Glatiramer Acetate

(BAN, USAN)
Synonyms: COP-1; Copolymer 1; Glatirameeriasetaatti; Glatiramer, acetato de; Glatiramer Asetat; Glatirameracetat; Glatirameri Acetas. acetate.
Cyrillic synonym: Глатирамер Ацетат.

💊 Chemical information

CAS — 28704-27-0 (glatiramer); 147245-92-9 (glatiramer acetate).
ATC — L03AX13.
ATC Vet — QL03AX13.

💊 Adverse Effects and Precautions

Immediate post-injection reactions are common with glatiramer acetate and include chest pain, palpitations or tachycardia, dyspnoea, throat constriction, urticaria, flushing (vasodilatation), and anxiety. These reactions are generally short-lived and resolve spontaneously. They have generally occurred only some months after treatment with glatiramer was started. Other common adverse effects include asthenia, nausea, constipation, diarrhoea, rash, sweating, arthralgia, hypertonia, and dizziness. Convulsions and anaphylactoid reactions have been reported rarely. Antibodies to the drug develop with chronic therapy but are of unknown clinical significance. Pain, erythema, inflammation, mass, pruritus, and induration may occur at the injection site; localised lipoatrophy and, rarely, skin necrosis has also been reported. Glatiramer acetate should be given with caution to patients with pre-existing cardiac disorders; such patients should be followed up regularly during treatment.
1. Ziemssen T, et al. Risk-benefit assessment of glatiramer acetate in multiple sclerosis. Drug Safety 2001; 24: 979–90.

Anaphylaxis.

A systemic anaphylactic reaction to glatiramer acetate developed in a patient who showed a strong immunoglobulin response including specific immunoglobulin E.1
1. Rauschka H, et al. Severe anaphylactic reaction to glatiramer acetate with specific IgE. Neurology 2005; 64: 1481–2.

Effects on the skin.

Localised lipoatrophy at the injection site developed in 6 patients receiving glatiramer acetate.1 Examination of 76 patients over a 6-month period in one centre2 revealed evidence of lipoatrophy in at least one injection site in 34 patients; of these, 5 cases were severe. Prevalence of lipoatrophy was much higher than expected, and in some cases, it occurred only a few months after treatment started.2 Erythema nodosum confirmed by biopsy has been reported in one patient;3 spontaneous resolution occurred without stopping treatment.
1. Drago F, et al. Localized lipoatrophy after glatiramer acetate injection in patients with remitting-relapsing multiple sclerosis. Arch Dermatol 1999; 135: 1277–8
2. Edgar CM, et al. Lipoatrophy in patients with multiple sclerosis on glatiramer acetate. Can J Neurol Sci 2004; 31: 58–63
3. Thouvenot E, et al. Erythema nodosum and glatiramer acetate treatment in relapsing-remitting multiple sclerosis. Multiple Sclerosis 2007; 13: 941–4.

💊 Interactions

UK licensed product information reports that an increased incidence of injection-site reactions to glatiramer acetate has been seen in patients also given corticosteroids.

💊 Pharmacokinetics

A substantial fraction of a subcutaneous dose of glatiramer is believed to be hydrolysed locally. Some of the injected dose is also presumed to enter the lymphatic system, either intact or partially hydrolysed.

💊 Uses and Administration

Glatiramer acetate, a random polymer of L-alanine, L-glutamic acid, L-lysine, and L-tyrosine, is a polypeptide that has some structural resemblance to myelin basic protein, and is used to reduce the frequency of relapses in the management of relapsingremitting multiple sclerosis. It is given by subcutaneous injection in a dose of 20 mg daily. It should not be given by the intravenous or intramuscular route. An oral formulation has been investigated with disappointing results.

Multiple sclerosis.

Reviews1,2 and a meta-analysis3 of controlled studies of glatiramer acetate in the treatment of multiple sclerosis concluded that it is of benefit, although one systematic review4 questions this and failed to find evidence to support its routine use. The mechanism of glatiramer acetate has also been reviewed.5
1. Simpson D, et al. Glatiramer acetate: a review of its use in relapsing-remitting multiple sclerosis. CNS Drugs 2002; 16: 825–50
2. Ruggieri M, et al. Glatiramer acetate in multiple sclerosis: a review. CNS Drug Rev 2007; 13: 178–91
3. Boneschi FM, et al. Effects of glatiramer acetate on relapse rate and accumulated disability in multiple sclerosis: meta-analysis of three double-blind, randomized, placebo-controlled clinical trials. Multiple Sclerosis 2003; 9: 349–55
4. Munari L, et al. Therapy with glatiramer acetate for multiple sclerosis. Available in The Cochrane Database of Systematic Reviews; Issu
4. Chichester: John Wiley; 2003 (accessed 09/01/08)
5. Schrempf W, Ziemssen T. Glatiramer acetate: mechanisms of action in multiple sclerosis. Autoimmun Rev 2007; 6: 469–75.

💊 Preparations

Proprietary Preparations

Arg.: Copaxone; Austral.: Copaxone; Austria: Copaxone; Belg.: Copaxone; Braz.: Copaxone; Canad.: Copaxone; Cz.: Copaxone; Denm.: Copaxone; Fin.: Copaxone; Fr.: Copaxone; Ger.: Copaxone; Gr.: Copaxone; Hung.: Copaxone; Irl.: Copaxone; Israel: Copaxone; Ital.: Copaxone; Mex.: Copaxone; Neth.: Copaxone; Norw.: Copaxone; NZ: Copaxone; Pol.: Copaxone; Port.: Copaxone; Rus.: Copaxone (Копаксон); Spain: Copaxone; Swed.: Copaxone; Switz.: Copaxone; Turk.: Copaxone; UK: Copaxone; USA: Copaxone.
Published May 08, 2019.