Methotrexate (Trexall and others): clinical use/uses-
Cancer therapy
Autoimmune disease
Ectopic pregnancies
A & B
B & C
A & C
A, B & C
Methotrexate:
Inhibitor of dihydrofolic acid reductase.
Exhibits antiproliferative action due to limiting purine, pyrimidines, and polyamine synthesis.
Both
Neither
Methotrexate is considered first-line treatment for individuals exhibiting early rheumatoid arthritis.
True
False
Methotrexate (Trexall, Rheumatrex):
Effective in treating autoimmune disorders such as psoriasis and rheumatoid arthritis.
Immunosupressant action results from B- and T-lymphocyte suppression due to folate metabolism inhibition.
Both
Neither
Methotrexate doses are higher when the drug is used for cancer therapy then doses used for immunosuppressant action.
True
False
Primary toxicities associated with methotrexate administration:
Methotrexate in the context of immunosuppression treatment: cirrhosis and hepatic fibrosis represent principal toxicities.
Methotrexate in the context of cancer chemotherapy: renal pathology, bone marrow suppression, ulcerative stomatitis.
Both
Neither
Methotrexate:
Dihydrofolate reductase inhibitor; thymidylate synthase inhibitor; competitive inhibitor with folate for dihydrofolate reductase.
Methotrexate decreases tetrahydrofolate (THF) synthesis which reduces purine and pyrimidine synthesis.
Both
Neither
Methotrexate exhibits specificity for the S-cell division phase and also slows G1- to S-phase transition.
True
False
Methotrexate pharmacokinetics:
Good oral absorption from the gut
Other routes of administration include IV, IM (intramuscular) or subcutaneous.
Both
Neither
Methotrexate pharmacokinetics:
Following administration methotrexate is transformed to an active methotrexate polyglutamate derivative, promoting extended drug retention of the cell.
Primary excretion is renal; plasma half-life is about 10 hours.
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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 ls) 4e
2017
Ritter JM Flower R Henderson G Loke YK
MacEwan D Robinson E Fullerton J Ch 54 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.
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 A
Medical Pharmacology & Therapeutics 6e Elsevier 2022
