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Telmisartan

 
Drug Info: Telmisartan
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Brand names: Micardis®

Chemical formula:



Telmisartan Oral tablet

What is this medicine?

TELMISARTAN (tel mi SAR tan) is used to treat high blood pressure.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

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

They need to know if you have any of these conditions:
•if you are on a special diet, such as a low-salt diet
•kidney or liver disease
•an unusual or allergic reaction to telmisartan, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. This medicine can be taken with or without food. Take your doses at regular intervals. Do not take your medicine more often than directed.

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

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

•digoxin
•potassium salts or potassium supplements
•warfarin

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Check your blood pressure as directed. Ask your doctor or health care professional what your blood pressure should be and when you should contact him or her. Call your doctor or health care professional if you notice an irregular or fast heart beat.

Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child, particularly in the second or third trimester. Talk to your health care professional or pharmacist for more information.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this drug affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can make you more drowsy and dizzy. Avoid alcoholic drinks.

Avoid salt substitutes unless you are told otherwise by your doctor or health care professional.

Do not treat yourself for coughs, colds, or pain while you are taking this medicine without asking your doctor or health care professional for advice. Some ingredients may increase your blood pressure.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor 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
•dark urine
•gout pain
•muscle pains
•slow heartbeat
•trouble passing urine or change in the amount of urine
•unusual bleeding or bruising
•yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•back pain
•change in sex drive or performance
•diarrhea
•sore throat or stuffy nose

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Tablets should not be removed from the blisters until right before use. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

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: Telmisartan
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Home > Library > Miscellaneous > Wikipedia
Main article: Angiotensin II receptor antagonist
Telmisartan
Systematic (IUPAC) name
2-(4-{[4-methyl-6-(1-methyl-1H-1,3-benzodiazol-2-yl)-2-propyl-1H-1,3-benzodiazol-1-yl]methyl}phenyl)benzoic acid
Identifiers
CAS number 144701-48-4
ATC code C09CA07
PubChem 65999
DrugBank APRD01247
Chemical data
Formula C33H30N4O2 
Mol. mass 514.617 g/mol
Pharmacokinetic data
Bioavailability 42–100%
Protein binding ≥99.5%
Metabolism Minimal hepatic
Half life 24 hours
Excretion Faecal 97%
Therapeutic considerations
Pregnancy cat.

D (Au), D (U.S.)
Legal status

S4 (Au), POM (UK), ℞-only (U.S.)
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Telmisartan (INN) (pronounced /tɛlmɪˈsɑrtən/) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. It is marketed under the trade names Normisaar (by Nabiqasim Pharmaceuticals Pakistan), Telminorm (by Ipca), Pritor or Kinzal (Bayer Schering Pharma), Micardis (Boehringer Ingelheim), Telma (Glenmark Pharma), Telday (Torrent Pharmaceuticals) and Teleact D by (Ranbaxy).

Contents

Administration

The usually effective dose Telmisartan ( T24 marketed by Rhys Healthcare) is 40 mg once daily. Some patients may already benefit at a daily dose of 20 mg. In cases where the target blood pressure is not achieved, telmisartan dose can be increased to a maximum of 80 mg once daily. [1]

Mode of action

Telmisartan (Teli marketed by cadila pharma) is an Angiotensin Receptor Blocker (ARB) that shows high affinity for the angiotensin II type 1 (AT1) receptors, has a long duration of action, and has the longest half-life of any ARB. [1][2]

In addition to blocking the Renin-Angiotensin System (RAS), telmisartan acts as a selective modulator of Peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. It is believed that telmisartan’s dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD). [2]

Telmisartan has binding affinity 3000 times greater for AT1 than AT2 receptors. Telmisartan also has the longest half life (24 hrs) of all angiotensin II type 1 receptor antagonists.

