Description:
MYCARDIX (telmisartan) is a nonpeptide angiotensin II receptor (type AT1) antagonist. Telmisartan is chemically described as 4'-[(1, 4’-dimethyl-2'-propyl [2,6'-bi-1H-benzimidazol]-1'- yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid. Its empirical formula is C33 H30 N4 O2, its molecular weight is 514.63.

Composition:
Each 20, 40 & 80mg film coated tablet contains:
Telmisartan………20, 40 & 80mg respectively.

Pharmacological Action:
Pharmacodynamic Properties
MYCARDIX (telmisartan) blocks the vasoconstrictor and aldosterone secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis. MYCARDIX (telmisartan) has much greater affinity (>3,000 fold) for the AT1 receptor than for the AT2 receptor. Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on rennin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of telmisartan on blood pressure.

Pharmacokinetic Properties:
Absorption
Following oral administration, peak concentrations (Cmax) of telmisartan are reached in 0.5-1 hour after dosing. Food slightly reduces the bioavailability of MYCARDIX (telmisartan)
Distribution:
MYCARDIX (telmisartan) is highly bound to plasma proteins (>99.5%), mainly albumin and •1 - acid glycoprotein. Plasma protein binding is constant over the concentration range achieved with recommended doses. The volume of distribution for telmisartan is approximately 500 liters indicating additional tissue binding.
Metabolism:
MYCARDIX (telmisartan) is metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. After a single dose, the glucuronide represents approximately 11% of the measured radioactivity in plasma. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan. Total plasma clearance of telmisartan is > 800 mL/min.
Elimination:
Following oral administration of MYCARDIX (telmisartan), most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine.

Indications & Usage:
MYCARDIX (telmisartan) is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Dosage & administration:
Dosage must be individualized. The usual starting dose of MYCARDIX (telmisartan) tablets is 40 mg once a day. Blood pressure response is dose related over the range of 20-80 mg.

Contraindications:
MYCARDIX (telmisartan) is contraindicated in patients who are hypersensitive to any component of this product.

Adverse Effects:
Adverse experiences have generally been mild and transient in nature and have only infrequently required discontinuation of therapy. The incidence of adverse events was not dose-related and did not correlate with gender, age, or race of patients.
Autonomic Nervous System: impotence increased sweating, flushing
Body as a Whole: allergy, fever, leg pain, malaise
Cardiovascular: palpitation, dependent edema, angina pectoris, tachycardia, leg edema, abnormal ECG.
CNS: insomnia, somnolence, migraine, vertigo, paresthesia, involuntary muscle contractions, hypoaesthesia
Gastrointestinal: flatulence, constipation, gastritis, vomiting, dry mouth, hemorrhoids, gastroenteritis, enteritis, gastroesophageal reflux, toothache, non-specific 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; and
Special Senses: abnormal vision, conjunctivitis, tinnitus, earache.

Warning & Precautions:
Pregnancy
Pregnancy Categories C (First trimester) and D (Second & third trimester)
Since there are no adequate or well-controlled studies in pregnant women, MYCARDIX (telmisartan) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers:
It is not known whether MYCARDIX (telmisartan) is excreted in human milk, because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Impaired Hepatic Function: As the majority of MYCARDIX (telmisartan) is eliminated by biliary excretion, patients with biliary obstructive disorders or hepatic insufficiency can be expected to have reduced clearance. Telmisartan tablets should be used with caution in these patients.

Impaired Renal Function: As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function may be anticipated in susceptible individuals. In patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure), treatment with angiotensin-converting enzyme inhibitors and angiotensin receptor antagonists has been associated with oliguria and/or progressive azotemia and (rarely) with acute renal failure and/or death. Similar results may be anticipated in patients treated with tablets.

Drug Interactions:
Digoxin: It is recommended that digoxin levels be monitored when initiating, adjusting, and discontinuing MYCARDIX (telmisartan) to avoid possible over- or under-digitalization.
Warfarin: Telmisartan administered for 10 days slightly decreased the mean warfarin trough plasma concentration, this decrease did not result in a change in International Normalized Ratio (INR).
Other Drugs: Co-administration of MYCARDIX (telmisartan) did not result in a clinically significant interaction with acetaminophen, amlodipine, glibenclamide, simvastatin, hydrochlorothiazide or ibuprofen. Telmisartan is not metabolized by the cytochrome P450 system and had no effects in vitro on cytochrome P450 enzymes, except for some inhibition of CYP2C19. MYCARDIX (telmisartan) is not expected to interact with drugs that inhibit cytochrome P450 enzymes; it is also not expected to interact with drugs metabolized by cytochrome P450 enzymes, except for possible inhibition of the metabolism of drugs metabolized by CYP2C19.

Over dosage:
Limited data are available with regard to over dosage in humans. The most likely manifestation of over dosage with MYCARDIX (telmisartan) tablets would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Telmisartan is not removed by hemodialysis.

Storage:
Store below 30ºC
Protect from light, heat and moisture.
Keep all medicines out of the reach of the children.