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Adults with hypertension can benefit from telmisartan's dual actions of lowering their chance of heart attack and stroke. A medical condition known as essential hypertension occurs when there is a prolonged elevation in arterial blood pressure without any discernible cause. An obstruction in the blood supply to the heart or brain results in heart attacks and strokes. It functions by preventing the body from using a hormone known as angiotensin II. Blood pressure rises as a result of this hormone's ability to narrow blood vessels. Telmisartan reduces high blood pressure by relaxing and widening blood vessels.
BRAND NAMES
Twynsta: It contains the active ingredients of amlodipine and telmisartan. It is available in the form of tablets used to treat essential hypertension.
Micardis: It contains the active ingredients of telmsartan. It is available in the form of tablets used to treat hypertension.
MECHANISM OF ACTION
Angiotensin II receptor blockers include telmisartan. It functions by obstructing an internal chemical that tightens blood vessels. Telmisartan causes the blood vessels to relax as a consequence. As a result, the heart receives more blood and oxygen, and blood pressure is lowered.
PHARMACOKINETICS
ABSORPTION
After oral administration, maximum plasma concentration was observed after 0.5 to 1 hour. The absolute bioavailability of telmisartan was 43%.
DISTRIBUTION
The volume of distribution of telmisartan was approximately 500 liters.
METABOLISM
The parent compound's glucuronide is the sole metabolite that has been detected in human plasma and urine, having been converted by conjugation to a pharmacologically inactive acyl-glucuronide. Telmisartan's metabolism does not include the cytochrome P450 isoenzyme.
EXCRETION
The majority of the given dosage of telmisartan was removed intact in feces by biliary excretion, with just trace quantities detectable in urine.
PHARMACODYNAMICS
An oral nonpeptide angiotensin II antagonist that targets the AT1 receptor subtype is called telmisartan. It is more receptive to the AT1 receptor subtype. Among commercially available ARBs, it has the highest affinity for the AT1 receptor and the lowest affinity for the AT2 receptors.
DOSAGE AND ADMINISTRATION
Telmisartan comes as a tablet that can be taken orally. It is usually taken with or without food.
It is available in tablets with the strengths of 20mg, 40mg, and 80mg.
DRUG INTERACTIONS
Drug interactions with telmisartan may include
- NSAIDs: ibuprofen, aspirin
- Blood thinner—heparin
- Heart problems: digoxin
- Hypertension drugs: lisinopril, enalapril, ramipril, and benzapril
- Diuretics: amiloride, spironolactone
- Muscle relaxants: tizanidine
- Antibiotics: trimethoprim
CONTRAINDICATIONS
Contraindications of telmisartan are hypersensitivity and co-administration with Askiren in patients with diabetes.
SIDE EFFECTS
Side effects of telmisartan may include
- Diarrhea
- Back pain
- Sinus pain
- congestion
Serious side effects of telmisartan may include
- Hoarseness
- Swelling of the face, throat, lips, eyes, or lower legs
- Blistering of the skin
- Difficulty breathing
OVERDOSE
Symptoms of overdose may include
- Fainting
- Dizziness
- Fast or slow heartbeat
TOXICITY
There is no remedy for telmisartan overdose. If symptoms of hypotension appear, supportive therapy should be initiated. Telmisartan cannot be eliminated by hemofiltration and is not dialysis-compatible.
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