Propacetamol

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A prodrug of paracetamol used for pain relief


Propacetamol
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Propacetamol is a prodrug of paracetamol (also known as acetaminophen) that is used for the management of pain and fever. It is administered intravenously and is rapidly converted to paracetamol in the body.

Pharmacology

Propacetamol is an ester of paracetamol and is designed to be more soluble in water, allowing for intravenous administration. Once in the bloodstream, propacetamol is hydrolyzed by plasma esterases to release paracetamol, which then exerts its effects by inhibiting the cyclooxygenase (COX) enzymes, primarily in the central nervous system.

Mechanism of Action

Skeletal formula of propacetamol

The mechanism of action of propacetamol is essentially that of paracetamol. Paracetamol is believed to inhibit the synthesis of prostaglandins in the central nervous system and work peripherally to block pain impulse generation. It also acts on the hypothalamic heat-regulating center to produce antipyresis.

Clinical Use

Propacetamol is used in clinical settings where oral administration of paracetamol is not feasible, such as in patients who are unable to swallow or require rapid pain relief. It is commonly used in postoperative pain management and in situations where rapid onset of analgesia is required.

Side Effects

The side effects of propacetamol are similar to those of paracetamol, including potential hepatotoxicity at high doses. Other side effects may include nausea, vomiting, and allergic reactions.

Advantages

The primary advantage of propacetamol over paracetamol is its ability to be administered intravenously, providing a rapid onset of action. This is particularly beneficial in acute care settings.

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Contributors: Prab R. Tumpati, MD