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Drug Action III > MS (MC) - Block 1 > Flashcards

MS (MC) - Block 1 Flashcards

1
Q

What are the tx options for acute exacerbations?

A

Start with corticosteroids
Mild: Oral prednisone or prednisolone
Severe, acute: IV methylprednisolone (Solu-Medrol)

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2
Q

MOA of steroids?

A

Inhibit leukocyte infiltration at site of inflammation, interfere with mediators of inflammatory responses and suppress humoral immune responses
* Reduce edema in area of demyelination
* Reduce BBB abnormalities and reduce CSF IgG synthesis

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3
Q

What are the adrs for Steroids?

A
  1. Cushing’s syndrome (chronic use)
  2. GI distress
  3. Impaired skin healing
  4. Hypertension
  5. Adrenal insufficiency
  6. Hyperglycemia, steroid diabetes
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4
Q

What are the cautions of long term steroid use?

A

Not used for prevention (or disease modifying therapy)

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5
Q

Are disease modifying therapies a cure for MS?

A

Not a cure still prone to relapse and progressive damage

All are immunomodulating agents

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6
Q

What are ABC therapies?

A

β-interferons and copaxone (ABCs of MS therapy):
* Home injectable treatments for relapsing-remitting MS (RRMS)
* likely shift from Th1 (pro-inflammatory) to Th2 (anti-inflammatory) cytokine profile

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6
Q

Interferon β-1b

Brand, Structure, MOA, ADR, Monitor, stabilizer

A

Betaseron, Extavia
Structure: 165 amino acid analog of human Interferon-β
* Cys17 -> Ser
* Also not glycosylated
* Produced in recombinant E.coli

MOA:
* Decreased expression of pro-inflammatory cytokines
* Decreases expression of class II MHC antigens
* Inhibition of helper T-cells

ADR: Inj site rednness and swelling, flu-like sx
* Therapy may cause patients to feel worse initially -> Can apply ice before and after to injection site to decrease redness/pain
* NSAIDs at regular intervals for 24 hrs after administration may help with flu-like symptoms

Moniotr:
* CBC, platelets, LFTs 1,3, 6 months
* THyroid function preiodically

Stabilizer: dextrose and albumin

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7
Q

Interferon β-1a

Brand, Structure, Stabilizers, ADR, Dosing, Monitoring

A

Avonex, Rebif
Structure: Same amino acid sequence as human IFN-β
Stabilizer: Albumin, sodium chloride and phosphate buffer (do not shake)
ADR: Inj site rednness and swelling, flu-like sx
Dosing:
* Avonex: QW IM
* Rebif: 3W SC

Monitoring: Hb, liver and thyroid function, blood chemistries

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8
Q

Plegridy

MOA

A

Pegylated interferon β-1a: PEG is attached to interferon -> longer duration SQ 2W

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9
Q

Glatiramer Acetate

Brand, MOA, Indication

A

Copaxone
MOA: Mix of synthetic polypeptides that modifies immune processes responsible for MS (TH1 to TH2 shift)
* Might also serve as decoy to locally generated auto-antibodies

Indication: Decreases frequency of attacks and severity of disability in RRMS (minimal disabilitiy)

ADR: generally well tolerated, inj site reaction
* Immediate post inj rx: facial flushing, chest pain, dyspnea, throat constriction, palpitations, anxiety (Usually benign and self-limiting)

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10
Q

Glatiramer Acetate Injection

Brand

A

Glatopa: generic equialent to Copaxone

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11
Q

Describe the number of inj for ABCs?

A
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12
Q

What is an examples of home injectable therapy?

A

Ofatumumab (Kesimpta)

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13
Q

Ofatumumab

Brand, MOA

A

Kesimpta
MOA: Fully human 149 kDa IgG1κ anti-CD20 Mab
* Binds to CD20 on B–cells -> B-cell lysis

ADR: Upper respiratory tract infections, inj-related rx
* Progressive multifocal leukoencephalopathy (PML), Hepatitis B virus (HBV) reactivation

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14
Q

What are the benefits of oral MS tx?

A

Increased adherence and easier admin

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15
Q

Describe the MOA of Sphingosine 1-phosphate (S1P) receptor modulator?

A

Causes internalization of receptor:
* Blocks release of lymphocytes from lymph nodes and thymus, reducing number in the blood
* Prevents activated and autoreactive cells from migrating to the CNS

16
Q

What are the S1P receptor modulators?

A
  1. Fingolimod
  2. Siponimod
  3. Ozanimod
  4. Ponesimod
17
Q

S1P Receptor Modulators

ADR, Metabolism

A

ADR: HA, high BP, abnormal liver tests, increased infection
Metabolsim: CYP450s
* Siponomod – contraindicated in patients with CYP2C93/3 genotype (may require reduced dosing)

18
Q

What are cardiac effects of S1P receptor modulators?

