Trandolapril

Brands of Trandolapril in Kenya:

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Trandolapril in Kenya : Cost, Price, Chemical Structure, Brands
Trandolapril Chemical structure

MODE OF ACTION:

Trandolapril is deesterified to the diacid metabolite, trandolaprilat, which is approximately eight times more active as an inhibitor of ACE activity. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor, angiotensin II. Angiotensin II is a potent peripheral vasoconstrictor that also stimulates secretion of aldosterone by the adrenal cortex and provides negative feedback for renin secretion. The effect of trandolapril in hypertension appears to result primarily from the inhibition of circulating and tissue ACE activity thereby reducing angiotensin II, decreasing vasoconstriction, decreasing aldosterone secretion, and increasing plasma renin. Decreased aldosterone secretion leads to diuresis, natriuresis, and a small increase of serum potassium.


INDICATIONS

Hypertension
Trandolapril is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive medication such as hydrochlorothiazide.
Heart Failure Post Myocardial Infarction or Left-Ventricular Dysfunction Post Myocardial Infarction
Trandolapril is indicated in stable patients who have evidence of left-ventricular systolic dysfunction (identified by wall motion abnormalities) or who are symptomatic from congestive heart failure within the first few days after sustaining acute myocardial infarction. Administration of trandolapril to Caucasian patients has been shown to decrease the risk of death (principally cardiovascular death) and to decrease the risk of heart failure-related hospitalization

CONTRAINDICATIONS

Trandolapril  is contraindicated in patients who are hypersensitive to this product, in patients with hereditary/idiopathic angioedema and in patients with a history of angioedema related to previous treatment with an ACE inhibitor.
Pharmacokinetics and Metabolism
Pharmacokinetics
Trandolapril’s ACE-inhibiting activity is primarily due to its diacid metabolite, trandolaprilat. Cleavage of the ester group of trandolapril, primarily in the liver, is responsible for conversion. Absolute bioavailability after oral administration of trandolapril is about 10% as trandolapril and 70% as trandolaprilat. After oral trandolapril under fasting conditions, peak trandolapril levels occur at about one hour and peak trandolaprilat levels occur between 4 and 10 hours. The elimination half-life of trandolapril is about 6 hours. At steady state, the effective half-life of trandolaprilat is 22.5 hours. Like all ACE inhibitors, trandolaprilat also has a prolonged terminal elimination phase, involving a small fraction of administered drug, probably representing binding to plasma and tissue ACE. During multiple dosing of trandolapril, there is no significant accumulation of trandolaprilat. Food slows absorption of trandolapril, but does not affect AUC or Cmax of trandolaprilat or Cmax of trandolapril.
Metabolism and Excretion
After oral administration of trandolapril, about 33% of parent drug and metabolites are recovered in urine, mostly as trandolaprilat, with about 66% in feces. The extent of the absorbed dose which is biliary excreted has not been determined. Plasma concentrations (Cmax and AUC of trandolapril and Cmax of trandolaprilat) are dose proportional over the 1-4 mg range, but the AUC of trandolaprilat is somewhat less than dose proportional. In addition to trandolaprilat, at least 7 other metabolites have been found, principally glucuronides or deesterification products.
Serum protein binding of trandolapril is about 80%, and is independent of concentration. Binding of trandolaprilat is concentration-dependent, varying from 65% at 1000 ng/mL to 94% at 0.1 ng/mL, indicating saturation of binding with increasing concentration.
The volume of distribution of trandolapril is about 18 liters. Total plasma clearances of trandolapril and trandolaprilat after approximately 2 mg IV doses are about 52 liters/hour and 7 liters/hour respectively. Renal clearance of trandolaprilat varies from 1-4 liters/hour, depending on dose.

Drug Interactions

Trandolapril did not affect the plasma concentration (pre-dose and 2 hours post-dose) of oral digoxin (0.25 mg). Coadministration of trandolapril and cimetidine led to an increase of about 44% in Cmax for trandolapril, but no difference in the pharmacokinetics of trandolaprilat or in ACE inhibition. Coadministration of trandolapril and furosemide led to an increase of about 25% in the renal clearance of trandolaprilat, but no effect was seen on the pharmacokinetics of furosemide or trandolaprilat or on ACE inhibition.

ADVERSE DRUG REACTIONS

General Body Function
Chest pain.
Cardiovascular
AV first degree block, bradycardia, edema, flushing, and palpitations.
Central Nervous System
Drowsiness, insomnia, paresthesia, vertigo.
Dermatologic
Pruritus, rash, pemphigus.
Eye, Ear, Nose, Throat
Epistaxis, throat inflammation, upper respiratory tract infection.
Emotional, Mental, Sexual States
Anxiety, impotence, decreased libido.
Gastrointestinal
Abdominal distention, abdominal pain/cramps, constipation, dyspepsia, diarrhea, vomiting, nausea.
Hemopoietic
Decreased leukocytes, decreased neutrophils.
Metabolism and Endocrine
Increased liver enzymes including SGPT (ALT).
Musculoskeletal System
Extremity pain, muscle cramps, gout.
Pulmonary
Dyspnea.
Postmarketing
The following adverse reactions were identified during post approval use of MAVIK. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
General Body Function
Malaise, fever.
Cardiovascular
Myocardial infarction, myocardial ischemia, angina pectoris, cardiac failure, ventricular tachycardia, tachycardia, transient ischemic attack, arrhythmia.
Central Nervous System
Cerebral hemorrhage.
Dermatologic
Alopecia, sweating, Stevens-Johnson syndrome and toxic epidermal necrolysis.
Emotional, Mental, Sexual States
Hallucination, depression.
Gastrointestinal
Dry mouth, pancreatitis, jaundice and hepatitis.
Hemopoietic
Agranulocytosis, pancytopenia.
Metabolism and Endocrine
Increased SGOT (AST).
Pulmonary
Bronchitis.
Renal and Urinary
Renal failure.

Reporting of suspected adverse reactions

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:


Trandolapril in Kenya
Trandolapril in Kenya
Trandolapril price in Kenya
Trandolapril Brands in Kenya

Trandolapril in Kenya
Trandolapril price in Kenya
Trandolapril Brands in Kenya formation

Clinical | Pharmacokinetic data


Pregnancy Category: D : Evidence of risk
Routes of Administration: Oral
Bioavailability: Not Available
Protein Binding: Trandolapril 80% (independent of concentration) Trandolaprilat 65 to 94% (concentration-dependent)
Metabolosim: Liver
Onset of Action: Not Available
Elimination Half life: 6 hours (trandolapril) 10 hours (trandolaprilat)
Excretion: Fecal and Kidney

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This Drug is not Subject to DDA drugs Act
Dosage Forms | Strengths:
Tablets

Drug Indentifiers:

CAS Number
PubChem
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard


Drug Images

References/ Citation:




What was the patient being treated for
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