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 sclerosis – Dalfampridine.
- Improves fatigue – Modafinil.
- 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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