moexipril

Action and Spectrum

Actions and Spectrum: 

moexipril is a medication belonging to the class of drugs called as angiotensin-converting enzyme (ACE) inhibitors. It primarily treats hypertension (high blood pressure) and congestive heart failure.  

Action: 

• ACE Inhibition: moexipril works by inhibiting the action of ACE, an enzyme involved in the production of angiotensin II. Angiotensin II is a potent vasoconstrictor, narrowing blood vessels and increasing blood pressure. By inhibiting ACE, moexipril reduces the formation of angiotensin II, leading to vasodilation (widening of blood vessels) and decreased blood pressure. 
• Bradykinin Potentiation: ACE inhibitors like moexipril also increase the levels of bradykinin. This substance causes the blood vessels to dilate and has a role in maintaining the balance of fluid and electrolytes. The potentiation of bradykinin contributes to the antihypertensive effects of moexipril. 

Spectrum: 

• Hypertension: moexipril is primarily used for the treatment of hypertension. Reducing blood pressure helps lower the risk of cardiovascular events like heart attacks, strokes, and kidney problems associated with high blood pressure. 
• Congestive Heart Failure: moexipril is also prescribed to manage congestive heart failure. It helps to improve symptoms, decrease hospitalizations, and increase survival rates in patients with this condition. 
• Diabetic Nephropathy: ACE inhibitors, including moexipril, have shown benefits in slowing the progression of kidney damage (nephropathy) in patients with diabetes. They can reduce proteinuria (excessive protein in urine) and delay the development of end-stage renal disease. 
• Left Ventricular Dysfunction: moexipril may be used to treat patients with left ventricular dysfunction, especially those with myocardial infarction (heart attack). It can help improve cardiac function and reduce the risk of subsequent cardiovascular events. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Pharyngitis 

Hypotension 

Polyuria 

Myalgia 

Sinusitis 

Cough 

Hyperkalemia 

Dizziness 

Nausea/vomiting 

Peripheral edema 

Headache 

Hyponatremia 

Rash 

Frequency not defined 

Syncope 

Chest pain 

Proteinuria 

Angioedema 

Arrhythmia 

Pneumonitis 

Black Box Warning

Black Box Warning: 

• ACE inhibitors like moexipril have been associated with potential harm to the developing fetus during pregnancy. These medications can cause injury or even death to the developing fetus, especially during the second and third trimesters. 
• oligohydramnios refers to a condition characterized by decreased amniotic fluid surrounding the fetus during pregnancy. While ACE inhibitors have been associated with this condition. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: moexipril is contraindicated in individuals with known hypersensitivity or allergy to moexipril or any other ACE inhibitor. Allergic reactions to ACE inhibitors can range from mild skin rash to severe reactions such as angioedema and anaphylaxis (a severe allergic reaction). 
• History of Angioedema: moexipril is contraindicated in patients with angioedema associated with previous ACE inhibitor use. Re-administration of ACE inhibitors in individuals with a history of angioedema can increase the risk of a recurrence, which may be life-threatening. 
• Pregnancy: moexipril should not be used during pregnancy. It can cause harm to developing fetus and may lead to fetal death or congenital malformations. If pregnancy is detected while taking moexipril, the medication should be discontinued promptly, and alternative antihypertensive therapy should be initiated. 
• Breastfeeding: moexipril is excreted into breast milk and can potentially harm nursing infants. Therefore, it is contraindicated during breastfeeding. If treatment with moexipril is necessary, breastfeeding should be discontinued. 
• Renal Artery Stenosis: moexipril is contraindicated in patients with bilateral renal artery stenosis (narrowing of both renal arteries) or stenosis of the artery to a solitary functioning kidney. ACE inhibitors, including moexipril, can reduce renal perfusion and cause acute renal failure in patients with significant renal artery stenosis. 
• Hyperkalemia: moexipril should not be used in patients with elevated potassium levels in the blood (hyperkalemia). ACE inhibitors can increase potassium levels, and in hyperkalemia, further elevation of potassium can lead to serious cardiac arrhythmias. 

