Pacific Pharma (Korea)


AA Medical
Full Prescribing Info
Each Pacsartan-T tablet contains telmisartan 40 mg and 80 mg, respectively. Telmisartan is chemically 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-bipenyl]-2-carboxylic acid. Its empirical formula is C33H30N4O2 and the molecular weight is 514.63.
Pharmacotherapeutic Group: Nonpeptide angiotensin II receptor (type AT1) antagonist.
Pharmacology: Pharmacodynamics: Mechanism of Action: Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium. 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 eg, vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis.
There is also an AT2-receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Telmisartan has much greater affinity (>3000-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. Angiotensin-converting enzyme inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because telmisartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Telmisartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of telmisartan on blood pressure.
Pharmacokinetics: General: Following oral administration, peak plasma concentrations (Cmax) of telmisartan are reached in 0.5-1 hr after dosing. Food slightly reduces the bioavailability of telmisartan, with a reduction in the area under the plasma concentration-time curve (AUC) of about 6% with the tablet 40 mg and about 20% after a 160 mg dose. The absolute bioavailability of telmisartan is dose-dependent. At 40 and 160 mg, the bioavailability was 42% and 58%, respectively. The pharmacokinetics of orally-administered telmisartan are nonlinear over the dose range 20-160 mg, with greater than proportional increases of plasma concentrations (Cmax and AUC) with increasing doses. Telmisartan shows bi-exponential decay kinetics with a terminal elimination half-life (t½) of approximately 24 hrs. Trough plasma concentrations of telmisartan with once daily dosing are about 10-25% of Cmax. Telmisartan has an accumulation index in plasma of 1.5-2 upon repeated once daily dosing.
Metabolism and Elimination: Following either IV or oral administration or 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).
In addition to the adverse reactions, the following reactions also occurred at a rate of 1% but at least as frequent in the placebo group: Influenza-like symptoms, dyspepsia, myalgia, urinary tract infection, abdominal pain, headache, dizziness, pain, fatigue, coughing, hypertension, chest pain, nausea and peripheral edema.
Discontinuation of therapy due to adverse reactions was required in 2.8% of 1455 patients treated with Telmimark tablets and 6.1% of 380 placebo patients in placebo-controlled clinical trials.
The incidence of adverse reactions were not dose-related and did not correlate with gender, age or race of patients.
The incidence of cough occurring with telmisartan in 6 placebo-controlled trials was identical to that noted for placebo-treated patients (1.6%).
Hypertension: Indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacological classes including the class to which Pacsartan-T principally belongs.
Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise and limited sodium intake. Many patients will require >1 drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines eg, those of the National High Blood Pressure Education Program's Joint National Committee on Prevention, Detection, Evaluation and Treatment of High Blood Pressure (JNC).
Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.
Elevated systolic or diastolic pressure causes increased cardiovascular risk and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (ie, patients with diabetes or hyperlipidemia) and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.
Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients and many antihypertensive drugs have additional approved indications and effects (eg, on angina, heart failure or diabetic kidney disease). These considerations may guide selection of therapy.
It may be used alone or in combination with other antihypertensive agents.
Cardiovascular Risk Reduction: For reduction of the risk of myocardial infarction, stroke or death from cardiovascular causes in patients ≥55 years at high risk of developing major cardiovascular events who are unable to take ACE inhibitors.
High risk for cardiovascular events can be evidenced by a history of coronary artery disease, peripheral arterial disease, stroke, transient ischemic attack or high-risk diabetes (insulin dependent or non-insulin dependent) with evidence of end-organ damage. Pacsartan-T can be used in addition to other needed treatment (eg, antihypertensive, antiplatelet or lipid-lowering therapy).
Studies of telmisartan in this setting do not exclude the possibility that telmisartan may not preserve a meaningful fraction of the effect of the angiotensin converting enzyme (ACE) inhibitor to which it was compared. Consider using the ACE inhibitor 1st, and if it is stopped for cough only, consider re-trying the ACE inhibitor after the cough resolves.
Dosage/Direction for Use
Hypertension: Dosage must be individualized. Usual Starting Dose: 40 mg once daily. Blood pressure response is dose-related over the range of 20-80 mg. Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. When additional blood pressure reduction beyond that achieved with Pacsartan-T 80 mg is required, a diuretic may be added.
Pacsartan-T may be administered with other antihypertensive agents.
Cardiovascular Risk Reduction: Recommended Dose: 80 mg once daily. It is not known whether doses telmisartan <80 mg are effective in reducing the risk of cardiovascular morbidity and mortality.
When initiating Pacsartan-T therapy for cardiovascular risk reduction, monitoring of blood pressure is recommended, and if appropriate, adjustment of medications that lower blood pressure may be necessary.
Special Populations: Elderly: Renal Impairment: No initial dosage adjustment is necessary for elderly patients or patients with renal impairment, including those on hemodialysis.
Administration: May be administered with or without food.
Symptoms: Limited data are available with regard to overdosage in humans. The most likely manifestation of overdosage with Pacsartan-T would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.
Treatment: If symptomatic hypotension should occur, supportive treatment should be instituted. Telmisartan is not removed by hemodialysis.
Special Precautions
Patients on Dialysis: May develop orthostatic hypotension; their blood pressure should be closely monitored.
Store below 30°C in dry place. Protect from light.
Shelf-Life: 36 months.
ATC Classification
C09CA07 - telmisartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Tab 20 mg x 3 x 10's. 40 mg x 3 x 10's. 80 mg x 3 x 10's.
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