Pharmacology of musculoskeletal system
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Important for nerve impulses, provides stability and movement, prevention of muscle spasms-proper metabolism works with vitamin D, PTH, calcitonin
Necessary for Calcium absorption, Vita D gets converted into Cholecalciferol from the sun, dairy products, etc.
- is a symptom not a disease
- inadequate sun exposure
- poor nutrition-Inadequate calcium intake
- Digestive malabsorption issues
- Cell membranes become hyperexcitable
- Side effects
- Prolongation of QT interval on EKG
- Increases risk of arrhythmias
- Nerve impulse excitability
- convulsions, confusion, abnormal behavior
Calcium carbonate/ citrate
Pharm Class: Hypocalcemia agent
- Therapeutic class: Calcium supplement.
- MOA: correct hypocalcemia-two most common salts for routine supplementation. Pharmacokinetics very depending on the route of administration.
- Preg Cat: B
- Indications: Hypocalcemia, osteoporosis, paget's disease, osteomalacia, chronic hypoparathyroidism, rickets, pregnancy, lactation and rapid childhood growth.
- Contraindications: Hypercalcemia, ventricular fibrillation, metastatic bone cancer, renal calculi.
- ALERT: When given through IV give slowly to avoid dysrhythmias and cardiac arrest.
- Adverse effects: potential for dysrhythmias with any imbalance of calcium in blood. IV administration of Calcium can lead to a fast increase and higher risk of side effects.
- Interactions: may increase dysrhythmias when administered with digoxin, may antagonize the effects of calcium channel blockers. Can decrease serum phosphate and potassium levels and magnesium levels.
- fat soluble, over dose resulting in hypercalcemia
- 400 units normal dose
calcitriol (Calcijex, Rocaltrol)
Pharm Class: Bone resorption inhibitor
- Therapeutic class: Vitamin D
- MOA: active form of vitamin D, promotes intestinal absorption of calcium, elevates serum levels of calcium. Usually prescribed with a calcium supplement.
- Preg. Cat: C
- Indications: impaired kidney function or hypoparathyroidism, treatment of rickets.
- Contraindications: Hypercalcemia, VItamin D Toxicity.
- Adverse effects: Can cause hypercalcemia and lead to S&S of Hypercalcemia.
- Interactions: Thiazide diuretics may enhance the effects of vitamin D causing hypercalcemia and leading to dysrhythmias.
*alendronate sodium (Fosamax)
Pharm Class: Bisphosphonate; bone resorption inhibitor.
- Therapeutic Class: Drug for osteoporosis
- MOA: Lowers serum alkaline phosphatase; enzyme associated with bone turnover. May take up to 1-3 months to reach therapeutic effect.
- Preg Cat. C
- Indications: Osteoporosis and Paget's disease.
- Alert: Should be taken on empty stomach for max absorption, patient should remain in upright position for at least 30 mins after administration.
- Contraindication: osteomalacia, esophagus abnormalities, caution: for renal impairment, heart failure, Hyperphosphatemia, liver disease, infections, GI problems, and pregnancy.
- Adverse effects: GI upset, esophageal irritation, osteonecrosis of the jaw (ONJ), hypocalcemia, hypophosphatemia, dyspepsia, arthralgia, myalgia, headache- Pathologic fractures may occur if the drug is taken longer than 3 months.
- Interactions: Calcium, iron, antacids can interfere with absorption.
Class:*Selective estrogen receptor modulators (SERM)
- Therapeutic class: Drug for osteoporosis prevention.
- MOA: decreases bone resorption and increases bone mass/density by acting through estrogen receptors. Can also lower TCL/LDL without lowering HDL.
- Preg. Cat: X
- Indications: Prevention of Osteoporosis-Give with food.
- Contraindications: Lactating patients, prego, history of DVT, hypersensitivity to drug.
- Alerts: Can increase risk of Venous thromboembolism.
- Adverse effects: hot flashes, Peri-menopausal symptoms.
- Interactions: Concurrent use with warfarin may decrease prothrombin time. Patients should not take this medication with cholesterol lowering drugs or ERT-Estrogen Hormone Therapy.
Calcitonin-will effect the body in the same way as natural Calcitonin.
- MOA: increases bone density- reduces risks of pathologic fractures. pulls calcium from the blood and into the bone.
