Goal of treatment:
Achieve the lowest possible arthritis disease activity & remission (if possible)
Minimize joint damage
Enhance physical function & quality of life
Suppress inflammation
Correct mechanical and structural abnormalities
Traditional disease modifying anti-rheumatic drugs
1. Methotrexate
2. Azathioprine (Imuran)
3. Cyclosporine (Neoral)
4. Sulfasalazine (Salazopyrin)
5. Chloroquine (Nivaquine)
6. Leflunomide (Azara)
7. Gold salts
, Drug name General PK MoA SEs CI
Drug name General PK MoA SEs CI
Methotrexat Mainstay in severe Orally 1. Anti-inflammatory Mucosal Alcohol use
severe RA (psoriatic) OR Interrupts ulceration and Liver/lung
e
Sulfasalazin not responding to IM adenosine pathway
Unknown nausea
Allergic disease
NSAIDS Rapid OoA Possible effects on Cytopenias (wbc
reactions (Sulfa)
e Alone or combined Benefits in 2- TNF pathways count)
Mild GI
Pregnancy
Myelosuppresion
(Salazopyrin Best 3 weeks 2. Immunosuppressive Liver cirrhosis
complaints
Relatively and toxic effects Interstitial
) inexpensive Due to (-) of folic
Mild cytopenias
pneumositis
(↓ no.
Generally safe acid metabolizing Alopecia
bloodcells)
enzyme “Methotrexate
Hepatotoxicity
Chloroquine Antimalarial drug 3. Inhibits:
Unknown fog”
NB toxicities on
Relatively safe Lymphocyte Birth
the defects
eye
(Nivaquine) Well tolerated proliferation Ophthalmological
Limited to prevent Production of NB examination
regular @
joint damage on its cytokines & bloodwork
baseline and 6-12
own rheumatoid factors ↓SEs with Folic acid
months
Use for mild, non- 4. Interferes with: thereafter
erosive disease Polymorphonuclear
leukocyte
Leflunomide Similar efficacy to Well ↓ chemotaxis
pain and Headache, Pregnancy
Methotrexate absorbed 5. inflammation
↓ cytotoxins and free diarrhea and Women of
(Arava) Alternative to after p.o. radical production
SLOWS progression(↓of nausea child-bearing
Methotrexate > 90% bound damage todamage
structural synovial Other: ↓ potential
intolerant patients to albumin membrane and bone) weight, allergic TERATOGENI
Azothioprine Precautions:
Monotherapy or T8-12
1/2 = weeks
14-18 Loss of appetite
reactions (flu- C
Liver & renal
combined with for effect
days (LONG = Liver problems
like syndrome), In
(Imuran) problems
Methotrexate NB LOADING Nausea,
skin rash,vomiting experimental
Allopurinol/ACE-(-) DOSES) Extreme
alopecia,fatigue
and animals
patients Rapidly hypokalemia
concerted to
Cyclosporine IMMUNOSUPPRESIV the (+) High BP
E drug metabolite Renal
(Neoral) Excreted in insufficiency
the urine & Infection
the feces Hirsutism
Metabolite
undergoes
biliary
recycling
Achieve the lowest possible arthritis disease activity & remission (if possible)
Minimize joint damage
Enhance physical function & quality of life
Suppress inflammation
Correct mechanical and structural abnormalities
Traditional disease modifying anti-rheumatic drugs
1. Methotrexate
2. Azathioprine (Imuran)
3. Cyclosporine (Neoral)
4. Sulfasalazine (Salazopyrin)
5. Chloroquine (Nivaquine)
6. Leflunomide (Azara)
7. Gold salts
, Drug name General PK MoA SEs CI
Drug name General PK MoA SEs CI
Methotrexat Mainstay in severe Orally 1. Anti-inflammatory Mucosal Alcohol use
severe RA (psoriatic) OR Interrupts ulceration and Liver/lung
e
Sulfasalazin not responding to IM adenosine pathway
Unknown nausea
Allergic disease
NSAIDS Rapid OoA Possible effects on Cytopenias (wbc
reactions (Sulfa)
e Alone or combined Benefits in 2- TNF pathways count)
Mild GI
Pregnancy
Myelosuppresion
(Salazopyrin Best 3 weeks 2. Immunosuppressive Liver cirrhosis
complaints
Relatively and toxic effects Interstitial
) inexpensive Due to (-) of folic
Mild cytopenias
pneumositis
(↓ no.
Generally safe acid metabolizing Alopecia
bloodcells)
enzyme “Methotrexate
Hepatotoxicity
Chloroquine Antimalarial drug 3. Inhibits:
Unknown fog”
NB toxicities on
Relatively safe Lymphocyte Birth
the defects
eye
(Nivaquine) Well tolerated proliferation Ophthalmological
Limited to prevent Production of NB examination
regular @
joint damage on its cytokines & bloodwork
baseline and 6-12
own rheumatoid factors ↓SEs with Folic acid
months
Use for mild, non- 4. Interferes with: thereafter
erosive disease Polymorphonuclear
leukocyte
Leflunomide Similar efficacy to Well ↓ chemotaxis
pain and Headache, Pregnancy
Methotrexate absorbed 5. inflammation
↓ cytotoxins and free diarrhea and Women of
(Arava) Alternative to after p.o. radical production
SLOWS progression(↓of nausea child-bearing
Methotrexate > 90% bound damage todamage
structural synovial Other: ↓ potential
intolerant patients to albumin membrane and bone) weight, allergic TERATOGENI
Azothioprine Precautions:
Monotherapy or T8-12
1/2 = weeks
14-18 Loss of appetite
reactions (flu- C
Liver & renal
combined with for effect
days (LONG = Liver problems
like syndrome), In
(Imuran) problems
Methotrexate NB LOADING Nausea,
skin rash,vomiting experimental
Allopurinol/ACE-(-) DOSES) Extreme
alopecia,fatigue
and animals
patients Rapidly hypokalemia
concerted to
Cyclosporine IMMUNOSUPPRESIV the (+) High BP
E drug metabolite Renal
(Neoral) Excreted in insufficiency
the urine & Infection
the feces Hirsutism
Metabolite
undergoes
biliary
recycling
