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A comprehensive set of questions and answers covering key concepts in advanced pharmacology, specifically focusing on beta-2 adrenergic agonists, pharmacokinetics, pharmacodynamics, and antibiotic use in surgical procedures. it's valuable for students preparing for exams in advanced pharmacology courses, offering detailed explanations and clinical applications of pharmacological principles. The questions delve into drug mechanisms, absorption, distribution, metabolism, excretion, and therapeutic implications, making it a useful study resource.
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What is the preferred treatment of acute asthma episodes and prevention of exercise induced asthma?
beta 2 adrenergic agonists
How are beta 2 adrenergic agonist agents divided? (duration of action)
intermediate action (3-6 hours)
long acting (>12 hours)
What is used in COPD patients to improve air flow and exercise tolerance?
beta 2 adrenergic agonists
Why does the beta 2 adrenergic agonist, salmeterol, have such a long duration of action?
it is highly lipophilic and has a high affinity for the beta 2 receptor because of a side chain that binds to the beta 2 receptor
How can beta 2 adrenergic agonists cause tachycardia?
peripheral vasodilation and cardiac stimulation (the heart does contain some beta 2 receptors but not many. the tachycardia is mainly caused by the vasodilation and reflex tachycardia)
What is another use for beta 2 adrenergic agonists besides treatment for respiratory issues?
continuous infusions of these drugs can stop premature labor (tocolytics)
What are the routes of administration for beta 2 adrenergic agonists?
PO, inhalation, SQ, IV
inhaled is preferred due to side effects and as effective as parenteral route
What percentage of the drug dose of a beta 2 adrenergic agonist actually reaches the lungs when given via metered-dose inhaler?
12%
If given via nebulizer, how much more of a beta 2 adrenergic agonist would you need to produce the same degree of bronchodilation as with a metered-dose inhaler?
Define pharmacokinetics.
Study of how drug concentrations change as it moves through the body (what is the body doing to the drug?)
Define pharmacodynamics.
Study of how the drug is exerting its effect on the body (receptor interactions, potency, etc)
What is absorption?
process of the drug entering the systemic circulation
What is distribution?
the process of the drug being circulated/disseminated through the body
True or False. Route of administration affects drug absorption.
true
A drug moving from the vasculature to the extravascular space is part of what aspect of pharmacokinetics?
distribution
What is biotransformation performed by?
enzymes
What is occuring when molecules are added to a drug to make it more polar to enhance removal from the body?
metabolism
Define pharmacobiophysics.
The drug's concentration in the plasma and the effect site
What is concerned with the effect site concentration and clinical effect?
pharmacodynamics
What is concerned with the plasma concentration and effect site concentration?
pharmacobiophysics
liver or kidney disease
What predicts the speed of recovery when discontinuing an infusion?
context-sensitive half time
What dose is calculated by: peak concentration x Vd / bioavailability?
loading dose
What dose is calculated by: peak concentration x clearance / bioavailability?
maintenance dose (give drug at same rate is it excreted)
When giving a loading dose followed by a maintenance dose in a renal impaired patient, which dose should be changed?
maintenance should be lowered, loading stays the same
What two things does volume of distribution (Vd) assume?
the drug distributes instantly
elimination does not occur before it is distributed
True or false. The more soluble a drug is and the more it binds to peripheral tissues, the larger the Vd.
true
What are causes of a small Vd?
high protein binding and ionization
What are causes of a large Vd?
high solubility and binding in tissues other than plasma
True or False. Protein-bound drugs have an exaggerated effect.
False, they are inactive (only free drugs are active)
What is the ultimate bioavailability of a drug?
amount of drug actually used
benzodiazepines
What drugs inhibit hepatic enzymes which metabolize drugs?
antibiotics
cimetidine
If plasma concentration is increased, clearence is _____?
decreased
What part of a drug is usually active? (ionized or nonionized)
nonionized
A weak base is more or less ionized at a lower pH?
more ionized
When is steady state achieved?
after 5 half times
Clearance is indirectly proportional to what?
half life and drug concentration
Clearance is directly proportional to what?
blood flow to clearing organ and drug dose
What is zero order kinetics?
constant elimination of a drug at a set rate
What is first order kinetics?
dependent on concentration (more drug we have, the higher the elimination
What does alpha distribution describe?
drug distribution from the plasma to the tissues
When does beta distribution begin?
begins as plasma concentration falls below tissue concentration
Although most are used as racemic mixtures in clinical practice
What is the bioavailability of IV drugs?
1; all of the drug is available
If drug concentration in central compartment is increased, then clearance is?
decreased
What is minimum inhibitory concentration of antibiotics?
the lowest concentration of a given antimicrobial at which an organism's growth is inhibited.
When must prophylactic antibiotics be given? Discontinued?
within 1 hour of incision
stop within 24 hours after surgery completed
In seriously ill or immunocompromized patients, should bactericidal or bacteriostatic agents be used?
bactericidal
Why should narrow-spectrum be the first choice rather than broad-spectrum antibiotics?
to preserve normal flora
Using less than the recommended dose is only acceptable in what two conditions?
renal or hepatic dysfunction
What percentage of surgical cases are complicated by infections?
1-5%
Why are cephalosporins the choice for surgical procedures in which the skin flora and normal flora of the GI/GU tract are the most likely pathogens?
broad spectrum and low incidence of side effects
Do preop steroids for PONV effect infection rates?
no
Good glucose control decreases the incidence of deep sternal infections in CV surgery populations by how much?
50% (continuous insulin better than intermittent)
How long before surgery should smokers attempt to stop to achieve a 50% reduced risk of postop infection?
4-8 weeks
When should re-dosing occur in procedures lasting longer than 4 hours or when large blood loss occurs?
every 1-2 half lives of the antibiotic (in patients with normal renal function)
What is the most common cause of bacteremia and fungemia in the hospital?
IV catheters
How is oral absorption in the elderly altered?
decreased gastic pH
reduced GI motility
How is distribution altered in the elderly?
increased total body fat
decreased albumin
How is metabolism altered in the elderly?
decreased hepatic flow
How is excretion altered in the elderly?
decreased GFR
In elderly patients with normal serum creatinine levels, what two antibiotics need dosing adjustments, what two antibiotics do not according to the examples given?
penicillins and cephalosporins do not need adjusting due to large therapeutic index
aminoglycosides and vancomycin might need adjusting
What is the chance of a patient with a penacillin allergy having an allergic reaction to cephalosporin?
1% (however, giving cephalosporins to patients with a positive penacillin skin test is not recommended)
What replacement antibiotics should be given to patients with documented IgE- mediated anaphylactic reactions?
clindamycin and vancomycin (vanc also given when MRSA likely)
What is the drug of choice for pneumococcal, streptococcal, and meningococcal infections?
penicillins
What two agents are susceptible to beta lactamases and are ineffective against most staph aureas strains?
Penicillin G and V
Transient bacteremia is very common in what type of procedures?
dental
How much K+ does 10 million units of PCN G have?
16 mEq (this is significant in patients with renal dysfunction as neurotoxicity and hyperkalemia possible)
Instead of giving aqueous PCN G, given sodium salt of PCN G or similar drug like ampicillin
Why is intrathecal penicillin forbidden?
potent convulsant
arachnoiditis and encephalopathy
True or False. Penicillin can be mixed into an antibiotic cocktail.
False
What drug competitively inhibits renal excretion of some drugs and is used in the tx of gout?
Probenecid
How much of an IM penicillin dose is excreted within the first hour?