NAPLEX Study Guide

Beta-1 receptor MOA

Bind mainly on heart, causing increasing heart rate and contractility

Selective beta-1 agonist

Dobutamine, Isoproterenol, Dopamine

Selective beta-1 antagonist

Metoprolol, Atenolol, Bisoprolol, Esomolol

Beta-2 receptor MOA

Bind mainly on lung, causing bronchodilation & bronchial muscle relaxation

Selective beta-2 agonist

SABA: Albuterol, Levalbuterol, Terbutaline

LABA: Salmeterol, Formoterol, Indacterol

Non-selective beta antagonist

Propranolol, Nadolol, Timolol

Alpha -2 MOA

Mainly on brain. Agonist cause decrease in Epi & NE and decrease in HR & BP)

Selective alpha-2 agonist

Clonidine, Guanfacine, Dexmedetomidine

Selective alpha-2 agonist

Clonidine, Brimonidine (for glaucoma)

Alpha-1 MOA

Mainly on peripheral smooth muscle & vasoconstriction. Agonist cause increase in BP. Antagonist cause decrease in BP

Selective alpha-1 agonist

Phenylephrine, Midodrine (for low BP), Oxymetazolin (for congestion)

Non-selective alpha & beta agonist

Epinephrine

• NE is more alpha in MOA (more peripheral BP impact for shock)

Non-selective alpha & beta antagonist

Carvedilol, Labetalol

Dopamine agonist

Levodopa, Pramipexole (for depression, parkinson, RLS)

Dopamine antagonist

First-gen antipsychotics

• Haloperidol, Fluphenazine, Chlorpromazine, Perphenazine

Partial dopamine agonist

Aripiprazole, Brexpiprazole, Cariprazine

Serotonin agonist

Triptans

• Sumatriptan

Buspirone, Lorcaserin (for weight loss)

Serotonin antagonist

Ondansetron, Palonosetron

Second-gen antipsychotics

• Aripiprazole, Olanzapine, Risperidone, Quetiapine, Ziprasidone, Lurasidone, Paliperidone

MAO inhibitor

Phenelzine, Isocarboxazid, Tranycypromine, Selegiline, Rasagiline

• Blocking MAO will increase catecholamine level—> excessive catecholamine level can cause hypertension crisis or serotonin syndrome

MAO additive effect

MAO inhibitor MOA:

• Hypertension crisis: inhibit MAO enzyme which blocks the breakdown of neurotransmitters that cause increase in Epi & NE & dopamine

  • Symptoms: HTN, tachycardia, agitation, death

  • DDI: bupropion, SNRI, TCA, stimulants, levodopa, linezolid, methylene blue, tyramine (from food)

• Serotonin syndrome: inhibit MAO enzyme which blocks the breakdown of 5-HT, causing 5-HT increase in serum

  • Symptoms: tremor, akathisia, clonus, hyperthermia, sweating

  • DDI: SSRI, SNRI, TCA, mirtazapine, trazodone, triptans, opioids, tramadol, buspirone, lithium, dextromethorphan, St. John’s wart

Benzodiazepine additive effects

Agonist to different receptors: BZD bind and enhance the effect of GABA (inhibitory neurotransmitter), causing relaxing, hypnotic and anticonvulsant effect on muscle

• Side effect associated: respiratory suppression (especially with the co-use of opioids)— BBW

Chelation effect

Definition: chelation happen when a drug bind to polyvalent cations (Mg2+, Ca2+, Fe2+), resulting in an indissoluble complex in the gut fluid. The medication efficacy will significantly decrease

• Quinolone antibiotics & Ca2+

• Azithromycin & Mg+ & Al3+

• Levothyroxine & antacids, multivitamine, sucralfate, Mg2+, Al3+, zinc

  • Itraconazole & PPI

CYP450 metabolism used by manufacture

• Increase bioavailability

  • Valacyclovir metabolize to acyclovir by CYP450

• Percent drug abuse

  • Lisdexamfetamine is lysine + amphetamine to prevent crushing or snorting of the drug

Common CYP inhibitors

G ♥ PACMAN

G: grapefuit

P: protease inhibitor (PIs)

• especially ritonavir

A: azoles

C: cyclosporine, cobicistat

M: macrolides

A: amiodarone & dronedarone

N: non-DHP CCBs

• diltiazem, verapamil

Common CYP inducers

PS PORCS

P: phenytoin (anti-seizure class)

S: smoking

O: oxcarbazepine

R: rifampin, rifabutin, rifapentine

C: carbamazepine

S: St. John’s wort

Pgp efflux pumps

MOA: located in GI

• With Pgp blocker, dry will have increased absorption, resulting in increased serum drug cons

• At the mean time, OATP1B1/3 pumps drug from blood to the liver

Pgp inducers

Carbamazepine

Dexamethasone

Phenobarbital

Phenytoin

Rifampin

St.John’s wort

Tipranavir

Pgp inhibitors

Anti-infection (clarithromycin, itraconazole, posaconazole)

