Analgesic Agents Flashcards
Suboxone
Generic Name: Buprenorphine/Naloxone
Drug Class: Analgesic; Opioid Partial Agonist and Antagonist Combination, CIII
Mechanism of Action:
Uses: opioid use disorder
Metabolism: Buprenorphine: hepatic, major substate of CYP3A4/5; Naloxone: hepatic via glucuronidation
Normal Daily Dose: 2mg/0.5 mg, 4mg/1mg, 8mg/2mg, 12mg/3mg
Soma
Generic Name: Carisoprodol
Drug Class: Centrally Acting Skeletal Muscle Relaxant; CIV
Uses: treats skeletal muscle conditions such as pain or injury
Mechanism of action: blocks pain sensation between the nerves and the brain
Normal Daily Dose: taken three times per day and at bedtime, should only be taken for two or three weeks; 250mg, 350 mg
Metabolize: Hepatic; major substrate of CYP2C19
Celebrex
Generic Name: Celecoxib
Drug Class: Cox-2 inhibitors (NSAID)
Uses: treat pain or inflammation such as arthritis, ankylosing spondylitis, and menstrual pain
Mechanism of action: selective inhibition of cyclooxygenase-2 (COX-2)
Normal Daily Dose: 100-200 mg twice a day
Metabolize: Hepatic 97%; major substrate of CYP2C9; moderate inhibitor of CYP2C8 and 2D6
Tylenol with Codeine
Generic Name: acetaminophen and codeine
Drug Class: Narcotic Analgesic; CII
Uses: to relieve moderate to severe pain, cough
Mechanism of Action: agonism if mu-opioid receptors
Normal Daily Doses: 1-2 tablets every 4 hours as needed
Metabolize: a prodrug that requires activation by CYP2D6 to morphine; substrate of CYP2D6
Flexeril
Generic Name: cyclobenzaprine
Drug Class: Centrally Acting skeletal muscle relaxant
Uses: to treat skeletal muscle conditions such as pain or injury
Mechanism of Action: blocks transmission through the neuromuscular junction at nicotinic receptors
Normal Daily Doses: 10 mg po three times a day. max quantity of 60mg.
Metabolize: Extensive hepatic; substrate of CYP1A2
Voltaren
Generic Name: diclofenac
Drug Class: NSAID
Uses: used to reduce pain and inflammation. osteoarthritis/rheumatoid arthritis
Mechanism of Action: inhibits cyclooxygenas-1 and -2 responsible for the production of prostaglandin
Normal Daily Doses: 50 mg 2-3 times a day or 75 mg twice a day. max daily dose of 150 mg
Metabolize: Hepatic; minor substrate of multiple CYP pathways
Fentanyl Transdermal System
Generic Name: Duragesic, Ionsys
Drug Class: Opioid Analgesic; CII
Uses: to ease pain
Mechanism of Action: a phenylpiperidine opioid agonist with predominant effects on the mu opioid receptor and is about 50-100 times more potent as an analgesic than morphine
Normal Daily Doses: 1 patch (100mcg) every 3 days (72 hr)
Metabolize: Extensive hepatic metabolism, CYP3A4/5 substrate
Hydrocodone/APAP
Other names: Norco, Lorcet, Vicodin,
Drug Class: Opioid Analgesic, CII
Uses: Severe pain
Mechanism of Action: unknown, but it is thought to be related to the presence of opiate receptors in the CNS
Normal Daily Doses: 10-20mg every 12 hours
Metabolize: this is prodrug activated to hydromorphone by CYP2D6
Advil, Motrin
Generic Name: ibuprofen
Drug Class: NSAID
Uses: used to reduce fever and treat pain/inflammation, osteoarthritis, juvenile rheumatoid arthritis
Mechanism of Action: inhibits the both the COX-1 and COX-2 and reversibly alters platelet function and prolongs bleeding time
Normal Daily Doses: 200-400 mg every 4-6 hours as needed. Max daily dose of 3200mg/day (rx strength); 1200mg/day (OTC)
Metabolize: Hepatic, CYP2C19, phase I substrate
