Composition and release form
The drug Lozap is available in the form of small tablets for parenteral administration. They are white, slightly elongated and convex on both sides. They have a soluble thin film shell. Packaged in blisters of 10 pieces. One cardboard package contains 3, 6, 9 blisters and includes instructions for use.
The active substance is potassium losartran.
Auxiliary components: cellulose, povidone, talc, magnesium stearate, macrogol, dyes, mannitol, croscarmellose sodium.
What is the advantage of Lozap Plus over Lozap
The indications for these drugs are the same. But Lozap is a single drug, and its “brother” with the Plus prefix is a combined drug. The latter operates on the basis of losartan potassium and hydrochlorothiazide. The second ingredient has diuretic properties, enhancing the effectiveness of the antihypertensive component.
Doctors prefer to prescribe this remedy to people with severe hypertension, as well as to patients with left ventricular hypertrophy. This medicine reduces the risk of death in people who have experienced a hypertensive crisis.
Significant differences between medications:
- Lozap plus has a more pronounced antihypertensive effect;
- regular Lozap has a smaller list of contraindications and adverse reactions, which is explained by the active component in the formula alone;
- Lozap is used by diabetics, and Lozap plus is prescribed for endocrine pathologies with great caution;
- Lozap plus is less favorable in terms of price, since it uses two components.
The doctor decides which medicine to choose - this is purely his area of responsibility.
pharmachologic effect
The drug belongs to the group of antihypertensive drugs. It is a specific angiotensin receptor agonist. After taking the medicine, there is a decrease in vascular resistance, a decrease in aldosterone and adrenaline levels in the bloodstream. In addition, the pressure in the pulmonary circulation is normalized, a pronounced diuretic effect occurs and the afterload on the body is reduced.
The drug prevents the development of hypertrophy of the muscular lining of the heart and improves people's susceptibility to physical activity.
While taking the drug, the angiotensin-containing enzyme is not blocked. Therefore, the level of bradykinin does not increase and the effect on the kinin system is prevented.
The pharmacological effect of the drug is the same for all patients, regardless of age and gender.
After one dose of medication, the hypotensive effect is observed after 6 hours and gradually decreases throughout the day. When a course is prescribed, pronounced results of therapy appear in patients after 3-4 weeks.
People suffering from liver cirrhosis should be careful when using antihypertensive drugs. The active ingredient occurs in their blood. Therefore, they need dose adjustment.
After oral administration, the tablets are quickly absorbed. The maximum content of the drug in the body is recorded after an hour. The drug is administered through the kidneys and intestines.
Lozap, 90 pcs., 50 mg, film-coated tablets
Hypersensitivity.
Patients with a history of angioedema (swelling of the face, lips, pharynx and/or tongue) should be closely monitored.
Arterial hypotension and water-electrolyte imbalance.
Symptomatic hypotension, especially after the first dose or after dose increases, may occur in patients with hypovolemia and/or hyponatremia as a result of high-dose diuretics, a low-salt diet, diarrhea, or vomiting.
It is necessary to either correct these conditions before prescribing Lozap®, or use initial doses of the drug.
Water and electrolyte disturbances.
Water and electrolyte disturbances are typical for patients with impaired renal function in combination with or without diabetes mellitus and require correction. In a clinical study conducted in type 2 diabetic patients with nephropathy, the incidence of hyperkalemia in the losartan group was higher than in the placebo group. This indicates the need for constant monitoring of potassium levels in the blood plasma and creatinine Cl levels - patients with heart failure and creatinine Cl levels from 30 to 50 ml/min require especially strict monitoring.
Prescribing potassium-sparing diuretics, potassium supplements and potassium-containing salt substitutes simultaneously with Lozap® is not recommended.
Liver dysfunction.
Taking into account pharmacokinetic data indicating a significant increase in plasma concentrations of losartan in patients with cirrhosis, patients with a history of impaired liver function (more than 9 points on the Child-Pugh scale) are recommended to prescribe the drug in lower doses. There is no experience with the use of the drug in patients with severe liver failure. Taking this into account, Lozap® is contraindicated in patients with severe liver failure.
Double blockade of the RAAS.
