pseudoephedrine/fexofenadine

Action and Spectrum

Actions and Spectrum:

fexofenadine is an antihistamine, whereas pseudoephedrine is a decongestant.

By constricting the blood vessels in the nasal passages, pseudoephedrine serves to lessen oedema and congestion. By doing so, you can ease nasal congestion brought on by colds, the flu, or allergies.

Histamine, a chemical the body releases in reaction to allergens, is what fexofenadine does to function. fexofenadine relieves allergy symptoms like runny nose, sneezing, itching, and watery eyes by inhibiting histamine

The upper respiratory system is the primary target of pseudoephedrine/fexofenadine’s spectrum of activity, while other bodily systems are not significantly impacted.

It is crucial to be aware that this drug may have adverse effects, including nausea, dry mouth, sleeplessness, and dizziness.

Drug Interaction

Adverse Reaction

Frequency not defined

CNS depression

Muscular weakness

Early menses

Faintness

Paresthesia

Blurred vision

Diplopia; tinnitus

Sedation ranging from mild drowsiness to deep sleep

Delirium, palpitation, seizures is less common

Disturbed coordination

Insomnia

Chills

Agranulocytosis

Tremors

Hepatic function abnormality, jaundice is rare

Tachycardia, palpitation ECG changes (eg, widened QRS)

Toxic psychosis

Lassitude

Thrombocytopenia

Dysmenorrhea

Acute labyrinthitis

Nausea

Vomiting

Cholestasis, hepatitis, hepatic failure

Facial dyskinesia

Tightness of the chest

Thickening of bronchial secretions

Arrhythmias (e.g., extrasystole, heart block)

Hypotension

Urinary retention

Impotence

Vertigo

Visual disturbances

Hypertension

Sweating

Diarrhea

Dizziness, sedation, and hypotension may occur in geriatric patients

Dryness of mouth, nose, and throat

Hemolytic anemia

Leukopenia

Fatigue

Dysuria

Restlessness, euphoria, nervousness

Wheezing

Nasal stuffiness

Epigastric distress

Ischemic colitis

Anorexia

Pancytopenia

Constipation

1-10%

Otitis media (2.5%)

Drowsiness (1.3%)

Fatigue (1.3%)

Myalgia (3%)

Vomiting (8%)

Somnolence (1.5%)

Dizziness (2%)

Dyspepsia (1.2%)

Headache (7.2%)

Diarrhea (3%)

Black Box Warning

Black Box Warning

The usage of the pseudoephedrine/ fexofenadine combination medication has no black box warning.

Contraindication / Caution

Contraindication/Caution:

Contraindication:

• People who are hypersensitive to any ingredient in the drug should not use pseudoephedrine/fexofenadine.
• People with severe hypertension, severe coronary artery disease, narrow-angle glaucoma, or urine retention shouldn’t use it.
• People who have taken a monoamine oxidase inhibitor (MAOI) during the last 14 days should not use the drug.

Caution:

• Patients with mild to severe hypertension, cardiovascular illness, diabetes, hyperthyroidism, prostatic hypertrophy, or renal impairment should use pseudoephedrine/fexofenadine with caution.

medication should also be used with caution in individuals who are pregnant or breastfeeding.

Pregnancy / Lactation

Pregnancy warnings:   

Pregnancy category: N/A

Lactation: Excretion into human milk is unknown

Pregnancy Categories:     

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

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

fexofenadine, a second-generation antihistamine, works as an inverse agonist at the H1 receptor, while pseudoephedrine, a sympathomimetic medication, functions as a nasal decongestant.

pseudoephedrine causes vasoconstriction, which reduces edema and congestion in the nasal passages, by activating alpha-adrenergic receptors in the nasal mucosa. The beta-adrenergic action of pseudoephedrine also contributes to its minor broncho dilatory effects.

fexofenadine prevents histamine-mediated allergic responses by specifically inhibiting histamine’s ability to bind to H1 receptors. When opposed to first-generation antihistamines, fexofenadine has fewer sedative effects since it does not penetrate the blood-brain barrier.

Pharmacodynamics

A sympathomimetic medication called pseudoephedrine causes vasoconstriction and reduces oedema and congestion in the nasal passages by activating alpha-adrenergic receptors in the nasal mucosa.

fexofenadine has negligible sedative effects since it struggles to cross the blood-brain barrier. fexofenadine has a lengthy duration of action and can successfully treat allergic rhinitis’s symptoms, such as itching, sneezing, and nasal congestion.

Pharmacokinetics

Absorption

For pseudoephedrine

Peak plasma concentrations of pseudoephedrine are reached within 1 to 2 hours after oral dosing due to its quick and efficient absorption from the digestive system. pseudoephedrine’s absorption can be slowed down by food.

For fexofenadine

In addition to being highly absorbed from the digestive system, fexofenadine very quickly reaches its peak plasma concentrations when taken orally. Fruit juice and meals can impair the bioavailability of fexofenadine by reducing absorption.

Distribution

For pseudoephedrine

pseudoephedrine is widely distributed and has a 90% protein binding efficiency. Pseudoephedrine is secreted in breast milk after passing through the placenta and the blood-brain barrier.

For fexofenadine

About 60 to 70% of fexofenadine is strongly linked to plasma proteins and is widely distributed in the body. Fexofenadine has negligible sedative effects since it has a difficult time crossing the blood-brain barrier.

Metabolism

For pseudoephedrine

pseudoephedrine is extensively metabolized to its active metabolite, nor pseudoephedrine, in the liver by cytochrome P450 (CYP) enzymes, notably CYP2D6. pseudoephedrine has an elimination half-life of around 6 hours.

For fexofenadine

The liver little processes fexofenadine, and it is mainly eliminated in the feces intact. The half-life of fexofenadine is around 14 hours.

Elimination and excretion

For pseudoephedrine

About 44 to 96% of the dosage of pseudoephedrine is excreted unaltered in the urine, where it is largely removed. pseudoephedrine is little excreted in the feces.

For fexofenadine

Less than 5% of the dosage of fexofenadine is excreted in the urine and most of it is found in the faeces. The liver little processes fexofenadine, and it is mainly eliminated in the feces intact.

Adminstartion

Administration:

Tablets of pseudoephedrine/fexofenadine are available and are used orally.

Adults should take one tablet of pseudoephedrine/fexofenadine twice a day, with or without meals. The pill shouldn’t be chewed or mashed; it should be consumed whole with water.

It’s essential to adhere to the dosage guidelines and not go above the daily maximum of two pills.

Because pseudoephedrine/fexofenadine has a stimulant impact on the central nervous system, it is crucial to avoid taking at bedtime.

Patient Information Leaflet

Patient information leaflet

Generic Name: pseudoephedrine/fexofenadine

Why do we use pseudoephedrine/fexofenadine?

A combination drug called pseudoephedrine/fexofenadine is used to treat symptoms of seasonal allergies and nasal congestion, including:

Sneezing, clogged nose, nasal blockage, scratchy throat, nose, eyes, moist eyes and sinus tension

A decongestant called pseudoephedrine works by constricting the blood vessels in the nasal passages, which lessens swelling and congestion.

An antihistamine, such as fexofenadine, inhibits the effects of histamine, which the body releases in reaction to allergens and is what causes the symptoms of allergies.