Triprolidine

Triprolidine: Uses, Dosage, Side Effects & Warnings

Introduction

Triprolidine is a first-generation antihistamine medication used to treat symptoms associated with allergies, hay fever, and the common cold. It is a sedating antihistamine that works by blocking the effects of histamine, a chemical released by the body during an allergic reaction. The chemical name of triprolidine is 2-[1-(1H-pyrrol-2-yl)propyl]-1,2,3,6-tetrahydropyridine, and its molecular formula is C 19H 22N 2. Triprolidine has been available as an over-the-counter (OTC) medication since the 1960s and is known for its ability to relieve nasal congestion, runny nose, sneezing, itchy and watery eyes, and itchy nose and throat.

Uses of Triprolidine

Triprolidine is primarily used to provide temporary relief from the following symptoms:

It is commonly used to treat symptoms associated with the common cold, such as sneezing, runny nose, and nasal congestion. Triprolidine is often combined with other medications like pseudoephedrine (a decongestant), guaifenesin (an expectorant), or dextromethorphan (a cough suppressant) to provide more comprehensive relief for cold and allergy symptoms.

Sources: https://www.ncbi.nlm.nih.gov/books/NBK548865/, Triprolidine“>https://pubchem.ncbi.nlm.nih.gov/compound/ Triprolidine

Dosage and Administration

Triprolidine is available in the form of oral tablets and liquid formulations. The recommended dosage for adults and children over 12 years of age is one 2.5 mg tablet or 5 mL of liquid every 4 to 6 hours, not exceeding 10 mg or 20 mL per day. For children aged 6 to 12 years, the recommended dosage is half the adult dose. Triprolidine should not be given to children under 6 years of age unless directed by a healthcare professional.

It is important to follow the dosage instructions on the product label or as prescribed by a healthcare provider. Triprolidine should be taken with food or milk to reduce the risk of stomach upset.

Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018021s028lbl.pdf

Side Effects and Precautions

Common side effects of triprolidine include:

Severe side effects, although rare, may include:

Triprolidine should be used with caution in individuals with certain medical conditions, such as glaucoma, prostatic hypertrophy, or cardiovascular disease. It may also cause drowsiness and impair the ability to drive or operate machinery.

Source: https://www.drugs.com/triprolidine.html

Drug Interactions

Triprolidine may interact with other medications, including:

It is important to inform your healthcare provider about all medications you are taking, including over-the-counter drugs, supplements, and herbal products, to avoid potential interactions.

Source: https://www.webmd.com/drugs/2/drug-63701/triprolidine-oral/details

Mechanism of Action

Triprolidine is a first-generation antihistamine that works by blocking the effects of histamine, a chemical released by the body during an allergic reaction. Histamine is responsible for many of the symptoms associated with allergies, such as nasal congestion, sneezing, and itching.

Triprolidine competes with histamine for binding sites on H 1 receptors, which are found in various tissues throughout the body, including the respiratory tract, blood vessels, and gastrointestinal tract. By binding to these receptors, triprolidine prevents histamine from exerting its effects, thereby reducing allergy symptoms.

In addition to its antihistamine properties, triprolidine also exhibits anticholinergic effects, which can lead to side effects such as dry mouth, blurred vision, and difficulty urinating. It also has sedative properties, which can cause drowsiness.

Source: https://www.ncbi.nlm.nih.gov/books/NBK548865/

Formulations and Combinations

Triprolidine is available as a single-ingredient product (monotherapy) or in combination with other active ingredients. Some common formulations and combinations include:

These combination products are designed to provide relief from multiple symptoms associated with allergies and the common cold, such as nasal congestion, runny nose, sneezing, coughing, and chest congestion.

Source: https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=018021

Alternatives to Triprolidine

While triprolidine is an effective antihistamine for treating allergy and cold symptoms, there are several alternative medications available. Some alternatives include:

The choice of medication or alternative treatment will depend on individual factors, such as the severity of symptoms, age, and other medical conditions.

Source: https://www.aafp.org/pubs/afp/issues/2018/0915/p411.html

Warnings and Contraindications

Triprolidine should be used with caution in individuals with the following conditions:

Triprolidine is contraindicated (should not be used) in individuals with:

It is important to consult with a healthcare professional before taking triprolidine, especially if you are pregnant, breastfeeding, or have any underlying medical conditions.

Source: https://www.drugs.com/cdi/triprolidine.html

Pharmacokinetics

Triprolidine is well absorbed after oral administration, with peak plasma concentrations typically reached within 1 to 4 hours. The medication is widely distributed throughout the body and crosses the blood-brain barrier, contributing to its sedative effects.

Triprolidine undergoes extensive metabolism in the liver, primarily through oxidation and hydroxylation. The metabolites are then excreted in the urine and feces. The elimination half-life of triprolidine is approximately 6 to 8 hours.

Certain factors, such as age, liver or kidney function, and concomitant medications, can affect the pharmacokinetics of triprolidine, potentially leading to increased or decreased drug levels in the body.

Source: https://www.ncbi.nlm.nih.gov/books/NBK548865/

Regulatory Status

Triprolidine is available as an over-the-counter (OTC) medication in many countries, including the United States, Canada, and several European nations. However, in some regions, it may require a prescription from a licensed healthcare provider.

In the United States, triprolidine is approved by the Food and Drug Administration (FDA) for OTC use as an antihistamine for the temporary relief of symptoms associated with allergies, hay fever, and the common cold. It is also available in combination products with other active ingredients, such as decongestants, expectorants, and cough suppressants.

The regulatory status of triprolidine may vary between countries, and it is essential to follow the guidelines and regulations specific to your location.

Source: https://www.fda.gov/drugs/resources-you-drugs/over-counter-otc-antihistamines

Research and Development

While triprolidine has been used as an antihistamine for several decades, ongoing research continues to explore its potential applications and investigate new formulations or combinations.

Clinical trials have been conducted to evaluate the efficacy and safety of triprolidine in various contexts, such as comparing it to other antihistamines or evaluating its use in combination with other medications for the treatment of allergic rhinitis, cough, and other respiratory conditions.

Researchers are also exploring the development of new formulations or delivery methods for triprolidine, such as sustained-release or controlled-release formulations, to improve its therapeutic profile and reduce the frequency of dosing.

Additionally, triprolidine may be studied for potential off-label uses or in combination with other therapeutic agents for the management of various conditions.

Source: https://clinicaltrials.gov/ct2/results?cond=&term=triprolidine&cntry=&state=&city=&dist=

Triprolidine