Pharmacology Flashcards
Heparin
[half-life elimination time]
1 -2 hours
2-Chloroprocaine
[rapid onset]
able to use high concentrations due to its low systemic toxicitiy
- unlike normally, does not depend on PKa, which is about 9 and thus more pronated (less likely to cross cell membrane) at physiologic pH
5-HT3
[receptor]
serotonin on platelets and GI tract
Adrenergic Agonists
[which 2 have the greatest increase on CO]
isoproterenol and dobutamien
Adrengergic Agonists
[which 2 cause a large decrease in renal blood flow]
phenylephrine and norepinephrine
Agents
[effect on SA node]
depresses SA node automaticity
- only modest effects on AV node; explains the occurrence of junctional tachycardia when administering an anticholinergic during inhalation anesthesia
Agents
[effects on blood pressure]
decrease
- Des, Sevo, and Iso decrease blood pressure due to a decrease in systemic vascular resistance
- halothane depression is due to decreases in myocardial contractility and cardiac output
Agents
[effects on cardiac output]
minimal decrease
Agents
[effects on CVP]
slight increase except for Sevoflurane
- However, around 1.5 MAC, sevo will show an increase in CVP, then drop again
Agents
[effects on heart rate]
increase heart rate
- Sevoflurane only increases HR when MAC > 1.5
- halothane has no effect on heart rate
Agents
[effects on minute ventilation]
decrease
- increase respiratory rate while decreasing tidal volume
- except for Isoflurane
Agents
[effects on pulmonary vascular resistance]
little to no effect
Agents
[effects on systemic vascular resistance]
decrease SVR
Agents
[ventilatory response]
decrease response to incrasing PaCO2
- Desflurane above 1 MAC has the greatest effect
Agents
[best for ablative procedures]
Sevoflurane
- no effect on AV conduction
- Isoflurane increases the refractoriness of accessory pathways
Alpha Blockers
[examples]
prazosin
phentolamine
phenoxybenzamine
Alpha-1 Agonists
[cardiovascular effects]
vasoconstriction
leading to an increase in peripheral vascular resistance, left ventricular afterload, and atrial blood pressure
Alpha-1 Agonist
[mechanism of action]
increase intracellular [Ca2+] leading to contraction of smooth muscles
Alpha-2 Agonists
[cardiovascular effects]
reduction of sympathetic outflow
peripheral vasodilation and lower blood pressure
Alpha-2 Agonists
[mechanism of action]
inhibits adenylate cyclase activity
- decreases the entry of calcium ions into neuronal terminal, which limits exit of norepinephrine
anesthetic agent with low potency and poor blood solubility
Desflurane
(and N2O)
Anti-Arrhythmic Agents
[Class I - type]
Na+ channel blocker
- blocks voltage-gated Na+ channels and decreases the slope of phase 0 (Vmax)
Anti-Arrhytmic Agents
[Class III - examples]
amiodarone and sotalol
Anti-Arrhytmic Agents
[largest increase in QT interval]
amiodarone
Anti-Arrhytmic Agents
[best for supraventricular arrhythmias]
adenosine
Anti-Arrhytmic Agents
[class I - examples]
quinidine
lidocaine
phenytoin
flecainide
Anti-Arrhytmic Agents
[Class II - examples]
esmolol and metoprolol
Anti-Arrhytmic Agents
[class II - type]
beta blocker
Anti-Arrhytmic Agents
[class III - type]
K+ channel blocker
- prolongs repolarization
Anti-Arrhytmic Agents
[Class IV - examples]
verapamil and diltiazem
Anti-Arrhytmic Agents
[class IV - type]
Ca2+ channel blocker
- blocks slow calcium channels
Anticholinergics
[effects on cardiovascular system]
tachycardia
- blockade of muscarinic receptors in the SA node
Anticholinergics
[respiratory effects]
decrease secretions
bronchodilation
Anticholinesterase
[muscarinic effects on gastrointestinal system]
increased spasm and salvation
Anticholinesterase
[muscarinic side effects on cardiovascular system]
decreased heart rate and bradyarrhythmias
Anticholinesterase
[muscarinic side effets on pulmonary system]
bronchospasm
Antimuscarinics
[3 examples]
atropine
scopolamine
glycopyrrolate
Atracurium
[metabolism]
ester hydrolysis and hofmann elimination
Atracurium
[side effects]
histamine release
- avoid in severe asthmatics
Atropine
[anti-sialagogue IM dose]
0.01 - 0.02 mg/kg
Barbiturates
[effect on ICP]
greatest decrease in ICP
Barbiturates
[effect on seizure threshold]
lowers seizure threshold
Barbiturates
[effects on cerebral physiology]
