Drug information of Amlodipine

Mechanism of effect

Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle

Pharmacodynamic

Amlodipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs)

Pharmacokinetics

After oral administration of therapeutic doses of Amlodipine besylate, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability has been estimated to be between 64 and 90%. The bioavailability of Amlodipine besylate is not altered by the presence of food. Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine.

Drug indications

Angina Pectoris , (hypertension (high blood pressure , Coronary Artery Disease (CAD

Dosage

Usual Adult Dose for Hypertension Initial dose: 5 mg orally once a day Maintenance dose: 5 to 10 mg orally once a day Small or fragile patients may be started on 2.5 mg orally once a day. Usual Adult Dose for Coronary Artery Disease Chronic stable or vasospastic angina, or angiographically documented coronary artery disease in patients without heart failure or an ejection fraction less than 40%: 5 to 10 mg orally once a day Usual Adult Dose for Angina Pectoris Chronic stable or vasospastic angina, or angiographically documented coronary artery disease in patients without heart failure or an ejection fraction less than 40%: 5 to 10 mg orally once a day Usual Pediatric Dose for Hypertension 6 to 17 years: 2.5 mg to 5 mg orally once a day Doses in excess of 5 mg daily have not been studied in pediatric patients.

Drug contraindications

hypersensitivity to drug or its components.

Side effects

nausea , abdominal pain , dizziness , fatigue , flushing , palpitations , edema , somnolence

Interactions

Atenolol , Aripiprazole , Aprepitant , Bosentan , Erythromycin , isosorbide dinitrate , Isoxsuprine , Tadalafil , Simvastatin , Yohimbine , Phentolamine Mesylate , Rivaroxaban , Bisoprolol , cefepime , Doxazosin , Dolasetron , Indinavir , Tocilizumab , Telmisartan , Bendroflumethiazide , Treprostinil , Lorlatinib , Nitrendipine , tropisetron , lasmiditan

Alerts

1- Worsening angina and acute myocardial infarction can develop after initiating or increasing the dosage of amlodipine, especially in patients with severe obstructive coronary artery disease. 2- Caution is recommended in patients with aortic stenosis, heart failure, and/or hepatic dysfunction. 3- Monitoring for symptoms of hypotension and edema is recommended when amlodipine is coadministered with CYP450 3A4 inhibitors. Blood pressure should be closely monitored when amlodipine is coadministered with CYP450 3A4 inducers. 4- Safety and effectiveness have not been established in pediatric patients less than 6 years of age.

Points of recommendation

1- Amlodipine may be administered with or without food. 2- Tell your doctor about any prescription and non-prescription medicines you are taking, including natural or herbal remedies. 3- It may be easier to take your dose if you do it at the same time every day, such as with breakfast or dinner, or at bedtime. Do not take more than one dose of Amlodipine besylate tablets at a time. 4- If you miss a dose, take it as soon as you remember. Do not take Amlodipine besylate tablets if it has been more than 12 hours since you missed your last dose. Wait and take the next dose at your regular time.

Pregnancy level

C

Related drugs

Amlober , eplerenone , Mibefradil , Nicardipine , Nisoldipine , Lercanidipine , Nitrendipine , Methyclothiazide