pharmachologic effect
Venous vasodilator, has an antianginal effect. Stimulates the formation of nitric oxide in the vascular wall, which is an endothelial relaxing factor. Reduces preload (dilatation of peripheral veins and reduction of blood flow to the right atrium) and afterload, total peripheral vascular resistance (TPVR) on the heart; reduces myocardial oxygen demand.
Restores blood flow through small endocardial vessels, improves blood flow in the epicardial coronary arteries, increases exercise tolerance in patients with coronary heart disease (CHD), angina pectoris.
In heart failure, it helps to unload the myocardium by reducing preload. Reduces pressure in the pulmonary circulation.
Compared to nitroglycerin, it has a slower but longer-lasting effect (up to 10 hours). When taken orally, the onset of effect is after 30 - 45 minutes (with sublingual administration - after 15 - 20 minutes), duration - 4 - 5 hours.
Erinite
The domestic drug erinite is a peripheral vasodilator, dilating mainly the vessels of the venous bed. Pentaerythrityl tetranitrate is used as the active ingredient in erinite. The drug also has an antianginal (anti-ischemic) effect. The pharmacological effect of erinite is due to a decrease in preload and afterload on the heart, which is achieved as a result of an increase in the lumen of the peripheral veins and a decrease in blood flow to the right atrium in the first case and a decrease in total peripheral vascular resistance in the second. In addition to this, the drug also has a direct coronary dilation effect. Erinite redirects coronary blood flow to areas with insufficient blood supply. In patients suffering from coronary heart disease and angina pectoris, it increases the ability to tolerate physical activity. In case of heart failure, erinite relieves part of the load from the heart muscle and reduces hypertension in the pulmonary circulation. If we compare the drug with nitroglycerin, it “swings” more slowly, but is characterized by a longer action. As you know, nitrates are the main group of antianginal drugs. It should be noted that organic erinite nitrate is significantly inferior in popularity to other nitrates: nigroglycerin, isosorbide dinitrate and isosorbide-5-mononitrate.
The answer to this question lies in the plane of the effectiveness of the pharmacological action: in the doses in which erinite is produced, it cannot be competitive with other drugs in this group.
Erinite is produced in tablet dosage form. When taken orally, it is relatively slowly absorbed from the gastrointestinal tract. The dose of the drug is determined by the doctor individually in each specific case. According to general recommendations, Erinite should be taken 20 mg 3-4 times a day; if necessary, according to indications, the dose can be increased to 40 mg taken 4 times a day or up to 80 mg taken twice a day. Given the slow development of the therapeutic effect, erinite is not intended for use for the purpose of relieving angina symptoms. Cerebral circulatory disorders require a particularly careful approach if it is necessary to use erinite in such patients. The same applies to older people. With prolonged drug therapy using erinite, the therapeutic effect may weaken due to the development of tolerance to the drug. This can be avoided to some extent by reducing the frequency of taking the drug to 1 time per day and additionally taking another antianginal drug. In conclusion, it should be noted that the use of erinite excludes the possibility of consuming alcoholic beverages during the treatment period.
Contraindications
Hypersensitivity, severe arterial hypotension (systolic blood pressure below 90 mm Hg, diastolic blood pressure below 60 mm Hg), collapse, shock, acute myocardial infarction occurring with hypotension, hemorrhagic stroke, traumatic brain injury, angle closure glaucoma, severe liver failure (risk of developing methemoglobinemia), severe renal failure, severe anemia, hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, severe aortic and/or mitral valve stenosis, hyperthyroidism, primary pulmonary hypertension (hyperemia of insufficiently ventilated alveolar zones can lead to to hypoxia), chronic heart failure with low left ventricular filling pressure, simultaneous use of phosphodiesterase-5 inhibitors (including sildenafil, vardenafil, tadalafil), lactose and sucrose intolerance, deficiency of sucrase-isomaltase, lactase or glucose-galactose malabsorption, hypersensitivity to the drug and its components, other organic nitrates, age under 18 years (efficacy and safety have not been established).
Carefully
Used for patients prone to arterial hypotension in elderly and dehydrated patients; with a history of orthostatic hypotension.
Use during pregnancy and breastfeeding
The use of the drug during pregnancy and lactation is contraindicated.
