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Colospa

Colospa
Colospa is intended to treat spasm of the gastrointestinal tract, intestinal and biliary colic, irritable bowel syndrome.

Brand: Mebeverine

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: November 2023
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Colospa 135 mg
240 pills - 135 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$161.97 $0.67 $77.63 Add to cart
120 pills - 135 mg $83.99 $0.70 $35.81 Add to cart
90 pills - 135 mg $68.93 $0.77 $20.92 Add to cart
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Product description

Pharmacotherapeutic group

Buy Colospa in Canada

  • blocker of "slow" calcium channels.

Pharmacological action

Pharmacodynamics

Selective blocker of "slow" calcium channels, derivative of 1,4-dihydropyridine. Has a vasodilating, antianginal and hypotensive effect. Reduces the current of Ca2+ in cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses inhibits the release of Ca2+ from intracellular stores. Reduces the number of functioning channels without affecting the time of their activation, inactivation and recovery. It separates the processes of excitation and contraction in the myocardium, mediated by tropomyosin and troponin, and in vascular smooth muscles, mediated by calmodulin. In therapeutic doses, it normalizes the transmembrane current of Ca2+, impaired in a number of pathological conditions, primarily in arterial hypertension. Does not affect the tone of the veins. Strengthens coronary blood flow, improves blood supply to ischemic zones of the myocardium without the development of the phenomenon of "steal", activates the functioning of collaterals. Expanding the peripheral arteries, it reduces the total peripheral vascular resistance, myocardial tone, afterload, myocardial oxygen demand and increases the duration of diastolic relaxation of the left ventricle. Virtually no effect on sinoatrial and atrioventricular nodes and has no antiarrhythmic activity. Increases renal blood flow, causes moderate natriuresis. The negative chrono-, dromo- and inotropic effects are overlapped by reflex activation of the sympathoadrenal system and an increase in the number of heart contractions in response to peripheral vasodilation.

The onset of the effect is 20 minutes when taken orally; duration of the effect - 12-24 hours (prolonged form of "retard").

Pharmacokinetics

Colospa tablet plate appearance

Absorption - high (more than 92-98%). Bioavailability is 40-60%. Food intake increases bioavailability. Has a "first pass" effect through the liver.

Penetrates the blood-brain barrier, excreted in breast milk.

Completely metabolized in the liver. The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in the metabolism of the drug. The half-life (T1 / 2) is 3.8-16.9 hours. In patients with hepatic insufficiency, the total clearance decreases and T1 / 2 increases.

There is no cumulative effect. Chronic renal failure, hemodialysis and peritoneal dialysis do not affect pharmacokinetics. With prolonged use, tolerance to the drug develops. Plasmapheresis can enhance elimination.

Indications for use Colospa

  • Ischemic heart disease - angina pectoris of exertion and rest (including variant).
  • Arterial hypertension (as monotherapy or in combination with other antihypertensive drugs).

Method of administration and dosage

The dosage regimen is set individually, depending on the severity of the disease and the response to the therapy. It is recommended to take the drug during or after meals with a little water.

Initial dose: 1 tablet (20 mg) twice a day. The dose can be increased if necessary. The maximum daily dose of the drug is 120 mg.

In elderly patients or patients receiving combined (antianginal or antihypertensive) therapy, with impaired liver function, in patients with severe cerebrovascular accidents, the dose should be reduced.

Overdose

Symptoms: headache, hyperemia of the skin of the face, decreased blood pressure, depression of the sinus node, bradycardia, arrhythmia.

Treatment: gastric lavage with the appointment of activated charcoal, symptomatic therapy aimed at stabilizing the activity of the cardiovascular system.

The antidote is calcium; slow intravenous administration of a 10% solution of calcium chloride or calcium gluconate is shown, followed by switching to a long-term infusion.

