Diabetes Medication – Incretins


Agents that reduce glucose levels in a new and
different way in these agents are grouped under
the term Incretins In the Incretins are themselves divided into two
major groups the first group is called DPP-4 inhibitors and there are two of these available for example
at the current time in Canada these are called Januvia or sitagliptin or Onglyza or saxagliptin these agents as I mentioned before act in
different way than other oral agents they have two
actions they taken in pill form and they act on hormones
in the body to stimulate insulin production by the pancreas and as you know producing
insulin lowers blood sugar a second action however of these agents is to inhibit glucagon production, now in type 2
diabetes you have an increase of glucagon constantly
above normal levels and glucagon stimulates your own liver to
produce glucose so by inhibiting glucagon you lower glucose
therefore these pills act in two ways, they stimulate insulin production lowering glucose in
that way and inhibiting glucagon production and therefore lower glucose
and that manner. Januvia comes as 100 mg tablet and is taken
once a day it is also comes as a premix form with metformin
and this is called Janumet The Janumet pill comes in two forms you may
have been prescribed Janumet with a 50 mg Januvia and a 500 mg metformin and that pill is
taken once in the morning and once at night or
twice a day it also comes in a different form Janumet
50/1000 that is 50 mg of Januvia and 1000 mg of
metformin giving you a total dose of two a day of 2000 mg of
metformin and 100 mg of Januvia. The other agent Onglyza comes as a 5 mg tablet
and as a 2.5 mg tablet the latter is reserved for smaller dose is when you have patients who may
have some renal impairment or kidney damage and therefore you may want some smaller dose
in that instance so the Onglyza is taken as of 5 mg tablet once a
day you may take it with a pill called metformin as
well to reduce your blood sugar and to act more
synergistically that means it really ask better
together to lower blood sugar. I should have pointed out another advantage of
these pills they do not cause hypoglycemia however if you take that pill not just with
metformin but also with the sulfonylureas then
you can get hypoglycemia So these are the DPP-4 inhibitors and their pills
that are taken usually with metformin that serve to
lower blood sugar that don’t cause hypoglycemia when taken with
metformin and as well they don’t produce weight gain The other agent of the Incretins that we want to
talk about are the GLP-1 Agonists, these are medications that are taken by
injection they act in the same way but in a much stronger
fashion than the DPP-4 agents they stimulate
insulin production and they inhibit glucagon production therefore they lower the blood sugar. There are two forms or two products in the GLP-1 market one is
called Byetta Byetta which is not currently available in Canada
but is available in the United States is other
name is exenatide. Byetta comes as an injection that’s taken as of 5
µg injection twice a day for the first 2 to 3 weeks after 2 to 3 weeks the doses increase to 10 µg
twice a day and that’s because these agents do
produce some nausea and sometimes even vomiting when first started, therefore is better to
start at the smaller dose and then increase to the
full dose. Byetta or exenatide also comes in a long-acting
variety which is still under investigation this is called BYDUREON BYDUREON comes as a 2 milligram dose but
it’s only taken once a whole week, once in a week and this agent again lowers blood sugar very
impressively does not cause hypoglycemia unless combined with an agent such as a
sulfonylurea and produces very significant weight loss isn’t just weight neutral it actually produces
weight loss in a slow and steady fashion and
continuous fashion this is not a tremendous amount of weight loss
is not 10 or 20 pounds it’s usually in the range of 5 to 8 pounds over time
but it’s very effective So just to review, we have BYDUREON we have Byetta and we have Victoza. Victoza or liraglutide is available in Canada it is a GLP-1 agonist is taken by injection just as Byetta is and it’s taken as a 0.6 mg dose to start because of the incidence of nausea or
vomiting which we want to reduce and after 2 to 3 weeks you increase the dose to 1.2 mg again taken
once a day this agent is very effective and in some cases where you want to try to
increase the effectiveness even a little more you
can try to increase the dose to 1.8 mg per day is always given by a pen or a injection device that
looks like a fountain pen as we use in giving insulin and it’s very easy to administer with very minimal
pain so this agent does three things it doesn’t cause
hypoglycemia and lowers your blood sugar and it produces weight loss these agents are very effective and they will be
very useful additional agent to use in the fight
against high blood sugars so in summary the Incretins act by stimulating
insulin production reducing glucagon production and therefore lowering the blood sugar they work very effectively more effectively than either agent alone when used with metformin and they don’t cause hypoglycemia when used alone or with metformin they do cause hypoglycemia on occasion if you’re using them with the sulfonylureas.

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