Trientine Hcl (trientine HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Trientine is a heavy metal antagonist that selectively chelates copper.
Trientine is a selective copper chelating agent that is structurally distinct from penicillamine; the drug forms a stable complex with copper that is readily excreted by the kidneys. Trientine also chelates other metals including iron and zinc. Urinary concentrations of copper, zinc, and iron increase in parallel with trientine excretion.
On a molar basis, trientine appears to be less potent than penicillamine as a cupriuretic agent in patients with Wilson disease. Following single oral doses of trientine hydrochloride (1.2 g) or penicillamine (500 mg), the 6-hour urinary copper excretion rate was 234 or 320 mcg, respectively, in patients previously treated with penicillamine, and 1326 or 1074 mcg, respectively, in treatment-naive patients.
Results of various trials in patients with Wilson disease, healthy volunteers, and diabetic patients indicate that peak plasma concentrations of trientine occur between 0.8-4 hours following oral administration. Food inhibits absorption of the drug. Trientine is metabolized to 2 major acetyl metabolites, DAT and MAT.
Although MAT also has chelating properties, the metabolite is a substantially weaker chelator of copper, iron, and zinc than the parent drug. Approximately 1% of an administered dose of trientine hydrochloride is excreted in the urine as unchanged drug and 8% is excreted as acetyl metabolites. In a study in healthy individuals, pharmacokinetics of trientine did not substantially differ between those with a fast or slow N-acetyltransferase (NAT) 2 phenotype, indicating that NAT 2 is unlikely to be responsible for the acetylation of trientine.
Following single-dose and steady-state dosing of trientine hydrochloride in healthy individuals, increased cupruresis was most evident during the first 12 hours with the highest rate occurring within the first 4 hours. Half-life of trientine hydrochloride is about 1.3-4 hours following single dosing, and about 10 hours following steady-state dosing at 1.2 g daily. The mean terminal half-life of trientene ranges from 13.8-16.5 hours.
After administration of 900 mg (3 tablets) of trientine tetrahydrochloride, the mean AUC was 11% lower compared to 750 mg (3 capsules) of trientine hydrochloride. After administration of 1500 mg (5 tablets) of trientine tetrahydrochloride, the mean AUC was comparable to 1250 mg (5 capsules) of trientine hydrochloride.
USES: This medication is used to treat a certain inherited disorder (Wilson's disease). This disorder causes too much copper to build up in the liver, brain, and other parts of the body. Trientine works by binding to copper, which helps your body get rid of extra copper.
This can decrease symptoms such as problems with speech/swallowing/coordination, tiredness, lack of appetite, abdominal pain, yellowing eyes/skin, fluid buildup in the legs/abdomen, uncontrolled movements, or muscle stiffness.
Generic name: trientine HCl
Pronunciation: (TRYE-en-teen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Trientine Hcl
Indications
The following indications are listed for Trientine Hcl:
- Wilson's Disease
Also known as: Hepatolenticular Degeneration, Lenticular Progressive Degeneration, Strumpell-Westphal Disease, Westphal's Disease, Westphal's Pseudosclerosis, Westphal-Strumpell Pseudosclerosis, Wilson's Syndrome.
Dosing
Recommended dosage regimens of trientine hydrochloride are based on limited clinical experience; studies have not been conducted evaluating specific doses and/or dosing intervals.
Trientine tetrahydrochloride is not substitutable on a mg-per-mg basis with other trientine products.
If switching from a trientine hydrochloride formulation to trientine tetrahydrochloride, note that the content of the active moiety (trientine base) is not the same as trientine tetrahydrochloride. A 250 mg capsuleof trientine hydrochloride contains 167 mg of trientine base; in contrast, each 300 mg tablet of trientine tetrahydrochloride contains 150 mg of trientine base.
Trientine hydrochloride capsules are administered orally on an empty stomach, at least 1 hour before or 2 hours after meals, and at least 1 hour apart from any other oraldrug, food, or milk. The total daily dosage should be administered in divided doses 2-4 times daily. The capsules should be swallowed whole with water and should not be opened or chewed.
Because of the potential for contact dermatitis, any site of exposure to the capsule contents should be washed immediately with water.
Store trientine hydrochloride capsulesin a tightly closed container in the refrigerator at 2-8oC.
Trientine tetrahydrochloride tablets are administered on an empty stomach, at least 1 hour before or 2 hours after meals, and at least 1 hour apart from any other oral drug, food, or milk. The total daily dosage should be administered in divided doses 2 times daily. The tablets should be swallowed whole without crushing, chewing, or dissolving. If a patient has difficulty swallowing a tablet whole, the scored tablet can be divided into 2 equal halves.
Do not remove trientine tetrahydrochloride tablets from blister packs until just before dosing and do not store tablets for future use after the blister has been opened.
Store trientine tetrahydrochloride tablets at 20-25degreesC; excursions permitted between 15-30degreesC.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Formal drug interaction studies have not been conducted to date with trientine. Administer trientene at least 1 hour apart from any oral drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Hypersensitivity to trientineor any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Data on adverse effects associated with trientine hydrochloridetherapy are limited; iron deficiency and systemic lupus erythematosus were reported in a clinical study of trientine in patients with Wilson disease.
The most common adverse effects (>5%) with trientine tetrahydrochloride are abdominal pain, change of bowel habits, rash, alopecia, and mood swings.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Although no controlled studies have been conducted specifically in pediatric patients, trientine hydrochloridehas been used clinically in patients as young as 6 years of age with no reported adverse experiences.
Because interruption of therapy for Wilson disease during pregnancy has resulted in acute liver failure, the American Association for the Study of Liver Diseases (AASLD) states that treatment should be continued during pregnancy. Although clinical experience is limited, use of trientine during pregnancy has been associated with successful outcomes for both mother and fetus. TheAASLD recommends that thedosage of trientine hydrochloride be reduced to the minimum necessary dosage during pregnancy, particularly during the third trimester, to promote better wound healing if cesarean section is performed. A dosage reduction of 25-50% of the pre-pregnancy dosage has been recommended with frequent monitoring of the patient.
The AASLD suggests that all medications used to treat Wilson disease are excreted into breast milk and generallyrecommends against use of these agents in nursing women due to the risk of causing copper deficiency in the infant.
The manufacturer makes no specific dosage recommendations for geriatric patients. Use caution and initiate treatmentat the lower end of the dosing range in geriatric patients.
Clinical studies of trientine did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients. Use trientine withcaution and initiate treatment at the lower end of the dosing range in geriatric patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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