Paper Example on Treating Hypertension & Heart Failure With Trandolapril

Trandolapril

It can be used in the treatment of mild to moderate hypertension. Its side effects include drowsiness, headache, vertigo, epistaxis, neutropenia, hyperuricemia, dyspnea, decreased libido.

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Indications: it can be used to treat hypertension, heart failure, and post-myocardial infarction

Contraindications: it should not be used on patients with induced angioedema, ACE hypersensitivity, and patients with diabetes mellitus, renal failure, and autoimmune disease and in pregnancy (Zhu et al., 2016)

Pharmacodynamics: inhibition of circulating and tissue ACE activity, decreases vasoconstriction, decrease secretion of aldosterone, decrease angiotensin II formation, and increase plasma renin.

Pharmacokinetics: 10% of it is bioavailable and 70% for the metabolite. 80% of it is protein-bound, and it is metabolized by the liver. About its 66% and 33% are excreted in feces and urine respectively within 6-10 hours (Bailey et al., 2017)

Benazepril

It can be used alone to treat high blood pressure or in combination with hydrochlorothiazide. It can also treat the failure of heart and diabetic neuropathy. Some reported side effects include abdominal pain, constipation, and impotence, loss of appetite and taste, severe dizziness, sore throat amongst other complications.

Indications: mild to essential hypertension

Contraindications: should not be used in patients with known hypersensitivity and those with a history of angioedema as a result of previous treatment using ACE inhibitors

Pharmacodynamics: Benazepril is activated to Benazeprilat. It then accelerates the transformation of angiotensin I to angiotensin II (which is a vasoconstrictor substance), which stimulates the adrenal cortex to produce aldosterone. Benazeprilat competes for attachment at the enzyme which converts angiotensin, preventing the transformation of ACE I to ACE II.

Pharmacokinetics: it is at least 37% bioavailable with a peak at half an hour or one hour. It is also 96.7% protein bound. The liver cleavages benazepril to benazeprilat which is joined to glucuronic acid and excreted in urine (Mochel et al., 2015)

Captopril

Captopril is used in the treatment of patients suffering from hypertension and congestive cardiac failure. It converts angiotensin I to angiotensin II as other ACE inhibitors. It has been reported to cause eosinophilia, anemia, cough, neutropenia, rash, fever, hypertension, pancytopenia, arthralgia and agranulocytosis

Indications: can be used on patients suffering from hypertension and congestive cardiac failure

Contraindications: should not be used on patients who are hypersensitive to it or other ACE inhibitors. It should be avoided in neonates. (Marte, F., & Cassagnol, M. (2018)

Pharmacodynamics: the two isomers of ACE (somatic and testicular forms). The C-domain of somatic isoform regulates the blood pressure, and the N-domain helps in differentiation and maturation of stem cells. Captopril has an inhibitory action on the C-domain

Pharmacokinetics: 60-75% is absorbed on fasting patients. It is also 25-30% bound to albumins. It has two main metabolites (captopril-cysteine disulfide and disulfide dimer of captopril) which usually undergo reversed mutual conversion (Peigneur, S., & Tytgat, J. 2018)

EnalaprilIt is a specific competitive ACE that converts angiotensin I to angiotensin II. Some known side effects are arthralgia, pancytopenia, rash, angioedema, neutropenia, eosinophilia, fever, and thrombocytopenia (Polverino et al., 2017)

Indications: can be used in the treatment of hypertension, proteinuria, congestive heart failure, and hypersensitive crisis.

Contraindications: should not be used on patients who are hypersensitive to it or any other ACE product. It should not be used in neonates and pediatric patients with glomerular filtration dysfunctions

Pharmacokinetics: it has nonlinear binding to plasma and tissues. Liver rapidly metabolizes enalapril to enalaprilat which converts ACE I to ACE II which regulates blood pressure.

Pharmacodynamics: it has an oral absorption of 60-70% and peak plasma concentration of one hour and clearance by four hours in the liver (Stage et al., 2017)

FosinoprilIt converts angiotensin I to angiotensin II and regulation of blood pressure, and it is a basic function of the renin-angiotensin-aldosterone system. The side effects are musculoskeletal pain, vomiting, creatinine, hyperkalemia, photosensitivity, Stevens-Johnson syndrome, anaphylactoid reactions, pancreatitis

Indications: used to treat mild-moderate hypertension

Contraindications: should not be used on patients having hypersensitivity to this product. It is also contraindicated to patients having hereditary angioedema, ACE inhibitor angioedema, and idiopathic angioedema

Pharmacodynamics: upon hydrolysis to fosinoprilat, it acts as a competitive inhibitor of RAAS. Renin cleaves angiotensin circulating in the blood to ATI by ACE which is then cleaved to ATII which then decreases blood pressure

Pharmacokinetics: it is converted to fosinoprilat which inhibit ACE which converts ATI to ATII thus regulates blood pressure (Araiza et al., 2015)

Lisinopril

The drug is effective to treat hypertension, congestive heart failure, and myocardial infarction in hemodynamically stable patients. It has been reported to cause neutropenia, anemia, thrombocytopenia, angioedema, kidney disease, agranulocytosis, pruritus, and arthralgia

