Pharmacodynamics and pharmacokinetics
Pharmacodynamics
What is Pentaflucin for? This is a combination drug that has an antipyretic effect. The drug is prescribed to relieve symptoms of flu and colds, as it eliminates headaches, nasal congestion, sore throat, and reduces cough.
Paracetamol is a non-narcotic analgesic and has an antipyretic effect. Blocks COX1 and COX2 in the central nervous system.
Ascorbic acid takes part in blood clotting and carbohydrate metabolism. Promotes tissue regeneration and increases resistance.
Diphenhydramine ( diphenhydramine ) has an antihistamine effect. Eliminates inflammation, swelling of the mucous membrane, has a sedative and hypnotic effect. Rutoside ( rutin ) reduces capillary fragility, reduces blood clotting, and is an antioxidant. Calcium gluconate regulates calcium metabolism.
Pharmacokinetics
Paracetamol is completely and quickly absorbed. Cmax is reached in 30-60 minutes. Quickly distributed in tissues. Has low protein binding. Metabolized in the liver. Eight active metabolites are conjugated with glutathione , with a deficiency of which the metabolites block the enzyme systems of hepatocytes with the development of necrosis. Excreted by the kidneys.
Cmax of Rutoside is achieved in 2-9 hours. T1/2 is 10-25 hours. Ascorbic acid is quickly absorbed. Cmax 4 hours. Metabolized in the liver.
Diphenine hydramide ( diphenhydramine ) is also rapidly absorbed. Its bioavailability is 50%. Cmax in 20-40 min. The highest concentrations are found in the lungs, brain, kidneys, and liver. Penetrates through the BBB. Within a day it is completely excreted by the kidneys. A large amount is excreted in milk, which causes a sedative effect in infants.
Pentaflucin for children, granules for the preparation of solution for oral administration, 3 g, 10 pcs.
Taking 5 or more grams of paracetamol can lead to liver damage in patients with the following risk factors: long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John's wort, or other drugs that stimulate liver enzymes; regular consumption of ethanol in excess quantities; glutathione deficiency (due to malnutrition, cystic fibrosis, HIV infection, starvation, exhaustion).
Symptoms of an overdose of parecetamol: during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, abdominal pain; impaired glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In case of severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia.
Treatment: the victim should undergo gastric lavage, prescribe adsorbents (activated carbon) and consult a doctor.
Symptomatic therapy: within the first hour after the expected overdose, it is advisable to use activated carbon orally. Four or more hours after the suspected overdose, it is necessary to determine the concentration of paracetamol in plasma (earlier determination of paracetamol concentration may be unreliable). Treatment with acetylcysteine can be carried out up to 24 hours after taking paracetamol, but the maximum hepatoprotective effect can be obtained in the first 8 hours after an overdose. After this, the effectiveness of the antidote drops sharply. If necessary, acetylcysteine can be administered intravenously. In the absence of vomiting, an alternative option (if it is not possible to quickly obtain hospital care) is the use of methionine orally. Treatment of patients with severe liver dysfunction 24 hours after taking paracetamol should be carried out in conjunction with specialists from a poison control center or specialized liver disease department.
Symptoms caused by diphenhydramine: depression or excitation (especially in children) of the central nervous system, depression, dilated pupils, dry mouth, dysfunction of the gastrointestinal tract.
Treatment: there is no specific antidote, treatment is symptomatic.
Symptoms of an overdose of ascorbic acid: diarrhea, nausea, flatulence, spastic abdominal pain, frequent urination, nephrolithiasis, insomnia, irritability, hypoglycemia. When using more than 1000 mg - headache, increased excitability of the central nervous system, insomnia, nausea, vomiting, diarrhea, hyperacid gastritis, damage to the mucous membrane of the gastrointestinal tract, inhibition of the function of the insular apparatus of the pancreas (hyperglycemia, glucosuria), hyperoxaluria, nephrolithiasis, damage to the glomerular apparatus of the kidneys, decreased capillary permeability (possible deterioration of tissue trophism, increased blood pressure, hypercoagulation, development of microangiopathies). High doses of ascorbic acid (more than 3000 mg) can cause temporary osmotic diarrhea and gastrointestinal disturbances, such as nausea and stomach discomfort.
Treatment: symptomatic, forced diuresis.
Symptoms of an overdose of calcium gluconate: hypercalcemia; with chronic overdose, general and muscle weakness, depression, mental disorders, appetite disturbances, nausea, vomiting, constipation, decreased blood pressure, and heart rhythm disturbances may develop.
