AMBESYL Amlodipine Besilate 5mg Tablet 1's
RXDRUG-DRP-1276-1pc
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Essential hypertension, chronic stable and vasospastic angina pectoris.
Dosage/Direction for Use
Adults: For both hypertension and angina the usual initial dose is 5 mg amlodipine once daily which may be increased to a maximum dose of 10 mg depending on the individual patient's response.
In hypertensive patients, amlodipine has been used in combination with a thiazide diuretic, alpha blocker, beta blocker, or an angiotensin converting enzyme inhibitor. For angina, amlodipine may be used as monotherapy or in combination with other antianginal medicinal products in patients with angina that is refractory to nitrates and/or to adequate doses of beta blockers.
No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta blockers, and angiotensin-converting enzyme inhibitors.
Special populations: Older patients: Amlodipine used at similar doses in older or younger patients is equally well tolerated. Normal dose regimens are recommended in older patients, but increase of the dose should take place with care (see Precautions and Pharmacology: Pharmacokinetics under Actions).
Hepatic impairment: Dose recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautious and should start at the lower end of the dosing range (see Precautions and Pharmacology: Pharmacokinetics under Actions).
Renal impairment: Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dose is recommended. Amlodipine is not dialysable.
In hypertensive patients, amlodipine has been used in combination with a thiazide diuretic, alpha blocker, beta blocker, or an angiotensin converting enzyme inhibitor. For angina, amlodipine may be used as monotherapy or in combination with other antianginal medicinal products in patients with angina that is refractory to nitrates and/or to adequate doses of beta blockers.
No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta blockers, and angiotensin-converting enzyme inhibitors.
Special populations: Older patients: Amlodipine used at similar doses in older or younger patients is equally well tolerated. Normal dose regimens are recommended in older patients, but increase of the dose should take place with care (see Precautions and Pharmacology: Pharmacokinetics under Actions).
Hepatic impairment: Dose recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautious and should start at the lower end of the dosing range (see Precautions and Pharmacology: Pharmacokinetics under Actions).
Renal impairment: Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dose is recommended. Amlodipine is not dialysable.
Overdosage
In humans experience with intentional overdose is limited.
Symptoms: Available data suggest that gross overdose could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to and including shock with fatal outcome have been reported.
Treatment: Clinically significant hypotension due to amlodipine overdose calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities and attention to circulating fluid volume and urine output.
A vasoconstrictor may be helpful 6 restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade.
Gastric lavage may be worthwhile in some cases. In healthy volunteers the use of charcoal up to 2 hours after administration of amlodipine 10 mg has been shown to reduce the absorption rate of amlodipine.
Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.
Symptoms: Available data suggest that gross overdose could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to and including shock with fatal outcome have been reported.
Treatment: Clinically significant hypotension due to amlodipine overdose calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities and attention to circulating fluid volume and urine output.
A vasoconstrictor may be helpful 6 restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade.
Gastric lavage may be worthwhile in some cases. In healthy volunteers the use of charcoal up to 2 hours after administration of amlodipine 10 mg has been shown to reduce the absorption rate of amlodipine.
Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.
Administration
May be taken with or without food.
Contraindications
Amlodipine is contraindicated in patients with: hypersensitivity to dihydropyridine derivatives, amlodipine or to any of the excipients; 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 myocardial infarction.
Special Precautions
The safety and efficacy of amlodipine in hypertensive crisis has not been established.
Patients with cardiac failure: Patients with heart failure should be treated with caution. In a long-term, placebo-controlled study in patients with severe heart failure (NYHA class III and IV) the reported incidence of pulmonary oedema was higher in the amlodipine treated group than in the placebo group (see Pharmacology: Pharmacodynamics under Actions).
Calcium channel blockers, including amlodipine, should be used with caution in patients with congestive heart failure, as they may increase the risk of future cardiovascular events and mortality.
Patients with hepatic impairment: The half-life of amlodipine is prolonged and AUC values are higher in patients with impaired liver function; dose recommendations have not been established. Amlodipine should therefore be initiated at the lower end of the dosing range and caution should be used, both on initial treatment and when increasing the dose. Slow dose titration and careful monitoring may be required in patients with severe hepatic impairment.
