Medications
— ACE (angiotensin- converting enzymes)
— Beta blockers (beta-adrenergic blocking agents)
— Calcium channel blockers
— Diuretics
— Sulfonylureas
— Meglitinides
— Biguanides
— Thiazolidinediones
— Alpha-glucosidase inhibitors
— Pramlintide (Symlin)
— Exenatide (Byetta)
Treatment Options
Certain medications are used to combat the complications resulting from hypertension.
ACE (angiotensin- converting enzymes) inhibitors are commonly prescribed.
They work by preventing a protein called angiotensin 1 from converting into angiotensin 2. When angiotensin 2 is reduced the blood vessels are able to relax and expand. This lowers blood pressure. ACE inhibitors also decrease the total blood volume in the body which means: less blood to pump = lower blood pressure. They also protect the kidneys, making them a wise choice for many people at risk or recovering form heart disease.
Examples:
benazepril - Lotensin by Novartis
captopril - Capoten by Bristol-Myers Squibb
enalapril - Vasotec by Merck
fosinopril - Monopril by Bristol-Myers Squibb
imidapril - Not approved for human use in the USA - approved in Japan
lisinopril - Prinivil by Merck or Zestril by Astra-Zeneca
moexipril - Univasc by Schwarz Pharma
quinapril - Accupril by Pfizer
perindopril erbumine - Aceon by Rhone-Polenc Rorer
ramipril - Altace by Hoechst Marion Roussel, King Pharmaceuticals
trandolapril - Mavik by Knoll Pharmaceutical (BASF)
ACE inhibitors work very well at first, but over time the angiotensin 2 levels in the body begin to rise again. ARB’s (angiotensin 2 receptor blockers) block angiotensin 2 receptors on cell walls. They are used in conjunction with ACE inhibitors because angiotensin 2 is also produced in other areas of the body. In some cases they can also be used without an ACE inhibitor and still produce beneficial results. They, just like ACE inhibitors, also protect the kidneys.
Examples:
candesartan cilexetil - Atacand by Astra Merck
eprosartan - Teveten
irbesartan - Avapro by Sanofi
losartan - Cozaar by Merck
olmesartan medoxomil - Benicar by Sankyo Pharma
telmisartan - Micardis
valsartan - Diovan by Novartis
[back to top] Beta blockers (beta-adrenergic blocking agents) block norepinephrine from binding to its receptors in the body. Norepinephrine is adrenaline and is responsible for increases in blood pressure resulting from stress or excitement. Your body has 2 primary beta receptors: beta 1 and beta 2. There are beta blockers that primarily block beta 1 receptors (selective) and there are beta blockers that block either beta receptor (nonselective). Beta 1 receptors are responsible for heart rate and heart beat strength. Beta 2 receptors are responsible for smooth muscle function in the body. Taking beta blockers will slow nerve impulses to the heart and slow its contractions. This lowers the heart rate which reduces blood pressure.
Beta blockers also impact blood sugar levels which could potentially affect insulin requirements for a person with diabetes. Taking them can also increase a person’s risk of developing diabetes. People with asthma should NOT take beta blockers because it may narrow the airways.
[back to top] Calcium channel blockers, also called calcium blockers, are medications that reduce the heart’s pumping strength and relax blood vessels. This is done by blocking calcium from entering certain muscle cells. By blocking the calcium there is a cascade of muscle contraction that is avoided and vasodilatation is the result. This vasodilatation then reduces blood pressure.
[back to top] Diuretics are medications that help reduce the amount of water in the body. They are used to treat the build-up of excess water in the body. They act on the kidneys to increase urine output. This loss of excess water helps to lower blood pressure. This loss of water may also lead to the loss of nutrients so a person should be monitored to prevent complications.
