Alogliptin (alogliptin benzoate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Alogliptin benzoate, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is an antidiabetic agent.
Alogliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme that inactivates the incretin hormones: glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Alogliptin selectively inhibits DPP-4 with no effect on DPP-8 or DPP-9 in vitro at concentrations approximating those from therapeutic exposures. Alogliptin increases circulating concentrations of GLP-1 and GIP in a glucose-dependent manner.
GLP-1 and GIP stimulate insulin secretion from pancreatic beta-cells in a glucose-dependent manner (i.e., when glucose concentrations are elevated). GLP-1 also decreases glucagon secretion from pancreatic alpha-cells, leading to reduced hepatic glucose production.
Alogliptin did not increase the QT interval corrected for rate (QTc) at daily dosages of 50 or 400 mg daily for 7 days in a randomized, placebo-controlled, active-comparator (moxifloxacin) study; the 400-mg dose produced plasma concentrations 19-fold higher than the maximum recommended clinical dose of 25 mg.
Following oral administration of a single dose of alogliptin (up to 800 mg) in healthy individuals, median time to peak plasma concentration was 1-2 hours; the drug has an absolute oral bioavailability of approximately 100%. Peak inhibition of DPP-4 occurs within 1--2 hours of administration with single and repeated dosing in patients with type 2 diabetes mellitus. Administration of alogliptin with food did not substantially alter total and peak exposure to the drug.
Alogliptin does not undergo extensive metabolism; 60-80% of the dose is excreted unchanged. Following administration of a radiolabeled dose of alogliptin, approximately 89% of administered radioactivity was excreted in urine (76%) and feces (13%). Terminal elimination half-life of alogliptin is approximately 21 hours following a single dose of 25 mg.
Age (range: 18--80 years), gender, and race do not have any clinically meaningful effect on the pharmacokinetics of alogliptin. Total and peak exposure to alogliptin are approximately 10% and 8% lower, respectively, in patients with moderate hepatic impairment (Child-Pugh class B); the effects of severe hepatic impairment (Child-Pugh class C) have not been studied. Exposure (as determined by plasma AUC) is increased 1.2-fold in patients with mild renal impairment (creatinine clearance >=60 to 90 mL/minute), 2-fold in patients with moderate renal impairment (creatinine clearance >=30 to <60 mL/minute), 3-fold in patients with severe renal impairment (creatinine clearance >=15 to <30 mL/minute), and 4-fold in patients with end-stage renal disease (creatinine clearance <15 mL/minute or requiring dialysis).
USES: Alogliptin is used with a proper diet and exercise program to control high blood sugar in people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems. Proper control of diabetes may also lessen your risk of a heart attack or stroke.
Alogliptin works by increasing levels of natural substances called incretins. Incretins help to control blood sugar by increasing insulin release, especially after a meal. They also decrease the amount of sugar your liver makes.
Generic name: alogliptin benzoate
Pronunciation: (AL-oh-GLIP-tin)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Alogliptin
Indications
The following indications are listed for Alogliptin:
- Type 2 Diabetes Mellitus
Also known as: Adult Onset Diabetes, Adult Onset Diabetes Mellitus, Adult Onset Dm, Diabetes Mellitus Type 2, Diabetes Mellitus Type Ii, Ketosis-Resistant Diabetes Mellitus, Ketosis-Resistant Dm, Maturity Onset Diabetes, Maturity Onset Diabetes Mellitus, Non-Insulin Dependent Diabetes Mellitus, Non-Insulin-Dependent Diabetes Mellitus, Type Ii Diabetes Mellitus.
Dosing
Dosage of alogliptin benzoate is expressed in terms of alogliptin.
When administered as a single-entity preparation, alogliptin may be administered orally once daily without regard to meals. Alogliptin tablets should be swallowed whole and should not be split.
When alogliptin is administered in fixed combination with metformin hydrochloride, the combination should be administered twice daily with food; dosage should be titrated gradually to minimize adverse GI effects of the metformin component. Fixed-combination tablets should be swallowed whole and should not be split before swallowing.
When alogliptin is administered in fixed combination with pioglitazone, the combination should be administered once daily without regard to meals. Fixed-combination tablets should be swallowed whole and should not be split before swallowing.
If a dose of alogliptin alone or in combination with metformin or pioglitazone is missed, the missed dose should be taken as soon as it is remembered followed by resumption of the regular schedule. If the missed dose is not remembered until the time of the next dose, the missed dose should be skipped and the regular schedule resumed; the dose should not be doubled to replace a missed dose.
Alogliptin and its metformin- or pioglitazone-containing combination products should be stored at 25degreesC (excursions permitted to 15-30degreesC). Keep alogliptin/metformin hydrochloride fixed-combination tablets in a tightly closed container. Keep alogliptin/pioglitazone fixed-combination tablets in a tightly closed container and protect from moisture and humidity.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Alogliptin is principally renally excreted; cytochrome P-450 (CYP)-related metabolism is negligible.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known serious hypersensitivity (e.g., anaphylaxis, angioedema, severe cutaneous adverse reactions) to alogliptin.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Most common adverse reactions (incidence >=4%) in patients receiving alogliptin monotherapy include nasopharyngitis, headache, and upper respiratory tract infection.
Most common adverse reactions (incidence >=4%) in patients receiving alogliptin in combination with metformin include upper respiratory tract infection, nasopharyngitis, diarrhea, hypertension, headache, back pain, and urinary tract infection.
Most common adverse reactions (incidence >=4%) in patients receiving alogliptin in combination with pioglitazone include nasopharyngitis, back pain, and upper respiratory tract infection.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of alogliptin alone, in fixed combination with metformin, or in fixed combination with pioglitazone have not been established in pediatric patients. Effectiveness of alogliptin monotherapy was not demonstrated in a 52-week, randomized, double-blind, placebo-controlled trial in 151 pediatric patients 10--17 years of age with inadequately controlled type 2 diabetes mellitus.
There is insufficient evidence with alogliptin in pregnant women to determine a drug-associated risk of major birth defects or miscarriage. No adverse developmental effects were observed when alogliptin was administered to pregnant rats and rabbits during organogenesis at exposures 180- and 149-times the 25 mg clinical dose, respectively, based on plasma drug exposure.
There is no information regarding the presence of alogliptin in human milk, the effects on the breast-fed infant, or the effects on milk production. Alogliptin is distributed into milk in lactating rats. The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for alogliptin and any potential adverse effects on the breast-fed infant from alogliptin or from the underlying maternal condition.
No dosage adjustment is necessary based on age.
Of 9052 patients in clinical trials of alogliptin, 24.9% were 65 years of age and older; 4.3% were 75 years of age and older. No substantial differences in safety and efficacy relative to younger adults were observed.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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