NAPLEX _ Drug Interactions

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  1. CYP Inducers
    -- Definition?
    -- Net Effect?
    -- Prodrug Effect?
    • Inducers = compounds that either increase the production of the enzyme OR increase the activity of the enzyme
    • Net Effect: Increase metabolism of substrate
    • -- inDucers = DECREASE levels/effects of substrates (Subtherapeutic)
    • Prodrug EffectIncrease levels of active drug form
  2. CYP Inhibitors
    -- Definition?
    -- Net Effect?
    -- Prodrug Effect?
    • Inhibitors = compounds that inhibit the activity of the enzyme
    • Net Effect: Decrease metabolism of substrates
    • -- iNhibitors = INCREASE levels/effects/ADR/toxicities of substrates (Toxicity / ADRs) 
    • Prodrug Effect: Decrease levels of active drug form
  3. 3A4 Substrates (9 classes)
    • Analgesics (buprenophine || diclofenac || fentanyl || hydrocodone || methadone || oxycodone || tramadol)
    • Anticoagulants (apixaban || rivaroxaban || R-warfarin)
    • Antidiabetic drugs (nateglinide, repaglinide || pioglitazone || saxagliptin || sitagliptin)
    • Antiplatelet drugs (cilostazol || prasugrel || ticagrelor)
    • Cardiovascular drugs (amiodarone || diltiazem, verapamil || eplerenone || ivabradine || nifedipine || quinidine || ranolazine || tolvaptan)
    • Immunosuppressants (cyclosporine || tacrolimus || sirolimus)
    • Statins (atoravastatin || lovastatin || simvastatin)
    • Key HIV drugs (atazanavir || efavirenz || ritonavir || tipranavir)
    • PDE-5 inhibitors (avanafil || sildenafil || tadalafil || verdenafil)
  4. CYP INDUCERS
    • PS PORCS " (BIG INDUCERS)
    • Phenytoin
    • Smoking
    • Phenobarbital
    • Oxcarbazepine (and Eslicarbazepine)
    • Rifampin (and rifabutin, rifapentine)
    • Carbamazepine
    • St. John's Wort
    • ** inDucers == DECREASE levels/effects of substrates
  5. CYP INHIBITORS
    • " G <3 PACMAN " (BIG INHIBITORS)
    • Grapefruit
    • Protease Inhibitors (atazanavir | cobicistat, efavirenz | darunavir | ritonavir)
    • Azole Antifungals (fluconazole | itraconazole | ketoconazole | posaconazole | voriconazole | isavuconazole)
    • C = Cyclosporin, Cimetidine, Cobicistat
    • Macrolides (Clarithromycin, Erythromycin || but not azithromycin)
    • Amiodarone (& Dronedarone)
    • Non-DHP CCBs (Diltiazem & Verapamil)
    • ** iNhibitors == INCREASE levels/effects/ADR/Toxicities of substrates
  6. Breast Cancer Resistant Protein (BCRP)
    = efflux pump that works to prevent drugs from penetrating tissues such as brain, intestines, liver and kidneys
  7. Organic Anion Transporting Polypeptide (OATP)
    function is uptake in liver
  8. Organic Anion Transporter (OAT)
    Organic Cation Transporter (OCT)
    present in the gut, the liver and the kidneys == functions include uptake of subsrates
  9. P-glycoproteins (P-gp)
    • = efflux transporters found in the gut and other organs
    • PUMP drugs back into the gut (to exit out of the body)
    • ** if an inducer is given that causes the production of more pumps, the blood levels of the substrate will decrease
    • Important P-gp Substrates:
    • -- Digoxin
    • -- Calcineurin inhibitors (tacrolimus & cyclosporine)
    • -- Anticoagulants (dabigatran, apixaban & rivaroxaban)
  10. AMIODARONE
    - with digoxin and warfarin?
    - statins?
    • MUST dose decrease digoxin and warfarin by 30-50% when starting amiodarone
    • -- drug interaction between warfarin and amiodarone generally peak in 2 weeks, but can take up to 6 weeks
    • Simvastatin, Lovastatin, Atorvastatin == use lower doses
  11. DIGOXIN
    - renal?
    - K?
    - Drugs that decrease HR (HR<60)
    • Digoxin is P-gp substrate and interactions are important --> narrow therapeutic range
    • Decline in renal function == INcreases digoxin levels
    • Hypokalemia == digoxin toxicity is more likely
    • -- BUT digoxin toxicity causes HYPERkalemia
    • Dec in HR == primarily Beta-blockers and Non-DHP CCBs
    • -- other drugs that can lower HR (amiodarone, dexmedetomidine (Precedex), clonidine, opioids)
    • **Drugs Increase Digoxin Levels: quinidine, verapamil, erythromycin, clarithromycin, itraconazole, cyclosporine, propafenone, spironolactone, and a few others.
  12. Grapefruit Juice/Fruit Interactions
    • Inhibits 3A4 --> increase concentrations of 3A4 substrates
    • ** needs substantial amount (>1.2 liters)
    • Avoid Grapefruit == simvastatin, lovastatin, nifedipine, tacrolimus (transplant medications)
    • ** EXAM PURPOSES: Avoid Grapefruit/Juice if asked about 3A4 substrate! **
  13. Lamotrigine & Valproate
    • combination == high risk of Severe Rash
    • ** requires careful titration and self monitoring
  14. Monoamine Oxidase Inhibitors, Opioids and Serotonin Syndrome
    • MAO is the enzyme that metabolizes monoamines (neutrotransmitters which include dopamine, epinephrine, NE, serotonin)
