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Medication Safety Issues
Sound-alike/look-alike issues:
Copaxone® may be confused with Compazine®
Pronunciation
(gla TIR a mer AS e tate)
U.S. Brand Names
Index Terms
Generic Available
No
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Management of relapsing-remitting type multiple sclerosis, including patients with a first clinical episode with MRI features consistent with multiple sclerosis
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women. Use in pregnancy only if clearly necessary.
Lactation
Excretion in breast milk unknown/use caution
Contraindications
Hypersensitivity to glatiramer acetate, mannitol, or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Chest pain: May or may not occur with the immediate postinjection reaction; described as a transient pain usually resolving in a few minutes; often unassociated with other symptoms.
• Lipoatrophy: May occur locally at injection site and may not resolve; advise patient to follow proper injection technique and rotate site daily.
• Immune response: Although there has not been a systematic evaluation of glatiramer's potential to affect other immune functions, it may interfere with recognition of foreign antigens undermining the body's tumor surveillance and defense system against infection.
• Systemic reactions: Immediate postinjection systemic reactions occur in a substantial percentage of patients (~16% in studies); symptoms (anxiety, chest pain, dysphagia, flushing, palpitations, urticaria) may begin within minutes of injection and are usually self-limited and transient. These symptoms generally occur several months after initiation of glatiramer.
Disease-related concerns:
• Renal impairment: Safety and efficacy has not been established in patients with renal impairment.
Special populations:
• Elderly: Safety and efficacy has not been established in the elderly.
• Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precautions:
• Administration: For SubQ use only, not for I.V. administration.
• Antigenic: Glatiramer acetate is antigenic, and may possibly lead to the induction of untoward host responses. Glatiramer acetate-reactive antibodies (IgG subtype) form in most patients.
Adverse Reactions
>10%:
Cardiovascular: Vasodilation (20%), chest pain (13%)
Central nervous system: Pain (20%), anxiety (13%)
Dermatologic: Rash (19%)
Gastrointestinal: Nausea (15%)
Local: Injection site reactions: Inflammation (49%), erythema (43%), pain (40%), pruritus (27%), mass (27%)
Neuromuscular & skeletal: Weakness (22%), back pain (12%)
Respiratory: Dyspnea (14%)
Miscellaneous: Infection (30%), flu-like syndrome (14%), diaphoresis (15%)
1% to 10%:
Cardiovascular: Edema (8%; includes peripheral and facial), palpitation (7%), tachycardia (5%), syncope (3%), hypertension (1%)
Central nervous system: Fever (6%), migraine (4%), chills (3%), nervousness (2%), speech disorder (2%), abnormal dreams (1%), emotional lability (1%), stupor (1%)
Dermatologic: Bruising (8%), pruritus (5%), erythema (4%), urticaria (3%), skin nodule (2%), eczema (1%), pustular rash (1%)
Endocrine & metabolic: Amenorrhea (1%), impotence (1%), menorrhagia (1%)
Gastrointestinal: Vomiting (7%), gastroenteritis (6%), weight gain (3%), dysphagia (2%), dental caries (1%)
Genitourinary: Urinary urgency (5%), vaginal moniliasis (4%)
Local: Injection site reactions: Hemorrhage (5%), hypersensitivity (4%), fibrosis (2%), lipoatrophy (2%), abscess (1%), edema (1%)
Neuromuscular & skeletal: Neck pain (8%), tremor (4%)
Ocular: Diplopia (3%), visual field defect (1%)
Respiratory: Rhinitis (7%), bronchitis (6%), cough (6%), laryngismus (5%), hyperventilation (1%)
Miscellaneous: Lymphadenopathy (7%), hypersensitivity (3%)
<1% (Limited to important or life-threatening): Anemia, angioedema, aphasia, appetite increased, arthritis, asthma, atrial fibrillation, bradycardia, cervical cancer, cholecystitis, colitis, cataract, corneal ulcer, Cushing's syndrome, dermatitis, dry eyes, dry skin, esophagitis, gastrointestinal carcinoma, gastrointestinal hemorrhage, gastrointestinal ulcer, gout, hallucination, hepatomegaly, hypotension, injection site necrosis, leukopenia, libido decreased, mania, mouth ulceration, optic neuritis, orthostatic hypotension, pancreatitis, pancytopenia, photophobia, pneumonia, priapism, pyelonephritis, seizures, skin cancer, splenomegaly, stomatitis, urethritis
Postmarketing and/or case reports (limited to important or life-threatening): Allergic reaction, anaphylactoid reaction, angina, arrhythmia, blindness, carcinoma (breast, bladder, lung, ovarian), cardiomyopathy, cholelithiasis, cirrhosis, CNS neoplasm, glaucoma, heart failure, hepatitis, leukemia, hypercholesterolemia, lupus erythematosus, lymphoma-like reaction, meningitis, MI, neuralgia, pericardial effusion, peripheral vascular disease, pulmonary embolism, renal failure, sepsis, spasm, stroke, thrombocytopenia, thrombophlebitis, thrombosis
Drug Interactions
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy modification
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Risk D: Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Risk C: Monitor therapy
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Vaccinial infections may develop. Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
Storage
Store in refrigerator at 2°C to 8°C (36°F to 46°F); excursions to room temperature for up to 1 month do not have a negative impact on potency. Avoid heat; protect from intense light.
