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Immunosuppressant Drugs

#BasicPharmacology

Drug Action and Characteristics for Step 1

DrugActionMechanism CategoryClass of ImmunosuppressantPossible Side EffectsDistinguishing Factor of Side EffectPossible Use CasesAdditional Information for Step 1
GlucocorticoidsRegulate gene expressionGene RegulationSteroidWeight gain, osteoporosisOsteoporosisAsthma, autoimmune diseasesCushing's syndrome risk
CyclosporineInhibits calcineurin phosphatase activityEnzyme InhibitionCalcineurin InhibitorKidney dysfunction, hypertensionKidney dysfunctionOrgan transplantationGingival hyperplasia
TacrolimusInhibits calcineurin phosphatase activityEnzyme InhibitionCalcineurin InhibitorKidney dysfunction, diabetesDiabetesOrgan transplantationLess nephrotoxic than Cyclosporine
SirolimusInhibits mTOR kinase activity; blocks T cell proliferationEnzyme InhibitionmTOR InhibitorHyperlipidemia, anemiaHyperlipidemiaKidney transplantationNot nephrotoxic
AzathioprineInhibits DNA synthesisDNA Synthesis InhibitionAntimetaboliteBone marrow suppression, liver toxicityLiver toxicityRheumatoid arthritisProdrug of 6-mercaptopurine
MethotrexateInhibits AICAR transformylase; anti-inflammatoryEnzyme InhibitionAntimetaboliteLiver toxicity, folic acid deficiencyFolic acid deficiencyCancer, rheumatoid arthritisFolinic acid as rescue therapy
Mycophenolate mofetilInhibits Inosine monophosphate dehydrogenaseEnzyme InhibitionAntimetaboliteDiarrhea, leukopeniaLeukopeniaOrgan transplantationSelective for lymphocytes
LeflunomideInhibits dihydroorotate dehydrogenaseEnzyme InhibitionPyrimidine Synthesis InhibitorLiver toxicity, hypertensionHypertensionRheumatoid arthritisTeratogenic
CyclophosphamideAlkylates DNADNA AlkylationAlkylating AgentBone marrow suppression, bladder toxicityBladder toxicityCancer, lupusHemorrhagic cystitis risk
InfliximabBinds to TNF-a preventing its actionCytokine InhibitionTNF-alpha InhibitorInfections, infusion reactionsInfusion reactionsCrohn's disease, rheumatoid arthritisChimeric antibody
AdalimumabBinds to TNF-a preventing its actionCytokine InhibitionTNF-alpha InhibitorInfections, injection site reactionsInjection site reactionsRheumatoid arthritis, psoriasisFully human antibody
EtanerceptBinds to TNF-a preventing its actionCytokine InhibitionTNF-alpha InhibitorInfections, injection site reactionsInjection site reactionsRheumatoid arthritis, psoriasisFusion protein
OmalizumabBinds to IgE preventing its actionImmunoglobulin InhibitionIgE InhibitorAnaphylaxis, injection site reactionsAnaphylaxisAsthma, chronic urticariaMonoclonal antibody
TofacitinibInhibits JAK enzymesEnzyme InhibitionJAK InhibitorInfections, elevated liver enzymesElevated liver enzymesRheumatoid arthritis, psoriatic arthritisOral administration
RituximabBinds to CD20. Causes depletion of circulating B cellsCell DepletionCD20 Monoclonal AntibodyInfusion reactions, infectionsInfusion reactionsNon-Hodgkin lymphoma, rheumatoid arthritisChimeric antibody
TocilizumabAntagonists at IL-6 receptorsCytokine InhibitionIL-6 InhibitorElevated liver enzymes, infectionsElevated liver enzymesRheumatoid arthritis, giant cell arteritisMonoclonal antibody
SarilumabAntagonists at IL-6 receptorsCytokine InhibitionIL-6 InhibitorElevated liver enzymes, infectionsElevated liver enzymesRheumatoid arthritisMonoclonal antibody
AbataceptInterferes with T-cell activationT-cell ModulationCTLA-4 InhibitorInfections, headacheHeadacheRheumatoid arthritis, juvenile idiopathic arthritisFusion protein
Answers
2023 August 29
Axon Advocate
Axon Advocate

