Description
release form
tablets
packaging 30 pcs
Pharmacological action
Immunostimulating drug. It has antiviral activity against DNA and RNA genomic viruses. It has a pronounced antichlamydia effect. The activity of the drug is associated with its ability to induce the formation in the body of high titers of endogenous interferons, especially interferon alpha.
Intramuscular administration of Neovir at a dose of 250 mg for detected serum concentrations of interferon is equivalent to the administration of 6-9 million IU of recombinant interferon alpha.
Neovir activates bone marrow stem cells, T lymphocytes and macrophages. It shows immunomodulatory activity, normalizing the balance between subpopulations of T-helper and T-suppressor cells. With a number of diseases, Neovir is able to reduce the production of tumor necrosis factor (HIV infection, herpes) in the body and activate natural killer cells (in case of tumor diseases). Significantly increases the activity of polymorphonuclear leukocytes.
In case of HIV infection, Neovir has an immunomodulating effect: it increases the absorption activity of blood serum, increases the ability of leukocytes to synthesize interferon alpha, and stimulates the formation of reactive oxygen species by phagocytes.
Peak activity of interferons in the blood and tissues is observed through increases the absorption activity of blood serum, increases the ability of leukocytes to synthesize interferon alpha, stimulates the formation of reactive oxygen species by phagocytes.
Peak activity of interferons in the blood and tissues is observed through increases the absorption activity of blood serum, increases the ability of leukocytes to synthesize interferon alpha, stimulates the formation of reactive oxygen species by phagocytes.
Peak activity of interferons in the blood and tissues is observed throughpaliperidone is an antagonist of 1- and 2-adrenergic receptors and H1-histamine receptors. Paliperidone does not have affinity for cholinergic, muscarinic, and β 1 and β 2 adrenergic receptors. The pharmacological activity of the (+) and ( ) – enantiomers of paliperidone is the same in qualitative and quantitative terms.
Antipsychotic effect due to blockade of D2-dopaminergic receptors of the mesolimbic and mesocortical system. It causes less suppression of motor activity and to a lesser extent induces catalepsy than classical antipsychotics (antipsychotics).
Balanced central antagonism of serotonin and dopamine can reduce the propensity for extrapyramidal side effects and expand the therapeutic effect of the drug, covering the negative and productive symptoms of schizophrenia. In most patients, equilibrium paliperidone concentrations were achieved after 4 5 days of taking the drug once a day. Paliperidone is an active metabolite of risperidone. Features of the release of the active substance from the Invega ® preparation provided smaller fluctuations in the maximum and minimum concentrations of paliperidone than those observed with conventional dosage forms (concentration fluctuation index is 38% compared to 125% for conventional dosage forms).
After taking paliperidone tablets, the (+) and ( ) enantiomers interconvert, and the ratio of AUC – AUC (+) / AUC ( ) – in equilibrium is about 1.6. The absolute bioavailability of paliperidone after oral administration is 28% (23 33% with a confidence interval of 90%). Paliperidone binds predominantly to β 1-acid glycoprotein and albumin.
Biotransformation and elimination of
1 week after taking one standard tablet containing 1 mg paliperidone, 59% of the dose was excreted unchanged in the urine, which indicates that paliperidone is not subjected to intensive metabolism in the liver. About 80% of the drug was found in urine and about 11% in feces. Four in vivo methods of paliperidone metabolism are known, none of which covers more than 6.5% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole cleavage. In vitro studies have shown that the CYP2D6 and CYP3A4 isoenzymes of cytochrome P450 may play a role in paliperidone metabolism, but evidence that they play a significant role in paliperidone metabolism in vivo has not been obtained. Helps reduce left ventricular hypertrophy. It does not affect the plasma lipids (TG, low density lipoproteins, high density lipoproteins) does not affect carbohydrate metabolism (including in patients with concomitant diabetes mellitus). Reduces the sensitivity of the vascular wall to norepinephrine and angiotensin II, stimulates the synthesis of prostaglandin E2, reduces the production of free and stable oxygen radicals. The antihypertensive effect develops by the end of the first week, persists for 24 hours against a background of a single dose.
Indications
Arterial hypertension.
Contraindications
Hypersensitivity to indapamide, other sulfonamide derivatives or other components of the drug, decompensation of renal function (anuria) and / or liver (including encephalopathy), hypokalemia, concomitant use of drugs that extend the QT interval, lactation, age up to 18 years (effectiveness and safety have not been established).
Special instructions
In patients taking cardiac glycosides, laxatives, against the background of hyperaldosteronism, as well as in elderly people, regular monitoring of the content of K + ions and creatinine is shown.
While taking indapamide, the concentration of K +, Na +, Mg 2+ ions in the blood plasma (electrolyte disturbances), pH, the concentration of glucose, uric acid and residual nitrogen should be systematically monitored.
The most careful control is shown in patients with cirrhosis of the liver (especially with edema or ascites – the risk of developing metabolic alkalosis, which increases the manifestations of hepatic encephalopathy), coronary heart disease, heart failure, as well as in the elderly.
The high-risk group also includes patients with an increased QT interval on the electrocardiogram (congenital or developing against the background of any pathological process).
The first measurement of the concentration of K + in the blood should be carried out during the first week of treatment.
Hypercalcemia with indapamide may be due to previously undiagnosed hyperparathyroidism.
In patients with diabetes, it is extremely important to control the level of glucose in the blood, especially in the presence of hypokalemia.