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Other Medications
Many people think that insulin is the only treatment for someone with diabetes. While it is the most popular, it is not the only treatment. People with type 1 diabetes need insulin because they don’t produce it. On the other hand, people with type 2 diabetes are more complex in their treatment because, in many cases, they still produce insulin but are less sensitive to it. In this case it would be necessary to help increase the body’s ability to utilize the insulin that is already there, not give it more insulin.
For someone who suffers from type 2 diabetes there are other medications, in pill form, to help control blood sugar levels. These other medications are split into five classes and they are as follows:
[back to top] Sulfonylureas
Sulfonylureas were introduced into the market in 1955. They target the beta cells of the pancreas and stimulate them to produce more insulin. This is only possible for someone who is type 2 because a person with type 1 diabetes has no functional beta cells. If the beta cells are producing insulin then it is possible to enhance that production through proper medication.
There are three generations of sulfonylureas and they each have different strengths, dosages, and side effects. The following is a chart of the different generations:
Generation Drug Duration Dose Range Daily Doses
1st Orinase (tolbutamide)
6-10 hours 500-3000 mg 2-3
1st Tolinase (tolazamide)
100-1000 mg 1-2
1st Diabinese (chlorpropamide)
24-72 hours 100-500 mg 1-2
2nd Glucotrol (glipizide)
12 hours 2.5-40 mg 1-2
2nd Glucotrol XL (ext. rel. glipizide)
24 hours 2.5-20 mg 1
2nd Micronase, Diabeta (glyburide)
18-24 hours 1.25-2 mg 1-2
2nd Glynase (micronized gly.)
24 hours 3-12 mg 1-2
3rd Amaryl (glimepiride)
24 hours 1-8 mg 1
Low blood sugar is possible when taking sulfonylureas but less likely than when taking insulin and less intense. They work best when taken at the same time every day and they are generally taken before meals.
Side effects include low blood sugar, nausea, bloating, heartburn, anemia, and weight gain. These are most common in the first few months of use so it is wise to monitor yourself closely. People with type 1 diabetes should avoid taking sulfonylureas as should people with kidney disease or liver disease.
[back to top] Meglitinides
Meglitinides are similar to sulfonylureas in that they stimulate the pancreas to release insulin. The difference is that they work in ways similar to first phase insulin release by a person without diabetes. They are rapid acting and act only when glucose levels are high. For this reason they are taken before meals and they are less likely to cause hypoglycemia.
There are only two meglitinides available and they are:
Drug Duration Dose Range Daily Doses
Prandin
(repaglinide) 3 hours .5-4 mg 2-3
Starlix
(nateglinide) 3 hours 60-120 mg 2-3
Prandin is derived from benzoic acid and was approved by the FDA in 1997 and Starlix is derived from D-phenylalinine and was approved in 2000. Just like sulfonylureas, meglitinides DO NOT work for people with type 1 diabetes because they require functional beta cells in order to be effective.
Meglitinides can be combined with certain types of insulin but there are numerous contraindications with other medications. There are also a number of side effects including low blood sugar, nausea, vomiting, diarrhea, cold and flu like symptoms, muscle aches, joint aches, headaches, back pain, and upper respiratory infections. They should also be avoided by people with liver disease and shouldn’t be combined with alcohol or blood thinners.
[back to top] Biguanides
Biguanides lower glucose production by the liver and enhance insulin sensitivity in muscle cells to increase glucose uptake. These characteristics make them very helpful for people with type 2 diabetes because increased glucose production by the liver is the most common cause of high blood sugar levels upon waking. When taken alone they also help lower blood sugar levels after eating with no chance of hypoglycemia. This decrease in blood sugar levels can also lead to a reduction in insulin injections.
Biguanides were originally introduced in 1957 in 2 different forms, phenformin and metformin. Phenformin was the first biguanide to hit the market but was soon removed due to several deaths. The deaths were a result of lactic acidosis and it wasn’t until 1979, in France, that metformin was found to be 20% less likely to cause these side effects. Lactic acidosis is the result of the body’s inability to empty metformin from the body. Finally, in 1994 the U.S. cleared metformin for use by people with type 2 diabetes.