Drug Action and Characteristics for Step 1

DrugActionMechanism CategoryClass of ImmunosuppressantPossible Side EffectsDistinguishing Factor of Side EffectPossible Use CasesAdditional Information for Step 1
GlucocorticoidsRegulate gene expressionGene RegulationSteroidWeight gain, osteoporosisOsteoporosisAsthma, autoimmune diseasesCushing's syndrome risk
CyclosporineInhibits calcineurin phosphatase activityEnzyme InhibitionCalcineurin InhibitorKidney dysfunction, hypertensionKidney dysfunctionOrgan transplantationGingival hyperplasia
TacrolimusInhibits calcineurin phosphatase activityEnzyme InhibitionCalcineurin InhibitorKidney dysfunction, diabetesDiabetesOrgan transplantationLess nephrotoxic than Cyclosporine
SirolimusInhibits mTOR kinase activity; blocks T cell proliferationEnzyme InhibitionmTOR InhibitorHyperlipidemia, anemiaHyperlipidemiaKidney transplantationNot nephrotoxic
AzathioprineInhibits DNA synthesisDNA Synthesis InhibitionAntimetaboliteBone marrow suppression, liver toxicityLiver toxicityRheumatoid arthritisProdrug of 6-mercaptopurine
MethotrexateInhibits AICAR transformylase; anti-inflammatoryEnzyme InhibitionAntimetaboliteLiver toxicity, folic acid deficiencyFolic acid deficiencyCancer, rheumatoid arthritisFolinic acid as rescue therapy
Mycophenolate mofetilInhibits Inosine monophosphate dehydrogenaseEnzyme InhibitionAntimetaboliteDiarrhea, leukopeniaLeukopeniaOrgan transplantationSelective for lymphocytes
LeflunomideInhibits dihydroorotate dehydrogenaseEnzyme InhibitionPyrimidine Synthesis InhibitorLiver toxicity, hypertensionHypertensionRheumatoid arthritisTeratogenic
CyclophosphamideAlkylates DNADNA AlkylationAlkylating AgentBone marrow suppression, bladder toxicityBladder toxicityCancer, lupusHemorrhagic cystitis risk
InfliximabBinds to TNF-a preventing its actionCytokine InhibitionTNF-alpha InhibitorInfections, infusion reactionsInfusion reactionsCrohn's disease, rheumatoid arthritisChimeric antibody
AdalimumabBinds to TNF-a preventing its actionCytokine InhibitionTNF-alpha InhibitorInfections, injection site reactionsInjection site reactionsRheumatoid arthritis, psoriasisFully human antibody
EtanerceptBinds to TNF-a preventing its actionCytokine InhibitionTNF-alpha InhibitorInfections, injection site reactionsInjection site reactionsRheumatoid arthritis, psoriasisFusion protein
OmalizumabBinds to IgE preventing its actionImmunoglobulin InhibitionIgE InhibitorAnaphylaxis, injection site reactionsAnaphylaxisAsthma, chronic urticariaMonoclonal antibody
TofacitinibInhibits JAK enzymesEnzyme InhibitionJAK InhibitorInfections, elevated liver enzymesElevated liver enzymesRheumatoid arthritis, psoriatic arthritisOral administration
RituximabBinds to CD20. Causes depletion of circulating B cellsCell DepletionCD20 Monoclonal AntibodyInfusion reactions, infectionsInfusion reactionsNon-Hodgkin lymphoma, rheumatoid arthritisChimeric antibody
TocilizumabAntagonists at IL-6 receptorsCytokine InhibitionIL-6 InhibitorElevated liver enzymes, infectionsElevated liver enzymesRheumatoid arthritis, giant cell arteritisMonoclonal antibody
SarilumabAntagonists at IL-6 receptorsCytokine InhibitionIL-6 InhibitorElevated liver enzymes, infectionsElevated liver enzymesRheumatoid arthritisMonoclonal antibody
AbataceptInterferes with T-cell activationT-cell ModulationCTLA-4 InhibitorInfections, headacheHeadacheRheumatoid arthritis, juvenile idiopathic arthritisFusion protein
🔥 3
Masih Hedayati
Masih Hedayati

Hmmm, hirsutism for cyclosporin? Thank you for the post!

17:04
Yashar Haghighi
Yashar Haghighi

This is a great! thanks for posting it

18:30
2024 March 13
Rebecca Josiah
Rebecca Josiah

Thank you

08:34
2024 April 01
Masih Hedayati
Masih Hedayati

Thank you

03:55
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