Pramoxine Hydrochloride: A Topical Anesthetic for Itch and Pain Relief

Overview:

Pramoxine hydrochloride is approved by the FDA in various over-the-counter (OTC) topical products. Pramoxine hydrochloride has a long history of safe use when used as directed. Pramoxine hydrochloride was first developed as a local anesthetic in the mid-20th century, in 1950. In the year 1970, Pramoxine hydrochloride started to gain recognition as a valuable local anesthetic for dermatological use. Its development was part of ongoing efforts to discover and refine local anesthetic agents that could effectively provide temporary relief from itching and minor pain. While Pramoxine hydrochloride has a long history of use, ongoing research may explore its potential applications, optimization of formulations, and safety considerations. This article aims to present a summary of Pramoxine hydrochloride, including its pharmacological properties, therapeutic applications, and safety considerations.

Drug Group:

Pramoxine hydrochloride belongs to the class of local anesthetics known as amino amides.

Available Doses and Dosage Forms:

Pramoxine hydrochloride is available in various forms for topical use. Some common forms include:

• Creams: Pramoxine hydrochloride cream is a famous formulation applied directly to the skin. It typically contains a combination of Pramoxine hydrochloride and other ingredients that provide a soothing and moisturizing effect. Available in the strength of 10 mg (milligrams) /1ml (milliliter).

• Gels: Pramoxine hydrochloride gel is another topical form that is commonly used. It has a gel-like consistency and is easy to apply to the affected area.

• Sprays: Pramoxine hydrochloride sprays are convenient for applying the medication to larger areas of the skin or areas that are hard to reach. They often come in aerosol form and can be sprayed directly on the affected area. Available in the strength of one percent pramoxine.

• Lotions: Pramoxine hydrochloride lotions are also available, providing a lighter and more liquid consistency than creams. They are easily spreadable and can be used for broader body areas. Available in the strength of 1 mg/1mL.

For Patients:

What Are Hemorrhoids?

Hemorrhoids, also referred to as piles, are a condition that involves swollen and inflamed veins located in the lower rectum (anus). They can cause discomfort, pain, itching, and bleeding during bowel movements. There are multiple ways to relieve the symptoms of hemorrhoids. Individuals can improve their diet by including more fiber-rich foods like fruits, vegetables, and whole grains and staying well-hydrated to prevent constipation.

Over-the-counter creams or ointments can be used for itching and discomfort, and sitz baths taken multiple times daily can provide relief. It is crucial to avoid straining during bowel movements. If these self-care methods do not work, a healthcare professional may recommend medical interventions such as rubber band ligation (a medical procedure to treat internal hemorrhoids located in the rectum or anus), sclerotherapy (which involves injecting a sclerotherapeutic agent in the vein), or surgery.

How Does Pramoxine Hydrochloride Work?

Upon topical application, Pramoxine hydrochloride engages with the nerve endings in the skin, mucous membranes, or specific tissues affected by hemorrhoids. By obstructing the sodium channels inherent in the membranes of nerve cells, Pramoxine impedes the genesis and transmission of nerve impulses. Consequently, the customary pain signals ordinarily conveyed to the brain are prevented from reaching their intended destination. This resultant numbing effect furnishes temporary alleviation from the pruritus and discomfort frequently linked to hemorrhoids.

What Is the Dosage of Pramoxine Hydrochloride?

The dosage of Pramoxine hydrochloride varies depending on the specific formulation, indication, and individual factors.

How Effective Is Pramoxine Hydrochloride?

Pramoxine hydrochloride is generally considered an effective topical anesthetic for temporary relief from itching and discomfort associated with various conditions, including hemorrhoids. The efficacy of Pramoxine hydrochloride can differ among individuals and is influenced by the severity of symptoms and the underlying cause. In cases of mild to moderate hemorrhoids, Pramoxine hydrochloride is effective in providing substantial relief and enhancing the overall well-being of the affected person.

What Are the Things to Inform the Doctor Before Taking Pramoxine?

• Before using Pramoxine hydrochloride, it is important to inform the doctor and pharmacist if there are any allergies to Pramoxine hydrochloride, other topical anesthetics, or any other medications.

