Pharm: Anti-Inflammatory Drugs Brief Study

5 cardinal signs of inflammation:

• Redness

• Heat

• Swelling/edema

• Pain

• Loss of function

4 steps of the inflammatory response:

1. The damaged tissues release histamines, increases blood flow to the area.

2. Histamine causes the capillaries to leak phagocytes and clotting factors.

3. Phagocytes engulf bacteria, dead cells, and cellular debris.

4. Platelets move out of the capillaries to seal the wound.

2 main groups of anti-inflammatories:

1. Steroidal anti-inflammatory drugs

   1. Primarily glucocorticoids

2. Non-steroidal anti-inflammatory drugs (NSAID’s)

What is one of the main ways that inflammatory mediators are produced?

Arachidonic Acid Pathway.

What is the end result of the arachidonic acid pathway?

Production of inflammatory chemicals.

• Prostaglandins

• Leukotrienes.

• Etc..

Which enzymes act on the Arachidonic Acid Pathway?

• COX

  • produces prostaglandins thromboxanes

• Lipooxygenase

  • produces leukotrienes

What do steroids do?

• Block phospholipase.

• Blocks the earliest part of the arachidonic acid pathway.

How do NSAID’s reduce inflammation?

• Inhibit COX

• OR they block prostaglandin receptors

What are the 2 main types of corticosteroids?

• Mineralcorticoids

• Glucocorticoids

What do glucocorticoids inhibit?

Phospholipase.

What is the enzyme that turns phospholipids in the cell membrane to arachidonic acid?

• Starts the arachidonic acid pathway.

Phospholipase.

Exogeneous (from outside the body) glucocorticoids:

• Prednisone

• Prednislone

• Hydrocortisone

• Dexamethasone

• Methylprednislone

What are glucocorticoids classified by?

Duration of activity:

• Short-acting

• Intermediate-acting

• Long-acting

Intermediate-acting glucocorticoids:

1. “Preds”

• Prednisone

• Prednisolone

  • Cats need!

• Methylprednisolone

2. Triamcinolone

Long-acting glucocorticoids:

• Dexamethasone

• Betamethasone

• Flumethasone

• Isoflupredone

Benefits/functions of glucocorticoids:

• Help the body deal with stress.

• Decreases inflammation

• Stabilize lysosomal membranes inside the cells

• Keep capillaries from getting leakier.

Cats seem more resistant to steroid effects.

T/F?

True.

You must _______ steroids SLOWLY!

Taper.

Rules to using glucocorticoids safely:

• Determine a cause BEFORE starting them.

• Try other drugs first?

• Doses are guesses!

• Try to avoid continuous use.

• If an animal has been on them and needs to be off the,. decrease SLOWLY!.

What are the 2 forms of COX?

• COX1= “Good guy”

• COX2= “Bad guy”

COXn2 selective inhibitors:

• Carprofen- Rimadyl

• Meloxicam- Metacam

• Deracoxib- Deramaxx

• Robenacoxib- Onsior

• Firocoxib- Previcox

What is “Wind-up”?

A process where prolonged, intense pain signals bombard the spinal cord

Is it true that NSAID’s usually aren’t strong enough?

Yes.

What are some things of note for Carprofen (Rimadyl)?

• Only FDA approved for dogs in the USA

• Very tasty, dogs can potentially get into the bottle)

• Bad effect on the liver.

How much of Meloxicam (metaclam) can we use?

No more than ONE dose.

What are some things of note for Robenacoxib (Onsior)?

• One of the best newer NSAID’s

• Animals must be greater than 5.5# and 4 months old.

• Use for up to 3 days.

What do prostaglandin receptor anatagonists do?

• Grapiprant - Galliprant

Inhibit prostaglandins so they can’t make pain travel to the brain.

Products that protect the cartilage from degredation.

Chondroprotective agents.