Triprolidine: Uses, Dosage, Side Effects & Warnings
Table of Contents
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:
- Allergic rhinitis (nasal inflammation and congestion due to allergies)
- Hay fever
- Urticaria (hives or skin rash)
- Sneezing
- Runny nose
- Itchy and watery eyes
- Itchy nose and throat
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:
- Drowsiness
- Dry mouth
- Dizziness
- Constipation
- Blurred vision
- Headache
- Nausea
Severe side effects, although rare, may include:
- Difficulty urinating
- Rapid or irregular heartbeat
- Seizures
- Allergic reactions (rash, swelling, difficulty breathing)
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:
- Other antihistamines, which can increase the risk of sedation and drowsiness
- Alcohol, which can enhance the sedative effects of triprolidine
- Central nervous system (CNS) depressants, such as opioid analgesics, sedatives, and hypnotics, which can increase the risk of excessive sedation and respiratory depression
- Monoamine oxidase inhibitors (MAOIs), which can lead to increased anticholinergic effects
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:
- Triprolidine hydrochloride (HCl) tablets or liquid
- Triprolidine HCl and pseudoephedrine HCl (decongestant)
- Triprolidine HCl and guaifenesin (expectorant)
- Triprolidine HCl, pseudoephedrine HCl, and guaifenesin
- Triprolidine HCl and dextromethorphan HBr (cough suppressant)
- Triprolidine HCl, pseudoephedrine HCl, and codeine phosphate (cough suppressant)
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:
- Second-generation antihistamines (e.g., cetirizine, loratadine, fexofenadine), which are less sedating and have fewer anticholinergic effects
- Nasal corticosteroids (e.g., fluticasone, triamcinolone), which are used to reduce nasal inflammation and congestion
- Decongestants (e.g., pseudoephedrine, oxymetazoline), which can provide relief from nasal congestion
- Leukotriene inhibitors (e.g., montelukast), which can help prevent and treat symptoms of allergic rhinitis
- Natural remedies (e.g., quercetin, nettles, butterbur) may provide relief for some individuals
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:
- Glaucoma or increased intraocular pressure
- Prostatic hypertrophy or bladder neck obstruction
- Cardiovascular disease or hypertension
- Thyroid disorders
- Diabetes
- Seizure disorders
Triprolidine is contraindicated (should not be used) in individuals with:
- Known hypersensitivity or allergy to triprolidine or any of the ingredients in the product
- Monoamine oxidase inhibitor (MAOI) therapy (currently or within the past 14 days)
- Severe liver or kidney disease
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=
