Hello……I AM PARACETAMOL

Paracetamol (acetaminophen) – a name we have identified with fever and pain. A drug we have consumed the most in our life. The first drug (most probably) we have tasted. A drug which will always be there in side packet or cupboard.  A common household drug.  Do we really know enough about this drug ?

Birth and Controversy:

Paracetamol (recommended international nonproprietary name) (acetaminophen) was synthesized  by Morse in 1878 and first used clinically by von Mering. Study on Pracetamol came to a full stop when clinical studies showed paracetamol had a slight tendency to produce methemoglobinemia (presence of higher level of methemoglobin).   In 1950s, the studies carried out by Brodie and Axelro led to its “rediscovery” and marketing in the United States as an analgesic. In 1956, 500 mg tablets of paracetamol went on sale under the trade name Panadol in the United Kingdom  In 1963, paracetamol was added to the British Pharmacopoeia. It gained popularity since then as an analgesic agent with few side-effects and little interaction with other pharmaceutical agents.

Mechanism of Action:

 Paracetamol is great for headaches, fever, minor aches and pains but won’t reduce inflammation

Enzyme Cyclooxygenase helps to form prostaglandins, which are pain- and inflammation-mediating signaling molecules. Paracetamol blocks cyclooxygenase (COX) enzymes, most probably COX-3 (based on latest findings). There is still some pieces missing in this mechanism, because of which research is still on.

Image: C&EN journal, Volume 92 Issue 29 | pp. 31-32

Dosage:

For adults the maximum amount of paracetamol intake allowed is 1 gram (1000 mg) per dose and 4 grams (4000 mg) per day.

Children under 16 need to take a lower dose, depending on their age or weight.

 For very young children, paracetamol liquid is given using a measuring spoon or oral syringe- the FDA says – never a kitchen spoon.

Facts on Paracetamol:

• Combinations (e.g. with codeine) are better active than paracetamol alone. Known as an opioid, Codeine is a slightly stronger painkiller. Opioid painkillers work like natural pain-reducing chemicals called endorphins.
• Caffeine is added to paracetamol to make it more effective. Caffeine is a mild stimulant that helps reduce fatigue. Caffeine is also thought to enhance the painkilling effect of paracetamol.
• while you are taking Paracetamol + Caffeine combination, avoid drinking lots of caffeine-containing drinks like tea, coffee, cola
• Drug of choice in patients that cannot be treated with non-steroidal anti-inflammatory drugs (NSAID), such as people with bronchial asthma, peptic ulcer disease, hemophilia, salicylate-sensitized people, children under 12 years of age, pregnant or breastfeeding women
• Medindia’s database currently has 4507 Brands of Generics of Paracetamol listed.
• The generic Paracetamol combination is manufactured by 1737 companies in India.
• Paracetamol from Jan Aushadhi provides drug at nominal price almost 25% of the market price of the branded drug but are equivalent in quality and efficacy as expensive branded drugs.

Be Careful:

• Paracetamol is broken down in the liver and excreted by the kidneys. As a result, overdoses commonly lead to liver failure and damaged kidneys.
• Paracetamol is in fact the leading cause of acute liver failure in the western world and is the most overdosed drug in many countries.
• Taking paracetamol with alcohol, even in small amounts, can increase the risk of liver damage and/or kidney disease.
• The World Health Organization recommends that Paracetamol be given to children with fever higher than5°C (101.3°F).

References:

1. Acta Pol Pharm.2014 Jan-Feb;71(1):11-23
2. CNS Drug Reviews, Vol. 12, No. 3–4, 2006