4 mg
142
Antacids
- tums
- neutralize the acid currently in the stomach by
combining with HCl
- sodium bicarbonate (tums), magnesium hydroxide (milk
of magnesia), calcium carbonate, and aluminum
hydroxide
- can cause less uptake of other PO drugs
- pre med: anecdotal, sodium bictrate best
143
Sodium Bicarbonate (Tums)
- antacid
- highly soluble, rapid action ins stomach, brief duration
- can cause alkalosis
- may increase sodium levels -- bad for heart problems
144
Magnesium Hydroxide (Milk of Magnesia)
- no acid rebound
- laxative effect
- high doses can cause hypermagnesemia leading to renal
dysfunction and neuro effects
145
Calcium Carbonate
- rapid absorption, metabolic alkalosis, hypercalcemia
| - acid rebound
146
Aluminum Hydroxide
- minimal absorption, phosphate depletion
| - decreased gastric emptying -- constipation
147
Sucralfate
coats ulcerated lesions, viscous suspension
148
Metoclopramide (Reglan)
- prokinetic
- dopamine antagonist -- not for Parkinson's
- increases gastric emptying and LES tone, relaxes
pylorus and duodenum
- good oral absorption and renal elimination (decrease
the dose in renal patients)
- preop adjunct for gastric emptying, antiemetic,
gastroparesis Tx, GERD, Dx of anterior pituitary function
- dose: 10 mg IV or 0.15 mg/kg
- effects: dry mouth, cramping, dysrhythmias,
extrapyrimidal, hirsuitism, maculopapular rash
- don't use with GI obstruction
149
Bicitra
30 ml cup of nonparticulate antacid that neutralizes stomach pH
150
Droperidol
- dopamine antagonist
- 0.625 mg dose
- significant decrease in PONV
- black boxed
151
Dexamethasone (Decadron)
- decreased NV for 24 hours
- pediatric dose: 0.1 mg/kg
- adult dose: 4-10 mg
152
beta 1
- heart -- increased heart rate, contractility, and conduction
velocity
- fat cells -- lipolysis
153
beta 2
- blood vessels -- dilation
- smooth muscle (bronchioles, uterus, kidneys, liver) --
dilation, relaxation, renin secretion, glycogenolysis,
gluconeogensis
- pancreas -- insulin secretion
154
alpha 1
- blood vessels -- constriction
- pancrease -- inhibits insulin secretion
- intestine and bladder -- relaxation, constriction of
sphincters
155
alpha 2
- postganglionic -- inhibition of NE release
- CNS -- increase in potassium
- platelets -- aggregation
156
Phentolamine
- reversible, non selective alpha antagonist
- decrease BP, reflex tachycardia, increase NE which
increases CO
- treats acute HTN emergency, pheochrmocytoma, and
ANS hyperreflexia
157
Prazosin
- reversible, alpha 1 antagonist
- decreases preload and afterload
- antiHTN, treats preop BP in patients with pheochromo,
Reynaud's dz, and BPH
158
Terazosin (Hytrin)
- reversible, alpha 1 antagonist
- relaxes smooth muscle of prostate and bladder and
systemic vasculature
- treats BPH and HTN
159
Tamulosin (Flomax)
- reversible, alpha 1 antagonist
- vesicle trigone muscle relaxation
- Tx: BPH
160
Yohimbine
- reversible alpha 2 antagonist
- increases NE release
- too much causes HTN and tachycardia
- Tx: idiopathic orthostatic hypotension, impotence
161
Phenoxybenzamine (PO)
- irreversiable, non specific alpha antagonist
- alpha 1 > alpha 2
- causes orthostatic hypotension
- prevents inhibitory action of epi on insulin secretion
- Tx: BP in pheo patients and Reynauds dz
162
Propanolol (Inderal)
- nonselective B antagonist
- decrease HR, contractility, and CO
- decreased HR last longer than decreased contractility
- Na+ retention
- hepatic metabolism
163
Beta blockers with hepatic metabolism
Propanolol, Metropolol, Labetolol, Carvedilol
164
Nadolol
- nonselective beta antagonist
- long duration of action
- Tx: HTN and angina
- insulin induced hypoglycemia, airway resistance
165
Timolol
- nonselective beta antagonist
- Tx: glaucoma -- decreases IOP by decreasing production
of aqueous humor
- decreased HR and BP with opthalmic drops
- insulin induced hypoglycemia, airway resistance
166
Sotalol
- nonselective beta antagonist
- prolongs cardiac AP by increasing refractory period
