List of 56 Drugs That Should Not Be Mixed With Viagra Contains Some Surprises
It is important to take this medication regularly and to follow your doctor’s instructions regarding blood pressure monitoring to ensure that you are getting the maximum benefit from the medication.
Telmisartan
Telmisartan is an ARB used to treat hypertension, diabetic nephropathy, and congestive heart failure.
Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects.
Type Small Molecule Groups Approved, Investigational Structure
Structure for Telmisartan (DB00966)
- 4′-((1,4′-dimethyl-2′-propyl(2,6′-bi-1H-benzimidazol)-1′-yl)methyl)-(1,1′-biphenyl)-2-carboxylic acid
- 4′-((4-methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid
- 4′-[(1,4′-dimethyl-2’propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl]-[1,1′-biphenyl]-2-carboxylic acid
- 4′-[(1,7′-dimethyl-2′-propyl-1H,3’H-2,5′-bibenzimidazol-3′-yl)methyl]biphenyl-2-carboxylic acid
- Telmisartan
Pharmacology
Used alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart failure (only in patients who cannot tolerate ACE inhibitors).
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Telmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. It has the highest affinity for the AT1 receptor among commercially available ARBS and has minimal affinity for the AT2 receptor. New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects, as PPARγ is a nuclear receptor that regulates specific gene transcription, and whose target genes are involved in the regulation of glucose and lipid metabolism, as well as anti-inflammatory responses. This observation is currently being explored in clinical trials. Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmisartan works by blocking the vasoconstrictor and aldosterone secretory effects of angiotensin II.
Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT1-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmisartan does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels. Studies also suggest that telmisartan is a partial agonist of PPARγ, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPARγ activators.
Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).
Highly bound to plasma proteins (>99.5%), mainly albumin and a1-acid glycoprotein. Binding is not dose-dependent.
Minimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.
Following either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).
Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Intravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.
Pathways
| Pathway | Category |
|---|---|
| Telmisartan Action Pathway | Drug action |
Pharmacogenomic Effects/ADRs
Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Products
Our datasets provide approved product information including: dosage, form, labeller, route of administration, and marketing period.
Brand Name Prescription Products
| Name | Dosage | Strength | Route | Labeller | Marketing Start | Marketing End | Region | Image |
|---|---|---|---|---|---|---|---|---|
| Act Telmisartan | Tablet | 40 mg | Oral | Actavis Pharma Company | 2012-10-19 | 2018-06-11 | Canada | |
| Act Telmisartan | Tablet | 80 mg | Oral | Actavis Pharma Company | 2012-10-19 | 2018-06-11 | Canada | |
| Alembic-telmisartan | Tablet | 40 mg | Oral | Alembic Pharmaceuticals Limited | Not applicable | Not applicable | Canada | |
| Alembic-telmisartan | Tablet | 80 mg | Oral | Alembic Pharmaceuticals Limited | Not applicable | Not applicable | Canada | |
| Kinzalmono | Tablet | 80 mg | Oral | Bayer Ag | 2016-09-08 | Not applicable | EU | |
| Kinzalmono | Tablet | 40 mg | Oral | Bayer Ag | 2016-09-08 | Not applicable | EU | |
| Kinzalmono | Tablet | 80 mg | Oral | Bayer Ag | 2016-09-08 | Not applicable | EU | |
| Kinzalmono | Tablet | 20 mg | Oral | Bayer Ag | 2016-09-08 | Not applicable | EU | |
| Kinzalmono | Tablet | 80 mg | Oral | Bayer Ag | 2016-09-08 | Not applicable | EU | |
| Kinzalmono | Tablet | 80 mg | Oral | Bayer Ag | 2016-09-08 | Not applicable | EU |
Generic Prescription Products
| Name | Dosage | Strength | Route | Labeller | Marketing Start | Marketing End | Region | Image |
|---|---|---|---|---|---|---|---|---|
| Ach-telmisartan | Tablet | 40 mg | Oral | Accord Healthcare Inc | 2014-03-12 | Not applicable | Canada | |
| Ach-telmisartan | Tablet | 80 mg | Oral | Accord Healthcare Inc | 2014-03-12 | Not applicable | Canada | |
| Ag-telmisartan | Tablet | 40 mg | Oral | Angita Pharma Inc. | 2021-10-12 | Not applicable | Canada | |
| Ag-telmisartan | Tablet | 80 mg | Oral | Angita Pharma Inc. | 2021-10-12 | Not applicable | Canada | |
| Apo-telmisartan | Tablet | 40 mg | Oral | Apotex Corporation | 2014-07-18 | Not applicable | Canada | |
| Apo-telmisartan | Tablet | 80 mg | Oral | Apotex Corporation | 2014-07-18 | Not applicable | Canada | |
| Auro-telmisartan | Tablet | 80 mg | Oral | Auro Pharma Inc | 2016-04-08 | Not applicable | Canada | |
| Auro-telmisartan | Tablet | 40 mg | Oral | Auro Pharma Inc | 2016-04-08 | Not applicable | Canada | |
| Bio-telmisartan | Tablet | 40 mg | Oral | Biomed Pharma | Not applicable | Not applicable | Canada | |
| Bio-telmisartan | Tablet | 80 mg | Oral | Biomed Pharma | Not applicable | Not applicable | Canada |
Mixture Products
| Name | Ingredients | Dosage | Route | Labeller | Marketing Start | Marketing End | Region | Image |
|---|---|---|---|---|---|---|---|---|
| Aa-telmisartan-amlodipine | Telmisartan (80 mg) + Amlodipine besylate (10 mg) | Tablet | Oral | Aa Pharma Inc | 2021-05-05 | Not applicable | Canada | |
| Aa-telmisartan-amlodipine | Telmisartan (40 mg) + Amlodipine besylate (5 mg) | Tablet | Oral | Aa Pharma Inc | Not applicable | Not applicable | Canada | |
| Aa-telmisartan-amlodipine | Telmisartan (80 mg) + Amlodipine besylate (5 mg) | Tablet | Oral | Aa Pharma Inc | 2021-05-05 | Not applicable | Canada | |
| Aa-telmisartan-amlodipine | Telmisartan (40 mg) + Amlodipine besylate (10 mg) | Tablet | Oral | Aa Pharma Inc | Not applicable | Not applicable | Canada | |
| Ach-telmisartan Hctz | Telmisartan (80 mg) + Hydrochlorothiazide (25 mg) | Tablet | Oral | Accord Healthcare Inc | 2014-05-27 | Not applicable | Canada | |
| Ach-telmisartan Hctz | Telmisartan (80 mg) + Hydrochlorothiazide (12.5 mg) | Tablet | Oral | Accord Healthcare Inc | 2014-05-27 | Not applicable | Canada | |
| Act Telmisartan/hct | Telmisartan (80 mg) + Hydrochlorothiazide (25 mg) | Tablet | Oral | Actavis Pharma Company | 2012-10-02 | 2018-04-30 | Canada | |
| Act Telmisartan/hct | Telmisartan (80 mg) + Hydrochlorothiazide (12.5 mg) | Tablet | Oral | Actavis Pharma Company | 2012-10-02 | 2018-04-30 | Canada | |
| Actelsar HCT | Telmisartan (40 mg) + Hydrochlorothiazide (12.5 mg) | Tablet | Oral | Actavis Group Hf | 2016-09-07 | Not applicable | EU | |
| Actelsar HCT | Telmisartan (80 mg) + Hydrochlorothiazide (12.5 mg) | Tablet | Oral | Actavis Group Hf | 2016-09-07 | Not applicable | EU |
Categories
- Agents Acting on the Renin-Angiotensin System
- Agents causing angioedema
- Agents causing hyperkalemia
- Angiotensin 2 Receptor Blocker
- Angiotensin II receptor antagonists
- Angiotensin II receptor blockers (ARBs) and calcium channel blockers
- Angiotensin II receptor blockers (ARBs) and diuretics
- Angiotensin II receptor blockers (ARBs), plain
- Angiotensin II Type 1 Receptor Blockers
- Angiotensin II Type 2 Receptor Blockers
- Angiotensin Receptor Antagonists
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- BCRP/ABCG2 Inhibitors
- Benzene Derivatives
- Benzimidazoles
- Biphenyl Compounds
- BSEP/ABCB11 Substrates
- Cardiovascular Agents
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- Hypotensive Agents
- P-glycoprotein inhibitors
- UGT1A3 substrates
show 3 more Substituents Aromatic heteropolycyclic compound / Azacycle / Azole / Benzimidazole / Benzoic acid / Benzoic acid or derivatives / Benzoyl / Biphenyl / Carboxylic acid / Carboxylic acid derivative / Heteroaromatic compound / Hydrocarbon derivative / Imidazole / Monocarboxylic acid or derivatives / N-substituted imidazole / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound
Chemical Identifiers
References
Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. Pubmed.
- Sharpe M, Jarvis B, Goa KL: Telmisartan: a review of its use in hypertension. Drugs. 2001;61(10):1501-29. [Article]
- Smith DH: Treatment of hypertension with an angiotensin II-receptor antagonist compared with an angiotensin-converting enzyme inhibitor: a review of clinical studies of telmisartan and enalapril. Clin Ther. 2002 Oct;24(10):1484-501. [Article]
- Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. doi: 10.3762/bjoc.6.25. [Article]
- Galzerano D, Capogrosso C, Di Michele S, Galzerano A, Paparello P, Lama D, Gaudio C: New standards in hypertension and cardiovascular risk management: focus on telmisartan. Vasc Health Risk Manag. 2010 Mar 24;6:113-33. [Article]
Clinical Trials
| Phase | Status | Purpose | Conditions | Count |
|---|---|---|---|---|
| 4 | Completed | Prevention | Atrial Fibrillation | 2 |
| 4 | Completed | Prevention | Cardiovascular Disease (CVD) | 1 |
| 4 | Completed | Prevention | Cerebrovascular Accident | 1 |
| 4 | Completed | Prevention | High Blood Pressure (Hypertension) | 1 |
| 4 | Completed | Treatment | Abdominal Aortic Aneurysm (AAA) | 1 |
| 4 | Completed | Treatment | Cardiovascular Disease (CVD) / Cerebrovascular Accident / Chronic Kidney Disease (CKD) / Hypertension, Essential Hypertension | 1 |
| 4 | Completed | Treatment | Chronic Kidney Disease (CKD) / Proteinuria | 1 |
| 4 | Completed | Treatment | Congestive Heart Failure (CHF) | 1 |
| 4 | Completed | Treatment | Coronary Arteriosclerosis / High Blood Pressure (Hypertension) | 1 |
| 4 | Completed | Treatment | Coronary Artery Disease (CAD) / Diabetes / High Blood Pressure (Hypertension) | 1 |
Pharmacoeconomics
Dosage Forms
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral | |
| Capsule, coated | Oral | |
| Capsule, coated | Oral | 80 mg |
| Tablet | Oral | 25 mg |
| Tablet, coated | Oral | 40 mg |
| Tablet, coated | Oral | 80 mg |
| Tablet | Oral | 20 mg/1 |
| Tablet | Oral | 40 mg/1 |
| Tablet | Oral | 80 mg/1 |
| Tablet | Oral | 40 mg |
| Tablet | Oral | 80 mg |
| Tablet | Oral | |
| Tablet | Oral | 12.5 mg |
| Solution | Oral | |
| Tablet | Oral | 40.0 mg |
| Tablet | 80 Mg | |
| Tablet | Oral | 30 MG |
| Tablet | Oral | 60 MG |
| Tablet, film coated | Oral | 20 MG |
| Tablet, film coated | Oral | 40 MG |
| Tablet, film coated | Oral | 80 MG |
| Tablet, film coated | Oral | |
| Tablet | Oral | 50 mg |
| Tablet, film coated | Oral | |
| Tablet | Oral | 20 MG |
| Tablet | Oral | 12.50 mg |
| Tablet | Oral | 25.00 mg/tablet |
| Tablet | Oral | 40.00 mg |
| Tablet | Oral | 80.00 mg |
| Tablet, multilayer | Oral | |
| Tablet | Oral | 10 mg |
| Tablet | Oral | 5 mg |
| Tablet, coated | Oral |
Prices
| Unit description | Cost | Unit |
|---|---|---|
| Micardis 30 40 mg tablet Box | 110.11USD | box |
| Micardis HCT 30 40-12.5 mg tablet Box | 106.34USD | box |
| Micardis HCT 30 80-12.5 mg tablet Box | 106.18USD | box |
| Micardis 30 80 mg tablet Box | 103.92USD | box |
| Micardis HCT 30 80-25 mg tablet Box | 100.48USD | box |
| Micardis 30 20 mg tablet Box | 99.7USD | box |
| Micardis 20 mg tablet | 3.29USD | tablet |
| Micardis hct 40-12.5 mg tablet | 3.29USD | tablet |
| Micardis hct 80-12.5 mg tablet | 3.29USD | tablet |
| Micardis hct 80-25 mg tablet | 3.29USD | tablet |
| Micardis 40 mg tablet | 2.24USD | tablet |
| Micardis 80 mg tablet | 2.24USD | tablet |
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
| Patent Number | Pediatric Extension | Approved | Expires (estimated) | Region |
|---|---|---|---|---|
| US5591762 | No | 1997-01-07 | 2014-01-07 | US |
| CA2060624 | No | 1999-12-21 | 2012-02-04 | Canada |
| US6358986 | No | 2002-03-19 | 2020-01-10 | US |
| US7998953 | No | 2011-08-16 | 2020-06-06 | US |
| US8003679 | No | 2011-08-23 | 2022-10-06 | US |
Properties
State Solid Experimental Properties
| Property | Value | Source |
|---|---|---|
| melting point (°C) | 261-263 °C | Not Available |
| water solubility | Practically insoluble | Not Available |
| logP | 7.7 | Not Available |
