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Product Name
:
MICARDROXI
Chemical Name
:
Telmisartan
Therapeutic Category
:
Cardiovascular drugs
Pharmacologic Category
:
Angiotensin II Receptor Blocker
Pharmaceutical Form
:
Tablets
Composition
:
Telmisartan 40mg/ 80mg
Dosing
 
Dosing: Adult

Hypertension: Oral: Initial: 40 mg once daily; usual maintenance dose range: 20-80 mg/day. Patients with volume depletion should be initiated on the lower dosage with close supervision.

Cardiovascular risk reduction: Oral: Initial: 80 mg once daily. Note: It is unknown whether doses <80 mg/day are associated with a reduction in risk of cardiovascular morbidity or mortality.

Dosing: Geriatric

Hypertension: Oral: Initial: 20 mg/day; usual maintenance dose range: 20-80 mg/day

Cardiovascular risk reduction: Oral: Initial 80 mg once daily

Dosing: Renal Impairment

No adjustment required; hemodialysis patients are more susceptible to orthostatic hypotension


Dosing: Hepatic Impairment

Initiate therapy with low dose; titrate slowly and monitor closely.

Use
 

Treatment of hypertension (may be used alone or in combination with other antihypertensive agents); cardiovascular risk reduction in patients ≥55 years of age unable to take ACE inhibitors and who are at high risk of major cardiovascular events (eg, MI, stroke, death)

Adverse Reactions
 

1% to 10%:

Cardiovascular: Intermittent claudication (7%; placebo 6%), chest pain (≥1%), hypertension (≥1%), peripheral edema (≥1%)

Central nervous system: Dizziness (≥1%), fatigue (≥1%), headache (≥1%), pain (≥1%)

Dermatologic: Skin ulcer (3%; placebo 2%)

Gastrointestinal: Diarrhea (3%), abdominal pain (≥1%), dyspepsia (≥1%), nausea (≥1%)

Genitourinary: Urinary tract infection (≥1%)

Neuromuscular & skeletal: Back pain (3%), myalgia (≥1%)

Respiratory: Upper respiratory infection (7%), sinusitis (3%), cough (≥1%), pharyngitis (1%)

<1% (Limited to important or life-threatening): Abnormal ECG, abscess, allergic reaction, anaphylaxis, anemia, angina, angioedema, arthritis, asthma, atrial fibrillation, bradycardia, cerebrovascular disorder, CHF, conjunctivitis, creatinine kinase increased, depression, diabetes mellitus, eczema, edema, epistaxis, erectile dysfunction, fixed drug eruption, fungal infection, gastroenteritis, gout, hepatic dysfunction, hypercholesterolemia, hyperkalemia, hypersensitivity, hypoglycemia (diabetic patients), hypotension, impotence, insomnia, MI, migraine, neoplasm, orthostatic hypotension (more frequent in dialysis patients), otitis media, renal failure, rhabdomyolysis, reflux, serum creatinine increased, syncope, tachycardia, tendon pain, thrombocytopenia, uric acid increased

Contraindications
 
Hypersensitivity to telmisartan or any component of the formulation; concomitant use with aliskiren in patients with diabetes mellitus
Warnings / Precautions Drug
 

Concerns related to adverse effects:

• Hyperkalemia: May occur; risk factors include renal dysfunction, diabetes mellitus, concomitant use of potassium-sparing diuretics, potassium supplements and/or potassium containing salts. Use cautiously, if at all, with these agents and monitor potassium closely.

• Hypotension: Symptomatic hypotension may occur upon initiation in patients who are salt- or volume-depleted (eg, those treated with high-dose diuretics); correct volume depletion prior to administration. This transient hypotensive response is not a contraindication to further treatment with telmisartan.

• Renal function deterioration: May be associated with deterioration of renal function and/or increases in serum creatinine, particularly in patients with low renal blood flow (eg, renal artery stenosis, heart failure) whose glomerular filtration rate (GFR) is dependent on efferent arteriolar vasoconstriction by angiotensin II; deterioration may result in oliguria, acute renal failure, and progressive azotemia. Small increases in serum creatinine may occur following initiation; consider discontinuation only in patients with progressive and/or significant deterioration in renal function.

Disease-related concerns:

• Aortic/mitral stenosis: Use with caution in patients with significant aortic/mitral stenosis.

• Hepatic impairment: Use with caution in patients who have biliary obstructive disorders or hepatic dysfunction.

• Renal artery stenosis: Use telmisartan with caution in patients with unstented unilateral/bilateral renal artery stenosis. When unstented bilateral renal artery stenosis is present, use is generally avoided due to the elevated risk of deterioration in renal function unless possible benefits outweigh risks.

