CS612: EXAM 1 NSAIDs and Analgesics: Mechanisms, Uses, and Adverse Effects

What class is Acetaminophen?

Analgesic/antipyretic

What is Acetaminophen mainly used for?

Pain, fever

How does Acetaminophen work?

Primarily central analgesic/antipyretic; minimal peripheral anti-inflammatory effect

What are the major adverse effects of Acetaminophen?

Overdose → NAPQI-mediated hepatic injury

What is the exam pearl for Acetaminophen?

NAC replenishes glutathione; think liver toxicity

What class is Aspirin?

Salicylate; irreversible COX inhibitor

What is Aspirin mainly used for?

Pain, fever, inflammation; antiplatelet use

How does Aspirin work?

Irreversibly inhibits COX → ↓ prostaglandins and platelet TXA2

What are the major adverse effects of Aspirin?

GI bleeding, ulcer, tinnitus/salicylism, hypersensitivity

What is the exam pearl for Aspirin?

Irreversible platelet inhibition lasts platelet lifespan; avoid in Reye syndrome risk

What class is Capsaicin?

Topical analgesic; TRPV1 agonist/desensitizer

What is Capsaicin mainly used for?

Localized neuropathic/musculoskeletal pain

How does Capsaicin work?

Activates TRPV1 then depletes/desensitizes substance P signaling

What are the major adverse effects of Capsaicin?

Burning/irritation

What is the exam pearl for Capsaicin?

Topical heat/burning initially is expected

What class is Lidocaine?

Local anesthetic; sodium-channel blocker

What is Lidocaine mainly used for?

Local anesthesia; topical neuropathic pain

How does Lidocaine work?

Blocks voltage-gated Na+ channels

What are the major adverse effects of Lidocaine?

CNS toxicity, seizures, cardiac toxicity with systemic exposure

What is the exam pearl for Lidocaine?

Blocks Na+ channels; toxicity can be neurologic then cardiovascular

What class is Celecoxib?

Selective COX-2 inhibitor

What is Celecoxib mainly used for?

Pain/inflammation, OA/RA

How does Celecoxib work?

Preferentially inhibits COX-2 → ↓ prostaglandins

What are the major adverse effects of Celecoxib?

CV thrombotic risk, renal injury; GI effects still possible

What is the exam pearl for Celecoxib?

Less platelet/GI effect than nonselective NSAIDs, but CV/renal risk remains

What class is Diclofenac?

NSAID

What is Diclofenac mainly used for?

Pain/inflammation

How does Diclofenac work?

Reversible COX inhibition

What are the major adverse effects of Diclofenac?

GI bleeding, renal injury, hepatotoxicity, CV risk

What is the exam pearl for Diclofenac?

NSAID with notable hepatotoxicity signal

What class is Ibuprofen?

NSAID

What is Ibuprofen mainly used for?

Pain, fever, inflammation

How does Ibuprofen work?

Reversible COX-1/COX-2 inhibition

What are the major adverse effects of Ibuprofen?

GI bleeding, renal injury, edema/BP/CV risk

What is the exam pearl for Ibuprofen?

Common nonselective NSAID

What class is Indomethacin?

NSAID

What is Indomethacin mainly used for?

Inflammatory pain; gout/acute inflammation

How does Indomethacin work?

Reversible COX inhibition

What are the major adverse effects of Indomethacin?

GI/CNS adverse effects, renal injury

What is the exam pearl for Indomethacin?

Potent NSAID; high adverse-effect burden

What class is Ketorolac?

NSAID

What is Ketorolac mainly used for?

Short-term moderate/severe acute pain

How does Ketorolac work?

Reversible COX inhibition

What are the major adverse effects of Ketorolac?

GI bleeding, renal injury, bleeding

What is the exam pearl for Ketorolac?

Think short-term use; strong GI/renal/bleeding concerns

What class is Meloxicam?

NSAID; relatively COX-2 preferential

What is Meloxicam mainly used for?

OA, RA, inflammatory musculoskeletal pain

How does Meloxicam work?

Reversibly inhibits COX enzymes → ↓ prostaglandins

What are the major adverse effects of Meloxicam?

GI ulcer/bleeding, renal injury, edema, ↑ BP, CV thrombotic risk

What is the exam pearl for Meloxicam?

