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Trandolapril

Pronouncation: (tran-DOE-lah-prill)
Class: Angiotensin converting enzyme (ACE) inhibitor

Trade Names:
Mavik
- Tablets 1 mg
- Tablets 2 mg
- Tablets 4ߙmg

Pharmacology

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Reduces the formation of the vasopressor hormone angiotensin II by inhibiting ACE. Results in decreased BP and reduced sodium reabsorption and potassium retention.

Pharmacokinetics

Absorption

Food slows absorption, but does not affect AUC. Plasma concentration and AUC are dose-proportional. Bioavailability is 10% as trandolapril and 70% as trandolaprilat (metabolite). T _max is 1 h for trandolapril and 4ߙto 10 h for trandolaprilat.

Distribution

Trandolapril is 80% protein bound and is independent of concentration. Binding of trandolaprilat is concentration-dependent (from 65% to 94%). Vd is 18ߙL.

Metabolism

Trandolaprilat is the major metabolite and is 8 times more active than trandolapril. Other metabolites are glucuronides or de-esterification products.

Elimination

33% of parent drug and metabolites are recovered in urine and 66% in feces. Trandolapril t _½ is 6 h. The t _½ of trandolaprilat is 10 h.

Peak

Time to peak effect is 4 h.

Duration

Duration of action is 24 h.

Special Populations

Renal Function Impairment

Plasma trandolapril and trandolaprilat are approximately 2-fold greater and renal Cl is decreased approximately 85% in patients with Ccr less than 30 mL/min and in hemodialysis patients.

Hepatic Function Impairment

In patients with mild to moderate alcoholic cirrhosis, plasma concentration of trandolapril and trandolaprilat were 9- and 2-fold greater, respectively, but inhibition of ACE activity was not affected. Consider lower doses in hepatic insufficiency.

Elderly

In patients 65 yr and older, plasma concentrations of trandolapril are increased in hypertension.

Indications and Usage

Heart Failure Post-MI/Left-Ventricular Dysfunction Post-MI

For stable patients who have evidence of left-ventricular systolic dysfunction (identified by wall motion abnormalities) or who are symptomatic from CHF within the first few days after sustaining acute MI.

Hypertension

Treatment of hypertension either alone or in combination with other antihypertensive drugs.

Contraindications

Hypersensitivity or history of angioedema with any ACE inhibitor.

Dosage and Administration

Heart Failure Post-MI/Left-Ventricular Dysfunction Post-MI
Adults

PO 1 mg/day. Following initial dose, titrate patients (as tolerated) toward a target dosage of 4 mg/day.

Renal/Hepatic function impairment

PO For patients with a Ccr less than 30 mL/min or with hepatic cirrhosis, starting dosage is 0.5 mg/day.

Hypertension
Adults

PO 1 to 2 mg every day initially with usual maintenance doses of 2 to 4 mg every day.

Storage/Stability

Store tablets at controlled room temperature (68° to 77°F).

Drug Interactions

Capsaicin

Cough may be exacerbated.

Digoxin

May cause increased or decreased digoxin levels.

Diuretics

Possible hypotensive effect. Use lower starting doses.

Indomethacin, salicylates (eg, aspirin)

May reduce hypotensive effects, especially in low renin or volume-dependent hypertensive patients.

Lithium salts

Increased serum lithium levels and increased risk of lithium toxicity.

Loop diuretics

Effects of loop diuretics may be decreased.

Phenothiazines

Enhanced hypotensive effect.

Potassium supplements or potassium-sparing drugs

May increase serum potassium levels.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (11%); syncope (6%); bradycardia (5%); cardiogenic shock, intermittent claudication (4%); stroke (3%).

CNS

Dizziness (23%).

GI

Dyspepsia (6%); gastritis (4%); diarrhea (1%).

Lab Tests

Elevated serum uric acid (15%); elevated BUN (9%); elevated creatinine (5%).

Metabolic

Hyperkalemia, hypocalcemia (5%).

Musculoskeletal

Myalgia (5%).

Respiratory

Cough (35%).

Miscellaneous

Asthenia (3%); angioedema (0.13%); anaphylactoid reactions.

Precautions

Warnings

Pregnancy

When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.

Pregnancy

Category D (second and third trimester); Category C (first trimester).

Lactation

Undetermined. Avoid use in nursing women, if possible.

Children

Safety and efficacy not established.

Elderly

Reduce doses if needed.

Renal Function

Reduce dosage. Decreases in renal function may occur if renal function is dependent on the renin-angiotensin system; patients with renal artery stenosis may experience acute renal failure.

Anaphylactoid reactions

Angioedema and anaphylactoid reactions are rarely reported but are potentially life-threatening.

Angioedema

Use with extreme caution in patients with hereditary angioedema.

Cough

Chronic nonproductive cough may occur.

Hepatic failure

May occur. Discontinue drug if patient develops jaundice.

Hypotension/first-dose effect

Hypotension may occur during initiation of therapy, especially in patients with severe salt or volume depletion or those with CHF.

Neutropenia or agranulocytosis

Has occurred with other ACE inhibitors; risk appears greater in patients with renal dysfunction, heart failure, or immunosuppression. Periodically monitor WBC counts in these patients.

Overdosage

Symptoms

Hypotension.

Patient Information

Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
Advise patient to try to take each dose at about the same time each day.
Inform hypertensive patient that drug controls, but does not cure, hypertension and to continue taking drug as prescribed even when BP is not elevated.
Caution patient not to change the dose or stop taking unless advised by health care provider.
Instruct patient to continue taking other medications for condition as prescribed by health care provider.
Instruct patient in BP and pulse measurement skills.
Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
Emphasize to hypertensive patient the importance of the following other modalities on BP control: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
Emphasize to heart failure patient the importance of the following other modalities that can help control heart failure symptoms: weight control, progressive exercise program, smoking cessation, and moderate intake of alcohol and salt.
Advise heart failure patient to weigh daily, keep a record of daily weights, and notify health care provider if rapid weight gain (eg, 5 pounds in 1 wk) is noted or if edema or shortness of breath are getting worse.
Caution patient that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to excessive fall in BP resulting in lightheadedness or fainting.
Advise patient that medication may cause dizziness or lightheadedness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
Instruct patient to stop taking drug and immediately report any of the following symptoms to health care provider: sore throat, fever, swelling of the hands or feet, irregular heartbeat, chest pains, fainting, swelling of the face, lips, eyelids, or tongue, difficulty breathing.
Instruct patient to inform health care provider if a persistent cough develops while taking this medication.