Patients with renal impairment: Amlodipine may be used in such patients at normal doses. Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine is not dialysable.
Patients with cardiac failure: Patients with heart failure should be treated with caution. In a long-term, placebo-controlled study in patients with severe heart failure (NYHA class III and IV) the reported incidence of pulmonary oedema was higher in the amlodipine treated group than in the placebo group (see Pharmacology: Pharmacodynamics under Actions).
Calcium channel blockers, including amlodipine, should be used with caution in patients with congestive heart failure, as they may increase the risk of future cardiovascular events and mortality.
Patients with hepatic impairment: The half-life of amlodipine is prolonged and AUC values are higher in patients with impaired liver function; dose recommendations have not been established. Amlodipine should therefore be initiated at the lower end of the dosing range and caution should be used, both on initial treatment and when increasing the dose. Slow dose titration and careful monitoring may be required in patients with severe hepatic impairment.
Patients with renal impairment: Amlodipine may be used in such patients at normal doses. Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine is not dialysable.
Use In Pregnancy & Lactation
Pregnancy: Pregnancy The safety of amlodipine in human pregnancy has not been established.
In animal studies, reproductive toxicity was observed at high doses (see Pharmacology: Toxicology: Preclinical safely data under Actions).
Use in pregnancy is only recommended when there is no safer alternative and when the disease itself carries greater risk for the mother and foetus.
Breast-feeding: It is not known whether amlodipine is excreted in breast milk. A decision on whether to continue/discontinue breast-feeding or to continue/discontinue therapy with amlodipine should be made taking into account the benefit of breast-feeding to the child and the benefit of amlodipine therapy to the mother.
Fertility: Reversible biochemical changes in the head of spermatozoa have been reported in some patients treated by calcium channel blockers. Clinical data are insufficient regarding the potential effect of amlodipine on fertility. In one rat study, adverse effects were found on male fertility (see Pharmacology: Toxicology: Preclinical safely data under Actions).
In animal studies, reproductive toxicity was observed at high doses (see Pharmacology: Toxicology: Preclinical safely data under Actions).
Use in pregnancy is only recommended when there is no safer alternative and when the disease itself carries greater risk for the mother and foetus.
Breast-feeding: It is not known whether amlodipine is excreted in breast milk. A decision on whether to continue/discontinue breast-feeding or to continue/discontinue therapy with amlodipine should be made taking into account the benefit of breast-feeding to the child and the benefit of amlodipine therapy to the mother.
Fertility: Reversible biochemical changes in the head of spermatozoa have been reported in some patients treated by calcium channel blockers. Clinical data are insufficient regarding the potential effect of amlodipine on fertility. In one rat study, adverse effects were found on male fertility (see Pharmacology: Toxicology: Preclinical safely data under Actions).
Adverse Reactions
Summary of the safely profile: The most commonly reported adverse reactions during treatment are somnolence, dizziness, headache, palpitations, flushing, abdominal pain, nausea, ankle swelling, oedema and fatigue.
List of adverse reactions: The following adverse reactions have been observed and reported during treatment with amlodipine with the following frequencies: Very common (61/10); common (61/100 to <1/10); uncommon (61/1,000 to <1/100); rare (61/10,000 U <1/1,000); very rare (<1/10,000).
Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
Blood and lymphatic system disorders: Very rare: Leukocytopenia, thrombocytopenia.
Immune system disorders: Very rare: Allergic reactions.
Metabolism and nutrition disorders: Very rare: Hyperglycaemia.
Psychiatric disorders: Uncommon: Depression, mood changes (including anxiety), insomnia. Rare: Confusion.
Nervous system disorders: Common: Somnolence, dizziness, headache (especially at the beginning of the treatment). Uncommon: Tremor, dysgeusia, syncope, hypoaesthesia, paraesthesia. Very rare: Hypertonia, peripheral neuropathy. Not known: Extrapyramidal disorder.
Eye disorders: Common: Visual disturbance (including diplopia).
Ear and labyrinth disorders: Uncommon: Tinnitus.
