Lozap, 100 mg 90 pcs.

Lozap is a hypotensive.

Pharmacodynamics

The hypotensive drug, is a specific angiotensin II receptor antagonist (AT₁ subtype). Does not inhibit kinase II, an enzyme that degrades bradykinin. Reduces RPS, blood concentrations of adrenaline and aldosterone, BP, pressure in the small circulatory circle; reduces post-load, has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with heart failure.

After a single dose, the hypotensive effect (decreases cAH and dAH) reaches a maximum after 6 hours, then gradually decreases over 24 hours.

The maximum hypotensive effect is reached 3-6 weeks after initiation of the drug.

Pharmacological data indicate that plasma concentrations of losartan are significantly increased in patients with cirrhosis, so patients with a history of liver disease should be prescribed at a lower dose.

Pharmacokinetics

Lozartan is rapidly absorbed from the GI tract. Bioavailability is about 33%. It has “first pass” effect through liver, metabolized by carboxylation with participation of CYP2C9 isoenzyme of cytochrome P450 with formation of active metabolite. Binding to plasma proteins is 99%. Time to reach C_max losartan – 1 hour, active metabolite – 3-4 hours after oral administration. T_1/2 is 1.5-2 h and its main metabolite is 6-9 h, respectively. About 35% of the dose is excreted with the urine, about 60% – through the intestine.

Indications

Arterial hypertension; heart failure (as part of combined therapy, with intolerance or ineffective therapy with ACE inhibitors).

Active ingredient

Composition

Active ingredient: potassium losartan 100 mg;

Auxiliary substances:

core:

MCC, 160 mg;

mannitol, 100 mg; crospovidone, 20 mg;

Colloidal anhydrous silica – 4 mg;

talc – 8 mg; magnesium stearate – 8 mg.

Film coating:

Sepiphilm 752 (white) (hypromellose, MCC, macrogol 2000 stearate, titanium dioxide) – 13.8 mg;

macrogol 6000 – 0.2 mg

How to take, the dosage

Ingestion, regardless of meals. Frequency of administration – once a day.

In case of arterial hypertension, the average daily dose is 50 mg. In some cases, to achieve a greater effect, the dose is increased to 100 mg in 2 doses or once a day.

The starting dose for patients with heart failure is 12.5 mg once daily. Typically, the dose is increased at weekly intervals (i.e., 12.5 mg/day, 25 mg/day, and 50 mg/day) to an average maintenance dose of 50 mg once daily, depending on patient tolerance.

When the drug is administered to patients receiving high-dose diuretics, the starting dose of Lozap should be reduced to 25 mg once daily.

There is no need to adjust the dose in elderly patients or patients with impaired renal function, including patients on hemodialysis.

Patients with impaired liver function should be prescribed lower doses of Lozap.

In elderly patients as well as in patients with impaired renal function, including patients on dialysis, there is no need to adjust the initial dose.

Interaction

Can be administered with other hypotensive agents.

No clinically significant interaction with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital has been noted.

In patients with dehydration (previous treatment with high doses of diuretics) a significant decrease of BP may occur.

It potentiates (mutually) the effect of other hypotensive agents (diuretics, beta-adrenoblockers, sympatholytics).

Induces risk of hyperkalemia when combined with potassium-saving diuretics and potassium preparations.

Special Instructions

Correction of dehydration should be performed before prescribing Lozap or treatment should be started with a lower dose of the drug.

The drugs affecting the renin-angiotensin system may increase blood urea and serum creatinine concentrations in patients with bilateral renal stenosis or arterial stenosis of the single kidney. Blood potassium concentration should be regularly monitored during treatment, especially in elderly patients with impaired renal function.

Contraindications

Side effects

Nervous system and sensory organs: 1% or more – dizziness, asthenia, fatigue, headache, insomnia; less than 1% – anxiety, sleep disturbance, drowsiness, memory disturbance, peripheral neuropathy, paresthesia, hypoesthesia, migraine, tremor, ataxia, depression, syncope, tinnitus, taste disturbance, vision changes, conjunctivitis.

Respiratory system: 1% or more – nasal congestion, cough*, upper respiratory tract infections (elevated body temperature, sore throat, sinusopathy*, sinusitis, pharyngitis); less than 1% – dyspnea, bronchitis, rhinitis.

Gastrointestinal organs: 1% or more – nausea, diarrhea*, dyspeptic phenomena*, abdominal pain; less than 1% – anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.

Musculoskeletal system: 1% or more – cramps, myalgia*, pain in the back, chest, legs; less than 1% – arthralgia, pain in the shoulder, knee, arthritis, fibromyalgia.

Cardiovascular system: orthostatic hypotension (dose-dependent), palpitation, tachy or bradycardia, arrhythmia, angina pectoris, anemia.

Urogenital system disorders: less than 1% – urgent urge to urinate, urinary tract infections, impaired renal function, impaired libido, impotence.

Skin disorders: less than 1% – dry skin, erythema, flushing, photosensitization, increased sweating, alopecia.

Allergic reactions: less than 1% – urticaria, rash, pruritus, angioedema, including face, lips, pharynx and/or tongue.

Others: hyperkalemia (serum potassium >5.5 mmol/l).

Overdose

Symptoms: marked BP decrease, tachycardia, bradycardia may occur due to parasympathetic (vagus) stimulation.

Treatment: forced diuresis, symptomatic therapy; hemodialysis is not effective.

Similarities