Anda di halaman 1dari 8

Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects

Fungal Cyclic Peptide Antibiotic


Cyclosporine(Neoral, Gengraf, A: PO or IV Binds to cyclophilin to Prophylaxis for organ rejection Gingival hyperplasia
Sandimmune) M: Hepatic (P450) form a complex that following transplant (ie, kidney, GI distress
E: Metabolites excreted inhibits calcineurin heart, liver, BMT, lung, and Increased risk of infections and
in feces Highly selective pancreas) malignancies
inhibition of T cell Treatment of graft versus host Hirsutism
activation by blocking reactions (often in combination Hypertension
cytokine production with corticosteroids) Nephrotoxicity
(especially IL-2) Autoimmune disorders (ie, RA and Neurologic effects (seizures
severe psoriasis) and tremor)
Macrolide Antibiotics
Sirolimus (Rapamune) A: PO Binds to FK-binding Liver and kidney transplantation Blood dyscrasias
M: Metabolized in protein, inhibiting the Potentially useful in conjunction Hepatic artery thrombosis
intestinal wall and response of T cells to with cyclosporine with which it Increased risk of infections and
hepatic (P450) cytokines without acts synergistically malignancies
E: Metabolites excreted affecting cytokine Hyperlipidemia
in feces production Hypertension
Rash
Peripheral edema
Inhibits P450 enzymes
Tacrolimus/FK-506 (Prograf, A: PO or IV Binds to FK-binding 10–100 times more potent Asthenia
Hecoria) M: Hepatic (P450) protein and forms a immunosuppression Blood dyscrasias
E: Metabolites excreted complex that inhibits than cyclosporine GI (diarrhea, nausea,
in feces calcineurin Liver, cardiac, and kidney abdominal pain)
Calcineurin regulates the transplantation Hyperglycemia due to new
T cells ability to produce onset diabetes
interleukins Increased risk of infections and
malignancies
Nephrotoxicity
Neurotoxicity
Hyperkalemia
Inhibits P450 enzymes
Glucocorticoid
Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
Prednisone A: PO Impaired release of Administered before, during, and Adrenal suppression
M: Metabolized in cytokines from after transplant surgery (always (cushingoid reactions)
multiple tissues macrophages and used in combination with other associated with an inability to
including the liver granulocytes immunosuppressants, such regulate endogenous
(P450 minor) Suppression of T cell as cyclosporine, for organ glucocorticoid levels following
E: Metabolites excreted proliferation and transplantation) use
in urine activation Autoimmune diseases (eg, RA, SLE, Osteoporosis (LTU)
Suppression of antibody and dermatomyositis) Redistribution of body fat
production Treatment of acute graft versus Inhibition of growth
Reduction of host rejection (suppress secondary Myopathy
accumulation of [antibody] response via B cell Development of cataracts,
macrophages suppression) glaucoma
Seems to spare B cell Attenuation of allergic reactions Kaposi's sarcoma with
population under normal Treatment of asthma prolonged use
conditions Treatment of PCP pneumonia Psychiatric disturbances
Inhibit migration of cells Treatment of ITP Inhibits P450 enzymes
that cause acute Treatment of lupus nephritis and Induces P450 enzymes
rejection of an organ, nephrotic syndrome
which is an inflammatory
response
Anti TNF-α Agents
Thalidomide(Thalomid) A: PO May act as a selective Treatment and prophylaxis of Dizziness
M: Undergoes inhibitor of TNF-α but erythema nodosum leprosum Drowsiness
nonenzymatic immunologic effect Treatment of multiple myeloma GI distress (diarrhea, nausea,
hydrolysis varies on condition Treatment of GVHD constipation, abdominal pain)
E: Metabolites excreted Peripheral neuropathy
in urine Edema
Hypocalcemia
Increased risk of thrombosis
Etanercept (Enbrel) A: SC Solution of TNF receptor Treatment of RA and juvenile RA CNS symptoms suggestive of
M: Possibly linked to Fc portion of demyelinating conditions
metabolized by human IgG1 Increased risk of infections and
reticuloendothelial Acts as a competitive malignancies
system inhibitor of TNF
Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
Binds TNF and blocks its
interaction with the cell
surface receptors
