DPP-IV inhibitors are a group of medications that includes Vildagliptin (Galvus) (dipeptidyl peptidase IV inhibitors). The same class of medications also includes the drugs Sitagliptin, Linagliptin, and Saxagliptin.
It is a diabetes medication that is thought to be more effective than sitagliptin at lowering blood sugar levels.
It works by preventing the DPP-IV enzyme from cleaving endogenous GLP-1 (glucagon-like peptide 1).
Thus, it predominantly affects endogenous GLP-1 levels by boosting them through an indirect route.
It lowers blood sugar through a glucose-dependent mechanism, postpones stomach emptying, and curbs appetite.
It is thought to reduce glycated hemoglobin more effectively than Sitagliptin (Januvia).
Vildagliptin (Galvus) Uses:
- It is recommended for use as monotherapy in a subset of individuals with type 2 diabetes mellitus, particularly those who are intolerant to metformin.
- It is marketed under the trade name Galvus-met and is additionally used in conjunction with metformin. Sulfonylureas, insulin, and SGLT2 inhibitors like dapagliflozin and empagliflozin can all be used with it.
- Vildagliptin shouldn't be combined with GLP-1 analogs including Semaglutide, Liraglutide, Exenatide, and albiglutide as well as another DPP-IV inhibitor.
Vildagliptin (Galvus) Dose:
50 mg of it is given twice daily, just after meals.
Any of the following groups of medications can be combined with it:
- Biguanides (metformin)
- Sulfonylureas (Glyburide, Glimepiride, and Gliclazide)
- SGLT2 blockers (Empagliflozin, Dapagliflozin, and Ertugliflozin)
- Magletinides (Repaglinid and nateglinide)
- Anti-glucosidase agents (Acarbose)
Additionally, it should not be combined with a GLP-1 analog or another medication in the same class.
Dosage of vildagliptin (Galvus) in kids:
It is not advised for use in kids.
Risk Category for Pregnancy: C
Pregnant women have not been investigated with vildagliptin. Other recommended treatments like insulin and metformin ought to be utilized instead.
It is best to prevent maternal hyperglycemia to reduce the risk of problems brought on by uncontrolled gestational diabetes.
Use during breastfeeding
Mothers who are nursing their babies have not been researched. It is advisable to consider the treatment's hazards as well as advantages before beginning it.
Vildagliptin (Galvus) Dose in Kidney disease:
Patients with mild renal impairment may benefit from using it. The dose should be cut in half in patients with mild renal impairment (creatinine clearance of 30 ml/min to 60 ml/min).
It is advised to avoid taking it in cases of severe renal impairment and in those with CrCl values below 30 ml/minute.
In people with kidney disease, linagliptin (Tradjenta) is the chosen DPP-IV inhibitor.
Vildagliptin (Galvus) Dose in Liver disease:
Patients who suffer from hepatic impairment can utilize it.
Patients with mild, moderate, or severe hepatic illness do not experience any changes in the drug's pharmacokinetics.
However, other drug-related side effects, particularly gastrointestinal ones, might prevent its usage in these patients.
Additionally, people whose preexisting impaired liver functions are triple the upper limits of normal should delay starting medication.
Side effects of Vildagliptin (Galvus):
Gastrointestinal Side effects:
- early satiety and postmeal fullness
Respiratory side effects:
Hepatobiliary side effects:
- Abdominal pain
Other side effects:
- skeletal pains
- increased creatinine
Contraindication to Vildagliptin (Galvus):
- Responses to vildagliptin or any other ingredient in this formulation that cause hypersensitivity (eg anaphylaxis and edema).
Precautions and warnings
- The usage of DPP-4 inhibitors can result in excruciating, incapacitating joint discomfort. After treatment, these symptoms may start to manifest as soon as a few days or years later. When something is stopped, they can vanish.
- Symptoms could return if DPP-4 inhibitor medication is restarted.
- Bullous pemphigoid has been connected to the usage of DPP-4 inhibitors. The DPP-4 inhibitor ought to be stopped at that point.
- Contact your doctor right away if you notice any blisters or erosions.
- Symptoms of bullous pemphigoid should be considered. Call a dermatologist right away.
- Anaphylaxis and angioedema are two severe hypersensitivity events that have been recorded.
- In case you experience hypersensitive responses, stop using the product.
- The majority of things happen in the first three months following therapy.
- After the initial treatment, these occurrences are also possible.
- If the patient develops angioedema brought on by other DPP-4 inhibitors, use caution.
- It has been connected to acute pancreatitis, such as hemorrhagic and necrotizing pancreatitis.
- Be mindful of the warning signs and symptoms of pancreatitis, which include nausea and vomiting.
- If you think you could have pancreatitis, stop taking the medication right away. Get the right medical care.
- Patients with a history of pancreatitis or current cases should exercise caution. We don't know if these patients are more vulnerable.
The effects on the renal system
- Acute renal impairment brought on by a decline in renal function may be treated with dialysis.
- Impaired absorption:
- Changes in transit or anatomical structure brought on by gastric bypass or sleeve gastrectomy surgery may have an impact on absorption.
- The therapeutic efficacy of Glucagon-like peptide-1 after exposure.
Be conscious of your pancreatitis symptoms and warning signals.
By having a gastric bypass or sleeve gastrectomy, endogenous secretion can be enhanced.
- Impaired absorption:
- DPP-4 inhibitors have been associated with myocardial infarction in cardiac outcome trials involving people with type 2 diabetes and atherosclerotic heart disease.
- Vildagliptin, according to the American Heart Association, may worsen myocardial infarction.
- Except for saxagliptin, the ADA may advise DPP-4 inhibitors for individuals with HF.
- Extreme caution should be used by patients who have the end-stage renal disease (ESRD), severe or moderate renal impairment, or both. They might require peritoneal dialysis, hemodialysis, or both.
- For patients with significant renal dysfunction, vildagliptin administration changes are required.
In individuals with stable glycemic management, check glycated hemoglobin twice a year.
The glycated hemoglobin of those with uncontrolled blood sugar is examined four times each day.
Additionally, keep an eye on your weight, SMBG (self-monitoring of blood glucose), and renal function.
How to administer Vildagliptin (Galvus)?
It is taken by mouth. It should ideally be taken with meals.
It could be suggested to patients who have a lot of gastrointestinal adverse effects to taking the medication in between meals.
Mechanism of action (MOA) of Vildagliptin (Galvus):
It is an inhibitor of DPP-IV. Enzymes called DPP-IV cut and deactivate endogenous GLP (Glucagon-like Peptide).
A glucose-dependent process involving GLP results in the release of insulin.
Vildagliptin increases insulin secretion, suppresses appetite (reduces hunger), and delays stomach emptying by extending the action of endogenous GLP.
Vildagliptin's half-life is three hours.
The peak medication concentration is reached within an hour of oral administration, or the start of the activity.
Elimination: It undergoes enzymatic metabolism rather than the CYP-450 route. Renal excretion is the method used to remove 23% of the medication from the body.
International Brand Names of Vildagliptin:
- Galvus (Novartis)
Vildagliptin Brand Names in Pakistan: