Etanercept

Question 1

What class of drugs does Etanercept belong to?

Answer 1

Immunomodifiers/cytokine modulators

Biologicals

Question 2

What is Etanercept?

Answer 2

A dimeric fusion protein.

consists of 2 human p75 soluble TNF receptors linked to a Fc fragment of the human IgG antibody.

Question 3

What is Etanercept indicated for?

Answer 3

the treatment of severe active RA in adults,
severe juvenile idiopathic arthritis,
ankylosing spondylitis and severe plaque psoriasis.

Question 4

Where is Etanercept placed in RA therapy?

Answer 4

With or without MTX

Question 5

What is the weekly dose of Etanercept?

Answer 5

either self administered 50mg via subcut injection once a week

or self administered 25mg subcut twice weekly

Question 6

What is the mechanism of action of Etanercept?

Answer 6

The dimeric soluble form of the p75 TNF receptor allows Etanercept to bind competitively to 2 TNF molecules, effectively removing them from circulation and inhibiting their function

Question 7

What are the characteristic pharmacokinetic and pharmacodynamic parameters regarding Etanercept?

Answer 7

Absorption reaches max concentration at 24-96 hours following single dose.
absolute Bioavailabiltiy: 76%
Volume of distribution: 10.4L
Clearance: slow 0.066L/h in patients with RA (lower than in healthy volunteers)
Half life: 80 hours

Question 8

What are some precautions associated with Etanercept use?

Answer 8

predisposition to infection
children
heart failure,
demyelinanting disorders
history of malignancy
history of blood disorders

Use with caution if hepatic impairment

Avoid in pregnancy (class B2) and breast feeding

Question 9

What is contraindicated to Etanercept use?

Answer 9

active infection
concomitant treatment with IL-1 antagonists (anakinra)
sepsis

Question 10

What are the alarm bells with Etanercept use?

Answer 10

monitor for TB infection
Patient to report symptoms or signs of bloo dyscrasias or infection including persistent cough, weight loss, fever ,sore throat, bruising, bleeding, paleness

Question 11

What are the adverse effects associated with Etanercept use?

Answer 11

sometimes severe TB, septicaemia, hep B reactivation
Nausea, abdominal pain, worsening heart failure.
hypersensitivty reactions
fever, headache, depression, antibody formation including lupus-like syndrome.
pruritus, injection site reactions and blood disorders

Question 12

What are the interactions asociated with Etanercept use?

Answer 12

vaccines. Avoid concomitant use