Zofenopril Calcium Drug Introduction, Mechanism of Action, Uses, and Side Effects

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Zofenopril Calcium Drug Introduction, Mechanism of Action, Uses, and Side Effects

Zofenopril Calcium is an angiotensin-converting enzyme inhibitor and antioxidant. ACE is the target. Zofenopril Calcium is a prodrug designed to be metabolically hydrolyzed to produce the active free sulfhydryl molecule zofenoprilat, an angiotensin-converting enzyme (ACE) inhibitor.

In rat models, Zofenopril Calcium enhances the healing of peripheral nerve damage. Zofenopril Calcium enhances active calcium uptake into the Sarcoplasmic Reticulum and accelerates SR calcium cycling.

It is the most potent drug and is eliminated by the liver naturally.

Structure and Properties of Zofinopril Calcium

structure and properties of zofinopril calcium

Source: PubChem

Zofenopril Calcium is the calcium salt of Zofenopril, a sulfhydryl angiotensin-converting enzyme (ACE) inhibitor having antihypertensive action.

Zofenopril calcium is an organic calcium salt that is the zofenopril hemicalcium salt. A precursor to zofenoprilat.Its IUPAC name is calcium;(2S,4S)-1-[(2S)-3-benzoylsulfanyl-2-methylpropanoyl]-4-phenylsulfanylpyrrolidine-2-carboxylate.

Its molecular formula is C22H22Ca0.5NO4S2, with a molecular weight of 448.58 g. It is soluble in DMSO when warmed with 50 º C water baths and is insoluble both in water and Ethanol.

What is ACE Inhibitor?

Angiotensin-converting enzyme (ACE) inhibitors are exclusively used to treat excessive blood pressure and congestive heart failure. They are also used to prevent renal disease in some people.

 These medications widen blood arteries and reduce blood pressure by blocking the effects of angiotensin-converting enzyme (ACE), an enzyme that helps control blood pressure.

How Does Zofenopril Calcium Work as ACE Inhibitor?

In the lungs, Zofinopril Calcium works as ACE Inhibitor. Angiotensin-converting enzymes (ACE) catalyzes the conversion of angiotensin I to angiotensin II. Angiotensin II is an active vasoconstrictor that causes blood vessels to contract and raises systemic blood pressure.

 Furthermore, angiotensin II raises blood osmolality and volume by causing water and salt retention in the kidneys.

ACE inhibitors lower angiotensin II levels by blocking the enzyme, causing blood arteries to expand (vasodilation) and, as a result, lower systemic blood pressure.

How Is Zofenopril Calcium Detected and Extracted?

For detecting Zofenopril and zofenoprilat in human plasma, a simple, highly sensitive specific LC-MS-MS approach was devised. The free sulfhydryl groups of zofenoprilat and its internal standard were preserved.

It is done with N-ethylmaleimide (NEM) treatment, which forms succinimide derivatives to avoid oxidative degradation. Toluene was utilized to extract the chemicals and their fluorine derivatives, which were employed as internal standards.

The dried extracts were reconstituted and then chromatographed before being monitored by a triple-stage quadrupole apparatus in negative ion spray ionization mode.

The approach was used to assess zofenopril and zofenoprilat plasma concentrations in 18 healthy volunteers given 60 mg of zofenopril calcium salt orally.

What Are the Uses of Zofenopril Calcium?

ACE inhibitors are used to treat a variety of comorbidities, including heart failure, heart attack, coronary artery disease, diabetes, chronic renal disease, migraine, and scleroderma.

Zofenoprilate has been shown to suppress ACE while preserving endothelial function. It inhibited doxorubicin’s pro-apoptotic effects, stimulated mitosis in bovine coronary venular endothelial cells (CVEC), and increased cell survival concentration-dependently.

In addition, zofenoprilat stimulated angiogenesis in porcine coronary arteries. Zofenoprilat seems to promote the proliferation of coronary endothelial cells, which results in angiogenesis through reversing apoptosis.

It functions as an anticonvulsant, apoptosis inhibitor, cardioprotective agent, EC (peptidyl-dipeptidase A) inhibitor, prodrug, and a vasodilator.

Is Zofenopril Calcium Helpful in Hypertension and Myocardial Infection?

Zofenopril is used to treat essential hypertension that is mild to moderate. Zofenopril is approved for treating acute myocardial infarctions with or without signs or symptoms of heart failure in hemodynamically stable individuals who are not undergoing thrombolytic therapy.

Angiotensin-converting enzyme inhibitors (ACEIs), which were first licenced to treat hypertension, are now frequently used to enhance the clinical prognosis of patients with acute myocardial infarction (AMI) and congestive heart failure.