Metformin is derived from the French lilac plant which, similarly to phenformin, was too toxic for human consumption. There are also side effects linked to metformin such as metallic taste, nausea, diarrhea, cramping, fullness, loss of appetite, bloating, headaches, vitamin b12 deficiency, and agitation.
Drug Duration Dose Range Daily Dose
Glucophage
(metformin) 8-12 hours 500-2550 mg 2-3
Glucophage XR
(metformin) 24 hours 500-2550 mg 1
Glucovance
(metformin + Glyburide) 12-18 hours 250/1.25 –
2000/20 mg 2-3
Contraindications for metformin use include diabetic ketoacidosis (DKA), alcoholism, kidney disease, liver disease, heart attack, and pregnancy.
[back to top] Thiazolidinediones
Thiazolidinediones, also known as glitazones, target the muscle cells and fat cells to increase their sensitivity to insulin. They also target the liver to prevent the overproduction of glucose. The combination of these effects effectively lowers blood sugar levels. Another benefit of these medications is their ability to lower triglyceride levels and increase levels of HDL’s in the blood. But these benefits can be negated by elevated LDL levels when taking rosiglitazone.
There are currently 2 different types of thiazolidinediones, pioglitazone and rosiglitazone. They are not recommended as the first line of defense against diabetes. Typically they are used after other medications have failed to lower blood sugar levels to safe ranges. Both types are associated with risks and side effects including sinusitis, upper respiratory infections, sore throat, swelling of the legs, fluid retention, headaches, anemia, weight gain, toothaches, muscle aches, and liver failure. In the case of liver failure, signs to look for include fatigue, nausea, vomiting, loss of appetite, fluid retention, and muscle aches. Regular tests should be done on the liver to keep the possibility of these side effects to a minimum. There are contraindications for the use of these products such as people at risk of heart failure, people with kidney or liver disease, edema, or pregnancy. They also increase fertility in women with polycystic ovary disease.
It is common to combine the use of thiazolidinediones with biguanides, sulfonylureas, and/or insulin. Typically the other medications are decreased prior to the use of the thiazolidinediones. The typical time it takes for the thiazolidinediones to be effective is 6-8 weeks.
Drug Dose Range Daily Doses
Actos
(pioglitazone) 15-45 mg 1
Avandia
(rosiglitazone) 2-8 mg 1-2
Avandamet
(rosiglitazone + metformin)
[back to top] Alpha-glucosidase inhibitors
Alpha-glucosidase inhibitors, also known as starch blockers, target enzymes in the intestines and slow the breakdown of carbohydrates. The alpha-glucosidase inhibitors must be taken with the first bite of a meal. The slowing of the breakdown of carbs in the intestines will slow the absorption of carbs into the blood and prevent sugar spikes after meals. Benefits are also seen in lower fasting blood glucose levels when taking alpha-glucosidase inhibitors.
There are side effects associated with the use of alpha-glucosidase inhibitors such as diarrhea, gas, bloating, nausea, and abdominal pain. These side effects tend to decrease over time. One way to decrease the severity of these side effects is to begin treatment with small doses and work your way up to the optimal dose.
Alpha-glucosidase inhibitors are commonly used in combination with other diabetes medications. One form, Glyset, is commonly used in combination with a sulfonylurea. The other form, Precose, may be used with a sulfonylurea, metformin, or insulin. When taken alone AGI’s don’t cause lows but when taken in combination other medications must be adjusted accordingly.
Drug Duration Dose Range Daily Doses
Precose
(acarbose) 4 hours 25-300 mg 3
Glyset
(miglitol) 4 hours 25-300 mg 3
Who can use diabetes pills?
Only people with type 2 diabetes can benefit from diabetes pills. They can be used by people who have had diabetes for less than 10 years or are currently taking less than 20 units of insulin. After a period of time it is less likely these medications will be effective. It is also common for them to cease being effective after long periods of use. This is usually combated by oral combination therapy. It is not safe for pregnant women to take diabetes pills. They are best treated by diet, exercise, and insulin.
