Norvasc

Description overdue on 08/09/2014

• Latin name: Norvasc
• ATC code: C08CA01
• Active substance: Amlodipine (Amlodipine)
• Manufacturer: Pfizer Menyufekchuring Doychlend GmbH (Germany)

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications Norvasc
• Contraindications
• Side effects
• Norvaks, instructions for use (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Synonyms
• Babies
• With alcohol
• With antibiotics
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

1 tablet, as active substance, contains 6,935 mg amlodipine besilate   (Amlodipine 5 mg) or 13, 87 mg of amlodipine besylate (amlodipine 10 mg).

As auxiliary substances are:

• sodium starch glycolate type A ;
• microcrystalline cellulose ;
• anhydrous calcium hydrogen phosphate ;
• magnesium stearyl t .

Product form

Tablets containing 5 mg (Norvasc 5 mg) or 10 mg (Norvasc 10 mg) amlodipine. According to the description of White or almost white, in the form of an octahedron with uneven sides. On one side embossed logo «Pfizer" on another, the active substance content, respectively, «AML-5" or «AML-10."

One pack holds 14 or 30 tablets of 5 or 10 mg.

Pharmacological action

Norvasc has antihypertensive and anti-anginal activity.

Pharmacodynamics and pharmacokinetics

Amlodipine is a derivative dihydropyridine . The mechanism of action associated with blocking calcium channels (BPC) and inhibiting transmembrane transfer of calcium in the vascular smooth muscle cells (mostly) and cardiomyocytes (to a lesser degree). Thus manifested hypotensive and antianginal effects.

The antihypertensive effect is determined by a direct relaxant effect on vascular smooth muscle.

Reduction   myocardial ischemia   It goes two ways:

Amlodipine acts on peripheral arterioles contributing to their expansion. In this connection, it reduced peripheral vascular resistance (total peripheral vascular resistance) with practically unaltered HR (heart rate), which leads to lower energy consumption and a decrease in myocardial oxygen demand.

The drug increases arterioles and coronary and peripheral arteries, in zones of normal myocardium and in ischemic, thereby increasing the oxygen supply of the myocardium in patients with vasospastic angina, preventing the development of coronary spasm.

At hypertension   disposable daily dose Norvasc provides the normalization of blood pressure over 24 hours (standing and lying). With the gradual action does not lead to a sharp decrease in blood pressure.

Patients suffering angina   disposable daily dose of the drug increases the potential of physical activity, inhibits the development of angina attack   and slow d epressiyu segment ST It reduces the frequency of angina attacks, and regular use nitroglycerin .

Application Norvasc patients with cardiovascular disease (including coronary atherosclerosis with lesions 1st vessel and to stenosis   3 or more arteries, as well as atherosclerosis carotid arteries), which moved percutaneous angioplasty . myocardial infarction   or suffering on angina It prevents changes intima-media thickness of the carotid arteries and greatly reduces the incidence of deaths for these reasons. Also reduces the number of hospitalizations for progression Heart failure and unstable angina It reduces the frequency of the possible interventions for the resumption of normal coronary blood flow .

It does not increase the risk of deaths or complications in patients with III-IV heart failure functional class (according to NYHA) In the treatment of digoxin, ACE inhibitors and diuretics . No effect on myocardial contractility and conductivity, does not lead to reflex increase in heart rate, a positive effect on the speed glomerular filtration rate Slows down platelet aggregation, shows a weak natriuretic effect. It reinforces the severity microalbuminuria   diabetic nephropathy . No adverse effects on plasma lipids and metabolism.

Absorption:

For oral therapeutic dose is well absorbed.

The blood reaching Cmax after 6 - 12 hours.

Approximately equal to Vd - 21 l / kg.

The absolute bioavailability - 64 - 80%.

Communication with the plasma proteins is approximately 97, 5%.

Penetrates through the BBB, food intake does not affect the absorption of amlodipine.

Metabolism and excretion:

Total clearance - 0 43 l / h / kg.

T1 / 2 of 35-50 hours. In severe heart failure and liver failure is increased to 56-60 hours.

The plasma is stable CSS observed after 7-8 days of continuous use.

Conversion to the inactive metabolite in the liver.

10% of unchanged drug and 60% educated metabolites excreted by the kidneys.

Not removed during dialysis, removing the milk has not been studied.

