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Chapter 13

Chapter 13. Drugs for Muscles and Joint Disease and Pain. Muscles and Joints. Bones of the skeletal system provide framework of the body Are connected at joints Joint: place of union or junction between 2 or more bones Skeletal muscles: provide movement at joints, contractile tissues.

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Chapter 13

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  1. Chapter 13 Drugs for Muscles and Joint Disease and Pain

  2. Muscles and Joints • Bones of the skeletal system provide framework of the body • Are connected at joints • Joint: place of union or junction between 2 or more bones • Skeletal muscles: provide movement at joints, contractile tissues

  3. Anatomy of a Joint

  4. Bones, Muscles, and Tendon for Movement at Elbow Joint

  5. Three Types of Muscle

  6. Muscle Relaxants • Skeletal muscle contractions voluntarily • Neurotransmitter acetylcholine (Ach) • binds with receptors on muscle cell membrane • calcium is released, causing a contraction • Relaxation occurs when ACh is broken down by acetylcholinesterase

  7. Muscle Relaxants Medications • Acts on motor neurons or at neuromuscular junction • Block normal muscle function by • Blocking release of ACh • Preventing destruction of Ach • Preventing ACh from reaching receptors

  8. Dispensing Issues ofMuscle Relaxants • To avoid drug interactions, drug history needed before administering • Technician often obtains drug history • Sedative properties cause patient to relax, reducing reflex impulse conduction

  9. Side Effects of Muscle Relaxants • Sedation • Reduced mental alertness • Reduced motor abilities • GI upset • Avoid alcohol when taking these drugs

  10. carisoprodol (Soma) • Skeletal muscle relaxant subject to abuse • Scheduled substance in many states • Causes drowsiness and dizziness • Toxicity risk increases with alcohol or other CNS depressants

  11. cyclobenzapine (Flexeril) • Centrally acting skeletal muscle relaxant related to TCAs • Treats muscle spasms associated with acute musculoskeletal conditions • Onset of action is within 1 hour • Not to be used more than 2 to 3 weeks

  12. Discussion Most muscle relaxants are not controlled substances, so why are they highly abused? They are abused due to the relaxing feeling that patients have from taking them.

  13. Inflammation and Swelling • Analgesics used to relieve pain • Nonnarcotic analgesic used for mild-to-moderate pain, inflammation, and fever • Two types of pain • Somatic: dull, throbbing pain from skin, muscle, or bone • Visceral: sharp, stabbing pain from organs

  14. Inflammation • Pain pathway in tissue injury • PGs can cause inflammation, tissue damage, and fever • Nonnarcotic analgesics interrupt pathway, inhibiting enzyme to synthesize PGs • Relieves inflammation and pain • Reduces fever

  15. Pain Pathway in Tissue Injury

  16. NSAIDs • Properties of nonsteroidal anti-inflammatory drugs (NSAIDs) • Analgesic (pain relieving) • Anti-inflammatory • Antipyretic (fever reducing) • Prototype NSAID is aspirin

  17. Therapeutic Uses of NSAIDs • Inflammation and pain of arthritis and rheumatism • Headache • Menstrual cramps • Backache • Muscle aches • Flu • Fever • Gouty arthritis

  18. Mechanism of Action of NSAIDs • Inhibit PG synthesis in inflamed tissues • Prevents sensitization of pain receptors • Generally act peripherally, not centrally like other pain killers

  19. The GI System and NSAIDs • Primary side effect is GI upset • One in five chronic NSAID users develop some type of GI gastropathy • Many patients need to take a proton pump inhibitor with NSAIDs

  20. Side Effects of NSAIDs • Nausea • Abdominal cramps • Heartburn • Ulcers • Indigestion • Kidney damage • Acute renal failure • Fluid retention • Hypertension • Hyperkalemia • Liver abnormalities • Bone marrow depression • Tinnitus and others

  21. Interactions with NSAIDs • Other NSAIDs including aspirin • Beta blockers • Cyclosporine • Digoxin • Diuretics • Methotrexate • Oral hypoglycemics • Warfarin

  22. Tips for NSAID Users • Take with food • Use antacids or proton pump inhibitor • Do not use gastric irritants (ETOH) • Stop NSAID before any surgical procedure • Use the lowest possible dose • Be aware of side effects • Take sufficient fluids • If sensitive to aspirin, avoid NSAIDs

  23. Precautions of NSAIDs • Concurrent use with multiple NSAIDs, including aspirin, should be discouraged • Could lead to additive or synergistic toxicity • Use of NSAIDs and opiates may be synergistic • Considerable patient-to-patient variability to different NSAIDs

  24. ibuprofen (Advil, Motrin) • Controls fever well • Can be alternated with aspirin • OTC: 200 mg tablet, caplet, or capsule (solids) • Rx: 400 mg, 600 mg, and 800 mg solids (tablets)

  25. naproxen (Naprosyn) • Least risky NSAID for cardiovascular events • Used in lowest effective dose for least amount of time

  26. COX-2 Inhibitors • 2 enzymes critical in inflammation process • Cyclooxygenase-1 (COX-1): extensive role in body, including protecting GI lining • Cyclooxygenase-2 (COX-2): pain, inflammation • Drugs only block the COX-2 enzyme which is induced during inflammation

  27. Therapeutic Uses of COX-2 Inhibitors • Rheumatoid arthritis • Osteoarthritis • Menstrual cramps • Acute pain

  28. celecoxib (Celebrex) • First COX-2 inhibitor to be approved • GI upset is primary side effect • Only COX-2 inhibitor on the market • All others recalled by FDA

  29. Dispensing Issues of celecoxib (Celebrex) • Technician—attach the label “Take with Food” • Beware of cross-sensitivity with sulfonamides • May increase cardiovascular risk • Look-alike and sound-alike • Celebrex • Cerebyx (anticonvulsant)

  30. allopurinol (Zyloprim) • Used to prevent gout attacks • Liver function should be monitored • Used with caution with diuretics

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