phenylephrine and cocoa butter rectal

Action and Spectrum

Actions and spectrum: 

phenylephrine is a sympathomimetic agent that acts as a vasoconstrictor. When used rectally, phenylephrine constricts blood vessels in the rectal area, which can help relieve symptoms such as swelling, itching, and discomfort. 

cocoa butter, on the other hand, is an emollient and moisturizing agent. When used rectally, cocoa butter helps lubricate the rectal area, making bowel movements smoother and more comfortable. 

The combination of phenylephrine and cocoa butter in rectal preparations is commonly used for the temporary relief of hemorrhoidal symptoms, such as pain, swelling, itching, and irritation associated with hemorrhoids. phenylephrine constricts blood vessels in the affected area, reducing swelling and discomfort, while cocoa butter provides lubrication and moisturization to ease bowel movements. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Allergic reaction 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with the use of phenylephrine and cocoa butter rectal preparations. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity or allergy: Individuals with a known hypersensitivity or allergy to phenylephrine, cocoa butter, or any other ingredients in the product should not use it. 
• Severe cardiovascular disease: Phenylephrine is a vasoconstrictor and may increase blood pressure. Individuals with severe cardiovascular disease, such as severe hypertension, coronary artery disease, or cardiac arrhythmias, should avoid using phenylephrine. 
• Closed-angle glaucoma: phenylephrine can cause pupil dilation, which may worsen the symptoms of closed-angle glaucoma. People with this condition should avoid using phenylephrine. 
• Urinary retention: phenylephrine can potentially worsen urinary retention in individuals with underlying urinary obstruction or bladder dysfunction.

Caution: 

• Cardiovascular conditions: phenylephrine can increase blood pressure and heart rate. Individuals with cardiovascular conditions such as high blood pressure, heart disease, or a history of heart attack or stroke should use phenylephrine rectal preparations under caution. 
• Diabetes: phenylephrine can affect blood sugar levels and may interfere with diabetes management. Individuals with diabetes should monitor their blood sugar levels closely while using phenylephrine rectal preparations. 
• Pregnancy and lactation: The use of phenylephrine and cocoa butter rectal preparations during pregnancy and lactation should be discussed with a healthcare professional. It is important to weigh the potential benefits against any potential risks to the mother and baby. 

Comorbidities: 

• Thyroid disorders: phenylephrine can potentially affect thyroid function and interfere with thyroid hormone tests. Individuals with thyroid disorders should inform their healthcare provider before using phenylephrine rectal preparations. 
• Prostate enlargement: phenylephrine can cause urinary retention or difficulty in urination. Men with prostate enlargement, such as benign prostatic hyperplasia (BPH), should exercise caution when using phenylephrine rectal preparations. 

Pregnancy / Lactation

Pregnancy consideration: Not assigned 

Lactation: excreted in 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 is a sympathomimetic drug that acts as an alpha-adrenergic agonist. It stimulates alpha-adrenergic receptors in the smooth muscles of blood vessels, causing vasoconstriction and narrowing of the blood vessels. This leads to a reduction in swelling and congestion in the nasal passages or rectal area. 

cocoa butter, on the other hand, is a natural fat derived from the cocoa bean. It serves as a base or carrier in rectal preparations, providing lubrication and facilitating the delivery of the active ingredient (phenylephrine) to the affected area. 

When used rectally, phenylephrine and cocoa butter combine to provide localized vasoconstriction and relief from congestion or inflammation in the rectal area. The vasoconstrictive action helps reduce swelling, itching, and discomfort associated with hemorrhoids or other rectal conditions.  

Pharmacodynamics: 

phenylephrine, as an alpha-adrenergic agonist, acts primarily on alpha-adrenergic receptors located in the smooth muscles of blood vessels. When applied rectally, phenylephrine constricts the blood vessels in the rectal area, leading to reduced swelling and congestion. 

The vasoconstrictive effect of phenylephrine helps to decrease blood flow to the rectal area, which can alleviate symptoms such as itching, swelling, and discomfort associated with hemorrhoids or other rectal conditions. By narrowing the blood vessels, phenylephrine reduces the volume of blood in the affected area, resulting in a reduction of congestion and inflammation. 

cocoa butter, being a natural fat, acts as a lubricant and emollient. It helps to soften the rectal tissues, making the application of the rectal preparation more comfortable and facilitating the absorption of phenylephrine into the affected area.  

Pharmacokinetics: 

Absorption 

When applied rectally, phenylephrine and cocoa butter are absorbed through the rectal mucosa. phenylephrine is a vasoconstrictor that acts locally in the rectal area, and its absorption into the systemic circulation is minimal. cocoa butter acts as a carrier and helps facilitate the absorption of phenylephrine into the rectal tissues. 

Distribution 

phenylephrine, when absorbed, may undergo limited systemic distribution. However, due to its vasoconstrictive action, it primarily acts locally in the rectal area. cocoa butter, being a fat-based substance, may distribute within the rectal tissues, providing lubrication and emollient properties. 

Metabolism 

phenylephrine is metabolized in the liver by enzymes such as catechol-O-methyltransferase (COMT). The metabolites are primarily inactive and are eliminated through urine. However, the metabolism of phenylephrine following rectal administration is minimal since it primarily acts locally. 

Elimination and excretion 

phenylephrine and its metabolites are primarily eliminated through the kidneys via urine. The rectal application of phenylephrine may result in minimal systemic absorption and subsequent renal excretion. cocoa butter is not metabolized but rather can be excreted through feces. 

Adminstartion

Administration: 

• Wash hands thoroughly before handling the rectal suppository or applicator. 
• If using a suppository, remove it from the packaging and make sure it is at room temperature for easy insertion. If using an applicator, follow the instructions provided with the product. 
• Find a comfortable position, such as lying on your side with one leg bent towards your chest. 
• Gently insert the suppository or applicator into the rectum. For suppositories, it is usually recommended to insert it about 1 inch into the rectum. For applicators, follow the specific instructions provided with the product. 
• Once inserted, it is important to keep the suppository or applicator in place for the recommended duration. This allows the phenylephrine and cocoa butter to melt or disperse, facilitating absorption and providing local relief. 
• Wash hands again after administration. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: phenylephrine and cocoa butter rectal 

Pronounced: (Fen-i-lef-rin/ ko-ko-uh buht-er rek-tuhl)  

Why do we use phenylephrine and cocoa butter rectal? 

• Hemorrhoid relief: phenylephrine is a vasoconstrictor that helps to shrink swollen blood vessels in the rectal area, providing temporary relief from hemorrhoids. 
• Anal itching and discomfort: The combination of phenylephrine and cocoa butter can help soothe itching and discomfort associated with various rectal conditions, such as hemorrhoids or anal fissures. 
• Proctitis or proctosigmoiditis: These rectal inflammatory conditions can cause pain, swelling, and discomfort. phenylephrine and cocoa butter rectal preparations may be used to alleviate these symptoms. 
• Pre- and post-anorectal surgery: These preparations may be used before and after anorectal surgery to reduce swelling, relieve pain, and promote healing.