Indication

Telmisartan is indicated in the treatment of essential hypertension. [1]

Key Recent Clinical Trials

ONTARGET

The ONTARGET Trial Programme (The Ongoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial) was one of the largest ARB clinical study programmes ever undertaken.[3]

Salim Yusuf, Lead Investigator and Director of the Population Health Research Institute at McMaster University, Hamilton, Canada, presented the results of the l trial at the 57th Annual Scientific Session of the American College of Cardiology (ACC) in Chicago, USA. [4] The results were then published in The New England Journal of Medicine in April 2008.[5]

25,620 patients from 733 centres in 41 countries were randomised for 5.5 years of treatment of either telmisartan, the ACE inhibitor ramipril or a combination of the two. The study aimed to investigate the role of telmisartan in Cardiovascular (CV) protection through the primary composite outcome of death from CV causes, myocardial infarction, stroke or hospilization for heart failure, in high CV risk patients.

The results revealed that telmisartan was as effective as ramipril but with lower rates of cough and angioedema which led to fewer discontinuations. The combination group experienced similar efficacy but with increased risk of hypotensive symptoms. Moreover, even in a patient population selected to tolerate ACE inhibitors, telmisartan was shown to be better tolerated and associated with higher treatment compliance than ramipril. [6]

TRANSCEND

As part of the ONTARGET study, patients who could not tolerate ACE inhibitors were randomly assigned to receive either telmisartan or placebo as part of the TRANSCEND (Telmisartan Randomized Assessment Study in ACE Intolerant Subjects with Cardiovascular Disease (CVD)) study. Results from this study were published in the Lancet, September 2008. An accompanying editorial comments: "Overall, data supporting use of angiotensin-receptor blockers to prevent vascular events in various cardiovascular groups, other than heart failure, are incomplete. TRANSCEND's results challenge the non-inferiority shown in ONTARGET and suggest no more than a modest effect, if any at all." [7]

PROTECTION

The PROTECTION programme (Programme of Research tO show Telmisartan End-organ proteCTION) consisted of ten trials with 6,875 patients from 32 countries.[8]

The programme examined the efficacy of telmisartan or telmisartan/ hydrochlorothiazide at different stages of the cardiovascular and renal continuum. The trials were conducted in patients with varying degrees of cardiovascular risk from around the world

The 10 studies in the programme evaluated the effect of telmisartan on blood pressure control in two general patient populations: patients at high risk for cardiovascular disease and patients with various renal pathologies. In all the studies, telmisartan was compared either to placebo or to a gold standard medication such as the ACE inhibitors ramipril and enalapril or the ARBs losartan and valsartan.

Telmisartan met and sometimes exceeded the gold standards (ACEIs and other ARBs) during the programme. In at-risk patient populations, telmisartan induced strong and sustained blood pressure lowering throughout the critical morning period where CV risk is highest ,and renoprotective effects at every stage of the renal continuum. [9][10]

PRoFESS

PRoFESS - Prevention Regimen For Effectively Avoiding Second Strokes. Therapy with telmisartan initiated soon after an ischemic stroke and continued for 2.5 years did not significantly lower the rate of recurrent stroke, major cardiovascular events, or diabetes. (ClinicalTrials.gov number, NCT00153062)[11]

See also

Angiotensin Receptor Blockers: Drug discovery and development

External links

References

  1. ^ a b c Pritor prescribing information
  2. ^ a b Benson SC et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension 2004 May; 43(5): 993-1002.
  3. ^ The ONTARGET Investigators. Telmisartan, Ramipril, or Both in Patients at High Risk for Vascular Events N Engl J Med 2008;358:1547-59.
  4. ^ http://www.ICMAedu.com
  5. ^ The ONTARGET Investigators. Telmisartan, Ramipril, or Both in Patients at High Risk for Vascular Events N Engl J Med 2008;358:1547-59.
  6. ^ http://www.ICMAedu.com
  7. ^ The Lancet 2008;372(9644): 1128–1130.
  8. ^ Weber M. The telmisartan Programme of Research tO show Telmisartan End-organ proteCTION (PROTECTION) programme. J Hypertens 2003;21 (Suppl 6):S37–S46.
  9. ^ Weber M. The telmisartan Programme of Research tO show Telmisartan End-organ proteCTION (PROTECTION) programme. J Hypertens 2003;21 (Suppl 6):S37–S46.
  10. ^ http://www.pritor.com
  11. ^ http://clinicaltrials.gov/show/NCT00153062
v • d • e
Antihypertensives: agents acting on the renin-angiotensin system (C09)
ACE inhibitors
("-pril")
AIIRAs/
("-sartan")
Renin inhibitors/
("-kiren")

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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