Eritadine
Dosage form
Syrup
Compound
1 ml of syrup contains:
Active substance:
Desloratadine – 0.50 mg
Excipients
: propylene glycol – 100 mg, sorbitol – 150.0 mg, anhydrous citric acid – 0.50 mg, sodium citrate dihydrate – 1.26 mg, sodium benzoate – 1.0 mg, disodium edetate – 0.25 mg, sucrose – 490 .0 mg, flavor No. 15864 – 0.75 mg, sunset yellow dye – 0.023 mg, purified water – up to 1 ml.
Description
Transparent orange liquid.
Pharmacotherapeutic group
Antiallergic agent – H1-histamine receptor blocker.
ATX code
: R06AX27.
Pharmacological properties
Pharmacodynamics
Long-acting non-sedating antihistamine. It is the primary active metabolite of loratadine. Suppresses the release of histamine from mast cells. Inhibits the cascade of allergic inflammation reactions, including the release of pro-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, and the release of adhesion molecules such as P-selectin. Thus, it prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects, reduces capillary permeability, and prevents the development of tissue edema and smooth muscle spasm.
The drug has no effect on the central nervous system, does not cause drowsiness (the use of desloratadine at the recommended dose of 5 mg per day is not accompanied by an increase in the incidence of drowsiness compared to the placebo group) and does not affect the speed of psychomotor reactions. Does not cause prolongation of the QT interval on the ECG.
The effect of the drug begins within 30 minutes after oral administration and continues for 24 hours.
Pharmacokinetics
Desloratadine is well absorbed from the gastrointestinal tract. Determined in blood plasma 30 minutes after oral administration. The maximum concentration is achieved on average 3 hours after administration. Does not penetrate the blood-brain barrier. The binding to plasma proteins is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 mg to 20 mg once a day, no clinically significant accumulation of the drug is observed. Concomitant ingestion of food or grapefruit juice does not affect the distribution of desloratadine when used at a dose of 7.5 mg once daily. Desloratadine is not an inhibitor of CYP3A4 and CYP2D6 and is not a substrate or inhibitor of P-glycoprotein. Intensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine combined with a glucuronide. Only a small part of the dose taken orally is excreted unchanged by the kidneys (<2%) and through the intestines (<7%). The half-life is on average 27 hours.
Indications for use
- allergic rhinitis (elimination or relief of sneezing, nasal congestion, nasal mucus, itchy nose, itchy palate, itching and redness of the eyes, watery eyes);
- urticaria (reduction or elimination of skin itching, rash).
Contraindications
- Hypersensitivity to desloratadine, other components of the drug or loratadine.
- Pregnancy and breastfeeding period.
- Children's age up to 6 months.
- Hereditary diseases: fructose intolerance, impaired absorption of glucose-galactose or deficiency of sucrase-isomaltase in the body (due to the presence of sucrose and sorbitol in the composition).
Use during pregnancy and breastfeeding
The use of the drug during pregnancy is contraindicated due to the lack of clinical data on the safety of desloratadine during pregnancy. Desloratadine is excreted into breast milk, therefore the use of desloratadine during breastfeeding is contraindicated.
Carefully
Severe renal failure, patients with a history of seizures.
Directions for use and doses
Inside, regardless of the time of meal, with a small amount of water.
Children aged 6 to 12 months – 1 mg (2 ml syrup) 1 time per day.
Children aged 1 to 5 years – 1.25 mg (2.5 ml of syrup) 1 time per day.
Children aged 6 to 11 years – 2.5 mg (5 ml syrup) 1 time per day.
Adults and adolescents over 12 years old – 5 mg (10 ml syrup) 1 time per day.
For seasonal (intermittent) allergic rhinitis (symptoms lasting less than 4 days a week or less than 4 weeks a year), the course of the disease must be assessed. If symptoms disappear, desloratadine should be discontinued; if symptoms reappear, the drug should be resumed. For year-round (persistent) allergic rhinitis (symptoms lasting more than 4 days a week or more than 4 weeks a year), desloratadine should be taken throughout the entire period of allergen exposure.
Side effect
In children aged 6 to 23 months, the following side effects were observed, the frequency of which was slightly higher than when using placebo (“dummies”): diarrhea (in 3.7% of cases), increased body temperature (2.3%), insomnia (2.3%).
In children aged 2 to 11 years, when using the drug Desloratadine syrup, the frequency of side effects was the same as when using placebo.
According to the results of clinical studies in children aged 6 to 11 years, no side effects were identified when taking the drug in recommended doses (2.5 mg/day).