Cardiovascular drug (amiodarone, carvedilol, conivaptan, diltiazem, dronedarone)

HIV drug (ledipasvir)

HIV drug (cobicistat, ritonavir)

Other (cyclosporine, fibanserin, ticagrelor)

Common DDI

Amiodarone + Warfarin

• Amiodarone is CYP2C9 inhibitor

• Start warfarin at lower dose <5 mg or decrease warfarin dose by 30-50%

Amiodarone + Digoxin

• Amiodarone is Pgp inhibitor and digoxin is Pgp substrate

  • Effect: decrease digoxin excretion, increase risk of bradycardia

• Start oral digoxin dose at 0.125 mg QD or decrease digoxin dose by 50%

Digoxin + Loop diuretics

• Loop will decrease conc of K, Mg, Ca, Na, and decrease in these electrolytes will increase digoxin toxicity (arrhythmia, nausea, vomiting, vision changes, bradycardia)

Statin + strong CYP3A4 inhibitors

Valproate + Lamotrigine

• Valproate will decrease lamotrigine metabolism, causing SE like SJS/TEN

• Start lamotrigine with starter kit and titrate Q2wks

Smoking + Antipsychotics, Hypnotics, Antidepressants, Warfarin, Anxiolytics, Caffeine

• CYP1A2 inducer

QTC prolonging drug

Antiarrhythmics

Anti-infections

• Antimalarials: hydroxychloroquine

• Azoles (except isavuconazonium)

• Lefamulin

• Macrolides

• Quinolones

Antidepressants (highest risk with citalopram & escitalopram)

Antipsychotics

• First gen: haloperidol, thioridone, etc

• Second gen (highest risk with ziprasidone)

Antiemetics: ondansetron

Oncology medication

• Androgen deprivation therapy: leuprolide

• Tyrosine kinase inhibitors: nilotinib

• Arsenic trioxide

Other: Donepazil, Hydroxyzine, Loperamide, Ranolazine, Methadone, Cilostazol, Fingolimod, Solifenacin

Ototoxicity causing drug

Aminoglycosides

• Gentamicin, Tobramycin, Almikacin

Cisplatin

Loop diuretics (especially in rapid IV)

• FUrosemide, Bumetanide, Ethacrynic acid

Salicylates

• ASA, Salsalate, Mg salicylate

Vancomycin

Nephrotoxic drug

Anti-infections

• Aminoglycosides, Amphotericin B, Polymyxins, Vancomycin

Cisplatin

Calcineurin inhibitors

• Cyclosporine, Tacrolimus

Loop diuretics

• Furosemide, Torsemide, bumetanide, ethacrynic acid

NSAIDs

Radioactive dye

Anticholinergic drug

Antidepressant/ Antipsychotics

• Paroxetine, TCAs, First-gen antipsychotics

Sedating antihistamine

• Diphenhydramine, Brompheniramine, Chlorpheniramine, Doxylamine, Hydroxyzine, Meclizine, Cyproheptadine

Centrally-acting anticholinergics

• Benztropine, Trihexyphenidyl

Muscle relaxant

• Baclofen, Carisoprodol, Cyclobenzaprine

Antimuscarinics (for urinary incontinence)

• Oxybutynin, Darfenacin, Tolterodine

Other

• Atropine, Belladonna, Dicyclomine

Drugs that affect potassium lvl

Increase lvl due to:

• ACE/ ARB-i, Spirololactone, Canagliflozin, Cyclosporine, Tacrolimus, Bactrim, Drospirenone, Aliskiren, Potassium supplement

Decrease lvl due to:

• Beta-2 agonist, Diuretics, Insulin, Sodium polystyrene sulfonate

Drugs that affect folic acid lvl

Decreased lvl due to:

• Phenytoin, Fosphenytoin, Phenobarbital, Primidone, MTX

Drugs that affect G6PD

Dapsone, Methylene blue, Nitrofurantoin, Pegloticase, Primaquine, Rasburicase, Quinidine, Quinine, Sulfonamide

Common vesicant

Vasopressors (e.g., dopamine, norepinephrine, vasopressin, phenylephrine, etc)

Anthracycline (e.g., doxorubicin)

Vinca alkaloids (e.g., vincristine)

Digoxin

Foscarnet

Mannitol

Mitomycin

Nafcillin

PromethazineCVP

PVC compatibility

Drug that requires NON-PVC containers: LATTIN (leach absorbs to take in nutrients)

• Lorazepam

• Amiodarone

• Tacrolimus

• Taxanes

• Insulin

• Nitroglycerin

Dextrose compatibility

Drugs that can only be mixed in dextrose: Only Sugar Always

• Oxaliplatin

• Sulfamethoxazole/ trimethoprim

• Amphotericin B

Saline Compatibility

Drugs thats can only be mixed in saline: A DIAbetic Cant Eat Pie

• Ampicillin

• Daptomycin

• Infliximab

• Ampicillin/ sulbactam

• Caspofungin

  • Ertapenem

• Phenytoin

Fatal precipitation

Calcium + Ceftriaxone

Calcium + Phosphate

* Warning: LR contains calcium

Common filter needle size

Most common filer needle size: 0.22 micron filter

Parental nutrition often use 1.2 micron filter needles for lipids and calcium-phosphate particulate

Drugs that can't be refrigerated

Trick: Dear Sweet Pharmacist, Freezing Makes Me Edgy

• Dexmedetomidine (Percedex)

• Sulfamethoxazole/ trimethoprim

• Phenytoin- crystalize*

• Furosemide- crystalize*

• Metronidazole

• Moxifloxacin

• Enoxaparin

• Acetaminophen

• Acyclovir- crystalize*

• Deferoxamine- crystalize*

• Pentamidine- crystalize*

• Levetiracetam

• Valproate

Drugs that should be protected from the light

Trick: Protect Every Necessary Med from Daylight

• Phytonadine (vitamine K)

• Epoprostenol

• Nitroprusside

• Micafungin

• Doxycycline

Discoloration caused by drugs

Red

• Anthracyclines

• Rifampin- urine, saliva, sweat, tears

Blue

• Mitoxantrone

Yellow

• MTX

• Multivitamin Infusion

Yellow/ Orange

• Tigecycline- teeth

Brown

• IV iron- urine

Component of social determinants of health

• Education access and quality

• Health care access and quality

• Economic stability

• Social and community context

• Neighborhood and built environment

CrCl contradiction in CKD

CrCl <60

nitrofurantoin

CrCl contradiction in CKD

CrCl <50

TDF (Complera, Delstrigo, Stribild)

Voriconazole IV

CrCl contradiction in CKD

CrCl <30

TAF (Biktarvy, Descovy, Genvoya, Odefsey, Symtuza)

NSAIDs

Dabigatran

Potassium-sparing diuretics

eGFR contradiction in CKD

eGFR <30

Metformin

Phosphate binders

Aluminum hydroxide (Al³⁺ based)

• SE: aluminum toxicity (CNS effect), osteomalacia, constipation

• Max duration 4 wks

Calcium acetate (Ca²⁺ based)

• SE: hypercalcemia, constipation

Sucroferric oxyhydroxide, ferric citrate (metal based)

• SE: iron toxicity, discolored feces, constipation (ferric citrate)

Lanthanum carbonate (metal based)

• Warning & contradiction: GI perforation, GI obstruction, fecal impaction, ileus

• SE: nausea, diarrhea, constipation

• Chew tablet thoroughly to avoid GI effect

Sevelamer (non-calcium, non-metal based)

• Warning

  • Reduce absorption of vitamin D, E, K, and folic acid

  • Tablet form cause dysphagia (caution of pt who has trouble swallowing)

• Contradiction: bowel obstruction

• SE: n/v, diarrhea, metabolic acidosis (sevelamer hydrochloride)

• Lower cholesterol & LDL

Phosphate binders DDI

Polyvalent ion (Al³⁺, Fe³⁺, Ca²⁺)

Levothyroxine

Quinolone

Tetracyclines

Vitamin D analogs & calcimimetics

Calcitriol, calcifediol, doxercalciferol, paricalcitol (vitamin D analog)

• Warning & contradiction: hypercalcemia, vitamin D toxicity

• SE: hyperphosphatemia, n/v/d

• Take with food to decrease GI upset

Cinacalcet, etecalcetide (Calcimimetics)

• Warning: hypocalcemia (QTc prolongation, seizure), GI bleed, decreased bone turn over

• SE: n/v/d, anorexia, myalgia

Erythropoiesis stimulating agent

Epoetin alfa, darbepoetin alfa

• SE: HTN, DVT/PE/stroke

• ONLY initiate when Hgb <10 g/dL

• D/c if Hgb >11

• Assess iron panel & give IV iron as ESA ONLY works with adequate iron

Vadadustat

• PO ESA for dialysis >3 mon pts

Drugs that increase potassium level

Canagliflozin

Calcineurin inhibitors (cyclosporine, tacrolimus)

Drospirenone- containing OC

Potassium-sparing diuretics

ACE/ARB

Bactrim

Hyperkalemia treatment

1. Stabilize the heart→ calcium (gluconate > chloride)

2. Move K

   • → insulin + dextrose

   • → sodium bicarb (for metabolic acidosis)

   • → albuterol (SE: tachycardia, chest pain)

3. Remove K

   • → loop diuretics (monitor volume)

   • → sodium polystyrene sulfonate

   • → patiromer