Dynacirc CR Calcium-channel blocker of the dihydropyridine group. Yellow powder. Insoluble in water, soluble in alcohol, acetone, chloroform.
Pharmacology Dynacirc CR
Pharmacological action – hypotensive, vasodilating. Blocks calcium channels, inhibits the entry of calcium ions into smooth muscle cells of the vascular wall and miokardiotsity, reduces their ability to contract. Exhibits selectivity for vascular smooth muscle compared with myocardium. Lowering the concentration of calcium ions into vascular smooth muscle cells leads to expansion of the coronary arteries and peripheral arteries and arterioles. The hypotensive effect caused mainly vasodilation and a decrease in PR, is accompanied by reflex tachycardia, which masks the negative inotropic effect. Does not inhibit the sinoatrial or atrioventricular node. It has a diuretic (increase urine output mechanism is unclear). Antihypertensive effect persists for 12 hours after a single dose and reaches a maximum after 2-4 weeks of the course application.
If ingestion is absorbed by 95%. Taking into account the bioavailability of “first pass” through the liver is 15-24% (may be increased in people older than 65 years). Cmax is achieved in 1.5 h. Bound to plasma proteins at 95%. Completely metabolized to form six metabolites. Excreted in the urine (60-65%) and faeces (25-30%) in the form of metabolites. Passes into breast milk. It has no embryotoxic, teratogenic, carcinogenic and mutagenic.
Application of the Dynacirc CR
Hypertension.
Contraindications Dynacirc CR
Hypersensitivity, shock, unstable angina, acute myocardial infarction (first 4 weeks), liver (hepatitis), severe renal impairment (Cl creatinine
Restrictions apply Dynacirc CR
Decompensated heart failure, the value of SBP
Pregnancy and breastfeeding Dynacirc CR
Contraindicated in pregnancy.
Category of the fetus by FDA – C.
At the time of treatment should stop breastfeeding.
Side effects Dynacirc CR
Cardio-vascular system and blood (hematopoiesis, hemostasis): flushing the face, tachycardia, chest pain, angina (especially at the beginning of treatment), hypotension, anemia, leukopenia, thrombocytopenia, rarely – bradycardia, thrombocytopenic purpura, in some cases – a myocardial infarction.
The nervous system and sensory organs: fatigue, nervousness, headache, dizziness, blurred vision, is rare – anxiety.
Urogenital system: peripheral edema (legs, feet), increased urinary frequency, impotence.
From the digestive tract: dry mouth, nausea, epigastric discomfort, intestinal, diarrhea, liver damage, is rare – loss of appetite, hepatitis.
The respiratory system: cough, bronchospasm, including accompanied by a lack of air.
Allergic reactions: pruritus, urticaria, eczema, and rare – angioedema.
Other: gynecomastia, weight gain, rash, elevated liver enzymes, rare – hyperglycemia, arthralgia, very rarely – gingival hyperplasia.
Interaction Dynacirc CR
Strengthens the hypotensive effect of antihypertensive drugs (including diuretics, propranolol). Increases the plasma level of digoxin, cyclosporine, theophylline and reduces – quinidine. Potentiates the negative inotropic effect of quinidine and amiodarone. Cimetidine and ranitidine (increased levels in plasma), anesthetic facilities, fentanyl increase hypotension. Anticonvulsants (including phenytoin, carbamazepine) decrease in plasma concentration of rifampicin accelerates the metabolism.
Overdose Dynacirc CR
Symptoms: severe hypotension, cardiac failure, shock, pulmonary edema, tachycardia or bradycardia, increased central venous pressure, dizziness, headache, disorders of consciousness (even coma), mydriasis with preservation of response to light, hyperglycemia, metabolic acidosis.
Treatment: gastric lavage, activated charcoal assignment, the maintenance function of the cardiovascular system, including administration of calcium gluconate, dobutamine, norepinephrine, atropine and beta-agonists (at a bradycardia), plasma substitutes. Requires monitoring functions of the heart and lungs, control of BCC and diuresis. Hemodialysis is ineffective.
Dosage and administration Dynacirc CR
Inside, the initial dose – 2.5 mg 2 times a day, with liver and renal failure in elderly patients – 1.25 mg. In the case of lack of efficacy within 2-4 weeks may increase the dose to 5 mg (in rare cases up to 10 mg) 2 times a day. The maximum daily dose – 20 mg.
Precautions Dynacirc CR
In patients with diabetes, early treatment is recommended to control blood glucose levels. With caution and only in cases of urgent need to appoint functional disorders of the liver and kidney damage, congestive heart failure, sick sinus. Should refrain from the use in pediatric patients, as safety and efficacy in children is not defined.
