Pharmacology Pretest

Which organ is most associated with drug metabolism?

Comparison of amount of a drug that causes a therapeutic effect vs the amount at which it causes harm
Therapeutic range

At high doses, a drug with ___(small/large)____ therapeutic range will cause toxicity
Small therapeutic range

At high doses, a drug with ___(small/large)____ therapeutic range (aka therapeutic index aka therapeutic ratio) will likely not cause toxicity
Large therapeutic range

Are drug-drug interactions occasionally helpful?
Yes, sometimes drug-drug interactions can be used for the pt’s benefit

List common anticholinergic adverse effects
Dry mouth.
Blurred vision.
Dry eyes.
Urinary retention.
Dizziness due to drop in blood pressure on standing up (postural hypotension)
Cognitive problems (confusion)
Heart rhythm disturbance.
(they dry you up)

What does DMARD stand for?
Disease-modifying antirheumatic drug, used commonly in RA

**DMARDs are used in RA for modification of disease progression**

What does a DMARD (disease-modifying antirheumatic drug) do?
Slows disease progression
Used frequently in RA

List DMARDs (Disease-modifying antirheumatic drugs)
chloroquine and hydroxychloroquine (HCQ) (antimalarials)
ciclosporin (Cyclosporin A)
gold salts (sodium aurothiomalate, auranofin)
*methotrexate (MTX)*
sulfasalazine (SSZ)

disease/condition commonly treated by anticholinergics
GI problems
overactive bladder

Which of the following is a typical anticholinergic adverse effect?
dry mouth
watery eyes
is a typical anticholinergic adverse effect

How do anticholinergics work?
block acetylcholine in PNS and CNS
blocks some invol mm mvmt
inhibits parasympathetic involment, so decreased invol mvmt, digestion, mucus secretion

Phase I drug trial
20-100 people with disease condition
To determine KINETICS and SAFETY
(looks at absorption, distribution, metabolism, excretion of drugs; what happens to the drug inside the body)

Phase II drug trial
Patients with disease being treated

100’s of people with disease condition
to determine DOSE and SAFETY
(looks at pharmacodynamics, physical effects of drugs in body)

Phase III drug trial
300-3,000 people with disease condition

**This is a large clinical trial conducted just prior to submitting to the FDA for approval**

Phase IV drug trial
Post marketing analysis
1,000s of people with disease condition

Which phase of drug trial is conducted just prior to submitting the data to the FDA for approval?
Phase III

Drug therapy for PD does what?
Increase dopamine availability
Decrease acetylcholine activity

What is a drug holiday?
Re-sensitize receptor sensitivity through NOT using drug for a prescribed amount of time

Are drug holidays for PD safe and easy?
Should typically be done in-patient
monitored closely
might use IV drip of amantadine

Drug holidays are an easy and safe way to re-sensitize a PD pt’s to levodopa therapy

Drug holidays are effective, but hey are not easy, nor super safe. Should be done in-patient and monitored closely.

What is amantadine?
Dopamine promoter and antiviral drug
Treat and prevent the flu (influenza type A)
Treat PD symptoms caused by certain medications

Does exercise raise or lower blood sugar?
Exercise generally lowers blood sugar.

Exercise most often raises blood sugar.

Excess tylenol/ acetaminophen does what?
Causes liver damage
also thins blood

If pt taks more than 3-4 g of Tylenol / acetaminophen per day, what could happen?
liver damage
nausea & vomiting
blood in urine

All diuretics work in same place on nephron
Diuretics can work in different places on nephron
Can have filtration diruetics, prox tube diuretics, loop of henle diretics. . .

You cannot give combos of diuretics
Since diuretics work in diff places on nephron, can take multiple diuretics, and they can augment each other

Diuretic are often used to treat CHF
Diuretics can help clear fluid retention caused by CHF
Frequently used in conjunction with ACE inhibitors

Max dose for acetaminophen
Maximum Dose: 3 g per 24 hours

For hypertension, diuretic should be a ____________x per ____________drug
1x per day

Which of the following is true about diuretics?
-All work in same place on nephron
-When treating hypertension, we would typically choose a 1x/day drug
-You cannot give a combo of diuretics
-They are not used in CHF
-When treating hypertension, we would typically choose a 1x/day drug

All oral medications for diabetes cause low blood sugar
While the effect of most diabetes meds to reduce blood sugar, they might not cause LOW blood sugar.

List general mechanism of diabetes meds
Some meds reduce insulin resistance (metformin and glitazones)
some stimulate insulin release (sulfonylureas and meglitinides)
some slow absorption of sugar in gut (acarbose)
some prevent the breakdown of GLP-1, which allows more insulin to be produced after meals (gliptins)
some meds increase excretion of glucose in urine (gliflozins)

Type II diabetics never use insulin

Metformin and glyburide have the same mechanism
both are diabetes meds
metfromin reduces insulin resistance
glyburide stimulates release of insulin from the pancreas

Diuretics can cause orthostatic hypotension
Diuretics clear fluids, could lower total blood volume, can cause orthostatic hypotension

Metformin/ Formatet is . . . .
antidiabetic for Type II DM
decreases liver production of glucose
also increases sensitivity to insulin
excreted almost entirely unchanged

Glyburide/DiaBeta is . . .
antidiabetic for Type II DM (used when diet therapy fails)
Stimulates increase of release of insulin from pancreas (so requires some pancreas function)
Stim increase sensitivity at insulin receptor sites

Do Metformin and Glyburide have same mechanism?
Metformin decreases liver production of glucose
Glyburide stimulates increase of release of insulin from pancreas and increase sensitivity at insulin receptor sites

