Askofen ULTRA

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Askofen ULTRA: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Ascophen ULTRA

ATX code: N02BA71

Active ingredients: acetylsalicylic acid (Acetylsalicylic acid) + paracetamol (Paracetamol) + caffeine (Caffeine)

Manufacturer: Open Joint Stock Company Pharmstandard-Leksredstva (Russia)

Description and photo update: 2020-28-05

Prices in pharmacies: from 68 rubles.

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Askofen ULTRA is a combined analgesic drug.

Release form and composition

The drug is produced in the form of film-coated tablets: oval, shell and core - white or almost white (10 pcs. In blisters, in a cardboard box 1, 2 or 3 packs and instructions for use of Askofen ULTRA).

1 tablet contains:

active ingredients: acetylsalicylic acid - 250 mg, paracetamol - 250 mg, caffeine (anhydrous caffeine) - 65 mg;
auxiliary components: microcrystalline cellulose (microcrystalline cellulose 101), hyprolose (hydroxypropyl cellulose), hyprolose (low-substituted hydroxypropyl cellulose), aerosil (colloidal silicon dioxide), stearic acid, calcium stearate, talc;
film casing: Opadray 20A28380 WHITE [hypromellose (hydroxypropyl methylcellulose 2910), hyprolose (hydroxypropyl cellulose), titanium dioxide, talc].

Pharmacological properties

Pharmacodynamics

Askofen ULTRA is a combined preparation, the action of which is due to the following properties of its active ingredients:

acetylsalicylic acid: a non-steroidal anti-inflammatory drug (NSAID), has antipyretic and anti-inflammatory effects, relieves pain, especially in the presence of an inflammatory process. Promotes the improvement of microcirculation in the focus of inflammation, suppression of platelet aggregation and thrombus formation;
paracetamol: an analgesic non-narcotic agent, has antipyretic, analgesic and very mild anti-inflammatory effects. The effect is associated with the influence of paracetamol on the center of thermoregulation in the hypothalamus and a weak inhibition of prostaglandin synthesis in peripheral tissues;
caffeine: a psychostimulant substance that causes an increase in the reflex excitability of the spinal cord, expansion of the blood vessels of the brain, heart, kidneys and skeletal muscles, and reduces platelet aggregation. Excitation of the respiratory and vasomotor centers leads to a decrease in the feeling of fatigue and drowsiness, an increase in mental and physical performance. A low dose of caffeine in this combination helps to increase the tone of the cerebral vessels and accelerate blood flow, but practically does not stimulate the central nervous system.

Pharmacokinetics

After oral administration, acetylsalicylic acid is completely absorbed, it undergoes presystemic elimination in the intestinal wall, and deacetylation in the liver. It is hydrolyzed rapidly with the participation of cholinesterases and albuminesterases. The maximum concentration (C _max) in the blood is reached after 2 hours.

Binding to blood proteins (albumin) - 75-90%.

It is distributed in tissues in the form of salicylic acid anion.

It is metabolized mainly in the liver to form four metabolites found both in urine and in many tissues of the body.

The half-life (T _1/2) is no more than 1/3 hour.

It is excreted mainly in the urine as a result of active secretion in the renal tubules in the form of salicylate (60%) and its metabolites. The amount of unchanged salicylate depends on the pH (acidity) of the urine. Alkalinization of urine causes an increase in the ionization of salicylates, worsens their reabsorption and significantly increases excretion. The excretion rate depends on the dose, T _1/2 when taking small doses - 2-3 hours, while taking high doses, it can increase to 15-30 hours.

Elimination of salicylates in newborns is much slower than in adults.

After ingestion, caffeine is well absorbed throughout the intestine. Absorption occurs mainly due to lipophilicity rather than solubility of the substance in water. C _max of caffeine in blood reached after 50-75 minutes and is 1.6-1.8 mg / l.

