Telmisartan

 

1. Telmisartan
2. TelmisartanTelmisartan

 Generic name: telmisartan (TEL mi SAR tan)

Dosage forms: oral tablet (20 mg; 40 mg; 80 mg)
Drug class: Angiotensin receptor blockers

Telmisartan (Micardis) is an angiotensin II receptor blocker that is primarily used as an antihypertensive medicine.

It is used to treat the following conditions:

• Cardiovascular risk reduction:

  • It is used for cardiovascular risk reduction in patients 55 years of age or older who are at high risk of major cardiovascular events (eg, MI, stroke, death) and are unable to take ACE inhibitors.

• Hypertension:

  • It is used for the management of hypertension

• Label Use of Telmisartan in Adults:

  • Acute coronary syndrome (secondary prevention of cardiovascular events);

  • Stable coronary artery disease

Telmisartan (Micardis) dose in the treatment of Hypertension:

• Initial:
  • 20 to 40 mg orally once given daily
  • The dose should be titrated as needed based on the patient’s response up to 80 mg once a day.

Telmisartan (Micardis) dose in the treatment of Cardiovascular risk reduction:

• 80 mg orally once daily given

 

Not recommended for use in children.

 

Telmisartan (Micardis) pregnancy Risk Factor: D

• • Ramipril, an ACE inhibitor, prevents angiotensin II formation from angiotensin 1, and has pharmacologic effects similar to captopril.
  • Ramipril is also subject to enzymatic saponification in the liver by esterases to become its biologically active metabolite ramiprilat.
  • The pharmacodynamic effects of ramipril result from the competitive, high-affinity, and reversible binding of ramiprilat to the angiotensin-converting enzyme, thus preventing the formation of the potent vasoconstrictor angiotensin II.
  • The dissociation rate for this isomerized enzyme inhibitor complex is also slow
    • [US Boxed Warn] Drugs that affect the renin-angiotensin systems can cause injury or death in the developing fetus.

  o    Once you are aware that you are pregnant, stop immediately.

  • • Oligohydramnios is a condition that results from the use of drugs which act on the Renin-angiotensin System.
    • Oligohydramnios can cause fetal kidney dysfunction and skeletal malformations.
    • It is associated with hypotension, anuria and renal failure.
    • Examine the exposed fetus for signs of fetal growth, amniotic liquid volume, and potential organ formation.
    • Children exposed in utero to hyperkalemia, hypotension and oliguria should be evaluated (exchange transfusions, dialysis may be necessary).
    • These adverse events are often associated with maternal use during the second and third trimesters.
    • Chronic maternal hypertension, if not treated, can also lead to adverse events in the infant, mother, and fetus.
    • Angiotensin II receptor blocking agents should not be used to treat uncomplicated hypertension. They should be avoided by women with reproductive potential.

  Telmisartan (Micardis) use during breastfeeding:

  • • It is unknown if telmisartan can be found in breast milk.
    • Consider the possibility of serious side effects for breastfeeding infants. It is important to weigh the risks and benefits of drug exposure to the child as well as the benefits to the mother.

  This results in high potency, long-lasting action and high potency.

  • Angiotensin II, which increases the adrenergic output from CNS, also has a hypotensive effect through a CNS mechanism
  • Vasoactive kallikreins may be reduced in conversion to activehormones by ACE inhibitors, thereby reducing blood pressure

 

Telmisartan (Micardis) dose in kidney disease:

• No dosage adjustment required
• hemodialysis patients are more susceptible to orthostatic hypotension

 

Telmisartan (Micardis) dose in liver disease:

• Start therapy with low dose
• titrate slowly and monitor closely.

 

Side Effects of Telmisartan (Micardis) Include:

• Cardiovascular:

  • Intermittent Claudication
  • Chest Pain
  • Hypertension
  • Peripheral Edema

• Central Nervous System:

  • Dizziness
  • Fatigue
  • Headache
  • Pain

• Dermatologic:

  • Dermal Ulcer

• Gastrointestinal:

  • Diarrhea
  • Abdominal Pain
  • Dyspepsia
  • Nausea

• Genitourinary:

  • Urinary Tract Infection

• Neuromuscular & Skeletal:

  • Back Pain
  • Myalgia

• Respiratory:

  • Upper Respiratory Tract Infection
  • Sinusitis
  • Cough
  • Flu-Like Symptoms
  • Pharyngitis

 

Contraindication to Telmisartan (Micardis) Include:

• • • Hypersensitivity to telmisartan, or any component of it, is a known condition
    • Patients with diabetes can concurrently take aliskiren
    • pregnancy
    • Breastfeeding
    • fructose intolerance

