Glatiramer Acetate

Registered South African indications:

• Multiple sclerosis

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Pre-existing cardiac disorders
• May impair the ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: inj

Relapsing, remitting multiple sclerosis 
- Characterised by at least 2 attacks of neurological dysfunction over the preceding 2 years

• SC: 20mg, dly

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To be given at the same time each day

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Should not be administered by intravenous or intramuscular routes

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A decision concerning long term treatment should be made on an individual basis by the treating physician

Not established for use in children below 18 years

Pregnancy

• Caution; not recommended
• Studies in animals have not shown reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of glatiramer acetate during pregnancy unless the benefit to the mother outweighs the risk to the foetus
• The use of glatiramer acetate during pregnancy appears to be low risk. In addition, the benefits of the drug in reducing the number of relapses of multiple sclerosis appear to outweigh the potential, but unknown risks to the embryo-foetus
• Current data on pregnant women indicate no malformative or feto/neonatal toxicity of glatiramer acetate. To date, no relevant epidemiological data are available
• If indicated, glatiramer acetate should not be withheld because of pregnancy
• A 2012 prospective observational multicenter study evaluated the pregnancy outcomes in 423 cases where the mother had multiple sclerosis. In this study, 17 were exposed to glatiramer acetate, 88 to interferon beta, and 318 nonexposed. Glatiramer acetate was not associated with a higher frequency of spontaneous abortions to other negative pregnancy and foetal outcomes

Breastfeeding

• Caution; not recommended
• It is unknown whether glatiramer acetate or its metabolites are excreted in human milk
• In rats, no significant effects on offspring were observed except for a slight reduction in body weight gains in the offspring of mothers dosed during pregnancy and throughout lactation
• In a 2012 study using a nationwide database from Germany, pregnancy and breastfeeding outcomes in women with multiple sclerosis were compared in three groups: glatiramer (N=41), interferon-beta (N=78), and pregnancies not exposed to these agents (N=216). 170 of 335 women throughout all three groups breastfed exclusively. Significantly reduced relapse rates of multiple sclerosis during the first 3 months occurred compared with nonexclusive breastfeeding or nonbreastfeeding women (p<0.0001)
• A risk to the newborns/infants cannot be excluded. A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from therapy taking into account the benefit of breast feeding for the child and the benefit of therapy for the woman

Renal Impairment

• Caution; no information available,

Hepatic Impairment

• Caution; no information available

Elderly

• Caution; no information available

Porphyria information

• Possibly porphyrinogenic (PSP)

Drugs in sport

• Permitted - No warnings

Central Nervous System Disorders

• Anxiety
• Depression
• Nervousness
• Abnormal dreams
• Confusional state
• Euphoric mood
• Hallucination
• Hostility
• Mania
• Personality disorder
• Suicide attempt
• Headache
• Hypertonia
• Migraine
• Speech disorder
• Syncope
• Tremor
• Carpal tunnel syndrome
• Cognitive disorder
• Convulsion
• Dysgraphia
• Dyslexia
• Dystonia
• Motor dysfunction
• Myoclonus
• Neuritis
• Neuromuscular blockade
• Nystagmus
• Paralysis
• Peroneal nerve palsy
• Stupor
• Asthenia

Cardiovascular Disorders

• Palpitations
• Tachycardia
• Extrasystoles
• Bradycardia
• Paroxysmal tachycardia
• Vasodilatation
• Varicose vein
• Chest pain

Respiratory Disorders

• Dyspnoea
• Cough
• Seasonal rhinitis
• Apnoea
• Epistaxis
• Hyperventilation
• Laryngospasm
• Lung disorder
• Choking sensation
• Influenza
• Bronchitis
• Rhinitis

Gastrointestinal Disorders

• Nausea and vomiting
• Anorectal disorder
• Constipation
• Dental Caries
• Tooth Abscess
• Dyspepsia
• Dysphagia
• Faecal incontinence
• Colitis
• Colonic polyp
• Enterocolitis
• Eructation
• Oesophageal ulcer
• Periodontitis
• Rectal haemorrhage
• Salivary gland enlargement
• Mucous membrane disorder
• Gastroenteritis

Hepatobiliary Disorders

• Abnormal hepatic function tests
• Cholelithiasis
• Hepatomegaly
• Toxic hepatitis

Genitourinary Disorders

• Micturition urgency
• Pollakiuria
• Urinary retention
• Haematuria
• Nephrolithiasis
• Urinary tract disorder
• Urine abnormality
• Breast engorgement
• Erectile dysfunction
• Pelvic prolapse
• Priapism
• Prostatic disorder
• Abnormal cervical smear
• Testicular disorder
• Vaginal haemorrhage
• Vulvovaginal disorder
• Vaginal Candidiasis
• Pyelonephritis

Endocrine and Metabolic Disorders

• Goitre
• Hyperthyroidism
• Anorexia
• Increased weight
• Alcohol intolerance
• Gout
• Hyperlipidaemia
• Increased sodium
• Decreased ferritin
• Chills
• Hypothermia

Musculoskeletal Disorders

• Arthralgia
• Back pain
• Neck Pain
• Arthritis
• Bursitis
• Flank pain
• Muscle atrophy
• Osteoarthritis

Skin and Subcutaneous Tissue Disorders

• Rash
• Ecchymosis
• Hyperhidrosis
• Pruritus
• Skin disorder
• Urticaria
• Angioedema
• Contact dermatitis
• Erythema nodosum
• Skin nodule
• Injection site reactions
• Peripheral oedema
• Facial oedema
• Cyst
• Abscess
• Cellulitis
• Furuncle
• Skin necrosis
• Skin erythema
• Benign neoplasm of skin
• Skin cancer

Immune, Blood and Lymphatic System Disorders

• Anaphylaxis
• Infection
• Herpes Simplex
• Herpes Zoster
• Neoplasm
• Lymphadenopathy
• Leukocytosis
• Leukopenia
• Splenomegaly
• Thrombocytopenia
• Abnormal lymphocyte morphology
• Hypersensitivity
• Fever

Sensory Disorders

• Dysgeusia
• Visual field defect
• Diplopia
• Eye Disorder
• Cataract
• Corneal lesion
• Dry eye
• Eye haemorrhage
• Eyelid ptosis
• Mydriasis
• Optic atrophy
• Ear disorder
• Otitis Media

Others

• Abortion
• Hangover
• Post vaccination syndrome
• Pain in extremity

No significant interactions

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See Additional Prescribing Points

None routine. Specific cases may require

• Renal function

Corticosteroids

• An increased incidence of injection site reactions has been seen in glatiramer acetate patients receiving concurrent administration of corticosteroids

Theoretical interaction with protein-bound substances

• In vitro work suggests that glatiramer acetate in blood is highly bound to plasma proteins but that it is not displaced by, and does not itself displace, phenytoin or carbamazepine
• Nevertheless, as glatiramer acetate has, theoretically, the potential to affect the distribution of protein-bound substances, concomitant use of such medicinal products should be monitored carefully

The mechanisms by which glatiramer acetate exerts its effects in patients with multiple sclerosis (MS) are not fully understood. However, it is thought to act by modifying immune processes that are currently believed to be responsible for the pathogenesis of MS. Studies in animals suggest glatiramer acetate acts on innate immune cells, including monocytes, dendritic cells and B cells, which in turn modulate adaptive functions of B and T cells inducing anti-inflammatory and regulatory cytokine secretion.

Injection (per ml) 20mg

• Copaxone pre-filled syringe  (Teva) originator