Drug Interactions Flashcards

1
Q

What can drug interactions do?

A

Reduce therapeutic effects
Increase therapeutic effects
Inc or reduce toxicity

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2
Q

What are common outlets for drug therapy?

A

Hypertension
Heart failure
Pain
Cancer

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3
Q

What are the goals of combination drug therapy?

A

Enhance desired therapeutic results

Dec drug induced toxicity

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4
Q

What are some classifications of drug interactions?

A

Pharmacokinetic (delivery of a drug to site of action altered by second drug)
Pharmacodynamic (response of the drug target is modified by a second drug)

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5
Q

Where do pharmacokinetic interactions take place?

A

GI, plasma, liver, kidney

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6
Q

Where do pharmacodynamic interactions take place?

A

Target organ

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7
Q

What interaction can occur in the GI tract?

A

Interactions can reduce the entry of drugs into the systemic circulation

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8
Q

What are some drugs that reduce systemic entry to the GI tract?

A

Aluminum containing medicines
Sucralfate reduced absorption to Ciprofloxacin and Azithromycin
omepazole (raise stomach PH)

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9
Q

What are some interactions that happen before administration?

A

Phenytoin is precipitates dextrose solution

Amphotericin precipitates in saline

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10
Q

What is protein bumping?

A

Interactions in serum that can cause an increased amount of free drug

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11
Q

What does metabolism of biotranformation refer to?

A

Disapperance of a drug when it changed chemically into another compound - a metabolite

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12
Q

What is the basic chemical process for a drug being metabolized?

A

Converting of a nonpolar, lipid-soluble compound to a more polar form that is more water soluble and can be readily excreted in the urine

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13
Q

What is the spectrum of cosequences of drug metabolism?

A
Inactive products (majority)
Active metabolites
Similar to parent drug
New action
Toxic metabolites
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14
Q

What are prodrugs (drugs in less actiev or inactive form) administered for?

A

Absorption
Overcome potential destruction by stomach acid
Minimize expose to high reactive chemical species
Allow for selective generation of active metabolites at target in vivo

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15
Q

What is cytochrome P450 (mixed function oxidases)?

A

A group of enzymes that are hemoproteins

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16
Q

What is Phase I of drug metabolism?

A

Oxidation (P450 dependent)
Oxidations (P450 independent)
Reduction
Hydrolyses

17
Q

What is Phase II of drug metabolism?

A

Conjugation to -OH, -NH2 and -SH functions on drug molecule

Subgroups added

18
Q

What are some phase I reactions?

A

Function to convert lipophilic molecules to more polar molecules bu introducing (unmasking) a polar functional group (OH, NH2, SH)
Most frequently involved in drug metabolism are catalyzed my microsomal mixed function oxidases

19
Q

What are drug interactions due to hepatic metabolism?

A

Due to interaction at phase I enzymes

P450 common

20
Q

What are the most common and important CYP450?

A

CYP3A4 (30%)
CYP2C9 (20%)
CYP1A2 (15%)

21
Q

What is the Cytochrom P450 nomenclature for CYP2D6?

A
CYP = cytochrome P450
2 = genetic family
D = genetic subfamily 
6 = specific gene
22
Q

What is CYP3A4 responsible for in terms of metabolism?

A
Most calcium channel blockers
Benzos
HIV PIs
HMG-CoA reductase inhibitors 
Cyclosporine
Non-sedating antihistamines
Cisapride
23
Q

Where would CYP3A4 be found?

A

GI tract and liver

24
Q

What is the main form of CYP inhibitors?

A

Through competition for the same isozyme

25
Q

What are some drugs which are CYP3A4 inhibitors?

A
Ketoconazole
Itraconazole
Fluconazle
Cimetidine 
Grape fruit juice
Amiodarone
Ritonavir
26
Q

What are some CYP3A inducers?

A

Carbamazepine
Rifampin
Phenobarital
Phenytoin

27
Q

What is the action of cytochrome P450 2D6?

A

Catalyzes primary metabolism of codeine, B-blockers and trucyclic antidepressants

28
Q

What is CYP2D6 inhibited by?

A

Fluoxetine

29
Q

What does CYP2C9 primarily metabolize?

A

Most NSAIDS (COX-2)
S-warfarin (active)
Phenytoin

30
Q

What is CYP2C9 inhibited by?

A

Fluconazole

31
Q

Which CYP is induced by smoking tobacco?

A

CYP1A2

32
Q

What does CYP1A2 primarily catalyze in metabolism?

A

Theophylline
Imipramine
Propranolol
Clozapine

33
Q

What inhibits CYP1A2?

A

Many fluorquiolone antibiotics
Fluvoxamine
Cimetidine