decrease CMR, CBF, and ICP
Benzodiazepines
[effects on cerebral physiology]
slightly decreases CMR, CBF, and ICP
Benzodiazepines
[mechanism of action]
enhance GABA receptor affinity, but do not directly activate
Benzodiazepines
[pregnancy and labor]
crosses placenta and may lead to CNS depression
- may increase risk of cleft lip/palate when given during first trimester
Bleomycin
[adverse effects]
pulmonary fibrosis
Bronchodilators
[order of effectiveness]
Beta agonists
glucocorticoids
leukotriene blockers
mast-cell stabilizers
theophyllines
anticholinergics
Bupivacaine
(marcaine)
[duration of action]
5 - 15 hours (anesthesia)
- epinephrine is less effective in prolonging anesthesia because duration of action is independent of local blood flow
Calcium Channel Blockers
[greatest risk of SVT]
verapamil and diltiazem
Cerebral Vasospasm
[treatment]
Nimodipine
Cisatracurium
[metabolism]
Hofmann elimination
Cisplatin
[adverse effects]
renal impairment
Clomipramine
[drug class]
tricyclic anti-depressant
Clomipramine
[treatment]
obsessive-compulsive disorder
Clonidine
(catapres)
[mechanism of action]
alpha-2 agonist
- less selective and longer acting than dexmedetomidine (precedex)
Context Sensitive Half-Time
[definition]
time necessary for the plasma drug concentration to decrease 50% after discontinuing a continuous infusion
Coronary Steal Syndrome
theory that coronary vasodilators that target smaller coronary vessels would redistribute blood from ischemic to nonischemic areas
- Examples: Isoflurane, adenosine, dipyridamole, and nitroprusside
- not clinically proven
Creatinine Clearance
[equation estimate]
[140 - age] x kg
divided by
72 x [creatinine%]
- multiply by 85% for women
- “Cockroft and Gault” equation
Cryoprecipitate
[components]
von willebrands
fibrinogen
factor VIII and XIII
Cyclosporine
[mechanism of action]
calcineurin inhibitor
Cyclosporine
[treatment]
immunosuppression for organ transplant
Anesthetic implications of decreased SVR
- excess perfusion relative to oxygen needs
- loss of body heat due to increase cutaneous blood flow
- enhanced delivery of drugs to NMJ
Desflurane
[vaporizer]
desflurane is heated to 39oC to raise its partial pressure to 1,500 mmHg
- ensures a constant concentration despite changes in barometric pressure or temperature
Desflurane
[Blood:Gas]
0.42
Desflurane
[Brand name]
Suprane
Desflurane
[MAC]
6.0
Desflurane
[vapor pressure]
660
Dexmedetomidine
(precedex)
[adverse effects]
antimuscarinic effects
- dry mouth and blurred vision
Dexmedetomidine
(precedex)
[mechanism of action]
alpha-2 agonist
Dexmedetomidine
[receptor selectivity]
alpha-2 > alpha-1
Dextrose 5%
[osmolarity]
252
Diffusion Hypoxia
occurs with abrubtly ending inhalation of N2O
Diuretics
[3 K+-Sparing Examples]
Spironolactone (aldactone)
Triamterene (dyrenium)
amiloride (midamor)
Diuretics
[4 Loop Examples]
Furosemide (lasix)
Bumetanide (bumex)
Torasemide (demadex)
Ethacrynic acid (edecrin)
Dobutamine
[effects]
enhances cardiac output without changing blood pressure
Dobutamine
[receptor selectivity]
Beta-1 >> beta-2
Droperidol
[mechanism of action]
D2 Antagonist
Droperidol
[side effets]
dystonia
QT prolongation
decreased seizure threshold
Drugs causing decreased renal perfusion
NSAIDS
ACE inhibitors
IV contrast
cyclosporines
drugs causing direct tubular injury
aminoglycosides
IV contrast
heavy metals
myoglobin and hemoglobin
HIV protease
Edrophonium
[reversal dose of Atropine]
0.014 mg per mg of anti-cholinesterase
Effect on MAC
[hypernatremia]
increase
Effect on MAC
[alpha-2 agonists]
decrease
Effect on MAC
[Cyclosporine]
increase
Effect on MAC
[hyperthermia]
increases
Effect on MAC
[hyponatremia]
decrease
Effect on MAC
[Lidocaine]
decrease
Epinephrine
[receptor selectivity]
Beta-1 > alpha-1 = alpha-2 = beta-2
Esmolol
[cardiovascular effects]
lowers heart rate and, to a lesser extent, blood pressure
Etomidate
[Adrenocortical Suppression]
inhibits converstion of cholesterol to cortisol through 11-beta-hydroxylase
- avoid in septic or hemorrhaging patients
- usually only seen in infusions or repeated doses
Etomidate
[drug interactions]
fentanyl prolongs half-life
opioids decrease myoclonus
Etomidate
[mechanism of action]
GABAA agonist
First Pass Hepatic Effect
[which route of administration?]
