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Focus on PHARMACOLOGY ESSENTIALS FOR HEALTH PROFESSIONALS CHAPTER 29 Drugs Used to Treat Musculoskeletal Conditions Figure 29-1 The skeletal system and its functions. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Calcium • Most abundant mineral in body • Proper balance and interaction with other minerals and hormones is essential to optimal function of several body system. • Typical body has 1–2 kg of calcium, 99% of which is in bones. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Osteoporosis • Bones become thinner and weaker during aging: osteopenia • Osteoporosis: bone mass is reduced enough to cause abnormal functioning • Increased incidence of fracture • Occurs more often in women than men, often in postmenopausal women because of reduced estrogen levels Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Table 29-1 Drugs Used to Treat Osteoporosis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Bisphosphonates: Uses • Highly selective inhibitor of bone demineralization and resorption; appears to increase bone density • Used to treat osteoporosis; some for Paget’s disease; some for hypercalcemia of malignancy; some for postmenopausal osteoarthritis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Bisphosphonates: Adverse Effects • Bisphosphonates commonly cause various GI upsets, including: – Flatulence – Acid regurgitation – Dysphagia – Gastritis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Bisphosphonates: Adverse Effects (conditions) • Other adverse effects include: – Headache – Musculoskeletal pain – Rash Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Bisphosphonates: Contraindications • Contraindicated in severe renal impairment, hypocalcemia, lactation, pregnancy • Used cautiously in patients with congestive heart failure, hypophosphatemia, liver disease, fever or infection, peptic ulcer Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Bisphosphonates: Patient Information • Review the correct administration with patients. • Advise patients to report fever accompanied by arthralgia and myalgia. • Instruct patients to take 30 minutes before food, beverages, or other medications. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Calcitonin: Uses • Derived from salmon, lowers serum calcium and phosphate levels by action on bones and kidneys; inhibits bone resorption, thereby increasing bone density • Used to treat osteoporosis in postmenopausal women, hypercalcemia, and symptomatic Paget’s disease Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Calcitonin: Adverse Effects • Headache • Eye pain • Anaphylaxis (reported for human calcitonin only) • Urinary frequency • Chills Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Calcitonin: Adverse Effects • • • • Chest pressure Weakness Nasal congestion Shortness of breath Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Calcitonin: Contraindications • Avoid in patients with history of allergy (especially to fish) • Safe use in children, pregnancy, and lactation not established • Cautious use in patients with renal impairment or pernicious anemia Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Calcitonin: Patient Information • Advise patients to report redness, warmth, or swelling at injection site. • Instruct patients to check with physician before taking OTC preparations such as supervitamins and antacids. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini DMSO • Dimethyl sulfoxide, known as DMSO, is a topical agent that can help reduce pain and inflammation in various musculoskeletal disorders. Only use under a physician’s guidance. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Raloxifene (Evista): Uses • A selective estrogen-receptor modulator (SERM); acts by combining with estrogen receptors to decrease bone resorption and increase bone mass and density • Used to prevent and treat osteoporosis and to reduce risk of breast cancer in postmenopausal women Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Raloxifene: Adverse Effects • • • • • Hot flashes Migraines and other types of headache Flu-like symptoms Vaginal bleeding Uterine and urinary tract disorders Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Raloxifene: Adverse Effects • • • • Breast pain Depression Insomnia Dizziness Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Raloxifene: Contraindications • Contraindicated in women who may become pregnant and in those with venous thromboembolic disease • Not to be used with systemic estrogen replacement therapy • Should be used cautiously with diazepam, lidocaine, and diazoxide Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Raloxifene: Patient Information • Advise patients to report unexplained calf pain or tenderness. • Instruct patients to avoid prolonged restriction of movement during travel. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Rheumatoid Arthritis (RA) • Systemic autoimmune disease that involves inflammation of joint-lining membranes; also affects internal organs • Occurs 2–3 times more often in women (onset usually at ages 40–60) • Joints affected include hands, feet, wrists, spine, shoulders, ankles, and hips Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Table 29-2 Disease-Modifying Drugs for Rheumatoid Arthritis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Table 29-2 (continued) Disease-Modifying Drugs for Rheumatoid Arthritis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Gold Compounds: Uses • Mechanism of action not clearly understood • Used to treat active RA Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Gold Compounds: Adverse Effects • Common: syncope, bradycardia, thickening of tongue, metallic taste in mouth • Serious: thrombocytopenia, leukopenia, aplastic anemia Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Gold Compounds: Contraindications • Uncontrolled diabetes • Renal or hepatic insufficiency • Hepatitis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Gold Compounds: Patient Information • Instruct patients to report adverse effects. • Advise patient to report unusual color or odor of urine, and to avoid contact with anyone who has a cold, has had a recent vaccination, or has been exposed to a communicable disease. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Hydroxychloroquine (Plaquenil): Uses • Mechanism of action unclear • Used to treat RA and systemic lupus erythematosus Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Hydroxychloroquine: Adverse Effects • Common: fatigue, headache, mood or mental changes, anxiety, difficulty focusing or blurred vision, anorexia, nausea and vomiting, abdominal cramps • Serious: retinopathy Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Hydroxychloroquine: Contraindications • Safety in pregnancy and lactation not established. • Cautious use in patients with hepatic disease, alcoholism, impaired renal function Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Hydroxychloroquine: Patient Information • Advise patients to follow drug regimen exactly as prescribed and to keep drug out of reach of children. • Instruct patients to get regular eye exams. • Instruct patients to avoid breast feeding. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Hydroxychloroquine • Acute or chronic diseases that affect liver architecture or function also affect hepatic metabolism of some drugs. • Elderly patients may therefore have markedly affected drug elimination and need dosage adjustment. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Methotrexate (Folex, Mexate): Uses • Folic-acid blocker and immunosuppressant that affects lymphocyte and macrophage function • Used to treat severe psoriasis, psoriatic arthritis, and RA; also to maintain remission in neoplastic disease Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Methotrexate: Adverse Effects • Common: GI upset and mouth sores, amenorrhea • Serious: bone-marrow suppression, infertility Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Methotrexate: Contraindications • Contraindicated in: pregnancy and lactation, men and women of childbearing age, hepatic and renal insufficiency, preexisting blood dyscrasias • Cautious use in patients with infections, peptic ulcer, colitis, poor nutritional status Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Methotrexate: Patient Information • Advise patients of the dangers of this drug and explain symptoms to immediately report. • Warn patients to avoid alcohol. • Tell patients to avoid sunlight and UV light and to wear sunglasses. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Methotrexate • Prolonged use of small doses can lead to hepatotoxicity. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Sulfasalazine (Azulfidine): Uses • Locally acting sulfonamide that may exert an anti-inflammatory effect • Used to treat RA, juvenile chronic arthritis, and ankylosing spondylitis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Sulfasalazine: Adverse Effects • Common: nausea, vomiting, headache, rash • Serious: anemia, oligospermia, blood dyscrasias, liver injury, allergic reactions Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Sulfasalazine: Contraindications • Contraindicated in patients with agranulocytosis, intestinal and urinary tract obstruction, or porphyria; pregnancy and lactation • Cautious use in severe allergy or bronchial asthma, hepatic or renal impairment, or in children younger than 6 years Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Sulfasalazine: Patient Information • Instruct patients that urine and skin may turn orange-yellow. • Women should not breast feed. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Gout and Gouty Arthritis • Characterized by crystal deposits in and around joint spaces, leading to acute inflammation of joint • Gout commonly affects men after age 50. • Three manifestations: hyperuricemia, acute gouty arthritis, chronic gouty arthritis Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Table 29-3 Anti-Gout Medications Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Colchicine: Uses • Uses: anti-inflammatory agent used to treat gout; inhibits formation of white blood cells • Adverse effects: Common: GI disturbances decreased absorption of vitamin B12 • Contraindications: severe cardiac, renal, hepatic, blood, and GI diseases Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Colchicine: Uses • Patient education: Advise patients to report severe GI symptoms or signs of bone-marrow depression. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Colchicine in Elderly Patients • Colchicine must be used cautiously in elderly patients because of its possible adverse GI, cardiac, renal, and hepatic effects. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Allopurinol (Aloprim): Uses • Improves solubility of uric acid; used to control chronic, not acute, gout Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Allopurinol: Adverse Effects • Common: drowsiness, headache, dizziness, nausea and vomiting, abdominal pain • Serious: hepatotoxicity, renal insufficiency Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Allopurinol: Contraindications • Contraindicated children (except in those with hyperuricemia secondary to cancer and chemotherapy) • Safety in pregnancy and lactation not established. • Cautious use in patients with impaired hepatic or renal function, history of peptic ulcer, lower GI tract disease, and bone-marrow suppression Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Allopurinol: Patient Information • Advise patients to drink 3 quarts of fluid per day. • Instruct patients to report diminishing urine output, cloudy urine, unusual color or odor to urine, pain or discomfort during urination, itching and rash. • Patients should avoid driving and sun exposure. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Uricosuric Agents: Uses • Competitively inhibit renal tubular reabsorption of uric acid to promote its excretion • Used to treat severe attacks of gout Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Uricosuric Agents: Adverse Effects • GI irritation • Allergic dermatitis • Nephrotic syndrome Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Uricosuric Agents: Contraindications • Contraindicated in patients with blood dyscrasias and uric-acid kidney stone • Safety in pregnancy, lactation, or in children younger than 2 years not established. • Cautious use in patients with peptic ulcer Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Uricosuric Acid: Patient Information • Advise patients to drink 3 quarts of fluid per day. • Physicians may advise patients to restrict intake of high-purine foods (organ meats, meat soups, and gravy). Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Uricosuric Acid: Patient Information • Instruct patients to not stop treatment, or not to take aspirin or OTC medications without consulting physician. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Muscle Spasms and Pain • Often associated with traumatic injuries and spasticity from disorders such as cerebral palsy, stroke, or head and spinal cord injuries • Two types of muscle spasms: tonic and clonic Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Table 29-4 Centrally Acting Muscle Relaxants Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Table 29-4 (continued) Centrally Acting Muscle Relaxants Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Centrally Acting Skeletal Muscle Relaxants • Uses: treat local spasms to reduce pain and increase range of motion • Adverse effects: sedation, weakness, fatigue • Contraindications: some contraindicated in liver disease, porphyria, children, pregnancy, lactation Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini Centrally Acting Skeletal Muscle Relaxants • Patient information: avoid alcohol, other CNS depressants. Patients with diabetes must closely monitor glucose levels. Focus on Pharmacology: Essentials for Health Professionals, Second Edition Jahangir Moini