No

Angiotensin II Antagonists

Treatment of hypertension; may be used alone or in combination with other antihypertensive agents

C (1st trimester); D (2nd & 3rd trimester)

Avoid use in the nursing mother, if possible, since telmisartan may be excreted in breast milk. The drug should be discontinued as soon as possible when pregnancy is detected. Drugs which act directly on renin-angiotensin can cause fetal and neonatal morbidity and death.

Hypersensitivity to telmisartan or any component; hypersensitivity to other A-II receptor antagonists; primary hyperaldosteronism; bilateral renal artery stenosis; pregnancy (2nd and 3rd trimesters)

Avoid use or use a smaller dose in patients who are volume depleted; correct depletion first. Deterioration in renal function can occur with initiation. Use with caution in unilateral renal artery stenosis and pre-existing renal insufficiency; significant aortic/mitral stenosis. Use with caution in patients who have biliary obstructive disorders or hepatic dysfunction.

May be associated with worsening of renal function in patients dependent on renin-angiotensin-aldosterone system.

Cardiovascular: Hypertension (1%), chest pain (1%), peripheral edema (1%)

Central nervous system: Headache (1%), dizziness (1%), pain (1%), fatigue (1%)

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

Genitourinary: Urinary tract infection (1%)

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

Respiratory: Upper respiratory infection (7%), sinusitis (3%), pharyngitis (1%), cough (1.6%)

Miscellaneous: Flu-like syndrome (1%)

<1% (Limited to important or life-threatening symptoms): Angioedema, allergic reaction, elevated liver enzymes, decrease in hemoglobin, increased serum creatinine and BUN, impotence, sweating, flushing, fever, malaise, palpitations, angina, tachycardia, abnormal EKG, insomnia, anxiety, nervousness, migraine, vertigo, depression, somnolence, paresthesia, involuntary muscle contractions, constipation, flatulence, dry mouth, hemorrhoids, gastroenteritis, enteritis, reflux, toothache, gout, hypercholesterolemia, diabetes mellitus, arthritis, arthralgia, leg cramps, fungal infection, abscess, otitis media, asthma, dyspnea, bronchitis, rhinitis, epistaxis, dermatitis, eczema, pruritus, rash, frequent urination, cystitis, abnormal vision, conjunctivitis, tinnitus, earache, cerebrovascular disorder

Signs and symptoms of overdose include hypotension, dizziness and tachycardia; treatment is supportive; vagal stimulation may result in bradycardia

Digoxin levels may be increased.

Lithium: Risk of toxicity may be increased by telmisartan; monitor lithium levels.

Potassium-sparing diuretics (amiloride, potassium, spironolactone, triamterene): Increased risk of hyperkalemia.

Potassium supplements may increase the risk of hyperkalemia.

Trimethoprim (high dose) may increase the risk of hyperkalemia.

Warfarin serum concentrations may be decreased (not associated with alteration in INR); monitor INR closely.

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.

Telmisartan does not require prodrug conversion prior to drug action

Time to peak: 0.5-1 hours

Duration: Up to 24 hours

Protein binding: >99.5%

Metabolism: Hepatic, via conjugation to inactive metabolites

Bioavailability: 42% to 58% (dose-dependent)

Half-life, terminal: 24 hours

Elimination: Total body clearance: 800 mL/minute; 97% of a dose is excreted in the feces via extensive biliary secretion

Adults: 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.

May be administered without regard to food

Supine blood pressure, electrolytes, serum creatinine, BUN, urinalysis, symptomatic hypotension, and tachycardia

The angiotensin II receptor antagonists appear to have similar indications as the ACE inhibitors. While these drugs have been shown to be effective in treating hypertension, their efficacy in heart failure is being vigorously evaluated. The angiotensin II antagonists are especially useful in providing an alternative therapy in those patients who have intractable cough in response to ACE-inhibitor therapy. Similar to ACE inhibitors, pre-existing volume depletion caused by diuretic therapy may potentiate hypotension in response to angiotensin II antagonists.

May cause dizziness or fatigue, may rarely cause insomnia, anxiety, nervousness, depression, or sedation

None noted

No information available to require special precautions

No effects or complications reported

Take exactly as directed. Do not miss doses, alter dosage, or discontinue without consulting prescriber. Do not alter salt or potassium intake without consulting prescriber. Monitor blood pressure on a regular basis as recommended by prescriber; at the same time each day. You may experience postural hypotension (change position slowly when rising from sitting or lying, when climbing stairs, or bending over); or transient nervousness, headache, or dizziness (use caution when driving or engaging in tasks requiring alertness until response to drug is known). Report unusual weight gain or swelling of ankles and hands; swelling of face, lips, throat, or tongue; persistent fatigue; dry cough or difficulty breathing; palpitations or chest pain; CNS changes; gastrointestinal disturbances; muscle or bone pain, cramping, or tremors; change in urinary pattern; or changes in hearing or vision. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Tablet: 40 mg, 80 mg