Treatment: parenteral administration of calcitonin at a dose of 5-10 IU/kg/day in 500 ml of 0.9% sodium chloride solution for 6 hours.
Rutoside. There is no information about overdose.
Interaction
Pentaflucin enhances the effect of drugs that reduce platelet aggregation and reduce blood clotting.
Increases the side effects of non-narcotic analgesics , NSAIDs , glucocorticoids , methotrexate sulfonylurea derivatives .
Combination with barbiturates , Diphenin , Carbamazepine , anticonvulsants , Rifampicin , Zidovudine and alcoholic beverages should be avoided.
Pentaflucin Day/Night granules intravenous 5 g x10 Uralbiopharm
Pentaflucin Day/Night granules intravenous 5 g x10 Uralbiopharm
ATX code: R05X (Other combination products used for colds)
Dosage form PENTAFLUCINE DAY/NIGHT granules for preparation. solution for oral administration: 5 g pack. 5 or 10 pcs.
reg. No.: LP-001388 dated 12/20/11 - Valid
Release form, composition and packaging Granules for the preparation of a solution for oral administration of different shapes and sizes: round, cylindrical or irregular in shape, white, white with a yellowish tint and yellow-green color.
1 pack ascorbic acid 200 mg calcium gluconate monohydrate 200 mg caffeine monohydrate 20 mg paracetamol 500 mg rutoside (in trihydrate form) 20 mg
Excipients: povidone 17.4 mg, sugar 3.9426 g, saccharin 50 mg, citric acid 50 mg.
5 g - bags (5) - cardboard packs. 5 g - sachets (10) - cardboard packs.
Clinical and pharmacological group: Drug for symptomatic treatment of acute respiratory diseases
Pharmacotherapeutic group: A remedy for eliminating the symptoms of acute respiratory infections and “colds”
Indications Pentaflucin daily is used in adults for the symptomatic treatment of acute respiratory diseases (ARI) and acute respiratory viral infections (ARVI), accompanied by high fever, chills, headache and muscle pain.
ICD-10 codes
Dosage regimen Pentaflucin daily is used orally after meals, 1 sachet 3-4 times a day for 3-5 days.
Dissolve the contents of one sachet of the drug in 1/2 cup (125 ml) of hot water (t=70°C) and drink. A slight sediment in the glass is allowed. Use freshly prepared solution. Shake before use.
Side effect
At the recommended dosage, adverse reactions are rare.
Sometimes allergic skin reactions, nausea, vomiting, headache, general weakness, dizziness may occur.
Ascorbic acid
From the urinary system: moderate pollakiuria (when taking a dose of more than 600 mg/day), with long-term use of large doses - hyperoxaluria, nephrolithiasis (from calcium oxalate), damage to the glomerular apparatus of the kidneys.
From the digestive system: irritation of the gastrointestinal mucosa.
Allergic reactions: skin rash, skin hyperemia.
Other: inhibition of the function of the pancreatic insular apparatus (hyperglycemia, glycosuria).
Calcium gluconate
From the digestive system: constipation, irritation of the gastrointestinal mucosa.
Caffeine
From the nervous system: excitement, anxiety, tremor, restlessness, headache, dizziness, increased reflexes, tachypnea, insomnia.
From the cardiovascular system: palpitations, tachycardia, arrhythmias, increased blood pressure.
From the digestive system: nausea, vomiting, exacerbation of peptic ulcer.
Paracetamol
From the digestive system: nausea, epigastric pain.
From the hematopoietic system: anemia, thrombocytopenia, methemoglobinemia.
Allergic reactions: skin rash, itching, urticaria, angioedema.
With long-term use in high doses, hepatotoxic and nephrotoxic effects are possible.
Rutoside
Allergic reactions: skin rash
From the digestive system: nausea, diarrhea, heartburn.
From the nervous system: headache.
From the cardiovascular system: “flushes” of blood to the face.
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.
Contraindications for use - hypersensitivity to the components of the drug, - severe impairment of liver or kidney function, - blood diseases with a tendency to hemorrhage, - deficiency of glucose-6-phosphate dehydrogenase, - childhood (up to 18 years), - congenital intolerance to fructose, glucose- galactose malabsorption, sucrose-isomaltase deficiency.
With caution In Gilbert's syndrome (constitutional hyperbilirubinemia).
The drug contains sugar (1 sachet contains 0.33 XE of sugar), which should be taken into account by patients with diabetes.