Relative COX-2 preference, but NOT as selective as celecoxib

What class is Naproxen sodium?

NSAID

What is Naproxen sodium mainly used for?

Pain, fever, inflammation

How does Naproxen sodium work?

Reversible COX-1/COX-2 inhibition

What are the major adverse effects of Naproxen sodium?

GI bleeding, renal injury, edema/BP/CV risk

What is the exam pearl for Naproxen sodium?

Longer-acting NSAID; same major class toxicities

What class is Nepafenac?

Ophthalmic NSAID prodrug

What is Nepafenac mainly used for?

Ocular inflammation/pain after surgery

How does Nepafenac work?

Converted to amfenac; inhibits COX

What are the major adverse effects of Nepafenac?

Ocular irritation, delayed healing/bleeding risk

What is the exam pearl for Nepafenac?

Ophthalmic NSAID; remember local ocular adverse effects

What class is Amitriptyline?

TCA

What is Amitriptyline mainly used for?

Neuropathic pain

How does Amitriptyline work?

Inhibits NE/5-HT reuptake; analgesic effects in descending pathways

What are the major adverse effects of Amitriptyline?

Anticholinergic effects, sedation, orthostasis, cardiac conduction toxicity

What is the exam pearl for Amitriptyline?

TCA + neuropathic pain; anticholinergic and cardiac toxicity

What class is Carbamazepine?

Anticonvulsant; Na+ channel blocker

What is Carbamazepine mainly used for?

Trigeminal neuralgia; seizures

How does Carbamazepine work?

Use-dependent voltage-gated Na+ channel blockade

What are the major adverse effects of Carbamazepine?

Hyponatremia, rash/SJS-TEN, blood dyscrasias, interactions

What is the exam pearl for Carbamazepine?

Classic drug for trigeminal neuralgia

What class is Duloxetine?

SNRI

What is Duloxetine mainly used for?

Neuropathic pain; depression/anxiety

How does Duloxetine work?

Inhibits NE/5-HT reuptake

What are the major adverse effects of Duloxetine?

Nausea, insomnia, BP changes, serotonin toxicity

What is the exam pearl for Duloxetine?

SNRI used for neuropathic pain

What class is Gabapentin?

Gabapentinoid

What is Gabapentin mainly used for?

Neuropathic pain; seizures

How does Gabapentin work?

Binds α2δ subunit of voltage-gated Ca2+ channels

What are the major adverse effects of Gabapentin?

Sedation, dizziness, edema

What is the exam pearl for Gabapentin?

α2δ calcium-channel ligand; renal elimination

What class is Pregabalin?

Gabapentinoid

What is Pregabalin mainly used for?

Neuropathic pain; fibromyalgia; seizures

How does Pregabalin work?

Binds α2δ subunit of voltage-gated Ca2+ channels

What are the major adverse effects of Pregabalin?

Dizziness, somnolence, edema, weight gain

What is the exam pearl for Pregabalin?

Similar mechanism to gabapentin; more predictable kinetics

What class is Venlafaxine?

SNRI

What is Venlafaxine mainly used for?

Depression/anxiety; neuropathic pain adjunct

How does Venlafaxine work?

Inhibits NE/5-HT reuptake

What are the major adverse effects of Venlafaxine?

Nausea, BP elevation, discontinuation symptoms, serotonin toxicity

What is the exam pearl for Venlafaxine?

SNRI; higher doses emphasize NE effects

What class is Baclofen?

GABA-B agonist

What is Baclofen mainly used for?

Spasticity

How does Baclofen work?

Activates GABA-B receptors → reduces excitatory neurotransmission

What are the major adverse effects of Baclofen?

Sedation, weakness, hypotonia; withdrawal with abrupt stop

What is the exam pearl for Baclofen?

GABA-B = spasticity; abrupt withdrawal can be dangerous

What class is Carisoprodol?

Centrally acting muscle relaxant; metabolite meprobamate

What is Carisoprodol mainly used for?

Acute musculoskeletal spasm

How does Carisoprodol work?

CNS depressant effects

What are the major adverse effects of Carisoprodol?

Sedation, dependence/misuse, withdrawal

What is the exam pearl for Carisoprodol?

Metabolized to meprobamate; dependence concern