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Pharmacology > IMMUNOPHARMACOLOGY > Flashcards

IMMUNOPHARMACOLOGY Flashcards

1
Q

Cytotoxic Agents

A

Antimetabolites

Alkylating agents

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2
Q

Azathioprine
MOA
Drug interactions

A

Purine antimetabolite
Prodrug of 6-mercaptopurine converted to 6-MP
- 6-MP is converted to metabolites that inhibit de novo puine nucleotide synthesis–> suppression of B and T cell function of immunoglobulin production and of IL-2 secretion.

DI: Inactivation of drugs has to do with Xanthine oxidase

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3
Q

Glucocorticoids anti-inflammatory MOA

A

Inhibition of PLA2

Reduction of transcription of COX-2 (inflammatory cancer)

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4
Q

Glucocorticoids AE

A 
Short term use: HTN 
hyperglycemia 
immunosuppresion
psychotic reactions 
cognitive impairment

Long term use:
Myopathy
Cushing’s syndrome
osteoporosis

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5
Q

Glucocorticoids uses:

A 
Prevent treat transplant rejection
Treat autoimmune disorders such 
- RA
- SLE
- Psoriasis
- Asthma 
- IBD
In palliative care glucocorticoids arae used to alleviate pain; nausea and fatigue
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6
Q

Calcineurin inhibitors

MOA?

A 
Cyclosporine
- primarily metabolized by CYP 3A4
- forms a complex w/ cyclophilin (immunophilin).
- complex inhibits calcineurin
Tacrolimus
- Binds to FK-binding protein (FKBP)
- FKBP is an immunophilin
- Tacrolimus -FKBP complex inhibits calcineurin
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7
Q

Calcineurin

A

Phosphatase used to activat T- Cell specific Transcription factor (NFAT)

NFAT is required for induction of cytokine genes

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8
Q

Cyclosporine adverse effects

A 
Nephrotoxicity*: limiting and occurs in majority of patients
tremor
HTN
Hyperglycemia
Hyperlipidemia
Osteoporosis
Hirsutism*
Gum Hyperplasia*
- Very little bone marrow toxicity
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9
Q

Cyclosporine USES?

A

Organ transplant
Uveitis
Rheumatoid Arthritis
Psoriasis

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10
Q

Tacrolimus Adverse Effects

A 
Nephrotoxicity
Neurotoxicity*
Hyperglycemia
HTN
Hyperkalemia
GI complaints
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11
Q

Tacromlimus uses

A
  • transplant rejection prevention of kidneys liver and heart

- topical formulation is used for topical dermatitis and psoriasis

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12
Q

MOA of sirolimus a Proliferation signal inhibitor:

A

Sirolimus

  • structurel similar to tacrolimus
  • also binds to FKBP but does not inhibit calcineurin
  • inhibits Serine-threonine kinase mTOR*–>blocks IL-2-driven T- cell proliferation.
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13
Q

Sirolimus Adverse Effects?

A 
Myelosuppresion*
Hepatotoxicity
Diarrhea
Hypertriglyceridemia
Pneumonitis
Headache
  • Nephrotoxicity is less common than w/ calcineruin inhibitors!!!
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14
Q

Sirolimus uses

A

Renal transplantation
Sirolimus-eluting stents are used to inhibit restenosis of the blood vessels in patients with severe CAD by reducing cell proliferation.

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15
Q

Inhibitors of Angiogenesis MOA?

A

Thalidomide

  • MOA unclear
  • inhibits synthesis of TNF-a
  • now called an immunomodulatory drug
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16
Q

Thalidomide indications

A

“MEL”
Erythema nodosum
Leprosum
multiple myeloma

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17
Q

Cytotoxic agents

A

Antimetabolites:

  • Azathioprine
  • Methotrexate
  • Mycophenolat mofetil
  • Leflunomide

Alkylating agents:
Cyclophosphamide

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18
Q

Azathioprine AE:

A

AE:

  • Bone marrow suppression
  • GI disturbances
  • increase in infections and malignancies
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19
Q

Azathioprine inactivation depends on the action of what enzyme?
What drug interaction should be avoided when taking AZA?

A

Xanthine oxidase

Allopurinol: used for control of hyperuricemia. Patients receiving allopurinol should have the dose of azathioprine reduced.

