The angiotensin-converting enzyme is inhibited by the competitive agent cilazapril. It inhibits the renin-angiotensin-aldosterone pathway by preventing the conversion of angiotensin I to angiotensin II. Angiotensin II's suppression results in vasodilation since it possesses potent vasoconstrictive effects. As a result, it is recommended for the treatment of heart failure and hypertension.
Off-Label uses in Adults:
- ST-elevation & Non–ST-elevation
- Patients with a stable coronary artery disease.
Cilazapril dose in Adults
For heart failure:
- 0.5% once daily. To reach the maximum amount of 2.5 mg once per day, increase the dose gradually.
For Hypertension:
- 2.5 milligrammes used once daily. To reach the maximum dose of 10 mg per day, increase the dose gradually at intervals of two weeks.
For a diuretic:
- The typical daily dose is 2.5–5 mg.
Dose in Childrens
The manufacturer has not recommended any dose in the pediatric age group.
Pregnancy Risk Factor X
- [Canadian Boxed Warn]
- It is not advised to use it while pregnant because it could harm or kill the foetus.
- When pregnancy is confirmed, discontinue using it right away.
- Patients on ACE-I or ARBs treatment and planning to conceive should be switched to alternative therapies prior to conception.
- Drugs that disrupt the renin/angiotensin systems are linked to oligohydramnios because it is characterised by skeletal deformities and poor foetal renal function.
Use of Cilazapril while breastfeeding
- It is unknown if it is excreted into breastmilk. It is recommended that you avoid breastfeeding while it is active.
Dose adjustment in Renal Disease:
- For heart failure:
- Patients with CrCl of more than 40 mL/minute:
- 0.5 mg once a day to a maximum dose of 2.5 mg once a day.
- CrCl of 10 - 40 mL/minute:
- 0.25 - 0.5 mg once a day to a maximum dose of 2.5 mg once a day.
- CrCl of less than 10 mL/minute:
- Not recommended
- Patients with CrCl of more than 40 mL/minute:
- For hypertension:
- CrCl of more than 40 mL/minute:
- 1 mg once a day to a maximum dose of 5 mg once a day.
- CrCl 10 - 40 mL/minute:
- 0.5 mg once a day to a maximum dose of 2.5 mg once a day.
- CrCl of less than 10 mL/minute:
- Not recommended.
- CrCl of more than 40 mL/minute:
Dose adjustment in Liver disease:
- For Hypertension in patients with compensated cirrhosis:
- 0.5 mg or less once a day with caution.
Side Effects:
- Cardiovascular:
- Symptomatic hypotension
- Palpitations
- Orthostatic hypotension
- Central nervous system:
- Fatigue
- Headache
- Dizziness
- Gastrointestinal:
- Nausea
- Neuromuscular & skeletal:
- Weakness
- Renal:
- Increased serum creatinine
- Respiratory:
- Cough
Contraindication to Cilazapril include:
- cilazapril or another ACE inhibitor, or any ingredient in this formulation, could cause allergic reactions.
- Angioedema history to an ACE inhibitor
- Angioedema idiopathic or hereditary
- Ascites
- Anuria
- Concomitant use with the direct renin inhibitor - aliskiren
- Moderate-to-severe kidney impairment, with a GFR of 60mL/minute/1.73m2
- Pregnancy
- Breastfeeding
- Galactose intolerance
- Lapp lactase deficiency is also possible.
Warnings and Precautions
- Angioedema:
- It is possible to get angioedema in the neck and head that could compromise the airway.
- Patients at highest risk for ACE-I associated angioedema include patients with a prior history of angioedema, black-skinned patients of African descent, and the concomitant use of mTOR inhibitors like everolimus.
- Long-term monitoring may be necessary for patients with angioedema. Aggressive management is important.
- Cholestatic jaundice
- It is possible for cholestatic jaundice to progress to fulminant liver failure.
- If liver enzymes show marked elevations, ACE-Inhibitors must be stopped immediately.
- Cough:
- It is possible for patients to develop a dry, hacking and nonproductive cough after the drug has been used.
- This usually disappears once the drug is stopped, but it can sometimes take several months.
- Consideration should also be given to other causes of cough, such as pulmonary congestion brought on by heart failure.
- Hyperkalemia:
- Hyperkalemia is a risk for patients who are taking potassium-sparing diuretics, potassium supplement, or direct renin inhibitors.