oral
First Pass Hepatic Effect
GI tract to portal venous blood to liver before entering systemic circulation
- greatly reduces available drug
Flumazenil
(imidazobenzodiazepine)
[contraindications]
tricyclic anti-depressants
patients taking benzos for control of seizures
Flumazenil
(imidazobenzodiazepine)
[mechanism of action]
competitive antagonist of benzodiazepine binding site on GABAA receptors
H1 Antagonists
[2 examples]
diphenhydramine (benadryl)
promethazine (phenergan)
H2 antagonist
[gastrointestinal effects]
decreases gastric acid secretion from parietal cells
Halothane Hepatitis
[risk factors]
female, obese, middle aged, and multiple halothane exposures
Halothane
[cardiac risks]
slows conduction through SA node
- predisoposes patients to junctional arrhythmias and bradycardia
Histamine
[cardiovascular effects]
lowers blood pressure
increases HR and contractility
Ionized Drugs
[characteristics]
inactive
water soluble
cannot cross BBB or undergo hepatic metabolism
can be excreted renally
Isoflurane
[Blood:Gas]
1.5
Isoflurane
[brand name]
Florane
Isoflurane
[MAC]
1.2
Isoflurane
[vapor pressure]
238
Isoflurane
[why is emergence quicker than induction?]
agent continues to be absorbed by peripheral tissues dueing emergence
Ketamine
[adverse effects]
increased oral secretions
myoclonic movements
increased ICP
ocular effects
difficulty to assess anesthetic depth
Ketamine
[cardiovascular effects]
increases BP, HR, and CO
- when administered with a smalld ose of benzodiazepine or Propofol, sympathetic stimulation can be blunted or eliminated
Ketamine
[effects on cerebral physiology]
increase CBF and ICP
Ketamine
[mechanism of action]
NMDA antagonist
Ketamine
[ocular effects]
diplopia
mydriasis
nystagmus
blepharospasm
increased intraocular pressure
Ketorolac
[contraindications]
kidney failure and allergy to NSAIDs
- relative contraindications:
- asthma, risk of hemorrhage
Ketorolac
[equivalence to morphine]
standard dose of Ketorolac equals 6-12 mg of morphine
Ketorolac
[mechanism of action]
NSAID that inhibits prostaglandin synthesis
Labetalol
[cardiovascular effects]
lowers blood pressure without increasing heart rate
Lactated Ringer
[components]
Na+, Cl-, K+, Ca2+, and lactate
Lactated Ringer
[osmolarity]
273
Lidocaine
[effects on cerebral physiology]
decrease CMR, CBF, and ICP
Local Anesthetics
[cardiovascular effects]
depress myocardial automaticity
(spontaneous phase IV depolarization)
- can decrease contractility and conduction velocity at high concentrations
- inhibit nitric oxide, causing vasoconstriction
local anesthetics
[sodium bicarb]
shortens onset time
- alkinalizes drug
Loop Diuretics
[adverse effects]
- Hypo-
- K+, Ca2+, Mg2+
- Hyperglycemia
- metabolic alkalosis
Mannitol
[contraindications]
intracranial aneurysm
arteriovenous malformations
intracranial hemorrhage until open
Mannitol
[dose]
0.25 - 1 g/kg
Meperidine
(demerol)
[drug interactions]
monoamine oxidase inhibitors
- delirium or fatal hyperthermia
Metabolism
[4 basic pathways of metabolism]
oxidation
reduction
hydrolysis
conjugation
Metabolism
[phase I reactions]
reduction
hydrolysis
oxidation
Metoclopromide
[drug interactions]
blocked by anti-muscarinic drugs
increased side effects with droperidol
Metoclopromide
[black box warnings]
tardive dyskinesia
Metoclopromide
[contraindications]
GI obstruction
Parkinson’s
Pheochromocytoma
Metoclopromide
[drug class]
dopamine-2 antagonist
Minimal Alveolar Concentration
[definition]
concentration at 1 atm that prevents skeletal muscle movement in response to supramaximal stimulus in 50% of patients
muscle relaxants
[effect of respiratory acidosis]
potentiates blockade of NDMR and antagonizes reversal
- may prevent recovery in hypoventilating post-operative patients
Muscle Relaxants
[effects of Magnesium]
potentiates blockade
- competes with calcium at motor end-plate