Indications Norvasc

Indications for use of the drug Norvasc comply with recommendations to derivatives   dihydropyridine To appoint:

• at hypertension   (monotherapy or combination therapy with other antihypertensive drugs);
• at stable angina   and   Prinzmetal angina (vasospastic angina)   (monotherapy or combination therapy with other antianginal drugs).

Contraindications

• individual hypersensitivity to the components of Norvasc;
• hypotension   (severe).

With extreme caution:

• CHF nonischemic nature of class III-IV ;
• hypotension ;
• hypertrophic obstructive cardiomyopathy ;
• aortic stenosis ;
• hepatic failure ;
• sick sinus syndrome ;
• mitral stenosis ;
• age 18 years (safety and efficacy have not been tested);
• acute myocardial infarction (1 month after).

Side effects

Cardiovascular system:

• palpitations;
• peripheral edema (feet and ankles);
• excessive reduction of blood pressure;
• orthostatic hypotension ;
• development or enhancement Heart Failure ;
• vasculitis ;
• cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation);
• feeling chest pain;
• migraine ;
• myocardial infarction .

Musculoskeletal system:

• arthralgia ;
• myalgia ;
• muscle cramps;
• arthritis;
• back pain;
• myasthenia .

Peripheral and central nervous system:

• flushing;
• feeling hot;
• fatigue;
• drowsiness;
• dizziness;
• headache;
• malaise;
• increased sweating;
• fainting;
• asthenia ;
• paresthesia ;
• hypoesthesia ;
• peripheral neuropathy ;
• sleeplessness;
• tremor;
• lability of mood;
• nervousness;
• anxiety;
• depression ;
• convulsions;
• agitation;
• apathy;
• amnesia ;
• ataxia .

Digestive system:

• nausea;
• abdominal pain;
• vomiting;
• constipation or bloating;
• diarrhea;
• dyspepsia ;
• anorexia ;
• feeling thirsty;
• dry mouth;
• increased appetite;
• gingival hyperplasia ;
• gastritis ;
• hyperbilirubinemia ;
• pancreatitis ;
• jaundice;
• hepatitis ;
• increase in liver transaminases.

Hematopoietic system:

• t rombotsitopeniya ;
• thrombocytopenic purpura ;
• leukopenia .

Respiratory system:

• rhinitis ;
• breathlessness ;
• cough.

Urogenital:

• nocturia ;
• frequent or painful urination;
• gynecomastia ;
• impotence I;
• polyuria ;
• dysuria .

Metabolic disorders:

• hyperglycemia .

Allergic reactions:

• rash or itching;
• erythema multiforme ;
• angioedema ;
• hives .

Others:

• ringing in the ears;
• alopecia ;
• changes in body weight;
• blurred vision;
• ccomodation;
• diplopia ;
• xerophthalmia ;
• sore eyes;
• conjunctivitis ;
• taste perversion;
• nose bleed;
• chills;
• dermatitis ;
• parosmiya ;
• cold sweat;
• dermatoxerasia ;
• pigmented lesions of the skin.

Norvaks, instructions for use (method and dosage)

The required dose of the drug Norvasc, depending on the individual, can only set attending physician.

Accordingly the instructions for use Norvasc, the initial dose of 5 mg and can be increased to 10 mg, in connection with portability and the body by a physician.

A medicament for oral administration is shown once during the day. The tablet is swallowed whole with water.

Dosage adjustment, renal and hepatic failure (moderate severity), and in old age is required.

When combined with ACE inhibitors . thiazide diuretics . beta-blockers   dosing schedule remains unchanged.

Overdose

If overdose is possible sharp decline in blood pressure with further appearance reflex tachycardia   and excess peripheral vasodilation   (there is a possibility of severe resistant hypotension   with further shock   and fatal).

In the first two hours are assigned to receive adsorbents (e.g. Activated Carbon ), In some cases - gastric lavage. Patients are advised to take a horizontal position with raised legs. Actively supports the function of the cardiovascular system, monitor performance in the lungs and heart, as well as control the volume of circulating blood and urine output.

In the absence of contraindications apply vasoconstrictor drugs, normalization of vascular tone and blood pressure. Intravenous impose calcium gluconate . Hemodialysis   ineffective.

Cooperation

Perhaps the increased side effects inhibitors of microsomal oxidation , Due to the increasing concentration of amlodipine. Inductors of microsomal liver enzymes conversely reduce the amount of the active ingredient of the drug.