Use during pregnancy and breastfeeding Use of the drug during pregnancy and breastfeeding is contraindicated. If it is necessary to use the drug during lactation, stop breastfeeding for the entire period of treatment.
Use for liver dysfunction Contraindicated in severe liver dysfunction. Use for impaired renal function Contraindicated in cases of severe impaired renal function. Use in children Contraindicated in children and adolescents under 18 years of age. Special instructions To avoid toxic damage to the liver, you should not combine the drug with drinking alcoholic beverages. During the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose Symptoms (due to paracetamol): during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, abdominal pain, impaired glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In case of severe overdose - liver failure with progressive encephalopathy, coma, death, acute renal failure with tubular necrosis (including in the absence of severe liver damage), arrhythmia, pancreatitis. The hepatotoxic effect in adults occurs when taking 10 g or more.
Treatment: the victim should undergo gastric lavage, prescribe adsorbents (activated carbon) and consult a doctor.
Symptomatic therapy: administration of SH-group donors and precursors for the synthesis of glutathione - methionine within 8-9 hours after an overdose and acetylcysteine - within 8 hours. The need for additional therapeutic measures (further administration of methionine, intravenous administration of acetylcysteine) is determined in depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.
Drug interactions Avoid combining the drug with barbiturates, anticonvulsants, phenytoin, carbamazepine, rifampicin, zidovudine and other inducers of microsomal liver enzymes.
Paracetamol: reduces the effectiveness of uricosuric drugs. Concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (decreased synthesis of procoagulant factors in the liver).
Ethanol contributes to the development of acute pancreatitis.
Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, and the onset of end-stage renal failure.
Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
Caffeine: when caffeine is used together with cimetidine, oral contraceptives, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increasing its concentration in the blood).
Mexiletine - reduces caffeine elimination by up to 50%, nicotine - increases the rate of caffeine elimination.
Monoamine oxidase inhibitors, furazolidone, procarbazine and selegiline - large doses of caffeine can cause the development of dangerous cardiac arrhythmias or a marked increase in blood pressure.
Accelerates absorption and enhances the effect of cardiac glycosides, increasing their toxicity.
The combined use of caffeine with beta-blockers can lead to mutual suppression of therapeutic effects, with adrenergic bronchodilators - to additional stimulation of the central nervous system and other additive toxic effects.
Caffeine may decrease the clearance of theophylline and possibly other xanthines, increasing the potential for additive pharmacodynamic and toxic effects.
Ascorbic acid: increases the concentration of benzylpenicillin and tetracyclines in the blood.
At a dose of 1 g/day, it increases the bioavailability of ethinyl estradiol (including that contained in oral contraceptives).
Reduces the effectiveness of heparin and indirect anticoagulants.
Improves the absorption of iron preparations in the intestines (converts ferric iron to divalent iron), can increase the excretion of iron when used simultaneously with deferoxamine.
Acetylsalicylic acid (ASA), oral contraceptives, fresh juices and alkaline drinks reduce the absorption and absorption of ascorbic acid.
When used simultaneously with ASA, the urinary excretion of ascorbic acid increases and the excretion of ASA decreases. ASA reduces the absorption of ascorbic acid by approximately 30%.
Increases the risk of developing crystalluria during treatment with salicylates and short-acting sulfonamides, slows down the excretion of acids by the kidneys, increases the excretion of drugs that have an alkaline reaction (including alkaloids), and reduces the concentration of oral contraceptives in the blood.
When used simultaneously, it reduces the chronotropic effect of isoprenaline.
Calcium gluconate: concomitant use with quinidine may slow intraventricular conduction and increase the toxicity of quinidine. Forms insoluble complexes with tetracycline antibiotics (reduces the antibacterial effect).
Slows down the absorption of tetracyclines, digoxin, and oral iron supplements (the interval between doses should be at least 2 hours).
When combined with thiazide diuretics, it can increase hypercalcemia and reduce the effect of calcitonin in hypercalcemia. Reduces the bioavailability of phenytoin.
Pharmaceutically incompatible with carbonates, salicylates, sulfates (forms insoluble or sparingly soluble calcium salts). Reduces the effect of blockers of “slow” calcium channels.
Rutoside: the pharmacological effect is enhanced by ascorbic acid.
Conditions for dispensing from pharmacies
The drug is approved for use as a means of OTC.
Storage conditions and periods
Store the drug out of the reach of children, in a dry place protected from light at a temperature not exceeding 25°C.
