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, 5 pcs., 3 g, granules for the preparation of solution for oral administration
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 mucous membrane of the gastrointestinal tract.
Allergic reactions: skin rash, skin hyperemia.
Other: inhibition of the function of the pancreatic insular apparatus (hyperglycemia, glycosuria).
Changes in laboratory parameters (thrombocytosis, hyperprothrombinemia, erythropenia, neutrophilic leukocytosis, hypokalemia).
Diphenhydramine:
From the cardiovascular system: decreased blood pressure, palpitations, tachycardia, extrasystole.
From the respiratory system: dryness of the mucous membrane of the nose and throat, increased viscosity of sputum, a feeling of constriction in the chest or throat, sneezing, nasal congestion.
From the nervous system: headache, sedation, drowsiness, dizziness, loss of coordination, weakness, confusion, anxiety, agitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, neuritis, convulsions.
From the senses: impaired visual perception, diplopia, vertigo, tinnitus, acute labyrinths.
From the digestive system: dryness of the oral mucosa, epigastric pain, anorexia, nausea, vomiting, diarrhea, constipation.
From the genitourinary system: frequent or difficult urination, urinary retention, early menstruation.
From the hematopoietic organs: hemolytic anemia, thrombocytopenia, agranulocytosis.
Allergic reactions: urticaria, drug rash, anaphylactic shock, photosensitivity.
Other: increased sweating, chills.
Calcium gluconate:
Hypercalcemia.
From the digestive system: constipation, irritation of the mucous membrane of the gastrointestinal tract.
Paracetamol:
From the digestive system: nausea, epigastric pain.
From the hematopoietic system: anemia, thrombocytopenia, methemoglobinemia.
Allergic reactions: Stevens-Johnson syndrome, skin rash, itching, urticaria, angioedema.
With long-term use in high doses, hepatotoxic and nephrotoxic effects are possible.
Bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs.
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.
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 granules for intravenous injection solution.
approx. 5g 10 pcs. JSC Uralbiopharm 223 rub. order - Pentaflucin Daily gran. d/prig. solution for oral administration 5g package No. 5 JSC "Uralbiopharm"
RUB 143 order
PENTAFLUCINE (granules)
But it didn’t work out, the temperature fluctuated between 38-39 degrees and nothing worked except lying in semi-delirium.
On the second day, I gathered all my remaining strength and went to the doctor, hoping to hear a life-saving recipe for our recovery, but it turned out there was no special recipe - definitely antiviral drugs (in my case it was Ingaverin), drinking plenty of fluids and the same Paracetamol, which you can optionally replace with Pentaflucin or Fervex. We spent the rest of the day on the verge of 38-39 degrees with Paracetamol. On the third day, when Paracetamol was already running out, I finally remembered about Pentaflucin, which I had bought on the first day, and when I saw 39 on the thermometer again, without hesitation I diluted this powder for myself and my husband. Half an hour later, we were both fast asleep, and when we woke up a few hours later, we discovered that the temperature had dropped below 38 degrees and our condition was already more sane. Therefore, when in the evening the temperature began to rise again, we immediately took this miracle powder and slept soundly all night. Starting from the fourth day, we were recovering at a confident pace, a slight temperature was still present, but it no longer rose above 38 degrees, and the condition was getting better every hour, so Pentaflucin was taken only in the evening for prevention and better sleep. On the morning of the fifth day, the temperature finally dropped below 37 degrees. On the seventh day, I was already discharged from sick leave and cheerfully went to work, forgetting about the week-long nightmare called the flu. Of course, the antiviral drug, drinking plenty of fluids, and constant bed rest helped me in a quick recovery, but in alleviating the condition and lowering the temperature, it was Pentaflucin that played the main role, which coped with the temperature faster and better than the well-known Paracetamol.
Pentaflucin is sold in packages of 5 and 10 sachets, but some pharmacies sell it individually.
The cardboard packaging is dark blue; on the front side it contains brief information about the indications for use and the method of preparing the solution.
On the sides you can see: - expiration date, barcode and in this case the price. As you can see, it turns out to be quite inexpensive for such an effective remedy.
— Name and address of the company producing this product. I’m very glad that the product is produced in my city
— Detailed information about indications for use, method of use and doses (corresponds to the data in the instructions) This is very convenient, you don’t need to take out the instructions every time to remember the method of use.
— As well as the composition and information on storage of this drug
I would like to dwell on the composition, which, it seems to me, was very well chosen: - Ascorbic acid, known to everyone, improves immunity. — Diphenhydramine acts as a sleeping pill, so you fall asleep after using this drug very quickly and soundly. This pentaflucin is also called night pentaflucin, and for those who suffer from the disease on their legs there is day pentaflucin, which instead of diphenhydramine contains another component and does not cause drowsiness. — Calcium gluconate has an antiallergic effect. — Rutin is an antioxidant, good for capillaries. — Paracetamol in a content equal to one tablet of regular Paracetamol. That is, it turns out that Pentaflucin is the same Paracetamol, but enhanced with additional components, so it not only reduces the temperature, but also helps in recovery. I am not a doctor, so I will not discuss further the benefits or harms of such a composition; more detailed information can be found in the instructions or checked with specialists.
Inside there are 10 (in my case) bags of granules (now we only have 5 left) and instructions for use, printed in a very small and blurry font. Because of such an unfortunate font, the instructions are very difficult to read, although all the necessary information is in it, so I advise you to read it before use and especially pay attention to contraindications and side effects.
Each bag of granules also contains information about the composition and manufacturer, and the method of use is also clearly indicated (in pictures). I was a little confused by the method of application; although I can determine approximately 100 ml of water by eye, it is much more difficult to guess the temperature of 70 degrees. For myself, I defined approximately 70 degrees this way: the water is not boiling yet, but steam is already coming from it, I don’t know how correct this is, but there was no other way to cope with this task.
Inside the bag there are small granules of beige, white and yellow colors; they do not completely dissolve in water (this is also noted in the instructions). It is best to stir the prepared drink, and before the sediment sinks to the bottom, drink in small sips. For me, the taste seemed pleasant, ascorbic acid is clearly felt, but taste preferences are individual, so I don’t claim that everyone will like this taste. During the period of use, I experienced no side effects, and relief from symptoms occurred almost immediately.
I will briefly highlight the advantages that I noted: + Affordable price + There is some necessary information on the packaging + Quickly reduces the temperature + Really relieves the symptoms of flu and colds + Pleasant taste + Contains diphenhydramine, so it makes you fall asleep well + Contains ascorbic acid, so it not only alleviates the condition , but also helps the body fight the virus.
There are also disadvantages: - Unreadable instructions due to small and blurry font - When cooking, it is difficult to determine the required temperature.
In conclusion, I want to say that each body is individual and diseases are also different, so before using any drug, consult your doctor.
Be healthy!
