Telmisartan + Amlodipine


Concise Prescribing Info
Indications/Uses
HTN.
Dosage/Direction for Use
Adult : PO Each tab contains telmisartan (mg)/amlodipine (mg): 40/5, 40/10, 80/5, and 80/10: 1 tab once daily. Dosage is individualised and may be increased after at least 2 wk. Max: Telmisartan 80 mg and amlodipine 10 mg once daily.
Dosage Details
Oral
Hypertension
Adult: Available preparations:
Telmisartan 40 mg and amlodipine 5 mg
Telmisartan 40 mg and amlodipine 10 mg
Telmisartan 80 mg and amlodipine 5 mg
Telmisartan 80 mg and amlodipine 10 mg
1 tablet once daily. Dosage is individualised and may be increased after at least 2 wk. Max: Telmisartan 80 mg and amlodipine 10 mg once daily.
Hepatic Impairment
Mild to moderate: Max: 40 mg of telmisartan component. Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Biliary obstructive disorders, cardiogenic shock. Severe hepatic impairment. Pregnancy and lactation. Concomitant use w/ ACE inhibitors or aliskiren-containing products in patients w/ DM or renal impairment (GFR <60 mL/min).
Special Precautions
Patient w/ Na- or volume-depletion, idiopathic or hereditary angioedema, primary hyperaldosteronism, severe obstructive coronary artery disease, heart failure, recent MI, mitral or aortic stenosis, hypertrophic cardiomyopathy w/ outflow tract obstruction, DM. Patient undergoing surgery or dialysis. Renal (e.g. unilateral/bilateral renal artery stenosis) and mild to moderate hepatic impairment.
Adverse Reactions
Significant: Hypotension, angina, acute renal failure, hyperkalaemia, peripheral oedema. Rarely, angioedema.
Nervous: Dizziness, somnolence, migraine, fatigue, flu-like symptoms, headache, malaise, insomnia, vertigo, paraesthesia, hypoaesthesia, anxiety, depression, tremor, peripheral neuropathy.
CV: Orthostatic hypotension, oedema, syncope, chest pain, flushing, bradycardia, palpitation.
GI: Diarrhoea, nausea, dyspepsia, abdominal pain, constipation, gastritis, vomiting, dry mouth, hemorrhoids, gastroenteritis, gastroesophageal reflux, dysgeusia.
Resp: Sinusitis, pharyngitis, cough.
Hepatic: Increased hepatic enzymes.
Genitourinary: UTI, cystitis, micturition frequency, nocturia.
Endocrine: Impotence, hypercholesterolaemia, erectile dysfunction.
Musculoskeletal: Back pain, myalgia, arthralgia, muscle spasm, gout.
Ophthalmologic: Abnormal vision, conjunctivitis.
Otic: Tinnitus, earache.
Dermatologic: Hyperhidrosis, dermatitis, rash, eczema, pruritus.
Others: Pain.
Patient Counseling Information
This drug may cause syncope, somnolence, dizziness, or vertigo, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor electrolyte panels at baseline and periodically, urinalysis, BP, heart rate, liver and renal (e.g. serum creatinine, BUN, urinalysis) functions. Monitor for signs and symptoms for peripheral oedema, symptomatic hypotension.
Drug Interactions
Increased hypotensive effects w/ other antihypertensive agents and agents w/ BP lowering potential (e.g. baclofen, amifostine). Orthostatic hypotension may be aggravated by barbiturates, narcotics, or TCAs. Reduced therapeutic effect w/ corticosteroids.
Telmisartan: Reduced antihypertensive effect and risk of acute renal insufficiency w/ NSAIDs. May cause reversible increase in serum lithium concentration and toxicity. Increased risk of hyperkalaemia w/ K-sparing diuretics, K supplements or K-containing salt substitutes. 
Amlodipine: Increased exposure CYP3A4 enzyme inhibitors (e.g. protease inhibitors, azole antifungals, erythromycin, diltiazem). Decreased plasma concentration w/ CYP3A4 enzyme inducers (e.g. rifampicin). May increase systemic exposure of ciclosporin or tacrolimus.
Potentially Fatal: Dual blockade of the renin-angiotensin-aldosterone system (RAAS) by concomitant use w/ ACE inhibitors (e.g. ramipril) or aliskiren may cause an increased risk of hypotension, hyperkalaemia, and acute renal failure (esp in patients w/ DM or renal impairment).
Food Interaction
Food may decrease rate and extent of absorption. Alcohol may aggravate orthostatic hypotension.
Amlodipine: Increased BP-lowering effects w/ grapefruit or grapefruit juice. Decreased plasma concentration w/ St. John’s wort.
Action
Description: Telmisartan, a nonpeptide tetrazole derivative, is an angiotensin II type 1 (AT1) receptor antagonist producing its BP lowering effects by selectively blocking the binding of angiotensin II to angiotensin type 1 (AT1) receptors, thereby reducing angiotensin II-induced vasoconstriction, aldosterone release, and Na reabsorption.
Amlodipine, a dihydropyridine Ca channel blocker, reduces peripheral vascular resistance and BP by producing a relaxation of vascular smooth muscle and coronary vasodilation through inhibition of Ca ion transmembrane influx into cardiac and vascular smooth muscles.
Pharmacokinetics:
Absorption: Telmisartan: Rapidly absorbed from the GI tract. Absolute bioavailability: Dose dependent: 42% after 40 mg dose; 58% after 160 mg dose. Time to peak plasma concentration: Approx 0.5-1 hr.
Amlodipine: Well absorbed. Bioavailability: 60-65%. Time to peak plasma concentration: 6-12 hr.
Distribution: Telmisartan: Plasma protein binding: >99.5%, mainly albumin and α1 acid-glycoprotein.
Amlodipine: Volume of distribution: Approx 21 L/kg. Plasma protein binding: Approx 98%.
Metabolism: Telmisartan: Undergoes first-pass metabolism via conjugation to acylglucuronide.
Amlodipine: Extensively metabolised in the liver to inactive metabolites.
Excretion: Telmisartan: Mainly via faeces, as unchanged drug; urine (<1%). Terminal elimination half-life: Approx 24 hr.
Amlodipine: Via urine (<10% as unchanged drug, 60% as metabolites). Terminal elimination half-life: 30-50 hr.
Chemical Structure

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Click on icon to see table/diagram/image
Storage
Store at 25°C. Protect from moisture and light.
ATC Classification
C09DB04 - telmisartan and amlodipine ; Belongs to the class of angiotensin II receptor blockers (ARBs) and calcium channel blockers. Used in the treatment of cardiovascular disease.
Disclaimer: This information is independently developed by MIMS based on Telmisartan + Amlodipine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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