Exam 3 Medications Flashcards
acetaminophen
Drug Class: APAP
Indication: mild to moderate pain
MOA: inhibits prostaglandin synthesis (COX activity)
Onset/duration: 15 min/4 hr
Elimination: hepatic
Adverse Effects: liver toxicity b/c of highly reactive metabolite (NAPQI); unintentional overdoses
ibuprofen
Drug Class: NSAID
Indication: pain r/t inflammation
MOA: inhibits cyclo-oxygenase
Onset/duration: 60 min/4-6 hr
Elimination: hepatic, then renal
Adverse Effects:
- COX1>COX2 = bleeding
- COX2>COX1 = thrombosis/stroke
- all NSAIDS: renal toxicity, elevated BP/CV risk
morphine
Drug Class: opioid (gold standard)
Indication: moderate to severe pain
MOA: mu-opioid receptor agonist
3:1::oral:parenteral potency ratio
Onset: 30 min (PO); 5 min (IV)
Duration: 4 hrs; T1/2 = 2-4 hr
Elimination: glucuronidation
- Morphine-3-glucuronide (M3G); neurotoxicity/hyperalgesia)
- Morphine-6-glucuronide (M6G); analgesia, 1% of product)
fentanyl
Drug Class: opioid
Indication: moderate to severe pain
MOA: mu-opioid receptor agonist
Onset: IV - instantaneous transdermal - 12-24 hrs transmucosal - 5-15 min Duration: IV - 30-60 min transdermal - 72 hrs
Elimination: via CYP3A4 to inactive metabolites (fentanyl and nonfentanyl)
T1/2 = 2 hrs (IV)
naloxone
Drug Class: opioid reversal agent
Indication: opioid reversal
MOA: mu-opioid-receptor antagonist
Duration: 1h (IV), longer (SC)
Elimination: hepatic (T1/2 = 1-2 hr)
Adverse Effects: hyperalgesia, withdrawal syndrome, seizure, CV instability
Interactions: opioid agonists
tramadol
Drug Class: opioid
Indication: mild to moderate pain
MOA: weak mu-opioid agonist; weak NE/5HT reuptake inhibition
Elimination: O-demethylated to active metabolite (M1) via CYP2D6
-Renal/hepatic dosing based on CYP2D6/3A4 enzymes
IV controlled substance
Side Effects: sedation, dizziness, dry mouth, nausea, constipation, respiratory depression, seizure risk
Adverse Rxns: hypersensitivity rxns
Interactions: CNS depressants, carbamazepine, MAO-inhibitors, serotonin/norepinephrine-reuptake inhibitors (SSRI/SNRI), tricyclic antidepressants
anticonvulsants (general)
Indication: neuropathic/chronic pain syndromes
MOA: prevent bursts of action potentials on injured nerves by modulating/inhibiting sodium or calcium channels
- require upward/downward titration
- great variability in therapeutic response
pregabalin or gabapentin
Drug Class: anticonvulsant
Indication: neuropathic/chronic pain
MOA: calcium channel modulation
Elimination: renal
Adverse Effects: sedation, weight gain, peripheral edema, dizziness
Interactions: other CNS depressants
carbamazepine (tegretol)
oxcarbazepine (trileptal)
Drug Class: anticonvulsant
Indication: neuropathic/chronic pain
MOA: AED - sodium channel inhibitors
Elimination: auto-induction (increased rate of metabolism)
Adverse Effects: SIADH/hyponatremia, sedation, dizziness, nausea, leukopenia or thrombocytopenia (2%)
duloxetine
venlafaxine
Drug Class: SNRIs
Indication: neuropathic pain, some musculoskeletal syndromes
MOA: selective serotonin/norepi reuptake inhibition
Metabolism:
duloxetine: CYP2D6, 1A2
venlafaxine: CYP2D6 to active metabolite
Adverse Effects: N/V, suicide, withdrawal syndromes, serotonin syndrome
amitriptyline
nortriptyline
Drug Class: TCAs
Indication: neuropathic/chronic pain
MOA: tricyclic antidepressants - serotonin, noepi reuptake inhibition