• Renal impairment: Use with caution with pre-existing renal insufficiency and severe renal impairment.

Concurrent drug therapy issues:

• Angiotensin-converting enzyme (ACE) inhibitors and renin inhibitors: Concomitant use of an ACE-inhibitor or renin inhibitor (eg, aliskiren) is associated with an increased risk of hypotension, hyperkalemia, and renal dysfunction; concurrent use with ramipril is not recommended. Concomitant use with aliskiren should be avoided in patients with GFR <60 mL/minute and is contraindicated in patients with diabetes mellitus (regardless of GFR).

Interactions
 

ACE Inhibitors: Angiotensin II Receptor Blockers may enhance the adverse/toxic effect of ACE Inhibitors. Risk C: Monitor therapy

Alfuzosin: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy

Aliskiren: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Aliskiren may enhance the hypotensive effect of Angiotensin II Receptor Blockers. Aliskiren may enhance the nephrotoxic effect of Angiotensin II Receptor Blockers. Management: Avoid aliskiren use with ACEIs or ARBs in patients with diabetes or estimated glomerular filtration rate below 60 mL/min. In other patients receiving these combinations, monitor serum potassium, serum creatinine, and blood pressure periodically. Risk D: Consider therapy modification

Amifostine: Antihypertensives may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, antihypertensive medications should be withheld for 24 hours prior to amifostine administration. If antihypertensive therapy can not be withheld, amifostine should not be administered. Risk D: Consider therapy modification

Antihypertensives: May enhance the hypotensive effect of other Antihypertensives. Risk C: Monitor therapy

Canagliflozin: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Canagliflozin may enhance the hypotensive effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy

Cardiac Glycosides: Telmisartan may increase the serum concentration of Cardiac Glycosides. Risk C: Monitor therapy

CycloSPORINE (Systemic): Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of CycloSPORINE (Systemic). Risk C: Monitor therapy

Diazoxide: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy

Eplerenone: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy

Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy

Herbs (Hypotensive Properties): May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy

Hypotensive Agents: May enhance the adverse/toxic effect of other Hypotensive Agents. Risk C: Monitor therapy

Lithium: Angiotensin II Receptor Blockers may increase the serum concentration of Lithium. Management: Lithium dosage reductions will likely be needed following the addition of an angiotensin II receptor antagonist. Risk D: Consider therapy modification

MAO Inhibitors: May enhance the orthostatic hypotensive effect of Orthostatic Hypotension Producing Agents. Risk C: Monitor therapy

Methylphenidate: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: Angiotensin II Receptor Blockers may enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Angiotensin II Receptor Blockers. The combination of these two agents may also significantly decrease glomerular filtration and renal function. Risk C: Monitor therapy

Pentoxifylline: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy

Potassium Salts: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy

Potassium-Sparing Diuretics: Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C: Monitor therapy

Prostacyclin Analogues: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy

Ramipril: Telmisartan may increase the serum concentration of Ramipril. Concentrations of the active metabolite, ramiprilat, may also be increased. Risk C: Monitor therapy

Pregnancy
 
Pregnancy Risk Factor

D



Pregnancy Implications

[U.S. Boxed Warning]: Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected. The use of drugs which act on the renin-angiotensin system are associated with oligohydramnios. Oligohydramnios, due to decreased fetal renal function, may lead to fetal lung hypoplasia and skeletal malformations. Use is also associated with anuria, hypotension, renal failure, skull hypoplasia, and death in the fetus/neonate. The exposed fetus should be monitored for fetal growth, amniotic fluid volume, and organ formation. Infants exposed in utero should be monitored for hyperkalemia, hypotension, and oliguria.

Lactation
 

Excretion in breast milk unknown/not recommended

Monitoring Parameters
 
Blood pressure; electrolytes, serum creatinine, BUN
Mechanism of Action
 
Angiotensin II acts as a vasoconstrictor. In addition to causing direct vasoconstriction, angiotensin II also stimulates the release of aldosterone. Once aldosterone is released, sodium as well as water are reabsorbed. The end result is an elevation in blood pressure. Telmisartan is a nonpeptide AT1 angiotensin II receptor antagonist. This binding prevents angiotensin II from binding to the receptor thereby blocking the vasoconstriction and the aldosterone secreting effects of angiotensin II.
Pharmacodynamics / Kinetics
 

Onset of action: 1-2 hours

Duration: Up to 24 hours

Distribution: V d : 500 L

Protein binding: >99.5%; primarily to albumin and alpha 1 -acid glycoprotein

Metabolism: Hepatic 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: 0.5-1 hours

Excretion: Feces (97%)

Clearance: Total body: 800 mL/minute

 
   
 
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