Shelf life: 2 years. Do not use after expiration date.
Analogs
Level 4 ATC code matches:
Aflubin
Kofex
TeraFlu Bro
Suprima-Broncho
Sinupret
Bronchostop
Doctor Mom
Tonsilgon N
Tonsipret
Insti
Imupret
Antigrippin-Maximum
Antigrippin-ANVI
Atma
Viburkol
Travisil
RiniCold Broncho
Umkalor
Stodal
AnviMax
Coldrex Max Gripp , Coldflu , Antigrippin have a similar effect.
Reviews
The drug is used for symptomatic treatment of respiratory diseases . Everyone who has taken this drug notes its effectiveness, availability and low cost.
“It helps! Inexpensive and effective"
“It helps well and quickly with colds, quickly relieves the condition”
“Pentaflucin is an effective, efficient and inexpensive remedy”
“...an effective drug for the initial signs of a cold”
One of the disadvantages of the drug is its side effect - drowsiness. This is understandable because it contains diphenhydramine . Please note that there is Pentaflucin daily (without diphenhydramine), devoid of this undesirable effect.
Pentaflucin®
Combination of the drug with barbiturates, anticonvulsants, phenytoin, carbamazepine, rifampicin, zidovudine and other inducers of microsomal liver enzymes should be avoided.
Paracetamol:
reduces the effectiveness of uricosuric drugs. Concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (reduced synthesis of procoagulant factors in the liver).
Inducers of microsomal oxidation in the liver (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxications even with a small overdose.
Long-term use of barbiturates reduces the effectiveness of paracetamol.
Ethanol contributes to the development of acute pancreatitis.
Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, and the onset of end-stage renal failure.
Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
Diphenhydramine:
potentiates the effect of alcohol and drugs that depress the central nervous system. Monoamine oxidase inhibitors enhance the anticholinergic activity of diphenhydramine.
Ascorbic acid:
increases the concentration of benzylpenicillin and tetracyclines in the blood; at a dose of 1 g/day increases the bioavailability of ethinyl estradiol (including that included in oral contraceptives).
Reduces the effectiveness of heparin and indirect anticoagulants.
Improves the absorption of iron preparations in the intestines (converts ferric iron to divalent iron); may increase iron excretion when used concomitantly with deferoxamine.
Acetylsalicylic acid, oral contraceptives, fresh juices and alkaline drinks reduce absorption and absorption.
When used simultaneously with acetylsalicylic acid, the urinary excretion of ascorbic acid increases and the excretion of acetylsalicylic acid decreases. Acetylsalicylic acid reduces the absorption of ascorbic acid by approximately 30%. Increases the risk of developing crystalluria during treatment with salicylates and short-acting sulfonamides, slows down the excretion of acids by the kidneys, increases the excretion of drugs that have an alkaline reaction (including alkaloids), and reduces the concentration of oral contraceptives in the blood.
When used simultaneously, it reduces the chronotropic effect of isoprenaline. Barbiturates and primidone increase the excretion of ascorbic acid in the urine.
Calcium gluconate:
When used simultaneously with quinidine, intraventricular conduction may slow down and the toxicity of quinidine may increase.
Forms insoluble complexes with tetracycline antibiotics (reduces the antibacterial effect).
Slows down the absorption of tetracyclines, digoxin, and oral iron supplements (the interval between doses should be at least 2 hours).
When combined with thiazide diuretics, it can increase hypercalcemia and reduce the effect of calcitonin in hypercalcemia.
Reduces the bioavailability of phenytoin.
Pharmaceutically incompatible with carbonates, salicylates, sulfates (forms insoluble or sparingly soluble calcium salts).
Reduces the effect of slow calcium channel blockers.
Rutoside:
the pharmacological effect is enhanced by ascorbic acid.
Pentaflucin price, where to buy
You can buy it in many pharmacies in Moscow. The price of Pentaflucin in granules 5 g No. 10 sachets ranges from 109 rubles. up to 178 rub.
- Online pharmacies in RussiaRussia
ZdravCity
- Pentaflucin Daily gran.
d/prig. solution for oral administration 5g package No. 10 OJSC "Uralbiopharm" 229 rub. order - Pentaflucin granules for intravenous injection solution. approx. 5g 10 pcs. JSC Uralbiopharm
RUB 229 order
- Pentaflucin Daily gran. d/prig. solution for oral administration 5g package No. 5 JSC "Uralbiopharm"
RUB 143 order
