Glatiramer Acetate (Monograph)

Brand names: Copaxone, Glatopa [Web])
Drug class: Amino Acid Polymers

Medically reviewed by Drugs.com on Jun 10, 2024. Written by ASHP.

Introduction

Synthetic polypeptide mixture containing 4 naturally occurring amino acids with immunomodulatory and disease-modifying activity in multiple sclerosis.

Uses for Glatiramer Acetate

Multiple Sclerosis (MS)

Treatment of adults with relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting MS (RRMS), and active secondary progressive MS.

Glatiramer acetate is one of several disease-modifying therapies used in the management of relapsing forms of MS. Although not curative, these therapies have all been shown to modify several measures of disease activity, including relapse rates, new or enhancing MRI lesions, and disability progression.

The American Academy of Neurology (AAN) recommends that disease-modifying therapy be offered to patients with relapsing forms of MS who have had recent relapses and/or MRI activity. Clinicians should consider adverse effects, tolerability, method of administration, safety, efficacy, and cost of the drugs in addition to patient preferences when selecting an appropriate therapy.

Has been evaluated for primary progressive MS (PPMS)^{† [off-label]}.

Glatiramer Acetate Dosage and Administration

General

Patient Monitoring

• Routine laboratory monitoring is not considered necessary in patients receiving glatiramer acetate.

Dispensing and Administration Precautions

• Administer the initial self-administered dose under the supervision of a qualified healthcare professional.

• Using an autoinjector that is incompatible for use with the medication may increase the risk for medication errors (e.g., dose omission or administration of a partial dose).

• Several preparations of glatiramer acetate are commercially available (e.g., Copaxone, Glatopa and other generic preparations), and there are 2 commercially available dosage strengths of the drug. Glatiramer acetate 20 mg/mL is administered once daily and glatiramer acetate 40 mg/mL is administered 3 times a week; the 2 different dosage strengths are not interchangeable.

Administration

Administer only by sub-Q injection; do not administer IV.

Sub-Q Administration

Commercially available prefilled syringes intended for single use only; discard unused portion.

Allow prefilled syringes to reach room temperature by removing from refrigerator about 20 minutes prior to use.

Inject sub-Q into the arm, abdomen, hip, or thigh.

Localized lipoatrophy and skin necrosis reported; to minimize risk, follow proper injection technique and rotate injection sites with each injection.

Dosage

Available as glatiramer acetate; dosage expressed in terms of the salt.

Adults

Multiple Sclerosis

Sub-Q

Dosage recommendations differ based on dosage strength (20 or 40 mg/mL) used. Dosage strengths are not interchangeable.

If using the 20-mg/mL injection, recommended dosage is 20 mg once daily.

If using the 40-mg/mL injection, recommended dosage is 40 mg 3 times a week (administer injections at least 48 hours apart).

Special Populations

No special population dosage recommendations at this time.

Cautions for Glatiramer Acetate

Contraindications

• Known hypersensitivity to glatiramer acetate or mannitol.

Warnings/Precautions

Immediate Post-injection Reaction

Acute injection reactions reported after sub-Q injection. Symptoms, which are generally transient and self-limited and do not require treatment, include flushing, chest pain or tightness, palpitations, anxiety, dyspnea, constriction of the throat, tachycardia, and urticaria. Majority of symptoms occur within 1 hour, but may occur within seconds to minutes of administration.

Chest Pain

Transient chest pain reported, usually presenting >1 month after initiation of therapy. Some episodes occurred as part of immediate post-injection reactions, but many did not. Episodes generally last only a few minutes, often are not associated with other symptoms, and do not appear to produce clinically important sequelae. Some patients experience more than one such episode.

Lipoatrophy and Skin Necrosis

Localized lipoatrophy (i.e., loss of subcutaneous fat) and, rarely, skin necrosis at the injection site reported. Lipoatrophy may occur at various times after treatment initiation, sometimes after several months and is thought to be permanent. No known treatment for lipoatrophy.

Advise patients to follow proper injection technique and rotate injection sites daily to minimize risk.

Potential Effects on Immune Response

Because glatiramer acetate can modify immune response, the drug may interfere with immune functions.

Antibodies that react to glatiramer acetate are formed in most patients receiving the drug daily at the recommended dosage; current evidence suggests that such antibodies do not neutralize the drug’s therapeutic effects.

Hepatic Injury

Hepatic injury, including liver failure and hepatitis with jaundice, reported. May occur at various times after treatment initiation, most often within 1–3 months; generally self-limited after discontinuation of the drug.