Mechanism of Action
Glatiramer is a mixture of random polymers of four amino acids; L-alanine, L-glutamic acid, L-lysine and L-tyrosine, the resulting mixture is antigenically similar to myelin basic protein, which is an important component of the myelin sheath of nerves; glatiramer is thought to induce and activate T-lymphocyte suppressor cells specific for a myelin antigen, it is also proposed that glatiramer interferes with the antigen-presenting function of certain immune cells opposing pathogenic T-cell function
Pharmacodynamics/Kinetics
Distribution: Small amounts of intact and partial hydrolyzed drug enter lymphatic circulation
Metabolism: SubQ: Large percentage hydrolyzed locally
Dosage
Adults: SubQ: 20 mg daily
Administration: Other
For SubQ administration in the arms, abdomen, hips, or thighs; rotate injection sites to prevent lipoatrophy. Bring to room temperature prior to use. Visually inspect the solution; discard if solution is cloudy or contains any particulate matter.
Patient Education
This drug will not cure MS, but may help relieve the severity and frequency of attacks. This drug can only be given by subcutaneous injection. Your prescriber will instruct you in proper injection technique and syringe/needle disposal. You should also read the information leaflet supplied with each package to reinforce the injection instructions. Do not stop or change doses without consulting your prescriber. May cause a transient reaction after injection, including flushing, chest tightness, dyspnea, or palpitations (usually last 30 minutes or less). May cause weakness, dizziness, confusion, nervousness, or anxiety (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or nausea or vomiting (frequent mouth care and sucking on lozenges may help). Report chest pain or pounding heartbeat; persistent diarrhea or GI upset; infection (vaginal itching or drainage, sores in mouth, unusual fever or chills) or flu-like symptoms (swollen glands, chills, excessive sweating); bruising, rash, or skin irritation; joint pain or neck pain; swelling of puffiness of face; vision changes or ear pain; unusual cough or respiratory difficulty; alterations in menstrual pattern; skin depression, hard lump, redness, pain, or swelling at injection site; or any other persistent adverse reactions. Breast-feeding precaution: Consult prescriber if breast-feeding.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Ulcerative stomatitis, salivary gland enlargement, and oral moniliasis.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause anxiety or depression
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Assess potential for interactions with other prescriptions, OTC medications, or herbal products patient may be taking. Assess effectiveness and adverse response (eg, postinjection reactions - self-resolving flushing, chest tightness, dyspnea, palpitations). Teach patient proper use (reconstitution, injection technique, and syringe/needle disposal), possible side effects/appropriate interventions, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free]:
Copaxone®: 20 mg/mL (1 mL) [prefilled syringe; contains mannitol; packaged with alcohol pads]
Pricing: U.S. (www.drugstore.com)
Kit (Copaxone)
20 mg/mL (1): $2817.67
References
Bornstein MB, Miller A, Slagle S, et al, “A Pilot Trial of Cop 1 in Exacerbating-Remitting Multiple Sclerosis,” N Engl J Med, 1987, 317(7):408-14.
Cohen JA, Rovaris M, Goodman AD, et al, “Randomized, Double-Blind, Dose-Comparison Study of Glatiramer Acetate in Relapsing-Remitting MS,” Neurology, 2007, 68(12):939-44.
Comi G, Filippi M, Wolinsky JS, et al, “European/Canadian Multicenter, Double-Blind, Randomized, Placebo-Controlled Study of the Effects of Glatiramer Acetate on Magnetic Resonance Imaging-Measured Disease Activity and Burden in Patients With Relapsing Multiple Sclerosis,” Ann Neurol, 2001, 49(3):290-7.
Johnson KP, Brooks BR, Cohen JA, et al, “Copolymer 1 Reduced Relapse Rate and Improves Disability in Relapsin-Remitting Multiple Sclerosis: Results of a Phase III Multicenter, Double-Blind, Placebo-Controlled Trial,” Neurology, 1995, 45(7):1268-76.
Johnson KP, Brooks BR, Cohen JA, et al, “Extended Use of Glatiramer Acetate (Copaxone) is Well Tolerated and Maintains Its Clinical Effect on Multiple Sclerosis Relapse Rate and Degree of Disability,” Neurology, 1998, 50(3):701-8.
Noseworthy JH, Lucchinetti C, Rodriguez M, and Weinshenker BG, “Multiple Sclerosis,” N Engl J Med, 2000, 343(13):938-52.
International Brand Names
Lexi-Comp.com
Last full review/revision July 2009
Content last modified July 2009
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