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Pharm > Pharm Exam 1 > Flashcards

Pharm Exam 1 Flashcards

1
Q

1 potent inhibitor of OAT?

* Why is it given w/cidefovir? (explain)

A

Probenecid
- Given w/cidefovir to protect from otherwise severe renal toxicity by blocking uptake into the proximal tubules (from the blood)

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2
Q

3 Drugs transported by OAT?

A

Ci-Me-N

  • Cidefovir
  • Methotrexate
  • NSAIDs
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3
Q

1 drug class transported by OATP?

A

Statins

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4
Q

1 potent inhibitor of OATP?

* If given w/statins, where would it inhibit the uptake of statins and what would this cause?

A

Cyclosporin

- Inhibits statin uptake from blood to liver, increasing toxicity risk and decrease statin efficacy

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5
Q

4 Drugs transported by OCT?

A

Ci-Ci, pro met

  • Cisplatin
  • Cimetidine
  • Procainamide
  • Metformin
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6
Q

2 Drugs transported by P-gp/MDR-1?

A
  • Digoxin

- Loperamide

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7
Q

1 potent inhibitor of P-gp/MDR-1?

A

Cyclosporin

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8
Q

St. John’s Wort and rifampin induce which transporter protein type?

A

P-gp/MDR-1?

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9
Q

1 drug class transported by BCRP?

A

Statins

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10
Q

3 endogenous substrates of MRP?

A
  • Glutathione
  • Glucuronide
  • Sulfate-conjugates
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11
Q

What drugs induce expression of CYP450 enzymes?

A

Phen-Phen rifles St. John’s glowing pink cars.

  • Phenytoin
  • Phenobarbitol
  • Rifampin
  • St. John’s wort
  • Glucocorticoids
  • Pioglitazone
  • Carbamazepine
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12
Q

What drugs inhibit expression of CYP450 enzymes?

A

Eric’s red grape kept its clear fluid

  • Erythromycin
  • Ritonavir
  • Grapefruit juice (enterocytes, NOT liver)
  • Ketoconazole
  • Itraconazole
  • Clarithromycin
  • Fluconazole
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13
Q

E.g. of drug class that may compete for protein binding and increase the unbound fraction of other drugs?

A

Sulfanomides

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14
Q

2 drugs eliminated by zero-order kinetics?

A
  • Phenytoin

- Alcohol

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15
Q

3 types of rxns involved in phase I rxns?

A
  • Oxidation (CYP450)
  • Reduction
  • Hydrolysis
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16
Q

3 most common CYP450 enzyme subfamilies?

A
  • 3A
  • 2C
  • 2D
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17
Q

What classes of biochemical binding-site interactions are irreversible inhibitors of CYP3A4? (1). Reversible? (2)

A
  • REVERSIBLE: Competitive or allosteric

- IRREVERSIBLE: Suicide inhibitor (covalent binding)

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18
Q

Is gray baby syndrome related to phase 1 or 2 enzymes? (Excess or deficiency?)
- What drug leads to it?

A
  • Phase 2 deficiency
  • Chloramphenicol
    (results in circulatory collapse and cyanosis)
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19
Q

Chemicals in cigarette smoke, charbroiled food and cruciferous vegetables all induce CYP___.

A

1A2

20
Q

Chronic alcohol induces expression of CYP___

A

2E1

21
Q

Substrate specificity for OAT?

A

Broad range of low MW substrates

22
Q

Substrate specificity for OATP?

A

Broad range of substrates; Amphipathic Anions, MW > 350 Da

23
Q

Most drug interactions mediated by OCT/MATE are caused by what drug?
- How? (what organ)

A

Cimetidine

- Prevents renal elimination of other OCT-dependent drugs

24
Q

What 2 channels does cyclosporin inhibit?

A

OATP and P-gp/MDR-1

25
Q

What 2 channels transport statins?

A
  • OATP (influx)

- BCRP (efflux)

26
Q

What drug is given w/cisplatin to avoid nephrotoxicity?

A

Cimetidine.

27
Q

Substrate specificity for P-gp/MDR-1?

A
  • Broad substrate specificity, typically bulky hydrophobic structures with neutral/positive charge
28
Q

Would tumor cells upregulate or downregulate p-gp/MDR-1? Why?

A

Tumor cells often upregulate expression of P-gp/MDR1 to promote efflux of anti-cancer drugs

29
Q

Of the transporters mentioned, which one is not present at the apical gut lumen?

A

OAT

30
Q

Name the 3 most common CYP polymorphic genes.

A

CYP2D6, 2C9 and 2C19

31
Q

Which of the CYP proteins is linked to warfarin inactivation of the active metabolite, S-warfarin?

A

CYP2C9

32
Q

How does VCORC1 relate to warfarin?
What does VCORC1 do
What would happen with a mutation in VCORC1?

A
  • Warfarin nlly inhibits VCORC1
  • VCORC1 leads to formation of active clotting factor
  • VCORC1 mutation = warfarin resistance = low anticoagulation (need higher dose)
33
Q

What are the 3 non-pharmacological means of antagonizing drug effects?

A
  1. Chemical antagonism (e.g. chelation)
  2. Physiologic antagonism (use of opposing pw’s)
  3. Biologic antagonism (1 drug effects metab/PK of another)
34
Q

How is 95% of acetaminophen metabolized?
What about the other 5%?
Why is high dose dangerous?
* Treatment with what drug will elevate glutathione levels and shunt back to normal pw?

A
  • 95% is conjugated and eliminated
  • 5% converted to NAPQI, which can be conjugated
  • High dose shunts pw to NAPQI -> hepatotoxicity
  • N-acetyl cysteine
35
Q

Explain (in small amount of detail) the 5 parts of pre-clinical trials.
1) What 2 doses must be determined?

A
  1. Safety pharmacology (no effect dose + LD50)
  2. Toxicology
  3. PK testing (ADME)
  4. Drug interactions (CYP450, xporters)
  5. Chemical/pharmacological devo (stable? reproducible?)
36
Q

When does the FDA perform a review in the making of a new drug?

A
  • Reviews investigational new drug application (INDA)
  • Meets b/w phase II and III of clinical trials (to be sure it’s safe for larger pop.)
  • Reviews new drug application (NDA)
37
Q

What are the 3 things an IND application must have?

A
  1. Animal pharm and toxicology data
  2. Manufacturing info
  3. Clinical protocols/investigator info
  • Shows drug is reasonably safe and allows drug to be shipped across state lines
38
Q
  1. Purposes of phase I trial?

2. Trial design?

A
  1. Is it safe/tolerable; PK

2. Open label w/escalating dose

39
Q
  1. Purposes of phase II trial?

2. Trial design?

A
  1. Does it work in actual pts? Dosing; Efficacy; safety

2. Single/double-blind

40
Q

Purposes of phase III trial?

Trial design?

A
  1. Does it work in large pt population? Efficacy + safety

2. Double-blind

41
Q

What 4 things must be labeled on drug packaging?

A
  1. Dosage
  2. Adverse reactions
  3. Contraindications
  4. Special warnings/precautions
42
Q

Define the 3 classes of drug recall.

A

Class I: Reasonable probability that use of drug will cause serious adverse health consequences or death (e.g. microbial contamination)

Class II: Use of drug will cause temporary adverse health consequences, although probability of serious health consequences is remote

Class III: Use of drug is unlikely to cause adverse health consequences (e.g. quantity packaging error)

43
Q

What can happen when loperamide is given concurrently w/cyclosporin?

A

P-gp/MDR-1 receptors can be inhibited by cyclosporin, allowing loperamide to cross BBB can cause respiratory depression.

44
Q

Which protein transporter class has specificity that overlaps with CYP3A4?

A

P-gp/MDR-1

45
Q

In what phase of clinical trials of “proof of concept” established?

A

Phase II

Pharm (32 decks)

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