Indocin, Indocin SR, Tivorbex
Generic Name: indomethacin
Drug Class: NSAID
Uses: pain and inflammation; arthritis, gout, ankylosing spondylitis, osteoarthritis, rheumatoid arthritis
Mechanism of Action: inhibited by the COX-1
Normal Daily Doses: 20 mg three times day for 40 mg 2-3 times a day
Metabolize: 40% hepatic
Lidoderm
Generic Name: lidocaine
Drug Class: Local Anesthetic
Uses: Postherpetic neuralgia and localized pain
Mechanism of Action: stabilizing the neuronal membrane by inhibiting the ionic fluxes required
Normal Daily Doses: apply 1 patch topically for up to 12 hours in a 24 hour period
Metabolize: Not absorbed
Mobic
Generic Name: meloxicam
Drug Class: NSAID
Uses: reduces pain, tenderness, swelling, arthritis
Mechanism of Action: inhibits prostaglandin synthetase (COX-1 and COX-2)
Normal Daily Doses: 15 mg by mouth once a day/ 7.5 mg once a day
Metabolize: hepatic minor substrate of CYP3A4/5
Methadone, Dolophine, Methadose
Generic Name: methadone
Drug Class: Opioid Analgesic, CII
Uses: chronic pain, drug detoxification, opioid abuse
Mechanism of Action: binds to opiate receptors in CNS, causing inhibition ascending pain pathways
Normal Daily Doses: 2.5 mg po q8h-q12h (pain); 15-30 mg po q8h
Metabolize: Hepatic CYP2B6 and 3A4/5 substrate, moderate CYP2D6 inhibitor
Robaxin, Carbacot, Skelex
Generic Name: methocarbamol
Drug Class: Centrally Acting skeletal muscle relaxants, CNS depressant
Uses: musculoskeletal pain or spasm
Mechanism of Action: CNS depressant activity
Normal Daily Doses: 1500 mg po qid x 48-72 hr
Metabolize: hepatic via dealkylation and hydroxylation
MS Contin, Kadian, Avinza
Generic Name: morphine
Drug Class: Opioid Analgesic, CII
Uses: chronic and acute pain
Mechanism of Action: mu agonist
Normal Daily Doses: 10-20 mg po q12
Metabolize: Hepatic by glucuronidation
Aleve, Naprosyn
Generic Name: naproxen
Drug Class: NSAID
Uses: treats pain or inflammation caused by fever, arthritis, cramps, gout
Mechanism of Action: inhibits by blocking COX-1 and COX-2 enzymes
Normal Daily Doses: 250-550 mg bid
Metabolize: undergoes both Phase I and Phase II via the hepatic not CYP450
OxyContin
Generic Name: oxycodone
Drug Class: Opioid Analgesic, CII
Uses: chronic, moderate to severe pain
Mechanism of Action: bind to the mu opioid receptor of the CNS
Normal Daily Doses: 5-15 mg po q4-6 h prn
Metabolize: hepatic CYP3A4/5 substrate
Elmiron
Generic Name: pentosan
Drug Class: Urinary Analgesic
Uses: pain relief from interstitial nephritis
Mechanism of Action: relieving pain associated with interstitial cystitis is not known, but it has been found to adhere to the mucosal membrane of the bladder wall
Normal Daily Doses: 100 mg po tid
Metabolize: Metabolized in the liver and spleen via desulfation
Imitrex
Generic Name: sumatriptan
Drug Class: Antimigraine Serotonin Receptor Agonist
Uses: treats migraines, cluster headaches
Mechanism of Action: agonist of 5-HT subtypes 1B,1D, and 1F receptors
Normal Daily Doses: 25-100 mg po at onset of migraine, may repeat after 2 h prn; max 200mg/d
Metabolize: Hepatic via monoamine oxidase
Ultram
Generic Name: tramadol
Drug Class: Opioid Analgesic
Uses: pain, chronic, moderate to moderately severe, restless leg syndrome
Mechanism of Action: mu-opioid receptor agonist and serotonin and norepinephrine reuptake
Normal Daily Doses: 50 mg po q4-6 h prn, may titrate to 400 mg/d
Metabolize: hepatic via CYP3A4/5 and CYP2D6