In children aged 12-17 years, according to the results of clinical studies, the most common side effect was headache (5.9%), the frequency of which was no higher than when taking placebo (6.9%).
In adults and adolescents (12 years and older), according to the results of clinical studies, side effects were recorded in 3% of patients compared to the placebo group, of which the most common were: increased fatigue (1.2%), dry mouth (0). .8%), headache (0.6%).
Information on side effects is presented based on the results of clinical studies and observations of the post-registration period.
According to the World Health Organization (WHO), side effects are classified according to their frequency as follows: very common (> 1/10), common (> 1/100 to < 1/10), not common (> 1/10). 1000 to <1/100), rare (> 1/10000 to <1/1000), very rare (<1/10000); frequency unknown - based on available data, it was not possible to determine the frequency of occurrence.
From the mental side
: very rarely – hallucinations; frequency unknown – abnormal behavior, aggression.
From the nervous system
: often – headache; often (in children under 2 years of age) – insomnia; very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.
From the liver and biliary tract
: very rarely - increased activity of liver enzymes, increased bilirubin concentration, hepatitis; frequency unknown - jaundice.
From the digestive system
: often – dry mouth, often (in children under 2 years of age) – diarrhea; very rarely - abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increased appetite, weight gain.
From the cardiovascular system
: very rarely - tachycardia, palpitations; frequency unknown – prolongation of the QT interval.
From the musculoskeletal system
: very rarely – myalgia.
From the skin and subcutaneous tissues
: frequency unknown – photosensitivity.
General disorders
: often - increased fatigue, often (in children over 2 years old) - fever; very rarely - anaphylaxis, angioedema, shortness of breath, itching, rash, including urticaria; frequency unknown - asthenia.
Post-registration period. Children: frequency unknown - QT prolongation, arrhythmia, bradycardia, abnormal behavior, aggression.
If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms
. Taking a dose 5 times the recommended dose did not result in any symptoms. In clinical trials, daily use of desloratadine up to 20 mg for 14 days in adults and adolescents was not associated with statistically or clinically significant changes in the cardiovascular system. In a clinical pharmacological study, the use of desloratadine at a dose of 45 mg/day (9 times higher than recommended) for 10 days did not cause prolongation of the QT interval and was not accompanied by serious side effects.
Treatment
. If you accidentally ingest a large amount of the drug, you should immediately consult a doctor. Gastric lavage and activated charcoal are recommended; if necessary, symptomatic therapy.
Desloratadine is not eliminated by hemodialysis; the effectiveness of peritoneal dialysis has not been established.
Interaction with other drugs
Interactions with other drugs were not detected in studies with azithromycin, ketoconazole, erythromycin, fluoxetine and cimetidine. Eating does not affect the effectiveness of the drug. Desloratadine does not enhance the effects of alcohol on the central nervous system. However, cases of alcohol intolerance and alcohol intoxication have been reported during post-marketing use. Therefore, desloratadine should be used with caution simultaneously with alcohol.
special instructions
In the presence of severe renal failure, desloratadine should be used with caution. Caution should be exercised when using desloratadine in patients with a history of seizures, especially in pediatric patients. You should stop using the drug if seizures develop. There have been no studies of the effectiveness of desloratadine in rhinitis of infectious etiology.
Application in pediatrics.
The effectiveness and safety of desloratadine in children under 6 months of age has not been established.
Impact on the ability to drive vehicles and machinery
The potential for side effects such as dizziness and drowsiness should be taken into account. If such signs appear, you should refrain from performing these types of activities.
Release form
Syrup 0.5 mg/ml.
1, 2, 3, 4, 5, 10, 15, 20, 30, 40, 50, 60, 100, 120, 150, 200, 225 or 300 ml of the drug in dark glass bottles sealed with polyethylene stoppers and screw-on plastic caps or sealed with polyethylene or polymer plastic closures.
1, 2, 3, 4, 5, 10, 15, 20, 30, 40, 50, 60, 100, 120, 150, 200, 225 or 300 ml of the drug in bottles, polymer jars made of polyethylene or plastic, or made of plastic, sealed with polyethylene stoppers, stoppers and screw-on plastic caps, or sealed with polyethylene or polymer plastic closures.
