Pharmacological Effects Monopril:
Monopril – antihypertensive group of angiotensin-converting factor (APF). Active substance is monopril ester – fosinopril. Fosinopril after absorption into the blood esterases hydrolyzed to form the active metabolite fozinoprilata. Inhibition of angiotensin is due to binding of the phosphate group of fosinopril with angiotensin-converting factor, which reduces the pressor action of aldosterone and reduce its concentration in the blood. In this case, an increase of potassium content in blood serum and the loss of sodium and water excretion.
Fosinopril also inhibits metabolic destruction of bradykinin, thereby potentiated the hypotensive effect of monopril. Monopril increases resistance to physical stress, can reduce the severity of heart failure.
Hypotensive effect is not accompanied by changes in cerebral, renal blood flow and BCC. No effect on reflex activity of myocardium, does not violate the circulation in the internal organs, skin and skeletal muscle. Reduction in blood pressure after an oral monopril reaching a peak after 3-6 hours and lasts for days.
Heart failure monopril has a positive effect by inhibition of the renin-aldosterone system. Decreases as the preload on the heart muscle, and afterload.
Absorbability from the gastrointestinal tract is 30-40%. The ability of absorption is not dependent on consumption of food, but taking the drug before a meal slows absorption. Fozinoprilata maximum concentration in plasma observed after 3 hours after oral administration and does not depend on the dose of the drug.
Associated plasma protein 95% fosinopril. Metabolism occurs in the hepatocytes and the mucosa of the gastrointestinal tract.
Elimination of fosinopril is excreted in urine and, to a lesser extent in the bile. The half-life of approximately 11.5 hours. Heart failure, this figure increases to 14 hours.
When changes of renal function decreases elimination fozinoprilata 2 times more likely than patients without renal failure. In this case, absorption, protein binding and bioavailability do not change. Reduction of excretion by the kidneys fozinoprilata offset excretion in the bile in large quantities.
When held hemodialysis clearance fozinoprilata average 2% (for peritoneal dialysis, respectively, 7%) with respect to urea clearance.
In patients with impaired liver function (cirrhosis) decreased biotransformation of fosinopril in fozinoprilat, but the extent of metabolism remains the same. Clearance of the metabolite in these patients is 2 times slower compared with patients without impaired liver function.
Indications Monopril:
• Hypertension (both as monotherapy and in combined treatment in combination with a thiazide diuretic group);
• Combination therapy of heart failure.
How to use Monopril:
Apply inside. The dosage is set by the doctor individually.
Hypertension. The starting dose – 10 mg / day. However, the dosage can be changed depending on the degree of hypotensive action of 10 to 40 mg / day (only once). In case of failure also received a thiazide diuretic.
If the patient is already taking a diuretic before therapy monoprilom, the last dose should not exceed 10 mg / day (at constant medical monitoring patient response).
Chronic heart failure. The recommended starting dose is 5 mg 1-2 times a day. In the absence of proper effect to increase the dosage after 1 week up to a maximum of 40 mg / day.
Abnormal liver function and / or kidneys do not require a change in dosage. Patients older than 65 years have seen an increased susceptibility to monoprilu and reduced clearance rate, which requires reducing the dose if needed.
Side effects Monopril:
Urinary system: risk of renal failure or worsening of existing PN, the appearance of protein in the urine, disturbance of function of the prostate gland.
Cardiovascular system: orthostatic hypotension, palpitations, angina pectoris, fainting, hot flashes to the upper torso and head, myocardial infarction, heart failure, hypertensive crisis, arrhythmias.
Central nervous system: headache, dizziness, insomnia, weakness, anxiety, memory impairment, paresthesia, confusion, sleepiness, ischemic disorders, stroke.
Gastrointestinal tract: vomiting, nausea, diarrhea, hepatitis, pancreatitis, abdominal pain, cholestasis, constipation, stomatitis, anorexia, glossitis, flatulence, dry mouth, dysphagia, change in body weight.
Hematopoietic system: lymphadenitis.
Respiratory System: bronchospasm, development of pulmonary infiltrates, rhinorrhea, dyspnea, epistaxis, pharyngitis, dysphonia.
Allergic reaction: angioedema, pruritus, rash.
Change in laboratory parameters: an increase in urea, giperkreatinemiya, an increase of transaminases (liver), increased potassium concentration, decrease – sodium gipogemoglobinemiya, decreased hematocrit, leukopenia, ESR increase, eosinophilia, neutropenia.
Other: Gout.
Contraindications Monopril:
• Increased individual sensitivity, an allergic reaction to fosinopril and other components of the drug (can be cross-allergic reactions to other ACE inhibitors, factor);
• pregnancy and lactation;
• Children under 18 years (no data on safety and efficacy of the drug).