• Make sure to disclose all prescription and non-prescription medications and any vitamins, nutritional supplements, or herbal products the patient is taking.

• If someone is pregnant, planning to become pregnant, or breastfeeding, it is crucial to notify the doctor.

• If the patient becomes pregnant while using Pramoxine hydrochloride, contact the doctor promptly.

How Is Pramoxine Hydrochloride Administered?

Here are the instructions for using Pramoxine hydrochloride cream, gel, spray, lotion, pledgets, or hemorrhoidal foam:

• Begin by washing hands.

• Cleanse the affected area using warm water and mild soap, ensuring thorough rinsing.

• Gently pat the affected area dry using a clean, soft cloth or tissue.

• Apply a small amount of Pramoxine hydrochloride to the affected area, depending on the specific product the patient uses.

• After applying the medication, it is important to wash the hands thoroughly.

• If using Pramoxine hydrochloride pledgets, start by washing the hands.

• Clean the affected rectal area using mild soap and warm water, ensuring thorough rinsing.

• To dry the area, it is recommended to gently pat or blot it with a clean, soft cloth or tissue.

• Open the sealed pouch and remove the pledget.

• Pat the medication from the pledget onto the affected rectal area. If necessary, fold the pledget and leave it in place for up to 15 minutes.

• Dispose of the pledget safely, out of the reach of children.

• Wash hands thoroughly after removing the pledges.

• If using Pramoxine hydrochloride hemorrhoidal foam, start by washing hands.

• Cleanse the affected area using warm water and mild soap, ensuring thorough rinsing.

• To dry the area, it is recommended to gently pat or blot it with a clean, soft cloth or tissue.

• Shake the foam container before use.

• Dispense a small amount of foam onto a clean tissue and gently apply it to the affected rectal area.

• Wash hands thoroughly after applying the foam.

What Are the Side Effects of Pramoxine Hydrochloride?

Inform the doctor if the patient encounters any of the following symptoms while using Pramoxine hydrochloride, as they may indicate side effects that require attention: Redness, irritation, swelling, burning, stinging, or pain at the application site. Dryness at the application site.

Although rare, certain side effects can be serious. If the patient experiences any of the following symptoms, contact the doctor immediately:

• Bleeding at the application site.

• Hives (allergic reaction).

• Skin rash.

• Severe itching.

• Difficulty breathing or swallowing.

• The face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs get swollen.

• Hoarseness of voice.

Dietary Considerations:

Unless specifically instructed by the doctor, it is advisable to maintain a regular, balanced diet.

Missed Dose:

In the event of a missed dose, promptly administer the missed dose. Nevertheless, if the next scheduled dose is nearly due, omit the missed dose and adhere to the regular dosing schedule. Refrain from applying a double dose to compensate for the missed one.

Overdose:

Symptoms of a Pramoxine hydrochloride overdose may include:

• Excessive drowsiness or sedation.

• Confusion or disorientation.

• Difficulty breathing.

• Slow or shallow breathing.

• Slow heart rate.

• Low blood pressure.

• Fainting or loss of consciousness.

• Seizures.

• Bluish discoloration of the lips, skin, or nails (cyanosis).

It is crucial to acknowledge that the symptoms and intensity of an overdose may differ based on factors like the quantity consumed and the individual's overall well-being. Seeking immediate medical attention is vital to ensuring proper assessment, treatment, and potential reversal of the overdose's effects.

Storage

• Ensure the medication is stored in its original container, tightly sealed, and out of children's reach.

• Store it in a cool, dry place at room temperature (not in the bathroom).

• Pramoxine hydrochloride aerosol containers, sprays, or lotions should be kept away from fire, flame, or extreme heat.

• Avoid disposing of Pramoxine hydrochloride aerosol containers in an incinerator.

• To ensure the safe disposal of unneeded medications, follow special guidelines to prevent accidental consumption by pets, children, and others. Avoid flushing the medication down the toilet and use a medicine take-back program.

• Contact the pharmacist or the local garbage/recycling department for information on take-back programs in the community.

