ACE Inhibitors

By Stephen T. Sinatra, M.D., F.A.C.C., F.A.C.N., C.N.S., C.B.T.

Drugs in this class are lisinopril (Prinivil), enalapril (Vasotec), ramipril (Altace), benazepril (Lotensin), quinapril (Accupril), fosinopril (Monopril), and captopril (Capoten).

ACE is short for angiotensin-converting enzyme, a troublesome substance produced in the lungs that converts angiotensin I, a harmless molecule, into angio-tensin II, a potent blood vessel constrictor. ACE-inhibit-ing drugs, used for about thirty years in the treatment of high blood pressure, slow down ACE activity, result-ing in relaxation of blood vessel walls, lower blood pressure, and a reduced burden on the heart.


ACE inhibitors are effective in heart failure and after heart attacks, particularly for patients who also have high blood pressure. The medication can be used after a cardiac event to keep arteries relaxed and open so that more blood can reach the heart muscle.

A major heart attack can cause considerable damage to the heart muscle, making it harder to pump blood. The drugs help mobilize reconstruction activity, help prevent restenosis after stent implantation, and improve outcome after open-heart surgery. They decrease future adverse events in diabetics.

Not all ACE inhibitors are the same. The first generation of ACE inhibitors, including captopril, works only in the circulation. The drugs help blood pressure and heart failure, but do not blunt vascular inflammation.

I prefer drugs like ramipril and quinapril that work both in the circulation and in the endothelium (the lining of blood vessels) to block free radical oxidative activity and improve nitric oxide production. Nitric oxide keeps arteries dilated.

Overall, ACE inhibitors have a positive benefit-to-risk ratio and will cut your risk of cardiac events.

Possible Side Effects

The list includes headache, nausea, vomiting, abdominal pain, cough, low blood pressure, dizziness, chest tightness or pain, and tiredness. The most common side effect I’ve encountered is a dry, chronic cough. For some patients the cough is bad enough to make them stop taking the drug. As I wrote in January, this problem is underreported. That’s a disservice to patients. When I first started using ACE inhibitors many of my patients developed the cough. Most didn’t relate the cough to the drug, and neither did I in the beginning. I finally put two and two together after enough patients mentioned the cough, and if they did I stopped the drug. The cough would then usually disappear.

Patients who develop a cough from an ACE inhibitor need to ask their physician about angiotensin receptor blockers (ARBs). ACE inhibitors slow down the production of angiotensin II, while ARBs (as the name says) block the influence of angiotensin II by locking up cells’ receptors for it.

Low blood pressure is the second most frequent side effect I’ve seen from ACE inhibitors. That told me that the drug was working (reducing blood pressure). I wouldn’t worry unless a patient developed dizziness, light-headedness, or weakness, and perhaps faintness when arising from a chair. In that case, I would discontinue the medication or reduce the dosage.

Nutritional Deficiencies

ACE inhibitors deplete the body of zinc and may interact negatively with L-arginine, the amino acid that feeds the production of nitric oxide in endothelial cells. There is also potential for depleting sodium, vitamin B6, magnesium, phosphorus, potassium, and CoQ10.

Anyone taking an ACE inhibitor should supplement at least with a multivitamin and mineral formula. I also recommend extra zinc (men, 15–45 mg daily; women, 8–30 mg), magnesium (400–800 mg), potassium (99 mg three times daily or eat a banana, apple, or orange daily, if there is no kidney impairment), vitamin B6 (at least 6 mg), and CoQ10 (30–180 mg).

Natural ACE Inhibitors

Over the years I experimented with a variety of supplements as long-term alternatives to ACE inhibitors. Depending on the patient, the following supplements were helpful either singly or in combination:

  • Hawthorn berry (500 mg, 2–3 times per day) to increase blood flow in smaller vessels. It acts much like an ACE inhibitor, and also helps regulate heartbeat, promote circulation in the heart, and strengthen the heart’s pumping power.
  • Grapeseed extract (300 mg)
  • Raw garlic
  • Magnesium (400 mg)
  • Vitamin C (500–1,000 mg)
  • Nattokinase (50–100 mg)
  • Fish oil (2–4 g)
  • L-arginine (2–7 g)
  • The Awesome Foursome of CoQ10 (120–200 mg), magnesium (400 mg), carnitine (1–2 g on an empty stomach), and ribose (5 g 2–3 times daily) has been extremely effective alone for people with heart failure. With this natural ACE inhibitor combination I could often wean patients off the medication. Even in patients who didn’t respond to conventional treatment, I’ve been able to get significant improvement and better quality of life with the combination of a low-dose ACE inhibitor and the Awesome Foursome.

This article originally appeared in the April 2011 issue of Dr. Sinatra’s monthly written newsletter, Heart, Health & Nutrition. HMDI has reprinted this article with permission from Healthy Directions, LLC (© 2011 Healthy Directions, LLC).

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