Warnings and precautions

o    Angioedema

• • • Angioedema is a rare side effect of some angiotensin II receptor inhibitors (ARBs). It can occur anytime during treatment, especially after the first dose.
    • It could also affect the head and neck, potentially compromising the airway, or the intestine, causing abdominal pain.
    • Patients with idiopathic or hereditary angioedema or previous angioedema associated with ACE-inhibitor therapy are at an increased risk.
    • Patients with larynx, tongue, or glottis edema may need to be monitored frequently and for a prolonged period of time.
    • Patients who have had previous airway surgery may be at greater risk for obstruction.
    • If angioedema develops, stop treatment immediately.
    • It is crucial to be aggressive in early management.
    • Intramuscular (IM) administration of epinephrine is necessary.
    • Patients who have angioedema caused by ARBs should not be given.

o    Hyperkalemia:

• • • It is possible for this to happen. Risk factors include kidney dysfunction, potassium supplements and diabetes mellitus.
    • These agents should be used with caution and potassium should be monitored closely.

o    Hypotension

• • • Patients who have been treated with high-dose diuretics or salt-depleted can develop symptoms of hypotension.
    • correct volume depletion before administration.
    • It is not contraindicated to use transient hypotension.

o    Renal function deterioration:

• • • Telmisartan can cause a decrease in renal function in patients who are low in renal blood flow, such as those with heart failure or renal artery stenosis.
    • High-risk patients are at high risk of developing azotemia. This is because their glomerular filter rate (GFR), primarily depends on the efferent arterial vasoconstriction, which is mediated through angiotensin 2.
    • Deterioration can lead to oliguria, acute kidney failure, or progressive azotemia.
    • After initiation, small increases in serum creatinine may occur.
    • Patients with progressive and severe impairment of renal function must stop taking the medication.

o    Aortic/mitral stenosis:

• • • Patients with severe aortic/mitralstenosis should be cautious.

o    Ascites:

• • • Patients with ascites due cirrhosis, refractory or other causes should be avoided
    • If patients suffering from ascites or cirrhosis cannot avoid the use of the drug, it is important to monitor blood pressure and kidney function closely to prevent rapid progression to renal failure.

o    Hepatic impairment

• • • Patients with biliary obstruction disorders or hepatic dysfunction should be cautious.

o    Renal artery stenosis

• • • Patients with unstented unilateral/bilateral kidney artery stenosis should be cautious.
    • This should not be done in bilateral unstented renal artery stenosis because of the increased risk of renal dysfunction.

o    Renal impairment

• • • Pre-existing renal impairment or severe renal insufficiency should be avoided.

 

Monitor:

• Blood pressure
• electrolytes
• serum creatinine
• BUN

 

How to administer Telmisartan (Micardis)?

• It may be administered orally without regard to meals.

 

Mechanism of action of Telmisartan (Micardis):

• Angiotensin II acts as a vasoconstrictor.
• It also causes vasoconstriction. Angiotensin II stimulates the release aldosterone.
• Aldosterone releases sodium and water, which results in reabsorption.
• This causes an increase in blood pressure. Telmisartan, a nonpeptide AT1 receptor antagonist, is also known as Telmisartan.
• This binding stops angiotensin I from binding to the receptor, thereby blocking the vasoconstriction as well as the aldosterone-secreting effects of angiotensin 2.
• Onset of action:

• 1 to 2 hours

Duration:

• Up to 24 hours

Distribution: V :

• 500 L

Protein binding:

• >99.5%; primarily to albumin and alpha -acid glycoprotein

Metabolism:

• It is metabolized by the liver via conjugation to inactive metabolites; not metabolized via CYP

Bioavailability (dose-dependent):

• 42% to 58%
• Hepatic impairment: Approaches 100%

Half-life elimination: Terminal:

• 24 hours

Time to peak, plasma:

• 0.5 to 1 hours

Excretion:

• Via Feces (97%)

Clearance:

Total body: 800 mL/minute

 

 

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

International Brands of Telmisartan:

• ACT Telmisartan
• APO-Telmisartan
• Auro-Telmisartan
• Micardis
• MYLAN-Telmisartan
• PMS-Telmisartan
• RAN-Telmisartan
• SANDOZ Telmisartan
• TEVA-Telmisartan
• VAN-Telmisartan
• Actelsar
• Agimstan
• Alimax
• Biocardis
• Cardiz
• Chartoreg
• Cilzec
• Floxetin
• Kinzalmono
• Lemitens
• Mibetel
• Micardis
• Mitosan
• Mizart
• Osan
• Predxal
• Pritor
• Pritoral
• RAAS
• Safetelmi
• Saitan
• T-Sar
• Tazloc
• Telday
• Teli 40
• Teli 80
• Telma-20
• Telmed
• Telmican
• Telmicard
• Telmimax
• Telmirama
• Telmisar
• Telmitrend
• Telmotens
• Telsan
• Telsar
• Telstan
• Teltartan
• Teltas
• TESAA
• TEZEO
• Tolura

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