Glatiramer Acetate Products and Administration Errors

Medication errors have occurred when glatiramer acetate products are administered with incompatible autoinjectors. Some glatiramer acetate products can be administered by an optional compatible autoinjector; however, not all glatiramer acetate products have a marketed optional compatible autoinjector for administration.

Using an optional autoinjector that is not compatible for use may increase risk for medication errors. If using an optional autoinjector for administration, ensure the device is compatible for use with the specific glatiramer acetate product by referring to the autoinjector labeling.

Specific Populations

Pregnancy

Insufficient information to determine whether there is a drug-associated risk when used during pregnancy. No fetal harm observed in animal reproduction studies.

Lactation

Not known whether glatiramer is distributed into milk; the effects on nursing infants or on milk production also unknown. Based on low systemic exposure due to substantial local hydrolysis of glatiramer acetate following subcutaneous administration, breastfeeding is not expected to result in clinically relevant exposure of the infant to the drug. Consider benefits of breast-feeding along with mother's clinical need for glatiramer acetate and any potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.

Has been used for pediatric-onset MS (POMS)^{† [off-label]}; however, well-controlled studies with prolonged follow-up needed to assess long-term efficacy and safety.

Geriatric Use

Not studied in geriatric patients.

Renal Impairment

Pharmacokinetics not studied.

Common Adverse Effects

Most common adverse effects reported with glatiramer acetate 20 mg/mL (≥10%) include injection site reactions, vasodilatation, rash, dyspnea, chest pain.

Most common adverse effect reported with glatiramer acetate 40 mg/mL (≥10%) was injection site reactions.

Drug Interactions

Interactions with other drugs not fully evaluated to date.

No clinically important interactions reported with drugs commonly used in MS, including concurrent corticosteroid therapy for up to 28 days. Not formally evaluated in combination with interferon beta.

Glatiramer Acetate Pharmacokinetics

Distribution

Following sub-Q injection, some portion of the dose may enter the lymphatic circulation and some may enter systemic circulation. Does not appear to cross the blood-brain barrier.

Elimination

Metabolism

Substantial portion of sub-Q dose appears to be hydrolyzed locally at injection site to small oligopeptides and free amino acids.

Stability

Storage

Parenteral

Injection

2–8°C; protect from light. May be stored at room temperature (15–30°C) for ≤1 month. Do not freeze.

Actions

• Mechanism of action not fully elucidated; appears to modify immune processes responsible for the pathogenesis of MS.

• Induces and activates drug-specific suppressor T-cells that migrate into the CNS and down-regulate immune response (e.g., inflammation) to myelin antigens in the periphery.

Advice to Patients

• Advise patients to read the manufacturer’s patient information prior to beginning glatiramer acetate therapy and each time the prescription is refilled.

• Instruct patients and/or caregivers on proper injection techniques (including use of aseptic technique and avoiding reuse of syringes and needles and proper disposal of such equipment).

• Risk of immediate post-injection reaction. Advise patients that glatiramer acetate may cause various symptoms after injection, including flushing, chest pain, palpitations, anxiety, dyspnea, throat constriction, and urticaria. Inform patients that these symptoms usually are transient, occur within seconds to minutes after injection, and self-limited, and do not require specific treatment.

• Advise patients that they may experience chest pain either as part of an immediate post-injection reaction or in isolation. Inform patients that the pain should be transient (usually lasting only for a few minutes). Some patients may experience more than one such episode, usually beginning at least one month after beginning treatment. Advise patients to seek medical attention if they experience chest pain of unusual duration or intensity.

• Risk of lipoatrophy and skin necrosis at the injection site. Advise patients to follow proper injection technique and rotate injection areas and sites with each injection.

• Risk of hepatic injury. Advise patients on signs and symptoms of hepatic injury (e.g., nausea, loss of appetite, dark colored urine, yellowing of skin or sclera). Advise patients to contact their healthcare provider immediately if they experience these symptoms.

• Advise patients that the 20-mg/mL and 40-mg/mL strengths of glatiramer acetate are not interchangeable and are administered using different dosage schedules.

• Inform patients of the recommended storage instructions for glatiramer acetate. Advise patients not to expose the drug to higher temperatures, freezing temperatures, or to intense light.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Reload page with references included

Frequently asked questions

• Where and how should Copaxone be injected?
• What happens if an MS patient stops taking Copaxone?
• How long can you take Copaxone?
• How long does it take for Copaxone to be effective?
• How does Copaxone work for multiple sclerosis?

View more FAQ

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