Types of Multiple Sclerosis Medications and Treatments

Multiple sclerosis medications are prescribed to treat multiple sclerosis (MS), an autoimmune disorder that affects the central nervous system (CNS). These medications may prevent or slow down the progression of MS and related disabilities, reduce the duration and frequency of relapses, treat acute relapses and relieve MS-related symptoms.

Multiple sclerosis medications are prescribed to treat multiple sclerosis (MS), an autoimmune disorder that affects the central nervous system (CNS). A large array of medications and therapies are used to manage multiple sclerosis, which can affect a wide spectrum of neurological functions and cause disabilities.

Multiple sclerosis medications are systemic medications taken orally or administered as injections or infusions. The targets of multiple sclerosis medications are to:

• Prevent or slow down the progression of MS and related disabilities
• Reduce duration and frequency of relapses
• Treat acute relapses
• Relieve MS-related symptoms

The primary medications used to treat multiple sclerosis are known as disease-modifying drugs (DMDs). DMDs modulate or suppress the immune system in different ways to alter the course of the disease and prevent or reduce relapses.

• Disease-modifying drugs include both lab-manufactured biological protein formulations and synthetic drugs which work on the immune system. Several types of FDA-approved biologic medications such as interferons are the first type of medications to be approved for MS, and monoclonal antibodies are prescribed for treating multiple sclerosis.

Synthetic immunomodulatory drugs approved by FDA for treating MS include glatiramer, cladribine, and teriflunomide.

• A new class of drugs known as sphingosine 1-phosphate (S1P) receptor modulators, which include siponimod and ozanimod, are the latest to be approved by FDA to treat MS.

FDA has approved the cancer drug mitoxantrone for aggressive MS, while another cancer drug, cyclophosphamide, is often used off-label. Immunosuppressants used off-label for MS include drugs such as methotrexate and azathioprine, which are approved to treat rheumatoid arthritis, another autoimmune disorder.

Acute relapses/flare-ups of multiple sclerosis are treated with corticosteroids to speed up recovery, along with DMDs.

For symptom relief, a multitude of drug classes is prescribed, because MS symptoms range from mild to severe, affecting various neurological and neuromuscular functions. Medications are prescribed to treat symptoms such as pain, cognitive dysfunction, fatigue, and bowel and bladder problems.

Multiple sclerosis is an inflammatory autoimmune disorder that affects the central nervous system, which consists of the brain and the spine. The CNS regulates all bodily functions, processes sensory information, and enables appropriate neuromuscular responses to them.

In multiple sclerosis, an abnormal immune system attacks healthy nerve cells, causing inflammation and lesions in the brain and spine. The immune system primarily attacks myelin, a fatty substance that insulates nerve fibers (axons) and helps in the conduction of electrical signals.

Axons are long hair-like projections from nerve cells (neurons), which transmit signals between nerve cells. Damage to myelin and axons disrupts communication between nerve cells and leads to various neuromuscular disabilities, depending on the CNS region affected.

Multiple Sclerosis Types

The course of multiple sclerosis and its symptoms are unique to each individual. Multiple sclerosis is considered active if relapses occur, with evidence of lesions in MRI tests, over a specific period of time. MS is also characterized as worsening or non-worsening, depending on whether disabilities increase or remain stable after relapses.

Multiple sclerosis is categorized into the following four types, based on clinical characteristics, frequency of relapses, and time is taken for lesion development and disease progression.

Relapsing-remitting MS (RRMS)

Relapsing-remitting MS (RRMS) is the most common and accounts for approximately 85% of MS patients. RRMS is marked by recurrent attacks in different parts of the CNS with periods of partial or complete remission between relapses.

Each individual may experience different symptoms, and new symptoms may appear with each attack. Some symptoms may disappear completely during remission, but some may remain and worsen over the years because of cumulative effects from partial recoveries after relapses.

Two subtypes that may be grouped under RRMS are:

• Clinically isolated syndrome (CIS): A single episode of neurologic symptoms caused by inflammation and destruction of myelin (demyelination) in the CNS. This may be the first episode of RRMS.
• Benign MS: Patients with benign MS experience near-complete remission after a relapse, with little or no accumulated disability.

Secondary progressive MS (SPMS)

Secondary progressive MS (SPMS) initially may follow the course of relapse and remission. Approximately 50% of RRMS turns into SPMS within 10-15 years of onset. SPMS may or may not have relapse episodes, but the disease progressively worsens over time, with increasing disability.

