Pulmonary Pharamacology Flashcards
With the use of BETA-2 adrenergic Agonist, cAMP________in SMOOTH muscle
INCREASES
BETA-2 and an increase in cAMP will__________myosin light chain kinase
Inhibit
Inhibition of MLCK and an increase in cAMP will cause_______
SMOOTH muscle relaxation
Albuterol, Levalbuterol, Salmeterol, and Formoterol are examples of
INHALED BETA-2 Adgrenergic Agonsist
Salbutamol, Epinephrine, and Terbutaline are examples of
IV BETA-2 Adrenergic Agonsist
List Effects of using BETA-2. Adrenergic Agonsists
Bronchodilation
Vasodilation
Stimulation of NaK ATPase
Release of Glucagon
Decreased DBP
SIDE EFFECTS of BETA-2
Tremor
Tachycardia
HYPERglycemia
HYPOkalemia/magnesia
Decreased PaO2 (vasodilate in poorly ventilated lung-shunting)
Tolerance
Withdrawl
Patient on a non-selective BETA agonists can
target BETA-1
What medication is the prototype for inhaled BETA-2
Albuterol (little effect on heart)
Onset 5-10min
PO onset 15-30min
Duration 4-6 hours
Dose (acute) 4-8 puffs (90mcg/puff)
Racemic EPI can relieve _______ and _________
Airway Obstruction & Edema
What is the dose of Racemic EPI?
0.5mL of 2.25% IN 4mL NS
Muscarinic Antagonist (Anticholinergics) MOA
stops binding of ACh to M3 receptors, stops Gq, inactivates phospholipase C and IP3, causing bronchodilation
SIDE EFFECTS of M3 antagonists
Tachycardia
Dry Mouth
Blurred Vision
Mydriasis
GI upset
Nausea
Urinary retention
Tremors
Common M3 antagonist drugs
Ipratropium
Tiotropium
Atropine
Glycopyrrolate
Which M3 antagonist medication is short acting?
Ipratropium- good for COPD
Which M3 antagonist medication is long acting?
Tiotropium
Atropine can cross the ________and cause CNS effects
Blood Brain Barrier
What medication is a Methylhxanthine?
Theophylline
How do Methylxanthines work (MOA)?
Inhibit Phosphodiesterase, which stops the breakdown of cAMP, causing relaxation
Methylxanthines also decrease______&_____
Eosinophils & Neutrophils
Methylxanthines can also block________, which ________release of _______, _______, and ________
Adenosine; decreases; ACh; histamine; leukotrienes
What are the SIDE EFFECTS of using Methylzanthines?
GERD
GI upset
N/V
Restlessness
SEIZURES
ARRHYTHMIAS
DEATH
What is the toxic level of Methylxanthines (Theophylline)
> 20mcg/mL
MOA of Corticosteroids
Alter genetic expression of pro-inflammatory mediators & inflammatory gene products
(effects DNA transcription in ability to form certain proteins)
List of Corticosteroids
Fluticasone
Mometasone
Methylprednisolone
*Prednisone
Hydrocortisone
Fluticasone/Salmeterol
Budesonside/Formoterol
What are some SIDE EFFECTS of Corticosteroids?
Infection
HYPERglycemia
HTN
Adrenal Suppression
Psychosis
Ulcers
Osteoporosis
MOA for Leukotriene Modifiers
They block the conversion of Arachidonic Acid to leukotriene
Block leukotriene receptors
What medications are Leukotriene Modifiers?
Montelukast & Zileuton
What medications are Mast Cell Stabilizers?
Cromolyn Sodium & Nedocromil
MOA of Mast Cell Stabilizers
Stabilize mast cell by blocking mast cell degranulation, block release of histamine, block bronchoconstriction, mucosal edema and secretion
Which volatile anesthetics DO NOT decrease bronchomotor tone?
DESflurane & Nitrous Oxide
Which channels are sensitive to volatile anesthetics?
T-type Ca+ channels
Which IV anesthetics decrease bronchomotor tone?
Propofol, Ketamine, & Midazolam
What adjuncts can suppress cough, relax ASM, and blunt hemodynamic response to airway manipulation?
