Pharm MT 1 Part III

1. Ionization makes a drug molecule _____ lipid-soluble

Ionization is the process of gaining or losing an electron, resulting in the formation of charged particles called ions. When a drug molecule becomes ionized, it becomes more polar and less lipid-soluble. This is because lipid molecules are nonpolar, while ions are charged and therefore interact more readily with polar molecules. As a result, ionization decreases the ability of a drug molecule to dissolve in lipids and pass through lipid-rich barriers, such as cell membranes. Therefore, the correct answer is "less."

Explanation

Ionization is the process of gaining or losing an electron, resulting in the formation of charged particles called ions. When a drug molecule becomes ionized, it becomes more polar and less lipid-soluble. This is because lipid molecules are nonpolar, while ions are charged and therefore interact more readily with polar molecules. As a result, ionization decreases the ability of a drug molecule to dissolve in lipids and pass through lipid-rich barriers, such as cell membranes. Therefore, the correct answer is "less."

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2. There is more than one cytochrom P450 enzyme

True

False

pg. 24

There have been 100s found although far fewer are found in humans.
We are now aware that CYP enzymes may be involved in the metabolism of approx 75% of all drugs.

Explanation

pg. 24

There have been 100s found although far fewer are found in humans.
We are now aware that CYP enzymes may be involved in the metabolism of approx 75% of all drugs.

3. Where are P450 isoenzymes located specifically in the liver?

Nucleus of hepatocytes

Golgi of hepatocytes

Plasma membrane of hepatocytes

Endoplasmic recticulum of hepatocytes

Through an electron transport change that uses NADPH as a proton carrier, a drug bound to cytochrome P450 can be oxidized or reduced

p.23

Explanation

Through an electron transport change that uses NADPH as a proton carrier, a drug bound to cytochrome P450 can be oxidized or reduced

p.23

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6. What general category of antibiotics can lead to permanent teeth staining when given to a child before the age of 8?

Sulfa drugs

Cephalosporins

Tetracyclins

Aminoglycosides

The specific example was doxycycline (Vibramycin), and this is a sub-category of tetracyclines. It can deposit in bones, liver, spleen and teeth

Explanation

The specific example was doxycycline (Vibramycin), and this is a sub-category of tetracyclines. It can deposit in bones, liver, spleen and teeth

7. Metabolic reactions can transform an active drug into a less active form or into inactive metabolites. Metabolic reactions can also transform a prodrug into a more active drug or metabolite.

True

False

pg. 22

Explanation

pg. 22

8. Which of the following conditions DOES NOT result in hypoalbuinermia (low serum albumin levels)?

Renal dialysis patients

Burn patients

Elderly patients with chronic disease states

Malnourished patients

None of the above (they all result in hypoalbumineria)

Patients with extremely low serum albumin levels may not have the full expected drug action of effect due to the fact that protein bound drugs can reach higher concentrations between the blood and tissues.

Explanation

Patients with extremely low serum albumin levels may not have the full expected drug action of effect due to the fact that protein bound drugs can reach higher concentrations between the blood and tissues.

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10. There are substrates, inhibitors, and inducers for oral meds under the OD scope of practice

True

False

see pg. 25 for a list of inhibitors and inducers of the P450 system that are prescribed by ODs

Explanation

see pg. 25 for a list of inhibitors and inducers of the P450 system that are prescribed by ODs

11. Pharmacologic metabolic processes often result in drugs becoming more _____ and more _____-soluble.

Pharmacologic metabolic processes often result in drugs becoming more polar and more water-soluble. This means that during metabolism, drugs tend to undergo chemical changes that increase their polarity and their ability to dissolve in water. This is important because polar and water-soluble drugs are more easily absorbed, distributed, and eliminated from the body, making them more effective and safer for use.

Explanation

Pharmacologic metabolic processes often result in drugs becoming more polar and more water-soluble. This means that during metabolism, drugs tend to undergo chemical changes that increase their polarity and their ability to dissolve in water. This is important because polar and water-soluble drugs are more easily absorbed, distributed, and eliminated from the body, making them more effective and safer for use.

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12. Which of the following is NOT part of microsomal (P450) oxidation reactions?

Hydroxylation

Azo-reduction

Oxidation

Polarizing atom exchange

Microsomal oxidation reactions: hydroxylation, dealkylation, oxidation, polarizing atom exchange

azo-reduction is a microsomal REDUCTION reaction

pg. 23

Explanation

Microsomal oxidation reactions: hydroxylation, dealkylation, oxidation, polarizing atom exchange

azo-reduction is a microsomal REDUCTION reaction

pg. 23

13. What most commonly occurs in CYP inhibition?

Inhibitor drug metabolizes to CYP enzyme

Inhibitor drug prevents absorption of CYP enzyme

Inhibitor drug competitively binds to active site of enzyme

None of the above

When the CYP inhibitor drug binds to the active site of the enzyme it prevents normal enzyme binding and routine metabolism from occurring.

