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CMBM Exam 4 Gopi > Drug interactions > Flashcards

Drug interactions Flashcards

0
Q

goals of drug therapy

A

enhance desired therapeutic result

decrease drug induced toxicity

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1
Q

Drug actions can

A

increase/decrease therapeutic or toxic effects

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2
Q

some patients concerns about health system

A

suffering from pain
cost of prescriptions
wrong drug
drug interaction

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3
Q

Pharmacokinetic

A

delivery of a drug to its site of action

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4
Q

Pharmacodynamic

A

the response of drug target is modified

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5
Q

Pharmacokinetic interactions

A

GI tract
plasma
liver
kidney

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6
Q

Pharmacodynamic interactions

A

target organs

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7
Q

interaction before administration

A

Phenytoin PPTs out of dextrose solution

Amp B PPTs in saline

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8
Q

GI interactions that reduce entry of drugs into the systemic circulation

A

Metal containing drugs can reduce the absorption of expensive and life saving antibiotics
Some drugs require acidic environment to be in non charged form that is absorbed. Altered pH affects solubility

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9
Q

Protein “bumping” interaction in serum can result in

A

increased amount of free drug

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10
Q

metabolism and biotransformation refer to

A

disappearance of drug when it is changed chemically into another compound called a metabolite

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11
Q

When drug is metabolized usually converted from what form to what form?

A

nonpolar, lipid soluble to more polar form than is more water soluble (this aids in excretion through urine)

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12
Q

Advantages of prodrug

A

overcome potential destruction by stomach acid
minimize exposure to highly reactive chemical species
allow for selective generation of pharmacologically active metabolites at specific target sites in vivo

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13
Q

Phase I

A

oxidations - P450 dependent
oxidations - P450 independent
Reduction/Hydrolyses - P450 independent

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14
Q

Phase II

A

conjugation to -OH, -NH2, -SH
subgroups added
-glucuronate, acetate, glutathione, glycine, sulfate, methyl groups

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15
Q

Phase I reactions - purpose

A

convert lipophilic molecules into more polar molecules by introducing or unmasking polar functional group

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16
Q

Phase I reactions usually catalyzed by

A

CYPs

17
Q

Drug interactions due to hepatic metabolism

A

nearly always due to interaction at phase I enzymes

18
Q

CYPs most abundant to least

A

3A4
2C9
1A2
2E1

19
Q

CYP3A4

A

for metabolism of largest number of drugs
ex: Ca channel blocker, benzos, HIV protease inhibitors, HMG CoA, cyclosporine, non sedating antihistamines, cisapride
Present in GI and liver

20
Q

Inhibitors of CYP3A4

A

*Grapefruit juice
Antifungals - Ketoconazole, Itraconazole, Fluconazole
Ritonavir
Erythromycin, Clarithromycin

21
Q

Inducers of CYP3A4

A

Carbamazepine
Rifampin
*St. Johns wort
*Barbiturates - Phenobarbital

22
Q

CYP2D6

A

absent in 7% white ppl
Hyperactive in 30% East african
**metabolizes Codeine and beta-blockers

23
Q

Inhibitors of CYP2D6

A

Quinidine

24
Q

CYP2C9

A

*metabolizes NSAIDs (includes COX2)

25
Q

CYP2C9 inhibited by

A

Fluconazole

26
Q

CYP1A2 induced by

A

***Smoking tobacco

27
Q

CYP1A2

A

Propranolol

28
Q

CYP1A2 inhibited by

A

*Cimetidine - Histamine antagonist, lowers stomach pH

29
Q

Phase I reactions that do NOT involve CYPs

A

Amine oxidation
Dehydrogenation
Reduction
Hydrolyses

30
Q

Phase I prepares very …

A

lipophilic molecules for phase II reactions by creating a conjugation site

31
Q

Phase II reactions conjugate

A

a water soluble entity to aid in excretion by making molecule more polar, helps to eliminate it via urine or bile

32
Q

If metabolite for Phase I metabolism is sufficiently polar,

A

can be excreted by kidneys without need for conjugation

33
Q

if drug is too lipophilic

A

retained in the kidney tubules

34
Q

drugs with -OH, -NH2, or COOH group

A

may enter Phase II directly

35
Q

A highly polar drug conjugate may be

A

excreted by the kidney or bile

36
Q

Cardiac disease

A

can decrease hepatic blood flow

37
Q

St john wort with Indinavir

A

inhibits the drug activity

on a graph, would see lower concentration of Indinavir over the course of treatment

38
Q

Drug metabolites are generally more

A

polar than the parent drug

39
Q

most studied drug transporter

A

P-glycoprotein

40
Q

Inhibitor of P-glycoprotein

A

verapamil, ditiazem

these inhibitors will elevate levels of drug because they cant be transported for elimination

41
Q

warfarin plus NSAIDs

A

BAD - gastric bleeding

CMBM Exam 4 Gopi (10 decks)

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