pseudoephedrine

Actions and spectrum: 

pseudoephedrine is a sympathomimetic drug that acts primarily as a nasal decongestant. It constricts the blood vessels in the nasal passages, reducing swelling and congestion. pseudoephedrine also has mild stimulant effects, like other sympathomimetic drugs. 

The spectrum of pseudoephedrine’s action focuses on the respiratory system, particularly the nasal passages. It helps relieve nasal congestion associated with conditions such as the common cold, allergies, and sinusitis.

pseudoephedrine can also be found with other active ingredients in over-the-counter medications to relieve cold and allergy symptoms. 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Black Box Warning: 

pseudoephedrine does not have a specific black box warning. 

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: pseudoephedrine should not be used in individuals who have a known hypersensitivity or allergy to the medication. 
• Severe hypertension: pseudoephedrine can increase blood pressure and should be avoided in individuals with severe hypertension (high blood pressure). 
• Severe coronary artery disease: pseudoephedrine can stimulate the cardiovascular system and may worsen symptoms in individuals with severe coronary artery disease. 
• Severe cardiovascular disorders: Individuals with certain cardiovascular disorders, such as arrhythmias, tachycardia, or heart disease, should use caution when using pseudoephedrine, as it can increase heart rate and blood pressure. 
• Severe hyperthyroidism: pseudoephedrine may exacerbate symptoms in individuals with severe hyperthyroidism (overactive thyroid). 
• Closed-angle glaucoma: pseudoephedrine can cause pupil dilation and may worsen symptoms in individuals with closed-angle glaucoma. 
• Prostatic hypertrophy: pseudoephedrine can cause urinary retention and should be used with caution in individuals with prostatic hypertrophy (enlarged prostate).

Caution: 

• Hyperthyroidism: pseudoephedrine can worsen symptoms in individuals with hyperthyroidism, as it can increase heart rate and blood pressure. Close monitoring is advised in such cases. 
• Prostate problems: pseudoephedrine can cause urinary retention and may worsen symptoms in individuals with prostatic hypertrophy (enlarged prostate). It should be used with caution in these individuals. 
• Glaucoma: pseudoephedrine can cause pupil dilation and may worsen symptoms in individuals with glaucoma, especially closed-angle glaucoma. It is important to consult with an eye specialist before using pseudoephedrine. 
• Elderly population: Elderly individuals may be more susceptible to the cardiovascular side effects of pseudoephedrine. Close monitoring and appropriate dosage adjustments may be necessary. 
• Pregnancy and breastfeeding: pseudoephedrine should be used with caution during pregnancy and breastfeeding. It is important to consult with a healthcare professional for advice regarding its use in these situations. 

 

Comorbidities: 

• Cardiovascular disease: pseudoephedrine can increase heart rate and blood pressure, which may be problematic for individuals with hypertension, coronary artery disease, or arrhythmias. 
• Diabetes: pseudoephedrine can affect blood sugar levels and may interfere with diabetic medications. Individuals with diabetes should closely monitor their blood sugar levels before using pseudoephedrine. 
• Thyroid disorders: pseudoephedrine may exacerbate symptoms in individuals with hyperthyroidism, as it can increase heart rate and blood pressure. Close monitoring is advised in such cases. 
• Prostate problems: pseudoephedrine can cause urinary retention and may worsen symptoms in individuals with prostatic hypertrophy (enlarged prostate). It should be used with caution in these individuals. 
• Glaucoma: pseudoephedrine can cause pupil dilation and may increase intraocular pressure, which can be problematic for individuals with glaucoma, especially closed-angle glaucoma. It is important to consult with an eye specialist before using pseudoephedrine. 
• Seizure disorders: pseudoephedrine may lower the seizure threshold and potentially increase the risk of seizures in individuals with epilepsy or other seizure disorders. 

