Drug Interactions Flashcards

1
Q

What drug classes are most commonly involved in Drug to Drug Interactions?

A

NSAIDs
Anticoagulants
Antiplatelets
Cardiovascular drugs

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2
Q

What are some of the main risks for Drug to Drug Interactions?

A

Age
Narrow Therapeutic Index
Self-Prescribing

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3
Q

Medications or substances that increase the rate of metabolic activity of a specific CYP450 enzyme?

A

Inducers

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4
Q

Medications or substances that decrease the rate of metabolic activity of a specific CYP450 enzyme?

A

Inhibitors

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5
Q

Medications or substances that use CYP450 enzymes to be metabolized in the liver?

A

Substrates

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6
Q

What two mechanisms are responsible for the majority of drug interactions?

A

Induction and Inhibition

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7
Q

Efflux transporters found in the gut and other organs.
Pump drugs back into the gut (out of the bloodstream)

A

P-Glycoproteins

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8
Q

Inducers (CORRPPSESN)

A

Carbamazepine
Oxcarbazepine
Rifampin
Ritonavir
Phenytoin
Phenobarbital & Primidone
Smoking
Efavirenz
St. John’s Wort
Nafcillin

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9
Q

How long would it take to see a drug to drug interaction when administering an inducer?

A

2 - 3 weeks

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10
Q

2C9 Inhibitors

A

Bactrim
Metronidazole

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11
Q

2D6 Inhibitors

A

Tricyclic Antidepressants
Fluoxetine
Paroxetine

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12
Q

3A4 Inhibitors

A

Haloperidol
Azoles (anti-fungals)
Protease Inhibitors
NNRTIs
Diltiazem
Verapamil
Erythromycin

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13
Q

How long would it take to see a drug to drug interaction when administering an inhibitor?

A

2 - 3 days

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14
Q

Inhibitors (G-PACMAN)

A

Grapefruit
Protease Inhibitors
Azole (anti-fungals)
Cimetidine
Macrolides
Amiodarone
Non-Dihydropyridine Calcium Channel Blockers
(Diltiazem and Verapamil)

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15
Q

Serious adverse drug reactions?

A

Steven Johnson Syndrome
Toxic Epidermal Necrolysis (TEN)
Anaphylaxis

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16
Q

Medication that is pharmacologically inactive in the body.

A

Prodrugs

17
Q

Amiodarone

A

Inhibitor: 2C9, 2D6, 3A4
Decrease dose of Digoxin and Warfarin by 30-50%
Do not use grapefruit juice

18
Q

Azole Anti-fungals

A

Require low pH (acidic) for absorption
Avoid with drugs that increase pH
(antacids, H2 blockers, proton pump inhibitors)

19
Q

Digoxin

A

Narrow therapeutic index medication
Hypokalemia = ↑ Digoxin Toxicity
85% Renally Cleared. ↓ Renal Function = ↓ Digoxin Dose

20
Q

Statins

A

Substrates of 3A4 = ↑ levels with 3A4 inhibitors
Clinical outcome of higher risk for muscle toxicity

21
Q

What mechanism increases the level of the drug in the blood causing increased toxicity?

A

Inhibitors

22
Q

Lithium

A

100% Renally Cleared
Increased Lithium with:
NSAIDs
ACE-inhibitors
Angiotensin Receptor Blockers
Dehydration
Diuretics

23
Q

MAO Inhibitors

A

Tranylcypromine, Isocarboxazid, Phenelzine, Selegline

Metabolism is decresed in the presence of:
Norepinephrine & Epinephrine
Serotonin
Tyramine (aged, fermented, pickled, smoked)

Serotonin Syndrome or Hypertensive Crisis:
Antidepressants
Triptans
Dextromethorphan

24
Q

NSAIDs

A

COX Inhibitors block prostaglandin synthesis
Increased Risk of:
- Bleeding
- Kidney Injury
- Cardiovascular Toxicity

25
Q

Oral Contraceptives

A

CYP450 Enzyme Inducers can decrease effectiveness

Examples:
Anticonvulsants:
barbiturates, phenytoin, carbamazepine
St. John’s Wort
ABX:
Ampicillin, Sulfonamides, Rifampin, Tetracycline
Some Anti-Retrovirals
Smoking (more likely to form blood clots)

26
Q

Rifampin

A

GOLD STANDARD INDUCER
Strong Inducer of: CYP 2C9, 2C19, and 3A4
Will decrease the concentration of any drug that is a substrate listed above.
Used to treat TB and Leprosy

27
Q

Phenytoin

A

Induces CYP 2C8, 9 & 19, 3A4, and P-Glycoprotein
Highly protein bound (albumin)
Can displace medications from albumin
CAUTION with other CNS Depressants (additive effects)

28
Q

Carbamazepine

A

Strong 3A4 inducer and induces its own metabolism

3A4 Substrate
3A4 inhibitors will increase carbamazepine levels
3A4 inducers will decreases carbamazepine levels

29
Q

Tetracycline and Quinolone ABX

A

Ciprofloxacin, Levofloxacin, Moxifloxacin
Bind or Chelate with: Aluminum, Magnesium, Calcium, Iron, and Zinc
Decreased absorption of ABX

30
Q

Separate administration of what and for how long when prescribing Tetracyclines or Quinolones?

A

Vitamins
Iron Supplements
Antacids
Dairy
Sucralfate
Coated aspirin

31
Q

Warfarin (Pharmacokinetics)

A

Substrate of 2C9
Induction of 2C9 = ↓ Effectiveness
Inhibition of 2C9 = ↑ Effectiveness
Effectives is measured by INR

32
Q

Warfarin (Pharmacodynamics)

A

Combined toxicity of bleeding risks
Additive bleeding risk with NSAIDs & anti-platelets - no change in INR

33
Q

What herbal drugs will increase the risk of bleeding while on Warfarin?

A

Garlic
Ginkgo

34
Q

What supplements decrease the effectiveness of Warfarin?

A

Ginseng
Vitamin K (reversal agent)

35
Q

What classes of medications can cause hyperkalemia?

A

ACE Inhibitors
ARBs
Trimethoprim
Aldosterone Antagonists
NSAIDs
Digoxin

36
Q

What can hyperkalemia lead to?

A

Cardiac arrhythmias and sudden cardiac death

37
Q

CNS depressants that when used together cause additive effects

A

Alcohol
Opiates
Muscle Relaxers
Benzodiazepines
Hypnotics
Barbiturates

38
Q

Risk factors for Torsades de Pointes
(Polymorphic Ventricular Tachycardia)

A

Medications
QT interval > 500 msec
Bradycardia
Electrolyte abnormalities
Females
Congenital QT prolongation

39
Q

Red flag medications for long QT syndrome

A

Warfarin
Highly Active Anti-retroviral Therapy (HAART)
Amiodarone
Tricyclic Antidepressants
Quinolones
Antipsychotics
Antibiotics
Anti-aryhtmics
Anti-convulsants
Statins