telmisartan (Rx)

1-10%

Upper respiratory tract infection (7%)

Back pain (3%)

Sinusitis (3%)

Diarrhea (3%)

Cough (1.6%)

Influenza-like symptoms (≥1%)

Dyspepsia (≥1%)

Myalgia (≥1%)

Urinary tract infection (≥1%)

Abdominal pain ≥1%)

Headache (≥1%)

Dizziness (≥1%)

Pain (≥1%)

Fatigue (≥1%)

Coughing (≥1%)

Hypertension (≥1%)

Chest pain (≥1%)

Nausea (≥1%)

Peripheral edema (≥1%)

Pharyngitis (1%)

Frequency Not Defined

Autonomic nervous system: Impotence, increased sweating, flushing

Body as a whole: Allergy, fever, leg pain, malaise

Cardiovascular: Palpitations, dependent edema, angina pectoris, tachycardia, leg edema, abnormal ECG

Central nervous system: Insomnia, somnolence, migraine, vertigo, paresthesia, involuntary muscle contractions, hypoesthesia

Gastrointestinal: Flatulence, constipation, gastritis, vomiting, dry mouth, hemorrhoids, gastroenteritis, enteritis, gastroesophageal reflux, toothache, nonspecific gastrointestinal disorders

Metabolic: Gout, hypercholesterolemia, diabetes mellitus

Musculoskeletal: Arthritis, arthralgia, leg cramps

Psychiatric: Anxiety, depression, nervousness

Resistance mechanism: Infection, fungal infection, abscess, otitis media

Respiratory: Asthma, bronchitis, rhinitis, dyspnea, epistaxis

Skin: Dermatitis, rash, eczema, pruritus; Urinary: micturition frequency, cystitis;

Vascular: Cerebrovascular disorder

Special senses: Abnormal vision, conjunctivitis, tinnitus, earache

Postmarketing Reports

Most frequent spontaneously reported events include: headache, dizziness, asthenia, coughing, nausea, fatigue, weakness, edema, face edema, lower limb edema, angioneurotic edema, urticaria, hypersensitivity, sweating increased, erythema, chest pain, atrial fibrillation, congestive heart failure, myocardial infarction, blood pressure increased, hypertension aggravated, hypotension (including postural hypotension), hyperkalemia, syncope, dyspepsia, diarrhea, pain, urinary tract infection, erectile dysfunction, back pain, abdominal pain, muscle cramps (including leg cramps), myalgia, bradycardia, eosinophilia, thrombocytopenia, uric acid increased, abnormal hepatic function/liver disorder, renal impairment including acute renal failure, anemia, increased CPK, anaphylactic reaction, tendon pain (including tendonitis, tenosynovitis), drug eruption (toxic skin eruption mostly reported as toxicoderma, rash, and urticaria), hypoglycemia (in diabetic patients), and angioedema (with fatal outcome)

Rare cases of rhabdomyolysis have been reported

Contraindications

Hypersensitivity to telmisartan or any other component of this product

Coadministration with aliskiren in patients with diabetes

Cautions

Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death

Hyperkalemia may occur in patients on ARBs, particularly in patients with advanced renal impairment, heart failure, on renal replacement therapy, or on potassium supplements, potassium-sparing diuretics, potassium-containing salt substitutes or other drugs that increase potassium level

As the majority of telmisartan is eliminated by biliary excretion, patients with biliary obstructive disorders or hepatic insufficiency can be expected to have reduce clearance

Pregnancy (2nd and 3rd trimesters); significant risk of fetal or neonatal morbidity and mortality (see Black Box Warnings)

Dual blockade of the renin-angiotensin system with angiotensin-receptor blockers (ARBs), angiotensin-converting enzyme (ACE) inhibitors, or aliskiren is associated with increased risk of hypotension, hyperkalemia, and altered renal function (including acute renal failure) in comparison with monotherapy

Most patients receiving the combination of two RAS inhibitors do not obtain any additional benefit compared to monotherapy; avoid combined use of RAS inhibitors; closely monitor blood pressure, renal function and electrolytes in patients on benazepril and other agents that affect the RAS

Drug interaction overview

• Not for coadministration with aliskiren in patients with diabetes; avoid use of aliskiren with telmisartan in patients with renal impairment (GFR <60 ml/min/1.73 m²)
• When coadministered with digoxin, median increases in digoxin peak plasma concentration (49%) and in trough concentration (20%) were observed; monitor digoxin levels when initiating, adjusting, and discontinuing telmisartan

Pregnancy

May cause fetal harm when administered to a pregnant woman

Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death

Most epidemiologic studies examining fetal abnormalities after exposure to antihypertensive use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other antihypertensive agents

When pregnancy is detected, discontinue as soon as possible

Animal data

• Studies in rats and rabbits with telmisartan showed fetotoxicity only at maternally toxic doses

Clinical considerations

• Disease-associated maternal and/or embryo/fetal risk

  • Hypertension in pregnancy increases the maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (eg, need for cesarean section, postpartum hemorrhage)
  • Hypertension increases the fetal risk for intrauterine growth restriction and intrauterine death
  • Carefully monitor pregnant women with hypertension and managed accordingly

• Fetal/neonatal adverse reactions

  • Use of drugs that act on the RAS in the second and third trimesters of pregnancy can result in the following: oligohydramnios, reduced fetal renal function leading to anuria and renal failure, fetal lung hypoplasia, skeletal deformations, including skull hypoplasia, hypotension, and death
  • During pregnancy, perform serial ultrasound examinations to assess the intra-amniotic environment
  • Fetal testing may be appropriate, based on the week of gestation
  • If oligohydramnios is observed, discontinue telmisartan, unless it is considered lifesaving for the mother
  • Note: Oligohydramnios may not appear until after the fetus has sustained irreversible injury
  • Closely observe infants with histories of in utero exposure to telmisartan for hypotension, oliguria, and hyperkalemia
  • If oliguria or hypotension occurs, support blood pressure and renal perfusion
  • May require transfusions or dialysis as a means of reversing hypotension and/or substituting for disordered renal function

Lactation

There is no information regarding the presence of telmisartan in human milk, the effects on the breastfed infant, or the effects on milk production

Present in the milk of lactating rats

Advise a nursing woman not to breastfeed during treatment

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Angiotensin II receptor blocker; inhibits vasoconstrictor and aldosterone-secreting effects of angiotensin II

Absorption

Onset: 1-2 hr

Duration: <24 hr

Peak plasma time: 0.5-1 hr

Distribution

Protein bound: >99.5%

Vd: 500 L

Metabolism

Metabolized in liver to inactive metabolite

Elimination

Half-life: 24 hr

Dialyzable: No (HD)

Excretion: Feces (>97%), urine (small amount)

Oral Administration

Take with or without food

Storage

Store at 25ºC (77ºF); excursions permitted to 15-30ºC (59-86ºF)

Tablets should not be removed from blisters until immediately before administration