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
D-Isoephedrine
D-Isoephedrine

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.

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

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0002279
http://classyfire.wishartlab.com/tax_nodes/C0002811
http://classyfire.wishartlab.com/tax_nodes/C0002811
http://classyfire.wishartlab.com/tax_nodes/C0003899
http://classyfire.wishartlab.com/tax_nodes/C0001661
http://classyfire.wishartlab.com/tax_nodes/C0001897
http://classyfire.wishartlab.com/tax_nodes/C0002228
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0003073
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:51209
http://www.genome.jp/dbget-bin/www_bget?cpd:C02765
http://www.hmdb.ca/metabolites/HMDB0001943
http://www.genome.jp/dbget-bin/www_bget?drug:D08449
http://www.genome.jp/dbget-bin/www_bget?cpd:C02765
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=7028
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508190
https://www.chemspider.com/Chemical-Structure.6761.html
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=8896
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=51209
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1590
https://zinc.docking.org/substances/ZINC000000020259
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000195
http://www.pharmgkb.org/drug/PA451170
http://www.rxlist.com/cgi/generic/sudafed.htm
https://www.drugs.com/pseudoephedrine.html
https://en.wikipedia.org/wiki/Pseudoephedrine
*** Taking medicines without doctor's advice can cause long-term problems.
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