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Pharmacology > Immunosuppresants + Antirheumatoid > Flashcards

Immunosuppresants + Antirheumatoid Flashcards

1
Q

What are the treatment goals of rheumatoid arthritis

A

Early use of DMARDs
Use of combination of drugs
Avoid long term use of corticosteroids

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2
Q

What are DMARDs

What is their role in RA management

A

Disease modifying anti rheumatic drugs

Prevent disease progression by inhibiting chronic inflammation

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3
Q

What are the types of DMARDs used

A

Methotrexate
Sulfasalazine
Leflunomide
Hydroxychloroquine

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4
Q

What are indications of methotrexate

A

RA: agent of choice
Chemotherapy (it is a cancer drug)
Psoriasis
IBD

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5
Q

What is the mechanism of action of methotrexate for cancer treatment

A

Inhibit dihydrofolate reductase
Inhibit purine and pyrimidine synthesis
Inhibit DNA synthesis
Cytotoxic to rapidly dividing cells

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6
Q

What is the mechanism of action of methotrexate for non-chemotherapy use

A

Inhibit other enzymes of purine metabolism
Adenosine accumulates
Adenosine binds to gp GPCR on inflammatory cells
Inhibit T cell activation
Suppress intercellular adhesion molecule expression by T cells

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7
Q

What are PK properties of methotrexate

A 
Oral bioavailability 33%
IM bioavailability 76%
Admin: oral, IM, SC
High protein binding 50%
Hepatic metabolism 
Renal excretion 
Long T1/2
WEEKLY dosing
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8
Q

What are side effects of methotrexate

A 
Mucositis
Myelosupression 
Cirrhosis 
Pneumonitis
Pulmonary fibrosis 
Teratogenicity + abortifacient
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9
Q

What effect do PK properties have on methotrexate use

A

Switch to IM admin if poor response with oral
Weekly dosing due to long T1/2
DIs with NSAIDs

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10
Q

What are the prescribing rules of methotrexate

A

Weekly dosing
Toxicity monitoring: U+Es, LFT, FBC - Baseline, weekly, then 3monthly
FY1 not licensed to prescribe chemotoxic agents
Folic acid should be co-prescribed
Use contraception during treatment
Avoid pregnancy 3 months after stopping treatment

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11
Q

What are indications for sulfasalazine

A

RA

IBD

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12
Q

What is mechanism of action of sulfasalazine

A

A prodrug that is broken down in large intestine into 5-ASA (active component) and sulfapyridine
5-ASA inhibits T cell proliferation, IL-2 production, causes T cell apoptosis
Sulfapyridine causes SEs

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13
Q

What are side effects of sulfasalazine

A 
N+V
Rash
Heinz body anaemia
Megaloblastic anaemia 
Myelosupression
Oligospermia
Pneumonitis
Hepatitis 
Stevens Johnson syndrome
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14
Q

What are the prescribing rules for sulfasalazine

A

No toxicity monitoring required:
Safe in pregnancy
Not carcinogenic

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15
Q

What are the cautions for sulfasalazine

A

G6PD deficiency: drug can be a trigger for haemolytic anaemia
Aspirin allergy: cross sensitivity

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16
Q

What biological therapies are used in RA management

A

TNF inhibitors: infliximab, etanercept

Rituximab

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17
Q

What are indications for TNF inhibitors

A

RA: at least 2 DMARDs tried
IBD
Psoriasis

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18
Q

What is mechanism of action of TNF inhibitors

A

Monoclonal antibody that blocks TNF alpha
Reduce inflammation - reduce leukocyte recruitment to joint
Reduce angiogenesis - reduced VEGF
Reduce joint destruction - reduced MMP

19
Q

What are side effects of TNF inhibitors

A

TB reactivation: TNF alpha released by macrophages for granuloma formation and maintenance of infection

20
Q

What are prescribing rules for TNF alpha inhibitors

A

Screen for and treat latent TB before starting treatment

21
Q

What are indications for rituximab

A

RA
SLE
Vasculitis

22
Q

What is mechanism of action of rituximab

A

Monoclonal antibody that causes B cell depletion

Bind to CD20 and cause B cell apoptosis

23
Q

What are indications of cyclophosphamide

A

Lupus nephritis
ANCA vasculitis
Chemotherapy: solid, leukaemia, lymphoma

24
Q

What is mechanism of action of cyclophosphamide

A

Inhibit DNA replication by Cross linking DNA

Suppresses rapidly dividing cells, T cells, B cells

25
Q

What are the PK properties of cyclophosphamide

A

Prodrug: 4HCP is active metabolite
Hepatic metabolism by CYP450 enzymes
Renal excretion

26
Q

What are side effects of cyclophosphamide

A

Risk of malignancy: bladder, leukaemia, lymphoma
Infertility
Haemorhagic cystitis

27
Q

Why do you get haemorrhagic cystitis with cyclophosphamide

A

Acrolein is a metabolite toxic to bladder epithelium

28
Q

What are prescribing rules with cyclophosphamide

A

Monitor FBC and renal function

29
Q

What is mechanism of action of corticosteroids

A

Inhibit production of pro-inflammatory cytokines: IL-1, IL-2
Inhibit proliferation of Th1 and Th2 cells
By acting on intracellular glucocorticoid receptor to inhibit gene transcription

30
Q

What are indications for azathioprine

A 
Organ transplantation
SLE
Vasculitis 
IBD
Atopic dermatitis
31
Q

What is mechanism of action of azathioprine

A

Prodrug metabolised by TPMP enzyme
To 6MP then to antimetabolite
Inhibits purine synthesis
Inhibit DNA synthesis

32
Q

What are PD properties of azathioprine

A

TPMP enzyme is polymorphic
Low expression causes increased myelosupression risk
High expression causes risk of under-treatment

33
Q

What are prescribing rules for azathioprine

A

TPMP testing: identify patients prone to azathioprine toxicity
Monitor LFT, FBC

34
Q

What are side effects of azathioprine

A 
Myelosupression
Neutropenia
Pancytopenia 
Increased risk of infection
Increased risk of malignancy 
Hepatitis
Pancreatitis
35
Q

What are indications for calcineurin inhibitors

A

Transplantation
Atopic dermatitis
Psoriasis

36
Q

What are types of calcineurin inhibitors

A

Ciclosporin

Tacrolimus

37
Q

What is mechanism of action of calcineurin inhibitors

A

Inhibit calcineurin by binding to + forming complex with cyclophilin protein
Drug-cyclophilin complex binds to calcineurin
Calcineurin is a phosphatase in T cells involved in IL-2 synthesis
Inhibit IL-2 synthesis (thus Th1 mediated response)

38
Q

What are side effects of calcineurin inhibitors

A 
Nephrotoxicity 
Hypertension  
Hepatotoxicity
Hyperlipidaemia
N+V
39
Q

What are prescribing rules of calcineurin inhibitors

A

Monitor BP and renal function

40
Q

What are drug interactions of calcineurin inhibitors

A

CYP450 inducers/inhibitors

41
Q

What are indications of mycophenolate mofetil

A

Transplantation

42
Q

What is mechanism of action of Mycophenolate mofetil

A

Prodrug converted to mycophenolic acid
MPA inhibits inosine monophosphate dehydrogenase
IMD inhibits purine synthesis
Selective inhibition of B + T cell proliferation
(Sparing of other rapidly dividing cells)

43
Q

What are side effects of mycophenolate mofetil

A 
N+V
Peptic ulcers
Myelosupression
Neutropenia
Increased infection risk

Pharmacology (19 decks)

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