The combined use of amlodipine and   cimetidine   pharmacokinetics first remains unchanged.

Grapefruit juice in a volume of 240 ml and amlodipine 10 mg did not result in significant changes in the pharmacokinetics of the drug.

Clinically significant interactions with Norvasc NSAIDs   not detected.

Increased antihypertensive and anti-anginal action Norvasc possible while the use of loop and thiazide diuretics, ACE inhibitors, verapamil, nitrates and beta-blockers . There has also been increased hypotensive effect when co-administered neuroleptics and alpha 1-blockers .

Negative inotropic effect in the study Norvasc not observed. But it is worth remembering that the CCB may help to strengthen the effect of certain anti-arrhythmic drugs (eg, quinidine and amiodarone ).

The combined use of drugs lithium and CCBs may enhance the neurotoxicity first (nausea, diarrhea, vomiting, ataxia, tinnitus, tremor).

Amlodipine (in vitro) does not affect the binding of warfarin, digoxin, indomethacin   plasma proteins.

Concurrently receives and aluminum-magnesium-containing antacids, did not significantly affect the pharmacokinetics of amlodipine.

Chance of a single dose of sildenafil   (100 mg) during therapy Norvasc.

Reapply atorvastatin   80 mg amlodipine and 10 mg and is not accompanied by significant changes in pharmacokinetics first.

Pharmacokinetics cyclosporine   When combined with the admission of amlodipine practically unchanged.

Terms of sale

Norvasc prescription.

Storage conditions

Out of reach of children, at a temperature not exceeding 25 ° C.

Shelf life

4 years.

Cautions

In the treatment of hypertension drug Norvasc can be combined with alpha- and beta-blockers, thiazide diuretics, sublingual nitroglycerin, ACE inhibitors, long-acting nitrates, antibiotics, NSAIDs, and hypoglycemic agents   for internal use.

It can be used both in monotherapy and in combined therapy with other antianginal drugs For treatment angina .

The drug has no adverse effects on plasma lipids and metabolism, and therefore, can be administered to patients gout, diabetes and asthma .

Perhaps the use of Norvasc in the predisposition of the patient to vasospasm and vasoconstriction .

You may need to decrease the dose of the drug for patients of small stature, low birth weight, and patients with severe liver function disorders.

During the course of therapy should be to control body weight and be screened by a dentist, to prevent bleeding, pain and   gingival hyperplasia .

Analogs Norvasc

Match code ATC 4th level:

• Fenigidin
• Kordafleks
• Lerkamen
• Corinfar
• Vero Amlodipine
• Amlodipine
• Nifedipine

The drug Norvasc has many analogues, the most famous of which are presented below:

• Adalat;
• Zanidip;
• Kordafleks;
• Cordipin;
• Corinfar;
• Lerkamen;
• Nimopin;
• Nifedipine;
• Felodip etc.

Synonyms Norvasc

• Amlodipine;
• Amlo;
• Agen;
• Amlodak;
• Normodipin;
• Korvadil;
• Stamlo   etc.

Babies

Oral daily antihypertensive dose for patients aged 6 to 18 years old, is from 2, 5 mg to 5 mg (maximum). Effect of the drug for children under 6 years of age has not been studied.

With alcohol

The dose of 10 mg did not significantly affect the pharmacokinetics of ethanol (alcohol-containing beverages).

With antibiotics

A combination with antibiotics in the treatment hypertension .

During pregnancy (and lactation)

I do not recommend the appointment of Norvasc during pregnancy due to lack of reliable data in this period.

It should stop taking the drug during breast feeding or cancel the preparation itself.

Reviews of Norvasc

Positive reviews about Norvasc forums occupy a significant place. Among complaints often pay attention to the small peripheral edema and tachycardia . There are also completely negative reviews about this drug that is likely to be associated with incorrectly chosen regimen or dose of the drug.

Wondering what is best or Norvasc Amlodipine   domestic production, it is worth remembering that the quality of the products of pharmaceutical company «Pfizer» can not be doubted, while the funds produced by our manufacturers, unfortunately, often do not meet their requirements. Although both drugs contain one active ingredient - Amlodipine, for purity and weight content exceeds domestic import analogue.

Price Norvasc where to buy

Approximate price of Norvasc in pharmacy chains is 5 mg №14 - 300 rubles; 5 mg №30 - 550 rubles; 10 mg №14 - 500 rubles; 10 mg №30 - 950 rubles.

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