Therapeutic: anti–multiple sclerosis agents
Pharmacologic: receptor modulators
Treatment of relapsing forms of multiple sclerosis.
Converted by sphingosine kinase to the active metabolite fingolimod-phosphate, which binds to sphingosin-1 phosphate receptors, resulting in ↓ migration of lymphocytes into peripheral blood. This may ↓ lymphocyte migration into the CNS. Therapeutic Effects: ↓ frequency of relapses/delayed accumulation of disability.
Adverse Reactions/Side Effects
CNS: headache. EENT: blurred vision, eye pain, macular edema. Resp: cough, ↓ pulmonary function. CV: BRADYCARDIA, HEART BLOCK. GI: diarrhea, ↑ hepatic transaminases. Hemat: leukopenia, lymphopenia. MS: back pain. Misc: ↑ risk of infection.
PHYSICAL THERAPY IMPLICATIONS
Assess heart rate, ECG, and heart sounds, especially during exercise (see Appendixes G, H). Report an unusually slow heart rate (bradycardia) or signs of heart block and other arrhythmias, including palpitations, chest discomfort, shortness of breath, fainting, and fatigue/weakness.
Periodically assess balance, coordination, spasticity, gait, and other aspects of neuromuscular function. Document any improvement in function, but also report worsening of impairments or a relapse of multiple sclerosis symptoms.
Assess any breathing problems, and document signs of decreased pulmonary function such as shortness of breath, labored or difficult breathing, reduced pulse oximetry values, and cyanosis. Report severe or problematic respiratory impairments.
Watch for signs of leukopenia and lymphopenia, including fever, sore throat, mucosal lesions, and other signs of infection. Report these signs to the physician.
Assess any back pain to rule out musculoskeletal pathology; that is, try to determine if pain is drug induced rather than caused by anatomic or biomechanical problems.
Design and implement coordination, balance, gait training, and other therapeutic exercises to maintain function and complement drug effects in patients with MS.
Instruct patient to guard against infection (frequent hand washing, etc.), and to avoid crowds and contact with persons with contagious diseases.
Instruct patient to report other troublesome side effects such as prolonged or severe headache, blurred vision, eye pain, cough, or diarrhea.
Absorption: Well absorbed (93%) following oral administration.
Distribution: Extensively distributed to body tissues; 86% of parent drug distributes into red blood cells; active metabolite uptake 17%.
Metabolism and Excretion: Converted to its active metabolite, then metabolized mostly by the CYP4504F2 enzyme system, with further degradation by other enzyme systems. Most inactive metabolites excreted in urine (81%); <2.5% excreted as fingolimod and fingolimod-phosphate in feces.
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