[back to top] Pramlintide (Symlin)
Pramlintide was approved for use by people with diabetes on March 16, 2005. It may be used by a person with type 2 diabetes who is currently using insulin (they may also be using oral therapy) and not achieving optimal A1c levels. People with type 1 diabetes may also benefit from the use of pramlintide.
Symlin is a synthetic analog of amylin. Amylin is a naturally occurring hormone produced by the beta cells of the pancreas in humans. It works in combination with insulin and glucagon to help regulate blood sugar levels. Glucagon increases the release of glucose into the blood and amylin helps to suppress that.
Studies have shown that when Symlin is taken before meals it can help lower sugar spikes after meals, decrease fluctuations during the day, and level out A1c levels over time. These benefits are seen in people who are taking insulin and have actually allowed them to lower their insulin dose.
Weight loss is a common side effect seen with Symlin. Nausea is also common but it decreases over time.
It is not possible to mix Symlin and insulin in the same syringe due to their different chemistry. They must be injected separately.
[back to top] Exenatide (Byetta)
Exenatide is derived from the saliva of a lizard called a gila monster. It is known as a synthetic exendin-4 from a new class of medications known as incretin mimetics. Exendin-4 is a peptide made of 39 amino acids and it stimulates a receptor known as Glucagon Like Peptide-1 (GLP-1). It regulates insulin secretion, food intake, gastric emptying, and glucagon secretion.
Exenatide’s primary function is to increase insulin secretion. The benefit of this as opposed to other medications is that this only occurs during periods of elevated glucose levels. This decreases the risk of lows associated with other medications.
Similar to Symlin, exenatide must be injected, but not with insulin. Nausea is the most common side effect seen with exenatide supplementation but it diminishes over time.
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Treatment
Proper diet and exercise are the most common recommendations for lowering cholesterol, balancing blood sugar, and lowering blood pressure. A diet high in vegetables and “good” fats and low in sugar and “bad” fats is extremely beneficial to those with diabetes. Saturated (bad) fats are found in foods like margarine, most fast foods, red meats, and numerous dairy products and are recommended only in limited moderation. It is also recommended to avoid palm oil, coconut oil, and fried foods. The ADA recommends soft margarine with corn, safflower, soybean, or canola oil listed as the first ingredient.
Fish such as sardines, anchovies, tuna, and salmon are very high in essential fatty acids (omega 3, 6, and 9) which help lower cholesterol levels. Nuts are also high in essential fatty acids but tend to be salty and are calorie dense so they are recommended in small doses. There are also margarines that contain products called plant sterols and stanols. These natural sterols and stanols have a slew of scientific research that provide clinical proof of there ability to reduce cholesterol levels.
Fiber is also well known for its ability to lower cholesterol levels. Foods such as oatmeal, yams, brown rice, fruits, vegetables, and stabilized rice bran are high in either one or both types of fiber. This fiber also slows the digestion and release of glucose into the blood.
According to the ADA it is also wise to consume more products containing soy protein. Foods such as soybeans, tofu, miso, and soy milk are just a few examples of foods containing soy protein that can assist in lowering cholesterol levels.
Another less common but extremely beneficial way to lower cholesterol levels, balance blood sugar levels, and supplement the diet is the use of dietary supplements. Many of these supplements are beneficial to people with diabetes in a number of ways. There is an enormous body of clinical research done on these nutrients to prove their effectiveness and the natural health industry has experienced enormous growth because of this. Products like garlic, plant sterols, chromium, and specialty products like the Insul-Opt line have been proven effective for the diabetic community.
There are a few other complications that may impact some of the diabetic community:
— Celiac disease
— Hemochromatosis
— Frozen shoulder
These complications have ties to diabetes and further information is available.
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