Drugs For Multiple Sclerosis

DRUGS FOR MULTIPLE SCLEROSIS


DRUGS FOR MULTIPLE SCLEROSIS

Multiple sclerosis: An autoimmune disease resulting in neurons demyelination.

Drug

Mechanism

Route & Frequency

Adverse Effects

Interferon-β 1a Down-regulates expression of MHC molecules on antigen presenting cells.

↓ Pro-inflammatory.

↑ regulatory cytokines.

↓ T-cell proliferation

↓ Entry of inflammatory cells in CNS.

Intramuscular (i.m.), once a week. Flu-like symptoms

Altered LFT

Injection site reaction on s.c. route

Formation of neutralizing antibodies

Glatiramer – Resembles myelin basic protein in relapsing-remitting MS.

 

↑ Suppressor

T-Cells

Displace MBP by

binding to MHC

molecules

↓ Pro-inflammatory

↑ regulatory

cytokines

Subcutaneous, thrice a week Injection site reactions

Flushing

Chest tightness

Dyspnea

Palpitations

Anxiety

Lipoatrophy

Natalizumab – Monoclonal antibody against α4 subunit of α4β1 integrin on lymphocytes Prevents lymphocytes from binding to endothelial cells –> Inhibits transfer across

BBB & CNS entry.

 

Intravenous, once a month Progressive multifocal leukoencephalopathy, if used for >2years.
Fingolimod – Sphingosine 1-phosphate receptor modulator.

 

Traps lymphocytes in spleen & lymph nodes (Prevents their

egress) –> decreased CNS entry

Oral, once  aily. Altered LFT 1° heart  lock Bradycardia
Mitoxantrone – Anthracycline anticancer drug Topoisomerase II inhibition Intravenous, once in 3 months Cardiotoxicity

Acute leukemia

Dimethyl fumarate

(approved in UK; unapproved in USA)

Promotes anti-inflammatory

Properties. 

Inhibits pro-inflammatory cytokines.

Oral, twice a day. Progressive multifocal

leukoencephalopathy

Teriflunomide – Active metabolite of leflunomide Dihydroorotate dehydrogenase inhibitor Oral, once daily. Hepatotoxicity
Cladribine – Purine analog anticancer drug Inhibit DNA synthesis & repair Oral, 2 weeks for every year. Immunosuppression Secondary neoplasms Herpes zoster
Dalfampridine – 4-Aminopyridine K+ channel

blocker to improve

weakness in MS

Oral, once daily. Seizures

Features & drugs used:

  • Spasticity – Decreased by baclofen/tizanidine.
  • Gait in multiple sclerosisDalfampridine.
  • Improves fatigueModafinil.
  • Frequency of relapses – Decreased by beta-interferon/glatiramer.
  • Newer drug for relapse – Fingolimod.

Exam Important

DRUGS FOR MULTIPLE SCLEROSIS

  • Main drugs used for treating multiple sclerosis include Interferon-β 1a (DOC), Glatiramer, Natalizumab, Fingolimod, Mitoxantrone, Dimethyl fumarate, Teriflunomide, Cladribine & Dalfampridine.
  • Baclofen & tizanidine reduces spasicity in multiple sclerosis.
  • Dalfampridine helps is useful in cases with abnormal gait in multiple sclerosis.
  • Modafinil improves fatigue in multiple sclerosis patients.
  • Frequency of relapses in multiple sclerosis patient is decreased by beta-interferon/glatiramer.
  • Newer drug approved for relapse in multiple sclerosis patients is Fingolimod.
  • Teriflunomide is an active metabolite of leflunomide.
  • Natalizumab is a monoclonal antibody against α4 subunit of α4β1 integrin on lymphocytes, useful in treating multiple sclerosis.
  • Glatiramer resembles myelin basic protein in relapsing-remitting MS.

 

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