Binding to blood proteins (albumin) - 25–36%. Volume of distribution: adults - 0.4-0.6 l / kg, newborns - 0.78-0.92 l / kg.

It is actively distributed in all organs and tissues of the body. It overcomes the blood-brain barrier (BBB), easily crosses the placenta.

In adults, caffeine is metabolized primarily (over 90% of the dose taken) in the liver. About 80% of the dose taken is biotransformed into paraxanthine, 10% into theobromine, and about 4% into theophylline. Subsequently, these compounds are demethylated to monomethylxanthines and methylated uric acids. In children of the first years of life, no more than 10-15% of the dose of caffeine taken is metabolized.

T _1/2 in adults can be from 3.9 to 5.3 hours, in some cases it can reach 10 hours. Caffeine is excreted through the kidneys, in adults in unchanged form - 1–2%, the rest - in the form of metabolites.

After oral administration, absorption of paracetamol is high. Its C _max in the blood is reached in 0.5–2 hours and is 0.005–0.02 mg / ml. To achieve a therapeutically effective level of concentration of paracetamol in plasma, it should be prescribed at the rate of 10-15 mg per 1 kg (mg / kg) of the patient's weight.

Plasma proteins bind up to 15% of the dose.

It penetrates the BBB, less than 1% of the dose taken is found in breast milk.

Paracetamol is metabolized in the liver (90–95% of the dose taken). As a result of hydroxylation of 17% of the substance, 8 active metabolites are formed, which are converted into inactive metabolites after conjugation with glutathione. With a deficiency of glutathione, active metabolites can block the enzyme systems of hepatocytes and cause their necrosis. In the conjugation reaction with the formation of inactive glucuronides and sulfates, 80% of paracetamol enters. In addition, isoenzymes CYP1A2, CYP2E1 and, to a lesser extent, CYP3A4 are involved in the metabolism of paracetamol.

T _1/2 is 1-4 hours.

It is excreted through the kidneys mainly in the form of metabolites (conjugates), unchanged - less than 5%.

In elderly patients, paracetamol clearance decreases, T _1/2 increases.

The pharmacokinetics of the drug in case of impaired liver or kidney function has not been established, therefore, given the presence of acetylsalicylic acid and paracetamol in its composition, the appointment of Askofen ULTRA is contraindicated in patients with severe hepatic or renal insufficiency. For mild to moderate hepatic or renal impairment, caution is advised.

Indications for use

The indication for Askofen ULTRA is pain syndrome of moderate and mild intensity of various origins in patients over 15 years old, including the following diseases and conditions:

migraine;
headache;
neuralgia;
myalgia;
arthralgia;
toothache;
algodismenorrhea.

In addition, Askofen ULTRA is prescribed for adult patients for acute respiratory diseases and flu as an antipyretic agent.

Contraindications

Absolute:

phase of exacerbation of erosive and ulcerative lesions of the gastrointestinal tract (GIT);
perforation or gastrointestinal bleeding;
history of peptic ulcer;
complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid or other NSAIDs, including a history;
hemophilia or other blood clotting disorders;
hypoprothrombinemia;
hemorrhagic diathesis;
vitamin K deficiency;
arterial hypertension of the III degree;
portal hypertension;
chronic heart failure III – IV functional class according to NYHA classification (New York Heart Association);
severe degree of renal or hepatic failure;
deficiency of glucose-6-phosphate dehydrogenase;
glaucoma;
sleep disorders, increased nervous irritability;
surgical operations accompanied by severe bleeding;
concomitant therapy with methotrexate at a dose of more than 15 mg per week;
period of pregnancy;
breast-feeding;
age up to 15 years - for use as an anesthetic;
age up to 18 years - with febrile syndrome;
hypersensitivity to the components of the drug.

