Paracetamol:
- It is also known as acetaminophen
- It is para-aminophenol derivatives that possesses analgesic and antipyretic effects but is not anti-inflammatory agent.
- It is popular in use for human medicine due to less toxic effect than salicylates but limited application in veterinary medicine due to toxic effect, especially in cats.
MOA:
- Recent findings suggest that it selectively inhibits COX-2 than COX-1.
- It mediates its analgesic-antipyretic effects by inhibition of COX enzyme in brain.
Pharmacological Effect:
- It has good analgesic and antipyretic effect but has weak peripheral anti-inflammatory activity.
- It donot produce gastric irritation, erosion or bleeding that occur after administration of salicylates.
- It has no effect on platelets, bleeding time or excretion of uric acid.
Pharmacokinetics:
- Data on domestic animals is limited.
- In humans, it is well-absorbed orally and uniformly distributed in body
- It is bound to about 35% to plasma protein in blood
- It is metabolized in liver by conjugation with glucuronic acid (~60%), sulphate (~35%) and cysteine 30%.
- Small portion of paracetamol undergoes cytochrome P-450 mediated N-hydroxylation to form N-acetyl-p-benzoquinone.
- It is excreted as mercapturic acid in urine after reaction with glutathione.
Side effects/Adverse effects:
- In dogs, it causes renal, hepatic, GI and hematological effects
- In high dose, it causes damage to liver and kidney
- It can cause frank hemolysis by reducing lifespan of erythrocytes.
Drug Interactions:
- It should not be used in post-operative phase in animal that receive halothane.
- It potentiates the effect of oral anti-coagulant
- Additive action of analgesic with aspirin.
Contraindications and precautions:
- It is contraindicated in cat at any dosage.
- In dogs, it is not recommended to use in hepatic toxicity, live toxicity and hematological abnormalities
- It should be avoided in intermediate post-operative phase in dogs due to increased risk of hepatotoxicity.
Indications:
- It is occasionally used as oral analgesic in dog.
- In human, it is one of the best drugs to be used as antipyretic and most commonly used “over the counter (OTC)” analgesic.
Dose:
- Dogs: 10-15 mg/kg, PO, BID