Trandolapril
Encyclopedia
Trandolapril is an ACE inhibitor
used to treat high blood pressure, it may also be used to treat other conditions.
It is marketed by Abbott Laboratories
with the brand name Mavik.
that is deesterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system. Trandolapril has a half life of about 6 hours, and trandolaprilat has a half life of about 10. Trandolaprilat has about 8 times the activity of its parent drug. Approximately 1/3 of Trandolapril and its metabolites are excreted in the urine, and about 2/3 of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%.
Trandolapril acts by competitive inhibition of Angiotensin Converting Enzyme (ACE), a key enzyme in the renin-angiotensin system
(RAS pathway) which plays an important role in regulating blood pressure.
Side effects reported for trandolapril include nausea
, vomiting
, or diarrhea
; headache
; dry cough; dizziness
or lightheadedness
when sitting up or standing; hypotension
or fatigue
.
Patients also on diuretics may experience an excessive reduction of blood pressure after initiation of therapy with trandolapril. Trandolapril can reduce potassium loss caused by thiazide diuretics, and increase serum potassium when used alone. Therefore hyperkalemia
is a possible risk. Increased serum lithum levels can occur in patients who are also on lithium.
Trandolapril is teratogenic (US: pregnancy category
D) and can cause birth defects and even death of the developing fetus.
The highest risk to the fetus is during the second and third trimester. When pregnancy is detected, trandolapril should be discontinued as soon as possible.
Trandolapril should not be administed to nursing mothers.
and trandolapril has been found to reduce fibrosis
in obstructive uropathy
.
ACE inhibitor
ACE inhibitors or angiotensin-converting enzyme inhibitors are a group of drugs used primarily for the treatment of hypertension and congestive heart failure...
used to treat high blood pressure, it may also be used to treat other conditions.
It is marketed by Abbott Laboratories
Abbott Laboratories
Abbott Laboratories is an American-based global, diversified pharmaceuticals and health care products company. It has 90,000 employees and operates in over 130 countries. The company headquarters are in Abbott Park, North Chicago, Illinois. The company was founded by Chicago physician, Dr....
with the brand name Mavik.
Pharmacology
Trandolapril is a prodrugProdrug
A prodrug is a pharmacological substance administered in an inactive form. Once administered, the prodrug is metabolised in vivo into an active metabolite, a process termed bioactivation. The rationale behind the use of a prodrug is generally for absorption, distribution, metabolism, and...
that is deesterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system. Trandolapril has a half life of about 6 hours, and trandolaprilat has a half life of about 10. Trandolaprilat has about 8 times the activity of its parent drug. Approximately 1/3 of Trandolapril and its metabolites are excreted in the urine, and about 2/3 of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%.
Mode of action
Trandolapril acts by competitive inhibition of Angiotensin Converting Enzyme (ACE), a key enzyme in the renin-angiotensin system
Renin-angiotensin system
The renin-angiotensin system or the renin-angiotensin-aldosterone system is a hormone system that regulates blood pressure and water balance....
(RAS pathway) which plays an important role in regulating blood pressure.
Side effects
Side effects reported for trandolapril include nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
, vomiting
Vomiting
Vomiting is the forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose...
, or diarrhea
Diarrhea
Diarrhea , also spelled diarrhoea, is the condition of having three or more loose or liquid bowel movements per day. It is a common cause of death in developing countries and the second most common cause of infant deaths worldwide. The loss of fluids through diarrhea can cause dehydration and...
; headache
Headache
A headache or cephalalgia is pain anywhere in the region of the head or neck. It can be a symptom of a number of different conditions of the head and neck. The brain tissue itself is not sensitive to pain because it lacks pain receptors. Rather, the pain is caused by disturbance of the...
; dry cough; dizziness
Dizziness
Dizziness refers to an impairment in spatial perception and stability. The term is somewhat imprecise. It can be used to mean vertigo, presyncope, disequilibrium, or a non-specific feeling such as giddiness or foolishness....
or lightheadedness
Lightheadedness
Light-headedness is a common and often unpleasant sensation of dizziness and/or feeling that one may be about to faint, which may be transient, recurrent, or occasionally chronic. In some cases, the individual may feel as though his or her head is weightless. The individual may also feel as...
when sitting up or standing; hypotension
Hypotension
In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...
or fatigue
Fatigue (physical)
Fatigue is a state of awareness describing a range of afflictions, usually associated with physical and/or mental weakness, though varying from a general state of lethargy to a specific work-induced burning sensation within one's muscles...
.
Possible drug interactions
Patients also on diuretics may experience an excessive reduction of blood pressure after initiation of therapy with trandolapril. Trandolapril can reduce potassium loss caused by thiazide diuretics, and increase serum potassium when used alone. Therefore hyperkalemia
Hyperkalemia
Hyperkalemia refers to the condition in which the concentration of the electrolyte potassium in the blood is elevated...
is a possible risk. Increased serum lithum levels can occur in patients who are also on lithium.
Pregnancy and lactation
Trandolapril is teratogenic (US: pregnancy category
Pregnancy category
The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. It does not include any risks conferred by pharmaceutical agents or their metabolites that are present in breast...
D) and can cause birth defects and even death of the developing fetus.
The highest risk to the fetus is during the second and third trimester. When pregnancy is detected, trandolapril should be discontinued as soon as possible.
Trandolapril should not be administed to nursing mothers.
Additional effects
Combination therapy with paricalcitolParicalcitol
Paricalcitol is a drug used for the prevention and treatment of secondary hyperparathyroidism associated with chronic renal failure...
and trandolapril has been found to reduce fibrosis
Fibrosis
Fibrosis is the formation of excess fibrous connective tissue in an organ or tissue in a reparative or reactive process. This is as opposed to formation of fibrous tissue as a normal constituent of an organ or tissue...
in obstructive uropathy
Obstructive uropathy
Obstructive uropathy is a structural or functional hindrance of normal urine flow, sometimes leading torenal dysfunction .It is a very broad term, and does not imply a location or etiology.-Causes:...
.
External links
- Mavik (PDF from manufacturer's website)
- Tarka (PDF from manufacturer's website)
- Trandolapril (patient information)
- Trandolapril Information - rxlist.com (Rxlist.com, The Internet Drug Index)