Medical Pharmacology: Immunopharmacology (Immunosuppressants/Immunomodulators) Practice Questions
Certolizumab pegol (Cimzia)
Click on the correct answer.
Certolizumab pegol (Cimzia):
TNF antagonist: recombinant, humanized antibody Fab' fragment exhibiting specificity for TNF-α coupled polyetheleneglycol.
Certolizumab pegol is likely the only pegylated anti-TNF-α agent approved for treating rheumatoid arthritis and Crohn's disease.
Both
Neither
Concerning certolizumab pegol:
Pegylation of the Fab' fragment promotes sustained activity.
Exhibits effects that are both fast and lasting on signs and symptoms of certain immunological diseases as well as inhibiting joint damage and overall enhancing physical function.
Clinical use/uses of certolizumab pegol:
Adults with Crohn's disease
Rheumatoid arthritis
Active psoriatic arthritis
Active ankylosing spondylitis
All of the above
Certolizumab pegol (Cimzia) may be used in treating rheumatoid arthritis (RA) given that:
TNF-α represents an important, "key" mediator of inflammation-induced joint pathology, representing the central feature in RA.
Reduction in TNF-α levels results in the reduction in RA signs and symptoms. These results also apply to Crohn's disease.
Both
Either
Because TNF-α inhibitors rely on the same primary mechanism of action, responses to drugs belonging to this class are consistent patient to patient.
True
False
Certolizumab pharmacokinetics:
Subcutaneous route of administration.
Half-life of about two weeks
Both
Neither
The likelihood of anti-certolizumab antibodies developing during treatment is reduced by methotrexate.
True
False
Certolizumab exhibits either no or very limited placental transfer from mother to fetus; accordingly, this agent appears to be a good TNF inhibitor for use during pregnancy.
True
False
Given that prolonged administration of certolizumab pegol may result in the reduction in response over time, suggests that other drugs may be required such as:
TNF-α-receptor fusion protein (e.g. etanercept). This agent fuses the TNF receptor to the "constant" end of the IgG1 antibody.
Other anti-TNF-α monoclonal antibodies (e.g.infleximab, adalimumab, golimumab)
Abatacept (Orencia): T-cell signaling antagonist
Rituximab (Rituxan): the cell depleting drug; anti-CD20 antibody)
Certolizumab pegol is different from other TNF-α blockers given that it lacks an Fc region and therefore limits potential Fc-mediated adverse effects including "complement-dependent cytotoxicity or antibody-dependent cell-mediated cytotoxicity".
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Source Material:
Rothlin C Gutkind J Chapter 39
Immunosuppressants, Immunomodulation and Tolerance In
Goodman & Gilman's The Pharmacological Basis of Therapeutics
(Brunton LL Knollman BC eds) McGraw Hill LLC (2023).
Lake D & Briggs A Ch 55 Immunopharmacology
in Katzung's Basic & Clinical Pharmacology (Vanderah TW, ed)
16e McGraw Hill 2023.
Chrouos G Ch 39 Adrenocorticosteroids &
Adrenocortical Antagonists in Katzung's Basic & Clinical
Pharmacology (Vanderah TW, ed) 16e McGraw Hill 2023
Brezinski E Klickstein L Armstrong A Ch 46
Pharmacology of Immunosuppression in Principles of
Pharmacology: The Pathophysiologic Basis of Drug Therapy.
(Golan DE Armstrong EJ Armstrong AW, eds) 4e 2017
Ritter JM Flower R Henderson G Loke YK
MacEwan D Robinson E Fullerton J Ch 25 Anti-inflammatory and
Immunosuppressant Drugs Rang & Dale's Pharmacology 10e
Elsevier 2024.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 72 Immunosuppressants Elsevier 2022.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 75 Glucocorticoids in Nonendrocrine
Disorders Elsevier 2022.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 76 Drug Therapy for Rheumatoid Arthritis
Elsevier 2022.
Bass A Rogatsky Ch 32 Immunomodulatory Drugs
in Goldman-Cecil Medicine (Goldman L Schafer, eds) Elsevier
26e 2020
Leiva M Takemoto Ch 238 Immunosuppressants in
Lippincott Illustrated Reviews: Pharmacology 8e ((Walen et
al, eds) Wolters Kluwer 2023.
Hall J Hall M Ch 78 Adrenocortical
Hormones Guyton and Hall Textbook of Medical Physiology 14e
Elsevier 2021.
Waller DG Sampson A Hitchings Ch 38 The
Immune Response and Immunosuppressant Drugs
Medical Pharmacology & Therapeutics 6e Elsevier 2022
Waller DG Sampson A Hitchings Ch 30
Rheumotoid Arthritis, Other Inflammatory Arthrides and
Osteoarthritis Medical Pharmacology & Therapeutics 6e
Elsevier 2022
