Triprolidin

The following link will take the user to the National Toxicology Program (NTP) Test Agent Search Results page, which tabulates all of the "Standard Toxicology & Carcinogenesis Studies", "Developmental Studies", and "Genetic Toxicity Studies" performed with this chemical. Clicking on the "Testing Status" link will take the user to the status (i.e., in review, in progress, in preparation, on test, completed, etc.) and results of all the studies that the NTP has done on this chemical. [http://ntp-apps.niehs.nih.gov/ntp_tox/index.cfm?fuseaction=ntpsearch.searchresults&searchterm=486-12-4]

In acute poisoning with H1 antagonists, their central excitatory effects constitute the greatest danger. The syndrome includes hallucinations, excitement, ataxia, incoordination, athetosis, and convulsions. Fixed, dilated pupils with a flushed face, together with sinus tachycardia, urinary retention, dry mouth, and fever, lend the syndrome a remarkable similarity to that of atropine poisoning. Terminally, there is deepening coma with cardiorespiratory collapse and death, usuallY within 2 to 18 hours. Treatment is along general symptomatic and supportive lines. /Histamine Antagonists: H1 Antagonists/

... SIDE EFFECTS INCL DRYNESS OF ... RESP PASSAGES, SOMETIMES INDUCING COUGH; URINARY FREQUENCY & DYSURIA; PALPITATION; HYPOTENSION; HEADACHE; TIGHTNESS OF CHEST; TINGLING, HEAVINESS, & WEAKNESS OF HANDS. ... ALLERGIC DERMATITIS IS NOT UNCOMMON. /ANTIHISTAMINES/

IN SMALL CHILD ... SYNDROME OF POISONING INCL ... ATAXIA, INCOORDINATION, ATHETOSIS ... FIXED, DILATED PUPILS WITH FLUSHED FACE ... ARE COMMON. /ANTIHISTAMINES/

ALTHOUGH H1-BLOCKING DRUGS HAVE RELATIVELY HIGH MARGIN OF SAFETY, ACUTE POISONING WITH THEM IS COMMON. ... IN CHILDREN, 20 TO 30 TABLETS OR CAPSULES OF MOST COMMERCIALLY AVAILABLE ANTIHISTAMINES REPRESENTS LETHAL OR NEAR-LETHAL DOSE. /ANTIHISTAMINES/

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

triprolidine

DILI Negative

Oral

DOI:10.1016/j.drudis.2019.09.022

Externally tested on the eyes of rabbits and found to have a toxicity rating of 5, according to the degree of injury observed after 24 hr. The test is based on a scale of 1-10, with 1 being the least amount of injury.

H1 blockers are among the many drugs that induce hepatic microsomal enzymes, and they may facilitate their own metabolism. /Histamine Antagonists: H1 Antagonists/

Use is not recommended in newborn or premature infants because this age group has an increased susceptibility to anticholinergic side effects, such as central nervous system excitation, and an increased tendency toward convulsions. A paradoxical reaction characterized by hyperexcitability may occur in children taking antihistamines. /Antihistamines/

Dizziness, sedation, confusion, and hypotension may be more likely to occur in geriatric patients taking antihistamines. Geriatric patients are especially susceptible to the anticholinergic side effects, such as dryness of mouth and urinary retention (especially in males), of the antihistamines. If these side effects occur and continue or are severe, medication should probably be discontinued. /Antihistamines/

THERE IS NO SPECIFIC THERAPY FOR ANTIHISTAMINE POISONING, AND TREATMENT IS ALONG GENERAL SYMPTOMATIC AND SUPPORTIVE LINES. ... SHOULD BREATHING FAIL, MECH SUPPORT OF VENTILATION OFFER SAFER AND ... EFFECTIVE MEANS OF MAINTAINING RESP THAN USE OF ANALEPTICS WHICH ARE PRONE TO INITIATE OR INTENSIFY CONVULSIVE PHASE. /ANTIHISTAMINES/

4 to 6 hours.

Elimination: 3 to 3.3 hours

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.

Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)

Rapidly absorbed in the intestinal tract.

The H1 antagonists are well absorbed from the GI tract. Following oral administration, peak plasma concn are achieved in 2 to 3 hr and effects usually last 4 to 6 hr; however, some of the drugs are much longer acting ... . /Histamine Antagonists: H1 Antagonists/

... H1 antagonists are eliminated more rapidly by children than by adults and more slowly in those with severe liver disease. /Histamine Antagonists: H1 Antagonists/