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Musculoskeletal System > Joint Pain Pharm > Flashcards

Joint Pain Pharm Flashcards

1
Q

What are the 3 drugs used for the treatment of OA?

A

Pain relief/anti-inflammatory
1) Paracetamol
2) NSAIDs (eg. diclofenac, celecoxib)
3) Corticosteroids

Symptomatic slow-acting drugs for OA (SYSADOA)
4) Intra-articular hyaluronic acid

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2
Q

What is the moa of Intra-articular hyaluronic acid used as a SYSADOA?

A

Naturally occurring large glycosaminoglycan
a) shock absorption, traumatic energy dissipation, protective coating of cartilage, lubrication,
→ ↓pain and stiff ness

b) Induces biosynthesis of more hyaluronic acid and ECM

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3
Q

True or false: In addition to paracetamol, NSAIDs, corticosteroids, and HA, OTC supplements such as chondroitin sulphate and glucosamine have been proven to aid in treating osteoarthitis.

A

False.
Inadequate/inconsistent evidence despite being popular as supplements

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4
Q

What are the 3 primary targets of RA treatment?

A

1) Synovial tissues
2) Bone erosion
3) Joint deformity

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5
Q

What are 3 points for approaches to RA therapy?

A

1) Early diagnosis and treatment

2) Synthetic Disease-Modifying Anti-Rheumatic Drug (sDMARD) alone or in combination

3) Add biological DMARD targeted at TNF, IL-1R and IL-6

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6
Q

What are 3 therapeutic goals of RA?

A

1) Remission of joint symptoms
2) Return of full function
3) Maintenance of remission of DMARD therapy

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7
Q

What are 7 drugs used in the treatment of RA?

A

Anti-inflammatory agents:
1) NSAIDs
2) Corticosteroids

Conventional synthetic DMARD
3) Methotrexate
4) Sulfasalazine
5) Leflunomide
6) Hydroxychloroquine
7) Ciclosporin

Targeted synthetic DMARD
8) Tofacitinib/Baricitinib

Biologic DMARD
9) Anti-TNF mAB (eg. infliximab, adalimumab, etanercept)
10) IL-1R antagonist (eg. anakinra)
11) Anti-CTLA4Ig (eg. abatacept)
12) Anti-CD20 (eg. rituximab)
13) Anti-IL-6 receptor mAb (eg. Tocilizumab

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8
Q

What is the first-line choice DMARD therapy for RA?

A

Methotrexate (folic acid analog)

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9
Q

What is the moa of methotrexate in treating RA?

A

Major:
↑adenosine levels due to AICAR transformylase/ATIC inhibition

Minor:
Inhibits dihydrofolate reductase and thymidylate synthetase → ↓purine synthesis

Overall:
i) ↑extracellular adenosine and adenosine A2a receptor activation
ii) Anti-proliferative effect on T cells and inhibition of macrophage functions
iii) ↓pro-inflammatory cytokines, adhesion molecules. chemotaxis and phagocytosis

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10
Q

What are 5 AEs of methotrexate?

A

1) Nausea and vomiting
2) Mouth and GI ulcers
3) Hair thinning
4) Leukopenia
5) Hepatic fibrosis
6) Pneumonitis

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11
Q

How can the side effects of methotrexate (eg. nausea and vomiting) be minimised?

A

Concomitant folic acid or folinic acid given 12-24 hrs after methotrexate

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12
Q

What are the modes of administration of methotrexate?

A

1) Oral
2) SQ
3) IM

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13
Q

What is methotrexate often combined with for optimal effects in treating RA?

A

Other sDMARDs
(eg. hydroxychloroquine, ciclosporin, sulfasalazine, leflunomide)

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14
Q

Which is more effective at rescuing methotrexate toxicity, folate or folinic acid?

A

Folinic acid
- Folate cheaper but effect still limited by inhibition of dihydrofolate reductase inhibition

  • Folininc acid converted to N5, N10-Methylene-FH4 → bypass dihydrofolate reductase activity → more effective at rescuing methotrexate toxicity
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15
Q

How does Sulfasalazine (csDMARD) help in treating RA?

A

Metabolised to sulfapyridine (active) + 5-aminosalicyclic acid →
i) ↓IgA and IgM rheumatoid factors
ii) Suppression of T and B cell and macrophages
iii) ↓inflammatory cytokines

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16
Q

What are 5 AEs in sulfasalazine (csDMARD)?

A

1) Nausea and vomiting
2) Headache
3) Rash
4) Haemolytic anaemia
5) Neutropenia
6) Reversible infertility in men

17
Q

How does Leflunomide (csDMARD) help in treating RA?

A

Converted to teriflunomide (active) → inhibits dihydroorotate dehydrogenase → ↓ pyrimidine synthesis and growth arrest @ G1

i) inhibits T cell proliferation and B cell autoAb production
ii) inhibits NF-kB activation (pro-inflammatory pathway)

18
Q

What are 4 AEs of Leflunomide (csDMARD)?