- Tx: arrhythmias
- insulin induced hypoglycemia, airway resistance,
prolonged QT leading to v tach
- don't mix with Droperidol
167
Metropolol (Lopressor)
- beta 1 antagonist
- long acting
- decreased HR and contractility
- beta 2 effects with high doses
- 1-2 mg IV, comes as 1 mg/ml
- hepatic metabolism
168
Atenolol (Tenormin), Betaxolol
- beta 1 antagonist
- Tx: HTN and angina
- renal excretion
169
Esmolol (Brevibloc)
- beta 1 antagonist
- rapid onset (5 mins), short acting (10-30 mins)
- not available PO
- half life is 9 mins
- treatment of rapid vent rate (tachycardia) and HTN
- 0.5 mg/kg IV or 0.1-0.3 mg/kg/min
- hydrolysis by plasma esterases
170
Labetolol (Normondyne)
- alpha 1 and beta 1 and 2 antagonist
- a:B is 3:1 PO and 7:1 IV
- works in 5-10 mins
- half life is 5 hours
- decresased SVR, decreased HR, unchanged CO
- bronchospasm in asthmatics
- 0.1-0.5 mg/kg
- hepatic metabolism
171
Carvedilol (Coreg)
- beta and alpha 1 antagonist
- B:a = 10:1
- Tx: essential HTN, symptomatic heart failure
- edema, dizziness, bradycardia, hypotension, nausea,
diarrhea, blurred vision
- hepatic metabolism
172
reversal of BB
atropine
173
Side effects/therapeutic effects of BB
- negative inotropic and chronotropic effects
- AV node conduction decreased
- accentuates AV block (don't use if pt has AV block)
- increase concentrations of LA, fentanyl
- decrease MAC level necessary
- rebound symptoms with abrupt discontinuation
- aggravation of asthma
- coldness in extremities
- impaired response to anaphylactic shock
174
first line treatment of HTN
- in patients > 55 years old, CCB or thiazide diuretics
| - in patients < 55 years old, ACEi or ARB (sartans)
175
treatment of BB overdose
glucagon
176
BB and airway resistance
Nadolol, Timolol, Sotalol, Labetolol
177
BB effect on ECG
prolong QT, PR, and QRS
178
alpha 2 agonists
- decrease the release of NE via NE inhibition
- sympatholytics
- anesthetic adjuvants for analgesia
- Clonidine and Dexemetomidine
179
Clonidine
- alpha agonist
- mostly alpha 2 effects (a2:a1 is 200:1)
- antiHTN, used in withdrawal, can be administered
neuraxially
- adverse effects: reflex HTN crisis
- patch for opioid withdrawal, sedative, diagnosis of pheo
180
Dexmetomidate (Precedex)
- short acting alpha 2 agonist
- possesses anxiolytic, hypnotic, and analgesic properties
- easily aroused but comfortable while on infusion
- used in ICU
- side effects: hypotension and bradycardia
- caution with hypovolemia, hypotension, elderly, heart
block, vent dysfunction, DM, chronic HTN
- 1 mcg/kg over 10 mins or 0.2-0.7 mcg/kg/hour
- lack of respiratory depression and decreased need for
opioids
181
Effects of insulin administration
- carries glucose across cell membranes, enhances
glucose phosphorylation in cells, increases glucose and
K+ entry into adipose and muscle tissue, increased
synthesis of glycogon, protein, and fatty acid
- decreases glycogenolysis, gluconeogensis, ketogenesis,
lipolysis, and protein catabolism
182
potassium levels after insulin
- decrease
- can be used for treatment of hyperkalemia -- 10 units of
insulin and 25-50 g glucose as D50W
183
molecular structure of insulin
- 2 amino acid chains held together by 3 disulfide bonds
| - synthesized in beta cells of islets of langerhans
184
characteristics of insulin
- elimination: 5-10 mins (IV)
- metabolism: kidneys and liver
- duration: 30-60 mins
- basal rate: 1 unit/hr, 40 units/day
185
Lispro
- very rapid acting insulin analogue
- injected prior to meal
- bolus insulin
- onset: 5-15 mins, peak: 1 hour, duration: 4-5 hours
186
Regular (CZI)
- rapid acting bolus insulin
- IV (fastest) and SQ administration
- abrupt onset of hyperglycemia, ketoacidosis
- onset: 30 mins, peak: 2-3 hours, duration: 5-8 hours
187
Isophane (NPH)
- intermediate acting basal insulin
- 0.005 mg/U protamine
- SQ absorption decreased because of protamine
- onset: 2-5 hours, peak: variable, duration: 4-12 hours
