Clinical Activity (Sweatman) Flashcards

1
Q

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

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

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

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2
Q

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

A

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

**Neonates also have very different rates of perfusion

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3
Q

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

A

Clarithromycin and Carbamazepine BOTH are metabolized by CYP3A4

  • COMPETITIVE inhibition takes place
  • Carbamazepine gets out competed and toxicity can result
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4
Q

What group of antifungals are contraindicated with simvastin and Lovastatin?

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

Azoles act on CYP3A4 as well

Worst —> Best:

  • Voriconazole
  • Itraconazole
  • Fluconazole

Condition:
- Rhabdomylosis - Myoglobin in Kidneys

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5
Q

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

A
  1. Competitive Inhibition
    (e. g. Probenecid blocks Penicillin Excretion)
  2. Are Tubules Damaged??
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6
Q

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

A
  • Pramipexol

- Dofetilide

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7
Q

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

A

It gets down-regulated

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8
Q

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

A

Coriticosteroids upregulate ß2-receptors

Opiates Downregulate ß2 receptors

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9
Q

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

A
  1. Competitive Inhibition

2. pH in Renal Tubule

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10
Q

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

A

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
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11
Q

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

A

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
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12
Q

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

A
  • 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
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13
Q

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

A

True, clavulanate prevents ß-lactamases from cleaving Amoxicillin

**PIP/TAZO relationship is the same deal

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14
Q

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

A

False, this is a not at receptor interaction

  • Both act to lower LDL in different ways
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15
Q

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

A
  • Will be exhaled
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16
Q

What is P-gp?

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

P-gp = P-glycoprotein

Function:
- Energy Dependent Drug Efflux Pump

Where:
- Found at any tissue barrier

17
Q

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

A

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

18
Q

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

A
  • Vasoconstriction keeps the Drug from Spreading out (localized)
19
Q

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

A
  • Neutral pH will hinder absorption because acids need to be protonated to travel through stomach epithelium
20
Q

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

A

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

21
Q

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

A

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

22
Q

What should you not use to take you tetracyclines with?

- why?

A

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

23
Q

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

A

True, because components in it act on CYPs

24
Q

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

A

Vancyclovir
Valganciclovir

Prodrug Advantage - allows for increased absorption

25
Q

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

A
  1. Caramazepine
  2. Cyclosporine
  3. Digoxin
  4. Ethosuximide
26
Q

Which is quicker enzyme induction or enzyme inhibition?

- why?

A

Enzyme Inhibition is much quicker

  • Enzyme induction requires the synthesis of proteins which is time consuming
27
Q

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

A

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

28
Q

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

A
  • In the case of heavy metal ingestion
29
Q

Go Back on Look at His Mind Map

- lots of stuff not included in these FC’s

A

Go Back on Look at His Mind Map

- lots of stuff not included in these FC’s

30
Q

What things factor into Phamacokinetic metabolism?

- Pharmacodynamic?

A

Pharmacokinetic

  • Absorption
  • Distribution
  • Metabolism
  • Excretion

Pharmacodynamic

  • Additive
  • Synergistic
  • Antagonistic
31
Q

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

A

False, changing the EXTENT of absorption is more important clinically

32
Q

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

A
  • Older people and newborns have variable plasma protein levels
33
Q

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

A

**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

34
Q

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

A

True

35
Q

What effect does induction typically have on drugs?

- what phase of metabolism is typically involved in induction?

A

It shortens the drug half life

Phase II