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