| Caco2 permeability | -4.82 | ADME Research, USCD |
Predicted Properties
| Property | Value | Source |
|---|---|---|
| Water Solubility | 0.0035 mg/mL | ALOGPS |
| logP | 6.66 | ALOGPS |
| logP | 6.13 | Chemaxon |
| logS | -5.2 | ALOGPS |
| pKa (Strongest Acidic) | 3.62 | Chemaxon |
| pKa (Strongest Basic) | 5.86 | Chemaxon |
| Physiological Charge | -1 | Chemaxon |
| Hydrogen Acceptor Count | 4 | Chemaxon |
| Hydrogen Donor Count | 1 | Chemaxon |
| Polar Surface Area | 72.94 Å 2 | Chemaxon |
| Rotatable Bond Count | 7 | Chemaxon |
| Refractivity | 164.49 m 3 ·mol -1 | Chemaxon |
| Polarizability | 58.61 Å 3 | Chemaxon |
| Number of Rings | 6 | Chemaxon |
| Bioavailability | 0 | Chemaxon |
| Rule of Five | No | Chemaxon |
| Ghose Filter | No | Chemaxon |
| Veber’s Rule | No | Chemaxon |
| MDDR-like Rule | Yes | Chemaxon |
Predicted ADMET Features
| Property | Value | Probability |
|---|---|---|
| Human Intestinal Absorption | + | 1.0 |
| Blood Brain Barrier | + | 0.8794 |
| Caco-2 permeable | – | 0.8957 |
| P-glycoprotein substrate | Substrate | 0.6061 |
| P-glycoprotein inhibitor I | Non-inhibitor | 0.5261 |
| P-glycoprotein inhibitor II | Inhibitor | 0.8653 |
| Renal organic cation transporter | Non-inhibitor | 0.6047 |
| CYP450 2C9 substrate | Non-substrate | 0.7876 |
| CYP450 2D6 substrate | Non-substrate | 0.9116 |
| CYP450 3A4 substrate | Non-substrate | 0.5255 |
| CYP450 1A2 substrate | Inhibitor | 0.5699 |
| CYP450 2C9 inhibitor | Non-inhibitor | 0.5481 |
| CYP450 2D6 inhibitor | Non-inhibitor | 0.7796 |
| CYP450 2C19 inhibitor | Non-inhibitor | 0.5509 |
| CYP450 3A4 inhibitor | Non-inhibitor | 0.8309 |
| CYP450 inhibitory promiscuity | High CYP Inhibitory Promiscuity | 0.601 |
| Ames test | Non AMES toxic | 0.6432 |
| Carcinogenicity | Non-carcinogens | 0.9094 |
| Biodegradation | Not ready biodegradable | 0.9862 |
| Rat acute toxicity | 2.8075 LD50, mol/kg | Not applicable |
| hERG inhibition (predictor I) | Weak inhibitor | 0.9166 |
| hERG inhibition (predictor II) | Non-inhibitor | 0.7114 |
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)
Spectra
Mass Spec (NIST) Not Available Spectra
| Spectrum | Spectrum Type | Splash Key |
|---|---|---|
| Predicted GC-MS Spectrum – GC-MS | Predicted GC-MS | Not Available |
| Predicted MS/MS Spectrum – 10V, Positive (Annotated) | Predicted LC-MS/MS | Not Available |
| Predicted MS/MS Spectrum – 20V, Positive (Annotated) | Predicted LC-MS/MS | Not Available |
| Predicted MS/MS Spectrum – 40V, Positive (Annotated) | Predicted LC-MS/MS | Not Available |
| Predicted MS/MS Spectrum – 10V, Negative (Annotated) | Predicted LC-MS/MS | Not Available |
| Predicted MS/MS Spectrum – 20V, Negative (Annotated) | Predicted LC-MS/MS | Not Available |
| Predicted MS/MS Spectrum – 40V, Negative (Annotated) | Predicted LC-MS/MS | Not Available |
| LC-MS/MS Spectrum – LC-ESI-qTof , Positive | LC-MS/MS | Not Available |
| LC-MS/MS Spectrum – LC-ESI-QTOF , negative | LC-MS/MS | splash10-03di-0000090000-219191b231632ae82938 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , negative | LC-MS/MS | splash10-03di-0002490000-d9a86d68a321494f4172 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , negative | LC-MS/MS | splash10-00li-0095500000-433f75bf696d30339ffe |
| LC-MS/MS Spectrum – LC-ESI-QTOF , negative | LC-MS/MS | splash10-000i-0093100000-d1a212009af2d2b6d576 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , negative | LC-MS/MS | splash10-000i-0093000000-dc77c406187bdc1b4750 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-014i-0000900000-2da316f976108d0ab57a |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-03di-0000090000-fa13ab012f6c3edda644 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-0fri-0094500000-fc4e746d5acf7c28974b |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-000i-0093000000-739535a2fb80154ac329 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-000i-0093000000-7b45a183400fc2d5c56e |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-0079-0090000000-f2b72bb436b094188b4b |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-03di-0000090000-4193d926fb43b7e7650a |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-00ri-0090400000-4c927fd317a9c571c8c1 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-000i-0094000000-a362fb77a1bf330b4d4b |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-0f79-0095000000-c9574b21fc223d1415ff |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-000i-0090000000-0d0b0eddab1ab829b1c1 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-00di-0090000000-95cf0efe8a365f6e1b11 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , negative | LC-MS/MS | splash10-014i-0000900000-3c8f5cf8f5d9a897d72d |
| LC-MS/MS Spectrum – LC-ESI-QFT , negative | LC-MS/MS | splash10-01p9-0093450000-1dd7fd500cf0b3c0dc32 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , positive | LC-MS/MS | splash10-014i-0000090000-d2b14455bf61ea4f82a1 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , positive | LC-MS/MS | splash10-014i-0000090000-6187f6c1620a7c2b51b1 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , positive | LC-MS/MS | splash10-014i-0000090000-dc95af971f11219cb750 |
| LC-MS/MS Spectrum – LC-ESI-QTOF , positive | LC-MS/MS | splash10-014j-0000690000-92f9c219585dd2f6abdd |
| LC-MS/MS Spectrum – LC-ESI-QTOF , positive | LC-MS/MS | splash10-002b-0091820000-b4160c5238973be1326b |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-0002-0000900000-81da14e51168bd40dbc8 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-014i-0000090000-e488353a2ab5a5ca95c8 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-014i-0000090000-45ac38d5e068041afc7f |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-0002-0051930000-355f3efe4c799be31eee |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-004i-0091000000-0119ca397b44d63c12e1 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-004i-0190000000-c8f628b5d1752b565720 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-03fr-0290000000-e1a994dd22ac9af9bd71 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-014i-0000090000-79a32c207900b92a8001 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-014i-0000090000-522439ae25d7e43446e5 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-002b-0061930000-355af521f837490feefd |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-004i-0091000000-28e6d3e6afd2cee22baf |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-004i-0190000000-24d6dc729edb2e402cb5 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-03fr-0290000000-8ed1014ce3c441c09502 |
| LC-MS/MS Spectrum – LC-ESI-ITFT , positive | LC-MS/MS | splash10-0002-0000900000-683d2b1a6727533bf2cc |
| MS/MS Spectrum – ESI-QTOF , positive | LC-MS/MS | splash10-014j-0000690000-e5484f50567b0ed1d402 |
| MS/MS Spectrum – , positive | LC-MS/MS | splash10-014i-0011390000-909e49aea97bff3f66e6 |
| MS/MS Spectrum – , positive | LC-MS/MS | splash10-0bt9-2596000000-b809729f5d533c915b79 |
| MS/MS Spectrum – , positive | LC-MS/MS | splash10-014i-0020390000-96e1851c27d6f6e79183 |
| MS/MS Spectrum – , positive | LC-MS/MS | splash10-0bt9-0289000000-899a015c97aa18e79eb5 |
| MS/MS Spectrum – , positive | LC-MS/MS | splash10-06vi-3892000000-408ee10cb09fe63e849e |
| MS/MS Spectrum – , positive | LC-MS/MS | splash10-016s-1493650000-7139ff8e100efd8f486c |
| LC-MS/MS Spectrum – LC-ESI-QFT , positive | LC-MS/MS | splash10-016r-0081290000-363d23081a66306a3f9e |
List of 56 Drugs That Should Not Be Mixed With Viagra Contains Some Surprises
Public Citizen has published a list of 56 drugs that interact badly with erectile dysfunction pills such as Pfizer‘s Viagra. Public Citizen’s WorstPills.com site reports:
In combination with ED drugs, these 56 drugs can cause dangerous falls in blood pressure that could lead to a heart attack or stroke; a potentially harmful “overdose,” even when taking the recommended amount; and decrease the effectiveness of the ED drugs themselves.
The drugs include the usual suspects, such as nitrates for blood pressure. Taken in combination with Viagra, Cialis ior Levitra nitrates can lead to potentially lethal drops in blood pressure.
But the list also includes some surprises — household name drugs that shouldn’t be taken with ED pills — including Flomax, Provigil and grapefruit juice. Some drugs increase plasma concentrations of ED drugs, potentially leading to toxicity, and others reduce those concentrations, making the drugs ineffective. Some examples:
- Potential low blood pressure triggers:
- Flomax (Boehringer Ingelheim)
- Potential toxicity:
- Reyataz (Bristol-Myers Squibb)
- Grapefruit juice
- Diflucan (Pfizer)
- Gleevec (Novartis)
- Crixivan (Merck)
- Tykerb (GlaxoSmithKline)
- Mifeprex (Danco Labs)
- Viracept (Pfizer)
- Ketek (Sanofi-Aventis)
- Potential Inhibitors:
- Sustiva (BMS)
- Provigil (Cephalon)
- Viramune (Boehringer)
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First published on January 6, 2009 / 10:22 AM
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[Interaction between sildenafil and antihypertensive drugs: what is evidence-based?]
Hypertension is an important risk factor for erectile dysfunction (ED). Consequently, there is a high coincidence between hypertension and ED. Oral sildenafil (Viagra) is an effective treatment for ED in patients with treated or untreated hypertension. The most common adverse events of sildenafil (headache, flushing, hypotension) result from its moderate vasodilating properties. The concomitant use of sildenafil and organic nitrates is contraindicated because it may lead to a potentiation of the decreases in blood pressure and thus cause life-threatening hypotension. In contrast, the concomitant use of sildenafil and different classes of antihypertensive agents (beta-blockers, alpha-blockers, diuretics, ACE inhibitors, calcium antagonists) may lead to additive but not to potentiating blood pressure decreases. Thus, this combination is unlikely to cause clinically significant hypotension or an increased incidence of adverse events. Sildenafil is an effective and well-tolerated treatment for ED in patients taking concomitant antihypertensive medication, including those on multidrug regimens.
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Interactions to Monitor Between Erectile Dysfunction Drugs and Other Medications
Many of the medications used in the treatment of erectile dysfunction have interactions with other medications, so it is crucial for pharmacists to carefully examine patient profiles to optimize therapy and ensure safety.
An estimated 30 to 50 million men in the United States have erectile dysfunction (ED), a condition defined by an inability to achieve or maintain an erection firm enough for sexual intercourse. Although not a deadly condition, it often has a drastic effect on a person’s quality of life, leading many men with ED to seek treatment.
It is important to note that because the prevalence of ED increases with age, it is common for those affected to have other comorbidities or treatment regimens. Many of the medications used in the treatment of ED have interactions with other medications, so it is crucial for pharmacists to carefully examine patient profiles to optimize therapy and ensure safety.
The most common cause of ED is when blood flow to the penis is reduced. This can be caused by a multitude of reasons, but we most often see this issue arise commonly in patients who suffer from hypertension and atherosclerosis. The antihypertensive drugs designed to lower blood pressure in those patients can also contribute to reducing blood flow to the penis.
ED can also be associated with diabetes, obesity, smoking, and excessive alcohol consumption. Stress, anxiety, and depression can also psychologically affect a man’s ability to get an erection.
Phosphodiesterase type 5 (PDE-5) inhibitors are considered the first line and the mainstay treatment for ED. When sexually stimulated, nitric oxide is released locally, which increases cyclic guanosine monophosphate (cGMP). cGMP causes smooth muscle relaxation, which permits more blood flow into the penis, allowing for an erection. PDE-5 is a natural enzyme that degrades cGMP and shuts off the erection mechanism when sexual stimulation ends.