A

Bradycardia, prolongation of QT interval
* Requires cardiac monitoring for 6 hours after first dose
* Contraindicated in patients with cardiac conditions

19
Q

Terflunomide

MOA, ADR

A

MOA: Inhibits dihydroorotate dehydrogenase (enzyme in pyrimidine synthesis) -> inhibits T-cell and B-cell division
* Decrease in number of activated lymphocytes in CNS
* active metabolite of leflunomide

ADR: elevation of liver enzymes, reduced WBC, teratogenic
* May be up to 2 years before plasma levels decrease to sufficient amount

20
Q

Cladribine

MOA, ADR

A

MOA: Purine nucleoside analog prodrug – activated by deoxycytidine kinase
* Causes failure of DNA damage repair
* High levels of deoxycytidine kinase in T-cells and B-cells
* Reduces levels of pro-inflammatory chemokines

ADR: upper respiratory tract infection, lymphopenia, malignancy
CI: Patients who have reproductive potential with no effective contraception

21
Q

Dimethyl fumarate

MOA, ADR

A

MOA: Prodrug converted to monomethyl fumarate
* May activate nuclear factor (erythroid-derived 2)-like 2 (NRF-2) transcriptional pathway that reduces oxidative stress from demylination and anti-inflammatory

ADR: flushing, lymphopenia, N, diarrhea

22
Q

What is the active fumarate metabolite?

A

Monomethyl Fumarate

23
Q

What are the fumarates>

A
  1. Dimethyl Fumarate
  2. Monomethyl Fumarate
  3. Diroximel Fumarate
24
Q

What is the difference betwen monomethyl and diroximel fumarate?

A

Diroximel fumarate = delayed-release oral capsules and metabolized to mono

25
Q

MOA of Natalizumab

A

Humanized IgG4 monoclonal antibody binds to a4-subunit of a4b1 and a4b7 integrins expressed on leukocyte surface
* Inhibits α4-mediated adhesion of leukocytes to cognate receptor
* Blocks entry into brain

26
Q

Natalizumab

ADR

A
  1. Increases risk of progressive multifocal leukoencephalopathy (PML)
  2. Risk includes having antibodies to John Cunningham Virus (JCV)
27
Q

What are the sx of PML?

A
  1. Personality changes
  2. Changes in thinking and memory
  3. Onset of seizures
  4. Disturbances in vision
28
Q

Alemtuzumab

MOA, DOsing, ADR

A

MOA: rDNA-derived humanized IgG1κ mAB specific for CD52
* Depletes autoimmune inflammatory T and B cells

Dosing: Round 1 – one infusion/day on 5 consecutive days
* Round 2 (1 year later and following years) – one infusion/day on 3 consecutive days

ADR: Infusion rx, Graves
* Patients become lymphopenic so monitor for opportunisitc infections and hematologic tox

29
Q

Ocrelizumab

MOA, Monitoring, ADR

A

Humanized IgG Mab targeting CD20 on B lymphocytes
Monitoring: B-cell depletion can increase risk of infections
* If patients become hypogammaglobulinemic -> immunoglobulin replacement therapy

ADR: infusion rx, increases risk of cancer

30
Q

What is the MOA of chemotherapeutic agents?

A

Myelin damage caused by autoimmune response -> chemo can shorten attacks and slow progression by suppressing the immune system

31
Q

Mitoxantrone

MOA, ADR, BBW

A

MOA: Suppressed activity of T-cells, B-cells and macrophages
ADR: Serious side effects (last resort drugs)
* N, alopecia, menstrual dx, infections

BBW: leukemia, arrhythmias, cardiotox and CHF, hepatotox, and renal tox

32
Q

What are considered first line chemo drugs (characterisitcs)?

A

Less potent and burden of tx

33
Q

Summary of MS drugs?

A
34
Q

What is the tx for spasticity?

A

Requires pharm but should avoid CNS muscle relaxants

35
Q
A
36
Q

What are the med for spaciticty?

A

Baclofen and dalfampridine

37
Q

Baclofen

MOA, ADR, Counseling

A

MOA: GABAB receptor agonist
* Inhibit presynaptic neurons – reduce Ca2+ influx and hyperpolarizing the cell via K+ efflux
* Suppresses excitability by reducing calcium persistent inward currents in spinal motor neurons

ADR: sedation, n, vertigo
Conseling: withdrawl can occur
* If abruptly discontinue can cause seizures, anxiety, tachycardia, hallucinations, increased spasticity

38
Q

Dalfampridine

Indication, MOA, CI

A

Indication: manages walking impairment
MOA: K+ channel blocker
CI: Hx of seizures, moderate-severe renal impairment

Drug Action III (23 decks)

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