Adult: Available preparations:
Telmisartan 40 mg and amlodipine 5 mg tab
Telmisartan 40 mg and amlodipine 10 mg tab
Telmisartan 80 mg and amlodipine 5 mg tab
Telmisartan 80 mg and amlodipine 10 mg tab
As monotherapy or in combination with other antihypertensives: Initially, 40 mg/5 mg once daily; may be increased after at least 2 weeks of therapy. In patients requiring larger blood pressure reductions, an initial dose of 80 mg/5 mg once daily may be given. Max: 80 mg/10 mg once daily. Dosage is individualised and adjusted according to patient's clinical response. Elderly: ≥75 years Not recommended for initial therapy.
Not recommended for initial therapy. Mild to moderate: Max: 40 mg telmisartan once daily. Severe: Contraindicated.
May be taken with or without food.
Biliary obstructive disorders, severe hypotension, shock (including cardiogenic shock), obstruction of the outflow tract of the left ventricle (e.g. high-grade aortic stenosis), haemodynamically unstable heart failure after acute MI. Severe hepatic impairment. Pregnancy and lactation. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2).
Patient with predisposing factors for hyperkalaemia (e.g. dehydration, acute cardiac decompensation, metabolic acidosis, cellular lysis, concomitant use of drugs affecting the renin-angiotensin-aldosterone system and/or K supplements); volume and/or Na depletion (e.g. undergoing vigorous diuretic therapy, dietary salt restriction, diarrhoea, vomiting); unstented unilateral or bilateral renal artery stenosis, heart failure or CHF, primary aldosteronism, significant aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy, unstable angina pectoris, current or recent MI (within 1 month), idiopathic or hereditary angioedema or previous angioedema associated with ACE inhibitor therapy, ischaemic heart disease, diabetes mellitus. Patient undergoing surgery. Avoid use in patients with ascites due to cirrhosis or refractory ascites. Renal and mild to moderate hepatic impairment. Elderly.
Significant: Hyperkalaemia, hypotension or orthostatic hypotension, worsening angina and/or MI, peripheral oedema, deterioration of renal function, increased serum creatinine. Rarely, angioedema. Cardiac disorders: Bradycardia, palpitations. Ear and labyrinth disorders: Vertigo. Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea. General disorders and administration site conditions: Asthenia, chest pain, fatigue. Investigations: Increased hepatic enzymes. Musculoskeletal and connective tissue disorders: Arthralgia, back pain, muscle spasms, myalgia. Nervous system disorders: Dizziness, headache, somnolence, migraine, paraesthesia. Psychiatric disorders: Rarely, depression, anxiety, insomnia. Renal and urinary disorders: Rarely, cystitis, nocturia. Reproductive system and breast disorders: Erectile dysfunction. Respiratory, thoracic and mediastinal disorders: Cough. Skin and subcutaneous tissue disorders: Pruritus. Vascular disorders: Flushing.
Obtain baseline and periodic electrolyte panels (particularly serum K). Monitor renal function (serum creatinine, BUN, urinalysis), hepatic function, heart rate, blood pressure; signs of symptomatic hypotension and peripheral oedema.
Symptoms: Telmisartan: Hypotension, dizziness, tachycardia, bradycardia. Amlodipine: Excessive peripheral vasodilation, reflex tachycardia, marked and possibly prolonged systemic hypotension (including shock). Management: Symptomatic and supportive treatment. Induce emesis and/or perform gastric lavage; may give activated charcoal. Monitor serum electrolytes and creatinine frequently. In case of hypotension, place the patient in a supine position with elevation of extremities, salt and volume replacement must be given quickly. May give IV Ca gluconate to reverse the effects of Ca channel blockade.
Increased hypotensive effects with other antihypertensives or drugs with blood pressure-lowering effect (e.g. baclofen, amifostine). May aggravate orthostatic hypotension with barbiturates, narcotics, and antidepressants. Decreased antihypertensive effect with corticosteroids.
Telmisartan: Increased risk of hyperkalaemia with drugs affecting the renin-angiotensin-aldosterone system; K supplements, K-containing salts, K-sparing diuretics, or other agents that may increase K level (e.g. heparin, trimethoprim). May increase the serum concentrations of lithium and digoxin. Concomitant use with NSAIDs may reduce the effect of telmisartan and increase the risk of acute renal insufficiency.
Amlodipine: Increased exposure and risk of hypotension with strong or moderate CYP3A4 inhibitors (e.g. protease inhibitors, azole antifungals, macrolides, verapamil, diltiazem). May decrease serum concentration with strong CYP3A4 inducers (e.g. rifampicin). May increase the exposure of tacrolimus, ciclosporin, mTOR inhibitors (e.g. sirolimus, temsirolimus, everolimus), and simvastatin. Potentially Fatal: Dual blockade of the renin-angiotensin-aldosterone system by concurrent use of telmisartan and aliskiren may increase the risks of hypotension, hyperkalaemia, and changes in renal function, including acute renal failure.
Alcohol may aggravate orthostatic hypotension.
Amlodipine: May increase blood pressure-lowering effects with grapefruit or grapefruit juice. May decrease serum concentration with St. John's wort.
Description: Telmisartan, a nonpeptide angiotensin II type 1 (AT1) receptor antagonist, produces its blood pressure-lowering effects by selectively blocking the binding of angiotensin II to AT1 receptor, thereby reducing angiotensin II-induced vasoconstriction, aldosterone release, and Na reabsorption.
Amlodipine, a dihydropyridine Ca channel blocker, reduces peripheral vascular resistance and blood pressure by producing relaxation of vascular smooth muscle and coronary vasodilation through inhibition of Ca ion transmembrane influx into vascular smooth muscle and cardiac muscle. Pharmacokinetics: Absorption: Telmisartan: Rapidly absorbed from the gastrointestinal tract. Absolute bioavailability: 42-58% (dose-dependent). Time to peak plasma concentration: 0.5-1 hour.
Amlodipine: Well absorbed. Bioavailability: 64-90%. Time to peak plasma concentration: 6-12 hours. Distribution: Telmisartan: Volume of distribution: Approx 500 L. Plasma protein binding: >99.5%, mainly to albumin and α1-acid glycoprotein.
Amlodipine: Crosses the placenta and enters breast milk. Volume of distribution: 21 L/kg. Plasma protein binding: Approx 98%. Metabolism: Telmisartan: Metabolised in the liver via conjugation into inactive metabolites.
Amlodipine: Extensively metabolised in the liver. Excretion: Telmisartan: Mainly via faeces (primarily as unchanged drug). Terminal elimination half-life: Approx 24 hours.
Amlodipine: Via urine (10% as unchanged drug, 60% as metabolites). Terminal elimination half-life: 30-50 hours.
Store between 15-30°C. Protect from light and moisture.