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20
Q

AZAthioprine uses

A

Prevention of organ transplant rejection

severe RA

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21
Q

Methotrexate MOA

A

At low doses is used in Rheumatic diseases to inhibit Aminoimidazolecarboxamide ribonucleotide (AICAR) transformylase.
- accumulation of AMP–> increased adenosine–> immunosuppressive (potent inhibition of inflammation by adenosine).

AICAR tranformylase catalyzes the penultimate and final step in de novo purine biosynthesis which lead to synthesis of IMP.

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22
Q

Methotrexate AE

A 
Mucosal ulceration
Hypersensitivity pneumonitis
GI ulcerations
Nausea
Leukopenia
Anemia
cirrhosis is rare
Hepatotoxicity
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23
Q

Methotrexate toxicity can be reduced with?

A

Leucovorin

Folic acid

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24
Q

Methotrexate CIs

A

Pregnancy

25
Q

Methotrexate uses

A 
"RAPPS"
RA
Psoriasis
Psoriasis arthritis
Ankylosing spondylitis
SLE
26
Q

Mycophenolate Mofetil

MOA?

A

converted to mycophenolic acid
mycophenolic acid inhibits inosine monophosphate DH an enzyme in the de novo pathway of guanosinentriphosphate (GTP) synthesis.

This suppresses both B and T lymphocyte activation.
- lymphocytes lack enzymes necessary for the salvage pathway so they are susceptible to inhibitors of the de novo pathway

27
Q

Mycophenolate Mofetil AE

A 
Nausea
vomiting 
diarrrhea 
abdominal pain
headache 
HTN
Reversible myelosuppression
28
Q

Mycophenlate mofetil uses

A

Prophylaxis of transplant rejection

SLE

29
Q

Leflunomide MOA

A

Pro drug of teriflunomide
Teriflunomide inhibits dihydroorotate DH
decreases levels of UMP
UMP is essential for the synthesis of pyrimidines

30
Q

Leflunomide AE

A 
Diarrhea
Reversible alopecia
Rash
Myelosupression
Increases in aminotranferases activity
CBC and liver function tests should be monitored
Carcinogenic and teratogenic in animals
Contraindicated in pregnancy
31
Q

Leflunomide USES

A

“RaMS”
RA
SLE
Myasthenia Gravis

32
Q

Alkylating agents

A

Cyclophosphamide

  • one of the most effective immunosuppressive drugs available
  • destroys proliferating lymphoid cells
  • alkylates DNA and other molecules in resting cells
33
Q

Cyclophosphamide AE

A

Infertiltiy
Bone marrow suppression
Hemorrhagic cystitis
Rarely bladder carcinoma
Acrolein a metabolite is responsible for urinary toxicities
Long term use increases risk of infection and malignancy

34
Q

Cyclophosphamide USEs

A

treat SLE and other autoimmune diseases.

may take 3-6 months to show benefit.

35
Q

Hydrochloroquine AE

A

Hemolysis in patients w/ G6PD defeciency

Retinal damage: vision should be monitored

36
Q

Sulfasalazine structure

A

consists of sulfapyridine and 5-aminosalicylic (5-ASA) connected by diazo bond.

37
Q

Sulfasalazine MOA

A

Metabolized by bacteria in the colon to constituent moieties:

  • sulfapyridine is probably the active moiety in the tx. of rheumatoid arthritis.
  • 5-ASA moiety important in ulcerative colitis.
38
Q

Sulfasalazine AE

A 
Nausea vomiting
Headache rash
Neutropenia
Thrombocytopenia is very rare
Drug induced lupus is rare
Hemolysis in patients with G6PD def.
39
Q

Sulfasalazine uses

A

Ulcerative colitis
Rheumatoid arthritis
Crohn’s disease
Ankylosing spondylitis

40
Q

Immunosuppressive Antibodies

A

Polyclonal antibodies:
- Antilymphocyte (ALG) and Antithymocyte (ATG) Antibodies
- Rho(D) Immune Globulin
Monoclonal antibodies

41
Q

Antilymphocytic globobulin (ALG) and Antithymocyte Globulin (ATG) uses

A
  • Used before stem cell transplantation to prevent graft-versus-host reaction.
  • Also use for solid organ transplantation
42
Q