Caution 

• Hypotension: moexipril can cause a drop in blood pressure, particularly during the initial use or when the dosage is increased. Patients should be cautious when rising from a sitting or lying position, as it may cause dizziness or lightheadedness. Close blood pressure monitoring is necessary, especially at the beginning of treatment or when adjusting the dosage. 
• Renal Impairment: moexipril is eliminated from the body primarily through the kidneys. Therefore, caution is advised in patients with renal impairment. Dose adjustments may be necessary based on the severity of renal dysfunction. 
• Hepatic Impairment: moexipril is primarily metabolized in the liver. Patients with impaired liver function should be monitored, as the clearance of moexipril may be reduced. Dosage adjustments may be required in these individuals. 
• Electrolyte Imbalances: moexipril can occasionally cause electrolytes such as sodium and potassium imbalances. Caution is advised in patients with pre-existing electrolyte disturbances or those taking other medications that may affect electrolyte levels. Regular monitoring of electrolytes is recommended, especially in patients with renal impairment. 
• Surgery/Anesthesia: If a patient is scheduled for surgery or undergoing anesthesia, it is crucial to inform the healthcare providers about using moexipril. The medication may cause excessive hypotension during anesthesia with agents that cause vasodilation. The decision to continue or discontinue moexipril should be made in consultation with the healthcare team. 
• Diabetes: ACE inhibitors like moexipril can affect blood glucose levels. Patients with diabetes should monitor blood sugar levels closely while taking moexipril, as the medication may alter glucose control. 
• Angioedema: While angioedema is listed as a contraindication, it’s essential to be cautious in patients with a history of angioedema or allergic reactions. Close monitoring for signs of angioedema, such as swelling of the face, lips, tongue/throat, is necessary. If angioedema occurs, moexipril should be discontinued immediately. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C (First trimester), D (second and third trimester) 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

moexipril is an angiotensin-converting enzyme (ACE) inhibitor with pharmacological properties contributing to its therapeutic effects. As a prodrug, moexipril is converted in the body to its active form, moexiprilat, which inhibits ACE, the enzyme responsible for converting angiotensin I to angiotensin II. By inhibiting ACE, moexipril reduces the production of angiotensin II, leading to vasodilation (widening of blood vessels), decreased peripheral resistance, and lowered blood pressure.

Additionally, moexipril increases bradykinin levels, which further promotes vasodilation and contributes to the antihypertensive effects of the drug. moexipril effectively treats hypertension, congestive heart failure, and other conditions associated with renin-angiotensin-aldosterone system (RAAS) activation through these mechanisms. 

Pharmacodynamics: 

Mechanism of action: The action of moexipril involves its role as an angiotensin-converting enzyme (ACE) inhibitor. moexipril is a prodrug converted to its active metabolite, moexiprilat, in the body. moexiprilat is a potent and competitive ACE inhibitor, an enzyme involved in the renin-angiotensin-aldosterone system (RAAS). 

The primary function of ACE is to convert angiotensin I, a precursor peptide, into angiotensin II, a potent vasoconstrictor. Angiotensin II causes blood vessels to narrow and promotes the release of aldosterone, leading to sodium and fluid retention. These effects collectively increase blood pressure. 

By inhibiting ACE, moexiprilat reduces the conversion of angiotensin I to angiotensin II. This results in several beneficial effects: 

• Vasodilation: Angiotensin II is a potent vasoconstrictor, so by inhibiting its production, moexiprilat promotes the relaxation and dilation of blood vessels. This widens the blood vessels, reducing peripheral resistance and ultimately leading to a decrease in blood pressure. 
• Decreased Aldosterone Secretion: Angiotensin II stimulates the release of aldosterone from the adrenal glands. Aldosterone promotes sodium and fluid retention, which can contribute to increased blood pressure. By reducing angiotensin II levels, moexiprilat decreases aldosterone secretion, decreasing sodium and fluid retention. 
• Increased Bradykinin Levels: In addition to inhibiting ACE, moexiprilat also increases the levels of bradykinin, a substance that causes blood vessels to dilate. Bradykinin also plays a role in maintaining fluid and electrolyte balance. The potentiation of bradykinin contributes to the antihypertensive effects of moexipril. 

Overall, by inhibiting ACE and reducing the levels of angiotensin II while increasing bradykinin levels, moexiprilat helps to lower BP, improve blood flow, and reduce the workload on the heart. These effects make moexipril effective in treating hypertension and congestive heart failure. 

Pharmacokinetics: 

Absorption 

moexipril is well absorbed when taken orally. After oral administration, it undergoes rapid and extensive absorption from the gastrointestinal tract. The presence of food in the stomach may slightly delay the absorption of moexipril but does not significantly affect its overall bioavailability. 

