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 to lower cardiovascular risk in those over 55 who are at high risk of developing serious cardiovascular events (such MI, stroke, or death) but cannot take ACE inhibitors..

• Hypertension:

  • It is used for the management of hypertension

• Label Use of Telmisartan in Adults:

  • Coronary syndrome, acute (secondary prevention of cardiovascular events)

  • Stable coronary artery disease

Telmisartan (Micardis) dose in Adults

Telmisartan (Micardis) dose in the treatment of Hypertension:

• Initial:
  • 20 to 40 mg administered once daily orally
  • Depending on the patient's response, the dose should be adjusted as necessary, up to 80 mg once daily.

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

• 80 mg orally once daily given

Telmisartan (Micardis) dose in Children

Not recommended for use in children.

Telmisartan (Micardis) pregnancy Risk Factor: D

• Ramipril, an ACE inhibitor, is similar to captopril in its pharmacologic properties and blocks the production of angiotensin II from angiotensin I.
• Ramipril undergoes enzymatic saponification by esterases in the liver to produce ramiprilat, which is ramipril's physiologically active metabolite.
• The competitive, high-affinity, and reversible binding of ramiprilat to the angiotensin-converting enzyme causes ramipril to have pharmacological effects by inhibiting the production of the potent vasoconstrictor angiotensin II.
• This isomerized enzyme inhibitor complex has a slow dissociation rate.
• Warning: US Boxed Medications that interfere with the renin-angiotensin systems can harm or kill a developing foetus.
• Once you are aware that you are pregnant, stop immediately.
• Drugs that affect the Renin-angiotensin System can cause the condition oligohydramnios.
• Fetal kidney failure and skeletal abnormalities can result from oligohydramnios.
• Hypotension, anuria, and renal failure are all linked to it.
• Look for indications of foetal growth, amniotic fluid volume, and potential organ creation in the exposed foetus.
• Children exposed to hyperkalemia, hypotension, and oliguria while they were developing should be assessed (exchange transfusions, dialysis may be necessary).
• The use by mothers throughout the second and third trimesters is frequently linked to these negative side effects.
• If left untreated, chronic maternal hypertension can have negative effects on the pregnancy, mother, and baby.
• 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.
• High potency, sustained effect, and high potency are the outcomes.
• Angiotensin II, which boosts the CNS's adrenergic output, also lowers blood pressure via a CNS mechanism.
• ACE inhibitors may decrease the conversion of vasoactive kallikreins to active hormones, lowering blood pressure.

Dose for kidney disease:

• No change in dose is necessary
• Orthostatic hypotension is more likely to occur in hemodialysis patients.

Dose for liver disease:

• Start your therapy with a low dose, titrate cautiously, and keep an eye on things.

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

• Angioedema
  • Some angiotensin II receptor inhibitors can cause the rare adverse effect of angioedema (ARBs). Anytime during therapy, but especially after the first dose, it can happen.
  • Additionally, it might affect the head and neck, possibly impairing the airway, or the gut, resulting in discomfort in the abdomen.
  • Patients who have previously had idiopathic or genetic angioedema or angioedema linked to ACE-inhibitor medication are more vulnerable.
  • 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.
• 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.
• 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.
• 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.
  • Oliguria, severe renal failure, or progressive azotemia can result from deterioration.
  • Small increases in serum creatinine may happen after starting.
  • Patients with progressive and severe impairment of renal function must stop taking the medication.
• Aortic/mitral stenosis:
  • Patients with severe aortic/mitralstenosis should be cautious.
• Ascites:
  • Avoid patients with ascites caused by cirrhosis, refractory ascites, or other reasons.
  • If patients with cirrhosis or ascites are unable to refrain from taking the medication, it is crucial to regularly monitor blood pressure and kidney function to stop the rapid onset of renal failure.
• Hepatic impairment
  • Patients with biliary obstruction disorders or hepatic dysfunction should be cautious.
• Renal artery stenosis
  • Patients who have unilateral or bilateral renal artery stenosis that is untreated should exercise caution.
  • Due to the increased risk of renal impairment, this should not be done in cases of bilateral unstented renal artery stenosis.
• Renal impairment
  • Pre-existing renal impairment or severe renal insufficiency should be avoided.

Telmisartan: Drug Interaction

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.
• Vasoconstriction is another effect of it. Aldosterone is released when angiotensin II is stimulated.
• Sodium and water are released by aldosterone, which causes reabsorption.
• The result is a rise in blood pressure.
• Another name for Telmisartan is Telmisartan, which is a nonpeptide AT1 receptor antagonist.
• This binding prevents angiotensin I from attaching to the receptor, blocking both the effects of angiotensin 2 on vasoconstriction and the release of aldosterone.

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 not processed by CYP, but rather by the liver through conjugation to inactive metabolites.

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

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

Telmisartan (Micardis) Brands in Pakistan: