Drugs for RA Management

Mechanism of Pharmacokinetic Adverse Effects Contraindications

Drug Class Examples Uses Drug Interactions (DI)
Action s (PK) (A/E) (CI)

Blood dyscrasias
Renal & hepatic NSAIDs & Probenecid ↓ renal
Inhibits AICAR- clearance; Avoid live vaccines.
Transformylase, disease
Oral, Weekly First-line Herpes/ varicella
Inhibits Phenytoin,
dose; Excreted DMARD for infections
adenosine Hepatotoxicity, trimethoprim/sulphamethoxazole,
Methotrexate unchanged via RA; Slows Pregnancy /
Methotrexate deaminase Mucosal ulcers, triamterene->
(MTX) kidneys. disease lactation
Increase Nephropathy additive antifolate effect
progressio Elderly - liver and
adenosine NB ! Folic Acid Anticoagulants -> decrease
n. renal impairment
A2A receptor clotting factor synthesis
signalling (caution)

Immune Onset: 4-6 Retinal disease

Ocular toxicity
modulator weeks; If Mild RA, Monitor: FBCs,
Chloroquine Chloroquine (monitor vision),
(exact MOA effective → Lupus renal function, liver
QT prolongation
unknown). long-term use. function

Inhibits GIT, stomatitis,

dihydroorotate hypertension
Pregnancy (2-year
dehydrogenase, Increase liver
T½ = 14 days, washout required),
blocking enzymes,
Leflunomide Leflunomide Highly protein- Hypersensitivity,
pyrimidine Rare: hepatotoxic,
bound (>99%) Not for Juvenile RA
synthesis → ↓ SJS
(JRA)
T-cell Anaphylaxis
proliferation. Agranulocytosis

Cleaved in GIT
into
sulfapyridine
RA (often Hepatotoxicity, Extra : Decrease RF
(RA) + 5- Check: FBC,
combined Myelotoxicity, Inhibits T cell response
Sulfasalazine Sulfasalazine aminosalicylic Kidney & Liver
with MTX), Megaloblastic Decrease B cell antibody
acid (IBD) → function.
IBD anemia production
Suppresses IL-
1, IL-6, TNF-α,
B/T-cell activity.

Ciclosporin Ciclosporin Calcineurin - Not first- Nephrotoxicity, Ekstra: Immune function

inhibitor → line for RA Hypertension, Opportunistic infections
Prevents IL-2 Hirsutism
release,
 Mechanism of Pharmacokinetic Adverse Effects Contraindications
Drug Class Examples Uses Drug Interactions (DI)
Action s (PK) (A/E) (CI)

blocking T-cell
activation.

Cytostatic agent
→ Inhibits
purine Hepatotoxicity,
Rarely
Azathioprine Azathioprine synthesis, - Myelotoxicity, GI
used in RA
reducing upset
immune cell
proliferation.

Auronafin(oral), IM:Hypersensitivit
Rarely
Sodium Immune y, Nephritis,
Gold Salts IM 50 mg/week used for
aurothiomalate(I modulator Fibrosing
RA
V) alveolitis

Chelating agent, Rarely

Penicillamine Penicillamine immune - used for Severe toxicity .
modulation RA

Inhibits PDE4,
Psoriatic
increasing URI infections, Depression history,
Phosphodiesterase Oral arthritis (in
Apremilast cAMP, blocking N,V &D , Galactose
4 (PDE4) Inhibitor administration combo with
TNF-α, IL-12, insomnia, fatigue intolerance
DMARDs)
IL-17.

RA Ekstra: suppress the effects of

Inhibit JAK- (alternative cytokines by inhibiting signal
↑ LDL, ↑ Infection
STAT pathway, to biologics Active TB, transducer and activator
Janus Kinase Tofacitinib, Used alone or risk, DVT/PE
blocking or MTX Pregnancy, of transcription (STAT)-
(JAK) Inhibitors Baricitinib with MTX (rare), Herpes
cytokine failure) Lactation mediated
Super infection
signaling. ulcerative other downstream
colitis signalling pathways

Infusion reactions,
RA (often
Infliximab given ↑ Infection risk
TNF-α Inhibitors Infliximab + MTX combined
with MTX (TB,
with MTX)
histoplasmosis)

Etanercept Anti- TNF–α Infections Fusion protein

Injection site Used before McABs
Not McAB: reactions
fusion protein Demyelinating
Ligand binding neurologic
 Mechanism of Pharmacokinetic Adverse Effects Contraindications
Drug Class Examples Uses Drug Interactions (DI)
Action s (PK) (A/E) (CI)

portion of
TNF–α receptor
on IgG frame
disease
Binds circulating
and receptor
bound TNF–α

Infusion rxn
Anti-TNF–α Infusion rxn Fever
monoclonal RA, Fever Urticaria
Infliximab, antibodiesBinds Chron’s Urticaria Hypotension
Adalimumab, to circulating disease Hypotension Dyspnoea
Golimumab TNF–α Combine Dyspnoea Infections: UTI,
Binds receptor with MTX Infections: UTI, URTI
bound TNF-α URTI

Ekstra : Chimeric monoclonal Ab

T½ = 22 days
Targets CD20 Active infections, to CD20
Severe infusion Severe infusion
on B-cells, RA, B-cell Severe marker on B-cells
B-cell Inhibitors Rituximab toxicity toxicity, Hepatitis
leading to B-cell lymphomas immunosuppressio Cause depletion of circulating B–
-Antihistamines B reactivation
depletion. n cells by ADCC, CDC, Apoptosis
- Slow infusion
Reduce RF, ACPA .
↑LDL+
Blocks IL-6 Cholesterol,
RA,
IL-6 Receptor receptor, Neutropenia, Active infections, ↑ Hepatotoxicity with MTX, ↑
Tocilizumab - Juvenile
Inhibitors reducing Infection risk, Liver disease Cholesterol with statins.
RA (>2 yrs)
inflammation. Decrease
platelets

Blocks CD28
RA
T-cell Co- binding to Slower onset
(alternative Infusion reactions, Ekstra: Fewer infections than
Stimulation Abatacept CD80/86 (B7) than anti-TNFα Active infections
to TNF-α Infection risk infliximab
Blockers → Prevents T- antibodies
inhibitors)
cell activation.