Elimination: hepatic metabolism, then renal elimination - no dosing adjustments
Adverse Effects: secondary amines assoc. w/ anticholinergic effects than tertiary amines; decreased seizure threshold, orthostasis, QTc prolongation, serotonin syndrome
procain
lidocaine
Drug Class: local anesthetic
Indication:
MOA: inhibit sodium channels and impulse conduction along axons (penetration depends on molecular size, lipid solubility, degree of ionization)
Adverse Effects: systemic absorption - bradycardia, heart blocks, cardiac arrest, hypotension
*topical or spina/epidural
Adverse Effects:
(spinal/epidural) - autonomic blockade that disrupts GI/GU; (fecal incontinence/retention, hypotension, HA, hematoma)
lidocaine patches
Drug Class: local
Indication: post-herpetic neuralgia
MOA: inhibit Na channels; impose non-depolarizing conduction block of action potential
- minimal systemic effects
- co-analgesic in combo with opioid, antidepressant, anticonvulsant
- 12 hrs off patch/day; up to 3 at a time
adverse effects of opioids
CNS: dependence/abuse, sedation, psychotomimetic, vertigo, myoclonus, resp. depression, neurocognitive
GI: constipation, nausea
GU: urinary retention
Integumentary: flushing, urticaria, pruritis
Metabolic: stimulate ADH, prolactin, somatotropin, loss of libido
Cardiovascular: hypotension, reflex tachycardia
Ocular: miosis
Immune: decreased fxn with chronic dosing
amoxicillin
Drug Class: penicillin
Indication: G+ infections and some G- aerobes
MOA: PBP binding
Absorption: acid stable with good bioavailability, not impaired by food
Distribution: most tissue/body fluid
Elimination: renally unchanged
Adverse Effects: CNS, allergic rxn, interstitial nephritis
Interactions: warfarin
amoxicillin + clavulanate
Drug Class: penicillin + B-lactamase inhibitor
clavulanate has no antibacterial activity by itself - beta lactamase inhibitor
cephalexin
Drug Class: cephalosporin
Indication: susceptible strains of bacteria (ex: staphylococci and streptococci - skin infections)
MOA: PBP binding. 1st gen
Distribution: most tissy/body fluid (T1/2 = .5-1hr)
Elimination: renal
Adverse Effects: C. difficile, allergic rxn
cefepime
Drug Class: cephalosporin
Indication: susceptible strains of G+/-
MOA: PBP binding. 4th gen.
Dose: IV or IM ONLY
Distribution: most tissue/body fluid, CSF (T1/2 = 2h)
Elimination: renal
Adverse Rxns: encelphalopathy, seizures, thrombophlebitis, allergic rxn
imipenem
Drug Class: carbapenem
Indication: susceptible strains of G+ cocci, G- bacilli and cocci, mixed aerobic/anaerobic infections. extremely broad spectrum.
MOA: PBP binding
Dose: IV or IM ONLY
Distribution: widely distributed including CSF (T1/2 = 1h)
Elimination: renal
Adverse Effects: superinfections
Interactions: valproate (reduces levels, precipitating seizures)
vancomycin
Drug Class: glycopeptide
Indication: MRSA, MRSE, susceptible strains of G+ in pts with B-lactam allergy
MOA: binds to cell wall synthesis precursor molecules
Dose: oral is for C. diff infections. Draw trough immediately before infusing next dose.
Distribution: well distributed in tissue/fluids (T1/2=6h)
Elimination: renal
Adverse Effects: renal failure/nephrotoxicity, ototoxicity (reversible), red man syndrome from rapid IV infusion
doxycycline
Drug Class: tetracycline
Indication: broad, wide variety of G+ and G-. First line for rickettsial diseases. active against MRSA.