Cardiac disorders: Common: Palpitations. Uncommon: Arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation). Very rare: Myocardial infarction.
Vascular disorders: Common: Flushing. Uncommon: Hypotension. Very rare: Vasculitis.
Respiratory, thoracic and mediastinal disorders: Common: Dyspnoea. Uncommon: Cough, rhinitis.
Gastrointestinal disorders: Common: Abdominal pain, nausea, dyspepsia, altered bowel habits (including diarrhoea and constipation). Uncommon: Vomiting, dry mouth. Very rare: Pancreatitis, gastritis, gingival hyperplasia.
Hepatobiliary disorders: Very rare: Hepatitis, jaundice, hepatic enzyme increased*.
Skin and subcutaneous disorders:Uncommon: Alopecia, purpura, skin discolouration, hyperhidrosis, pruritus, rash, exanthema, urticaria. Very rare: Angioedema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, Quincke oedema, photosensitivity.
Musculoskeletal and connective tissue disorders: Common: Ankle swelling, muscle cramps. Uncommon: Arthralgia, myalgia, back pain.
Renal and urinary disorders: Uncommon: Micturition disorder, nocturia, increased urinary frequency.
Reproductive system and breast disorders: Uncommon: Impotence, gynaecomastia.
General disorders and administration site conditions: Very common: Oedema. Common: Fatigue, asthenia. Uncommon: Chest pain, pain, malaise.
Investigations: Uncommon: Weight increased, weight decreased mostly consistent with cholestasis.
List of adverse reactions: The following adverse reactions have been observed and reported during treatment with amlodipine with the following frequencies: Very common (61/10); common (61/100 to <1/10); uncommon (61/1,000 to <1/100); rare (61/10,000 U <1/1,000); very rare (<1/10,000).
Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
Blood and lymphatic system disorders: Very rare: Leukocytopenia, thrombocytopenia.
Immune system disorders: Very rare: Allergic reactions.
Metabolism and nutrition disorders: Very rare: Hyperglycaemia.
Psychiatric disorders: Uncommon: Depression, mood changes (including anxiety), insomnia. Rare: Confusion.
Nervous system disorders: Common: Somnolence, dizziness, headache (especially at the beginning of the treatment). Uncommon: Tremor, dysgeusia, syncope, hypoaesthesia, paraesthesia. Very rare: Hypertonia, peripheral neuropathy. Not known: Extrapyramidal disorder.
Eye disorders: Common: Visual disturbance (including diplopia).
Ear and labyrinth disorders: Uncommon: Tinnitus.
Cardiac disorders: Common: Palpitations. Uncommon: Arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation). Very rare: Myocardial infarction.
Vascular disorders: Common: Flushing. Uncommon: Hypotension. Very rare: Vasculitis.
Respiratory, thoracic and mediastinal disorders: Common: Dyspnoea. Uncommon: Cough, rhinitis.
Gastrointestinal disorders: Common: Abdominal pain, nausea, dyspepsia, altered bowel habits (including diarrhoea and constipation). Uncommon: Vomiting, dry mouth. Very rare: Pancreatitis, gastritis, gingival hyperplasia.
Hepatobiliary disorders: Very rare: Hepatitis, jaundice, hepatic enzyme increased*.
Skin and subcutaneous disorders:Uncommon: Alopecia, purpura, skin discolouration, hyperhidrosis, pruritus, rash, exanthema, urticaria. Very rare: Angioedema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, Quincke oedema, photosensitivity.
Musculoskeletal and connective tissue disorders: Common: Ankle swelling, muscle cramps. Uncommon: Arthralgia, myalgia, back pain.
Renal and urinary disorders: Uncommon: Micturition disorder, nocturia, increased urinary frequency.
Reproductive system and breast disorders: Uncommon: Impotence, gynaecomastia.
General disorders and administration site conditions: Very common: Oedema. Common: Fatigue, asthenia. Uncommon: Chest pain, pain, malaise.
Investigations: Uncommon: Weight increased, weight decreased mostly consistent with cholestasis.
