Full Prescribing Info
Amlodipine besylate.
AMBES-5: Each tablet contains amlodipine besylate 6.94 mg equivalent to amlodipine 5 mg.
AMBES-10: Each tablet contains amlodipine besylate 13.88 mg equivalent to amlodipine 10 mg.
Pharmacology: Pharmacodynamics: Amlodipine is classified as calcium ion influx inhibitor (slow channel blocker or calcium ion antagonist). It inhibits an influx of calcium ions across cell membrane into cardiac and vascular smooth muscles.
Amlodipine produces arteriolar vasodilation by acting directly on vascular smooth muscle. This mechanism results in a reduction of blood pressure. The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the two categories as follows: Amlodipine is a peripheral arteriolar vasodilator, thus it reduces total peripheral resistance (afterload) against which the heart works. Due to static heart rate, reduction in heart work causes reduction in myocardial energy and oxygen demand.
Mechanism of action of amlodipine may be related to blocking constriction and restoring blood flow in coronary arteries and arterioles. This inhibition of coronary spasm is responsible for the effectiveness in vasospastic (Prinzmetal's variant angina).
Pharmacokinetics: Absorption: After oral administration of therapeutic doses, amlodipine is well absorbed. It reaches peak plasma concentration within 6-12 hours after intake. The absolute bioavailability is approximately 64-90% while the distribution volume is equivalent to 21 litres/kg. Amlodipine can be taken either before or after meals as food has no effect on its absorption.
Metabolism and Elimination: Plasma elimination terminal half life of amlodipine is 30-50 hours making it suitable to be given as once daily dosage. The plasma level reaches steady state and remains consistent when taking consecutive doses for 7-8 days. Amlodipine is generally metabolized into inactive form at the liver, where 10% remains unchanged, and 60% of the metabolites will be excreted in the urine.
Hypertension: Amlodipine is used alone or in combination with other classes of antihypertensive drugs for the treatment of hypertension. Data from clinical outcome trials indicate that lowering the blood pressure with any of several classes of drugs, including thiazides, β-blockers, calcium-channel blockers, ACE inhibitors, or angiotensin II receptor antagonists will reduce the complications of hypertension.
Coronary Artery Disease: Angina: Amlodipine is used alone or in combination with other antianginal agents for the management of Prinzmetal's variant angina and chronic stable angina pectoris.
Angiographically Documented Coronary Artery Disease (CAD): Amlodipine is used in patients with recently documented coronary artery disease by angiography (without heart failure or an ejection fraction less than 40%) to reduce the risk of coronary revascularization procedure and hospitalization due to angina.
Notes: Data from a multicentre randomized controlled trial (ASCOT-BPLA) indicated that amlodipine-based regimen (amlodipine adding perindopril) reduced the risk of non-fatal myocardial infarction, fatal coronary heart disease, and stroke.
Dosage/Direction for Use
Adults and Geriatric Patients: Hypertension: The usual initial adult dosage is 2.5-5 mg once daily. In geriatric patients, an initial dosage of 2.5 once daily is recommended. This reduced initial dosage is also can be used in adults when amlodipine is added to an existing antihypertensive drug regimen. Subsequent dosage should be adjusted according to the patient's blood pressure response and tolerance and usually should not exceed 10 mg once daily. Generally, dosage is increased gradually at 7 to 14 day intervals until optimum control of blood pressure is maintained. The usual maintenance dosage in adults is 5-10 mg once daily.
Prinzmetal's variant angina or chronic stable angina: The usual adult dosage is 5-10 mg once daily. In geriatric patients, the lower dosage of 5 mg once daily is recommended. Adequate control of angina usually requires a maintenance dosage of 10 mg daily.
Angiographically Documented Coronary Artery Disease (CAD): The recommended adult dosage is 5-10 mg once daily. In clinical studies the majority of patients required a dosage of 10 mg daily.
Children 6-17 years of age: Hypertension: The usual dosage is 2.5-5 mg once daily. The safety and efficacy of dosages exceeding 5 mg daily have not been established.
Dosage in Hepatic Impairment: Hypertension: An initial dosage of 2.5 mg daily is recommended. Subsequent dosage should be adjusted according to patient response and tolerance but usually should not exceed 10 mg once daily.
Prinzmetal's variant angina or chronic stable angina: The dosage of 5 mg is recommended. Adequate control of angina usually requires a maintenance dosage of 10 mg daily.
Mode of Administration: Amlodipine is administered orally. Amlodipine generally can be given without regard to meals.
For treatment of overdose as following: Hypotension: Intravenous fluids, intravenous dopamine or dobutamine, calcium chloride, isoproterenol, metaraminol, or norepinephrine should be used as appropriate.