With a pronounced decrease in blood pressure - intravenous dopamine or dobutamine. In case of conduction disturbances, the administration of atropine, isoprenaline or the establishment of an artificial pacemaker is indicated. With the development of heart failure - intravenous administration of strophanthin. Catecholamines should be used only in case of life-threatening circulatory failure (due to their reduced efficacy, a high dosage is required, as a result of which the risk of increased tendency to arrhythmias due to intoxication increases).

It is recommended to control the content of glucose in the blood and electrolytes (potassium ions, calcium), since the release of insulin is impaired. Hemodialysis is not effective.

Interaction with other drugs

The severity of the decrease in blood pressure increases with the simultaneous use of other antihypertensive drugs, nitrates, cimetidine (to a lesser extent, ranitidine), inhalation anesthetics and tricyclic antidepressants.

Drugs from the group of blockers of "slow" calcium channels can further enhance the negative inotropic effect (decrease in the force of heart contraction) of antiarrhythmic drugs such as amiodarone and quinidine.

Nifedipine causes a decrease in the concentration of quinidine in the blood plasma; after discontinuation of nifedipine, a sharp increase in the concentration of quinidine may occur.

Increases the plasma concentration of digoxin and theophylline, in connection with which the clinical effect and the content of digoxin and theophylline in the blood plasma should be monitored.

Inducers of microsomal liver enzymes (rifampicin, etc.) reduce the concentration of nifedipine.

In combination with nitrates, tachycardia increases. The hypotensive effect is reduced by sympathomimetics, non-steroidal anti-inflammatory drugs (suppression of Pg synthesis in the kidneys and retention of Na+ and fluid in the body), estrogens (fluid retention in the body). Calcium supplements can reduce the effect of slow calcium channel blockers.

Nifedipine can displace drugs with a high degree of binding from the connection with proteins (including indirect anticoagulants - coumarin and indandione derivatives, anticonvulsants, nonsteroidal anti-inflammatory drugs, quinine, salicylates, sulfinpyrazone), as a result of which their concentration in blood plasma may increase ...

Suppresses the metabolism of prazosin and other alpha-blockers, as a result of which the hypotensive effect may be enhanced.

Nifedipine inhibits the excretion of vincristine from the body and can increase the side effects of vincristine; if necessary, the dose of vincristine is reduced.

Lithium preparations can increase toxic effects (nausea, vomiting, diarrhea, ataxia, tremors, tinnitus).

Procainamide, quinidine, and other drugs that cause prolongation of the QT interval may increase the risk of a significant prolongation of the QT interval.

Grapefruit juice inhibits the metabolism of nifedipine in the body, and therefore, their simultaneous intake is contraindicated.

Special instructions

During the period of treatment, it is necessary to refrain from taking ethanol.

It is recommended to stop treatment with the drug gradually.

It should be borne in mind that angina pectoris may occur at the beginning of treatment, especially after the recent abrupt withdrawal of beta-blockers (the latter should be withdrawn gradually).

The simultaneous appointment of beta-blockers must be carried out under conditions of close medical supervision, since this can cause an excessive decrease in blood pressure, and in some cases - an aggravation of the symptoms of heart failure.

With severe heart failure, the drug is dosed with great care.

Diagnostic criteria for prescribing the drug for vasospastic angina pectoris are: the classic clinical picture, accompanied by an increase in the ST segment, the occurrence of ergonovine-induced angina pectoris or spasm of the coronary arteries, the detection of coronary spasm by angiography or the detection of an angiospastic component without confirmation (for example, with different stress thresholds or with unstable angina pectoris, when electrocardiogram data indicate transient angiospasm).

For patients with severe obstructive cardiomyopathy, there is a risk of increased frequency, severity and duration of angina attacks after taking nifedipine; in this case, it is necessary to cancel the drug.

In patients on hemodialysis, with high blood pressure, irreversible kidney failure, with a reduced total amount of blood, the drug should be used with caution, a sharp drop in blood pressure may occur.