- Indications: osteoporosis, Hypercalcemia
Hormone Replacement Therapy (HRT)
Slow release sodium flouride
hydroxychloroquine sulfate (Plaquenil)
Class:*DMRAD-Disease modifying rheumatoid arthritis drugs
- Therapeutic class: antirheumatic drug; antimalarial.
- MOA: relieves severe inflammation of arthritis and lupus, exact mechanism of action not known.
- Preg. Cat: C
- Indications: rheumatoid arthritis and lupus erythematous patient who have not responded well to other anti-inflammatory drugs, as well as malaria prevention
- Contraindications: Hypersensitivity, retinal or visual field changes associated with med use.
- Adverse effects: can be Hepatotoxic, GI upset, anorexia, alopecia, headache, *blood dyscrasia.
- Interactions: antacids may prevent absorption, liver toxicity increases if patient drinks alcohol.
Biologics Tumor necrosis factor (TNF) blockers
Humira, Enbrel examples
- MOA: Genetically engineered proteins derived from human genes, designed to either inhibit specific components of the immune system or suppressing inflammation
- Adverse effects: Rare but serious – reactivation of TB, infections, neurological disorders such as MS, lymphoma, lupus like syndromes. Fewer side effects then DMRADS -GI upset, anorexia, alopecia, headache, ocular effects, blood dyscrasias
Corticoids and Glucocorticoids
Used to treat a wide variety of inflammatory disorders. Can be injected which is more effective. Many adverse effects-hyperglycemia, muscle weakness, bone thinning,gastric ulcers.
Pharm class: Xathine Oxidase Inhibitor
- Therapeutic class: Drug for Gout-Anti-hyperuricemia
- MOA: Take 1-3 weeks to take effect
- Indications: Inhibit the formation of uric acid preventing gout. prophylactically taken to reduce the severity of hyperuricemia associated with antineoplastics and radiation.
- Contraindications: hypersensitivity to drug, idiopathic hemochromatosis-, caution in patients with impaired hepatic or renal function, bone marrow depression and pregnancy.
- Adverse effects: rash, bone marrow depression, hepatotoxicity, renal failure
- Interactions: ototoxic when taken with thiazides, ACE inhibitors, antacids may inhibit absorption. potentiates anticoagulants.
- TAKE WITH WATER
Non-pharmacological remedies for muscle spasms
- Herbal remedies
- Kava – antianxiety
- Black cohosh – topically
- Castor oil – topically
- Capsaicin - topically
- Application of heat/cold
- Therapeutic ultrasound
- Assisted exercise
Cyclobenzaprine (Amrix, Flexeril)
- Therapeutic Class: Skeletal Muscle Relaxant
- Pharmaologic class: Centrally acting norepinephrine-releasing agent.
- MOA: Thought to work on CNS (centrally) increases norepinephrine activity by inhibiting reuptake to produce anticholinergic effect.
- Indications: Short term therapy for acute musculoskeletal conditions-unrelated to CNS, Fibromyalgia
- Contraindications: Hypersensitivity to Tricylic antidepressents (TCA), QT-interval prolongation- don't give to pt. recovering from MI.
- Idiopathic disease of the bone, theories suggest it is due to genetic factors or a viral infection early in life-possibly autoimmune?
- *affected bone may be in only one or two areas of the skeleton or widespread. The bone/s abnormally break down and reform.
Demineralization that breaks down bone into it's mineral components- Calcium becomes available for other areas in the body.
Bone building, accomplished by Osteoblasts-removes calcium from the blood to be placed in bone-Stimulated by hormone calcitonin
- Sodium permeability decreases across cell membranes.
- Causes: Hyperparathyroidism, Calcium supplements, Vitamin D supplements (calcitriol)
- Side effects:
- Shortening of QT interval on EKG
- Muscle twitches/weakness
- headache, dry mouth, thirst, increased urination and nausea vomiting.
Cholecalciferol- Conversion and reason
Inactive form of vitamin D
-synthesized from skin from cholesterol. Skin-Sunlight-ultraviolet light=increases levels of cholecalciferol in blood. Also obtained in Diet( Fish oil/ fatty fish, Egg yolk)
- Gets converted into Calcifediol where enzymes in the kidneys metabolize it into Calcitriol an active form of vitamin D.
- PTH: responsible for this conversion to increase the absorption of calcium through the GI tract.
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