pg. 24

Explanation

When the CYP inhibitor drug binds to the active site of the enzyme it prevents normal enzyme binding and routine metabolism from occurring.

pg. 24

14. What cytochrome P450 enzyme accounts for nearly half of all CYP activity?

CYP 1A

CYP 2C

CYP 2E

CYP 3A

pg. 24

Explanation

pg. 24

15. During drug metabolism, what is the general trend that occurs?

Drugs become more hydrophobic

Drugs become increasingly less active

Drugs are deposited more on various tissues

Drugs become more polar

pg. 23

Explanation

pg. 23

16. What percent of patients taking amiodarone present with corneal microdeposits?

1%

10%

50%

90%

Summary of adverse ocular effects of amiodarone:
- optic neuritis (1%)
- corneal microdepsoits (> 90%) causing visual distuburbance ( - visual disturbance (2-9%)
- halo vision (esp at night ) (
pg. 21
-

Explanation

Summary of adverse ocular effects of amiodarone:
- optic neuritis (1%)
- corneal microdepsoits (> 90%) causing visual distuburbance ( - visual disturbance (2-9%)
- halo vision (esp at night ) (
pg. 21
-

17. Check ALL the factors that allow a drug to more easily across plasma membranes.

Smaller molecular structure

Water-soluble

Ionization

Drugs that are lipid-soluble, smaller molecular structure and are NOT ionized have a better ability to pass thru plasma membranes (pg. 19).

Explanation

Drugs that are lipid-soluble, smaller molecular structure and are NOT ionized have a better ability to pass thru plasma membranes (pg. 19).

18. Which of the following drugs can result in optic neuritis/neuropathy and can deposit in the cornea and affect vision?

Phenytoin (Dylantin)

Mannitol with cisplatinum

Propofol (Diprivan)

Amiodarone (Pacerone, Cordarone)

amiodarone is a heart medication...this example was used to demonstrate drug deposition (pg. 21)

Explanation

amiodarone is a heart medication...this example was used to demonstrate drug deposition (pg. 21)

19. Which of the following does NOT require energy nor a transport carrier?

Passive diffusion

Carrier-assisted diffusion

Hydrophillic channels

Active transport

More than one of the above

All of the above require either energy or a transport carrier

passive diffusion + hydrophillic channels require no energy input and do not need a transport carrier

carrier-assisted diffusion only requires a transport carrier
active transport requires both energy an a transport carrier
(pg.19)

Explanation

passive diffusion + hydrophillic channels require no energy input and do not need a transport carrier

carrier-assisted diffusion only requires a transport carrier
active transport requires both energy an a transport carrier
(pg.19)

20. What are potential consequences of drug deposition?

Faster drug release

Slower drug release

Changes in the tissue

Drug inactivation

More than one of the above

Drug deposition occurs when a drug deposits in a specific tissue and accumulates. This may result in SLOWER drug release or eventual changes in the tissues

Explanation

Drug deposition occurs when a drug deposits in a specific tissue and accumulates. This may result in SLOWER drug release or eventual changes in the tissues

21. Choose ALL of the reactions that fall under Phase II reactions:

Glucuronide conjugation

Dealkylation

Ethereal sulfate conjugation

Acetylation

Transulfuration

Glutathion conjugation

pg.23

Explanation

pg.23

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22. When Nepafenac penetrates the cornea, it's converted into a more active form that acts as:

IOP reducer

Hemorrhage stabalizer

Analgesic

Edema reducer

Nepafenac, when it penetrates the cornea, is converted into a more active form that acts as an analgesic. This means that it functions as a pain reliever.

Explanation

Nepafenac, when it penetrates the cornea, is converted into a more active form that acts as an analgesic. This means that it functions as a pain reliever.

23. The drug propofol (Diprivan) has a short duration of action due to the rapid re-distribution to other tissues via the ____ system.

Gastrointestinal

Respiratory

Cardiovascular

CNS

Short duration of action is also due to its high metabolic clearance and high lipophilicty (pg.21). This drug is able to cross the blood brain barrier.

Explanation

Short duration of action is also due to its high metabolic clearance and high lipophilicty (pg.21). This drug is able to cross the blood brain barrier.

24. ACE Inhibitors are an example of a type of drug that results in a drug becoming ____ active than the parent drug

More

Less

ACE inhibitors are a type of drug that inhibits the angiotensin converting enzyme, which leads to the dilation of blood vessels and a decrease in blood pressure. This action makes the drug more active than the parent drug, as it enhances the drug's ability to lower blood pressure and treat conditions such as hypertension and heart failure.

Explanation

ACE inhibitors are a type of drug that inhibits the angiotensin converting enzyme, which leads to the dilation of blood vessels and a decrease in blood pressure. This action makes the drug more active than the parent drug, as it enhances the drug's ability to lower blood pressure and treat conditions such as hypertension and heart failure.

Pharm Mt 1 Part III