Ascofen ULTRA should be taken with caution according to indications for mild and moderate renal or hepatic failure, alcoholism, gout, hyperthyroidism, epilepsy, diabetes mellitus, a tendency to seizures, arrhythmias, coronary heart disease, chronic heart failure of I – II functional class according to the classification NYHA, uncontrolled arterial hypertension, peripheral arterial disease, cerebrovascular disease, chronic obstructive pulmonary disease, smoking; while using methotrexate at a dose of less than 15 mg per week, anticoagulants, NSAIDs, glucocorticosteroids (GCS), antiplatelet agents, selective serotonin reuptake inhibitors; in old age; if you have risk factors for dehydration (such as vomiting, diarrhea, before or after major surgery).

Askofen ULTRA, instructions for use: method and dosage

Ascofen ULTRA tablets are taken orally during or after meals.

Recommended dosage:

relief of pain syndrome in patients over 15 years old: 1 pc. 4-6 times a day for no more than 5 days;
migraine: 2 pcs. when the first signs of illness appear, the drug can be used for no more than 4 days;
febrile syndrome in adults: 2 pcs. 4 times a day at regular intervals. The duration of the course of treatment without consulting a doctor is no more than 3 days.

The maximum daily dose is 6 pcs.

The analgesic effect after taking 2 tablets usually comes quickly - after about 1/4 hour, with migraine - after 1/2 hour.

If you need a longer use of Askofen ULTRA, you should consult a doctor.

The drug should be taken with caution in patients over the age of 65, especially the elderly with low body weight.

Side effects

The frequency of side effects of Askofen ULTRA is given in accordance with the recommendations of the WHO (World Health Organization): very often - from 1/10; often - from 1/100 to 1/10; infrequently - from 1/1000 to 1/100; rarely - from 1/10 000 to 1/1000; extremely rare - less than 1/10 000; with an unknown frequency - the incidence of adverse events cannot be determined from the available data.

infections and invasions: rarely - pharyngitis;
metabolic and nutritional disorders: rarely - decreased appetite;
mental disorders: often - nervousness; infrequently - insomnia; rarely - internal tension, anxiety, euphoria;
from the nervous system: often - dizziness; infrequently - headache, tremor, paresthesia; rarely - pain in the paranasal sinuses, disorder of taste and / or attention, impaired coordination of movement, amnesia, hyperesthesia;
on the part of the organ of vision: rarely - visual impairment;
on the part of the organ of hearing: infrequently - tinnitus;
on the part of the cardiovascular system: infrequently - arrhythmia, increased heart rate;
on the part of the vessels: rarely - impaired peripheral circulation, hyperemia;
from the respiratory system, chest and mediastinal organs: rarely - rhinorrhea, hypoventilation, nosebleeds;
from the digestive system: often - abdominal discomfort, nausea; infrequently - vomiting, diarrhea, dry mouth; rarely - increased salivation, belching, flatulence, paresthesia in the mouth, dysphagia;
on the part of the skin and subcutaneous tissues: rarely - itching, hyperhidrosis, urticaria;
from the musculoskeletal system: rarely - pain in the neck and / or back, muscle spasms, musculoskeletal stiffness;
general disorders: infrequently - fatigue, increased excitability; rarely - heaviness in the chest, asthenia.

Side effects of Askofen ULTRA registered in the post-registration period:

mental disorders: anxiety;
from the immune system: hypersensitivity reactions;
from the nervous system: drowsiness, migraine;
on the part of the cardiovascular system: a feeling of palpitations;
from the side of the vessels: lowering blood pressure (BP);
from the digestive system: pain in the epigastrium and / or abdomen, dyspepsia, erosive and ulcerative lesions of the gastrointestinal tract (including ulcers of the stomach, duodenum and / or colon, peptic ulcer), gastrointestinal bleeding (including bleeding from a stomach ulcer, duodenum and / or rectum, upper gastrointestinal tract and / or stomach);
from the hepatobiliary system: hepatic failure;
from the respiratory system, chest and mediastinal organs: bronchospasm, shortness of breath;
from the skin and subcutaneous tissues: rash, erythema, erythema multiforme, angioedema;
general disorders: discomfort, malaise.

