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Sitagliptin

 
Drug Info: Sitagliptin
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Brand names: Januvia™



Sitagliptin tablets

What are Sitagliptin tablets?

SITAGLIPTIN (Januvia™) helps to treat type 2 diabetes. It helps to control blood sugar.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• kidney disease
• an unusual reaction to sitagliptin, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should this medicine be used?

Take this medicine by mouth. Swallow with a drink of water. Follow the directions on the prescription label. You can take it with or without food. Take your dose at the same time each day. Do not take more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with Sitagliptin?

• alcohol
• digoxin
• exenatide
• insulins
• nateglinide
• other drugs used to lower your blood sugar called sulfonylureas (examples: glimepiride, glipizide, glyburide)
• repaglinide

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking Sitagliptin?

Visit your doctor or health care professional for regular checks on your progress.

Learn how to check your blood sugar. Learn the symptoms of low and high blood sugar and how to manage them.

If you have low blood sugar, eat or drink something that has sugar. Make sure others know to get medical help quickly if you have serious symptoms of low blood sugar, like if you become unconscious or have a seizure.

If you are going to have surgery, tell your prescriber or health care professional that you are taking this medicine.

Wear a medical identification bracelet or chain to say you have diabetes, and carry a card that lists all your medications.

What side effects may I notice from receiving Sitagliptin?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• breathing problems
In combination with other diabetic medications, (like glyburide, glipizide, or insulin), sitagliptin may cause low blood sugar (hypoglycemia). Contact your health care professional if you experience symptoms of low blood sugar, which may include:
• anxiety or nervousness, confusion, difficulty concentrating, hunger, pale skin, nausea, fatigue, sweating, headache, palpitations, numbness of the mouth, tingling in the fingers, tremors, muscle weakness, blurred vision, cold sensations, uncontrolled yawning, irritability, rapid heartbeat, shallow breathing, and loss of consciousness

Symptoms of high blood sugar (hyperglycemia) include:
• dizziness, dry mouth, flushed dry-skin, fruit-like breath odor, loss of appetite, nausea, stomach ache, unusual thirst, frequent passing of urine

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• diarrhea
• headache
• stomach pain
• stuffy or runny nose

Where can I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 8/14/2006 1:34:00 PM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Sitagliptin
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Home > Library > Miscellaneous > Wikipedia
Sitagliptin
Systematic (IUPAC) name
(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Identifiers
CAS number 486460-32-6
ATC code A10BH01
PubChem 4369359
DrugBank DB01261
ChemSpider 3571948
Chemical data
Formula C16H15F6N5O 
Mol. mass 407.314 g/mol
Pharmacokinetic data
Bioavailability 87%
Protein binding 38%
Metabolism Hepatic (CYP3A4- and CYP2C8-mediated)
Half life 8 to 14 hours[1]
Excretion Renal (80%)[1]
Therapeutic considerations
Licence data

EU EMEA:link, US FDA:link
Pregnancy cat.

B(US)
Legal status

POM(UK) ℞-only(US)
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Sitagliptin (INN; previously identified as MK-0431, trade name Januvia) is an oral antihyperglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class, Sitagliptin being the only second generation DPP-4 inhibitor currently available in the USA. This enzyme-inhibiting drug is used either alone or in combination with other oral antihyperglycemic agents (such as metformin or a thiazolidinedione) for treatment of diabetes mellitus type 2. The benefit of this medicine is its lower side-effects (e.g., less hypoglycemia, less weight gain) in the control of blood glucose values. Exenatide (Byetta) also works by its effect on the incretin system.

Contents

Adverse effects

In clinical trials, adverse effects were as common with sitagliptin (whether used alone or with metformin or pioglitazone) as they were with placebo, except for extremely rare nausea and common cold-like symptoms.[2] There is no significant difference in the occurrence of hypoglycemia between placebo and sitagliptin.[2]

History

Sitagliptin was approved by the U.S. Food and Drug Administration (FDA) on October 17, 2006[3] and is marketed in the US as Januvia by Merck & Co. On April 2, 2007, the FDA approved an oral combination of sitagliptin and metformin marketed in the US as Janumet.

Mechanism of Action

See also: Dipeptidyl peptidase-4 inhibitors

Sitagliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones that are released in response to a meal.[4] By preventing GLP-1 and GIP inactivation, GLP-1 and GIP are able to potentiate the secretion of insulin and suppress the release of glucagon by the pancreas. This drives blood glucose levels towards normal. As the blood glucose level approaches normal, the amounts of insulin released and glucagon suppressed diminishes thus tending to prevent an "overshoot" and subsequent low blood sugar (hypoglycemia) which is seen with some other oral hypoglycemic agents.

See also

References

  1. ^ a b Herman G, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang A, Zeng W, Musson D, Winchell G, Davies M, Ramael S, Gottesdiener K, Wagner J (2005). "Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses.". Clin Pharmacol Ther 78 (6): 675–88. doi:10.1016/j.clpt.2005.09.002. PMID 16338283. 
  2. ^ a b "Januvia Side Effects & Drug Interactions". RxList.com. 2007. http://www.rxlist.com/cgi/generic/januvia_ad.htm. Retrieved 2007-11-28. 
  3. ^ U.S. Food and Drug Administration (October 17, 2006). "FDA Approves New Treatment for Diabetes". Press release. http://www.fda.gov/bbs/topics/NEWS/2006/NEW01492.html. Retrieved 2006-10-17. 
  4. ^ Herman G, Bergman A, Liu F, Stevens C, Wang A, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan A, Lasseter K, Dilzer S, Blum R, Wagner J (2006). "Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects.". J Clin Pharmacol 46 (8): 876–86. doi:10.1177/0091270006289850. PMID 16855072. 

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This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

 

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