HLTH 353 Lecture Notes - Lecture 8: Therapeutic Index, Theophylline, Digoxin

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1 Oct 2018

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Drugs & society - hlth 353 - exam 1 notes. Chapter 5 - how and why drugs work (lots of terms) Terms associated with drug use prescribed to be taken at one time or at stated intervals. Dose = a specific quantity of a therapeutic agent, such as a drug or medicine, Potency = the relationship between the therapeutic effect of a drug and the dose necessary to achieve that affect (most people refer to this as strength of medicine) Tolerance = decreased responsiveness to a drug, especially over a period of continued use. Pharmacokinetics = the process by which a drug is absorbed, distributed, metabolized, and eliminated by the body (many factors can affect this) The range in dose between the amount of drug necessary to cause a therapeutic effect and a tosic effect. This range is referred to as a drug"s therapeutic index. The area between the effective level and toxic level of the drug .

Related Questions

1) The neurotransmitters acetylcholine and norepinephrine are digested by enzymes that are located at the axon synapse or within the axon terminal of the neurons.

a)What are the names of these different types of enzymes?

b)Where are they located and what is the result of their enzymatic activity?

2) Explain how the Investigational New Drug process works as well as the four different phases of clinical trials. Why are some drugs still taken off the market after approval by the FDA?

3) A single IV injection of 100 mg drug with a half-life of 4 hours is administered to a young adult.

a) Plot drug concentration versus time on a graph making certain to clearly label.

b) How long will it take to eliminate > 95% of the drug?

c) If the volume of distribution is 4L, what is the clearance of the drug?

4) Many drugs are metabolized in the liver through the microsomal metabolizing system.

a) What specific enzymes are involved in this metabolism?

b) What are the main functions of these enzymes?

c) What are some factors that can contribute to individual drug metabolism variation? Explain.

5) Think of an emergency situation requiring immediate and intense physical exertion.

a) List as many body organs as you can and predict the desired level of activity [increased or decreased].

b) Which neurotransmitter would produce these effects and through what receptors?

6) It is interesting that a drug can produce a therapeutic effect and an undesired side effect in one situation, and that the same drug side effect may be considered a therapeutic effect in another situation. Explain this phenomenon using the drug promethazine as an example.

7) A patient brought into the emergency room is experiencing severe hypotension. Blood pressure reads 90/50.

a) What class of drugs is indicated for treatment and why?

b) What precautions should be observed when these drugs are administered?

c) What would be the first indication that too much drug has been administered?

8) Only certain drugs are capable of crossing the blood brain barrier.

a) How is the blood brain barrier different than barriers found in other areas of the body? Be specific.

b) What properties of drugs will make it more likely to cross the blood brain barrier? Explain your answers.

9) A 32-year-old, presents to the Emergency Department by ambulance with vomiting, confusion, salivation, and respiratory distress. The patient states that he was feeling fine until today when I started getting ill. He then vomits. During a physical exam you record the following information: Heart rate 45; Blood pressure 90/60; Respiratory rate 25; Temperature 36.6C; Pupils constricted. During your exam, 4 more ambulances arrive with patients with similar symptoms. You find out they were all riding in the same care on the Red Line when they began feeling ill.

a) What do you feel is happening and why?

b) Would you expect their symptoms to improve over time? Why or why not?

c) What drug would you prescribe to treat these patients and why?

10) Betty has diabetes and asthma. She also has developed high blood pressure, for which doctor just prescribed propranolol. One of your duties as a physicianâs assistant is to make sure patients are not prescribed drugs that are contraindicated because of other health problems.

a) What should you tell the doctor about Bettyâs prescription for propranolol and why?

b) Is there a more appropriate drug for Betty? Explain you answer.

Need help with biology questions:

1. To increase the excretion of an acidic drug, what would you do to the urine?

	A.	Make it more basic
	B.	None of the above
	C.	Make it neutral
	D.	Make it more acidic

2. G-Protein coupled receptors directly act on which of the following secondary messenger molecules:

	A.	cAMP
	B.	ATP
	C.	ADP
	D.	GTP
	E.	None of the above or more than one of the above

3. Drug A and Drug B both produce the same level of biological/physiological response. Drug A produces this effect with 100 mg/kg dose. Drug B produces this effect with 50 mg/kg dose. Which of the following is true?:

	A.	Drug B is more efficacious than Drug A. Both drugs are equally potent.
	B.	Drug A is more efficacious than Drug B. Both drugs are equally potent.
	C.	Drug A and B are equally efficacious. Drug A is more potent than Drug B.
	D.	Drug A and B are equally efficacious. Drug B is more potent than Drug A.

4. The stomach has a ______ pH, whereas the small intestines have a _______ pH. The colon has an approximately ___________ pH.

	A.	High; low; neutral
	B.	Low; high; neutral
	C.	Low; neutral; neutral
	D.	None of the above

5. Which receptor is most likely to reduce norepinephrine levels when activated?

	A.	alpha 2 adrenergic
	B.	alpha 1 adrenergic
	C.	dopamine D1 receptors

6. Which of the following statements are FALSE?

	A.	If the Vd of a drug is between 60 and 80 L the drug has likely distributed to the total body water of a 200 kg man.
	B.	In the enterohepatic system the activity of bacteria to remove conjugates from a drug in the gut will decrease the clearance of the drug.
	C.	Lipid drugs are more likely to be reabsorbed by the kidney from the urine.
	D.	A weak basic drug (pKa = 6) will be mostly ionized in urine of a pH= 3 and only the non- ionized drug will be eliminated.
	E.	The major conjugate in Phase 2 metabolism is glucuronide.

7. Isoproterenol (Î²-agonist) is a vasodilator that increases HR. What happens to systolic and diastolic pressures upon IV administration of isoproterenol?

	A.	â systolic; â diastolic
	B.	â systolic; â diastolic
	C.	â systolic; â diastolic
	D.	â systolic; â diastolic
	E.	None of the above

8. If you want to increase the blood concentration of a drug A, you can perform which of the following procedures:

	A.	Inhibit Drug A metabolism with Drug B
	B.	Enhance Drug A reabsorption from renal proximal tubule by changing ionization of Drug A with Drug B
	C.	Allow competition of Drug B with Drug A for active renal secretion processes
	D.	Increase the binding of Drug A to serum albumin
	E.	All of the above

9. Which of the following describes Phase I metabolism?

	A.	Inactive products are always produced in this phase.
	B.	Large molecules such as glucuronic acid are conjugated to drugs in this phase.
	C.	This phase may produce active metabolites from prodrugs.
	D.	This phase only occurs in the liver.

10. Which of the following is NOT an enzyme involved in the biosynthesis of biogenic amines?

	A.	Phenylethanolamine N-methyl Transferase
	B.	Dopamine Î²-hydroxylase
	C.	Tyrosine dehydroxylase
	D.	DOPA decarboxylase
	E.	All of the above

11. Why would an antibiotic at the same concentration be more active against bacteria in water than in serum or plasma? (Activity is measured in a test tube)

	A.	activity of the antibiotic is increased in water.
	B.	due to drug-protein interaction in serum
	C.	the antibiotic is more stable in water
	D.	all of the above
	E.	none of the above

12. Ion channels are targets for drugs. Which drug class targets Na+ channels?

	A.	Benzodiazepines
	B.	Beta blockers
	C.	Local anesthetics
	D.	Antihypertensive drugs (cardiac and smooth muscle)
	E.	Glibenclimide (diabetic drug)

13. _________________ not metabolized by catechol-O-methyltransferase (COMT).

	A.	Dopamine
	B.	Epinephrine
	C.	Phenylephrine
	D.	Norepinephrine
	E.	All of the above are metabolized by COMT.

Multiple Choice questions 2 points each

1. Creatinine clearance is a commonly used estimate of:

A)Glomerular filtration rate (mL/min)

B)Tubular secretion (mL/min)

C)Total renal blood flow (mL/min)

D)Renal reabsorption (cc/min)

E)Steady state muscle breakdown rate (mcg/min)

2. Which of the following is not a measure of exposure?

a) Peak concentration

b) Time of maximum concentration

c) Area under the concentration time curve

d) Concentration measured 2 hours after dose administration

3. A clinically impactful drug interaction based upon inhibition of cytochrome P450 is most likely when:

a)The drug is metabolized by multiple enzymes

b)The drug has a narrow therapeutic index

c)There is limited variation in interindividual enzyme activity in the involved enzyme

d)The drug is a substrate of P-glycoprotein

e)All of the above

2. Why are dose-response (or concentration-response) analyses recommended for drug approval by a regulatory agency?

a) To increase the potential for adverse reactions in clinical trials in order to fully characterize the safety profile

b) To prolong the length of time it takes for drug approval

c) To maximize the likelihood that optimal drug dose will be prescribed after approval

d) To reduce the costs of clinical trials

e) To explore all possible disease state indications at time of initial approval

5. Which of the following is true of inhaled delivery of an aerosolized drug suspension?

a)An ideal drug would have low first pass hepatic metabolism to maximize systemic absorption

b)In contrast to milled powders, drugs in suspension are dosed in partial pressures

c)Efficiency of drug delivery by multi-dose inhalers is highly dependent upon patient technique

d)Typical multi-dose inhalers produce a very homogenous particle size of drug

e)Nebulized delivery of drug by face mask is not appropriate for children, demented or obtunded patients

6. The apparent volume of distribution (Vd):

a)Does not represent an actual physiologic volume

b)Can never be higher than total body water volume

c)Can be determined using only the half life of a drug

d)Will be large in a drug that is highly bound to serum proteins

e)Is usually small in drugs that require a loading dose

7. Which of the following characteristics of a drug make it most amenable to removal by hemodialysis?

a)Large volume of distribution

b)Large molecular weight

c)Strong protein binding

d)Good water solubility

8. Which is the best predictor of need for dosage adjustment in hepatic disease?

Child Pugh score

Portal splanchnic pressure (as measured by peripheral heart rate)

Degree of fibrosis and shunt on ultrasound

Levels of liver function tests

There is no single marker of hepatic dysfunction

9. Fexofenadine is not metabolized but is a P-glycoprotein (Pgp) substrate. How does St. Johnâs Wort cause decreased serum fexofenadine levels?

Inhibition of gut Pgp

Induction of gut PgP

Induction of CNS Pgp

Inhibition of biliary Pgp

None of the above

10. Which of the following is the best measure of renal function?

a)age

b)random urine creatinine concentration

c)spot plasma creatinine concentration

d)estimated creatinine clearance (Cockroft Gault)

e)Child-Pugh

11. Which pharmacokinetic parameter is the best measure of total systematic drug exposure after an oral dose?

a)Cmax

b)Elimination half life

c)Absorption rate constant

d)Area under the curve

e)Clearance

12. Which of the following is a mechanism that would cause a drug to have zero order elimination in humans?

a)Ultra-metabolizer genotype

b)Enterohepatic recirculation

c)High serum protein binding

d)Saturation of the prime metabolic enzyme

e)Sustained release version of a drug

13. Phase II metabolic metabolism:

a)Involves the covalent binding of a polar side chain

B)Always follows phase 1 metabolism

c)Employs breaking of aromatic ring structures

d)Is not subject to pharmacogenetic variation

e)Occurs exclusively pre-systemically, in the gut lumen

14. Which is not a high profile FDA Initiative?

a)Orphan Disease Act

b)Childhood Vaccine Act

c)Rare Disease Act

d)Breakthrough Drug Designation

15 In explaining risk posed by pharmaceutical R&D, which is not a development risk:

a)Patient population

b)Clinical endpoint

c)Predictability of trials

d)Competitive advantage

16. The key pivotal trials undertaken as part of the IND are part of which phase of the clinical drug development process?

a)Phase I

b)Phase II

c)Phase III

d)Phase IV

17. Which is not an EU Regulatory Process

a)Centralized Procedure

b)Certificate of Pharmaceutical Product Procedure

c)De-Centralized Procedure

d)Mutual Recognition

18. The role of experimental medicine strategies is to

a)Explore disease and drug biology to support go/no go decisions

b)Generate and fully validate biomarkers for FDA approval

c)Primarily to co-develop diagnostic tests to be filed with the NDA (new drug application)

d)Harmonize FDA and EMA phase 1 requirements

e)Define the pharmacokinetics of exploratory drugs in healthy volunteers or selected patient populations

HLTH 353 Lecture Notes - Lecture 8: Therapeutic Index, Theophylline, Digoxin

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