By inhibiting PDE-5, drugs such as sildenafil (Viagra; Pfizer), tadalafil (Cialis; Eli Lilly and Co.), vardenafil (Levitra; Bayer Pharmaceuticals), and avanafil (Stendra; Metuchen Pharmaceuticals) work to temporarily maintain an erection.
PDE-5 inhibitors have very important interactions that we must keep in mind at all times. It is contraindicated to use these meds with nitrates [e.g., nitroglycerin (Nitrostat; Pfizer)], isosorbide mononitrate (Imdur; TopRidge Pharma), isosorbide dinitrate (Isordil; Bausch), or riociguat (Adempas; Bayer).
Doing so can result in severe hypotension, potentially leading to fainting, heart attack, or stroke. Patients who take nitrate-containing products for angina or other cardiac-related problems must avoid using PDE-5 inhibitors. If a patient experiences angina and needs nitroglycerin, it cannot be used until 24 hours after sildenafil or vardenafil, 12 hours after avanafil, and 48 hours after tadalafil.
In general, sexual activity can put a strain on the heart, so it ends up being an even more dangerous situation for those with cardiac issues if they take PDE-5 inhibitors. Additionally, PDE-5 inhibitors also need to be used in caution with other drugs that can cause hypotension, such as antihypertensives and alpha blockers, because they potentiate the hypotensive effects when used together.
Other than these interactions, PDE-5 inhibitors should also be avoided with moderate to strong CYP450 3A4 inhibitors, because these drugs can increase the levels of PDE-5 inhibitors in the body. The reverse is also true for the opposite; CYP450 3A4 inducers could decrease drug levels.
Alternative to PDE-5 Inhibitors
Apo-Telmisartan
How does this medication work? What will it do for me?
Telmisartan belongs to a class of medications known as angiotensin II receptor antagonists. These medications reduce blood pressure by blocking the actions of a chemical (angiotensin II) that causes blood vessels to constrict or tighten. It is used to treat mild-to-moderate high blood pressure.
When blood pressure is allowed to remain high for a long time, the blood vessels of the heart, kidneys, and brain may become damaged. This puts a person at increased risk for heart attack and stroke as well as kidney failure and blindness. Keeping blood pressure in the normal range can reduce the risk for these conditions.
Telmisartan is also used to reduce the risk of death caused by a heart attack or stroke, for people who cannot use another type of medication called angiotensin-converting enzyme inhibitor.
This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.
Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.
Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.
What form(s) does this medication come in?
40 mg
Each white-to-off-white, modified capsule-shaped, biconvex tablet engraved “APO” on one side and “TEL 40” on the other side contains 40 mg telmisartan. Nonmedicinal ingredients: magnesium stearate, mannitol, meglumine, potassium hydroxide, and povidone.
80 mg
Each white-to-off-white, modified capsule-shaped, biconvex tablet engraved “APO” on one side and “TEL 80” on the other side contains 80 mg telmisartan. Nonmedicinal ingredients: magnesium stearate, mannitol, meglumine, potassium hydroxide, and povidone.
How should I use this medication?
The recommended adult dose of telmisartan is 80 mg once a day at approximately the same time each day, with or without food. It will take about 2 weeks for reductions in blood pressure to become noticeable and another 2 weeks until the full effects of the medication are realized. People with reduced liver function are usually given 40 mg once daily to start.
It is important to take this medication regularly and to follow your doctor’s instructions regarding blood pressure monitoring to ensure that you are getting the maximum benefit from the medication.
If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.
Many things can affect the dose of a medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.
Store telmisartan at normal room temperature in a dry place (not in the bathroom) and keep it out of the reach of children. Do not remove tablets from their blister-pack until you are ready to take them.
Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.
Who should NOT take this medication?
- are allergic to telmisartan or to any of the ingredients of the medication
- have experienced angioedema as a reaction to any angiotensin receptor blocker (ARB)
- are pregnant or plan to become pregnant
- are breast-feeding
- have diabetes or kidney disease and are taking the medication aliskiren
- are allergic to certain sugars (fructose and/or sorbitol intolerant)
What side effects are possible with this medication?
Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent. The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.
The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.
Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.
