oxyphenonium

Action and Spectrum

Actions and spectrum: 

Action:  

• Smooth Muscle Relaxation: oxyphenonium’s anticholinergic activity leads to relaxation of smooth muscles in the GIT, genitourinary system, and other organs. This effect helps alleviate muscle spasms and cramps associated with irritable bowel syndrome (IBS) and overactive bladder. 
• Reduced Glandular Secretions: oxyphenonium inhibits the secretion of glands that are under cholinergic control, such as salivary and sweat glands. This can help manage conditions marked by excessive secretions. 
• Heart Rate and Rhythm Effects: oxyphenonium can affect heart rate and rhythm by blocking the effects of acetylcholine on the heart’s muscarinic receptors. This effect is particularly relevant in the treatment of certain arrhythmias. 
• Central Nervous System Effects: oxyphenonium’s anticholinergic properties can also lead to central nervous system effects, including potential sedation and cognitive changes. 

Spectrum:  

• Gastrointestinal System: Relief from gastrointestinal spasms, cramps, and symptoms of conditions like IBS. 
• Genitourinary System: Management of overactive bladder symptoms and urinary urgency. 
• Cardiovascular System: Influence on heart rate and rhythm, potentially used in certain arrhythmias. 
• Salivary Glands: Reduction of excessive salivation. 
• Sweating: Inhibition of sweat gland secretions. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Vomiting 

Flatulence 

Abdominal pain 

Epigastric pain 

Constipation 

Nausea 

Indigestion 

Diarrhea 

Fever 

Sore throat 

Black Box Warning

Black Box Warning: 

There were no black box warnings associated with oxyphenonium. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: oxyphenonium should not be used in individuals with a known hypersensitivity or allergy to the medication or any of its components. 
• Obstructive Conditions: oxyphenonium’s anticholinergic effects can worsen conditions like urinary retention, pyloric stenosis, and obstructive disorders of the gastrointestinal tract. 
• Cardiac Arrhythmias: oxyphenonium’s effects on heart rate and rhythm can be problematic in individuals with certain cardiac arrhythmias, particularly those sensitive to anticholinergic activity. 
• Severe Ulcerative Colitis: oxyphenonium’s anticholinergic effects can delay the emptying of the colon and worsen symptoms in individuals with severe ulcerative colitis. 
• Intestinal Atony: Individuals with decreased gastrointestinal motility or a lack of muscle tone (intestinal atony) should avoid oxyphenonium due to its potential to further reduce motility. 
• Toxic Megacolon: Oxyphenonium should be avoided in cases of toxic megacolon, a life-threatening complication of inflammatory bowel disease characterized by colonic dilation. 
• Preexisting Cognitive Impairment: Anticholinergic medications like oxyphenonium can worsen cognitive impairment in individuals with conditions like dementia. 
• Pregnancy and Lactation: As previously mentioned, oxyphenonium’s safety during pregnancy and lactation is not well established, and its use in these situations should be approached with caution. 

Caution: 

• Elderly Population: Elderly individuals are more susceptible to the anticholinergic effects of oxyphenonium, which can lead to side effects like confusion, memory impairment, constipation, and urinary retention. Dosage adjustments and careful monitoring are often necessary. 
• Pediatric Patients: oxyphenonium’s safety and efficacy in children and infants are limited, and its use in pediatric populations should be guided by a healthcare provider. 
• Cardiovascular Conditions: oxyphenonium can affect heart rate and rhythm, making it important to use caution in individuals with preexisting cardiac conditions, arrhythmias, or cardiovascular diseases. 
• Gastrointestinal Disorders: While oxyphenonium can help manage gastrointestinal spasms, it should be used cautiously in individuals with conditions like pyloric stenosis or obstructive disorders of the gastrointestinal tract. 
• Urinary Retention: Individuals with a history of urinary retention or benign prostatic hyperplasia should use oxyphenonium with caution due to its potential to exacerbate urinary retention. 
• Myasthenia Gravis: Anticholinergic medications like oxyphenonium can worsen symptoms of myasthenia gravis, a neuromuscular disorder characterized by muscle weakness.

Comorbidities: 

• Cardiovascular Conditions: Individuals with cardiovascular diseases, such as congestive heart failure, and arrhythmias, should use oxyphenonium with caution due to its potential to affect heart rate and rhythm. 
• Gastrointestinal Disorders: oxyphenonium is often used to manage gastrointestinal spasms, but it should be used cautiously in individuals with gastrointestinal disorders like gastroesophageal reflux disease (GERD), peptic ulcers, or inflammatory bowel disease. 
• Urinary Conditions: Individuals with urinary conditions like urinary retention, bladder outlet obstruction, or benign prostatic hyperplasia should be cautious when using oxyphenonium due to its potential to worsen urinary symptoms. 
• Respiratory Conditions: oxyphenonium’s anticholinergic effects can lead to respiratory symptoms like dry mouth, throat, and decreased mucus secretion, which may exacerbate respiratory conditions such as chronic obstructive pulmonary disease or asthma. 
• Neurological Disorders: Individuals with neurological disorders such as Parkinson’s disease, epilepsy, or myasthenia gravis should use oxyphenonium with caution due to its potential to worsen symptoms or interact with other medications. 
• Glaucoma: Individuals with a history of glaucoma, especially narrow-angle glaucoma, should avoid oxyphenonium due to its potential to increase intraocular pressure. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

oxyphenonium is an anticholinergic medication that exerts its pharmacological effects by selectively blocking the actions of acetylcholine, a neurotransmitter responsible for various bodily functions. It antagonizes muscarinic receptors, particularly the M1, M2, and M3 subtypes, leading to reduced cholinergic transmission. This results in relaxation of smooth muscles in the gastrointestinal tract and genitourinary system, helping to alleviate spasms and cramps.

Oxyphenonium also decreases glandular secretions, such as saliva and sweat, and can influence heart rate and rhythm. However, its anticholinergic properties can lead to side effects like dry mouth, blurred vision, constipation, and potential cognitive effects. The medication’s use should be tailored to individual patient factors, and its potential benefits should be balanced against the risk of adverse effects.  

Pharmacodynamics: 

• Smooth Muscle Relaxation: oxyphenonium’s blockade of muscarinic receptors in smooth muscle cells causes relaxation of the smooth muscles in the gastrointestinal tract and genitourinary system. This effect helps alleviate spasms, cramps, and discomfort associated with irritable bowel syndrome & overactive bladder. 
• Reduced Glandular Secretions: oxyphenonium inhibits the action of acetylcholine on glands regulated by the parasympathetic nervous system. This leads to a decrease in the secretion of substances like saliva and sweat, helping to manage conditions involving excessive secretions. 
• Cardiovascular Effects: By blocking muscarinic receptors in the heart, oxyphenonium can influence heart rate and rhythm. This effect can be particularly relevant in the treatment of certain arrhythmias. 
• Central Nervous System Effects: oxyphenonium’s anticholinergic properties can also impact the central nervous system, potentially leading to side effects like sedation, drowsiness, and cognitive changes. 
• Ophthalmic Effects: oxyphenonium’s antagonism of muscarinic receptors can cause pupil dilation (mydriasis) and relaxation of the ciliary muscle, leading to blurred vision and potentially exacerbating conditions like glaucoma.

Pharmacokinetics: 

Absorption 

oxyphenonium is typically administered orally as tablets or capsules. After oral administration, it is absorbed through the gastrointestinal tract. The absorption process may be influenced by factors such as the formulation, food intake, and the individual’s gastrointestinal conditions. 

Distribution 

Once absorbed, oxyphenonium is distributed throughout the body via the bloodstream. It can cross blood-brain barrier and distribute to various tissues, including those with smooth muscle and muscarinic receptors, where it exerts its pharmacological effects. 

Metabolism 

oxyphenonium undergoes metabolism primarily in the liver. The exact metabolic pathways and metabolites are not as well-documented as for some other drugs. It is possible that the medication undergoes enzymatic reactions in the liver to be transformed into metabolites that are then eliminated from the body. 

Elimination and excretion 

The elimination of oxyphenonium and its metabolites occurs through the urine. It is eliminated from the body through a combination of renal filtration and active secretion into the urine. The specific excretion pathways and rates can vary based on individual factors. 

Adminstartion

Administration: 

• Dosage: The appropriate dosage of oxyphenonium will be based on age, weight, and other factors. Do not adjust the dosage on your own without consulting your healthcare provider. 
• Timing: oxyphenonium is often taken before meals to help manage gastrointestinal symptoms. It is usually recommended to take it about 30 minutes to 1 hour before eating to allow time for the medication to take effect. 
• Food Interaction: Depending on the formulation and the specific guidance from your healthcare provider, you may need to take oxyphenonium on an empty stomach or with a small amount of food. Follow the instructions provided to ensure optimal absorption and effectiveness. 
• Consistency: Take oxyphenonium at the same time(s) each day as prescribed. This helps maintain consistent levels of the medication in your body. 
• Duration: Follow your healthcare provider’s recommendations regarding the duration of treatment. Do not stop taking oxyphenonium without consulting your healthcare provider, even if your symptoms improve. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: oxyphenonium 

Pronounced: (ox-ee-fen-OH-nee-um)  

Why do we use oxyphenonium? 

• Gastrointestinal Disorders: oxyphenonium is used to manage gastrointestinal spasms and cramps associated with conditions such as irritable bowel syndrome (IBS), functional dyspepsia, and other gastrointestinal motility disorders. It helps relieve abdominal discomfort and pain. 
• Overactive Bladder: oxyphenonium is used to treat overactive bladder, characterized by frequent urination. By relaxing the bladder muscles, it can help reduce urinary urgency and frequency. 
• Excessive Sweating: oxyphenonium’s ability to inhibit glandular secretions is used to manage conditions like hyperhidrosis, which involves excessive sweating. It helps reduce excessive sweating by decreasing sweat production. 
• Salivary and Respiratory Secretions: oxyphenonium can be used to control excessive salivary and respiratory secretions, which can be helpful in medical situations, such as managing drooling or excessive mucus production. 
• Diagnostic Procedures: oxyphenonium may be used to reduce gastrointestinal and respiratory secretions during diagnostic procedures, such as bronchoscopy or endoscopy, to improve visualization.