• Keeping all medications hidden and out of children's reach is crucial, as some containers are not child-resistant. Examples include weekly pill organizers, containers for eye drops, creams, patches, and inhalers.

• To prevent accidental poisoning, always secure safety caps and store the medication in a safe location that is elevated and out of sight and reach.

For Doctors:

Indications:

Indications for using Pramoxine Hydrochloride are as follows:

• Itchy Skin: Pramoxine hydrochloride is used to relieve itching caused by insect bites, minor burns, sunburns, rashes, eczema, poison ivy, and other skin irritations.

• Hemorrhoids: They can be applied topically to provide temporary relief from itching, swelling, and discomfort associated with hemorrhoids.

• Anal Fissures: Pramoxine hydrochloride may be used to alleviate pain, itching, and discomfort caused by anal fissures (small tears or cuts in the lining of the anus).

• Minor Skin Irritations: It is used to ease itching and discomfort caused by minor cuts, scrapes, and skin irritations.

Dose:

The appropriate dosage of Pramoxine hydrochloride can differ based on the product and individual circumstances.

• In creams available in the strength of 10 mg/1 ml.

• Sprays usually contain one percent Pramoxine hydrochloride.

• Lotions are available in strengths of one mg/1mL.

Dosing Considerations:

• The recommended dosage of Pramoxine hydrochloride depends on the formulation, i.e., if it is in spray, gel, or cream form.

• Pramoxine hydrochloride is applied topically as directed by the doctor or as needed. Systemic application is not advised.

• Avoid applying Pramoxine hydrochloride more frequently or in larger amounts than directed. Excessive use may cause adverse effects or complications.

• Special dosing adjustments may be necessary for children, elderly individuals, and those with specific medical conditions.

What Are the Pharmacological Aspects of Pramoxine Hydrochloride?

Pharmacodynamics

Pramoxine hydrochloride provides temporary relief from pain, itching, burning, and discomfort linked to minor lip and skin irritations and hemorrhoids. It accomplishes this by blocking voltage-gated sodium channels found on nerve cells, interrupting the transmission of signals that trigger these sensations.

Mechanism

Pramoxine hydrochloride exerts its therapeutic effects by reversibly attaching to and impeding the function of voltage-gated sodium channels in neurons. This action leads to a decrease in the permeability of sodium ions into the nerve cell. By binding to these sodium channels, Pramoxine hydrochloride effectively stabilizes the neuronal cell membrane. This stabilization prevents the normal fluctuations of ions, particularly sodium, required for depolarization and the propagation of action potentials along the nerve fibers. By inhibiting the propagation of action potentials, Pramoxine hydrochloride effectively stops transmitting signals that convey these unpleasant sensations to the brain. Consequently, individuals experience temporary relief from the symptoms associated with minor skin irritations and hemorrhoids.

Pharmacokinetics

Pharmacokinetics encompasses the processes of drug absorption, distribution, metabolism, and elimination within the body. There is no exact data available.

Here is an overview of the pharmacokinetics of Pramoxine hydrochloride:

• Absorption: Pramoxine hydrochloride is primarily administered topically, which means it is applied to the skin or mucous membranes. Upon application, it is absorbed into the underlying tissues. The rate and extent of absorption can vary depending on factors such as the specific formulation, the area of application, and the condition of the skin or mucous membranes.

• Distribution: Pramoxine hydrochloride is distributed within the tissues near the application site after absorption. It does not have significant systemic distribution, meaning it does not extensively enter the bloodstream or reach distant organs or tissues. This localized distribution limits the potential for systemic side effects.

• Metabolism: Pramoxine hydrochloride undergoes minimal metabolism in the body. It is primarily metabolized by ester hydrolysis, where it is broken down into inactive metabolites. The metabolic pathways and enzymes involved in Pramoxine hydrochloride metabolism are poorly studied.

• Elimination: The elimination of Pramoxine hydrochloride occurs mainly through renal excretion. After metabolism or inactivation in the body, the resulting metabolites are eliminated from the body via the kidneys and excreted in the urine.

