Tag: adverse effects

Pseudoephedrine and the Risk of PRES and RCVS: A New Focus on Patient Safety

It is important to learn about the rare, serious adverse effects of over-the-counter (OTC) medications. Pseudoephedrine, a commonly used decongestant, is one such drug that can have unexpected neurological consequences.

Recent updates in adverse event reports have highlighted the rare but important risks of posterior reversible encephalopathy syndrome (PRES) and reversible cerebral vasoconstriction syndrome (RCVS) associated with pseudoephedrine. Understanding these risks is crucial.

Pseudoephedrine: A Common but Potent OTC Drug

Pseudoephedrine is a sympathomimetic agent that acts by vasoconstricting the blood vessels in the nasal passages, which helps relieve nasal congestion. It is often included in many combination medications for treating the common cold, allergies, and sinus congestion. Pseudoephedrine-containing products have been marketed in Singapore since the 1980s, and no significant safety issues were reported locally until recently. However, overseas cases of rare neurological syndromes linked to pseudoephedrine have been documented, prompting regulatory agencies to enhance warnings and recommendations.

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Dose-dependence of COX-2 selectivity of coxibs

Coxibs are pro-thrombotic, but if given at a high dose, there would be COX-1 inhibition resulting in an antiplatelet effect and hence bleeding would occur. Therefore, would the two effects not cancel each other out, or would the prothrombic effect still be the predominant effect?

The pro-thrombotic effect still dominates since, for coxibs, the COX-2 inhibition is always more than the COX-1 inhibition.

Coxibs are selective inhibitors of COX-2. Selective inhibition of COX-2 results in shunting of the precursor arachidonic acid over to the COX-1 pathway. With COX-2 inhibited and COX-1 functional, there is a relative increase in the ratio of the thromboxane A2 (TXA2) produced via COX-1 to prostaglandin I2 (PGI2) or prostacyclin produced via COX-2, and also in some cell types via COX-1. As TXA2 promotes platelet aggregation, while PGI2 inhibits platelet aggregation, the increased ratio of TXA2 over PGI2 favours platelet aggregation, so there is an increased risk of thrombosis.

Although coxibs are selective for COX-2, the selectivity is dose-dependent. Therefore, at higher doses, there will be more inhibition of COX-1. However, in the case of the balance between the risk of thrombosis versus the risk of bleeding, there is little impact because, as the dose increases, there will still be more inhibition of COX-2 than COX-1. So the ratio of TXA2 to PGI2 remains in favour of thrombosis.

Importantly, the dose-dependence of the selectivity for COX-2 is significant with regards to the gastrointestinal adverse effects. A major advantage of the coxibs is that they have a lower risk of upper gastrointestinal tract (GIT) adverse effects as they do not inhibit COX-1 in the stomach. However, if the dose is increased, there is greater inhibition of COX-1 and, therefore, less sparing from upper GIT adverse effects.

Neuropsychiatric adverse events with leukotriene inhibitors

Neuropsychiatric adverse events are reported in some patients taking leukotriene inhibitors (e.g. montelukast and zileuton)

In 2009, the USA Food and Drug Administration (FDA) reported on an investigation of neuropsychiatric adverse events associated with the leukotriene pathway inhibitors, both the leukotriene receptor antagonists (e.g. montelukast) and the 5-lipoxygenase inhibitor (zileuton) (1).  It was concluded that “reported neuropsychiatric events include postmarket cases of agitation, aggression, anxiousness, dream abnormalities and hallucinations, depression, insomnia, irritability, restlessness, suicidal thinking and behavior (including suicide), and tremor”. The FDA, therefore, issued the following advice to patients and healthcare professionals:

Advice to patients and healthcare professionals

  • Patients and healthcare professionals should be aware of the potential for neuropsychiatric events with these medications.
  • Patients should talk with their healthcare providers if these events occur.
  • Healthcare professionals should consider discontinuing these medications if patients develop neuropsychiatric symptoms.”

Reference:
(1) Updated Information on Leukotriene Inhibitors: Montelukast (marketed as Singulair), Zafirlukast (marketed as Accolate), and Zileuton (marketed as Zyflo and Zyflo CR)

 

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