    • MAO inhibitors should NOT be used with Serotoneric drugs ==> serotonin syndrome and/or HTN crisis
    • Serotonin Syndrom Sx: agitation, hallucination, rapid HR, fever, excessive sweating, shivering or shaking, muscle twitching or stiffness, trouble with coordination and/or N/V/D
    • STOP MAOi for a period of time (wash-out period) before starting other serotonergic drugs (2 WEEKS)
    • --X-- --X--
    • Tyramine Metabolism decreased with non-selective MAOi
    • -- Selegiline Patches (the 2 higher doses) OR Rasagiline --> avoid foods high in tyramine
    • -- Foods _ aged cheese, air-dried meats, certain wines and beer || "aged, fermented, pickled, smoked"
    • --X-- --X--
    • Serotonin syndrome when OPIOIDs are used with other serotonergic medications
    • ** Serotonergic Drugs == SSRIs, SNRIs, TCAs, etc. **
  15. Codeine
    • = metabolized by 2D6 to its active (analgesic) metabolite 
    • -- poor metabolizers OR 2D6 inhibitors == diminished effects on tramadol
  16. Codeine
    • = a partial prodrug for Morphine and undergoes conversion by 2D6 enzyme
    • -- ultrarapid metabolizers or extensive metabolizers of 2D6 == will produce morphine rapidly ==> FATAL (patient, breastfeeding infant)
  17. Fentanyl
    Hydrocodone
    Oxycodone
    Methadone
    • == OPIOIDS
    • -- primarily metabolized by 3A4
    • -- 3A4 iNhibitors == suffer fatal respiratory depression (AVOID USE)
    • -- 3A4 inDucers == possible subtherapeutic response
  18. PDE5-Inhibitors
    • == approved for ED, pulmonary arterial hypertension, benign prostatic hypertrophy
    • ** CI with NITRATES == severe HYPOtension **
    • -- are 3A4 substrates = higher doses of 3A4 iNhibitors --> more dizziness, orthostasis, flushing, HA
  19. CHELATION RISKS:
    Quinolones
    Tetracyclines
    • Separate with (CAUSES CHELATION and INHIBIT ABSORPTION):
    • -- Antacids || Multivitamins || Magnesium || Aluminum || Calcium || Iron || Zinc
    • -- Didanosine || Sucralfate || Bile acid resins || Phosphate binders
    • -- ANY product containing these multivalent Cations
  20. Statins (3)
    • Increased statin levels ==> higher risk for Muscle toxicity (muscle aches, soreness, weakness, Rhabdomyolysis)
    • ** Atorvastatin || Simvastatin || Lovastatin == higher risk of drug interactions **
  21. BLEEDING RISK
    • Anticoagulants || Antiplatelets || other agents that increases bleeding risk have an additive risk (higher risk depending on dose, age, number of drugs being used that carry bleeding risk)
    • AVOID == NSAIDS || SSRIs || SNRIs || natural products
    • -- 5 G's == Ginko biloba | Garlic | Ginger | Glucosamine | Ginseng
    • -- Fish oils (higher doses) | vitamin E | Willow bark
  22. HyperKalemia Risk
    • Potassium is renally cleared == SEVERE RENAL Disease --> HYPERKALEMIA
    • ** Aldosterone Antagonist (spironolactone, eplerenone) == avoid use if K is high (> 5 mEq/L) **
    • -- Other Additive Potassium Accumulation == ACE | ARBs | aliskiren | amiloride | triamterene
  23. CNS Depression
    • CNS side effects -- caused by drugs that enter the CNS (lipophilic) and primarily involve sedation (somnolence), dizziness, confusion, altered consciousness
    • Additive CNS Effects (16): 
    • -- EtOH
    • -- most Pain medications
    • -- skeletal muscle relaxants
    • -- anticonvulsants
    • -- benzodiazepines
    • -- barbituates
    • -- hypnotics
    • -- mirtazapine
    • -- trazodone
    • -- dronabinol
    • -- nabilone
    • -- propranolol
    • -- clonidine
    • -- sedating antihistamines
    • -- cough suppressants
    • -- illicit substances
  24. QT Prolongation & Torsade De Pointe (TdP)
    [7 classes]
    • Normal QT interval: < 440 ms
    • QT interval > 500 ms == higher risk for developing Arryhythmias
    • KEY DRUGS (7 class):
    • -- Antiarryhythmics (Class I (Ia) & Class 3)
    • -- Antibiotics (Quinolones & Macrolides)
    • -- Azole Antifungals (most)
    • -- Antidepressants (Tricyclics, SNRIs, SNRIs, mirtazipine, trazodone || Sertraline preferred in cardiac patients)
    • -- Antiemetic agents (5-HT3 receptor antagonists, droperidol, phenothiazines)
    • -- Antipsychotics (aripiprazole || asenapine || chlorpromazine || clozapine || haloperidol || iloperidone || olanzapine || paliperidone || pimozide || quetiapine || risperidone || thiordazine || ziprasidone)
    • Other agents (Donepezil || Methadone)
  25. Ototoxicity (5)
    • Increase Risk == higher drug levels PLUS duration of exposure
    • KEY DRUGS (5):
    • -- Salicylates
    • -- Vancomycin
    • -- Aminoglycosides 
    • -- Cisplatin 
    • -- Loop diuretics

Card Set Information

Author:
HNguyen0287
ID:
334502
Filename:
NAPLEX _ Drug Interactions
Updated:
2017-09-26 18:57:01
Tags:
NAPLEX RxPREP DrugInteractions
Folders:
RxPREP
Description:
RxPREP _ NAPLEX Review - Drug Interactions
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