There is evidence that the simultaneous use of ACE inhibitors, ARB II or aliskiren increases the risk of arterial hypotension, hyperkalemia and renal dysfunction (including acute renal failure).
The use of Lozap® in combination with aliskiren is contraindicated in patients with diabetes mellitus and/or moderate or severe renal failure (GFR <60 ml/min/1.73 m2) and is not recommended in other patients (see “Contraindications”).
The use of Lozap® in combination with an ACE inhibitor is contraindicated in patients with diabetic nephropathy and is not recommended for other patients (see “Contraindications”).
IHD and cerebrovascular diseases.
As with the use of any antihypertensive drugs, too sharp a decrease in blood pressure in patients with coronary artery disease and cerebrovascular diseases can lead to myocardial infarction or ischemic stroke.
Heart failure.
In patients with heart failure with or without renal impairment, as with other drugs acting on the RAAS, there is a risk of developing severe hypotension and acute renal failure.
experience with the use of losartan in the treatment of patients with heart failure and concomitant severe renal failure in patients with severe CHF (functional class IV according to the NYHA
), as well as in patients with heart failure and life-threatening arrhythmias. With this in mind, caution should be exercised when prescribing losartan to these categories of patients.
Combined use with ACE inhibitors for CHF.
When using Lozap® in combination with ACE inhibitors, the risk of side effects may increase, especially renal dysfunction and hyperkalemia (see “Side Effects”). In these cases, careful observation and monitoring of laboratory parameters is necessary.
Hemodialysis.
During hemodialysis, the sensitivity of blood pressure to the action of AT1 receptor antagonists increases as a result of a decrease in blood volume and activation of the RAAS. It is necessary to adjust the dose of Lozap® under careful monitoring of blood pressure in patients on hemodialysis.
Kidney transplantation.
There are no data on the use of Lozap® in patients who have recently undergone a kidney transplant.
General anesthesia.
Patients receiving ARA II during general anesthesia and surgical procedures may develop arterial hypotension as a result of blockade of the RAAS. Very rarely, cases of severe arterial hypotension may occur, requiring IV fluids and/or vasopressors.
Aortic and mitral valve stenosis, hypertrophic obstructive cardiomyopathy.
When using the drug Lozap®, as well as other vasodilators, caution should be exercised in patients with hypertrophic obstructive cardiomyopathy or hemodynamically significant stenosis of the aortic or mitral valve.
Primary hyperaldosteronism.
Patients with primary hyperaldosteronism are usually resistant to treatment with antihypertensive drugs that affect the RAAS. In this regard, Lozap® is not recommended for use in such patients.
Elderly patients.
As a rule, patients over 75 years of age are recommended to start treatment with Lozap® with a dose of 25 mg/day.
Other special instructions and precautions.
As clinical experience with the use of ACE inhibitors, losartan and other AT1 receptor antagonists shows, these drugs are less effective in reducing blood pressure in patients of the Negroid race than in representatives of other races, possibly due to low renin activity in patients of this race.
Impact on the ability to drive vehicles and machinery.
Not studied. When driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, it should be taken into account that when using the drug, dizziness, drowsiness and fainting may occur.
Lozap indication
The use of Lozap is relevant for the following conditions:
- High blood pressure.
- Chronic course of heart failure.
- Prevention of the development of severe vascular and cardiac diseases among patients with hypertension and left ventricular enlargement.
- Nephropathy and high blood pressure in people with diabetes.
- Contraindications
- Absolute contraindications for use are:
- Increase in potassium levels in the blood.
- Low pressure.
- Individual intolerance to the medicinal components included in the composition.
- The time of bearing a child.
- Breastfeeding.
- Symptoms of dehydration.
- Children under 18 years of age.
At what blood pressure is it taken?
The annotation does not contain clear information about the range of pressure indicators that will be the target for Lozap. This means that only the physician who supervises the patient’s treatment can decide whether Lozap will be effective in a particular case.
There are drugs that can be used only in the early stages of hypertension, and there are those that correct high blood pressure values inherent in severe disease. And there are such means as Lozap, where there are no clear instructions in this aspect of the purpose.
However, it is known that more severe cases of hypertension require complex therapy, that is, more often in such a situation the doctor will prescribe the same Lozap plus.