In a research study, Zofenopril (10 mg/kg PO) was given to mice for 1, 8, and 24 hours to determine the optimum dose. H2S and NO levels in the heart and plasma were determined, as well as H2S and NO enzyme levels (cystathionine synthase, cystathionine lyase, 3mercaptopyruvate sulphur transferase, and endothelial nitric oxide synthase).

Mice were pretreated for 8 hours with Zofenopril or vehicle, followed by 45 minutes of ischemia and 24 hours of reperfusion. Pigs were given either a placebo or Zofenopril (30 mg/day orally) seven days before 75 minutes of ischemia and  48 hours of the period of reperfusion.

Zofenopril Calcium substantially increased plasma and cardiac H2S and NO levels in mice and plasma H2S (sulfane sulphur) levels in pigs.

How Is Zofenopril Calcium Helpful in Renal Failure?

Hypertension and renal illness frequently coexist, increasing the likelihood of future cardiovascular events. In the presence of concurrent renal illness, treating hypertensive individuals with an angiotensin-converting enzyme inhibitor may decrease disease development.

 Zofenopril Calcium, a third-generation lipophilic angiotensin-converting enzyme inhibitor, effectively lowers blood pressure in hypertensive patients and lowers the risk of fatal and non-fatal events in post-acute myocardial infarction and heart failure when administered alone or in combination with a thiazide diuretic.

In over 300 hypertensive patients with renal impairment, Zofenopril was found to have a comparable blood pressure-lowering impact regardless of illness stage, with higher effects when combined with a thiazide diuretic, particularly in those with mildly or moderately impaired kidney function.

Zofenopril inhibited renal angiotensin-converting enzyme inhibitors in animal models and avoided kidney morphological and functional abnormalities after ischemia-reperfusion damage.

Treatment of hypertensive patients for 18 weeks with a combination of Zofenopril 30 mg and hydrochlorothiazide 12.5 mg resulted in a reduction in albumin creatinine ratio of 8.4 mg/g (49.6 percent reduction from baseline values).

On the other side, no changes were observed in the glomerular filtration rate, variations similar to those obtained in the control group treated with a combination of irbesartan 150 mg and hydrochlorothiazide 12.5 mg.

As a result, preliminary evidence suggests that relatively long-term treatment with the angiotensin-converting enzyme inhibitor zofenopril Calcium alone or in combination with hydrochlorothiazide is effective in controlling blood pressure and may confer some kidney protection due to ACE inhibition properties.

How Does Zofenopril Calcium Have an Impact on Fertility, Pregnancy and Lactation?

The epidemiological data on the risk of teratogenicity following ACE inhibitor exposure during the first trimester of pregnancy is inconclusive; nonetheless, a slight increase in risk cannot be ruled out.

Unless the continuing use of an ACE inhibitor is deemed necessary, patients contemplating pregnancy should be switched to an alternate antihypertensive therapy with a proven safety profile in pregnancy.

ACE inhibitors should be discontinued promptly when pregnancy is detected, and, if necessary, alternative medication should be initiated.

Human fetotoxicity (decreased renal function, oligohydramnios, skull ossification retardation) and newborn toxicity (renal failure, hypotension, hyperkalemia) have been linked to ACE inhibitor treatment during the second and third trimesters.

If an ACE inhibitor has been used from the second trimester of pregnancy, an ultrasound of the renal function and skull is required. Infants born to moms who have taken ACE inhibitors should be regularly monitored for signs of hypotension.

Because no information on the use of Zofenopril during breastfeeding is available, Zofenopril is not suggested, and other medicines with better-proven safety profiles are preferred, especially when nursing a newborn or premature infant.

Can Zofenopril Calcium Cause Hypotension?

Like other ACE inhibitors, Zofenopril Calcium can induce a significant drop in blood pressure, especially after the first dosage. Symptomatic hypotension is uncommon in simple hypertension individuals.

It is more likely to develop in individuals who have had their electrolytes and volume reduced by diuretic medication, dietary salt restriction, dialysis, diarrhea, or vomiting, or who have severe renin-dependent hypertension.

Symptomatic hypotension has been documented in individuals with heart failure, with or without accompanying renal insufficiency. This can be more likely to happen in individuals with severe heart failure, as evidenced by the use of large dosages of loop diuretics, hyponatremia, or functional renal impairment.

 Treatment should begin under strict medical supervision, ideally in the hospital, with modest dosages and cautious dose titration in individuals at high risk of symptomatic hypotension.