A

1) Diarrhoea
2) Elevation of liver enzymes
3) Alopecia
4) Weight gain
5) Teratogenic

19
Q

How do chloroquine and hydroxychloroquine (csDMARD) help in treating RA?

A

Anti-inflammatory agents in RA:
i) ↓MHC class II exp. → ↓Ag presentation
ii) ↓TNF and IL-1 and cartilage resorption
iii) Antioxidant activity

20
Q

What are 4 AEs of chloroquine and hydroxychloroquine?

A

1) Nausea and vomiting
2) Stomach pain
3) Dizziness
4) Hair loss
5) Ocular toxicity

21
Q

What are 4 indications of tsDMARDs (JAKnibs) eg. tofacitinib?

A

1) Combined with methotrexate for moderate to severe RA

2) Monotherapy during methotrexate intolerance

3) Methotrexate + multiple bDMARD-refractive active RA

4) Psoriatic arthritis

22
Q

What is the general moa of tsDMARDs (JAKnibs) eg. tofacitinib?

A

JAK pathway inhibitor → blocks cytokine production (via blocking of JAK/STAT-activation of gene transcription)

23
Q

When is tsDMARDs (JAKnibs) eg. tofacitinib absolutely contraindicated for?

A

CANNOT combine with biological DMARDs

24
Q

What are 4 AEs of tsDMARDs (JAKnibs) eg. tofacitinib?

A

1) Cytopenia (eg. neutrophils, platelets, NK cells, Lymphocytes)

2) Immunosuppression (eg. VZV infection)

3) Anaemia (affects JAK2 by EPO)

4) Hyperlipidemia
- ↑total, LDL, HDL cholesterol
- ↑TGs

25
Q

What is the moa of Anakinra in treating RA?

A

Recombinant IL-1R antagonist SQ → block signalling
(less effective than anti-TNF bDMARDS)

26
Q

What are 2 AEs of Anakinra?

A

1) Infections
2) Injection site reaction

27
Q

What is the moa of Tocilizumab in treating RA?

A

Humanised mAb against IL-6R (α-chain) → prevents binding and homodimerisation of IL-6Rß signalling

28
Q

What are 4 AEs of Tocilizumab?

A

1) Infections
2) Skin eruptions
3) Stomatitis
4) Fever
5) Neutropenia
6) ↑ALT/AST
7) HLD
8) ↓CYP450 exp.

29
Q

What is the moa of Abatacept in treating RA?

A

Recombinant fusion protein with CTLA4-FclgG1
i) Binds to CD80 & CD86 → prevents CD28 activation
ii) T cell therapy (IV)

30
Q

What are 2 AEs of Abatacept?

A

1) Respiratory infection in COPD
2) ↑Lymphoma incidence

31
Q

What is the moa of Rituximab in treating RA?

A

Chimeric mAb IgG1 directed at CD20 on pre- and mature B cells →
i) Depletes CD20+ B cells
ii) B cell therapy (IV)
iii) Blocks Ag presentation
iv) ↓AutoAb and cytokines

32
Q

What are 2 AEs of Rituximab?

A

1) Rash in first dose
2) Respiratory infection in COPD

33
Q

What are 2 indications of TNF blockers used in the treatment of RA (eg. Adalimumab, Infliximab, Etanercept)?

A

1) RA px who do not respond well with sDMARD therapies
2) In combination with Methotrexate for optimal effects

34
Q

What are 4 AEs of TNF blockers used in the treatment of RA (eg. Adalimumab, Infliximab, Etanercept)?

A

1) Respiratory and skin infections
2) ↑risk of lymphoma
3) Optic neuritis
4) Exacerbation of multiple sclerosis
5) Leukopenia
6) Aplastic anemia

35
Q

What are 2 contraindications of TNF blockers used in the treatment of RA (eg. Adalimumab, Infliximab, Etanercept)?

A

1) Live vaccination
2) Hep B

36
Q

What should be done for a px undergoing TNF blockers used in the treatment of RA (eg. Adalimumab, Infliximab, Etanercept)?

A

Screen for latent or active TB

37
Q

How are the bDMARDs administered?

A

1) Anakinra (SQ)
2) Tocilizumab (SQ)
3) Abatacept (IV)
4) Rituximab (IV)

TNF signal blockers:
5) Infliximab (IV)
6) Adalimumab (SQ)
7) Golimumab (IV)
8) Etanercept (SQ)

38
Q

What is the moa of Etanercept (bDMARD)?

A

TNF signal blocker:
Decoy TNFR2 receptor-IgG1 fusion protein intercepts TNF

39
Q

Given that Leflunomide is teratogenic yet has a very long T1/2 (detectable even years after last dosing), what is given to “wash-out” the leflunomide in pregnant women?

A

Colestyramine

Musculoskeletal System (22 decks)

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