Side effects
As a rule, during the course of therapy, patients experience virtually no side effects. If they appear, they go away on their own and quickly, so there is no need to discontinue the drug. The following side effects are possible when taking Lozap:
- Dizziness, increased fatigue, headache, problems falling asleep. Migraines, anxiety, tremor, and depression are less common.
- Infection of the respiratory system. Signs of rhinitis, bronchitis and respiratory distress may appear.
- Dyspeptic symptoms, rarely gastritis, dry mouth, flatulence.
- Disturbance of the musculoskeletal system. Possible pain in the back and muscles, cramps.
- Signs of cardiac dysfunction are expressed in tachycardia, bradycardia, arrhythmia.
- Rarely, kidney problems, sexual dysfunction and infections of the urinary system appear.
- Allergic reactions, dry dermis, excessive sweating.
Negative reactions with long-term use
Prolonged use of the drug can lead to disorders of various organs and systems. This is due to the accumulation of the basic substance in the body.
Violations may be:
- Allergies in areas of special dermal sensitivity;
- Hair loss associated with increased dermal sensitivity and hyperhidrosis;
- Heartache;
- Nosebleeds;
- Malfunctions of the digestive organs - from flatulence and constipation to diarrhea and problems with appetite;
- Dysfunction of sensors, for example, smell, as well as taste buds;
- State of unreasonable anxiety;
- Frequent urination and false urge to urinate.
If such negative reactions occur, the doctor will either reduce the dosage or replace the medicine with a safer one.
Instructions for use of Lozap
The medicine is intended for oral administration, regardless of the time of meal. It is recommended to take the tablets once a day.
For severe hypertension, patients are prescribed 50 mg. According to clinical indications, the dosage can be doubled.
According to the attached instructions, in case of cardiac insufficiency, patients are prescribed 12.5 mg once a day. Every week the dose of the drug is increased by 2 times until it reaches 50 mg per day.
In cases where patients are simultaneously taking diuretic drugs, the therapeutic dose of Lozap should be reduced to 25 mg.
Elderly people and those with kidney problems do not need to change the therapeutic dosage.
Pharmacokinetics of the active substance
Once the component is in the digestive tract, it is well absorbed in these structures. The bioavailability of the main ingredient is 33%. It is not so important whether the intake is tied to food (the main requirement is to take the tablet at the same time).
The effect of “primary passage” through the liver is detected. It is metabolized with the formation of a specific metabolite, which has more pronounced hypotensive activity (tens of times), and also with the formation of an inactive metabolite.
The maximum content in the blood plasma is detected an hour after consumption. Peak values of the main metabolite are noticeable after three to four hours. More than 98% of the main ingredient and its active metabolite bind to plasma blood proteins (mostly albumin).
Losartan does not actually cross the BBB. The elimination period of losartan and the active metabolite is one and a half to two and a half hours. The active component is excreted by the renal and intestinal routes (approximately in the ratio of 35% urine/60% feces-bile). If a single dose does not exceed 100 mg, then Lozap and its composition do not create significant accumulations in plasma.
Interactions with drugs
Combining the drug with Fluconazole and Rifampicin leads to a decrease in the active substance.
Lozap increases the pharmacological activity of other antihypertensive drugs.
It is not recommended to take the medicine in parallel with non-steroidal anti-inflammatory drugs.
When interacting with potassium and potassium-sparing diuretics, it is important to monitor the level of the element in the blood to prevent the occurrence of hyperkalemia.
Patients with obvious symptoms of dehydration while taking diuretics may experience a rapid decrease in blood pressure when taking an antihypertensive drug.
Are there any advantages of Lozap over other means?
Comparative characteristics can never be taken as unconditional, because in each such assessment there will be many remarks. Lozap is indeed a good hypertensive drug, but in one case it will be enough and the predicted effectiveness will be fully justified. In another case, it will not give maximum effect, and doctors will look for another targeted remedy.
On average, cardiologists note that the drug is well tolerated by patients with CHF: it helps regulate tolerance to emotional and physical stress. The medicinal product reduces the level of adrenaline in the patient’s blood, and it also allows the heart to enlarge, i.e. Lozap prevents myocardial hypertrophy from developing.
