Paracetamol – Effect, Application & Risks

The first production of paracetamol as a reduction product of p-nitrophenol took place in 1878. The substance was used for the first time in medicine in 1887 by the German physician Josef von Mering (1849-1908), which, however, did not attract any attention. For the time being, paracetamol was not used in medicine.

This only changed after World War II. In 1948, the pharmacologists Bernard B. Brodie (1907-1989) and Julius Axelrod (1912-2004) discovered paracetamol a second time as a breakdown product of the substance phenacetin, which was used as a painkiller. The two scientists conducted research on new painkillers in New York on behalf of the American government and discovered that the analgesic effect of phenacetin and acetanilide was entirely due to paracetamol. Therefore, they recommended using paracetamol in its pure form because of the toxic side effects of the two substances.

In 1955, paracetamol was finally used in the USA for the first time as a finished drug. It has been available in tablet form since 1956. The painkiller entered the German market in 1959 as a mono-preparation called ben-u-ron. In 1977, the World Health Organization (WHO) included paracetamol in its list of essential medicines.

Medical application

As a finished drug, paracetamol is used to treat mild to moderate pain . These include:

• slight headache

• migraine

• osteoarthritis-related joint pain

• menstrual pain

• mild toothache

• sunburn

• earache

• Sore throat

• back pain

• lumbago

• Post-vaccination pain

• Fever

In addition, paracetamol can be combined with caffeine to treat mild to moderate pain. In this way, paracetamol achieves a 1.3 to 1.7 times greater effect than if the active substance were administered as a single preparation. In addition, the dose of paracetamol can be reduced.

Furthermore, the onset of the effect of the drug is accelerated by the caffeine. A further increase in effectiveness can be achieved by combining paracetamol and caffeine with acetylsalicylic acid (ASA). The DMKG (German Migraine and Headache Society) therefore recommends such a combination as a suitable remedy for the treatment of tension headaches and migraines.

Another possible combination is with tramadol or codeine to treat moderate or severe pain. Medicines for the treatment of feverish colds that are associated with headaches and body aches also contain active ingredients such as cough blockers, expectorants , antihistamines or vitamin C in addition to paracetamol .

mode of action

Paracetamol belongs to the drug group of non-opioid analgesics . In it, it is again assigned to the non-acidic antipyretic substances. In contrast to drugs such as ibuprofen and acetylsalicylic acid , paracetamol does not primarily accumulate in the acutely inflamed tissue, but rather in the brain and spinal cord. At this point, a subform of the enzyme Cox-3, which is responsible for the production of prostaglandins, is inhibited. These are tissue hormones that are important for mediating pain, inflammation and fever.

While acetaminophen is worse at reducing inflammation, it is effective at reducing fever. Paracetamol also affects the endocannabinoid system. This has the property of providing analgesic and calming effects. Another effect is achieved on the serotonin system, which in part affects the heart and circulatory system, the gastrointestinal tract and blood clotting.

To date, it has not been possible to clarify the exact effect of the drug. In the context of scientific studies, however, there were some potentially increasing effects on the organism. These explain the antipyretic and analgesic effects.

dosage and intake

Paracetamol is usually used in tablet form. Babies and young children can also receive suppositories, which are easier to administer than tablets, which are often spat out again. The paracetamol preparations are divided into age groups according to body weight and dosed accordingly. Sometimes the paracetamol is administered by an injection administered by the doctor.

When administered orally, paracetamol reaches its highest concentration in the blood after 30 to 60 minutes. If suppositories are given, this is the case after three to four hours. The drug is excreted by the kidneys. The usual dosage for adult patients is three to four tablets or capsules per day. Before taking it again, a break of 6 to 8 hours is necessary.

The maximum recommended dose must not be exceeded during use. Otherwise there is a risk of liver damage, which can be life-threatening. For adults, the maximum amount of paracetamol is eight tablets containing 500 milligrams of the active ingredient, which is 4 grams per day. For children, the maximum dose is lower depending on their age. The recommended paracetamol dose for them is a maximum of 10 to 15 milligrams per kilogram of body weight. The daily upper limit was set at 50 milligrams per kilo of body weight.

Forms, groups and active ingredients

Paracetamol is divided into monopreparations and combination preparations. The active ingredient is contained as a single agent in ben-u-ron ®, Parapaed ®, Captin ®, GRIPPEX ®, Perfalgan ® and Enelfa Dr. Henk ®. There are also a variety of generics.

Another group of drugs that contain paracetamol are the combination drugs. These include Thomapyrin ® and Fibrex ® with acetylsalicylic acid, Neopyrin ®, Azur ®, Vivimed ®, Octadon ®, COPYKRAL ® and Prontopyrin ® with caffeine as well as Gelonida ®, Paracetamol comp STADA ®, Nedolon ®, Titretta ®, talvosilen ® and Contraneural ® with codeine. Other combination medications are Buscopan plus ® with butylscopolamine, Zaldiar ® and DOLEVAR ® with tramadol, Doregrippin ® with phenylephrine, Migräne-Neuridal ® , Migräneflux MCP ® and Migräneton ® with metoclopramide. Multiple combinations are also possible.

Herbal, natural and pharmaceutical alternatives

A conceivable alternative to paracetamol are non-steroidal anti-inflammatory drugs such as ibuprofen or the acetylsalicylic acid contained in Aspirin ® . These agents cause greater inhibition of pain. However, their use can also lead to undesirable side effects.It is not always necessary to immediately take a painkiller when you have a headache. Sometimes drinking black coffee with lemon juice or using a herbal remedy such as rubbing in Japanese mint oil or peppermint oil can provide relief.

Drinking plenty of fluids and exercising in the fresh air are also helpful. Cold or warm compresses often help against neck pain instead of paracetamol.

Risks and side effects

In some cases, the use of paracetamol can be associated with risks. The drug should not be administered if the patient suffers from hypersensitivity to the active ingredient or acetaminophen derivatives that are chemically related to paracetamol. The same applies to severe damage to the liver cells.

In addition, in some patients a careful medical assessment of the benefits and risks is required before the drug can be administered. These include severe kidney dysfunction, liver dysfunction, the blood disorder Gilbert-Meulengracht disease and chronic alcohol abuse.

In principle, it can be used during pregnancy and breastfeeding, but it should not be used in high doses or over a long period of time. Paracetamol is generally well tolerated, so undesirable side effects rarely occur. Occasionally, however, negative effects such as allergic reactions, nausea , abdominal pain , haematopoietic disorders, cramped airways, shortness of breath or an increase in liver values ​​are possible.

An overdose of paracetamol is particularly alarming. There is a risk of serious damage to the liver. In larger doses, the drug has been subject to a prescription in Germany since 2008. On the other hand, smaller quantities can still be obtained in pharmacies without any problems. Occasionally, interactions with other medicines can occur due to paracetamol. Among other things, the excretion of the antibiotic chloramphenicol is disturbed.