Distribution 

moexipril is extensively distributed throughout the body. It has a moderate volume of distribution, indicating that it distributes into the tissues. moexipril and its active metabolite, moexiprilat, have been found to cross the BBB (blood-brain barrier) and the placenta in animal studies. Both moexipril and moexiprilat have been detected in breast milk. 

Metabolism 

moexipril undergoes hepatic metabolism primarily via esterase enzymes to its active metabolite, moexiprilat. moexiprilat is a potent and long-acting ACE inhibitor responsible for the pharmacological effects of moexipril. moexiprilat undergoes minimal further metabolism and does not significantly inhibit or induce cytochrome P450 enzymes. 

Elimination and Excretion 

moexipril and its metabolites are primarily eliminated via the renal route. Approximately 60-70% of an oral moexipril dose is excreted in the urine, with the majority being moexiprilat. The elimination half-life of moexiprilat is around 3-5 hours, allowing for once or twice-daily dosing. moexiprilat is also eliminated via biliary excretion, with a small portion of the drug excreted in the feces. 

Adminstartion

Administration: 

Oral administration 

moexipril is available in tablet form and is typically taken orally.  

• Dosage: The dosage of moexipril will vary based on the people’s condition and response to therapy. Do not change the dosage or stop taking moexipril without consulting your doctor. 
• Timing: moexipril can be taken with or without food. However, it is generally recommended to take it on an empty stomach, nearly 1 hour before or 2 hours after a meal, for optimal absorption. Following the prescribed dosing schedule is crucial to ensure consistent blood levels of the medication. 
• Swallowing: moexipril tablets should be swallowed whole with a glass of water.  
• Compliance: It is crucial to take moexipril regularly and simultaneously (s) each day to maintain a consistent level of the medication in the body.  
• If a dose is missed, taking it as soon as possible is generally recommended. However, if the next scheduled dose is missed, it should be skipped and the following dose should be taken at the appropriate time. It is important to avoid taking a double dose of the medication to compensate for the missed dose.
• Duration of Use: moexipril is usually a long-term medication for managing hypertension or heart failure. Follow your doctor’s instructions regarding the duration of use and continue taking the medication even if you feel well, as stopping suddenly can cause a rebound increase in blood pressure. 
• Interaction with Other Medications: moexipril may interact with certain medications, including diuretics (water pills), potassium supplements, nonsteroidal anti-inflammatory drugs (NSAIDs), and others. Inform your healthcare provider about all your medications, including prescription drugs, over-the-counter(OTC) drugs, and herbal supplements, to avoid any potential interactions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: moexipril 

Pronounced: [ moe-EX-i-pril ] 

Why do we use moexipril? 

moexipril primarily treats hypertension (high blood pressure) and congestive heart failure.  

• Hypertension: moexipril is prescribed to lower blood pressure in patients with hypertension. By inhibiting the angiotensin-converting enzyme (ACE), moexipril reduces the production of angiotensin II, which causes blood vessels to constrict. The relaxation and dilation of blood vessels leads to decreased blood pressure. Controlling hypertension with moexipril helps reduce the risk of cardiovascular events like strokes, heart attacks, and kidney problems associated with high blood pressure. 
• Congestive Heart Failure: moexipril is part of the treatment regimen for congestive heart failure. It helps improve symptoms, reduce hospitalizations, and increase survival rates in patients with this condition. By reducing the workload on the heart and dilating blood vessels, moexipril improves cardiac function and decreases the fluid buildup in congestive heart failure. 
• Diabetic Nephropathy: Diabetic nephropathy is a condition characterized by kidney damage that occurs as a complication of diabetes. moexipril has shown benefits in slowing the progression of kidney damage in patients with diabetes. It can reduce proteinuria (excessive protein in urine) and delay the development of end-stage renal disease. moexipril and other measures such as blood glucose control are used to manage diabetic nephropathy and protect kidney function. 
• Left Ventricular Dysfunction: moexipril may be prescribed for patients with left ventricular dysfunction, especially those with myocardial infarction (heart attack). It helps improve cardiac function and reduce the risk of subsequent cardiovascular events. moexipril is part of a comprehensive treatment approach for patients with left ventricular dysfunction to improve heart function and overall prognosis.