oxyphencyclimine

Action and Spectrum

Actions and spectrum: 

Action:  

• Smooth Muscle Relaxation: oxyphencyclimine’s anticholinergic effects lead to relaxation of smooth muscles in various organ systems. This effect is particularly useful in treating conditions where excessive smooth muscle contractions cause symptoms such as pain, spasm, or urgency. 
• Decreased Glandular Secretions: By inhibiting acetylcholine’s influence on glandular secretions, oxyphencyclimine can help reduce excessive secretions in organs like the digestive and respiratory tracts. 
• Anti-Spasmodic Effects: oxyphencyclimine’s ability to relax smooth muscles makes it effective in relieving spasms, cramps, and associated discomfort. 
• Reduced Motility: The drug’s impact on smooth muscle function can help slow down gastrointestinal motility, which can be beneficial in certain conditions like irritable bowel syndrome. 

Spectrum:  

• Gastrointestinal Disorders: oxyphencyclimine is used to relieve symptoms of gastrointestinal disorders characterized by spasms, cramps, and overactive smooth muscles. This includes conditions like irritable bowel syndrome (IBS) and functional dyspepsia. 
• Genitourinary Disorders: The drug can be used to manage overactive bladder symptoms, such as urinary urgency, frequency, and incontinence. 
• Peptic Ulcer Disease: oxyphencyclimine used as the treatment regimen for peptic ulcers to reduce stomach acid secretion and alleviate symptoms. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Xerostomia 

urinary retention 

cycloplegia 

loss of taste 

nervousness 

Impotence 

urticaria 

decreased sweating 

blurred vision 

increased ocular tension 

headache 

mental confusion 

constipation 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with the use of oxyphencyclimine. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Urinary Retention: oxyphencyclimine can further decrease urinary function, making it contraindicated in individuals with urinary retention. 
• Myasthenia Gravis: oxyphencyclimine’s effects on acetylcholine can worsen muscle weakness and fatigue in individuals with myasthenia gravis, a neuromuscular disorder. 
• Severe Ulcerative Colitis: Individuals with severe ulcerative colitis or toxic megacolon, a complication of certain inflammatory bowel diseases, should avoid using oxyphencyclimine due to the risk of exacerbating the condition. 
• Obstructive Uropathy: oxyphencyclimine can lead to urinary retention, which can be problematic in individuals with obstructive uropathy, a condition where there is a blockage in the urinary tract. 
• Hypersensitivity: People with a known hypersensitivity or allergy to oxyphencyclimine or related anticholinergic medications should not use this drug. 
• Paralytic Ileus: oxyphencyclimine can worsen or prolong paralytic ileus, a condition where the normal movement of the intestines is reduced or absent. 

Caution: 

• Elderly Patients: Older adults are more susceptible to the anticholinergic effects of medications like oxyphencyclimine. They may be at increased risk of side effects such as confusion, dry mouth, constipation, and urinary retention. 
• Patients with Existing Conditions: Individuals with certain medical conditions, such as cardiovascular diseases, epilepsy, or hyperthyroidism, should use oxyphencyclimine with caution. The medication’s effects on heart rate, blood pressure, and central nervous system can interact with these conditions. 
• Prostate Enlargement: oxyphencyclimine can exacerbate urinary symptoms in men with benign prostatic hyperplasia (enlarged prostate), potentially leading to urinary retention. 
• Gastrointestinal Conditions: Individuals with conditions like gastroesophageal reflux disease (GERD) or hiatal hernia may experience worsening symptoms due to the medication’s effects on gastrointestinal motility. 
• Pregnancy and Lactation: The safety of oxyphencyclimine during pregnancy and breastfeeding has not been well established. It should be used cautiously and only under the supervision of a healthcare provider when the benefits outweigh the potential risks.

Comorbidities: 

• Cardiovascular Conditions: Individuals with cardiovascular diseases such as congestive heart failure, arrhythmias, or hypertension should use oxyphencyclimine cautiously. The medication’s potential effects on heart rate and blood pressure could interact with these conditions. 
• Neurological Disorders: Conditions like epilepsy, Parkinson’s disease, or dementia can be affected by oxyphencyclimine’s anticholinergic effects. The medication might worsen symptoms or interact with other medications used to manage these disorders. 
• Gastrointestinal Disorders: Individuals with certain gastrointestinal conditions, such as inflammatory bowel disease (IBD) or diverticulitis, might experience worsened symptoms due to oxyphencyclimine’s effects on gastrointestinal motility. 
• Prostate Issues: Men with benign prostatic hyperplasia (enlarged prostate) might experience worsened urinary symptoms due to oxyphencyclimine’s potential to exacerbate urinary retention. 
• Glaucoma: oxyphencyclimine can increase intraocular pressure, which can be problematic for individuals with glaucoma, especially closed-angle glaucoma. 