MOA: binds to #0S ribosomal unit to disrupt bacterial protein synthesis
Distribution: wide, poor CSF penetration
Elimination: HEPATIC
Adverse Effects: photosensitivity, superinfection, tooth discoloration, long-bone in premature infants
Interactions: warfarin, lithium; calcium, magnesium, and iron decrease absorption (includes food - give doxy 1 hr before or 4 hrs after)
azithromycin
Drug Class: macrolide
Indication: susceptible G+ and G- bacteria strains
MOA: binds to 50S ribosomal subunit to disrupt protein synthesis
Distribution: most tissue/fluid (T1/2 = 60h)
Elimination: hepatic MORE than renal
Adverse Effects: ototoxicity, dysrhythmia (Torsades de Pointes), allergic rxn
Interactions: warfarin, medications that affect heart rhythm
gentamicin
Drug Class: aminoglycoside
Indication: serious infections by aerobic G- bacilli
MOA: binds to 30S ribosomal subunit to disrupt protein synthesis
Dose: IV and IM. NO PO
Distribution: well distributed in ECF, crosses placenta, concentrates in renal and inner ear cells (T1/2 = 2h)
Elimination: renally unchanged
Adverse Effects: irreversible ototoxicity, nephrotoxicity; hypersensitivity
Interactions: penicillins (synergy - don’t mix in IV bag); neuromuscular blockers, ototoxins, nehprotoxins
linezolid
Drug Class: oxazolidinone
Indication: severe infections by MDR G+ organisms (VRE, MRSA)
MOA: Binds to 50S ribosomal subunit (23-S portion) to disrupt protein synthesis. 1st in class.
Elimination: hepatic met. w/ renal excretion
Adverse Effects: bone marrow suppression (need CBC weekly), hepatotoxicity
Interactions: tyramine, MAO inhibitors (hypotension), SSRIs (serotonin syndrome)
clindamycin
Drug Class: other
Indication: susceptible anaerobes and some G+ aerobes
MOA: binds to 50S ribosomal subunit to disrupt protein synthesis (overlaps macrolide site)
Dose: intravaginally for bacterial vaginosis
Distribution: most tissue/fluid (T1/2 = 3h)
Elimination: hepatic met., active and inactive metabolites excreted in bile and urine
Adverse Effects: C. diff –> pseudomembranous colitis, cardiovascular effects w/ rapid IV, hypersensitivity rash, hepatotoxocitiy, blood dyscrasias
levofloxacin
Drug Class: fluoroquinolone
Indication: susceptible G- and some G+, atypicals
MOA: inhibits DNA gyrase and topoisomerase 4, preventing DNA replication and cell division
Absorption: rapid/complete absorption
Distribution: wide - concentrates in urine, stool, bile, saliva, prostate, bone (T1/2 = 5-7h)
Elimination: hepatic met., renal excretion
Adverse Effects: phototoxicity, QT prolongation, tendonitis w. rare tendon rupture
Interactions: warfarin, drugs that affect heart rhythm, calcium
metronidazole
Drug Class: other
Indication: susceptible anaerobes (C.diff), some protozoal infections, bacterial vaginosis
MOA: causes strand breaks in DNA structure
Dose: loading dose and maintenance dose
Elimination: hepatic met. (CYP3A4), then renal > biliary excretion (T1/2 = 6-8h)
Adverse Effects: pancreatitis, avoid 1st trimester
Interactions: ethanol, warfarin, phenobarbital, phenytoin
AVOID all alcohol - disulfiram-like rxn with violent vomiting
co-trimoxazole
Drug Class: other (trimethoprim + sulfamethoxazole)
Indication: susceptible organisms. effective against MRSA, but resistance is evolving
MOA: synergistic effect on folic acid metabolism
Elimination: hepatic met. then renal excretion
Adverse Effects: hyperkalemia, crystalluria w. renal damage
Avoid if sulfonamide allergy
Drink 8-10 glasses water/day to dilute urine
sulfamethoxazole
Drug Class: sulfonamide
Indication: susceptible G+ cocci, G- bacilli
MOA: inhibits folic acid synthesis required for growth
Dose: only available in combination with trimethoprim
Distribution: well absorbed, distribution to all tissues including pleural and ocular
Elimination: hepatic met. via acetylation, renal excretion of inactive but potentially dangerous metabolites
Adverse Effects: kernicterus (bilirubin accumulation in brain), Stevens-Johnson Syndrome, blood dyscrasia, hemolytic anemia, avoid w. sulfonamide allergy
Interactions: phenytoin, warfarin, sulfonylureas
trimethoprim
Drug Class: other
Indication: susceptible G+ bacilli and G- bacilli, some protozoa
MOA; inhibits folic acid synthesis required for growth
Distribution: completely absorbed w/ widespread distribution including placental transfer. lipophilic (cross blood-brain barrier)
Elimination: renally unchanged, concentrating in urine
Adverse Effects: N/V, glossitis, stomatitis. avoid in pregnancy/lactation/folate deficiency. hyperkalemia
