Composition, form of production and packaging
Tablets 1 tab.
amlodipine 2.5 mg
Excipients: corn starch, calcium phosphate dibasic, talc purified, silicon dioxide colloid, sodium starch glycolate, magnesium stearate.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
Tablets 1 tab.
amlodipine besylate 5 mg
Excipients: corn starch, calcium phosphate dibasic, talc purified, silicon dioxide colloid, sodium starch glycolate, magnesium stearate.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
Tablets 1 tab.
amlodipine besylate 10 mg
Excipients: corn starch, calcium phosphate dibasic, talc purified, silicon dioxide colloid, sodium starch glycolate, magnesium stearate.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the print edition of 2007.
PHARMACHOLOGIC EFFECT
Selective calcium channel blocker II class. It has antihypertensive, antianginal, antispasmodic and vasodilating effect. It blocks the flow of calcium ions into the cells of the smooth muscles of the vessels.
The mechanism of antihypertensive action is due to a direct relaxing effect on smooth muscle vessels.
The antianginal effect of the drug is associated with its ability to expand peripheral arterioles, which leads to a decrease in OPSS. Reducing the load leads to a decrease in myocardial oxygen demand. On the other hand, under the action of the drug due to the expansion of the coronary arteries, the intake of oxygen increases (especially with angiospastic angina).
The drug does not adversely affect the lipid composition of blood plasma. Has antiatherosclerotic, antithrombotic activity, increases the rate of glomerular filtration, has a mild natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria.
PHARMACOKINETICS
Suction
After taking the drug inside, amlodipine quickly and almost completely (about 90%) is absorbed from the digestive tract. C max is reached within 6-12 hours. Bioavailability is about 60-65%.
Distribution
C ss is established after 7-8 days of regular admission. V d is about 20 l / kg. Binding to blood plasma proteins - 95-98%. Amlodipine penetrates through the BBB, excreted in breast milk.
Metabolism
Amlodipine is biotransformed mainly in the liver with the formation of inactive metabolites.
Excretion
In unchanged form, less than 10% is output, in the form of inactive metabolites with urine - about 60%, with bile and through the intestine - 20-25%.
INDICATIONS
- Arterial hypertension (in the form of monotherapy or as part of a combination therapy with thiazide diuretics, ACE inhibitors, alpha and beta-blockers);
- stable angina pectoris;
- unstable angina;
- angiospastic angina (angina of Prinzmetal).
DOSING MODE
With arterial hypertension and angina pectoris prescribe the drug at a dose of 5 mg / day. If necessary, an increase in the daily dose to 10 mg is possible.
Patients with dilated cardiomyopathy start treatment with a dose of 2.5 mg / day, with good tolerability, a gradual increase in the daily dose to 10 mg is possible.The maximum daily dose is 10 mg.
When using Kalchek in combination therapy with thiazide diuretics, beta-blockers or ACE inhibitors, there is no need for correction of the dosing regimen of the drug.
SIDE EFFECT
From the cardiovascular system: palpitation, shortness of breath, hot flashes.
From the central nervous system and peripheral nervous system: dizziness, headache, drowsiness, a sense of fatigue; rarely - a change in mood, asthenia, muscle cramps, myalgia, impaired vision, paresthesia.
From the digestive system: dyspepsia, nausea, abdominal pain; rarely - increased activity of hepatic transaminases, cholestatic jaundice.
Dermatological reactions: skin rash, itching; rarely erythema multiforme.
Other: rarely - gynecomastia, impotence, frequent urination, swelling, gingival hyperplasia.
The drug is usually well tolerated.
CONTRAINDICATIONS
- arterial hypotension;
- Hypersensitivity to amlodipine and other dihydropyridine derivatives.
PREGNANCY AND LACTATION
Safety and effectiveness of the use of the drug Kalchek during pregnancy and lactation (breastfeeding) are not established. The use of the drug during pregnancy and lactation (breastfeeding) is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or baby. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug to patients with impaired liver function.
APPLICATION FOR CHILDREN
The experience of clinical use of the drug in children is absent.
SPECIAL INSTRUCTIONS
With caution should prescribe the drug to patients with impaired liver function, with stenosis of the aortic estuary, with chronic heart failure.
Possible simultaneous application of Kalchek with nitrates, NSAIDs, antibiotics, hypoglycemic drugs for oral administration.
Use in Pediatrics
The experience of clinical use of the drug in children is absent.
Impact on the ability to drive vehicles and manage mechanisms
Kalchek does not affect the ability to drive vehicles.
OVERDOSE
Symptoms: severe arterial hypotension.
Treatment: the patient should be given a horizontal position with raised legs; it is necessary to maintain the function of the cardiovascular system, monitor heart and lung function, control bcc and diuresis.
To restore the tone of the vessels used vasoconstrictive drugs (in the absence of contraindications to their use); To eliminate the effects of calcium channel blockade, gluconate is injected into / into the calcium. Hemodialysis is ineffective.
DRUG INTERACTION
With the simultaneous use of Kalchek and warfarin, there is no significant change in prothrombin time in healthy male volunteers.
Pharmacokinetic interaction
With the simultaneous application of Kalchek and digoxin, there was no change in serum digoxin concentration and its renal clearance.
The combined use of cimetidine and calcek does not affect the pharmacokinetic parameters of amlodipine.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, cool, protected from light, out of reach of children. Shelf life - 2 years.
