Trandolapril (trandolapril)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Trandolapril is an angiotensin-converting enzyme (ACE) inhibitor.
Trandolapril is an angiotensin-converting enzyme (ACE) inhibitor. Trandolapril undergoes deesterification to trandolaprilat in the liver, which is approximately 8 times more active at inhibiting ACE. The effect of trandolapril in reducing blood pressure appears to result primarily from inhibiting circulating and tissue ACE activity, which reduces angiotensin II formation, and results in decreased vasoconstriction, aldosterone secretion, and increased plasma renin.
A reduction in aldosterone secretion leads to diuresis, natriuresis, and small increases in serum potassium levels (averaging 0.1 mEq/L). A single 2-mg dose of trandolapril results in 70-85% inhibition of plasma ACE activity after 4 hours. Inhibition of plasma ACE activity declines by about 10% after 24 hours and by 50% after 8 days.
With chronic administration, maximum blood pressure lowering is attained within 1 week.
Following oral administration, absolute bioavailability is approximately 10% as trandolapril and approximately 70% as trandolaprilat. When administered under fasting conditions, peak plasma concentrations of trandolapril occur at about 1 hour and peak trandolaprilat levels occur between 4-10 hours. Administration of trandolapril with food decreases the rate of absorption, but does not affect the extent of absorption or peak plasma concentrations of the drug; the pharmacokinetic effects of food are not considered to be clinically significant.
The ACE activity of trandolapril is primarily due to its metabolite, trandolaprilat, which is converted from trandolapril in hepatocytes. In addition to trandolaprilat, there are at least 7 other metabolites, principally glucuronide conjugates or de-esterification products. Following oral administration of trandolapril, about a third of the parent drug and metabolites are recovered in the urine (mostly as trandolaprilat), and two-thirds are recovered in the feces.
Trandolapril is approximately 80% bound to plasma proteins independent of concentration, whereas binding of trandolaprilat is concentration-dependent (65% at 1000 ng/mL and 94% at 0.1 ng/mL). The elimination half-life of trandolapril is approximately 6 hours, and the elimination half-life of trandolaprilat is 22.5 hours.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. It is also used to treat heart failure and to improve survival after a heart attack.
Trandolapril belongs to a class of drugs known as ACE inhibitors. It works by relaxing blood vessels so blood can flow more easily.
Generic name: trandolapril
Pronunciation: (tran-DOL-a-pril)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Trandolapril
Indications
The following indications are listed for Trandolapril:
- Chronic Heart Failure
- Hypertension
- Left Ventricular Dysfunction Following Myocardial Infarction
Also known as: Congestive Heart Failure, Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Left Ventricular Dysfunction Following Acute Mi, Left Ventricular Dysfunction Following Acute Myocardial Infarction, Left Ventricular Dysfunction Following Ami, Left Ventricular Dysfunction Following Cardiac Infarct, Left Ventricular Dysfunction Following Cardiac Infarction, Left Ventricular Dysfunction Following Myocardial Infarct, Lv Dysfunction Following Mi, Systemic Arterial Hypertension.
Dosing
Dosage of trandolapril should be adjusted according to patient tolerance and response in all patients. Dosage should be adjusted carefully under close medical supervision in patients with heart failure, with or without associated renal insufficiency, because of the risk of hypotension; such patients should be followed closely for at least 2 weeks after initiation of trandolapril or diuretic therapy or dosage adjustment of either drug.
Trandolapril is administered orally. The manufacturer makes no specific recommendations for administering the drug with regard to meals.
Trandolapril is commercially available as 1 mg, 2 mg, and 4 mg tablets. Trandolapril is also commercially available in fixed combination with verapamil hydrochloride as extended-release tablets. See the prescribing information for additional information on the fixed combination preparation.
Store trandolapril tablets at 20-25degreesC (excursions permitted to 15-30degreesC).
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this 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
*Known hypersensitivity (e.g., history of angioedema) to trandolapril, another angiotensin-converting enzyme (ACE) inhibitor, or any ingredient in the formulation.
*History of hereditary/idiopathic angioedema.
*Concomitant aliskiren therapy in patients with diabetes mellitus.
*Concomitant use (within 36 hours) of a neprilysin inhibitor (e.g., sacubitril).
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
Adverse effects reported in >=1% of patients receiving trandolapril for the treatment of hypertension include cough, dizziness, and diarrhea.
Adverse effects reported at a greater frequency in patients receiving trandolapril for the treatment of left ventricular dysfunction after acute myocardial infarction (MI) compared to placebo include cough, dizziness, hypotension, hyperuricemia, elevated BUN concentrations, percutaneous transluminal coronary angioplasty (PTCA) or coronary artery bypass grafting (CABG), dyspepsia, syncope, hyperkalemia, bradycardia, hypocalcemia, myalgia, elevated serum creatinine concentrations, gastritis, cardiogenic shock, intermittent claudication, stroke, and asthenia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The manufacturer states that efficacy and safety of trandolapril in pediatric patients younger than 18 years of age have not been established.
If oliguria or hypotension occurs in neonates with a history of in utero exposure to trandolapril, blood pressure and renal function should be supported; exchange transfusions or dialysis may be required.
Drugs that act on the renin-angiotensin system (e.g., ACE inhibitors, angiotensin II receptor antagonists) reduce fetal renal function and increase fetal and neonatal morbidity and mortality when used in pregnancy during the second and third trimesters. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal effects include skull hypoplasia, anuria, hypotension, renal failure, and death.
Appropriate management of maternal hypertension during pregnancy is important to optimize outcomes for both the mother and fetus. Discontinue trandolapril as soon as possible when pregnancy is detected.
In the rare situation that use of trandolapril is deemed necessary, apprise the mother of the potential risk to the fetus. Perform serial ultrasound examinations to assess the intraamniotic environment. Fetal testing may be appropriate, based on the week of pregnancy; however, oligohydramnios may not appear until after the fetus has sustained irreversible injury. If oligohydramnios is observed, discontinue trandolapril unless it is considered lifesaving for the mother. Closely observe infants with histories of in utero exposure to trandolapril for hypotension, oliguria, and hyperkalemia.
Trandolapril and its metabolites are distributed into milk in rats.
Because of the potential for serious adverse reactions from trandolapril in nursing infants, the manufacturer states that the drug should not be used in nursing women.
The manufacturer makes no specific dosage recommendations in geriatric patients.
No substantial differences in safety and efficacy have been observed in geriatric patients relative to younger adults, but increased sensitivity cannot be ruled out.
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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