Pregnancy:
While taking the drug during pregnancy, the formation of fetal malformation, a sharp decrease in blood pressure in fetal and neonatal renal failure in the fetus, low water, hypoplasia of various skull bones, lung hypoplasia, contractures of hands and feet. Receiving the drug at later stages can also provoke fetal death. Fozinoprilat sucked into breast milk, so if you need to receive monopril breastfeeding is discontinued.
If the mother during pregnancy monopril taken, careful monitoring of the content of potassium in the newborn, the amount of urine and blood pressure.
Interaction with other drugs Monopril:
With simultaneous administration of antacids reduces drug absorption (monopril with aluminum hydroxide, simethicone, magnesium hydroxide and other drugs of this group to make a difference of 2 hours or more).
In combination with lithium salts, an increase of lithium in blood serum and the risk of overdose (with simultaneous reception, you may need to decrease the dose of monopril).
Nonsteroidal anti-inflammatory drugs (indomethacin, acetylsalicylic acid and others) reduce the hypotensive effect of ACE (which is most pronounced in patients with hypertension nizkoreninovogo character).
When you receive monopril with diuretics, as well as in the case of dialysis and diet with salt restriction should be aware that in the first 60 minutes after taking the drug may sharp drop in blood pressure.
Hyperkalaemia is possible in patients taking additional potassium-based drugs, heparin, dietary supplements with potassium and potassium-sparing diuretics (triamterene, amiloride, sporonolakton and others). This is especially in patients with diabetes mellitus, congestive heart failure.
Monopril increases the hypoglycemic effect of insulin and sulfonylureas.
Leukopenia is possible with a combination of monopril with cytostatics, allopurinol, procainamide, immunosuppressants.
Estrogens because of the ability to hold water to inhibit the hypotensive effect of fosinopril.
Potentiate the effects of monopril other antihypertensive drugs, opioids, funds for general anesthesia.
Overdose Monopril:
If overdose is possible an intense decrease in blood pressure, shock, slowing of heart rate, stupor, acute renal failure, violations of water-electrolyte balance. In case of exceeding the dose should stop taking the medicine, rinse the stomach, to appoint chelators, vasopressors, infusion isotonic sodium chloride solution. Next – symptomatic treatment. Hemodialysis is not effective.
Extras:
In renal failure, stenosis of both renal arteries, renal artery stenosis single kidney after renal transplantation in aortic stenosis, systemic connective tissue diseases, hemodialysis, hyponatremia, cerebral circulation insufficiency and other cerebrovascular disease, coronary heart disease, diabetes, heart failure vascular stage III-IV (classification NYHA), inhibition of blood, gout, lower blood volume (vomiting, diarrhea, special diet), gout used with caution.
Before taking this medication is stopped done before antihypertensive therapy for a few days. Diuretics should be discontinued 2-3 days before treatment monoprilom.
Both before and after treatment is necessary to monitor blood pressure, renal function, serum concentrations of potassium, urea, creatinine and other electrolytes and liver transaminases.
With the development of angioedema appoint injection of adrenalin (epinephrine) 1:1000 subcutaneously. Swelling of the mucous of the gastrointestinal tract develop abdominal pain that should be considered in the differential diagnosis of abdominal pain.
Increased risk of allergic reactions when used on a background of monopril high permeability hemodialysis membranes, and in the case anaforeza low density lipoprotein by dextran sulfate.
Patients with high risk of agranulocytosis (renal dysfunction, systemic connective tissue disease – scleroderma, SLE) is carried out regularly to determine the number of leukocytes (1 every 3-6 months and receive a 1-st year of therapy).
Excessive hypotonic effect may develop in the application of monopril in patients with heart failure (risk of oliguria, azotemia fatal). Therefore, the reception of monopril in these patients should be conducted under the supervision of a physician, especially in the first 14 days of treatment, in case of increasing the dosage or supplemental diuretics.
Reducing the dosage of the drug needed in case of hyponatremia. Hypertension is not a contraindication to the appointment of fosinopril (in the first 14 days of possible hypotension, but the numbers of blood pressure then stabilized).
The drug should be discontinued in case of yellowing of the skin (check the level of transaminases).
In patients with renal artery stenosis (or renal artery stenosis single kidney) may increase urea nitrogen and serum creatinine. Such an increase is reversible and goes away after you stop taking fosinopril.
Before performing any anesthesia (even at the dentist), a doctor should warn you that the patient is taking fosinopril.
Also increases the risk of dehydration in hot weather and exercise, what to consider when taking monopril.
Early treatment may dizziness, so drive vehicles and operate complex machinery is not recommended (especially in combination with diuretics).
Attention!
Before using the drug monopril you should consult your doctor. This instruction is given a free transfer and is intended solely for information. For more information, please contact the manufacturer annotations.
