NSAID/Opioid Patho Stuff

Acetic Acid

Diclofenac

Relatively selective for COX2

Propionic Acid

Ibuprofen, Fenoprofen, Ketoprofen, Naproxen, Naproxen sodium

Pyrrolizine carboxylic acid

Ketorolac

Potent, 5 day max treatment

Enol Acids

meloxicam - relatively selective cox2

piroxicam - non selective

Fenamates

Meclofenamate and Mefenamic acid

Pyranocarboxylic acid

Etodolac

Relatively more selective inhibitor of COX-2

Pyrazoles

Celecoxib

Better GI tolerability with chronic use.- Six COX-2 inhibitors (-coxibs), were initially approved for clinical use

Para-aminophenol

Acetaminophen

Noncompetitive reversible inhibitor by acting at the peroxide site of the COX enzymes

Inhibitory activity is reduced at sites of inflammation where peroxide levels are elevated

Natural Opioids

Morphine

Codeine

Semi-synthetic Opioids

Diacetylmorphine (heroin)

Oxycodone

Buprenorphine

Hydrocodone

Synthetic Opioids

Pethidine

Fentanyl

Methadone

Tramadol

Mu Opioid receptor

Recycle into the MEMBRANE

Delta Opioid receptor

DEGRADES

Kappa Opioid receptor

KANNOT degrade/recycle

Phenathrenes

Morphine

Codeine

Hydro/oxymorphone

hydro/oxycodone

Levorphanol

Phenylpiperidines

Meperidine

Fentanyl

Diphenylheptanes

Methadone - Long acting, L isomer superior to D isomer

Hydromorphone

Like morphine, but faster onset and higher potency

Oxymorphone

potent MOR agonist, oxycodone is metabolized into this

Hydrocodone

synthesized from codeine, equipotent to oxycodone

Levorphanol

Affinity for MOR as well as DOR and KOR

7x more potent than morphine

Less nausea and vomiting.

Meperidine

Lesser constipation and urinary retention (likely due to greater ability to enter CNS)

stronger than morphine

Butorphanol and nalbuphine

Competitive MOR antagonists, but analgesic effects mediated by agonist activity at KORs

Pentazocine

Weaker MOR antagonist or partial agonist but retains KOR agonist activity

Tramadol

Weak MOR agonist.- Part of the analgesic effect due to inhibition of NE and 5HT uptake M1 metabolite is several times more potent than parent drug

Similar analgesic effect to morphine and meperidine for mild-to-moderate pain

Methylnaltrexone and naloxegol

Only antagonizes peripheral effects

Post-op ileus

Alvimopan

Used for treatment of postoperative ileus in patients with less than 7days of opioid exposure

MOR antagonist, only peripherally

Diflunisal

Derivative of salicylic acid

Competitive inhibitor of COX

3 to 4 times more potent than aspirin