1, 2, 3, 4, 5, 10, 15, 20, 30, 40, 50, 60, 100, 120, 150, 200, 225 or 300 ml of the drug in vials made of polyethylene terephthalate, sealed with polymer screw caps made of polyethylene terephthalate.
A paper label or self-adhesive label is placed on each bottle or jar. Each bottle, jar, together with a plastic spoon, along with instructions for medical use, is placed in a cardboard pack.
It is allowed to pack bottles without a pack from 9 to 300 pieces with an equal number of instructions for medical use in a group package (for hospitals).
Storage conditions
Store at a temperature not exceeding 30 °C.
Keep out of the reach of children.
Best before date
2 years.
Do not use after expiration date.
Vacation conditions
Available without a prescription.
special instructions
When taken, the risk of developing arterial hypotension increases in elderly patients and dehydrated patients.
It is necessary to exclude alcohol consumption during treatment.
With prolonged use, the therapeutic effect may decrease (due to the development of tolerance). To reduce the risk of developing tolerance, it is recommended to observe a “nitrate-free” period (8 - 12 hours).
When using the drug once a day in combination with other antianginal drugs, the risk of developing tolerance is less.
The drug is not used to relieve angina attacks. Do not suddenly interrupt treatment with the drug.
Due to the fact that when using the drug, side effects such as dizziness, drowsiness and blurred vision may occur, it is therefore necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and rapid mental and motor reactions.
Registration number: Trade name: TRIAZAVIRIN® International nonproprietary or generic name: riamilovir Dosage form: capsules
Composition 1 capsule contains: Active ingredient: Riamilovir (TRIAZAVIRIN®) - 250 mg Excipients: Calcium stearate - 2 mg Weight of capsule contents - 252 mg Composition of capsule shell Capsule (body) No. 1: titanium dioxide (E171), quinoline yellow dye ( E104), sunset yellow dye (E110), medical gelatin. Capsule (cap) No. 1: titanium dioxide (E171), azorubine dye (E122), medical gelatin. Weight of capsule with contents - 328 mg
Description Hard gelatin capsules size No. 1, yellow body and red cap. The contents of the capsules are fine-crystalline powder or granules of yellow or yellow-green color.
Pharmacotherapeutic group Antiviral agent. ATX code: J05AX.
Pharmacological properties Pharmacodynamics The active substance of the drug TRIAZAVIRIN® - riamilovir - is a synthetic analogue of purine nucleoside bases (guanine) with a pronounced antiviral effect. It has a wide spectrum of antiviral activity against RNA-containing viruses. The main mechanism of action of the drug TRIAZAVIRIN® is inhibition of the synthesis of viral RNA and replication of genomic fragments. Pharmacokinetics: After oral administration, it is rapidly absorbed from the gastrointestinal tract. The maximum concentration (Cmax) is reached on average after 1–1.5 hours. Cmax with the recommended dosage regimen averages 4.8 mcg/ml. The AUC value (area under the concentration-time pharmacokinetic curve) of blood is 12.8 mcg/h*ml. The half-life (T1/2) is 1–1.5 hours. From 15 to 45% of riamilovir is excreted unchanged by the kidneys. The average calculated clearance is 246 ml/min.
Indications for use As part of complex therapy for influenza and other acute respiratory viral infections in adult patients.
Contraindications - hypersensitivity to the components of the drug; - pregnancy; - period of breastfeeding; - children under 18 years of age (efficacy and safety have not been determined); - renal/liver failure (efficacy and safety have not been determined).
Use during pregnancy and breastfeeding Due to the lack of strictly controlled studies in humans, the use of the drug during pregnancy is contraindicated (see section “Contraindications”). The use of the drug during breastfeeding has not been studied, therefore, if it is necessary to use the drug during lactation, breastfeeding should be stopped.
Method of administration and dosage TRIAZAVIRIN® is taken orally, regardless of meals, with a sufficient amount of drinking water. The capsule should be swallowed whole; it is not recommended to chew or crush the capsule. Taking the drug must be started no later than the 2nd day from the onset of the disease (manifestation of clinical symptoms of influenza and other acute respiratory viral infections). Recommended dose: for influenza and other acute respiratory viral infections: 1 capsule (250 mg) 3 times a day for 5 consecutive days. Maximum single dose: 1 capsule (250 mg). Maximum daily dose: 3 capsules (750 mg). If there is no improvement within 5 days of treatment, or the symptoms worsen, or new symptoms appear, you should consult your doctor. Use the drug only according to the indications, method of administration and in the doses indicated in the instructions.
