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Focus on

PHARMACOLOGYESSENTIALS FOR HEALTH PROFESSIONALS

CHAPTER

Drugs Used to Treat Musculoskeletal Conditions

29

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Multimedia Directory

Slide 6 Osteoporosis Video

Slide 25 Arthritis Video

Slide 38 Mechanism of Action of Methotrexate Animation

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Figure 29-1 The skeletal system and its functions.

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Osteoporosis Video

Click here to view a video on the topic of osteoporosis.

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Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Table 29-1 Drugs Used to Treat Osteoporosis

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir Moini

Bisphosphonates: Adverse Effects

• Bisphosphonates commonly cause various GI upsets, including:

– Flatulence

– Acid regurgitation

– Dysphagia

– Gastritis

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Bisphosphonates: Adverse Effects (conditions)

• Other adverse effects include:

– Headache

– Musculoskeletal pain

– Rash

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Calcitonin: Adverse Effects

• Headache

• Eye pain

• Anaphylaxis (reported for human calcitonin only)

• Urinary frequency

• Chills

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Calcitonin: Adverse Effects

• Chest pressure

• Weakness

• Nasal congestion

• Shortness of breath

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Raloxifene: Adverse Effects

• Breast pain

• Depression

• Insomnia

• Dizziness

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Arthritis Video

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Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Table 29-2 Disease-Modifying Drugs for Rheumatoid Arthritis

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Table 29-2 (continued) Disease-Modifying Drugs for Rheumatoid Arthritis

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Gold Compounds: Uses

• Mechanism of action not clearly understood

• Used to treat active RA

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir Moini

Gold Compounds: Contraindications

• Uncontrolled diabetes

• Renal or hepatic insufficiency

• Hepatitis

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir Moini

Hydroxychloroquine (Plaquenil): Uses

• Mechanism of action unclear

• Used to treat RA and systemic lupus erythematosus

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Mechanism of Action of Methotrexate Animation

Click here to view an animation showing the mechanism of action of methotrexate.

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Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Methotrexate: Adverse Effects

• Common: GI upset and mouth sores, amenorrhea

• Serious: bone-marrow suppression, infertility

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Methotrexate

• Prolonged use of small doses can lead to hepatotoxicity.

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Table 29-3 Anti-Gout Medications

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Allopurinol (Aloprim): Uses

• Improves solubility of uric acid; used to control chronic, not acute, gout

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Uricosuric Agents: Adverse Effects

• GI irritation

• Allergic dermatitis

• Nephrotic syndrome

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir 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 EditionJahangir Moini

Table 29-4 Centrally Acting Muscle Relaxants

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir Moini

Table 29-4 (continued) Centrally Acting Muscle Relaxants

Focus on Pharmacology: Essentials for Health Professionals, Second EditionJahangir 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 EditionJahangir Moini

Centrally Acting Skeletal Muscle Relaxants

• Patient information: avoid alcohol, other CNS depressants. Patients with diabetes must closely monitor glucose levels.