Isoproterenol, metaraminol, or norepinephrine should be used as appropriate.
Tachycardia, rapid ventricular rate in patients with antegrade conduction in atrial flutter or atrial fibrillation, Wolff-Parkinson-White or Lawn-Ganong-Levine syndrome: intravenous lidocaine or intravenous procainamide.
Bradycardia: Intravenous atropine, isoproterenol, norepinephrine, or calcium chloride, or use of electronic cardiac pacemaker, as appropriate.
It is contraindicated in patients with known hypersensitivity to amlodipine and drugs under dihydropyridine group or any component of the formulation.
Special Precautions
Increased angina and/or myocardial infarction has occurred with initiation or dosage titration of calcium blockers.
Because amlodipine is extensively metabolized by the liver and the plasma elimination half-life will be prolonged in patients with impaired hepatic function. The dose should be slowly adjusted in such patients.
Elderly patients and patients with hepatic impairment have decreased clearance of amlodipine with the resulting increase in AUC and half-life of the drug. These patients may be more sensitive to the hypotensive effects amlodipine and may require a lower initial dose.
Symptomatic hypotension with or without syncope can rarely occur; blood pressure must be lowered at a rate appropriate for the patient's clinical condition. However, there is a possibility for hypotension incidence in patients with severe aortic stenosis and/or hypertropic cardiomyopathy.
The safety and efficacy of amlodipine in children less than 6 years of age have not been established.
Use In Pregnancy & Lactation
Use in Pregnancy: Pregnancy Category C. Embryotoxic effects have been demonstrated in small animals. No well-controlled studies have not been conducted in pregnant women. Use in pregnancy only when clearly needed and when the benefits outweigh the potential hazards to the fetus.
Use in Lactation: It is not known whether amlodipine is excreted in breast milk. Use in breastfeeding is not recommended.
Adverse Reactions
The most common side effects are headache and edema.
Doses related side effects from amlodipine are edema, dizziness, flushing, and palpitation whereas unclear doses related side effects are headache, fatigue, nausea, abdominal pain and somnolence.
Rare side effects that a causal relationship is uncertain as follows: 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, peripheral neuropathy, 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.
Hemapoietic: Leucopenia, purpura, thrombocytopenia.
Very rare side effects are cardiac failure, pulse irregularity, extrasystoles, skin discoloration, urticaria, skin dryness, alopecia, dermatitis, muscle weakness, twitching, ataxia, hypertonia, migraine, cold and clammy skin, apathy, agitation, amnesia, gastritis, increased appetite, loose stools, coughing, rhinitis, dysuria, polyuria, parosmia, taste perversion, abnormal visual accomodation, and xerophthalmia.
Drug Interactions
The levels/ effects of amlodipine may be increased by α1-blockers, antifungal agents (azole derivatives), calcium channel blockers (nondihydropyridine), cyclosporine, moderate inhibitors of CYP3A4, strong inhibitors of CYP3A4, desatinib, diazoxide, fluconazole, grapefruit juice, herbs (hypotensive properties), macrolide antibiotics, magnesium salts, monoamine oxidase inhibitors, pentoxifylline, phosphodiesterase 5 inhibitors, prostacyclin analogues, protease inhibitors, quinupristin.
Amlodipine may increase the levels/effects of amifostine, antihypertensives, CYP1A2 substrates, hypotensive agents, magnesium salts, neuromuscular-blocking agents (non-depolarizing), nitroprusside, phenytoin, rituximab, tacrolimus.
The levels/effects of amlodipine may be decreases by barbiturates, calcium salts, carbamazepine, strong inducers of CYP3A4, defasirox, herbs (CYP3A4 inducers), herbs (hypertensive properties), methylphenidate, nafcillin, rifamycin derivatives, yohimbine.
Amlodipine may decrease the levels/effects of clopidogrel, quinidine.
Concurrent use with lithium potentially may result in the form of nausea, vomiting, diarrhea, ataxia, tremors, and/or tinnitus.
St. John's wort may decrease amlodipine levels.
Avoid using ephedra, yohimbe and ginseng. They may worsen hypertension.
Avoid using garlic. It may have increased antihypertensive effects.
Store in tight, light-resistant container, below 30°C.
MIMS Class
ATC Classification
C08CA01 - amlodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Tab 5 mg (white, circular, flat, bevel-edged, one side bisected, the other side "A-5" marked, compressed) x 10 x 10's. 10 mg (white, octagonal-shaped, flat, bevel-edged, one side bisected with "G" and "10" marked on each section and another side with "GPO" marked, compressed) x 10 x 10's.
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