glatiramer acetate

Action and Spectrum

Actions and Spectrum: 

glatiramer acetate is a medication that is a synthetic protein and is designed to mimic the structure of myelin basic protein (MBP).which is a component of myelin that is targeted by the immune system in MS.

By mimicking MBP, glatiramer acetate is thought to shift the immune system’s response away from attacking myelin and toward a more tolerable response. 

The spectrum of action of glatiramer acetate is specific to its use in the treatment of MS. It has been shown to reduce the frequency of relapses in patients with relapsing-remitting MS, as well as slow the progression of disability associated with the disease.

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Injection site erythema (66%) 

Injection site pruritus (40%) 

Weakness (41%) 

Anxiety (23%) 

Palpitations (17%) 

Injection site mass (27%) 

Hypertonia (22%) 

Arthralgia (24%) 

Vasodilation (27%) 

Injection site pain (73%) 

Chest pain (13-16% ) 

Injection site inflammation (49%) 

Rash (18%) 

Pruritus (18%) 

Flu syndrome (19%) 

Diarrhea (12%) 

Lymphadenopathy (12%) 

Dyspnea (19%) 

Injection site induration (13%) 

Injection site welt (11%) 

Pain (28%) 

1-10% 

Anorexia (8%) 

Injection site pain/inflammation (10%) 

Frequency not defined 

Asthenia 

Hypertonia 

Pain 

Arthralgia 

Anxiety 

Infection 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• glatiramer acetate is contraindicated in patients who have known hypersensitivity to the drug or any of its components. 

Caution 

• Injection site reactions: The most common side effect of glatiramer acetate is mild injection site reactions such as redness, pain, and swelling. Patients should be instructed on proper injection technique and rotating injection sites to minimize the risk of these reactions. 
• Immune system effects: glatiramer acetate is believed to work by modifying the immune system’s response, which can have effects on the body’s ability to fight infection. Patients should be monitored for signs of infection and advised to seek medical attention if they develop a fever, chills, or other symptoms of infection. 
• Pregnancy and breastfeeding: The safety of glatiramer acetate during pregnancy and breastfeeding is not well established, and it should only be used in these situations if the potential benefits outweigh the potential risks. 
• Kidney disease: glatiramer acetate is excreted primarily by the kidneys, and patients with kidney disease may be at increased risk of side effects. Dose adjustments might be necessary in patients with renal impairment. 
• Autoimmune disease: glatiramer acetate is used to treat autoimmune diseases, and patients with a history of autoimmune disease should be monitored closely for signs of disease flare or new autoimmune conditions. 
• Cardiovascular disease: Although glatiramer acetate is not believed to have significant cardiovascular effects, patients with a history of cardiovascular disease should be monitored closely during treatment. 

Pregnancy / Lactation

Pregnancy consideration:  

AU TGA pregnancy category: B1
US FDA pregnancy category: B  

Lactation:   

Excreted into human milk is known.   

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

The exact pharmacology of glatiramer acetate is not fully understood, but it is believed to work by modifying the immune response in patients with multiple sclerosis (MS). glatiramer acetate is a synthetic peptide made up of four amino acids, which are found in myelin basic protein (MBP). 

Pharmacodynamics: 

Mechanism of action: This medication is a synthetic amino acid copolymer, and its precise mechanism of action is not fully understood. It is believed to work by modulating the immune system, potentially by interfering with the antigen presenting function of certain immune cells, which may oppose pathogenic T-cell function. Additionally, it may activate T-lymphocyte suppressor cells that are specific for myelin antigen. 

Pharmacokinetics: 

Absorption 

The drug is not absorbed systemically and does not reach significant levels in the bloodstream. Instead, glatiramer acetate works locally in the tissues surrounding the injection site, where it modifies the immune response and reduces inflammation. 

Distribution 

After administration, both intact and partially hydrolyzed forms of the drug may enter the lymphatic circulation, with some also entering the systemic circulation. 

Metabolism 

The drug may undergo local hydrolysis during metabolism. 

Elimination and Excretion 

Because glatiramer acetate is not metabolized or excreted, it does not have a specific elimination half-life. 

Adminstartion

Administration: 

Subcutaneous administration 

glatiramer acetate is administered by subcutaneous injection, typically once daily or three times per week, depending on the specific dosing regimen prescribed by the healthcare provider. 

The medication is available in pre-filled syringes or autoinjectors, and the injection is typically given into the thigh, abdomen, or upper arm. Patients should be instructed on proper injection technique and rotating injection sites to minimize the risk of injection site reactions. 

glatiramer acetate should not be administered intravenously or intramuscularly, as these routes of administration have not been studied and may increase the risk of adverse effects. 

Patients should be advised to store glatiramer acetate in the refrigerator until use, but it can be stored at RT (room temperature) for up to one month if needed. Any unused medication should be discarded after the expiration date on the package. 

Patients should follow the dosing and administration instructions provided by their healthcare provider and should not adjust the dose or frequency of administration without consulting with their healthcare provider first. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: glatiramer 

Pronounced: [ gla-TIR-a-mer ] 

Why do we use glatiramer? 

glatiramer acetate is used to treat multiple sclerosis (chronic autoimmune disorder that affects the CNS). Specifically, glatiramer acetate is used to reduce the frequency of relapses and delay the progression of disability in patients with relapsing-remitting multiple sclerosis (RRMS). 

RRMS is the common form of multiple sclerosis, characterized by periods of relapse or flare-ups of symptoms, followed by periods of remission. glatiramer acetate is believed to work by modifying the immune system’s response. 

glatiramer acetate is not a cure for MS, but it can help to slow the progression of the disease and improve quality of life for patients with RRMS. It is typically used as a long-term treatment, and patients may require periodic monitoring and adjustments to their treatment regimen over time.