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z Several guidelines make specific recommendations concerning the use of
DPP-4 inhibitors.
z Exenatide and liraglutide are injected incretin therapies.
◦ They are effective in reducing HbA as well as body weight.
1c
◦ They are generally well tolerated and the most common adverse events
are gastrointestinal disturbances.
◦ Exenatide should not be used in patients with severe renal impairment or
end-stage renal disease and liraglutide should only be used with caution
in renal impairment.
◦ Acute pancreatitis is a potential concern for all incretin-based therapies,
including DPP-4 inhibitors and GLP-1 mimetics/analogues.
z Linagliptin is a relatively new addition to the DPP-4 inhibitor market. It has the
following characteristics:
◦ A very high affinity for its substrate and a high level of potency compared
with the other compounds in its class.
◦ 10,000 times more selective for DPP-4 than it is for either DPP-8 or DPP-9.
◦ Rapidly absorbed and has a long terminal half-life of more than 100 hours.
◦ Administered as a single 5 mg tablet at any time of the day with or without
food.
◦ Primarily excreted non-renally; therefore it can be used without dose ad-
justments or warnings in patients with renal impairment.
◦ In clinical trials, linagliptin alone or in combinations with other OADs has
demonstrated its ability to improve HbA , FPG, PPG and β-cell function.
1c
◦ Linagliptin is weight neutral and has proved to be well tolerated.

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