phenylephrine, pramoxine, glycerin and petrolatum rectal

Action and Spectrum

Actions and spectrum: 

• phenylephrine: It is a sympathomimetic agent that constricts blood vessels, leading to reduced swelling and congestion in the rectal area. 
• pramoxine: It is a local anesthetic that provides temporary relief from itching, pain, and discomfort in the rectal area. 
• glycerin: It is a hyperosmotic agent that draws water into the rectum, promoting bowel movement and softening the stool. 
• petrolatum: It is an emollient and lubricant that helps to soothe and protect the rectal area, reducing irritation and promoting healing. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Allergic reaction 

Black Box Warning

Black Box Warning: 

There are no specific black box warnings associated with the combination of phenylephrine, pramoxine, glycerin, and petrolatum in rectal form. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with a known hypersensitivity or allergy to any of the active ingredients or other related substances should avoid using this medication. 
• Severe cardiovascular disease: The use of phenylephrine, which is a vasoconstrictor, may be contraindicated in individuals with severe cardiovascular conditions such as severe hypertension, coronary artery disease, or certain arrhythmias. 
• Rectal bleeding: If you have active rectal bleeding or are experiencing severe rectal pain, the use of rectal medications may be contraindicated. 
• Severe ulcerative colitis: In individuals with severe ulcerative colitis or other severe inflammatory bowel diseases, the use of rectal medications may not be recommended.

Caution: 

• Underlying medical conditions: If there are any underlying medical conditions, such as cardiovascular disease, diabetes, thyroid disorders, or urinary retention, it is important to use caution and take medical advice before taking this medication. 
• Pregnancy and breastfeeding: If pregnant, planning to become pregnant, or breastfeeding, it is important to discuss the use of this medication with healthcare provider. They can weigh the potential benefits and risks to determine if it is safe for you and your baby. 
• Pediatric use: The safety and efficacy of this rectal preparation in children and infants may vary. It is important to consult with a healthcare professional for appropriate dosing and guidance. 
• Drug interactions: Inform healthcare provider about all the medications, supplements, and herbals that are taking to avoid potential drug interactions. 
• Pre-existing rectal conditions: If you have pre-existing rectal conditions such as hemorrhoids, fissures, or inflammation, use this rectal medication with caution, as it may cause irritation or worsen your condition.

Comorbidities: 

• Cardiovascular conditions: Individuals with cardiovascular diseases such as hypertension, heart disease, or arrhythmias should exercise caution as phenylephrine can affect blood pressure and heart rate. 
• Diabetes: Patients with diabetes should use caution when using medications containing glycerin, as it may affect blood sugar levels. 
• Thyroid disorders: Individuals with thyroid disorders, such as hyperthyroidism or hypothyroidism, should exercise caution as phenylephrine can potentially affect thyroid function. 
• Urinary retention: Patients with a history of urinary retention or bladder outlet obstruction should use caution when using medications containing phenylephrine, as it can exacerbate these conditions. 

Pregnancy / Lactation

Pregnancy consideration: Pregnancy Category: C 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• 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: 

• phenylephrine: phenylephrine is a sympathomimetic agent that acts as a selective alpha-1 adrenergic receptor agonist. It constricts blood vessels locally, reducing inflammation and swelling associated with hemorrhoids. 
• pramoxine: pramoxine is a local anesthetic that works by inhibiting the transmission of nerve impulses. It temporarily relieves from pain and itching in the rectal area. 
• glycerin: glycerin is a hyperosmotic agent that attracts water into the rectum, softening the stool and promoting bowel movement. It helps relieve constipation associated with hemorrhoids. 
• petrolatum: petrolatum, also known as petroleum jelly, acts as a protective barrier and emollient. It helps soothe and moisturize the affected area, reducing dryness and irritation.

Pharmacodynamics: 

• phenylephrine: phenylephrine acts as a selective alpha-1 adrenergic receptor agonist. By stimulating these receptors, it causes vasoconstriction in the blood vessels in the rectal area. This leads to decreased blood flow, reduced inflammation, and alleviation of swelling. 
• pramoxine: pramoxine is a local anesthetic that acts by blocking the pain signal transmissions from the nerves. It acts on sodium channels in the nerve fibers, preventing the initiation and conduction of pain impulses. This results in temporary relief from pain and itching in the rectal area. 
• glycerin: glycerin is a hyperosmotic agent that attracts water into the rectum. It helps to soften stools by increasing its water content. This facilitates easier bowel movements and relieves constipation associated with hemorrhoids. 
• petrolatum: petrolatum acts as an emollient and a protective barrier. It helps to soothe and moisturize the affected area by forming a barrier on the skin’s surface. This barrier prevents moisture loss and protects the skin from irritants, reducing dryness and further irritation.

Pharmacokinetics: 

Absorption 

When applied rectally, these medications are primarily absorbed through the rectal mucosa. phenylephrine and pramoxine can be systemically absorbed to a certain extent, while glycerin and petrolatum have minimal systemic absorption. 

Distribution 

After absorption, phenylephrine and pramoxine can enter the bloodstream and distribute throughout the body. They may bind to various tissues and receptors, exerting their effects. glycerin and petrolatum remain primarily localized in the rectal area. 

Metabolism 

phenylephrine and pramoxine undergo metabolism in the liver. They are subject to enzymatic reactions that can result in the formation of metabolites. glycerin and petrolatum are not metabolized and remain unchanged. 

Elimination and excretion 

The metabolites of phenylephrine and pramoxine, as well as any unmetabolized drug, are eliminated primarily through renal excretion. glycerin and petrolatum, being minimally absorbed systemically, are not extensively metabolized, and are not excreted in significant amounts. 

Adminstartion

Administration: 

• Wash hands before and after application. 
• clean the affected region with mild soap and water, and pat dry. 
• Squeeze a small amount of ointment onto fingertip or a clean applicator. 
• Apply thin layer of ointment onto the affected area. 
• Gently rub the ointment into the skin till it is absorbed. 
• Wash your hands again after application. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: phenylephrine, pramoxine, glycerin and petrolatum rectal 

Pronounced: (fen-uhl-EF-rin, pruh-MOK-seen, GLIS-uh-rin, and puh-TROL-uh-tum REK-tuhl)  

Why do we use phenylephrine, pramoxine, glycerin and petrolatum rectal? 

• Hemorrhoid Relief: These products can provide temporary relief from the discomfort, itching, and irritation associated with hemorrhoids (swollen blood vessels in the rectal area). 
• Anal Itching and Irritation: They can help soothe and alleviate itching, burning, and irritation in the anal area caused by conditions such as anal fissures, anal itching, or irritation from diarrhea. 
• Constipation Relief: glycerin rectal suppositories act as a mild laxative and is used to relieve occasional constipation by promoting bowel movements. 
• Lubrication: petrolatum-based rectal products provide lubrication and can help facilitate the insertion of rectal devices, such as thermometers or enema applicators.