Drug Interactions
Increased exposure & risk of hypotension w/ strong or moderate CYP3A4 inhibitors (PIs, azole antifungals, macrolides eg, erythromycin or clarithromycin, verapamil or diltiazem). Lower plasma conc w/ CYP3A4 inducers (rifampicin, Hypericum perforatum). Increased BP lowering effects w/ grapefruit or grapefruit juice & medicinal products w/ antihypertensive properties. Risk of hyperkalemia w/ dantrolene infusion & verapamil. Increase tacrolimus blood levels. Increased risk of hypotension w/ clarithromycin. Increase trough conc of ciclosporin in renal transplant patients. Increased exposure w/ simvastatin.
Caution For Usage
For caution against possible variation of physical aspect of medicine. Incompatibilities: Not applicable.
Storage
Store at room temperature not exceeding 25°C.
Action
Pharmacotherapeutic group: Calcium channel blockers, selective calcium channel blockers with mainly vascular effects, dihydropyridine derivatives. ATC code: CO8CA01.
Pharmacology: Pharmacodynamics: Amlodipine is a calcium ion influx inhibitor of the dihydropyridine group (slow channel blacker or calcium its antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. The mechanism of the antihypertensive action of amlodipine is due to a direct relaxant effect on vascular smooth muscle. The precise mechanism by which amlodipine relieves angina has not been fully determined but amlodipine reduces total ischaemic burden by the following two actions: Amlodipine dilates peripheral arterioles and thus, reduces the total peripheral resistance (afterload) against which the heart works. Since the heart rate remains stable, this unloading of the heart redoes myocardial energy consumption and oxygen requirements.
The mechanism of action of amlodipine also probably involves dilatation of the main coronary arteries and coronary arterioles, both in normal and ischaemic regions. This dilatation increases myocardial oxygen delivery in patients with coronary artery spasm (Prinzmetal's or variant angina).
In patients with hypertension, once daily dosing provides clinically significant reductions of blood pressure in both the supine and standing positions throughout the 24 hour interval. Dots the slow onset of action, acute hypotension is not a feature of amlodipine administration.
In patients with angina, once daily administration of amlodipine increases total exercise time, time to angina onset, and time to 1 mm ST segment depression, and decreases both angina attack frequency and glyceryl trinitrate tablet consumption.
Amlodipine has not been associated with any adverse metabolic effects or changes in plasma lipids and is suitable for use in patients with asthma, diabetes, and gout.
Pharmacology: Pharmacodynamics: Amlodipine is a calcium ion influx inhibitor of the dihydropyridine group (slow channel blacker or calcium its antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. The mechanism of the antihypertensive action of amlodipine is due to a direct relaxant effect on vascular smooth muscle. The precise mechanism by which amlodipine relieves angina has not been fully determined but amlodipine reduces total ischaemic burden by the following two actions: Amlodipine dilates peripheral arterioles and thus, reduces the total peripheral resistance (afterload) against which the heart works. Since the heart rate remains stable, this unloading of the heart redoes myocardial energy consumption and oxygen requirements.
The mechanism of action of amlodipine also probably involves dilatation of the main coronary arteries and coronary arterioles, both in normal and ischaemic regions. This dilatation increases myocardial oxygen delivery in patients with coronary artery spasm (Prinzmetal's or variant angina).
In patients with hypertension, once daily dosing provides clinically significant reductions of blood pressure in both the supine and standing positions throughout the 24 hour interval. Dots the slow onset of action, acute hypotension is not a feature of amlodipine administration.
In patients with angina, once daily administration of amlodipine increases total exercise time, time to angina onset, and time to 1 mm ST segment depression, and decreases both angina attack frequency and glyceryl trinitrate tablet consumption.
Amlodipine has not been associated with any adverse metabolic effects or changes in plasma lipids and is suitable for use in patients with asthma, diabetes, and gout.
MedsGo Class
Calcium Antagonists / Anti-Anginal Drugs
Features
Brand
Ambesyl
Full Details
Dosage Strength
5mg
Drug Ingredients
- Amlodipine
Drug Packaging
Tablet 1's
Generic Name
Amlodipine Besilate
Dosage Form
Tablet
Registration Number
DRP-1276
Drug Classification
Prescription Drug (RX)
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