PHL-bethanechol

PHL-bethanechol Uses, Dosage, Side Effects, Food Interaction and all others data.

PHL-bethanechol is a synthetic ester that was initially synthesized in 1935. As a cholinergic agent, bethanechol is similar in structure and pharmacological function to acetylcholine and is used in specific cases when stimulation of the parasympathetic nervous system is necessary. For example, bethanechol is readily used to treat postoperative or postpartum urinary retention. An advantage of bethanechol is that in contrast to acetylcholine, bethanechol is not degraded by cholinesterase allowing its effects to be longer-lasting.

PHL-bethanechol is selective for muscarinic receptors and has little to no impact on nicotinic receptors. The charged quaternary amine in the structure of bethanechol prevents it from crossing the blood-brain barrier which minimizes central nervous system related adverse effects.

Trade Name PHL-bethanechol
Availability Prescription only
Generic Bethanechol
Bethanechol Other Names Amidopropyldimethylbetaine, Bethanechol
Related Drugs neostigmine, pamabrom, Urecholine, Prostigmin Bromide, Bloxiverz
Type
Formula C7H17N2O2
Weight Average: 161.2221
Monoisotopic: 161.129002798
Groups Approved
Therapeutic Class
Manufacturer
Available Country Canada, United States
Last Updated: September 19, 2023 at 7:00 am
PHL-bethanechol
PHL-bethanechol

Uses

PHL-bethanechol is a muscarinic agonist used to treat postoperative and postpartum nonobstructive functional urinary retention and neurogenic atony of the bladder with retention.

PHL-bethanechol is indicated for the treatment of acute, functional postpartum and postoperative urinary retention. It is also indicated for the treatment of neurogenic atony of the bladder with retention.

PHL-bethanechol is also used to associated treatment for these conditions: Acute post-operative Urinary retention, Neurogenic atony of the urinary bladder, Non-obstructive postpartum urinary retention

How PHL-bethanechol works

PHL-bethanechol is a direct muscarinic agonist and stimulates the parasympathetic nervous system by binding to postganglionic muscarinic receptors.

Though there are 5 types of muscarinic receptors (M1, M2, M3, M4, M5), binding of bethanechol to M3 is most clinically significant since M3 receptors are present in intestinal smooth muscle and the bladder. The cholinergic effects of bethanechol lead to increased detrusor muscle tone to promote bladder emptying and increased smooth muscle tone which restores gastrointestinal peristalsis and motility.

As a result of selectivity for muscarinic receptors, bethanechol produces minimal to no nicotinic effects.

Toxicity

Symptoms of bethanechol overdose include nausea, vomiting, abdominal discomfort, salivation, sweating, and flushing of the skin.

In case of overdose, atropine sulfate is available as an antidote and although subcutaneous administration is preferred, it may be given intravenously in emergencies. In adults, the recommended dose of atropine is 0.6 mg and may be repeated every 2 hours based on the patient’s response. In infants and children up to 12 years of age, the recommended dose of atropine is 0.01 mg/kg (maximum single dose = 0.04 mg) and may be repeated every 2 hours until the desired response is achieved or until adverse effects of atropine limit usage.

In mice, the oral LD50 of bethanechol is 1510 mg/kg.

Food Interaction

  • Take on an empty stomach. Nausea and vomiting may occur if taken after food.

PHL-bethanechol Hypertension interaction

[Major] The use of cholinergic agonists, such as bethanechol and pilocarpine, is contraindicated in patients with pronounced bradycardia, hypotension

Elimination Route

After oral administration of bethanechol, maximum effectiveness of the drug on the bladder and GI tract typically occur after 60-90 minutes; however, effects may present as early as 30 minutes after administration. The duration of action of a typical oral dose of bethanechol is around 1 hour while higher doses (300-400 mg) may be effective for up to 6 hours.

Subcutaneously administered bethanechol produces effects more rapidly after 5-15 minutes with maximum effectiveness achieved after 15-30 minutes. The effects of subcutaneous bethanechol subside within 2 hours of administration.

Innovators Monograph

You find simplified version here PHL-bethanechol

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0004707
http://classyfire.wishartlab.com/tax_nodes/C0000278
http://classyfire.wishartlab.com/tax_nodes/C0000503
http://classyfire.wishartlab.com/tax_nodes/C0004225
http://classyfire.wishartlab.com/tax_nodes/C0002285
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0000323
http://classyfire.wishartlab.com/tax_nodes/C0003865
http://classyfire.wishartlab.com/tax_nodes/C0000117
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0002449
http://classyfire.wishartlab.com/tax_nodes/C0003609
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3084
http://www.hmdb.ca/metabolites/HMDB0015154
http://www.genome.jp/dbget-bin/www_bget?cpd:C06850
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2370
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507707
https://www.chemspider.com/Chemical-Structure.2280.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=39342
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=19257
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=3084
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1482
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000263
http://www.pharmgkb.org/drug/PA448613
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=297
http://www.rxlist.com/cgi/generic3/bethane.htm
https://www.drugs.com/cdi/bethanechol.html
https://en.wikipedia.org/wiki/Bethanechol
*** Taking medicines without doctor's advice can cause long-term problems.
Share