Pregnancy consideration: US FDA pregnancy category: Not assigned 

Lactation: Excreted into human milk: Yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology: 

pseudoephedrine is a sympathomimetic amine that acts primarily as a nasal decongestant. It belongs to the class of drugs known as alpha- and beta-adrenergic agonists. The exact mechanism of action of pseudoephedrine is not fully understood, but it is believed to stimulate alpha-adrenergic receptors in the nasal mucosa, leading to vasoconstriction and reduction of nasal congestion. 

pseudoephedrine also has indirect effects on the release of norepinephrine from nerve terminals, which further contributes to its decongestant activity. It has minimal direct effects on beta-adrenergic receptors.  

Pharmacodynamics: 

The pharmacodynamics of pseudoephedrine involve its interactions with adrenergic receptors, particularly alpha-adrenergic receptors. pseudoephedrine is a sympathomimetic amine that exhibits both direct and indirect effects on adrenergic receptors. 

pseudoephedrine acts as an alpha-adrenergic agonist, primarily targeting the alpha-1 receptors in the nasal mucosa. By binding to these receptors, it causes vasoconstriction and reduces the swelling of nasal tissues, leading to decongestion.  

Pharmacokinetics: 

Absorption 

pseudoephedrine is well absorbed from the gastrointestinal tract after oral administration. Its absorption is rapid, with peak plasma concentrations achieved within 1-2 hours. However, it undergoes extensive first-pass metabolism in the liver, leading to a lower bioavailability compared to the administered dose. 

Distribution 

pseudoephedrine is widely distributed throughout the body. It has a moderate volume of distribution, indicating that it distributes into the tissues beyond the plasma. It can cross the blood-brain barrier and placenta, and it is also found in breast milk. 

Metabolism 

pseudoephedrine undergoes hepatic metabolism primarily through the process of N-demethylation. The major metabolite formed is norephedrine (phenylpropanolamine), which also exhibits sympathomimetic activity. Other minor metabolites include p-hydroxyephedrine and p-hydroxynorephedrine. These metabolites are conjugated and eliminated in the urine. 

Elimination and excretion 

The elimination half-life of pseudoephedrine is 4-8 hours. It is primarily excreted unchanged or as metabolites in the urine. 40-50% of the dose is excreted unchanged, while the rest is eliminated as metabolites. 

Administration: 

pseudoephedrine is commonly available in oral formulations, such as tablets, capsules, or liquid. The specific instructions for administration may vary depending on the brand and dosage form of the medication. 

• Read the package instructions: Carefully read the label or package insert for dosing instructions, warnings, and precautions specific to the product you are using. 
• Oral administration: pseudoephedrine is usually taken orally with water. Swallow the tablet or capsule whole, without crushing or chewing, unless otherwise directed. 
• Timing of administration: pseudoephedrine is typically taken every 4 to 6 hours as needed for relief of nasal congestion. It is important to follow the recommended dosing schedule and not exceed the maximum daily dose. 
• Food and drink: pseudoephedrine can be taken with or without food. However, taking it with food may help reduce stomach upset. 
• Avoid late evening or nighttime use: pseudoephedrine is a stimulant and can cause sleep disturbances or insomnia. It is recommended to avoid taking pseudoephedrine close to bedtime to minimize the effect. 

Patient information leaflet 

Generic Name: pseudoephedrine 

Pronounced: (soo-doh-eh-FED-rin)  

Why do we use pseudoephedrine? 

pseudoephedrine is a decongestant commonly used to temporarily relieve nasal congestion associated with allergies, hay fever, sinus congestion, and the common cold. It acts by narrowing blood vessels in nasal passages, which helps to reduce congestion and swelling. 

The main uses of pseudoephedrine include: 

• Nasal congestion relief: pseudoephedrine effectively relieves nasal congestion caused by various conditions, such as allergies, sinusitis, and the common cold. It helps to clear nasal passages, making breathing easier. 
• Sinus congestion relief: pseudoephedrine can help relieve sinus congestion, often characterized by pressure and pain in the sinuses. By reducing nasal swelling, it helps to alleviate discomfort and promote sinus drainage.