- Patients with diabetes mellitus or underlying renal dysfunction are also at risk for hyperkalemia.
- Hypersensitivity reactions
- ACE-Inhibitors have been linked to severe allergic reactions, including anaphylaxis.
- Patients who receive hemodialysis with high flow dialysis membranes (example: AN69) and occasionally with dextran-sulfate-cellulose use during low density lipoprotein apheresis are often subject to allergic reactions.
- Hypotension and syncope:
- Hypotension is most common after the first dose. This is most common in patients with low volume.
- Neutropenia & agranulocytosis:
- Rarely, it can cause severe cytopenias, including neutropenia, angranulocytosis and aplasia.
- Renal function deterioration:
- Patients with heart disease and renal artery stenosis are at greater risk for deteriorating renal function.
- Oliguria, progressive and severe azotemia, as well as acute renal failure, may occur.
- Aortic stenosis
- Patients with severe aortic stenosis must use ACE inhibitors with caution due to the possibility of reduced coronary perfusion.
- Ascites:
- Ascites patients should be warned to avoid the drug.
- Collagen vascular disease:
- Hematologic toxicities can be caused by collagen vascular disease.
- Hypertrophic cardiomyopathy with outflow tract obstruction (HCM):
- The signs and symptoms of HOCM can get worse if afterload is reduced Avoid narrowing of the bilateral renal arteries.
- Take care if the renal artery is just narrowing one way.
- Renal impairment:
- Preexisting renal impairments should be avoided. Avoid rapid dose increases. Adjusting the dose may be necessary.
Cilazapril (United States: Not available): Drug Interaction
Note: Drug Interaction Categories:
- Risk Factor C: Monitor When Using Combination
- Risk Factor D: Consider Treatment Modification
- Risk Factor X: Avoid Concomitant Use
Risk Factor C (Monitor therapy). |
|
| Alfuzosin | May intensify blood pressure lowering medications' hypotensive effects. |
| Amphetamines | May lessen the effects of antihypertensive medications in treating hypertension. |
| Angiotensin II | The therapeutic efficacy of angiotensin II may be enhanced by angiotensin-converting enzyme inhibitors. |
| Antipsychotic Agents, Second Generation (Atypical) | Antipsychotic drugs can have a greater hypotensive effect when blood pressure-lowering medications are used (Second Gen [Atypical]). |
| Aprotinin | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| AzaTHIOprine | AzaTHIOprine's myelosuppressive effects may be enhanced by angiotensin-converting enzyme inhibitors. |
| Barbiturates | May intensify blood pressure lowering medications' hypotensive effects. |
| Benperidol | May intensify blood pressure lowering medications' hypotensive effects. |
| Brigatinib | May lessen the effects of antihypertensive medications in treating hypertension. The bradycardic effects of antihypertensive medications may be exacerbated by brutinib. |
| Brimonidine (Topical) | May intensify blood pressure lowering medications' hypotensive effects. |
| Dapoxetine | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Dexmethylphenidate | Antihypertensive agents may have a less therapeutic effect. |
| Diazoxide | May intensify blood pressure lowering medications' hypotensive effects. |
| Dipeptidyl Peptidase-IV Inhibitors | May worsen angiotensin-converting enzyme inhibitors' toxic or severe effects. The risk of angioedema in particular could rise. |
| Drospirenone | Drospirenone's hyperkalemic impact may be enhanced by angiotensin-converting enzyme inhibitors. |
| DULoxetine | By reducing blood pressure, DULoxetine may exacerbate hypotension. |
| Eplerenone | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Everolimus | May intensify angiotensin-converting enzyme inhibitors' harmful or hazardous effects. The risk of angioedema in particular could rise. |
| Ferric Gluconate | Angiotensin-Converting Enzyme Inhibitors might make ferric gluconate more harmful or poisonous. |
| Complex of Ferric Hydroxide Polymaltose | Ferric Hydroxide Polymaltose Complex may have a more negative or toxic effect when taken with angiotensin-converting enzyme inhibitors. Angioedema and allergic responses in particular may become more likely. |
| Gelatin (Succinylated). | Gelatin's harmful or toxic effects may be increased by angiotensin-converting enzyme inhibitors (Succinylated). Particularly, a higher risk of paradoxical hypotensive reactions to gelatin may exist (Succinylated). |
| Gold Sodium Thiomalate | Gold Sodium Thiomalate may have a more negative or toxic effect when used with angiotensin-converting enzyme inhibitors. Nitritoid responses have been linked to a higher risk, it has been highlighted. |
