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Apitim 5

Treatment of hypertension, angina pectoris


Amlodipine besylate, calculated on amlodipine ...................................................... 5 mg

Excipients q.s..................................................................................................... 1 capsule

(Avicel, dicalcium phosphate, PVP, sodium lauryl sulphate, sodium starch glycolate, aerosil, magnesium stearate).


DOSAGE FORM: Capsules.


PRESENTATION: Box of 3 blisters x 10 capsules.


PHARMACODYNAMICS: Apitim contains amlodipine which is a dihydropyridine calcium antagonist. Amlodipine inhibits the transmembrane influx of calcium into cardiac muscle and vascular smooth muscle by slow channel blocker of cell membrane. Due to amlodipine's effect, smooth muscle tonicity of blood vessels decreases to cause a decrease in peripheral resistance and reduction in blood pressure.

Apitim relieves angina pectoris by dilatation of peripheral arterioles and reduction of cardiac afterload. Since the heart rate remains stable, this unloading of the heart reduces myocardial energy consumption and oxygen requirements. Amlodipine dilates the main coronary arteries and arterioles, both in normal and ischemic regions. This dilatation increases myocardial oxygen delivery.


PHARMACOKINETICS: Oral bioavailability of amlodipine has been estimated to be between 60 to 80% and is altered by the presence of food. Amlodipine has a terminal elimination half-life of 30 to 40 hours and steady-state plasma concentrations are reached after 7 to 8 days of consecutive daily dosing. Amlodipine is extensively converted to inactive metabolites via hepatic metabolism and mostly excreted in the urine. In patients with hepatic impairment, the dose should be reduced and prolongs the interval of dosages.


INDICATIONS: Treatment of hypertension, especially in patients with metabolic complications such as diabetes.

Treatment of chronic stable angina pectoris, vasospastic angina pectoris


CONTRAINDICATIONS: Hypersensitivity to dihydropyridine derivatives.

No use in patients with heart failure not treated stably.


PRECAUTIONS: Impaired hepatic function, aortic stenosis, heart failure after acute myocardial infarction.


USE IN PREGNANCY: Calcium-channel blockers may inhibit early uterine contraction; however, they cause no adverse effect on parturition. Risk of hypoxia for embryos may occur in case of hypotension in the mother. In experimental animals, calcium-channel blockers have been reported to cause monsters with bone malformation. Therefore, amlodipine should not be administered to pregnant women, particularly in the first trimester of pregnancy.


USE IN LACTATION: It is not known whether amlodipine is excreted in human milk.


INTERACTIONS: Anesthetics enhance the effect of amlodipine and may cause a stronger hypotension.

Concurrent use of lithium and amlodipine may cause nervous toxicity, nausea, vomiting, diarrhoea.

Nonsteroidal anti-inflammatory drugs, particularly indomethacine may reduce the effect of amlodipine.

Caution should be taken when concomitant use of plasma-protein high-binding drugs (e.g. coumarine, hydantoine derivatives...) and amlodipine because amlodipine is also a protein high-binding agent and therefore the unbound concentration of the above drugs may be changed in the plasma.


ADVERSE EFFECTS: Frequently: ankle oedema (related with dosage), headache, dizziness, flushing and burning, fatigue, asthenia, palpitation, cramp, nausea, abdominal pain, indigestion, dyspnea.

Infrequently: excessive hypotension, tachycardia, chest pains, rash, pruritus, muscular pains, joint pains, dyssomnia.

Rarely: extrasystole, gums hyperplasia, urticaria, increase in hepatic enzyme levels, hyperglycaemia, confusion, diversified rash.

Inform your physician about any adverse effects occur during treatment.


OVERDOSAGE: Amlodipine intoxication is rarely reported.

Treatment of overdosage: monitor cardio-vascular system by electrocardiogram and treat symptoms of cardiovascular effects along with emptying stomach and administering activated charcoal. If necessary, adjustment of electrolytes should be advised. In cases of bradycardia and cardiac block, intravenous injection with atropine, intravenous injection in drops with calcium gluconate, isoprenaline or adrenalin or dopamine should be given. Patients with reduction of circulatory volume need to transfuse sodium chloride 0.9% solution, adrenalin. If no results, combination of isoprenaline and amrinon should be used.


DOSAGE & ADMINISTRATION: Dosage should be adjusted according to each patient's response.

The usual initial dose is 5 mg once daily, which may be increased to a maximum dose of 10 mg once daily.

No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta-blockers or angiotensin-converting enzyme inhibitors.

Or as directed by the physician.

Read the directions carefully before use.

Consult the physician for more information.

This drug is for prescriptions only.

Shelf-life: 36 months from the manufacturing date.

Storage conditions: Store in dry places; not exceeding 30oC.

Specifications: Manufacturer's.

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