- abdominal pain
- anxiety
- back or leg pain
- constipation
- diarrhea
- difficulty sleeping
- dizziness
- drowsiness
- dry mouth
- eczema or skin rash
- gas
- headache
- heartburn
- joint pain
- muscle cramps or spasms
- nausea
- nervousness
- rash
- tiredness
- upper respiratory tract infection (such as colds or sinus infections)
- upset stomach
- vomiting
Although most of these side effects listed below don’t happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
- chest pain
- dizziness, fainting, or lightheadedness
- symptoms of low blood sugar (e.g., cold sweat, cool pale skin, headache, fast heartbeat, weakness)
- shortness of breath
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- signs of kidney problems (e.g., decreased urination, nausea, vomiting, swelling of the feet and ankles)
- signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
- signs of too much potassium in the body (e.g., irregular heartbeat, muscle weakness, generally feeling unwell)
- swelling of ankles, feet, or hands
- symptoms of a urinary tract infection (e.g., pain when urinating, urinating more often than usual, low back or flank pain)
- unexplained muscle pain, tenderness, or weakness
- vision changes
Stop taking the medication and seek immediate medical attention if any of the following occur:
- signs of a serious blood infection (e.g., chills, confusion, fever or low body temperature, shakiness, irregular heartbeat)
- signs of a serious allergic reaction (e.g., swelling of face, lips, tongue, or throat; hives; difficulty breathing)
Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.
Are there any other precautions or warnings for this medication?
Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.
Drowsiness/reduced alertness: Telmisartan may cause drowsiness or dizziness, affecting your ability to drive or operate machinery. Avoid these and other hazardous tasks until you have determined how this medication affects you.
Kidney disease: Telmisartan may affect kidney function, especially for people who already have kidney problems. Taking this medication along with the medication aliskiren or an angiotensin-converting enzyme inhibitor (ACEI) further increases the risk of kidney problems. If you have reduced kidney function or kidney disease, renal artery stenosis (narrowing of blood vessels in the kidneys), or congestive heart failure, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
If you experience symptoms of decreased kidney function, such as puffy hands, face or feet, high blood pressure, unusual muscle cramping, or darkened urine, contact your doctor as soon as possible.
Liver disease: Telmisartan is removed from the body by the liver. On rare occasions, it may cause liver problems. If you have liver disease or decreased liver function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.
Low blood pressure: If you have orthostatic hypotension (a sudden drop in blood pressure caused by standing up, which may lead to fainting), you should be cautious while taking telmisartan, as it can worsen the condition. The first time this medication is taken, it may cause dizziness, lightheadedness, or fainting. This may be reduced by taking the medication in a sitting position and being careful to rise slowly to a standing position. The dizziness usually improves after the first dose, but if the medication is stopped and then started again, it may reappear. Your doctor may also adjust the dose.
Potassium levels: This medication may affect potassium levels in the blood, especially when used for heart failure, or when taken with other medications called ACE inhibitors, aliskiren, or diuretics such as spironolactone. Your doctor will monitor your potassium levels while on this medication. Avoid using salt substitutes that contain potassium while you are taking telmisartan.
Pregnancy: Telmisartan may cause severe harm to an unborn fetus and should not be taken during pregnancy. If you discover you are pregnant while taking this medication, stop taking the medication and tell your doctor at once.
Breast-feeding: It is not known if telmisartan passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
Children: The safety and effectiveness of using this medication have not been established for children.
What other drugs could interact with this medication?
There may be an interaction between telmisartan and any of the following:
- aldesleukin
- aliskiren
- alpha-blockers (e.g., alfuzosin, doxazosin, silodosin, tamsulosin)
- amifostine
- amphetamines (e.g., dextroamphetamine, lisdexamfetamine)
- angiotensin-converting enzyme inhibitors (ACEIs; captopril, enalapril, ramipril)
- other angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
- antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- barbiturates (e.g., secobarbital, phenobarbital)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- brimonidine
- celecoxib
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- clonidine
- cyclosporine
- dexmethylphenidate
- digoxin
- dipyridamole
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- drospirenone
- duloxetine
- eplerenone
- guanfacine
- heparin
- hydralazine
- isosorbide dinitrate or isosorbide mononitrate
- levodopa
- lithium
- low molecular weight heparins (e.g., dalteparin, enoxaparin, tinzaparin)
- methyldopa
- methylphenidate
- minoxidil
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
- nitroglycerin
- nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., naproxen, ibuprofen)
- obinutuzumab
- pentoxifylline
- phosphodiesterase 5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
- potassium supplements or medications that increase potassium in the blood
- rituximab
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
- sodium phosphates
- tacrolimus
- tizanidine
- tolcapone
- tolvaptan
- trimethoprim
- yohimbine
If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:
- stop taking one of the medications,
- change one of the medications to another,
- change how you are taking one or both of the medications, or
- leave everything as is.
An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.
Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.