Monclonal antibodies

A

TNF-a inhibitors

  • Infliximab
  • Adalimumab
  • Etanercept
43
Q

Anti-TNF-a drugs adverse effects

A
  • Cytopenias can occur: CBC should be monitored regularly
  • Serious infections are the most important potential adverse effects of TNF inhibition
  • Drugs should not be given to patients with an active infection
  • *Patients should be screened for latent TB infection before and during tx. w/ a TNF inhibitor.
  • Patients may be at risk for malignancies
44
Q

Infliximab

A
  • Chimeric monoclonal antibody
  • Binds with high affinity and specficity to humna TNF-a
  • Used in the tx. of rheumatoid arthritis; psoriatic arthirtis; ankylosing spondylitis; Crohn’s disease; and ulcerative colitis.
45
Q

Adalimumab

A

Fully humna IgG1 anti-TNF monoclonal antibody

  • Binds soluble TNF-a and prevents its interation with TNF receptors.
  • Used in the tx. of rheumatoid arthritis; psoriatic arthritis; ankylosing spondylitis; Crohn;s disease and ulcerative colitis.
46
Q

Etanercept

A

Not a true Mab

  • Ligand-binding portion of a human TNF-a receptor fused to the Fc portion of human IgG1.
  • Binds to TNF-a and prevents it from interacting w/ its receptors.
47
Q

Etanercept uses

A 
RA
Ankylosing spondylitis
Plaque psoriasis
polyarticular juvenile idiopathic arthritis
psoriatic arthritis
48
Q

Omalizumab
MOA?
USE?

A
  • Anti-IgE recombinant humanized monoclonal antibody
  • Binds to IgE and prevents IgE from binding to mast cells and basophils thereby preventing release of inflammatory mediators after allergen expopsure
  • Used in asthma refractory to inhaled corticoids and evidence of allergic sensitization
  • also approved for chronic urticaria
49
Q

Basiliximab

A
  • IL-2 receptor antagonist
  • Chimeric human-mouse IgG
  • Binds to the IL-2 receptor
  • Used in combination w/ ther immunosuppressants to prevent transplant rejection.
50
Q

Rituximab

A
  • Chimeric murine-human monoclonal antibody that binds to the CD20 molecule on B lymphocytes.
  • Causes depletion of circulating B cells
  • Used for tx. of non-hodgkins lymphoma and chronic lymphocytic leukemia
  • Also approved for rheumatoid arthritis.
51
Q

Anakinra
MOA
USE

A
  • IL-1 receptor antagonist
  • Recombinant version of the naturally occurring human IL-1RA that prevents IL-1 from binding to its receptor.
  • Approved for moderate to severe rheumatoid arthritis
52
Q

Abatacept
MOA?
USE?

A
  • Fusion protein that interferes w/ T-cell activation
  • Used for moderate to severe rheumatoid arthritis
  • Used for moderate to severe polyarticular juvenile idiopathic arthritis.
53
Q

Immunostimulants

A

Aldesleukin
Interferons
Bacillus Calmette-Guerin (BCG)

54
Q

Aldesleukin
MOA?
USE?

A
  • Recombinant interleukin-2 (IL-2)
  • IL-2 is lymphokine that promotes the production of cytotoxic T lymphocytes and activates NK cells.
  • Aldesleukin is indicated for the adjunctive treatment of renal cell carcinoma and malignant melanoma
55
Q

Interferons

USE?

A 
Hairy cell leukemia
chronic myelogenous leukemia
malignant melanoma
Kaposi sarcoma
hep B and C infections
56
Q

Bacillus Calmette-Guerin (BCG)

A

attenuated live culture of Mycibacterium bovis

  • active against tumors MOA unknown
  • indicated for tx. and prophylaxis of carcinoma of the urinary bladder.
AE: hypersensitivity 
shock
chills 
fever
malaise
immune complex disease
57
Q

Drugs used to stop transplant rejection:

A 
Glucocorticoids - prevent and treat
Tacrolimus - prevention of rejection for HLK (heartLiverKidney)
Azathioprine
Mycophenolate - prophylaxis
Basiliximab - renal transplant
58
Q

Drugs used for rheumatoid arthritis

A 
Glucocorticoids
Cyclosporine
Azathioprine (SEVERE)
Methotrexate
Leflunomide
hydroxychloroquine (MILD)
sulfasalzine
Infliximab
adalimumab
Etanercept
Rituximab
Anakinra (moderate-->severe)
Abatacept (moderate to severe)
59
Q

Renal transplant drugs

A

Sirolimus

Basiliximab

Pharmacology (27 decks)

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