Primary progressive MS (PPMS)

Primary progressive MS is characterized by continued progression of MS without relapses or remissions. Neurological symptoms and disabilities accumulate and steadily worsen over time.

Progressive-relapsing MS (PRMS)

In progressive-relapsing MS, occasional relapses occur with a steady progression of disease and accumulation of disabilities.

Symptoms of MS are unique to each individual and vary depending on the CNS region affected by the disease. The severity of symptoms depends on the MS type and its progression. Classic symptoms of MS include the following:

• Fatigue, which occurs in nearly 80% of MS patients
• Pain, which occurs in up to 50% of MS patients at some point
• Acute inflammation (acute transverse myelitis) on both sides of spinal cord sections, with symptoms such as:
• Numbness, tingling, itching, and/or other abnormal sensations (paresthesia), an early symptom of MS
• Weakness in arms and/or legs
• Back pain radiating to legs, arms, chest, and belly
• Bladder, bowel, and sexual dysfunction
• Muscle cramping and/or stiffness (spasticity)
• Walking difficulties, and loss of balance and coordination
• Dizziness and vertigo
• Tremor
• Heat intolerance
• Inflammation of the optic nerve (optic neuritis)
• Involuntary eye movements (nystagmus)
• Blurred vision and other vision problems
• Facial muscle twitching (myokymia)
• Slurred speech and other speech difficulties
• Swallowing problems
• Hearing loss
• Facial nerve pain (trigeminal neuralgia)
• Cognitive problems such as difficulty with concentration, attention span, learning, memory, and comprehension
• Depression, mood swings, and irritability
• Bipolar disorder, usually in the late stages of MS
• Seizures in a few patients

As with most autoimmune disorders, it is unclear what exactly causes multiple sclerosis. Evidence is inconclusive, but research indicates multiple sclerosis may be triggered by a combination of factors such as:

• Genetic predisposition: Susceptibility to MS may occur due to variations in a gene known as HLA-DRB1, which has been consistently associated with MS. HLA-DRB1 gene encodes proteins that help immune cells such as T-cells, distinguish between the body’s own proteins and foreign ones.
• Viral infections: Viral infections may activate self-reactive T-cells in the CNS, which otherwise remain dormant. Some viruses and bacteria may produce proteins that mimic the body’s proteins, which can make T-cells attack the body’s own cells along with the foreign antigens.
• Vitamin D deficiency: Low vitamin D levels may be a cause of MS. Vitamin D helps reduce inflammation by lowering the secretion of pro-inflammatory proteins (cytokines) and increasing the release of anti-inflammatory cytokines by immune cells.
• Geographic factors: Lower sunlight exposure in higher latitudes is thought to play a role in MS. The incidence of MS is lower in tropical regions in comparison to the northernmost and southernmost regions, though there are several exceptions that may be explained by genetic factors and vitamin D-rich diets.

Triggers for MS

Triggers for MS relapse episodes include:

• Stress
• Fatigue and lack of sleep
• Heat
• Infections
• Poor diet
• Skipping MS medications
• Drug interactions
• Smoking

Currently, there is no cure for multiple sclerosis, but the condition can be managed with appropriate treatment, and lifestyle modifications to avoid triggers. Treatment can help relieve symptoms, prolong remission periods, slow down disease progression and limit disability.

Treatments and medications are individualized depending on the type of MS and the symptoms. Medications constitute the mainstay treatment for multiple sclerosis. Many new disease-modifying drugs have been approved by FDA between 2017 and 2018, and research continues to find safer and more effective drugs. 

Therapies used in the treatment of MS include:

• Medications
• Physical and occupational therapies to rehabilitate after a relapse.
• Stem cell transplantation.
• Plasma exchange (plasmapheresis), is a procedure in which the patient’s plasma, which contains the destructive immune cells, is removed and replaced with a plasma substitute or donated plasma.
• Surgical procedures to relieve symptoms such as neuropathic pain, limb spasticity, or bowel problems.

Medications prescribed for multiple sclerosis are of two primary types:

Disease-modifying drugs include:

• Immunomodulators
• Immunosuppressants
• Sphingosine 1-phosphate (S1P) receptor modulators

Symptom management drugs include:

• Corticosteroids
• Dopamine agonists
• Skeletal muscle relaxers
• Neuromuscular blockers
• Alpha-2 adrenergic agonists
• Potassium channel blockers
• Acetylcholinesterase inhibitors
• Benzodiazepines
• Stimulants
• Anticonvulsants
• Selective serotonin-norepinephrine reuptake inhibitors (SNRIs)
• Nonsteroidal anti-inflammatory drugs (NSAIDs)
• Antispasmodic agents
• Laxatives
• Antidiarrheals

Disease-modifying drugs

Disease-modifying drugs modulate or suppress the immune system in different ways to slow down disease progression and limit disabilities.