Patients with impaired liver function are closely monitored and, if necessary, the dose of the drug is reduced and / or other dosage forms of nifedipine are used.

If during therapy the patient needs to undergo surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy.

During treatment, positive results are possible with a direct Coombs reaction and laboratory tests for antinuclear antibodies.

Caution should be taken simultaneously with disopyramide and flecainamide due to a possible increase in the inotropic effect.

Effects on the ability to drive a car and other mechanisms

In some patients, especially at the beginning of treatment, the drug may cause dizziness, which reduces the ability to drive a car or other mechanisms. In the future, the degree of restrictions is determined depending on the individual tolerance of the drug.

Contraindications

Hypersensitivity to nifedipine or other dihydropyridine derivatives, other components of the drug, cardiogenic shock (risk of myocardial infarction), collapse, severe aortic stenosis, chronic heart failure (in the stage of decompensation), severe arterial hypotension (systolic blood pressure below 90 mm Hg Art.), acute period of myocardial infarction (during the first 4 weeks), pregnancy (during the first 20 weeks), lactation, age up to 18 years (efficacy and safety have not been established).

With care: severe stenosis of the aortic orifice or mitral valve, hypertrophic obstructive cardiomyopathy, severe bradycardia or tachycardia, sick sinus syndrome, malignant arterial hypertension, mild or moderate arterial hypotension, myocardial infarction with left ventricular failure, unstable angiotensin cardiac glycosides, concomitant use of rifampcin, severe cerebrovascular accident, liver and / or kidney dysfunction, hemodialysis (risk of arterial hypotension), old age, gastrointestinal obstruction, pregnancy after 20 weeks.

Pregnancy and lactation

The appointment of nifedipine to pregnant women is indicated only if the intended benefit to the mother outweighs the potential risk to the fetus.

Nifedipine is not recommended during the first 20 weeks of pregnancy.

The drug is excreted in breast milk, therefore it is recommended to stop breastfeeding while taking the drug. There are no data on the use of Calcigard retard by lactating women.

Side effect

From the side of the cardiovascular system: Manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, development or worsening of heart failure, "flushing" of blood to the skin of the face, flushing of the skin of the face, feeling of heat), tachycardia, palpitations, arrhythmia, peripheral edema, pain in the chest. Rarely - an excessive decrease in blood pressure, fainting, in some patients, especially at the beginning of treatment, angina attacks may occur, which requires discontinuation of the drug; described isolated cases of myocardial infarction.

From the side of the central nervous system: Headache, dizziness, increased fatigue, weakness, drowsiness. With prolonged intake in high doses, paresthesia of the extremities, depression, anxiety, extrapyramidal (parkinsonian) disorders (ataxia, "mask-like" face, shuffling gait, stiffness of the arms and legs, tremors of the hands and fingers, difficulty swallowing).

From the digestive system: Dry mouth, increased appetite, dyspepsia (nausea, diarrhea or constipation). Rarely - gingival hyperplasia (bleeding, soreness, swelling). With prolonged use - liver dysfunction (intrahepatic cholestasis, increased activity of hepatic enzymes).

From the side of hematopoietic organs: anemia, asymptomatic agranulocytosis, thrombocytopenia, thrombocytopenic purpura, leukopenia.

Allergic reactions: Rarely - skin itching, urticaria, exanthema, exfoliative dermatitis, photodermatitis. Very rarely - autoimmune hepatitis.

From the side of the musculoskeletal system: arthritis, arthralgia (rarely), joint swelling, myalgia, cramps of the upper and lower extremities.

From the urinary system: increased daily urine output, deterioration of renal function (in patients with renal failure).

Others: Rarely - difficulty breathing, cough; very rarely - visual impairment (including transient blindness at the maximum concentration of nifedipine in the blood plasma), gynecomastia (in elderly patients, completely disappearing after discontinuation of the drug), hyperglycemia, galactorrhea, pulmonary edema, bronchospasm, weight gain.