Significant dehydration can lead to the development of acute renal failure (decreased glomerular filtration). Patients need to compensate for water loss and carefully monitor renal function at the beginning of treatment.
Indapamide can give a positive result when conducting a doping control.
Patients with arterial hypertension and hyponatremia (due to diuretics) need to stop taking angiotensin-converting enzyme inhibitors 3 days before taking angiotensin-converting enzyme inhibitors (if necessary, diuretics can be resumed somewhat later), or they are prescribed initial low doses of angiotensin-converting enzyme inhibitors.
Derivatives of sulfonamides can exacerbate the course of systemic lupus erythematosus (must be borne in mind when prescribing indapamide).
Pediatric use: efficacy and safety in children not established.
Ingredient srdldkp 1 mg hypromellose (hypromellose 4000) – 4278.4 mg of lactose monohydrate – 168.5132.1 mg of silicon colloidal dioxide (aerosil) – 1 mg of magnesium stearate – 2 mg
Shell: hypromellose (hydroxypropyl methylcellulose) – 5.94 mg macrogol (polyethylene glycol 4000) – 1.29 mg talc – 0.462 mg titanium dioxide – 1.29 mg dye tropeolin O – 0.018 mg.
Dosage and administration
Tablets are taken orally at a dose of 1.5 mg once a day (in the morning).
If the hypotensive effect is insufficient, after 2 weeks of treatment, the dose is increased to 5 7.5 mg / day.
Maximum dose: 10 mg / day in 2 divided doses (in the morning).
Side effects
From the gastrointestinal tract: possible nausea / anorexia, dry mouth, gastralgia, vomiting, diarrhea, constipation.
From the nervous system: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression rarely – increased fatigue, general weakness, malaise, muscle spasm, tension, irritability, anxiety.
On the part of the sensory organs: conjunctivitis, visual impairment.
From the respiratory system: cough, pharyngitis, sinusitis, rarely – rhinitis.
From the cardiovascular system: orthostatic hypotension, changes in the electrocardiogram (hypokalemia), arrhythmia, palpitations.
From the urinary system: frequent infections, nocturia, polyuria.
Allergic reactions: rash, urticaria, pruritus, hemorrhagic vasculitis.
Laboratory indicators: hyperuricemia, hyperglycemia, hypokalemia, hypochloremia, hyponatremia, hypercalcemia, increased plasma urea nitrogen, hypercreatininemia, glucosuria.
Other: flu-like syndrome, chest pain, back pain, infection, decreased potency, decreased libido, rhinorrhea, sweating, weight loss, tingling of limbs, pancreatitis, exacerbation of systemic lupus erythematosus.
Drug Interactions
Saluretics, cardiac glycosides, gluco- and mineralocorticoids, tetracosactide, amphotericin B (iv), laxatives increase the risk of hypokalemia.
With concomitant use with cardiac glycosides, the likelihood of developing digitalis intoxication with Ca 2+ drugs hypercalcemia with metformin may aggravate lactic acidosis. Increases the concentration of Li + ions in blood plasma (decreased excretion in the urine), lithium has a nephrotoxic effect.
Astemizole, iv erythromycin, pentamidine, sultopride, terfenadine, vincamine, antiarrhythmic drugs of class Ia (quinidine, disopyramide) and class III (amiodarone, bretilium, sotalol) can lead to the development of arrhythmias of the “torsades de pointes” type.
Nonsteroidal anti-inflammatory drugs, glucocorticosteroids, tetracosactides, sympathomimetics reduce the hypotensive effect, baclofen enhances.
Combination with potassium-sparing diuretics may be effective in some categories of patients, however, the possibility of developing hypo- or hyperkalemia, especially in patients with diabetes mellitus and renal failure, is not completely ruled out.
Angiotensin-converting enzyme inhibitors increase the risk of hypotension and / or acute renal failure (especially with existing renal artery stenosis).
Increases the risk of impaired renal function when using iodine-containing contrast agents in high doses (dehydration).
Patients need to restore fluid loss before iodine-containing contrast agents are used.
Imipramine (tricyclic) antidepressants and antipsychotics increase the hypotensive effect and increase the risk of orthostatic hypotension. Cyclosporine increases the risk of developing hypercreatininemia.
Reduces the effect of indirect anticoagulants (coumarin or indandion derivatives) due to an increase in the concentration of coagulation factors as a result of a decrease in the volume of circulating blood and an increase in their production by the liver (dose adjustment may be required).
Enhances neuromuscular transmission blockade that develops under the influence of non-depolarizing muscle relaxants.
Overdose
Symptoms: nausea, vomiting, weakness, dysfunction of the gastrointestinal tract, water-electrolyte disorders, in some cases – excessive reduction of blood pressure, respiratory depression. Patients with cirrhosis may develop liver coma.
Treatment: gastric lavage, correction of water-electrolyte balance, symptomatic therapy. There is no specific antidote.
Storage conditions
Keep dry, protected from light at a temperature not exceeding 25 ° C.
Shelf life
3 years.
Active ingredient
Indapamide
Dosage form
tablets prolong.
Possible product names
INDAPAMID RETARD TAB. P / O 1.5MG No. 30
INDAPAMID-RETARD TAB.P / O 1.5MG No. 30
INDAPAMID 0.0015 N30 TABLE MODIF P / O / ZIO-HEALTH /
INDAPAMID 0.0015 N30 TABLE PROLONG P / O srdlp Indapamide 1.5mg Tab. prolong. valid p / pl / rev X30 (R)