Immunomodulators

Immunomodulators work by blocking the activity of specific cytokines which promote autoimmune reactions and inflammation in MS. Immunomodulators are used for treating relapsing forms of multiple sclerosis (RRMS and active SPMS), reducing the frequency of relapses and slowing down the accumulation of disabilities.

Immunomodulators prescribed for MS may be biological preparations or synthetic formulations. Each drug works in a unique way to regulate immune activity. All biological medications are administered as injections or infusions, while synthetic drugs may be injections or oral formulations. 

The following are the immunomodulatory drugs approved by FDA for multiple sclerosis:

• Biologic drugs
  • Interferon beta-1b (Betaseron, Extavia)
  • Interferon beta-1a (Avonex, Rebif)
  • Peginterferon beta-1a (Plegridy)
  • Alemtuzumab (Lemtrada) is reserved for relapsing MS that hasn’t responded well to two or more alternate MS drugs 
  • Natalizumab (Tysabri)
  • Ocrelizumab (Ocrevus) for relapsing or primary progressive MS
  • Ofatumumab (Kesimpta)
• Synthetic drugs
  • Glatiramer acetate (Copaxone, Glatopa)
  • Teriflunomide (Aubagio)
  • Dimethyl fumarate (Tecfidera)
  • Monomethyl fumarate (Bafiertam)
  • Diroximel fumarate (Vumerity)

Sphingosine 1-phosphate (S1P) receptor modulators

S1P receptor modulators regulate immune activity by specifically blocking the activity of S1P receptors found on the surface of lymphocytes, a type of immune cell. This prevents the lymphocytes from leaving the lymph nodes and entering the bloodstream, and thus reduces their activity in the central nervous system.

S1P receptor modulators are oral drugs prescribed for RRMS and active SPMS. The following are the FDA-approved S1P receptor modulators:

• Fingolimod hydrochloride (Gilenya)
• Siponimod fumaric acid (Mayzent)
• Ozanimod hydrochloride (Zeposia)

Immunosuppressants

Immunosuppressants suppress immune reactions and are typically used for treating aggressive forms of multiple sclerosis which don’t respond to other drugs. Immunosuppressants may be administered as injections or taken orally. Some of the immunosuppressants are also cancer drugs used off-label for aggressive forms of MS.

FDA-approved:

• Mitoxantrone hydrochloride for worsening RRMS, SPMS, and PRMS
• Cladribine (Mavenclad) for RRMS or active SPMS that hasn’t responded to other medications

Off-label

• Azathioprine (Azasan, Imuran)
• Methotrexate (Trexall, Xatmep, Otrexup, Rasuvo,)
• Cyclophosphamide (Cytoxan)

Symptom management drugs are prescribed to address a wide variety of symptoms caused by the effect of MS lesions on the central nervous system. Medications used for relief from MS symptoms include the following:

Corticosteroids

Corticosteroids are potent anti-inflammatory agents, used to reduce inflammation and speed up recovery from acute relapse episodes. Corticosteroids used for MS relapses include:

• Methylprednisolone (Medrol, Solu-Medrol, Depo-Medrol)
• Dexamethasone (Hemady, Dexamethasone Intensol)
• Prednisone (Deltasone, Rayos)

Dopamine agonists

Dopamine agonists stimulate the release of dopamine, a chemical messenger (neurotransmitter) in the brain. Dopamine plays an important role in regulating many functions such as pleasure, movement, pain processing, and cognition.