| Heparin | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Heparins (Low Molecular Weight) | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Herbs (Hypertensive Properties) | May lessen the effects of antihypertensive medications in treating hypertension. |
| Herbs (Hypotensive properties) | May intensify blood pressure lowering medications' hypotensive effects. |
| Hypotension-Associated Agents | The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications. |
| Icatibant | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Levodopa-Containing Products | Levodopa-Containing Products' hypotensive effects may be amplified by blood pressure-lowering medications. |
| Loop Diuretics | May strengthen angiotensin-converting enzyme inhibitors' hypotensive effects. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be increased by loop diuretics. |
| Lormetazepam | May intensify blood pressure lowering medications' hypotensive effects. |
| Methylphenidate | May lessen the effects of antihypertensive medications in treating hypertension. |
| Molsidomine | May intensify blood pressure lowering medications' hypotensive effects. |
| Naftopidil | May intensify blood pressure lowering medications' hypotensive effects. |
| Nicergoline | May intensify blood pressure lowering medications' hypotensive effects. |
| Nicorandil | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Nicorandil | May intensify blood pressure lowering medications' hypotensive effects. |
| Nitroprusside | Blood pressure lowering medications may intensify Nitroprusside's hypotensive effects. |
| Nonsteroidal Anti-Inflammatory Drugs | Nonsteroidal Anti-Inflammatory Agents' negative/toxic effects may be increased by angiotensin-converting enzyme inhibitors. The combination can cause renal function to significantly decline. Angiotensin-Converting Enzyme Inhibitors' antihypertensive effects may be lessened by nonsteroidal anti-inflammatory drugs. |
| Pentoxifylline | May intensify blood pressure lowering medications' hypotensive effects. |
| Pholcodine | Pholcodine's ability to reduce blood pressure may help to increase hypotensive effects. |
| Phosphodiesterase 5 Inhibitors | May intensify blood pressure lowering medications' hypotensive effects. |
| Potassium Salts | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Potassium-Sparing Diuretics | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Pregabalin | Angiotensin-Converting Enzyme Inhibitors may intensify Pregabalin's negative/toxic effects. Risk of gioedema could rise. |
| Prostacyclin Analogues | May intensify blood pressure lowering medications' hypotensive effects. |
| Quinagolide | May intensify blood pressure lowering medications' hypotensive effects. |
| Racecadotril | May intensify angiotensin-converting enzyme inhibitors' harmful or hazardous effects. Angioedema may be more likely as a result of this combination. |
| Ranolazine | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Salicylates | May intensify angiotensin-converting enzyme inhibitors' nephrotoxic effects. The therapeutic benefit of angiotensin-converting enzyme inhibitors may be reduced by salicylates. |
| Sirolimus | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Tacrolimus (Systemic) | Tacrolimus's effect of making you more hyperkalemic may be enhanced by angiotensin-converting enzyme inhibitors (Systemic). |
| Temsirolimus | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Thiazide and Thiazide -Like Diuretics | May increase the angiotensin-converting enzyme inhibitors' hypotensive effects. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be increased by thiazide and thiazide-like diuretics. |
| TiZANidine | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Tolvaptan | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Trimethoprim | May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension. |
| Yohimbine | May lessen the effects of antihypertensive medications in treating hypertension. |
Risk Factor D (Regard therapy modification) |
|
| Aliskiren | Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects. Angiotensin-Converting Enzyme Inhibitors' hypotensive effects may be strengthened by aliskiren. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be made worse by aliskiren. Treatment: It is not advised for diabetic patients to take aliskiren along with ACEIs or ARBs. Combination therapy should be avoided in other patients, especially when CrCl is less than 60 mL/min. If present together, carefully watch blood pressure, potassium, and creatinine levels. |
| Allopurinol | Angiotensin-Converting Enzyme Inhibitors might make Allopurinol more likely to cause allergic or hypersensitive reactions. |
