ibuprofen/pseudoephedrine

Action and Spectrum

Actions and Spectrum: 

ibuprofen and pseudoephedrine are two different drugs that are often used together in cold and flu medications. They have different mechanisms of action and can have different effects on the body. 

ibuprofen is a nonsteroidal anti-inflammatory drug that works by reducing inflammation and pain in the body. It acts by inhibiting the production of prostaglandins (PG) which are chemicals that contribute to inflammation and pain. ibuprofen is commonly used to treat a variety of conditions, including headaches, fever, menstrual cramps, and arthritis. 

pseudoephedrine is a decongestant that works by contracting blood vessels in nasal passages, reducing swelling and congestion. This makes it easier to breathe and can relieve symptoms of nasal congestion associated with colds and allergies. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dizziness 

Neutropenia 

Tremor 

GI upset 

Convulsion 

Palpitations 

Insomnia 

Arrhythmia 

Hypertension 

Weakness 

CNS stimulation 

Abdominal pain 

Constipation 

Excitability 

NauseaVomiting 

Anxiety 

Thromboembolism 

Headache 

Hemolytic anemia 

Bronchospasm 

Aplastic anemia 

CHF 

Efoliative dermatitis 

Hepatotoxicity 

Drowsiness 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Allergy: Individuals who are allergic to ibuprofen or pseudoephedrine should not use these medications. 
• Asthma: pseudoephedrine can exacerbate symptoms in individuals with asthma, so it should be avoided in these individuals. 
• Cardiovascular disease: ibuprofen and pseudoephedrine can increase the risk of cardiovascular episodes such as heart attack and stroke, so they should be used with caution in individuals with a history of cardiovascular disease. 
• Gastrointestinal disorders: ibuprofen can cause gastrointestinal bleeding and ulceration, so it should be avoided in individuals with a history of stomach ulcers, bleeding disorders, or other gastrointestinal disorders. 
• High blood pressure: pseudoephedrine can increase blood pressure, so it should be avoided in individuals with uncontrolled hypertension. 
• Pregnancy: ibuprofen and pseudoephedrine should be used with caution in pregnancy and should only be used if the potential benefits outweigh the risks. 
• Breastfeeding: ibuprofen and pseudoephedrine can pass into breast milk and should be used with caution while breastfeeding. 

Caution 

• Age: ibuprofen and pseudoephedrine should be used with caution in elderly individuals and children under the age of 6 years old. 
• Liver and kidney disease: ibuprofen can cause liver and kidney damage and should be used with caution in individuals with pre-existing liver or kidney disease. 
• Dehydration: pseudoephedrine can cause dehydration, caution in individuals who are dehydrated. 
• Other medications: ibuprofen and pseudoephedrine can interact with other medications, including blood thinners, blood pressure medications, and antidepressants. It’s key to speak with a healthcare provider before taking these medications if you are taking other drugs. 
• Duration of use: ibuprofen should only be used for short periods of time, as prolonged use can increase the side effects such as stomach bleeding and ulceration. 
• Overdose: Overdosing on ibuprofen or pseudoephedrine can cause serious side effects, including liver and kidney damage, heart problems, and even death. It’s important to use these medications only as directed and to seek medical attention immediately if you suspect an overdose. 

Pregnancy / Lactation

Pregnancy consideration:  

AU TGA pregnancy category: C 

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Yes. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/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 available 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

Pharmacology: 

ibuprofen is a nonsteroidal anti-inflammatory drug that works by inhibiting the activity of the enzyme cyclooxygenase, which is responsible for the production of prostaglandins. Prostaglandins are chemical messengers in the body that are involved in inflammation, pain, and fever. By inhibiting COX, ibuprofen reduces the production of prostaglandins, which leads to a reduction in inflammation, pain, and fever. 

pseudoephedrine, on the other hand, is a sympathomimetic amine that works by stimulating the sympathetic nervous system. It acts as a decongestant by binding to and activating alpha-adrenergic receptors in the nasal passages. This causes the blood vessels in the nasal passages to constrict, which reduces swelling and congestion and improves airflow. 