Side effects Blood and lymphatic system disorders: increased number of eosinophils in the blood. Immune system disorders: allergic reactions (rash). Nervous system disorders: headache. Gastrointestinal tract disorders: dyspepsia (nausea, vomiting, bloating, pasty stools, flatulence, heartburn, abdominal pain, diarrhea, dry mouth). Renal and urinary tract disorders: increased erythrocytes, leukocytes, squamous epithelium in the urine, presence of bacteria in the urine. Laboratory and instrumental data: increased levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in blood plasma. General disorders and reactions at the injection site: weakness. If you experience the side effects listed in the instructions, or they get worse, or you notice any other side effects not listed in the instructions, tell your doctor. Overdose Symptoms: nausea, vomiting, dyspeptic disorders, stomach pain. Treatment: symptomatic therapy. If these symptoms occur, you should stop taking the drug and consult a doctor.
Interaction with other drugs No special clinical studies have been conducted to study interactions with other drugs. If you are using any medications (including over-the-counter medications), consult your doctor before using TRIAZAVIRIN®.
Special instructions The drug TRIAZAVIRIN® contains sunset yellow (E110) and azorubine (E122) dyes, which can cause allergic reactions. The effect on the ability to drive vehicles and machinery has not been studied, however, based on the range of adverse reactions, no effect on these types of activities is expected.
Release form Capsules, 250 mg. 10 capsules per blister pack made of polyvinyl chloride film and printed varnished aluminum foil. One or two blister packs, together with instructions for medical use of the drug, are placed in a cardboard pack.
Storage conditions : Protected from light at a temperature not exceeding 25 °C. Keep out of the reach of children. Shelf life: 5 years. Do not use after the expiration date.
Conditions of release Dispensed without a prescription.
Directions for use and doses
Erinit is taken orally (1 hour before meals) in the form of tablets of 10 - 20 mg (1 - 2 tablets) 3 - 4 times a day, if necessary - up to 40 mg 4 times a day, it is acceptable to prescribe 80 mg 2 times a day day.
To prevent nocturnal attacks of angina pectoris, 20 mg is prescribed before bedtime. The course of treatment usually lasts 2 - 4 weeks. A repeated course is prescribed with breaks, the duration of which depends on the course of the disease.
If necessary, sublingual administration of the drug is possible, but not to relieve an attack of angina.
Side effect
Allergic reactions, skin flushing, headache, tinnitus, dizziness, nausea, weakness, tachycardia, increased fatigue, anxiety, increased sweating, decreased blood pressure (BP), orthostatic hypotension; sometimes there is a disorder of intestinal function (diarrhea). When the dose is reduced or after stopping the drug, side effects disappear.
Overdose
When using the drug in large doses, tolerance may develop.
Symptoms: orthostatic hypotension, a feeling of compression of the head, throbbing headache, severe sweating, cold skin, covered with sticky sweat, or hyperemic, palpitations, bradycardia, conduction disturbances (blockade), difficulty breathing, Kussmaul breathing, bloody diarrhea, vomiting, dizziness, confusion, syncope, coma, fever, paralysis, visual impairment.
Treatment: gastric lavage, giving a horizontal position with legs raised, in case of severe arterial hypotension and/or in patients in shock - administration of fluid intravenous drip infusion solutions, monitoring the level of methemoglobin in the blood, if it increases - prescribing ascorbic acid in a dose 1 g orally, methylthioninium chloride (Methylene blue) IV up to 50 ml of 1% solution, toluidine blue - 2 - 4 mg/kg body weight IV quickly, if necessary - again at a dose of 2 mg/kg with an interval of 1 hour , oxygen therapy, hemodialysis, exchange transfusion.
Interaction with other drugs
If you are taking this drug with other medications at the same time, consult your doctor.
Under the influence of dihydroergotamine, the antianginal effect of erinitis may be reduced. The combination of these means is considered irrational.
It is possible to enhance the hypotensive effect when used simultaneously with vasodilators and antihypertensive drugs (beta-blockers, calcium channel blockers, etc.), antipsychotics, tricyclic antidepressants, monoamine oxidase inhibitors, procainamide, ethanol, phosphodiesterase-5 inhibitors.
The combination with anaprilin is rational, since the antianginal effect is enhanced.