Naloxone
[adverse effects]
may precipitate pulmonary edema and cardiac arrest
(rare)
Naloxone
[mechanism of action]
opioid antagonist
Cerebral Palsy
[response to NDMR]
resistance
Neostigmine
[onset and peak]
will see effects in 5 minutes
peaks at 10 min
Nitrates
[vascular effects]
venodilator > arterial dilator
- decrease preload
Nitroglycerin
[vascular effects]
venous dilation > arterial dilation
Nitrous can safely be administered in retinal reattachment surgeries as long as it is discontinued ____ minutes prior to bubble injection
15 minutes
Nitrous Oxide
[Blood:Gas]
0.47
Nitrous Oxide
[contraindictations]
COPD with blebs
venous air embolism
pneumothorax and pneumocephalus
acut intestinal obstruction
tympanic membrane
intraocular procedures
Nitrous Oxide
[duration of analgesic effects]
20 minutes
Nitrous Oxide
[effect on pulmonary vascular resistance]
increase PVR
- especially in patients with pre-existing pulmonary hypertension
Nitrous Oxide
[effect on vitamin B12]
inhibits vitamin B12 synthesis
- use with caution in pregnant patients and those deficient of the vitamin
Nitrous Oxide
[effects on right-to-left intracardiac shunt]
may increase shunting of blood and further jeapordize arterial oxygenation
Nitrous Oxide
[MAC]
104
NMDA Antagonists
[reason for neuroprotection]
during ischemia, [K+]i decreases and [Na+]i increases causing [Ca2+]i to increase
leads to release of glutamate which acts on the NMDA receptor, enhancing Ca2+ entry
Norepinephrine
[receptor selectivity]
alpha-1 = alpha-2 = beta-1
Norepinephrine
[cardiovascular effects]
arterial and venous vasoconstriction
- increased myocardial contractility
- rise in systolic and diastolic pressures
- However, increased afterload and reflex bradycardia prevent rise in cardiac output
Normal Saline
[osmolarity]
308
Normal Saline
[components]
Na+ and Cl-
Normothermic Shivering
[treatment]
meperidine (25-50mg)
clorpromazine (10-25mg)
butorphanol (1-2mg)
Ondanesetron
[mechanism of action]
5-HT3 antagonist
Ondanestron
[side effects]
dizziness, headache, QT prolongation
Ondansetron
[brand name]
Zofran
Opioids
[allergic reactions]
rare, although some anaphylactoid reactions may occur
- secondary to histamine release following morphine or meperidine
Opioids
[gastrointestinal effets]
decrease gastric emptying
increase biliary pressure
sphincter of Oddi spasms
Pancuronium
[allergic reactions]
patients who are hypersensitive to bromides may exhibit allergic reactions
Pancuronium
[arrhythmias]
predisposition to ventricular dysrhythmias
- increased atrioventricular conduction and catacholamine release
- avoid in combination with tricyclic anti-depressants and halothane
Pancuronium
[side effects]
hypertension and tachycardia via vagal response
arrhythmias
Phenelzine
[adverse effects]
decreases plasma cholinesterase activity
Phenylephrine
[receptor selectivity]
alpha-1 >> alpha-2
Phenytoin
[mechanism of action]
voltage-gated Na+ channel blocker
Physostigmine
[treatment]
anti-cholinergic toxicity
Plasmalyte
[osmolarity]
294
Plasmalyte
[components]
Na+, Cl-, K+, Mg2+, gluconate, and acetate
Propofol Infusion Syndrome
Prolonged high-dose infusions of Propofol that can lead to cardiac failure, rhabdomyolysis, metabolic acidosis, and kidney failure
Propofol
[effects on cerebral physiology]
decreases CMR, CBF, and ICP
Propofol
[lipid disorders]
due to its lipid emulsion, should be used cautiously in patients with disorders of lipid metabolism
- examples: hyperlipidemia and pancreatitis
Propofol
[mechanism of action]
GABAA agonist
- increased chloride conductance, resulting in hyperpolarization of the post-synaptic cell membrane and functional inhibition
Prostaglandin Inhibitors
[patent ductus arteriosus]
promote closure of persistent PDA
- specifically Ibuprofen and indomethacin
Most acidic drugs bind to _____, whereas basic drugs bind to _____.