Pharmacodynamics: 

Mechanism of action: ibuprofen works by inhibiting the synthesis of prostaglandins, which are produced by the enzymes, cyclooxygenase (COX-1 and COX-2). This action can result in an anti-inflammatory effect. Additionally, ibuprofen may alter lymphocyte activity, inhibit neutrophil aggregation, decrease proinflammatory cytokine activity, and inhibit chemotaxis. 

pseudoephedrine, on the other hand, stimulates the alpha-adrenergic receptors, which leads to bronchodilation and vasoconstriction. This action can help to relieve symptoms such as nasal congestion and improve breathing. 

Pharmacokinetics: 

Absorption 

ibuprofen is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 1-2 hours of oral administration. The bioavailability of ibuprofen is high, with approximately 80-90% of the drug reaching the systemic circulation. 

pseudoephedrine is also rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 1-2 hours of oral administration. The bioavailability of pseudoephedrine is lower than that of ibuprofen, with approximately 30-50% of the drug reaching the systemic circulation. 

Distribution 

ibuprofen is highly bound to plasma proteins, mainly albumin, and has a volume of distribution of approximately 0.1-0.2 L/kg. 

pseudoephedrine, on the other hand, is more lipophilic than ibuprofen and has a larger volume of distribution, ranging from 2.5 to 3 L/kg. 

Metabolism 

The drug undergoes rapid hepatic oxidation, leading to the formation of inactive metabolites. This metabolism primarily occurs through the action of the enzymes CYP2C9 and CYP2C19. 

The drug is metabolized in the liver through a process called N-demethylation, which results in the formation of inactive metabolites. 

Elimination and Excretion 

The half-life of the drug is relatively short, lasting between 2-4 hours. Drug is eliminated from the body through both urine and feces, with approximately 50-60% of the drug excreted in urine and 40-50% excreted in feces. 

Drug has a clearance of approximately 7.3-7.6 mL/min/kg, indicating the volume of blood cleared of the drug per unit time per unit body weight. The primary route of excretion for the drug is through urine, with a range of 43-96% of the drug excreted in this manner. 

Adminstartion

Administration: 

Oral administration 

ibuprofen and pseudoephedrine are typically available as an over-the-counter combination medication in tablet or capsule form. It’s important to read and follow the instructions on the label carefully, and to speak with a healthcare provider before taking these medications if you have other medical conditions or are taking other medications. 

ibuprofen and pseudoephedrine can be taken with or without food, but it’s recommended to take them with a full glass of water to help prevent stomach upset. They should be stored at room temperature (RT), away from heat and moisture, and kept out of the reach of children. 

It’s key to speak with a healthcare provider before taking these medications, especially if you have any underlying medical conditions or are taking other medications. They can provide guidance on the appropriate use of these drugs and help to manage any potential side effects or interactions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ibuprofen/pseudoephedrine 

Pronounced: [ EYE-bue-pro-fen-and-SOO-doe-ee-FED-rin ] 

Why do we use ibuprofen/pseudoephedrine? 

ibuprofen and pseudoephedrine are commonly used in combination to provide relief from symptoms associated with the common cold and flu, such as fever, headache, congestion, and sinus pressure. ibuprofen is a nonsteroidal anti-inflammatory drug that can help to reduce pain and inflammation, while pseudoephedrine is a decongestant that works by contracting blood vessels in the nasal passages to reduce swelling and congestion. 

In addition to cold and flu symptoms, ibuprofen and pseudoephedrine may also be used to treat other conditions, such as: 

• Allergies: pseudoephedrine can help to relieve nasal congestion and sinus pressure associated with allergies. 
• Sinusitis: pseudoephedrine can help to relieve congestion and pressure in the sinuses associated with sinusitis. 
• Menstrual cramps: ibuprofen can help to relieve the pain and inflammation associated with menstrual cramps. 
• Headaches: ibuprofen can help to relieve headaches, including tension headaches and migraines.