Which of the following is true about a pt’s oral meds for DM?
-They all work in same place on the nephron
-Type II DM pt’s never use insulin
-It is no surprise that many pts are on a combo of drugs
-Metformin and gyburide have the same mechanism of action so they should not be given together
-It is no surprise that many pts are on a combo of drugs

Tylenol PM/ acetaminophen + diphenhydramine is . . .
Tylenol PM

acetaminophen – analgesic, inhibits synthesis of prostaglandin mediator of pain and fever

diphenhydramine – antihistamine and antitussive, antagonizes histamine at H1 receptor sites (occupies receptor site), and is CNS depressant and anticholinergic (dries you up)

If pt is on diuretic, metformin, glyburide & tylenol pm, which might cause orthostatic hypotension?
Diuretic could cause orthostatic hypotension

Methylprednisolone/ Cadista/ Medrol is . . .
oral steroid, used in cases of acutely flared-up COPD
steroidal anti-inflam
Used in management of chronic illnes, acute allergy, SC injury
Suppresses inflam and modifies normal immune response
need to taper use, as it suppresses adrenal response

Coumadin/ warfarin is . . .
reduce risk of thromboses, thromboembolic events

Propranolol/ Inderal/ Innopran/ Hemangeol is . . .
Beta Blocker
*causes heightened risk of patient harm when used in error

Which of the following drugs could affect pt’s response to exercise?
-steroid inhaler
Is a beta blocker, HR will not raise in exercise

(while a case could be made that any/all of these drugs affect pt’s response to exercise, beta blockers are the most correct answer here)

Inhaled asthma meds are considered “topical”
Inhaled corticosteroids, aka glucocorticosteroids are referred to as topical corticosteroids

Define “tolerance”
-the ability or willingness to tolerate the existence of opinions or behavior that one does not necessarily agree with
-person’s diminished response to a drug, which occurs when the drug is used repeatedly and the body adapts to the continued presence of the drug.

(vs resistance, which refers to the ability of microorganisms or cancer cells to withstand the effects of a drug usually effective against them.)

Morphine/ MS Contin/ Roxanol is . . .
opioid antagonist
for severe pain
binds to opioid receptors in CNS, alters perception of and response to pain
depresses CNS, can cause respiratory depression (Jaxon had to be reminded to breathe)
Do not use with MAO inhibitors

If a pt need more and more MS Contin and Percocet to control pain, pt could be developing_______________________

Allergies are . . .
an abnormal or damaging immune response by the body to a substance (especially pollen, fur, a particular food, dust, or a medication)
Can become sensitized to drugs, devo an allergy to drugs which previously caused no problem (it is uncommon, but does happen)

For pts on coumadin, do we monitor the amount of medication (coumadin) in blood, or the prothrombin time (INR)?
We monitor the prothrombin time (INR)

INR is used to monitor pts on anticoag.
The normal range = 0.8-1.2
Pt on warfarin therapy range= 2.0-3.0
pt with mechanical heart valve= higher than 3

high INR = higher risk of bleeding, low INR = higher risk of developing a clot.

If pt has noticed they are extra bruisey and have been having nosebleeds, what advice would you give them?
-Suggest not using inhalers so much
-Have coumadin blood level monitored
-Have prothrombin INR checked
-Stop taking percoset
Have prothrombin INR checked

Oxycodone+ acetaminophen/ Percoset is . . .
opioid analgesic, binds to opiate receptors in CNS + non opioid analgesic, inhibits synth of prostoglandins
**do not use for pts with liver disease or renal disease**

Is COPD reversible?
COPD is not reversible.

Is asthma reversible?
Weeeeeelllllll. . . .
Yes, constriction caused by asthma is reversible.
But, once you have asthma, you rarely grow out of it (unless you had asthma before puberty, then you might grow out of it in your teenage years)

Does Propranolol/ Inderal/ Hemangeol make COPD sxs worse?
Propranolol can cause bronchospasm and wheezing (not good if you already have congested obstructed gunked-up crappy lungs)

What is the first step to effective COPD tx?
Stop smoking

What is theophylline/ Theochron?
used in tx of asthma and COPD
can feel jittery and ampy like too much caffeine

The adverse effects of theophylline are similar to caffeine
theophylline can feel jittery

What are COX 2 inhibitors?
non-steroidal anti-inflammatory drugs
directly targets cyclooxygenase-2, COX-2, an enzyme responsible for inflammation and pain
includes: celebrex/celecoxib, vioxx/rofecoxib, bextra/valedecoxib
cause the same amount of kidney probs as traditional NSAIDs

*can cause kidney impairment
*be cautious with use in pts with MI, CVI, thrombosis, hypertension
*decreases effectiveness of ACE inhibitors
*increases risk of bleeding with warfarin and aspirin

Cox-2 Inhibitors like Celebrex cause less kidney probs than trad NSAIDs
Celebrex and other Cox-2 inhibs cause just as much kidney damage as trad NSAIDs

Chronic corticosteroid use causes. . .
*immune suppression*
decreased/suppressed growth in children
decreased healing

Max acetaminophen dose
3 gm/ day

Key points about prednisone
Short tapering doses useful for acute pain (need to taper off)
Avoid long term use
Useful for CNS metastases

Diazepam and baclofen have essentially the same mechanism of action for tx of spasticity?

both block mono- and polysynaptic reflexes,
enhances GABA activity
ultimately is inhibitory to mm contraction

Which of the following is an adverse effect from chronic corticosteroid use?
-immune suppression
-urinary retention
-immune suppression

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