Dopamine agonists are FDA-approved medications for Parkinson’s disease, but used off-label to treat fatigue associated with MS. Dopamine agonists prescribed for MS is:

• Amantadine hydrochloride (Osmolex ER, Gocovri)

Skeletal muscle relaxers

Skeletal muscle relaxers are prescribed to treat muscle stiffness (spasticity) caused by my MS. Muscle relaxers used for MS include:

• Baclofen (Lioresal, Gablofen)
• Dantrolene sodium (Dantrium, Revonto, Ryanodex)

Neuromuscular blockers

Neuromuscular blockers temporarily relax spastic muscles by blocking nerve signals that make muscles contract. The FDA-approved neuromuscular blocker used to treat MS-related upper limb spasticity, and urinary incontinence caused by spasticity in the bladder muscle (detrusor) is:

• OnabotulinumtoxinA (Botox)

Alpha-2 adrenergic agonists

Alpha-2 adrenergic agonists work on the central nervous system to inhibit nerve signals that contract muscles. The FDA-approved alpha-2 agonist used to treat muscle spasticity is:

• Tizanidine hydrochloride (Zanaflex)

Potassium channel blockers

Potassium channel blockers improve the strength of the nerve signals transmitted by damaged (demyelinated) axons. Potassium channel blockers may help improve muscle function and walking in MS patients. The FDA-approved potassium channel blocker prescribed for MS is:

• Dalfampridine (Ampyra)

Acetylcholinesterase inhibitors

Acetylcholinesterase inhibitors increase the level of acetylcholine, a neurotransmitter that plays an important role in attention, learning, and memory. Acetylcholinesterase inhibitors are approved by FDA to treat cognitive dysfunction in Alzheimer’s and used off-label in MS to enhance cognition. Acetylcholinesterase inhibitors prescribed for MS include:

• Donepezil hydrochloride (Aricept)

Benzodiazepines

Benzodiazepines are sedative agents used as second-line treatment for MS-related spasticity and sleep disorders. Benzodiazepines have a high risk for addiction and FDA has not specifically approved them for MS. Benzodiazepines prescribed off-label include:

• Clonazepam (Klonopin)
• Diazepam (Valium)

Stimulants

Stimulants increase dopamine levels in the brain and are FDA-approved medications for sleep disorders (narcolepsy). Stimulants have the potential for addiction. Stimulants prescribed off-label for the treatment of fatigue and cognitive dysfunction associated with MS include:

• Modafinil (Provigil)
• Armodafinil (Nuvigil)
• Methylphenidate hydrochloride (Concerta, Ritalin, Methylin)
• Dextroamphetamine sulfate (Dexedrine)

Anticonvulsants

Anticonvulsants are anti-seizure medications that inhibit the hyperactivity of neurons in the brain. Anticonvulsants are used off-label for MS to treat neuropathic pain, tremors, muscle spasticity, and spasms. Anticonvulsants include:

• Gabapentin (Neurontin, Gralise)
• Carbamazepine (Tegretol, Epitol, Carbatrol)
• Pregabalin (Lyrica)
• Topiramate (Topamax, Qudexy XR, Trokendi XR)
• Phenytoin sodium (Dilantin, Phenytek)

Selective serotonin-norepinephrine reuptake inhibitors (SNRIs)

SNRIs work by increasing the level of serotonin and norepinephrine, two important neurotransmitters that regulate mood. SNRIs are approved by FDA to treat depression and several types of pain syndromes. Commonly prescribed SNRIs treat pain and depression associated with MS is:

• Duloxetine hydrochloride (Cymbalta)

Nonsteroidal anti-inflammatory drugs (NSAIDs)

NSAIDs control inflammation by blocking the production of inflammatory substances in the body. Common NSAIDs prescribed to treat pain and inflammation in MS include:

• Ibuprofen (Motrin, Advil, Caldolor)
• Naproxen sodium (Naprosyn, Aleve, Anaprox DS)
• Diclofenac potassium (Cambia, Zipsor)
• Indomethacin (Indocin)

Antispasmodic agents

Antispasmodic agents reduce muscle spasms in the bladder and are used to treat MS symptoms such as urinary urgency and incontinence. FDA-approved antispasmodic agents include:

• Tolterodine tartrate (Detrol)
• Oxybutynin chloride (Ditropan XL, Gelnique, Oxytrol)

Laxatives

Laxatives and stool softeners are over-the-counter medications to treat constipation. Laxatives used to relieve constipation associated with MS include:

• Docusate sodium (Colace, Silace)
• Psyllium (Konsyl Fiber, Metamucil MultiHealth Fiber)
• Methylcellulose (Citrucel)

Antidiarrheals

Antidiarrheals help control diarrhea by slowing down the muscles of the bowel. Diarrhea isn’t a typical symptom of MS but may occur due to the impaction of stools or overuse of stool softeners and laxatives. Antidiarrheal medication commonly prescribed for diarrhea is:

• Diphenoxylate/atropine (Lomotil)

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• Never stop taking your medication and never change your dose or frequency without consulting with your doctor.