22, Adewunmi Abudu Street, Ajao Estate, Lagos, Nigeria
Tel: 234-0805 598 9266
Canopus West Africa Ltd
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN:A4-6281): Amlodipine 5 mg
Pack size: 3 x 10’s
Tablet (NRN:A4-6178): Amlodipine 10 mg
Pack size: 3 x 10’s
Amlodipine is a long-acting calcium channel blocker. Its empirical formula is C20H25CIN205.C6H603S.
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. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites.
The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels.
Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle coils.
Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
Pharmacokinetics and Metabolism
After oral administration of therapeutic doses of Amlodipine, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability has been estimated to be between 64 and 90%.
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. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients.
Elimination from the plasma is biphasic with a terminal elimination half-life of about 30 - 50 hours. Steady-state plasma levels of amlodipine are reached after 7 to 8 days of consecutive daily dosing.
- Coronary Artery Disease (CAD)
- Chronic Stable Angina
- Vasospastic Angina (Prinzmetal's or Variant Angina)
- Angiographically Documented CAD
- Angina Pectoris
- Acute Myocardial Infarction
- Grapefruit Juice
PREGNANCY Category B
AMLOCAN-1 0 tablets are not recommended in nursing mothers because its safety in infants and newborns has not been studied.
Cardiovascular: arrhythmia (including ventricular tachycardia and atrial fibrillation), bradycardia, chest pain, hypotension, peripheral ischemia, syncope, tachycardia, postural dizziness. postural hypotension, vasculitis.
Central and Peripheral Nervous System: hypoesthesia, neuropathy peripheral, paresthesia, tremor, vertigo.
Gastrointestinal: anorexia, constipation, dyspepsia, dysphagia, diarrhea, flatulence, pancreatitis, vomiting, gingival hyperplasia.
General: allergic reaction, asthenia, back pain, hot flushes, malaise, pain, rigors, weight gain, weight decrease.
Musculoskeletal System: arthralgia, arthrosis, muscle cramps, myalgia.
Psychiatric: sexual dysfunction (male and female), insomnia, nervousness, depression, abnormal dreams, anxiety, depersonalization.
Respiratory System: dyspnea, epistaxis.
Skin and Appendages: angioedema, erythema multiforme, pruritus, rash, rash erythematous, rash maculopapular.
Special Senses: abnormal vision, conjunctivitis, diplopia, eye pain, tinnitus.
Urinary System: micturition frequency, micturition disorder, nocturia.
Autonomic Nervous System: dry mouth, sweating increased.
Metabolic and Nutritional: hyperglycemia, thirst.
Hemopoietic: leukopenia, purpura, thrombocytopenia.
Dosage & Administration
One tablet daily.