Drug Interactions - Quiz 2 Flashcards
What is pharmacodynamics?
The effect or change that a drug has on the body
What drugs are affected by coadminstration with polyvalent cations?
Quinolones, tetracyclines, levothyroxine, bisphosphonates
What is pharmacokinetics?
The effect the body has on the drug
What is the primary enzyme expressed in the liver?
CYP450
What drug blocks the renal excretion of penicillin?
Probenacid
What are prodrugs?
Inactive drug that is converted by CYPs to an active drug
What are the benefits of prodrugs?
- INcrease bioavailability
- Prevent drug abuse
What is the activity of prodrugs in the presence of CYP inhibiutors and inducers?
Inhibitors: concentration of active drug decreases
Inducers: concnetration of active drugs inrease
What are the most common CYP inhibitors?
Grapefruit
Protease Inhibitors
Azole
Cyclosporine, cobicistat
Macrolides (clarithromycin and erythomycin)
Amiodarone
Non-DHP CCBs (diltiazem and verapamil)
What are the common CYP inducers?
Phenytoin
Smoking
Phenobarbital
Oxcarbazepine
Rifampin
Carbamazepine
St John’s wort
How long in the lag time when an inducer has been discontinued?
2-4 wks
Common Pgp substrates?
Anticoagulants: apixaban, rivaroxaban
CV drugs: digoxin, diltiazem, verapamil
Immunosuppressants: cyclosporine, tacrolimus
Colchicine
Common pgp inducers?
Carbamazepine, phenobarbital, phenytoin, rifampin, St Johns
Common pgp inhibitors?
CV: amiodarone, diltiazem, verapamil
HIV: cobicistat, ritonavir
Cyclosporine
When adding warfarin to amiodarine what do you need to adjust? Vice versa?
Warfarin at low dose ≤5 mg
Decrease warafarin dose by 30-50% depending on INR
What is the cause of amiodarone and warfarin interaction?
Amiodarone is a CYP2C9 inhibitor increasing risk for bradycardia (Check for other drugs: beta blockers, clonidine, diltiazem, verapamil for decreased HR)
Reduse PO digoxin 50% when adding on amiodarone
What is the cause of amiodarone and digoxin interaction?
Amiodarone inhibits pgp
What electrolytes are decreased by loop diuretics? digoxin?
K, Mg, Ca, Na
Decreased K and Mg, increased Ca
What are drugs that decrease HR? How should you monito?
Amiodarone,digoxine, clonidine, beta blockers, diltiazem, verapamil
Monitor HR: 60-100 BPM
What statins are increaed with conmittant use of strong CYP3A4 inhibitors? How do you address interaction?
Lovastatin, simvastatin, atorvastatin
Non-CYP statins: pitavastatin, pravastatin, rosuvastatin
What enzyme metabolizes waraafarin?
CYP2C9
Inhibitors-> Increased levels -> Increased INR and bleeding risk
Inducers -> derease levels -> decreased INR and increases clotting risk
What should not be taken with CYP3A4 substrates?
Grapefruit juice
How do you does lamotrigine and valproate together?
Starter kit initiates lamotrigine with lower doses and tritates every 2 wks
MOA inhibitors increases what catecholamines?
Epi, NE, DA, 5-HT
Hypertensive crisis and serotonin syndrome
Counseling points of MAOIs?
2 wk wash out period when switching between MOAI and serotonergic agents
* 5 weeks if initiating fluoxetin
Avoid tyramine containig foods (aged cheeses, dried meats, sauerkraut)
What opioid are CYP3A4 substrates?
Fentanyl, hydrocodone, oxycodone, methadone
Smoking induces what CYP enzyme?
1A2
What drugs increase risk for bleeding?
- Anticoags
- Antiplatelets
- NSAIDs
- SSRIs, SNRIs
- Garlic, ginger, gingko, ginseng, glucosamine
Drugs that cause kyperkalemia?
- RAAS inhibitors
- Potassium sparing diuretics (amiloride, triamterene)
- salt substitute, calcineurin inhibiotrs
QT prolongationcan lead to ?
Torsades de pointes
q
What are the ADRs asscoaited with CNS depression?
- Somnolence
- DZ
- Confusion
- Cognitive impairment
- Altered consciousness
- Falls
What medications should not be taken together to avoid CNS depression?
- Opioids
- Benzos
- Alcohol
Drugs that cause ototoxicity?
- Aminoglycosides
- Cisplatin
- Loops
- Aspirin
- Vancomycin
Drugs that cause nephrotox?
- Aminoglycosides, vanc, amphotericin B, polymixins
- Cisplatin
- CIs
- Loops
- NSAIDs
- Contrast dyes (radiographic)
Anticholinergic toxicity is moreconcerning for who?
Elderly
Drugs that increase risk for orthostasis>
PDE5-I
with
CYP3A4 inhibotrs, Nitrates, or a-1 blockers