D-Isoephedrine - General Information
An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. [PubChem]
Pharmacology of D-Isoephedrine
D-Isoephedrine is a sympathomimetic agent, structurally similar to ephedrine, used to relieve nasal and sinus congestion and reduce air-travel-related otalgia in adults. The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations either as single-ingredient preparations, or more commonly in combination with antihistamines and/or paracetamol/ibuprofen. Unlike antihistamines, which modify the systemic histamine-mediated allergic response, pseudoephedrine only serves to relieve nasal congestion commonly associated with colds or allergies. The advantage of oral pseudoephedrine over topical nasal preparations, such as oxymetazoline, is that it does not cause rebound congestion (rhinitis medicamentosa).
D-Isoephedrine for patients
PSEUDOEPHEDRINE - ORAL
IMPORTANT NOTE: The following information is intended to supplement, not substitute for, the expertise and judgment of your
physician, pharmacist or other healthcare professional. It should not be construed to indicate that use of the drug is safe,
appropriate, or effective for you. Consult your healthcare professional before using this drug.
PSEUDOEPHEDRINE - ORAL
COMMON BRAND NAME(S): Afrin, Afrinol, Chlor-Trimeton, Novafed, Sudafed
Pseudoephedrine is used to provide relief from the nasal or sinus congestion caused by allergies or the common cold, or ear
congestion caused by inflammation or infection.
HOW TO USE:
It is recommended to drink plenty of fluids while taking this medication, unless your doctor instructs you to do otherwise.
Sustained-release or long acting tablets and capsules must be swallowed whole. Chewing or crushing them will destroy the long
action and may increase side effects.
If symptoms do not improve after 7 days or are accompanied by a high fever, notify your doctor. Do not increase the dose or take
this more frequently than recommended.
Mild stomach upset, trouble sleeping, dizziness, headache, nervousness, or loss of appetite may occur. If any of these effects
persist or worsen, notify your doctor or pharmacist promptly.
Tell your doctor immediately if any of these unlikely but serious side effects occur: fast/irregular heartbeat, difficulty urinating,
uncontrolled shaking or tremor.
Tell your doctor immediately if any of these rare, but very serious side effects occur: seizures, chest pain, mental/mood changes.
A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious
allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.
If you notice other effects not listed above, contact your doctor or pharmacist.
Before taking pseudoephedrine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: pre-existing heart problems, kidney
or liver disease, lung disease, emphysema, high blood pressure, overactive thyroid, diabetes mellitus, glaucoma, difficulty urinating
or an enlarged prostate, history of seizures.
This drug should be used only if clearly needed during pregnancy. Discuss the risks and benefits with your doctor.
Pseudoephedrine passes into breast milk and may have undesirable effects on a nursing infant. Using this drug while breast-feeding is
Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use,
especially of: sleeping pills, sedatives, tranquilizers, muscle relaxants, medication for depression, high blood pressure drugs.
Tell your doctor if you have taken any MAO inhibitors (e.g., furazolidone, phenelzine, selegiline, tranylcypromine) within the last
If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national
poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. Symptoms of overdose may
include irregular or unusually slow or rapid heartbeat, unusual nervousness or excitement, rapid breathing, confusion, hallucinations,
Talk with your doctor, pharmacist or nurse about diseases you have and drugs you are already taking before using any new medication.
If you miss a dose, take it as soon as remembered if within an hour. If you do not remember until later, skip the missed dose and resume
your usual dosing schedule. Do not "double-up" the doses.
Store at room temperature between 59 and 86 degrees F (between 15 and 30 degrees C) away from moisture and sunlight. Do not store in the
bathroom. Keep all medicines away from children and pets.
MAO inhibitors and beta adrenergic blockers increase the effects of pseudoephedrine. Sympathomimetics may reduce the antihypertensive effects of methyldopa, mecamylamine, reserpine and veratrum alkaloids.
Patients with severe hypertension, severe coronary artery disease, and patients on MAO inhibitor therapy. Also contraindicated in patients with hypersensitivity or idiosyncrasy to sympathomimetic amines which may be manifested by insomnia, dizziness, weakness, tremor or arrhythmias.
Children under 12: Should not be used by children under 12 years.
Nursing Mothers: Contraindicated because of the higher than usual risk for infants from sympathomimetic amines.
Additional information about D-Isoephedrine
D-Isoephedrine Indication: For the treatment of nasal congestion, sinus congestion, Eustachian tube congestion, and vasomotor rhinitis, and as an adjunct to other agents in the optimum treatment of allergic rhinitis, croup, sinusitis, otitis media, and tracheobronchitis. Also used as first-line therapy of priapism.
Mechanism Of Action: D-Isoephedrine acts directly on both alpha- and, to a lesser degree, beta-adrenergic receptors. Through direct action on alpha-adrenergic receptors in the mucosa of the respiratory tract, pseudoephedrine produces vasoconstriction. D-Isoephedrine relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect.
Drug Interactions: Alseroxylon Increased arterial pressure
Isocarboxazid Increased arterial pressure
Linezolid Possible increase of arterial pressure
Methyldopa Increased arterial pressure
Bromocriptine The sympathomimetic increases the toxicity of bromocriptine
Tranylcypromine Increased arterial pressure
Midodrine Increased arterial pressure
Moclobemide Moclobemide increases the sympathomimetic effect
Pargyline Increased arterial pressure
Phenelzine Increased arterial pressure
Rasagiline Increased arterial pressure
Reserpine Increased arterial pressure
Trimipramine The tricyclic increases the sympathomimetic effect
Protriptyline The tricyclic increases the sympathomimetic effect
Nortriptyline The tricyclic increases the sympathomimetic effect
Amitriptyline The tricyclic increases the sympathomimetic effect
Amoxapine The tricyclic increases the sympathomimetic effect
Clomipramine The tricyclic increases the sympathomimetic effect
Imipramine The tricyclic increases the sympathomimetic effect
Desipramine The tricyclic increases the sympathomimetic effect
Doxepin The tricyclic increases the sympathomimetic effect
Deserpidine Increased arterial pressure
Guanethidine The agent decreases the effect of guanethidine
Food Interactions: Not Available
Generic Name: Pseudoephedrine
Synonyms: Not Available
Drug Category: Adrenergic Agents; Vasoconstrictor Agents; Bronchodilator Agents; Central Nervous System Agents; Sympathomimetics
Drug Type: Small Molecule; Approved
Absorption: Pseudoephedrine is readily and almost completely absorbed from the GI tract and there is no evidence of first-pass metabolism.
Toxicity (Overdose): Common adverse reactions include nervousness, restlessness, and insomnia. Rare adverse reactions include difficult/painful urination, dizziness/lightheadedness, heart palpitations, headache, increased sweating, nausea/vomiting, trembling, troubled breathing, unusual paleness, and weakness.
Protein Binding: Pseudoephedrine does not bind to human plasma proteins over the concentration range of 50 to 2000 ng/mL
Half Life: 9-16 hours
Dosage Forms of D-Isoephedrine: Tablet Oral
Tablet, extended release Oral
Chemical IUPAC Name: (1S,2S)-2-methylamino-1-phenylpropan-1-ol
Chemical Formula: C10H15NO
Pseudoephedrine on Wikipedia: https://en.wikipedia.org/wiki/Pseudoephedrine
Organisms Affected: Humans and other mammals