Indication: used in hypertension and congestive heart failure

Contraindications: it is contraindicated to patients with hypersensitivity to Lisinopril and those who had shown signs of angioneurotic edema following previous treatment with it

Pharmacodynamics: it inhibits the effects of RAAS. It induces the secretion of aldosterone from the cortex of adrenal glands. Vasopressin is secreted following secretion of ATII which subsequently increases blood pressure by constricting arteries (Trachtman et al., 2015)

Pharmacokinetics: it is 20-25% bioavailable, which is not affected by food. It has a half-life of up to about 40 hours with an average peak of 12.6 hours. It does not bind to proteins. It is excreted through urine

MoexiprilIt is used to treat hypertension as well as renal impairment. It can lead to hypotension, myalgia, pharyngitis, sinusitis, hyponatremia, peripheral edema, syncope, proteinuria, hepatic and renal failure, agranulocytosis, pneumonitis.

Indication: it can be used to treat hypertension in children and adults as well as renal impairment.

Contraindications: should not be used in patients with a history of ACE I and other angioedema. It should not be used on diabetic patients with concomitant aliskiren

Pharmacokinetics: it is not completely absorbed with a maximum of 13% and is affected by food. It is 50% protein binding and is rapidly converted to moexiprilat in organ tissues. The drug has a half-life of 1 hour and is eliminated via the renal system

Pharmacodynamics: it works by restraining the ACE activity by resultant peripheral vasoconstriction and decreased ATII formation, increased plasma renin activity and low (Zisaki et al., 2015)

Ramipril

It is used in the treatment of hypertension, heart failure, and diabetic kidney disease. It causes side effects such as headaches, coughs, angioedema, high levels of potassium in blood and kidney problems (Augustin et al., 2018)

Indications: can be used on patients suffering from hypertension, heart failure and those having diabetic kidney disease

Contraindications: it should not be used in pregnancy and breastfeeding. It should not be used on patients with the renovascular disease, severe renal impairment, or those patients who have a history of reaction to it or other ACE products.

Pharmacodynamics: converted to ramiprilat in the liver which antagonizes effects of RAAS thus lowering blood pressure

Pharmacokinetics: it is absorbed up to 50-60% but affected by food. It is also about 73% protein binding and its metabolized by the liver. The metabolites are excreted through urine after 2-4 hours

Perindopril

It can be used in the treatment of hypertension and patients with stable coronary artery disease. Adverse effects include angioedema, hypotension, hyperkalemia, cough, impaired renal function, and neutropenia. (Mancia et al., 2015)

Indications: it is indicated to treat patients with essential hypertension and stable coronary artery disease.

Contraindications: it is contraindicated to patients having hypersensitivity to it or other ACE products and also to those patients having hereditary angioedema.

Pharmacodynamics: it is hydrolyzed to perindoprilat while decreases blood pressure by antagonizing the RAAS effect.

Pharmacokinetics: it has 65-75% bioavailable with 10-20% protein binding. It is highly metabolized in the liver and eliminated through urine. It has a life of 1.2 hours (Zheng et al., 2016)

For patients asking for an opinion about the angiotensin converting enzyme inhibitors medication, I would advise them to go through the manufacturer's provided precaution before deciding otherwise to use them to prevent the undesirable health effects these drugs may produce. With practical communication skills acquired through training, I will communicate to the patient the findings

References

Abrams, D., & Brodie, D., (2016). The clinical management of patients on partial/total extracorporeal support. Current opinion in critical care, 22(1), 73-79.

Alexander, S. P., Fabbro, D., Kelly, E., Marrion, N. V., Peters, J. A., Faccenda, E., ... & Davies, J. A. (2017). The concise guide to PHARMACOLOGY 2017/18: Enzymes. British journal of pharmacology, 174, S272-S359.

Bailey, K. R., Boerwinkle, E., Beitelshees, A. L., & Tanaka, T. (2017). Genetic Variants Associated With Uncontrolled Blood Pressure on Thiazide Diuretic/b-Blocker Combination Therapy in the PEAR (Pharmacogenomic Evaluation of Antihypertensive Responses) and INVEST (International Verapamil-SR Trandolapril Study) Trials.

Mochel, J. P., Fink, M., Peyrou, M., Soubret, A., Giraudel, J. M., & Danhof, M. (2015). Pharmacokinetic/pharmacodynamic modeling of renin-angiotensin-aldosterone biomarkers following angiotensin-converting enzyme (ACE) inhibition therapy with benazepril in dogs. Pharmaceutical research, 32(6), 1931-1946.

Strauss, M. H., & Hall, A. S. (2016). The divergent cardiovascular effects of angiotensin-converting enzyme inhibitors and angiotensin receptor blockers on myocardial infarction and death. Progress in cardiovascular diseases, 58(5), 473-482.

Vallerand, A. H. (2018). Davis's drug guide for nurses. FA Davis.

Zhu, H. J., Langaee, T. Y., Gong, Y., Wang, X., Pepine, C. J., Cooper-DeHoff, R. M., ... & Markowitz, J. S. (2016). CES1P1 variant 816A> C is not associated with hepatic carboxylesterase one expression and activity or antihypertensive effect of trandolapril. European journal of clinical pharmacology, 72(6), 681-687.