Local Anesthetics
Magnesium Sulfate can
improve bronchodilation and can be given via IV or NEB treatment
Beta agonist activate
adenylate cyclase, which activates an increase in cAMP
Methylxanthines block________, which increases cAMP and promotes vasodilation
PDE(phosphodiesterase and blocks adenosine
M3 antagonist block
ACh, promoting bronchodilation
cAMP________in VASCULAR smooth muscle when agonist bind Gs couple receptors
INCREASES, causing a decrease in vascular tone
IP (prostacycline) has the same affects as
Beta-2
Alpha-2 bind to Gi protein, causing cAMP to ________in the vascular smooth muscle, ________vascular tone
DECREASE; increase (activates MLCK)
An ______in cAMP will ______MLCK, causing________
increase; inhibit; relaxation
Endothelin-1 is a potent
vasoCONTRICTOR
What receptors are bound to Gq proteins?
Alpha-1, ET-A, and M3
What happens to IP3 levels in vascular smooth muscle when agonist bind to Gq receptors?
IP3 increases, causing an increased release in Ca+, causing contraction of vascular tone
Alpha-1 binds
catecholamines
Increased cGMP causes
relaxation
L-arginine breaks down into
Nitric Oxide, influenced by blood flow (sheering force), which releases Ca+ and increases the formation of nitric oxide and nitric oxide synthase
What are the 3 mechanisms for cGMP?
Inhibits Ca+ entry
Activates K+channels (hyperpolarizing)
Activates MLCP (not MLCK), to breakdown MLCK
ALL causing VASODILATION
What medications are used to treat PH?
Inhaled nitric oxide
Phosphodiesterase inhibitors
Endothelin receptor antagonists
Prostacyclin Derivatives
Prostaglandins
Should PH therapy be discontinued?
NO!!
How do you avoid increases in Pulmonary Vascular Resistance?
Avoid:
Hypoxia
Hypercarbia
Acidosis
Pain
Hypothermia
Ketamine
Nitrous
Avoid Large deceases in SVR
Preserve Preload, CO, & perfusion
Use vasopressors for intra-op HOTN
What medication can either improve or have no harmful effects on PH
Etomidate
Opioids
Low Volatile agent Concentrations
Decreased flow through the lungs to the _______will affect CO
Right side of the heart
Inhaled Nitric Oxide treats PH by
activating guanyl cyclase to increase cGMP and improves perfusion. to ventilated lung units
Inhaled Nitric Oxide causes vaso/broncho_______& is an anti______, _____, and ______
Dilation; thrombotic, inflammatory, and proliferative
Giving systemic sodium nitroprusside, nitroglycerinne, prostraglandin I2, and PDE5 inhibitors will
worsen any shunt since medications given systemically will oncrease blood flow to areas that are NOT vented well
Inhaled therapy is better because it causes
localized effects
In treating PH, phosphodiesterase inhibitors
increase and prevent the breakdown of cGMP and cAMP, decrease Ca+ levels, causing vasodilation and smooth muscle relaxation
What medications are PDE inhibitors?
Milrinone, Sildenafil, & Tadalafil
PDE inhibitors in myocardial cells are ________ _______
Positive inotropes
PDE inhibitors in the systemic vasculature cause
Vasodilation & Hypotension
Which PDE inhibitors are present in high amounts in the lungs?
PDE-5
SIDE EFFECTS of PDE5 inhibitors
Headache
Nasal Congestion
Dyspepsia (indigestion)
Flushing
Priapism (prolonged erection)
MOA of Endothelin Receptor Antagonists in the treatment of PH
Block ET-A &/or ET-B, relaxing vascular smooth muscle, decrease smooth muscle cell proliferation
What medications are considered Endothelin Receptor Antagonists
Bosentan & Ambrisentan
What are the SIDE EFFECTS of Endothelin receptor antagoonosist?
Side effects are related to vasodilatory properties (like flushing)
What are Prostacyclin Derivatives/Prostaglandin medications?
Epoprostenol, Iloprost, Prostacyclin,Trepostinil, & Remodulin (IV)
MOA of Prostacyclin Derivatives/Prostaglandins
Increase PGI2 to target IP receptors, inhibit smooth muscle cell growth & platelet aggregation, improve oxygenation.
(all results in relaxation of vascular smooth muscle)
