Pharmacological Treatment Options for _____Osteoporosis______

Kun Cai, PharmD Candidate 2007

Therapeutic Class/Agents / Therapeutic Class/Agents / Therapeutic Class/Agents / Therapeutic Class/Agents
Product Availability
Generic (Brand) / Glucocorticoid injections
Triamcinolone (Aristocort), methylprednisolone (Medrol) / Tramadol (ultram) / Hyaluronic Acid Derivatives
(biolon, euflexxa, healon, hyalgan) / Opioid
Codeine (3 Tylenol #3)
Hydrocodone (3 Vicodin/Lortab)
Morphine (MSIR, Roxanol, MS Contin)
Oxycodone (Percocet/Roxicodone)
Hydromorphone (Dilaudid)
Fentanyl (Duragesic)
Mechanism
of Action / Corticosteroids regulate gene expression subsequent to binding specific intracellular receptors and translocation into the nucleus. Corticosteroids exert a wide array of physiologic effects including modulation of carbohydrate, protein, and lipid metabolism and maintenance of fluid and electrolyte homeostasis. Decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability. / Binds to u-opiate receptors in the CNS causing inhibition of ascending pain pathways, altering the perception of and response to pain; also inhibits the reuptake of norepinephrine and serotonin, which also modifies the ascending pain pathway. / Hyaluronic acid is an important constituent of normal cartilage with viscoelastic properties providing lubrication with motion and shock absorbency during rapid movements. Endogenous HA also may have anti-inflammatory effects. / Opioid drugs block pain perception in the cerebral cortex by binding to specific receptor molecules within the neuronal membranes of synapses. This binding results in a decreased synaptic chemical transmission through the CNS thus inhibition the flow of pain sensations into the higher centers.
EFFICACY
(Indication/Use, Clinical Data Support) / Intra-articular glucocorticoid injections can provide excellent pain relief and anti-inflammation effect, particularly when a joint effusion is present. / Alternative to those who have contraindications to COX-2 inhibitors, nonselective NSAIDs, impaired renal function; Adjunct therapy to NSAIDs / Injections temporarily and modestly increase viscosity. HA injections were reported to decrease pain, many studies were short term and poorly controlled and placebo injections also reduced OA pain dramatically. / Opiods drugs are indicated for moderate and severe pain.
Alternative to those who have contraindications to COX-2 inhibitors, nonselective NSAIDs, impaired renal function; Adjunct therapy to NSAIDs
SAFETY
(Major Drug Interactions,
Pre-cautions, Contra-indications,
Adverse Effects,
Pregnancy Risk Category) / Adverse effects:
Cardiovascular: edema, hypertension, arrhythmia
CNS: insomnia, nervousness, seizure, headache, mood swings
Dermatologic: hirsutism, acne, skin atrophy
Endocrine: diabetes mellitus, adrenal suppression, hyperlipidemia, cushing’s syndrome, growth suppression, glucose intolerance, hypokalemia, sodium and water retentions
GI: indigestion, increased appetite, peptic ulcer, nausea, vomiting
Neuromuscular: arthralgia, muscle weakness, osteoporosis, fractures
Ocular: cataracts, glaucoma
Others: infection, hypersensitivity reaction
Contraindications: hypersensitivity. Virus infection, fungal, or tubercular skin lesions, administration of live virus vaccines, serious infections.
Drug interactions: methylprednisolone is minor substrate of CYP3A4, inhibits CYP2C8, 3A4
Pregnancy category: C / Adverse effects: cardiovascular: flushing;
CNS: dizziness, headache, insomnia, somnolence
Dermatologic: pruritus
GI: constipation, nausea
Neuromuscular: weakness
Contraindications: hypersensitivity, opioid-dependent patients, acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids or psychotropic drugs.
Drug interactions: minor substrate of CYP2B6, major substrate of 2D6, minor substrate of 3A4
Pregnancy category: C / Adverse effects:
Injection site reaction: pain, redness, swollen; allergy reaction: redness, rash
Contraindications:
Hypersensitivity to avian product.
Pregnancy category: C / Adverse effect:
Bradycardia, hypotension, dizziness, drowsiness,euphoria,lighteadednes, mood changes, physiological dependence, pruritus, rash, constipation, gastric distress, heartburn, nausea, vomiting, respiratory depression.
Contraindications:
Hypersensitivity, CNS depression, severe respiratory depression
Pregnancy category: C/D (prolonged use or high doses at term)
Therapeutic Class/Agents / Therapeutic Class/Agents / Therapeutic Class/Agents / Therapeutic Class/Agents
Dosage & Administration
(Include renal and/or hepatic adjustments) / Injection should not be used more than 3-4 x/year
Methylprednisolone:
Large joints: 20-80mg IA, small joints: 4-10 mg IA
Triamcinolone acetonide: Adults: Initial: Smaller joints: 2.5-5 mg IA, larger joints: 5-15 mg IA / 200-300 mg PO divided into 4 doses,
Dosage adjustment in renal impairment:
Immediate release: Clcr < 30 ml/ min: administer 50-100 mg dose every 12 hours
Extended release: should not be used in patients with CLcr< 30 ml/min
Dosage adjustment in hepatic impairment:
Immediate release: 50mg every 12 hours
Extended release: should not be used in patients with severe hepatic dysfunction / Osteoarthritis of the knee: Intra-articular:
Eulexxa™: Inject 20 mg (2 mL) once weekly for 3 weeks
Hyalgan®: Inject 20 mg (2 mL) once weekly for 5 weeks; some patients may benefit with a total of 3 injections
Orthovisc®: Inject 30 mg (2 mL) once weekly for 3-4 weeks
Supartz™: Inject 25 mg (2.5 mL) once weekly for 5 weeks
Synvisc®: Inject 16 mg (2 mL) once weekly for 3 weeks (total of 3 injections) / Titration individually to appropriate analgesic effect
Monitoring
(Efficacy and Toxicity Parameters) / Efficacy: pain, range of motion, grip strength, mobility, ADL function
Toxicity: blood pressure, blood glucose, electrolytes / Efficacy: pain, range of motion, grip strength, mobility, ADL function
Toxicity: pain relief, respiratory rate, blood pressure and pulse; signs of tolerance or abuse / Efficacy: pain, range of motion, grip strength, mobility, ADL function
Toxicity: pain, redness, swollen, rash in injection site / Efficacy: pain, range of motion, grip strength, mobility, ADL function
Toxicity: pain relief, respiratory rate, blood pressure and pulse; signs of tolerance or abuse
Patient Education / Avoid alcohol. Limit intake of caffeine or stimulants. If you have diabetes, monitor glucose levels closely. Report excessive nervousness or sleep disturbances, any signs of infection, vision changes, excessive or sudden weight gain (>3 lb/week); swelling of face or extremities; respiratory difficulty; muscle weakness, change in color of stools or persistent abdominal pain / Use exactly as directed. Drug may cause physical and psychological dependence. Do not use alcohol or other prescription or OTC medications (especially pain medications, sedatives, antihistamines or cough preparations) without consulting prescriber. Maintain adequate hydration (2-3L/day). You may experience drowsiness, dizziness, or blurred vision, nausea, vomiting or loss of appetite or constipation. Report severe unresolved constipation, respiratory difficulty or shortness of breath, excessive sedation or increased insomnia and restlessness, seizures or chest pain or palpitations. / Report to your health care provider any adverse effects such as redness, swollen and pain in the injection site, any hypersensitivity reaction such as rash, itching in the injection site, edema and difficulty breathing. / If self-administered, use exactly as directed; do not increase dose or frequency. Drug may cause physical and/or psychological dependence. Take with food or milk. While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. May cause dizziness, lightheadedness, confusion, or drowsiness (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known); or nausea or vomiting (frequent mouth care, frequent sips of fluids, chewing gum, or sucking lozenges may help). Report chest pain or palpitations; persistent dizziness, shortness of breath, or respiratory difficulty; unusual bleeding or bruising; or unusual fatigue and weakness.
Cost
(1-month) / Triamcinolone
4 mg (30): $50.99
Methylprednisolone
4 mg (25): $33.86 / 50 mg (30): $33.81 / Injection (Synvisc)
8 mg/mL (2): $220.88
8 mg/mL (6): $638.98 / Tablets (Lortab 2.5)
2.5-500 mg (30): $28.55
Tablets (Lortab 5)
5-500 mg (30): $30.86
References
(Guidelines, Drug Info Sources) / American College of Rheumatology: Recommendations for the Medical Management of Osteoarthritis of the Hip and Knee
Lexi-comp / American College of Rheumatology: Recommendations for the Medical Management of Osteoarthritis of the Hip and Knee
Lexi-comp / American College of Rheumatology: Recommendations for the Medical Management of Osteoarthritis of the Hip and Knee
Lexi-comp / American College of Rheumatology: Recommendations for the Medical Management of Osteoarthritis of the Hip and Knee
Lexi-comp

Kun Cai, PharmD Candidate 2007 Pharmacotherapy Presentation – Pharmaceutical Care Rotation

University of Maryland School of Pharmacy Happy Harry’s Pharmacy Patient Care Center, Perryville, MD