Pharmacodynamics of Zestoretic:
Combined antihypertensive drug.
Derivative of benzothiadiazepine selectively blocks the transport system of sodium ions, potassium and chlorine, stopping its transport across the apical membrane into cells of the epithelium of the thick segment of ascending part of Henles loop. The suppression of the re-absorption of ions leads to their excretion from the body. Ions of calcium and magnesium are excreted simultaneously with the ions of sodium, potassium and chlorine. Hypocalcemia does not develop due to active re-absorption in the distal convoluted canalize of the Henles loop.
It is effective in case of any fluctuations of acid-base balance, preserves a diuretic effect both in case of acidosis and alkalosis.
The drug blocks the conversion of angiotensin I to angiotensin II, resulting in decreased release of norepinephrine from the endings of sympathetic fibers, vasoconstrictor effect, secretion of aldosterone by the adrenal cortex and increase of the amount of bradykinin by decreasing its inactivation of angiotensin converting enzyme.
Bradykinin stimulates B2-kinin receptors in vascular endothelium, leading to rapid release of prostacyclin and other vasodilator substances that cause smooth muscle relaxation.
It reduces the total peripheral vascular resistance without affecting heart rate.
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Pharmacokinetics of Zestoretic:
80 % the drug is absorbed in the gastrointestinal tract after ingestion on an empty stomach. The maximum concentration in plasma is achieved in 2 hours. Connection with plasma proteins is 40 %.
The therapeutic effect develops in 2 hours after intake and lasts for 8-12 hours. It penetrates through the blood-brain and placental barrier, and is excreted in breast milk. Metabolism occurs in the liver.
The half-life is 6.4 hours. It is eliminated by the kidneys, about 75% in an unmodified form.
The therapeutic effect develops within 1 hour after ingestion, reaches its maximum after 6 hours and lasts for 24 hours. It doesn’t cause the withdrawal syndrome. It penetrates through the blood-brain and placental barrier, and is excreted in breast milk. It is not metabolized.
The half-life is 12 hours. Elimination occurs in the kidneys in unchanged form.
Indications for use:
It is used to treat hypertension.
Severe renal and hepatic failure, congenital angioedema (or in anamnesis), patients undergoing haemodialysis, pregnancy and lactation, age under 18, hypersensitivity.
Zestoretic is used with caution in case of:
Bronchial asthma, ischemic heart disease, gout, psoriasis, systemic connective tissue diseases, hypersensitivity
Pregnancy and lactation:
Recommendations for the FDA are category D. The drug is contraindicated in case of pregnancy and lactation.
Method of application and dose:
The drug is taken inside at the dosage of 1 tablet (hydrochlorothiazide/lisinopril: 12,5/5 mg and 12.5/10 mg and 12.5-20 mg) 1 times a day.
The highest daily dose: 1 tablet of 12.5 mg of hydrochlorothiazide and 20 mg of lisinopril.
The highest single dose: 1 tablet of 12.5 mg of hydrochlorothiazide and 20 mg of lisinopril.
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Side effects of Zestoretic:
Central and peripheral nervous system: headache, dizziness, depression, sleep disturbances, paresthesia.
Respiratory system: pneumonia, pulmonary edema.
Hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia, hemolytic anemia.
Cardiovascular system: orthostatic hypotension, rarely – arrhythmia.
Musculoskeletal system: cramps of calf muscles.
Dermatological reactions: photosensitivity, rash, and rarely toxic epidermal necrolysis.
Senses: blurred vision.
Urinary system: glycosuria, hyperuricemia.
Reproductive system: impotence.
Central and peripheral nervous system: headache, dizziness, sleep disturbances, paresthesia, confusion.
Respiratory system: dry cough, shortness of breath, sinusitis, bronchospasm.
Hematopoietic system: anemia, thrombocytopenia, agranulocytosis, pancytopenia.
Cardiovascular system: hypotension, tachycardia, rarely – pain in the chest, flushing.
Digestive system: glossitis, vomiting, diarrhoea, constipation, rarely – hepatitis, cholestatic jaundice, pancreatitis.
Musculoskeletal system: myalgia, cramps of calf muscles.
You may buy Zestoretic at our website in any quantity.
Zestoretic dermatological reactions: rash.
Special senses: tinnitus, breach of taste perception, blurred vision.
Urinary system: dysuria, rarely – acute renal failure.
Reproductive system: erectile dysfunction.
It enhances the effects of depolarizing muscle relaxants.
Patients with diabetes require the correction doses of oral hypoglycemic agents and insulin preparations in case of the reception of hydrochlorothiazide.
It increases hypoglycemic effect of corticosteroids, adrenocorticotropic hormone, carbenoxolone, amphotericin b, cardiac glycosides.
Anticholinergic drugs increase the bioavailability of hydrochlorothiazide.
The simultaneous use with the lithium drug may cause a manifestation of a paradoxical antidiuretic effect.
The simultaneous use of vitamin D and calcium may develop hypercalcemia.
The simultaneous use of cyclosporine increases the risk of development of gout and hyperuricemia.