albumin (acidic)
alpha-1 glycoprotein (basic)
Proton Pump Inhibitors
[mechanism of action]
bind to proton-pump on parietal cells in the gastric mucosa and inhibit H+ secretion
Pseudocholinesterase Deficiency
[drugs known to decrease activity]
Echothiophate
neostigmine
phenelzine
metoclopromide
esmolol
pancuronium
oral contraceptives
Pulmonary Hypertension
[treatment]
nitric oxide
“The speed in an inhalation induction is slowed by right-to-left shunting. The change in the rate of induction is LEAST pronounced when using _____”
Isoflurane
- right-to-left shunting more pronounced with high blood:gas solubilities
Which inhalational agent is most likely associated with a junctional rhythm?
halothane
The rate of _____ determines the rate of induction with volatile agents
FA/FI
Which of the following is most responsible
for maintenance of cardiac output during isoflurane
administration?
increased heart rate
- results in maintenance of cardiac output due to preserved carotid baroreceptor reflex
“Desflurane vaporizer dial must be set ______ at higher elevations”
(higher or lower)
higher
“For intermediate-acting NDMR, a palpable post-tetanic twtich appears about _____ before spontaneous recovery of the first TOF twitch”
10 minutes
“Time to recovery is prolonged in proportion to the duration of anesthesia for which agents?”
soluble anesthetics
(isoflourane and halothane)
Rocuronium
[metabolism and excretion]
no metabolism
eliminated mostly by liver
Second Gas Effect
high-volume uptake of one gas accelerates the rate of increase of the alveolar pressure of a concurrently administered “second” gas
Seizure
[treatment]
Propofol (50-100mg)
phenytoin (500-1000 mg slowly)
midazolam (1-5mg)
Sevoflurane
[brand name]
Ultane
Sevoflurane
[Blood:Gas]
0.65
Sevoflurane
[MAC]
2.4
Sevoflurane
[vapor pressure]
160
Sodium Nitroprusside
[adverse effects]
cyanide toxicity
- metabolic acidosis, cardiac arrhythmias, and increased venous oxygen content
Speed of Induction
[effects of right-to-left shunt]
slow induction
Speed of Induction
[relationship to Cardiac Output]
inverse relationship
- an increased cardiac output results in a rapid uptake and therefore a slower induction
- CO mostly influeces soluble anesthetics
- Example: Isoflurane
St. John’s Wort
[adverse drug interactions]
MAO inhibitors and Meperidine
- increased risk of serotonin syndrome
Amyotrophic Lateral Sclerosis
[response to Succinylcholine]
contractures
Myasthenia Gravis
[response to Succinylcholine]
resistant
Autoimmune disorders
[response to Succinylcholine]
hypersensitivity
Sulfonamides
[risks in neonates]
displaces uconjugated bilirubin from binding sites on albumin, leading to bilirubin encephalopathy
Thiazide Diuretics
[adverse effects]
- Hypo-
- K+, Na+, Mg2+
- Hyper-
- glycemia, uricemia, lipidemia, Ca2+
Tricyclic Anti-depressants
[drugs to avoid]
indirect-acting vasopressors and those with sympathetic stimulation
- pancuronium, ketamine, meperidine, and local with epi
Valproic Acid
(depakote)
[drug interactions]
benzodiazepines
- may precipitate a psychotic episode
Valproic Acid
[mechanism of action]
increases GABA and inhibitis NMDA
Valproic Acid
(depakote or valproate)
[treatment]
seizures and bipolar disorder
Vecuronium
[metabolism]
biliary excretion
(some renal)
Vincristine
[adverse effects]
neuropathy
volatile agents
[effect on dead space]
increase
- due to the decrease in tidal volume
volatile agents
[effects on cerebral physiology]
decrease CMR, but increase CBF and ICP
volatile agents
[effects on PaCO2]
increase