Ephedrine

Ephedrine Uses, Dosage, Side Effects, Food Interaction and all others data.

Pseudoephedrine is both an α-and β-adrenergic receptor agonist. It causes vasoconstriction via direct stimulation of α-adrenergic receptors of the respiratory mucosa. It also directly stimulates β-adrenergic receptors causing bronchial relaxation, increased heart rate and contractility.

Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect. This is its main and direct mechanism of action. The displaced noradrenaline is released into the neuronal synapse where it is free to activate the postsynaptic adrenergic receptors.

Ephedrine is a sympathomimetic amine that activates adrenergic receptors, increasing heart rate and blood pressure, and causing bronchodilation. The therapeutic window is wide as patients can be given doses of 5mg up to 50mg. Patients should be counselled regarding the pressor effects of sympathomimetic amines and the risk of tachyphylaxis.

Trade Name Ephedrine
Availability Prescription only
Generic Ephedrine
Ephedrine Other Names Efedrina, Ephedrine, L-Ephedrine
Related Drugs albuterol, dexamethasone, methylprednisolone, midodrine, Ventolin, Xopenex, phenylephrine, Ventolin HFA, norepinephrine, Levophed
Weight 30mg, 15mg, 15mg/5ml,
Type Tablet, Syrup, Intravenous
Formula C10H15NO
Weight Average: 165.2322
Monoisotopic: 165.115364107
Protein binding

(-) Ephedrine is 4.9±0.3% bound to human serum albumin and (+) Ephedrine is 6.9±1.4% bound to human serum albumin.

Groups Approved
Therapeutic Class Decongestant
Manufacturer Karachi Chemical Industries, Ambee Pharmaceuticals Ltd, Essential Drugs Company Ltd, Opsonin Pharma Ltd, Reliance Pharmaceuticals Ltd
Available Country Pakistan, Bangladesh, United States
Last Updated: September 19, 2023 at 7:00 am
Ephedrine
Ephedrine

Uses

Pseudoephedrine is a decongestant of the mucous membranes of the upper respiratory tract, especially the nasal mucosa, sinuses and eustachian tube. It is used for the symptomatic relief of allergic rhinitis (hay fever), vasomotor rhinitis, the common cold, influenza (flu) and ear congestion caused by ear inflammation or infection. Pseudoephedrine can also be used as a bronchodilator.

Pseudoephedrine is a stereoisomer of Ephedrine with similar but less potent pharmacological activity. It has nasal and bronchial decongestant activity.

Ephedrine is also used to associated treatment for these conditions: Allergic Disorder, Bronchial Asthma, Common Cold, Cough, Depression, Fever, General Anesthesia Induced Hypotension, Headache, Joint Pain, Myasthenia Gravis, Narcolepsy, Nasal Congestion, Rhinorrhoea, Sore Throat, Dry cough

How Ephedrine works

Ephedrine is a direct and indirect sympathomimetic amine. Ephedrine activates adrenergic α and β-receptors as well as inhibiting norepinephrine reuptake, and increasing the release of norepinephrine from vesicles in nerve cells. These actions combined lead to larger quantities of norepinephrine present in the synapse, for longer periods of time, increasing stimulation of the sympathetic nervous system. Ephedrine's stimulation of α-1 receptors causes constriction of veins and a rise in blood pressure, stimulation of β-1 adrenergic receptors increase cardiac chronotropy and inotropy, stimulation of β-2 adrenergic receptors causes bronchodilation.

Dosage

Ephedrine dosage

As a decongestant and symptomatic treatment for upper respiratory tract infections the recommended dose is:

Adults: 1 tablet every 4 to 6 hours, up to maximum of 240 mg in 24 hours

Children:

  • 6-12 years of age: 1/2 tablet every 4 to 6 hours daily
  • 2-5 years of age: 1/4 tablet every 4 to 6 hours daily
  • Less than 2 years of age: This drug is not advised unless specifically recommended by a physician.

Side Effects

Serious adverse effects associated with the use of Pseudoephedrine are rare. Symptoms of central nervous system excitation may occur, including sleep disturbances and, rarely, hallucinations have been reported. Skin rashes, with or without irritation, have occasionally been reported.

Toxicity

Patients experiencing an overdose of ephedrine will present with rapidly increasing blood pressure. Manage overdose with blood pressure monitoring, and possibly the administration of parenteral antihypertensives. The LD50 in mice after oral administration is 785mg/kg, after intraperitoneal administration if 248mg/kg, and after subcutaneous administration is 425mg/kg.

Precaution

Although Pseudoephedrine has virtually no pressor effects in normotensive patients, it should be used with caution in patients suffering mild to moderate hypertension. As with other sympathomimetic agents, Pseudoephedrine should be used with caution in patients with hypertension, heart disease, diabetes, hyperthyroidism, elevated intraocular pressure and prostatic enlargement. Caution should be exercised when using the product in the presence of severe hepatic impairment or moderate to severe renal impairment.

Food Interaction

No interactions found.

Volume of Distribution

Oral ephedrine has an average volume of distribution of 215.6L.

Elimination Route

Oral ephedrine reaches an average Cmax of 79.5ng/mL, with a Tmax of 1.81h, and a bioavailability of 88%.

Half Life

Oral ephedrine has a plasma elimination half life of approximately 6 hours, but there is a large degree of inter-patient variability.

Clearance

Oral ephedrine has a clearance of 23.3L/h but there is a high degree of inter-patient variability.

Elimination Route

Ephedrine is mainly eliminated in the urine. Approximately 60% is eliminated as the unmetabolized parent compound, 13% as benzoic acid conjugates, and 1% as 1,2-dihydroxypropylbenzene.

Pregnancy & Breastfeeding use

Although Pseudoephedrine has been in widespread use for many years without apparent ill consequence, there are no specific data on its use during pregnancy. Caution should therefore be exercised by balancing the potential benefit of treatment to the mother against any possible hazards to the developing foetus. Pseudoephedrine is excreted in breast milk in small amounts but the effect of this on breast-fed infants is not known.

Contraindication

Pseudoephedrine is contraindicated in-

  • Hypersensitivity of individuals to this drug
  • Severe hypertension and coronary artery disease
  • Concurrent use of Mono Amine Oxidase Inhibitor (MAOI) drugs

Acute Overdose

As with other sympathomimetic agents, symptoms of overdosage include irritability, restlessness, tremor, convulsions, palpitations, hypertension and difficulty in micturition. Necessary measures should be taken to maintain and support respiration and control convulsions. Gastric lavage should be performed if indicated. If desired, the elimination of Pseudoephedrine can be accelerated by acid diuresis or by dialysis.

Innovators Monograph

You find simplified version here Ephedrine

Ephedrine contains Ephedrine see full prescribing information from innovator Ephedrine Monograph, Ephedrine MSDS, Ephedrine FDA label

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:15407
http://www.genome.jp/dbget-bin/www_bget?cpd:C01575
http://www.hmdb.ca/metabolites/HMDB0015451
http://www.genome.jp/dbget-bin/www_bget?drug:D00124
http://www.genome.jp/dbget-bin/www_bget?cpd:C01575
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=9294
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507538
https://www.chemspider.com/Chemical-Structure.8935.html
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=3966
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=15407
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL211456
https://zinc.docking.org/substances/ZINC000000074836
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000228
http://www.pharmgkb.org/drug/PA449466
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=556
http://www.rxlist.com/cgi/generic/ephedrine.htm
https://www.drugs.com/ephedrine.html
https://en.wikipedia.org/wiki/Ephedrine
*** Taking medicines without doctor's advice can cause long-term problems.
Share