Zofenopril may cause a further decrease of systemic blood pressure in certain people with heart failure who have normal or low blood pressure. This impact is expected and is not typically grounds for discontinuing therapy. If hypotension develops symptomatic, the dose of Zofenopril may need to be reduced or discontinued.

If hypotension occurs, the patient should be positioned supine. Volume replacement with normal intravenous saline may be necessary. The emergence of hypotension following the initial dosage does not impede further cautious dose titration with medication following good treatment.

What Are the Side Effects of Using Zofenopril Calcium?

The following list the most common potential negative hazards associated with Hydrochlorothiazide / Zofenopril calcium-containing medications. This is not an exhaustive list.

These adverse effects are conceivable; however, they are not usually experienced. Some of the negative effects maybe not yet severe.

 Consult your doctor if you have any of the following adverse symptoms, especially if they persist. Photosensitivity, dry mouth, electrolyte imbalance, gastrointestinal issues, and vomiting are possible symptoms.

It can induce uric acid excess in the blood, weakness, gout, abnormal cardiac rhythm, lipid changes, drowsiness, and muscle soreness.

Other possible adverse effects include hypotension, increased thirst, and an excess of glucose in the system. Allergic reactions, rash, lethargy, headache, cough, and nausea, are possible side effects.

What Are Precautions While Taking Zofenopril Calcium?

Inform your doctor about your current prescriptions, over-the-counter items (e.g. vitamins, herbal supplements, etc.), allergies, pre-existing disorders, and current health problems before using Zofenopril Calcium (e.g. pregnancy, upcoming surgery, etc.).

Some medical issues may be more sensitive to the drug’s negative effects. Take as advised by your doctor or as instructed on the package insert.

Your medical condition determines the dosage. Inform your doctor if your illness gets worsens or persists. The following are some key counseling points.

Avoid taking Zofenopril Calcium at sleep since it causes frequent urination. Consult your medical consultant if you have dry mouth, thirst, weakness, lethargy, drowsiness, restlessness, disorientation, muscular aches or cramps.

The pills should not be chewed, divided, or crushed. Drink plenty of fluids to avoid being dehydrated or overheated. Using water, swallow the entire pill.

Frequently Asked Questions (FAQs):

What Is the Purpose of Zofenopril?

Zofenopril is an ACE inhibitor having antihypertensive, antioxidant, and cardioprotective characteristics and the capacity to increase endothelial function and protect against ischemia.

How Is Zofenopril Calcium Helpful in The Case of Heart Failure?

ACE inhibitors expand blood arteries, increasing blood flow. This reduces the amount of effort that the heart needs to undertake. They also aid in blocking angiotensin, a chemical in the blood produced as a result of heart failure.

Is Zofenopril Helpful in Kidney Protection?

Treatment with Zofenopril Calcium ACE inhibitors protects the kidneys by decreasing systemic blood pressure intraglomerular pressure, having an antiproliferative impact, lowering proteinuria, and having a lipid-lowering effect in proteinuric individuals (secondary due to reduction of protein excretion).

Is It Alright to Drive or Operate Heavy Machinery After Taking Zofinopril Calcium?

If you feel sleepiness, dizziness, hypotension, or a headache as a side effect of Zofenopril Calcium, you should not use heavy machinery. If the medication causes sleepy, dizziness, or drops in your blood pressure, you should not drive.

Please take care of these side effects when using Zofenopril Calcium. Always see your doctor for suggestions tailored to your body and health problems.

When Should You Not Use Zofenopril Calcium?

A contraindication is a hypersensitivity to zofenopril calcium. Furthermore, you should not take Zofenopril Calcium if you have any of the following conditions: allergic reactions, asthma, breastfeeding, diabetes, heart disease, high cholesterol level, kidney disease, liver disease, or you are pregnant.

Do Zofenopril Calcium Tablets Cause Respiratory Issues?

Dyspnea, sinusitis, rhinitis, glossitis, bronchitis, and bronchospasm have been recorded seldom. ACE drugs have been linked to the start of angioneurotic oedema involving the facial and oropharyngeal tissues in a limited fraction of individuals.

In rare situations, angioneurotic oedema of the upper airways has resulted in lethal airway blockage.

Conclusion

Zofenopril Calcium is a medication of the ACE inhibitor family having lipophilic characteristics. It is an effective medication having pharmacological effects. It is essential in hypertension and myocardial infection.

It is also beneficial in cases of renal failure. However, it is not without its drawbacks. If you have any medical issues, you should exercise extreme caution when using this medication.

It causes dizziness and should be avoided if driving, pregnant, or lactating. Before using it, you should visit your doctor.

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