First Generation Sulfonylureas -
These medications are occasionally still used today.
In case you
didn't already know, a person with diabetes can have alternative
treatments that will allow them to bypass the hassle of insulin
injections. One such treatment comes in various forms of the drug
Sulfonylureas. These drugs are considered "first generation"
because they have been used to treat men and women with diabetes
since the 1950s and require more milligrams of the medicine to
equal the effects of the so-called "second generation"
Sulfonylureas. While not used as often as the "second" generation
of sulfonylureas, you may still see them, and thus should be
familiar with their names.
Here are a few examples of first generation Sulfonylureas:
1. Acetohexamide: You may recognize this drug
by its brand name "Dymelor". It begins to work within 60 minutes
after ingested and can last up to 12 hours. Acetohexamide is taken
most often is one or two doses on a daily basis, with a maximum
dose of 1.5 grams. These pills come in strengths of 250 mg and 500
mg. You must use caution when taking this drug due to potential
kidney problems.
2. Tolbutamide: The brand name for this drug is
called "Orinase" and it is the only Sulfonylurea drug that is short
acting. Tolbutamide is broken down immediately by the liver and
because of this it begins to work quickly and is out of the system
within 10 hours. You can find this drug in strengths of 250 mg and
500 mg. Tolbutamide is also considered very safe for the elderly
because it enters the system and disappears very quickly. This
medicine is typically taken before each meal.
3. Chlorpropamide: This drug comes in the brand
names of "Glucamide" and "Diabinase". It is one of the longest
acting of the first generation Sulfonylureas drugs. Because
of this, it was the cause of a large amount of hypoglycemia cases
in the past. Chlorpropamide stayed in the system for more than a
day, over 24 hours in many instances. It comes and strengths of 100
mg and 250 mg. There is a high risk of kidney problems because once
Chlorpropamide is broken down by the body, it forms into other
chemicals which are still active and are eliminated very slowly
through the urine.
4. Tolamide: The brand name for this drug is
called "Tolinase" and comes in strengths of 100 mg, 250 mg, and 500
mg. This is also a long acting Sulfonylureas drug but does not stay
in the system quite as long as Chlorpropamide - about 20 hours or
so. Tolamide can take up to four hours or more before the effects
are noticed. And like most of these first-generation Sulfonylureas
drugs, it is excreted through the urine which can cause kidney
problems.
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