Toxicity:

While Pramoxine hydrochloride is generally safe when used correctly, it is important to be cautious about excessive use or misuse, which can result in potential toxicity.

Here are some important points to consider regarding the toxicity of Pramoxine hydrochloride:

• Overdose: Exceeding the recommended dose of Pramoxine hydrochloride can raise the risk of toxicity, with overdose symptoms including dizziness, drowsiness, blurred vision, nausea, vomiting, and breathing difficulties. In severe instances, it can even lead to seizures or loss of consciousness.

• Allergic Reactions: Certain individuals may have hypersensitivity or allergies to Pramoxine hydrochloride. Allergic reactions can manifest as mild skin irritation or more severe symptoms like rash, itching, swelling, and breathing difficulties.

• Pre-existing Conditions and Interactions: Pramoxine hydrochloride may interact with other medications or exacerbate certain pre-existing conditions.

• Prolonged Use: Pramoxine hydrochloride for an extended period or in excessive amounts beyond the recommended duration can result in skin irritation or increased sensitivity.

Clinical Studies:

Extensive clinical trials and research studies have investigated the effectiveness and safety of Pramoxine hydrochloride in managing symptoms like itching, pain, and discomfort caused by minor skin irritations and hemorrhoids. These studies have also explored the combination of Pramoxine hydrochloride with other active ingredients to enhance therapeutic outcomes potentially. Clinical studies follow strict research protocols, including randomized controlled trials (RCTs), to carefully evaluate the efficacy and safety of Pramoxine hydrochloride. These trials often involve comparing Pramoxine hydrochloride with placebos or established treatments to assess its relative advantages and potential side effects.

What Are the Contraindications of Pramoxine Hydrochloride?

There are a few contraindications associated with the use of Pramoxine hydrochloride.

These include:

• Hypersensitivity: Individuals who have a known hypersensitivity or allergic reaction to Pramoxine hydrochloride or any of its components should avoid using products containing this medication.

• Severe Skin Conditions: Pramoxine hydrochloride may not be suitable for individuals with severe skin conditions, such as deep wounds, severe burns, or infections.

• Open Wounds or Broken Skin: It is generally recommended to avoid using Pramoxine hydrochloride on open wounds or damaged skin, as it can potentially hinder the natural healing process or lead to irritation.

Warnings and Precautions:

Various warnings associated with Pramoxine Hydrochloride are:

• With Pramocine hydrochloride, there is always a risk of hypersensitivity reactions.

• Pramoxine hydrochloride is a local anesthetic and may lead to toxicity if used in excessive amounts or absorbed systemically.

• Pramoxine hydrochloride may interact with certain medications, including other local anesthetics, antiarrhythmics, and antibiotics.

• Using Pramoxine hydrochloride carries a minimal risk of potential systemic adverse effects. These can include central nervous system depression, allergic reactions, or other unexpected reactions.

What Are the Drug Interactions of Pramoxine Hydrochloride?

• The concurrent administration of Pramoxine hydrochloride and 1,2-Benzodiazepine can synergistically amplify the likelihood or magnitude of central nervous system depression.

• When Pramoxine hydrochloride is combined with Abemaciclib, Abiraterone, Acetaminophen, Acetyl sulfisoxazole, Acetic acid, Adagrasib, Afatinib, and Acetazolamide it can cause methemoglobinemia (abnormal type of hemoglobin known as methemoglobin present in the blood).

• The simultaneous administration of Pramoxine hydrochloride and Acetophenazine carries the potential to heighten the risk or magnitude of central nervous system depression.

Specific Considerations:

• Use in Children: Pramocaine hydrochloride should be used with caution, as safety and effectiveness in pediatric patients may vary. Pediatric patients or children may require dosage adjustments or closer monitoring during treatment.

• Pregnancy and Breastfeeding: The use of Pramoxine hydrochloride during pregnancy and breastfeeding should be discussed with a healthcare professional. It is not considered safe during pregnancy or breastfeeding.

• Underlying Medical Conditions: Any underlying condition, such as liver or kidney function, should be considered when using Pramoxine hydrochloride.