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Triprolidine

Generic name: triprolidine systemic

Brand names: Zymine, Zymine XR, Tripohist, Histex Syrup, Histex PD Drops, Vanahist PD, M-Hist PD, Vanaclear PD, Histex

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Liquid, Oral:

Generic: 0.313 mg/mL (50 mL)

Liquid, Oral, as hydrochloride:

Dr Manzanilla Antihistamine: 0.938 mg/mL (30 mL) [alcohol free, dye free, sugar free; contains sodium benzoate; bubble-gum flavor]

Histex PD: 0.938 mg/mL (30 mL) [alcohol free, dye free, sugar free; contains propylene glycol, saccharin sodium; bubble-gum flavor]

Histex PDX: 1.25 mg/mL (30 mL [DSC]) [alcohol free, dye free, sugar free; contains methylparaben, propylene glycol, propylparaben; bubble-gum flavor]

M-Hist PD: 0.625 mg/mL (30 mL) [contains fd&c red #40, propylene glycol, sodium benzoate, sorbitol; strawberry-banana flavor]

Generic: 0.625 mg/mL (30 mL, 50 mL); 0.938 mg/mL (30 mL)

Syrup, Oral, as hydrochloride:

Dr Manzanilla Antihistamine: 2.5 mg/5 mL (237 mL) [alcohol free, dye free, sugar free; contains sodium benzoate; bubble-gum flavor]

Histex: 2.5 mg/5 mL (237 mL) [alcohol free, dye free, sugar free; contains propylene glycol, saccharin sodium; bubble-gum flavor]

Tablet Chewable, Oral, as hydrochloride:

Histex: 1.25 mg [DSC] [dye free, sugar free; berry flavor]

Pharmacology

Mechanism of Action

Triprolidine is an H1-receptor antagonist, which provides dose-related suppression of histamine-induced wheel and flare reactions (Simons 1986). It is useful for the prevention and suppression of the signs and symptoms of allergic rhinitis and other upper respiratory allergies.

Pharmacokinetics/Pharmacodynamics

Metabolism

Extensively hepatic (Simons 1986)

Excretion

Urine (~1% as unchanged triprolidine) (Simons 1986)

Time to Peak

1.7 ± 0.5 hours (Simons 1986)

Half-Life Elimination

2.1 ± 0.8 hours (Simons 1986)

Use: Labeled Indications

Upper respiratory allergies: Temporary relief of runny nose; sneezing; itchy nose and throat; and itchy, watery eyes caused by hay fever (allergic rhinitis) or other upper respiratory allergies.

Contraindications

OTC labeling: When used for self-medication, do not use if you are taking sedatives or tranquilizers or with any other triprolidine-containing products.

Documentation of allergenic cross-reactivity for Antihistamines is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Dosage and Administration

Dosing: Adult

Upper respiratory allergies: Oral: 2.5 mg every 4 to 6 hours (maximum 10 mg/day)

Dosing: Geriatric

Avoid use (Beers Criteria [AGS 2019]).

Dosing: Pediatric

Note: Oral liquid formulations (liquid, syrup) are available in multiple concentrations; use caution when ordering and/or administering to avoid confusion; verify concentration. Safety and efficacy for the use of cough and cold products in infants and young children is limited; the AAP warns against the use of these products for respiratory illnesses in infants and young children; the FDA does not recommend OTC use in infants and children <2 years of age due to the risk of serious and life-threatening adverse effects (including death) and recommends to use with caution in pediatric patients ≥2 years of age (AAP 2018; FDA 2017).

Upper respiratory allergies:

Oral liquid:

Triprolidine 0.313 mg/mL: Oral:

Infants ≥4 months and Children <2 years: 1 mL (0.313 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 2 to <4 years: 2 mL (0.626 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 4 to <6 years: 3 mL (0.939 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 6 to <12 years: 4 mL (1.252 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children ≥12 years and Adolescents: 8 mL (2.504 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Triprolidine 0.625 mg/mL: Oral:

Infants ≥4 months and Children <2 years: 0.5 mL (0.313 mg) every 6 hours; do not exceed 4 doses in 24 hours

Children 2 to <4 years: 1 mL (0.625 mg) every 6 hours; do not exceed 4 doses in 24 hours

Children 4 to <6 years: 1.5 mL (0.938 mg) every 6 hours; do not exceed 4 doses in 24 hours

Children 6 to <12 years: 2 mL (1.25 mg) every 6 hours; do not exceed 4 doses in 24 hours

Children ≥12 years and Adolescents: 4 mL (2.5 mg) every 6 hours; do not exceed 4 doses in 24 hours

Triprolidine 0.938 mg/mL: Oral:

Infants ≥4 months and Children <2 years: 0.33 mL (0.31 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 2 to <4 years: 0.67 mL (0.628 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 4 to <6 years: 1 mL (0.938 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Triprolidine 1.25 mg/mL: Oral:

Infants 4 months to <2 years: 0.25 mL (0.313 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 2 to <4 years: 0.5 mL (0.625 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children 4 to <6 years: 0.75 mL (0.938 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Oral syrup:

Triprolidine 2.5 mg/5 mL: Oral:

Children 6 to <12 years: 2.5 mL (1.25 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children ≥12 years and Adolescents: 5 mL (2.5 mg) every 4 to 6 hours; do not exceed 4 doses in 24 hours

Tablet, chewable (1.25 mg/tablet): Oral:

Children 6 to <12 years: 1.25 mg every 4 to 6 hours; do not exceed 4 doses in 24 hours

Children ≥12 years and Adolescents: 2.5 mg every 4 to 6 hours; do not exceed 4 doses in 24 hours

Administration

Oral: Administer with enclosed dropper.

Storage

Store at room temperature.

Drug Interactions

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. Monitor therapy

Amphetamines: May diminish the sedative effect of Antihistamines. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Consider therapy modification

Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Monitor therapy

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Consider therapy modification

Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving antihistamines (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Consider therapy modification

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Monitor therapy

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Avoid combination

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Monitor therapy

Pitolisant: Antihistamines may diminish the therapeutic effect of Pitolisant. Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Avoid combination

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Consider therapy modification

Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Tetrahydrocannabinol and Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification

Adverse Reactions

There are no adverse reactions listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

  • CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery, driving).

Concurrent drug therapy issues:

  • Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

  • Pediatric: Antihistamines may cause excitation in young children.

Dosage form specific issues:

  • Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated with hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007). See manufacturer's labeling.

Other warnings/precautions:

  • Appropriate use: Prior to self-medication (OTC use), contact health care provider if you have breathing problems (eg, chronic bronchitis, emphysema), glaucoma, or difficulty urinating because of enlarged prostate. Discontinue use and contact health care provider if new symptoms develop; if symptoms do not improve within 7 days or are accompanied by fever; or if nervousness, dizziness or sleeplessness occur. Do not exceed recommended dosage.

Pregnancy

Pregnancy Considerations

Information related to the use of triprolidine in pregnancy is limited (Aldridge 2014; Gilboa 2009). Antihistamines may be used for the treatment of rhinitis in pregnant women, although agents other than triprolidine may be preferred (Wallace 2008).

Patient Education

  • Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
  • Patient may experience fatigue or anxiety (HCAHPS).
  • Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Source: Wolters Kluwer Health. Last updated February 6, 2020.