Disease ModifyingAnti-
Rheumatic Drugs
(DMARDs)
Kalsoom Saleem
CMS # 8107
Bones
 Articular cartilage-joins two bones
 Acting as shock absorber
 Continuously subjected to wear and tear caused by stress on
bones
National Institute of Arthritis and Musculoskeletal and Skin Diseases Information Clearinghouse
The Arthritis Foundationwww.arthritis.org
Rheumatoid
Arthritis
 Autoimmune disease
 Causes systemic effects, shortens life and reduces mobility
 Etiology:
 Unknown
 Genetics
 Environmental factors
 Infection
 Autoimmunity
 Signs and Symptoms:
 Joint inflammation
 Pain and stiffness
 Fatigue, fever
National Institute of Arthritis and Musculoskeletal and Skin Diseases Information Clearinghouse
The Arthritis Foundationwww.arthritis.org
Treatment
Goals
Relieve pain
Reduce inflammation
Slow joint damage
Improve functioning
National Institute of Arthritis and Musculoskeletal and Skin Diseases Information Clearinghouse
The Arthritis Foundationwww.arthritis.org
Drug
Treatment
• COX-selective
• COX-non-
selective
NSAIDs
• Biologics
• Synthetic
DMARDs
• Cortisone
• Hydrocortisone
Corticosteroids
• Paracetamol
Another
analgesic
National Institute of Arthritis and Musculoskeletal and Skin Diseases Information Clearinghouse
The Arthritis Foundationwww.arthritis.org
Classification
Synthetic
Abatacept
Azothioprine
Choloroquine &
Hydrocholoroquine
Methotrexate
Sulfasalazine
National Arthritis Action Plan: A Public Health Strategy,
Centers for Disease Control and Prevention, National Center for Chronic Disease Prevention and Health Promotion
Abatacept
Pharmacokin-
etics
Monotherapy
or
combination
therapy
60-100= 750
mg
>60 Kg=500
mg IV
3 doses-IV (1
day, 2 week, 4
week)
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 642
Adverse
Effects
Hypersensitivity
Lymphomas
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical PharmacologyCh. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 642
Azithioprine
MOA
TPMT-Liver
6-thioguanine
Disturbs
function of IL-
1,2, B &T-cells
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill
Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs, Antirheumatic
Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg
Pharmacokin-
etics
Drugs rapidly
metabolized and
cleared from blood
Patient deficient
inTMPT-suffer
myelosuppression
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 642
Adverse
effects
Bone
marrow
depression
Alopecia
GI
disturbances
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 642
Chloroquine &
hydroxychloro
quine-
MOA
Unclear
Depression ofT-lymphocytes
Inhibition of DNA/RNA synthesis
Trapping of free radicalsBertram G.Katzung, Susan B.Masters, Anthony J.Trevor,
McGrawHill Publications, Basic and clinical Pharmacology, Ch.
36, NSAIDs,Antirheumatic Drugs, Nonopioid AnelgesicsAnd
th
Pharmacokin-
etics
Well absorbed
50% protein binding
Half-life = 45 days
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 642
Adverse
effects
Ocular
toxicity
Abdominal
pain
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology,Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 643
Biologics-
TNF--
blocking
agents
Adalimumab Eternacept Certolizumab Golimumab Infliximab
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 643
Adalimumab
Pharmacokin-
etics
Used SC
Half-life=10-20 days
Dose = 40-60 mg
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 643
Adverse
Effects
Opportunistic
infections
Leukopenia
Skin
infections
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 643
Eternacept
Pharmacokin-
etics
SC
25 mg
twice/week
Half-life =
4.5 days
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 644
Adverse
Effects
Adverse Effects
Juvenile
Arthritis
Psoriasis
Systemic
Lupus
Erthymatosus
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 644
Certolizumab-
MOA
Pharmacokin-
etics
Half-life = 14 days
Clearance decreases with decrease in
body weight
Dose = 400 mg initially followed by 200
mg every 2nd week.
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 645
Adverse
effects
Opportunistic infections
Fungal
infections
Bacterial infections
Tuberculosis
Bertram G.Katzung, Susan B.Masters, Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch. 36, NSAIDs,
Antirheumatic Drugs, Nonopioid Anelgesics And Drugs Used toTreat Gout, 12th Ed., 2012, pg 646
B-cell Blocking
agents
Rituxan, Rituximab, Genentech USA, 2013. http://www.rituxanforra.com/patient/considering-treatment/anti-tnfs
Rituximab
Pharmacokin-
etics
IV
Dose = 1000 mg
Duration = 2 weeks for 6-9 months
Bertram G.Katzung, Susan B.Masters,Anthony J.Trevor, McGrawHill Publications, Basic and clinical Pharmacology, Ch.
36, NSAIDs,Antirheumatic Drugs, NonopioidAnelgesicsAnd Drugs Used toTreat Gout, 12th Ed., 2012, pg 646
Adverse
Effects
Flu
Rituxan, Rituximab, Genentech USA, 2013. http://www.rituxanforra.com/patient/considering-treatment/anti-tnfs
DMARDs

DMARDs