Golimumab(Simponi) SC Monocolonal antibodies Rheumatoid arthritis Headache
against TNF-α Psoriatic arthritis Cardiac arrhythmias
Ankylosing spondylitis Increased risk for infections
and malignancies
Adalimumab (Humira) SC Rheumatoid arthritis Increased risk for infections
Infliximab(Remicade) IV JRA (Adalimumab only) and malignancies
Psoriatic arthritis GI distress (abdominal pain,
Ankylosing spondylitis nausea, vomiting)
Plaque psoriasis Infusion-related reactions
Ulcerative colitis (fevers, chills, pruritis, chest
Crohn's disease pain, dyspnea, hypotension,
myalgia)
Certolizumab pegol (Cimzia) SC Humanized antibody Fab Rheumatoid arthritis Increased risk for infections
fragment of TNF- Crohn's disease and malignancies
αmonoclonal antibody Nausea
that binds to and
selectively neutralizes
human TNF-α
Cytotoxic Agents
Azathioprine (Imuran, A: PO and IV Blocks de novo purine Autoimmune diseases (ie, RA, SLE) Leukopenia
Azasan) M: Hepatic, prodrug synthesis and interferes Prophylaxis of rejection in renal Thrombocytopenia
slowly converted to 6- with DNA synthesis transplants Rash
mercaptopurine Somewhat more effect GI disturbances
E: Metabolites excreted on T cells than B cells Hepatotoxicity
in urine Increased risk of malignancies
Cyclophosphamide(Cytoxan) A: PO, IV, IM, and Inhibits DNA and RNA Chemotherapy for solid tumor Hematologic disturbances
intracavitary synthesis via cross- malignancies (anemia, leukopenia,
M: Hepatic (P450) linking of these Treatment of pediatric nephrotic thrombocytopenia)
E: Parent drug and molecules syndrome Severe nausea and vomiting
metabolites excreted in Destroys any Hemorrhagic cystitis
urine proliferating lymphoid Cardiotoxic
cells (more effective Alopecia
Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
suppression of B cell Decreased fertility
proliferation) Inhibits P450 enzymes
Induces P450 enzymes
Methotrexate/MTX (Trexall, A: PO, IM, IV, and Inhibits dihydrofolate Treatment of autoimmune diseases GI tract irritation (diarrhea,
Rheumatrex) intrathecal reductase blocking (eg, RA and psoriasis) ulcerative stomatitis)
E: Majority excreted synthesis of nucleoside Chemotherapy Hepatotoxicity
unchanged in urine phosphates inhibiting Combined therapy Pneumonitis
DNA synthesis with cyclosporinewith graft versus Bone marrow suppression
Rapidly proliferating host reactions following BMT Severe rashes
cells are destroyed Severe opportunistic infections
Tumor lysis syndrome
Nephrotoxicity
Enzyme Inhibitors
MycophenolateMofetil A: PO and IV Metabolite (MPA) Prophylaxis for heart, liver, and Hypertension
(Cellcept, Myfortic) M: Metabolized inhibits inosine kidney transplant rejection Hyperglycemia
presystemically to monophosphate Typically used Hypercholesterolemia
active metabolite in dehydrogenase, an with cyclosporine and prednisone Neutropenia
liver and GI tract enzyme in the de novo Increased risk of lymphoma
E: Metabolites excreted purine synthesis and skin malignancies
primarily in urine pathway Increased risk of infection
Blocks de novo purine
synthesis
Results in inhibition of B
and T lymphocyte
proliferation
Leflunomide(Arava) A: PO Inhibits dihydroorotate Treatment of RA Alopecia
M: Hepatic dehydrogenase, an GI distress (diarrhea, nausea,
E: Metabolites excreted enzyme in the de novo constipation, abdominal pain)
in urine and feces pyrimidine synthesis Hepatotoxicity
pathway Hypertension
Blocks de novo Interstitial lung disease
pyrimidine synthesis Peripheral neuropathy
Results in inhibition of B Malignancies
and T lymphocyte Inhibits P450 enzymes
proliferation
Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
Tofacitinib(Xeljanz) A: PO Inhibits Janus kinase RA Increased risk for infections
M: Hepatic (P450) to enzymes which is and malignancies
active metabolite involved in
E: Parent drug and hematopoiesis and
metabolites excreted in immune cell function
urine
Apremilast (Otezla) A: PO Inhibits PDE 4 thus Plaque psoriasis GI distress (nausea, diarrhea)
M: Hepatic (P450) increasing the level of Psoriatic arthritis
E: Metabolites excreted cAMP and thus
in feces and urine regulating inflammatory
compounds
ANTIBODY IMMUNOSUPPRESSANT FACTS

Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects


Antilymphocyte Globulin / IV Antibodies that bind to T Treatment and prevention of Headache
Lymphocyte Immune lymphocytes causing them to be acute rejection following Fever
Globulin(Atgam) destroyed by complement kidney transplants Rash
Treatment of aplastic anemia Leukopenia
in patients not suitable for Thrombocytopenia
BMT
Immune GlobulinIntravenous IV Precise mechanism of action Treatment of patients with Dyspnea
/IGIV / IVIG unknown immunodeficiency syndromes Hypersensitivity reactions
May act via increase of suppressor Treatment of Kawasaki Tachycardia
T cells or diminution of helper T syndrome (reduction of
cells systemic inflammation and
prevention of coronary
aneurysms)
Treatment of severe asthma
Treatment of some
autoimmune diseases (eg, ITP,
MS, and SLE)
Tocilizumab(Actemra) IV Monoclonal antibody that acts as an RA and JRA Elevated hepatic
antagonist of IL-6 receptor thereby transaminases
decreasing activation of Increased risk of infections
inflammatory cascade and malignancies
Demyelinating disease
Basiliximab (Simulect) IV Monoclonal antibody that blocks Prophylaxis of acute rejection Hypertension
the αchain of the IL-2 receptor on following renal transplants Edema
activated T lymphocytes Fever
Tremor
Muromonab-CD3 (Orthoclone IV Monoclonal antibody, directed Treatment of acute rejection Blood dyscrasias
OKT3) towards CD3 molecule on the following kidney, heart, or liver Cytokine release syndrome
surface of all T cells resulting in transplants (flu-like symptoms)
inhibition of T cells to function as T Photophobia
lymphocytes CNS reactions
(encephalopathy, cerebral
edema, aseptic meningitis)
Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
Neurologic reactions
(headache, seizures)
Ustekinumab (Stelara) SC Monoclonal antibody that blocks Plaque psoriasis Increased risk for infection
the action of IL13, IL 23 which in Psoriatic arthritis Dermatologic
turn blocks NK cell activation and complications (exfoliative
CD4 cell activation dermatitis, erythrodermic
Inhibits production of MCP-1, TNF psoriasis
a, IP 10 and IL 8
Secukinumab(Cosentyx) SC Monoclonal antibody that binds to Plaque psoriasis Increased risk for infection
and thus blocks the action of IL17A Nasopharyngitis
Belimimab (Benlysta) IV Monoclonal antibody that blocks SLE GI distress (nausea,
the activity of human B lymphocyte diarrhea)
stimulator protein thus preventing
B cell survival
Ofatumumab(Arzerra) IV Monoclonal antibody that binds to CLL Progressive multifocal
Rituximab(Rituxan) IV the CD 20 molecule on B CLL leukoecephalopathy
lymphocytes causing cell death NHL Reactivation of Hepatitis B
Granulomatosis with Increased risk of infection
polyangiitis GI distress (nausea,
RA diarrhea)
Microscopic polyangiitis
Alemtuzmab (Campath, IV Monoclonal antibody that binds to B cell CLL Autoimmune diseases
Lemtrada) CD52 molecule on B an T cells Relapsing MS Cytopenias
causing cell death Increased risk for infections
and malignancies
Natalizumab(Tysabri) IV Monoclonal antibody that binds MS Progressive multifocal
to α4 subunit of intergrin Crohn's disease leukoecephalopathy
molecules (a molecule responsible
for the adhesion and migration of
cells from the vasculature to
inflamed tissue)
Fingolimod (Gilenya) A: PO Active metabolite blocks the MS Headache
M: Hepatic (P450) to lymphocyte's ability to emerge
active metabolite from the lymph node
Drug Pharmacokinetics Mechanism of Action Clinical Uses Side Effects
E: Primarily excreted
as metabolites in
urine
Teriflunomide(Aubagio) PO Inhibits pyrimidine synthesis MS Hepatotoxicity
Teratogenic effects
Belatacept(Nulojix) IV Blocks T cell activation by binding Prophylaxis for acute renal Increased risk for infections
to CD80 and CD86 transplant rejection and malignancies
Anakinra (Kineret) SC Blocks IL K1 RA Nasopharyngitis
Neonatal-onset multisystem Headache
inflammatory disease Increased risk for infection
Abatacept(Orencia) IV, SC Binds to proteins on antigen RA Headache
presenting cells inhibiting their JRA Nasopharyngitis
subsequent activation of T cells