D-Isoephedrine
D-Isoephedrine Uses, Dosage, Side Effects, Food Interaction and all others data.
D-Isoephedrine is structurally related to ephedrine but exerts a weaker effect on the sympathetic nervous system. Both drugs naturally occur in in ephedra plant which have a history of use in traditional Eastern medicine and were first researched in the west in 1889. The decongestant effect of pseudoephedrine was described in dogs in 1927.
D-Isoephedrine causes vasoconstriction which leads to a decongestant effect. It has a short duration of action unless formulated as an extended release product. Patients should be counselled regarding the risk of central nervous system stimulation.
| Trade Name | D-Isoephedrine |
| Availability | Rx and/or OTC |
| Generic | Pseudoephedrine |
| Pseudoephedrine Other Names | d-Isoephedrine, d-Pseudoephedrine, Isoephedrine, Pseudoefedrina, pseudoéphédrine, Pseudoephedrine, Pseudoephedrinum |
| Related Drugs | epinephrine topical, sodium chloride nasal, phenylephrine nasal, Afrin, doxylamine |
| Type | |
| Formula | C10H15NO |
| Weight | Average: 165.2322 Monoisotopic: 165.115364107 |
| Protein binding | -pseudoephedrine is 6.6±0.4% bound to human serum albumin and 22.5±3.2% protein bound in serum. +pseudoephedrine is 6.7±1.2% protein bound to human serum albumin and 25.4±3.9% protein bound in human serum. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
D-Isoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.
D-Isoephedrine is a sympathomimetic amine used for its decongestant activity.
D-Isoephedrine is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Allergies, Common Cold, Common Cold Associated With Cough, Common Cold/Flu, Cough, Cough caused by Common Cold, Eye allergy, Fever, Flu caused by Influenza, Headache, Irritative cough, Nasal Allergies, Nasal Congestion, Nasal Congestion caused by Common Cold, Pain, Perennial Allergy, Priapism, Respiratory Allergy, Rhinorrhoea, Seasonal Allergic Rhinitis, Seasonal Allergies, Sinus Congestion, Sinusitis, Sneezing, Sore Throat, Symptoms of Acute Bronchitis Accompanied by Coughing, Throat irritation, Upper Respiratory Tract Infection, Upper respiratory tract congestion, Upper respiratory tract signs and symptoms, Dry cough, Minor aches and pains, Sinus pain, Watery itchy eyes, Airway secretion clearance therapy
How D-Isoephedrine works
D-Isoephedrine acts mainly as an agonist of alpha adrenergic receptors and less strongly as an agonist of beta adrenergic receptors.[A10896] This agonism of adrenergic receptors produces vasoconstriction which is used as a decongestant and as a treatment of priapism. D-Isoephedrine is also an inhibitor of norepinephrine, dopamine, and serotonin transporters.
The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria. D-Isoephedrine is also a partial agonist of the anococcygeal muscle. D-Isoephedrine also inhibits NF-kappa-B, NFAT, and AP-1.
Toxicity
The oral LD50 of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.
Patients experiencing an overdose of pseudoephedrine may present with giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty urinating, muscle weakness, muscle tension, anxiety, restlessness, insomnia, toxic psychosis, cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. Treat overdose with symptomatic and supportive treatment including removal of unabsorbed drug.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
D-Isoephedrine Drug Interaction
Moderate: amphetamine / dextroamphetamine, duloxetineMinor: ascorbic acidUnknown: fexofenadine, diphenhydramine, loratadine, ubiquinone, omega-3 polyunsaturated fatty acids, cyclobenzaprine, fluticasone nasal, escitalopram, pregabalin, guaifenesin, montelukast, acetaminophen, cyanocobalamin, cholecalciferol, alprazolam, ondansetron, cetirizine
D-Isoephedrine Disease Interaction
Major: cardiovascular diseaseModerate: GI narrowing, PKU, BPH, diabetes, glaucoma
Volume of Distribution
The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.
Elimination Route
A 240mg oral dose of pseudoephedrine reaches a Cmax of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a Tmax of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng*h/mL fed and 7535.1±333.0ng*h/mL fasted.
Half Life
The mean elimination half life of pseudoephedrine is 6.0h.
Clearance
A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.
Elimination Route
55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.
Innovators Monograph
You find simplified version here D-Isoephedrine
