Clinical Activity (Sweatman)

Question 1

What the advantage of taking medicine with food vs. no food?

• what aspect of ADME is affected?
• Risk of Fatty Foods?

Answer 1

ABSORPTION - affected

Advantage:
- eating food with a pill reduces gastric irritation

Fatty Foods:
- Lipophilic drugs may not be absorbed well with fatty foods because they’ll stay with the food and get excreted

Question 2

What is the major variable affected the distribution of a drug after it is given Intramuscularly or Subcutaneously?

Answer 2

Perfusion of the Site greatly affects what will happen to the drug after it is injected

**Neonates also have very different rates of perfusion

Question 3

What drug is contraindicated with Carbamazepine (mood stabilizer) and why?
- classify this interaction

Answer 3

Clarithromycin and Carbamazepine BOTH are metabolized by CYP3A4

• COMPETITIVE inhibition takes place
• Carbamazepine gets out competed and toxicity can result

Question 4

What group of antifungals are contraindicated with simvastin and Lovastatin?

• why?
• Which or these is the worst?
• What condition could mixing these drugs cause?

Answer 4

Azoles act on CYP3A4 as well

Worst —> Best:

• Voriconazole
• Itraconazole
• Fluconazole

Condition:
- Rhabdomylosis - Myoglobin in Kidneys

Question 5

What are two major factors that affect Renal Tubule Secretion (RTS)?

Answer 5

1. Competitive Inhibition
   (e. g. Probenecid blocks Penicillin Excretion)
2. Are Tubules Damaged??

Question 6

Cimetidine and Trimethoprim can act to block renal tubule secretion of what drugs?

Answer 6

• Pramipexol

- Dofetilide

Question 7

What usually happens to a receptor when over-stimulated by a drug?

Answer 7

It gets down-regulated

Question 8

What groups of drugs act at the ß2-receptor to upregulate its presence?
- which down regulates the receptor by its presence?

Answer 8

Coriticosteroids upregulate ß2-receptors

Opiates Downregulate ß2 receptors

Question 9

What are some factors to consider when thinking about drug reabsorption in the distal tubule?

Answer 9

1. Competitive Inhibition

2. pH in Renal Tubule

Question 10

T or F: an acidic pH in the renal tubule can help cure Acetylsalacyclic Acid overdose

Answer 10

False, overly basic pH’s do this

You want a basic pH because this deprotonates the acid (making it charged) - charged ions are excreted in the distal tubule

• You might give the patient bicarb to do this

Question 11

What are the two ways that a receptor can be agonized?

Answer 11

Directly
- Depends on duration of Ligand binding

Indirectly (drugs from a different class)

• Could Exhaust the Neurotransmitter that Needs to be used
• Could cause Off target effects

Question 12

Why should you not eat leafy green vegetables while taking Warfarin?
- what about NSAIDs?

Answer 12

• Vegetables high in Vit. K are bad with Warfarin because Warfarin acts to prevent the action of Vit. K in making clotting proteins in the liver
• NO DO NOT TAKE NSAIDs with Warfarin

Question 13

T or F: the relationship between Amoxicillin and Clavuanate is a not at receptor interaction

Answer 13

True, clavulanate prevents ß-lactamases from cleaving Amoxicillin

**PIP/TAZO relationship is the same deal

Question 14

T or F: for fear of a competitive interaction you should avoid taking Simvastatin with Niacin.

Answer 14

False, this is a not at receptor interaction

• Both act to lower LDL in different ways

Question 15

You are given and inhaled anesthetic before surgery. How will that drug leave your body?

Answer 15

• Will be exhaled

Question 16

What is P-gp?

• what does it do?
• Where is it found?

Answer 16

P-gp = P-glycoprotein

Function:
- Energy Dependent Drug Efflux Pump

Where:
- Found at any tissue barrier

Question 17

What happens if you foods containing lots of Tyramine while taking an MAOI?

Answer 17

You can get Tyramine overdose because Tyramine is acted on by MonoAmine Oxidase

Question 18

Why would you give a vasocontricting agent with a local anesthetics?

Answer 18

• Vasoconstriction keeps the Drug from Spreading out (localized)

Question 19

What will a neutral pH created by an antacid do the the absorption of acidic compounds in the stomach?

Answer 19

• Neutral pH will hinder absorption because acids need to be protonated to travel through stomach epithelium

Question 20

What happens if you try to chew up an enterically coated drug?

Answer 20

The drug will get broken down and made ineffective in the stomach or it will get released at the inappropriate time

Question 21

What’s the effect of taking a laxative with another drug?

Answer 21

The other drug may be expelled too fast to reach maximal efficacy

Question 22

What should you not use to take you tetracyclines with?

- why?

Answer 22

Milk - tetracycline chelates the calcium rendering it ineffective (it also chelates calcium in bone etc.)

Question 23

T or F: grapefruit juice has a huge tendency to change activity of drugs.

Answer 23

True, because components in it act on CYPs

Question 24

What herpes drugs are actually activated by 1st pass metabolism?
- what is the advantage of giving them as a prod-drug

Answer 24

Vancyclovir
Valganciclovir

Prodrug Advantage - allows for increased absorption

Question 25

Most drugs have a large therapeutic window. What 3 drugs did Sweatman tell have narrow therapeutic windows?

Answer 25

1. Caramazepine 2. Cyclosporine 3. Digoxin 4. Ethosuximide

Question 26

Which is quicker enzyme induction or enzyme inhibition? | - why?

Answer 26

Enzyme Inhibition is much quicker - Enzyme induction requires the synthesis of proteins which is time consuming

Question 27

What is the issue with taking cyclosporin and tacrolimus with a kidney transplant?

Answer 27

They can cause loss of the transplant due to drug toxicity since they are metabolized by the liver

Question 28

In what situation would you definitely need to administer a chelating agent?

Answer 28

- In the case of heavy metal ingestion

Question 29

Go Back on Look at His Mind Map | - lots of stuff not included in these FC's

Answer 29

Go Back on Look at His Mind Map | - lots of stuff not included in these FC's

Question 30

What things factor into Phamacokinetic metabolism? | - Pharmacodynamic?

Answer 30

Pharmacokinetic - Absorption - Distribution - Metabolism - Excretion Pharmacodynamic - Additive - Synergistic - Antagonistic

Question 31

T or F: affecting the the rate absorption is extremely clinically significant.

Answer 31

False, changing the EXTENT of absorption is more important clinically

Question 32

Why would you need to be more conscious of dosing with a drug like warfarin with older people and newborns?

Answer 32

- Older people and newborns have variable plasma protein levels

Question 33

What factor should be considered the most when determining whether plasma protein will play an important role in the distribution of a drug?

Answer 33

**How much drug there is relative to the Plasma Protein **Way more drug than plasma protein binding sites, then affects aren't that significant **Way less drug than binding sites then a change in binding can become very significant

Question 34

T or F: it takes a long time to build up a drug in adipose tissue and it takes a long time to get it back out

Answer 34

True

Question 35

What effect does induction typically have on drugs? | - what phase of metabolism is typically involved in induction?

Answer 35

It shortens the drug half life Phase II