- NPH: Neutral Protamine Hagedorn
188
Ultralente
- long acting basal insulin
- large particle size and crystal formation
- no intraop use, not available IV
- onset: slow, peak: 10-14 hours, duration: 18-24 hours
189
Insulin durations
ASPART < Lispro < Regular < Isophane < Ultralente
190
ASPART (Novalog)
- onset: 15-30 mins
- peak: 1-2 hours
- duration: 2-4 hours
191
Insulin correction doses
- 1 unit lowers blood glucose 25-30 mg/dl
| - units/hour: (blood glucose - 100)/40
192
Exubera
- inhaled insulin
| - helps lower A1C levels when combined with oral agents
193
Hypoglycemia
- diphoresis, tachycardia, htN
- mental confusion, seizures and coma, brain death
- Tx: 50-100 ml of 50% glucose solution IV or glucagon
0. 5-1 mg SQ (N/V)
194
insulin resistance
- patients requiring > 100 units a day
- acute: associated with trauma, increased cortisol
- chronic: insulin antibodies form, sulfonylureas
195
insulin and drug interactions
- epi -- inhibits secretion of insulin
- AB (tetracycline and chloramphenicol) and salicylates --
inc duration of action of insulin and may have direct
hypoglycemic effects
- MAOi -- potentiate hypoglycemic effects
196
Glyburide
- oral insulin
- sulfonylurea
- stimulates insulin secretion
- hypoglycemia risk
- decreases hepatic production of VLDL
- only treats DMII
- high protein binding (90-95% albumin)
- metabolism: liver and kidneys
- crosses placenta and causes fetal hypoglycemia
- primary failure: 20% of DMII don't respond to max dose
- secondary failure: 10-15% stop responding
197
Repaglinide
- oral insulin
- meglitinides
- stimulate insulin secretion
- risk of hypoglycemia
198
Metformin
- oral insulin
- biguanide
- inhibits glucose production by the liver
- low risk of hypoglycemia
- not bound to plasma proteins
- completely eliminated by kidneys (avoid in renal dz)
- must take 2-3 times a day
- used if sulfonylurea tx failed
- anorexia, nausea, diarrhea, lactic acidosis*
199
Acarbose
- alpha-glucosidase inhibitor
- slow digestion and absorption of carbs
- doesn't induce hypoglycemia
- can be used with insulin
- flatulence, abdominal cramping, diarrhea
200
Glipizide and allergy
2nd generation sulfonylurea
201
Dobutamine
- sympathomimetic ionotrope
- increase CO, coronary BF, mO2 supply
- decrease PVR, LV filling pressure, mO2 demand
- use: CHF and CAD
- alpha 1 and beta 1 and 2
- increase contractility
- 4 mg/ml
202
Dopamine
- sympathomimetic ionotrope
- increases CO, MAP, mO2 supply and demand
- use: shock, support BP
- alpha 1/2, beta 1/2, DA 1/2
- increases contractility
- 400 mg in 10 mg D5W
203
Epinephrine
- sympathomimetic vasopressor
- increases CO, HR, MAP, bronchodilation, mO2 demand
- use: anaphylaxis, v fib
- alpha 1/2, beta 1/2
- increases contractility
- 1 mg/ml
- infusion: 1 mg in 250 ml D5W
204
Milrinone
- phosphodiesterase inhibitor, ionotrope and vasodilator
- decrease MAP, SVR, PA pressures, LV filling pressures
- uses: arterial/venous vasodilation
- decreases afterload
- 1 mg/ml
205
Nicardipine
- CCB
- decrease MAP, mO2 demand
- increase HR, coronary BF, mO2 supply
- use: angina, HTN, arterial vasodilator
- decreases afterload
- supplied 25 mg/10 ml
206
NTG
- nitrate vasodilator
- decrease PVR, Ca, mO2 demand
- increase HR, mO2 supply
- A/V vasodilation, CAD
- decrease afterload
- dilution: 100 mcg/ml
207
Nitroprusside
- nitrate vasodilator
- decrease PVR, Ca
- increase HR
- use: A/V vasodilator
- decrease afterload
- dilution: 100 mcg/ml
208
Norepinephrine
- sympathomimetic vasopressor
- decrease HR
- increase MAP, PVR, mO2 demand
- A/V vasoconstriction
- alpha 1/2 and beta 1
- increase afterload
- 4 mg/ml
- infusion: 4 mg in 500 ml D5W
209
Phenylephrine
- sympathetic non-catechol vasopressor
- decrease HR, CO
- increase MAP, PVR, coronary BF
- use: hypotension with tachycardia
- alpha 1/2 and beta 1
- increase afterload
210
Vasopressin
- ADH vasopressor
- increases PVR
- use: arterial vasocontriction, refractory hypotension and
SVR
- V1/2
- 20 U/ml
