EFFERALGAN ® Paracetamol

EFFERALGAN ® is a paracetamol based drug

THERAPEUTIC GROUP: Analgesics and antipyretic drugs

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications EFFERALGAN ® Paracetamol

EFFERALGAN ® is successfully used both in the symptomatic treatment of mild and moderate acute pain and in the treatment of febrile adult and adolescent conditions.

Mechanism of action EFFERALGAN ® Paracetamol

EFFERALGAN ® is a drug widely used in the clinical setting for significant analgesic and antipyretic effects.

In contrast to classic non-steroidal anti-inflammatory drugs, paracetamol, the active ingredient of EFFERALGAN ®, seems able to carry out a selective inhibitory activity against some cyclo-oxygenases selectively expressed at the level of nervous tissue and known as COX 3.

The inhibition of these enzymes results in a significant decrease of some prostaglandins and other chemical mediators such as PGE2 and bradykinin involved respectively in the onset of fever, thanks to the action performed at the level of hypothalamic thermoregulatory centers, and in the genesis of pain, given the stimulatory action against peripheral nerve endings of nociceptors.

From a pharmacokinetic point of view, on the other hand, following oral administration, paracetamol is rapidly absorbed in the gastrointestinal tract and subjected to a first-pass hepatic metabolism which reduces its bioavailability by about 30%.

Linked to plasma proteins, paracetamol is distributed to various tissues, managing to permeate both the placenta and the blood-brain barrier, and thus fulfilling its therapeutic function.

After a half-life of about 1-3 hours and after having been metabolized again to the hepatic level, mainly glucuronate is excreted through the urine.

Studies carried out and clinical efficacy

1. THE PARACETAMOL IN THE TREATMENT OF RENAL COLICAS

Emerg Med J. 2011 Dec 20.

Interesting clinical study demonstrating that treatment with paracetamol intravenous may be particularly effective in the treatment of colic pain associated with renal colic, in a similar way to that done by morphine.

2. THE PARACETAMOL IN CRITICAL ILLNESSES

Crit Care Resusc. 2012 Mar; 14 (1): 74-80.

An interesting review that shows that despite the fact that paracetamol is used clinically very frequently in critically ill patients, there are still no statistically significant clinical trials capable of validating the effectiveness of this treatment.

3. ACETYLCISTEIN IN PARACETAMOL OVERS

Curr Pharm Biotechnol. 2012 Feb 20.

Study supporting the efficacy and safety of acetylcysteine in preventing liver damage associated with paracetamol overdose. For treatment to be effective, reducing mortality from liver failure as well, it is important to maintain it for 21 to 72 hours.

Method of use and dosage

EFFERALGAN ®

Tablets for oral use of 500 mg paracetamol

In adults it is generally recommended to take one tablet 3-4 times a day, and only if this dosage is not sufficient to guarantee an effective therapeutic action could the dose be increased up to a maximum of 6 tablets per day.

In adolescents between the ages of 13 and 15 the maximum dose is 3 tablets per day.

Warnings EFFERALGAN ® Paracetamol

Although EFFERALGAN ® is a salable drug without a prescription, it would be advisable to consult your doctor before taking it.

Particular attention should be maintained by patients suffering from liver and kidney diseases, given the increased risk of side effects and poisoning, both acute and chronic.

In any case, treatment with paracetamol should be understood as a therapy limited in time, useful for overcoming acute episodes of pain.

The EFFERALGAN ® based therapy should not exceed 3 days of treatment, and if there were no appreciable results it would be appropriate to suspend therapy and consult your doctor.

PREGNANCY AND BREASTFEEDING

The ability of paracetamol to selectively inhibit the cyclooxygenase nerve isoforms involved in the genesis of pain and fever, without thereby causing a sharp decline in total prostaglandins, greatly limits the risk of important side effects on the fetus.

In fact, different studies show that taking paracetamol during pregnancy, according to the appropriate medical indications, is not associated with the appearance of fetal malformations or recurrent abortions as documented for non-steroidal anti-inflammatory drugs.

In light of these findings, and given the low concentrations of paracetamol present in breast milk, the intake of EFFERALGAN ® in pregnancy should take place under strict medical supervision.

Interactions

Patients undergoing paracetamol therapy should pay particular attention to the simultaneous intake of:

Alcohol, due to increased liver toxicity of paracetamol;
Diuretics, ACE inhibitors, angiotensin II antagonists, methotrexate and cyclosporin, given the ability to enhance the hepatotoxic and nephrotoxic effects of paracetamol;
Active ingredients capable of altering gastric motility, due to the ability to significantly vary the absorption of paracetamol;
Antibiotics and substrates of cytochromial enzymes, as they can alter the normal pharmacokinetic and pharmacodynamic properties of paracetamol;
NSAIDs and opioids, given the increased analgesic effect of their interaction.

Contraindications EFFERALGAN ® Paracetamol

The use of EFFERALGAN ® is contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, hepatic and renal insufficiency, high grade haemolytic anemia and glucose 6 phosphate dehydrogenase enzyme deficiency.

Undesirable effects - Side effects

The intake of paracetamol, especially when carried out for prolonged periods of time or at particularly high doses, could facilitate the appearance of adverse reactions such as:

Thrombocytopenia, neutropenia and leukopenia with its consequences;
Diarrhea and abdominal pain;
Allergic reactions both of cutaneous nature (urticaria, erythema, rash) and vascular (hypotension);
Increased transaminases;
Hepato and nephrotoxicity.

It is also very important to consider the high risk of paracetamol intoxication, especially in hepatic and nephropathic patients, in which the side effects could be clinically relevant.