| Amifostine | The hypotensive effects of amifostine may be strengthened by blood pressure reducing medications. Treatment: Stop taking blood pressure medications at least 24 hours before taking amifostine. If taking blood pressure medicine cannot be stopped, amifostine should be avoided. |
| Angiotensin II Receptor Blockers | May worsen angiotensin-converting enzyme inhibitors' toxic or severe effects. Angiotensin-Converting Enzyme Inhibitors' serum levels may rise in response to angiotensin II receptor blockers. Management: Ramipril and telmisartan are not advised for US labelling. It is unknown whether another ACE inhibitor and ARB combo would be less dangerous. If at all possible, think about combining different elements. |
| Grass Pollen Allergen Extract (5 Grass Extract) | Grass pollen allergen extract may have a more negative or toxic effect if angiotensin-converting enzyme inhibitors are used (5 Grass Extract). In particular, ACE inhibitors may raise the possibility of life-threatening allergic reactions to grass pollen allergen extract (5 Grass). |
| Iron Dextran Complex | Angiotensin-Converting Enzyme Inhibitors might make Iron Dextran Complex more harmful or poisonous. Patients who take ACE inhibitors may be more prone to responses of this nature. Management: Carefully follow the iron dextran instructions for setting up resuscitation equipment, educating staff before administering iron dextran, and using a test dosage before to the first therapeutic dose. |
| Lanthanum | May lower angiotensin-converting enzyme inhibitors' serum concentration. Angiotensin-converting enzyme inhibitors should be given at least two hours before or after lanthanum. |
| Lithium | The serum concentration of lithium may rise in response to angiotensin-converting enzyme inhibitors. It is likely that you will need to lower your lithium dosage after adding an ACE inhibitor. Observe how patients respond to lithium following the addition or discontinuation of concomitant ACE inhibitor medication. |
| Obinutuzumab | The effects of blood pressure lowering medications may become more hypotensive as a result. Treatment: Starting 12 hours before the obinutuzumab injection and continuing for 1 hour after the infusion, you may temporarily stop taking blood pressure-lowering medications. |
| Sodium Phosphates | The nephrotoxic impact of sodium phosphates may be enhanced by angiotensin-converting enzyme inhibitors. Particularly, there may be an elevated risk of acute phosphate nephropathy. Treatment: You can temporarily stop taking ACEIs or explore for alternatives to the oral sodium phosphate bowel preparation to prevent this combo. Keep yourself adequately hydrated, and keep a close eye on your renal function. |
| Urapidil | Angiotensin-Converting Enzyme Inhibitors may interact with them through an unidentified method. Avoid taking urapidil and ACE inhibitors simultaneously as a management strategy. |
Risk Factor X (Avoid Combination) |
|
| Bromperidol | The hypotensive effects of bromperidol may be strengthened by blood pressure-lowering medications. The hypotensive effects of blood pressure-lowering medications may be lessened by bromperidol. |
| Sacubitril | The negative or hazardous effects of sacubitril may be increased by angiotensin-converting enzyme inhibitors. Angioedema may be more likely as a result of this combination. |
Monitor:
- Blood pressure
- BUN
- Serum Creatinine
- Liver function tests
- CBC
- Plasma glucose in patients with diabetes.
How to take Cilazapril?
It may be administered as oral medicine with or without regard to meals.
Mechanism of action of Cilazapril:
- Cilazapril, when converted to its active metabolite cilazaprilat, inhibits angiotensin-converting enzyme (ACE).
- It prevents angiotensin I from angiotensin 2, which is a powerful vasoconstrictor.
The Onset of action of cilazapril is 1 - 2 hours and the peak antihypertensive effect is seen in 3 - 7 hours, reduction in the systemic vascular resistance and pulmonary capillary wedge pressure takes 2 - 4 hours. It isRapidly absorbedTheIts durationIt can last up to 24 hours. The bioavailability The active (terminal) medication has an oral absorption rate of about 57%, and its half-life is 36 to 49 hours. The majority of it is eliminated through urine as an unaltered medication.
International Brands of Cilazapril: (Not approved in the US)
- APO-Cilazapril
- CO Cilazapril
- Inhibace
- MYLAN-Cilazapril
- PHL-Cilazapril
- PMS-Cilazapril
- TEVA-Cilazapril
- Abapril
- Cilaril
- Cilazil
- Dynorm
- Inhibace
- Inocar
- Justor
- Kemicilaz
- Pipredo
- Prilatop
- Vascace
- Zapril
- Zapritens
Cilazapril Brands in Pakistan:
No brands available in Pakistan
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