NSAID

Question 1

Pharmacological effects

Answer 1

1. Anti-inflammatory
2. Antiallergic
3. Antipyretic
4. Platelet aggregation inhibition- thromboxane (aspirin)
5. Anti-endotixic - colic in eq(Meloxicam, Flumixin)
6. Spasmolytic
7. Antineoplastic - some need COX(piroxicam)

Question 2

Cell damage => membrane phospholipids release=>(PPA) Arachidonic acid => ?

Answer 2

1. Lipoxygenase: Leukotrienes , lipoxins - role in asthma
2. Cyclooxygenase: COX-1 (Housekeeping) , COX-2 (Inflammation), COX-3 (thalamus, pain sensation+ production -paracetamol)
3. epoxigenase

Question 3

Pharmacokinetics

Answer 3

Weak acids , ionized and non-ionized form
Absoroption starts in stomach
*Ion trapping: COOH can easily diffuse into the cell , dissociate threre to CO2+H and cannot leave - ULCERATION (Aspirin)
*Better coated due to stomach irritation
*Binding albumin (hypoalbuminemia= inc toxicity) - drug interaction
*Conjugated to glucaronic acid in liver
*Not for more that a week for cat, off lable- meloxicam can be given life long

Question 4

Side Effects

Answer 4

1. GI ulceration (due to ion trapping and dec. PGE) - Omeperazole to prevent
2. Kidney damage : dec PGE cause vasodolation - inc RBF (dehydration, infusion)
3. Hepstotoxic- (paracetamol) liver oxidation - never in cats! (Methaemoglobin)
4. Platelet aggregation - surgery
5. Cartilage damage (meloxicam and Carprofen are safe)
6. fetal damage (metamizole is safe)

Question 5

Acidic substances:

Salicylates

Answer 5

1. Acetylsalicylic acid - COX-1
2. Na salicylate - COX-2 Selective (farm animals)
3. Slazine : in the large intestine degraded to antibiotics + NSAID - colitis (pets)

Question 6

Arilpropionic acids

Answer 6

1. Carprofen - COX-2 very safe (golden+labs hepstotoxic)
2. Ketoprofen - COX-1 selective (max 1 week , platelet agg.)
3. Vedaprofen - COX-2 selective (eq)

*NEVER use ibuprofen , naproxen

Question 7

Non-acidic:

1. Oxicams!
   * Butryl pyrazolidine

Answer 7

1. Meloxicam : COX-2 selective- only one recommended for long term for cats, one dosge in large animals, taking with food, Anti-endotixic : Eq-colitis, Ca-enteritis, Cow-mastitis
2. Piroxicam: COX-1 selective , treats prostate tumour
3. Tenoxicam- not used

*Phenylbutazone - antinflammatory used in horses

Question 8

Colic NSAID?

Answer 8

Fluxin meglumine - antioxidant+antispasmolytic - colic in eq

Question 9

1. Pyrazolone

2. Analine derivative

Answer 9

1. Metamizole: COX-3 - analgestic , safe (no kidney/stomach effect), not in cats , pregnancy safe!, antispasmotytic
2. Analine derivative: paracetamol- COX-3 never in cats

Question 10

COXIB!

Answer 10

COX-2 highly selective , safest drug
Mavacoxib (trocoxil) - long HL(once a month) dog , give with food

Deracoxib (like meloxicam) , firocoxib (safest) robenacoxib (cats) ,cimicoxib (dogs),

Question 11

1. Heteroaryl acetic acid

2. Anthranilic acid

Answer 11

1. Diclofenac- not used
   Etodolac - like meloxicam
2. Flunixin-meglumin: COX-1 antioxidant+ antispasmolytic, anti-endotoxic
   Tolfenamic acid - COX-1