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: 

oxyphencyclimine is an anticholinergic medication that exerts its effects by blocking the actions of acetylcholine, a neurotransmitter responsible for various bodily functions. By binding to muscarinic receptors, particularly those in smooth muscles and glands, oxyphencyclimine inhibits acetylcholine’s influence, leading to relaxation of smooth muscles, reduced glandular secretions, and diminished muscle contractions. This pharmacological action helps alleviate conditions marked by spasms, cramps, and excessive secretions, such as gastrointestinal and genitourinary disorders.  

Pharmacodynamics: 

• Muscarinic Receptor Antagonism: oxyphencyclimine acts as a competitive antagonist at muscarinic receptors, specifically the M1, M2, and M3 subtypes. By binding to these receptors, it inhibits the binding of acetylcholine, a neurotransmitter, and prevents its effects. 
• Smooth Muscle Relaxation: oxyphencyclimine’s blockade of muscarinic receptors in smooth muscles leads to relaxation of these muscles. This effect is particularly prominent in the gastrointestinal and genitourinary systems, where it can relieve spasms and cramps. 
• Reduction in Glandular Secretions: By inhibiting acetylcholine’s effects on muscarinic receptors in glands, oxyphencyclimine decreases the production of glandular secretions. This can help alleviate symptoms related to excessive secretions, such as runny nose or excessive salivation. 
• Decreased Muscle Contractions: oxyphencyclimine’s action on muscarinic receptors results in reduced muscle contractions in various organ systems. This effect is utilized to manage conditions characterized by overactive muscle contractions. 
• Cardiovascular Effects: oxyphencyclimine’s anticholinergic effects can lead to mild heart rate acceleration due to its impact on the M2 receptors in the heart. However, this effect is usually less pronounced than with other anticholinergic medications. 
• CNS Effects: oxyphencyclimine can have central nervous system effects, including potential sedation, due to its ability to cross the blood-brain barrier and influence muscarinic receptors in the brain.

Pharmacokinetics: 

Absorption 

oxyphencyclimine is usually administered orally, and its absorption from the gastrointestinal tract is slow. The drug is subject to first-pass metabolism in the liver, which can affect its bioavailability. The time it takes for oxyphencyclimine to reach peak plasma concentrations varies, and it may be influenced by factors such as food intake. 

Distribution 

oxyphencyclimine is distributed throughout the body, and it crosses blood-brain barrier, allowing it to have central nervous system effects. The drug binds to muscarinic receptors in various tissues, contributing to its pharmacological effects. The extent of protein binding and the drug’s volume of distribution influence its distribution within the body. 

Metabolism 

oxyphencyclimine undergoes hepatic metabolism primarily through the cytochrome P450 enzyme system, specifically the CYP2D6 and CYP3A4 enzymes. These metabolic processes results in the formation of metabolites. Individual variability in enzyme activity can impact the rate of metabolism and the overall effectiveness of the drug. 

Elimination and excretion 

The metabolites of oxyphencyclimine are excreted through urine, with a smaller portion being eliminated in feces. The drug and its metabolites undergo renal excretion, and impaired kidney function can affect their elimination, potentially necessitating dose adjustments in individuals with renal impairment. 

Adminstartion

Administration: 

• Dosage: The recommended dosage of oxyphencyclimine can vary based on the condition being treated, the patient’s age, and other factors.  
• Timing: oxyphencyclimine is usually taken before meals to reduce the risk of gastrointestinal side effects. Taking it on an empty stomach or at least one hour before meals can help optimize its absorption and effectiveness. 
• Consistency: Try to take oxyphencyclimine at the same times each day to maintain consistent blood levels of the medication. 
• Duration of Use: Follow your healthcare provider’s instructions regarding the duration of treatment. Do not stop taking oxyphencyclimine without consulting your healthcare provider, even if you feel better. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: oxyphencyclimine 

Pronounced: (ok-see-fen-SYE-kli-meen)  

Why do we use oxyphencyclimine? 

• Gastrointestinal Disorders: oxyphencyclimine is often prescribed to alleviate symptoms of gastrointestinal conditions characterized by spasms and cramps. It can be used to treat conditions like irritable bowel syndrome (IBS) and functional dyspepsia, helping to relieve abdominal pain and discomfort. 
• Genitourinary Disorders: oxyphencyclimine may be used to manage urinary urgency, frequency, and incontinence caused by overactive bladder. It can help relax the muscles of the bladder, reducing unwanted contractions. 
• Peptic Ulcer Disease: oxyphencyclimine can be used in combination with other medications to manage symptoms of peptic ulcer disease. By reducing stomach acid secretion and relaxing smooth muscles, it can help alleviate pain and discomfort associated with ulcers. 
• Gastroesophageal Reflux Disease (GERD): oxyphencyclimine may be used to manage symptoms of GERD by reducing muscle contractions in the lower esophagus and decreasing acid reflux. 
• Spasms and Cramps: In certain cases, oxyphencyclimine can be prescribed to relieve muscle spasms and cramps in other parts of the body, although its primary use is for gastrointestinal and genitourinary conditions.