Pharmacology Review Flashcards
Differently Classes of NSAIDs
Salicylate (acetylated) Salicylate (non-acetylated) Popionic acids (phenyl-propionic acid) Acetic acids Oxicams Fenamates Nonacidic Selective COX-2 inhibitors
When is NSAID therapy considered a failure?
2 weeks at max anti-inflammatory dose
MOA of NSAIDs
Inhibit cyclooxyrgenase which impairs the transformation of arachidonic acid to prostaglandins to prostacyclin and thromboxanes
What do COX-1 enzymes regualte?
Normal cellular processes such as gastric cytoprotection, vascular homeostasis, platelet aggregation, kidney function
SE of NSAIDs
GI Renal CV Liver Pulmonary Hematologic Malignancy Dermatologic Healing of musculoskeletal injuries
Renal SE of NSAIDs
Renal vasoconstriction Acute renal failure Hypertension Hyperkalemia Hyponatremia Edema Increased risk of renal cell cancer
Hepatic SE of NSAIDs
Elevation of liver transaminases
NSAID associated liver injury
More common in SLE and RA
Pulmonary SE of NSAIDs
SE more related to nonselective COX 1/2 inhibitors (less with COX2 selective)
Bronchospasm
Pulmonary infiltrates with eosinophilia
Hematologic SE of NSAIDs
Neutropenia
Anti platelet effects due to COX-1 inhibition
Anti-platelet Activity with NSAIDs
Need to continue ASA for cardioprotection
Interaction with warfarin (increase INR)
Higher risk of bleeding with anticoagulant use
CNS SE with NSAIDs
Aseptic meningitis
Tinnitus (usually salicylates)
Psychosis and cognitive impairment (indomethacin, elderly)
Dermatologic SE with NSAIDs
Drug rash
Pseudoporphyria
Blistering skin lesions (TENS, SJS)
Fracture Healing Effects with NSAIDs
Non-union
Avoid NSAIDs up to 90 days post fracture
Contraindications for NSAIDs
N: nursing or pregnancy S: serious bleeding A: allergy, asthma, angioedema I: impaired renal function D: drug (anticoagulants)
Acetylated Salicylate Medication
Aspirin
How is the acetylated salicylate class different from the other classes?
Irreversible platelet inhibition for the life of the platelet
Medications in the Propionic Acids Class
Naproxen
Ibuprofen
Naproxen
Less CV risk
Naproxen base or naproxen sodium
Ibuprofen
Advil or Motrin
Short duration of effect
Alternative to naproxen
Medications in the Acetic Acids Class
IV Ketorolac (Toradol) Indomethacin (Indocin)
Ketorolac (Toradol)
Adjust dose based on age and weight
Moderate to severe post-op pain
Risk of gastropathy >5 days
Not for chronic pain or inflammation
Indomethacin (Indocin)
Immediate release and extended release formulations
Treats acute gout and pericarditis
Not for chronic use
May be associated with aplastic anemia
Medications in the Oxicams Class
Meloxicam (Mobic)
Prioxicam (Feldene)
Meloxicam (Mobic)
Long duration
Slow onset
Low doses: COX-2 selective
Piroxicam (Feldene)
Treatment of chronic pain and inflammation poorly responsive to other NSAIDs
>20 mg QD = serious GI complications
Selective COX-2 Inhibitor Medication
Celecoxib (Celebrex)
Celecoxib (Celebrex)
No effect on platelets
Decreased GI toxicity
Dose related renal and CV effects (higher = more problems)
Pain Management with Fractures
Acetaminophen (APAP) or NSAID
Sometimes narcotic analgesic
Indications for Narcotics in Fractures
Significant soft tissue swelling or ecchymosis Pain at rest Night pain Pain uncontrolled by NSAIDs or APAP Anyone who had surgery May just need at night
Narcotics for Pain Relief
Codeine
Hydrocodone
Oxycodone
Codeine
Weak opioid
Mild to moderate pain
Schedule II/III
Metabolized to morphine
Medications with Hydrocodone
Lorcet
Lortab
Norco
Vicodin
Hydrocodone
Schedule III Moderate to severe pain Onset: 10-20 min Duration: 4-8 hours Combination with acetaminophen
Medications with Oxycodone
Percocet
Roxicet
Endocet
Oxycodone
Schedule II Moderate to moderately severe pain Onset: 10-30 minutes Combination with acetaminophen Avoid long acting for acute pain
Long Acting Oxycodone Medication
MS Contin
MOA of Noloxone (Narcan)
Reverses respiratory depression, sedation, and analgesia
Never use Extended Release and Long Acting Opioid Analgesics in what Situations
Acute pain
Narcotic naive patient
Toxicities of Opioids in General
Sedation and respiratory depression Constipation (need a bowel regimen) Decreased effectiveness of diuretics QT prolongation Check for cytochrome P450 inhibitors or inducers
Cytochrome P450 Inhibitors
Bupropion Fluoxetine Paroxetine Cimetidine Acyclovir Duloxetine Fluoroquinolones Ketoconazole PPIs Verapamil Diltiazem Grapefruit juice
Cytochrome P450 Inducers
Carbamazepine Isoniazid Tobacco Rifampin St. John's wort
Extended Release and Long Acting Opioids
Morphine sulfate ER: MS Contin, Kadian, Embeda, Avinza Buprenorphine transdermal: butrans Methadone: dolophine Fentanyl transdermal: duragesic Hydromorphone: exalgo
Rules for Transdermal Administration
Never cut or tear a patch
Heat exposure can increase release and absorption
Application of Transdermal Administration
Chest, side of waist, upper arm
Avoid hairy areas
Rotate sites
Wash site with water only
MOA of Tramadol
Mu receptors
Inhibits NE and serotonin
Tramadol
Effective for relief of neuropathic pain
Improved functional outcomes for fibromyalgia
May not be more effective than NSAIDs or nortriptyline for chronic pain
Metabolism of Tramadol
Hepatic
Use Caution with Tramadol in what Populations
Elderly
Renal insufficiency
Skeletal Muscle Relaxants
Cyclobenzaprine (Flexeril)
Tizanadine (Zanaflex)
Metaxalone (Skelaxin)
Diazepam (Valium)
Duration of Use of Muscle Relaxants
1-2 weeks
SE of Muscle Relaxants
Sedation
Anticholinergic
Muscle Relaxants with High Potential for Abuse
Diazepam (Valium)
Carisoprodol (Soma)
Muscle Relaxants + NSAIDs
Synergistic effect for treatment of acute back pain