Overdose

In case of an overdose, the combined composition of Askofen ULTRA should be taken into account.

Symptoms of an overdose of acetylsalicylic acid: with a mild degree of intoxication (plasma concentration 0.15–0.3 mg / ml) - increased sweating, nausea, vomiting, dizziness, headache, confusion, tinnitus, deafness. With severe intoxication (plasma concentration above 0.3 mg / ml) - fever, hyperventilation, anxiety, respiratory alkalosis, ketoacidosis, metabolic acidosis, significant depression of the central nervous system (including coma), cardiovascular collapse, respiratory failure. In children and the elderly, the development of chronic intoxication is most likely when acetylsalicylic acid is taken in a daily dose of more than 100 mg / kg of body weight for several days.

Treatment: with a mild degree of intoxication - lower the dose or stop taking the drug. If there is a suspicion that during the last hour the patient has taken more than 120 mg / kg of salicylates, then repeated intake of activated charcoal is indicated. If a single dose of more than 120 mg / kg of salicylates is suspected, a determination of their plasma concentration is required. In addition, to determine the severity of intoxication, it is necessary to take into account clinical and biochemical parameters. With a plasma concentration of salicylates above 0.5 mg / ml (for children under 5 years old - 0.35 mg / ml), intravenous (i.v.) administration of sodium bicarbonate, above 0.7 mg / ml (or in severe metabolic acidosis) is indicated - therapy of choice is hemoperfusion or hemodialysis.

Symptoms of a paracetamol overdose: loss of appetite, nausea, vomiting, pallor of the skin, discomfort in the abdominal cavity and / or abdominal pain. A single dose of paracetamol at a dose of 7500 mg (or more) for adults and more than 140 mg / kg of body weight for children causes cytolysis of hepatocytes with complete and irreversible liver necrosis, liver failure, metabolic acidosis and encephalopathy. In some cases, coma and death can result from these disorders. 12–48 hours after an overdose, an increase in the concentration of bilirubin, the activity of microsomal liver enzymes and lactate dehydrogenase, and a decrease in the level of prothrombin are observed. The clinical manifestation of symptoms of liver damage occurs 2 days after taking an excessive dose of paracetamol and reaches its maximum on 4-6 days. In case of an overdose, intoxication may appear, more often in children, elderly patients, with malnutrition, the presence of liver diseases caused by chronic alcoholism, or while taking inducers of microsomal liver enzymes. It can lead to the development of fulminant hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis (including fatal ones).

Treatment: the clinic of acute overdose of paracetamol develops within the first 24 hours after ingestion of a high dose. In this regard, if an overdose is suspected, immediate hospitalization of the patient is required and the determination of the paracetamol content in the blood plasma. During the first 8 hours, the most effective administration of methionine and intravenous administration of acetylcysteine (donors of SH-groups and precursors of glutathione synthesis). Additional therapeutic measures are carried out as needed, taking into account the level of concentration of paracetamol in the blood and the period after the overdose. A careful observation of the patient's condition and the appointment of symptomatic therapy are shown, as well as regular (every 24 hours) laboratory tests to determine the activity of liver microsomal enzymes. The activity of these enzymes in most cases is normalized within 7-14 days. For very severe intoxication, a liver transplant may be necessary.

Caffeine overdose symptoms: pyrexia, headache, insomnia, anxiety, nervousness, agitation, delirium, anxiety, mental agitation, confusion, muscle twitching, convulsions, nausea, vomiting (possibly with blood), gastralgia, urinary frequency, dehydration, increased tactile or pain sensitivity, tinnitus, tachycardia, arrhythmia, with severe overdose - hyperglycemia.

Treatment: lower the dose or stop taking caffeine.

special instructions

Do not take Askofen ULTRA while using medications containing acetylsalicylic acid or paracetamol!

After taking acetylsalicylic acid, the increased risk of bleeding persists for 4-8 days. Severe bleeding (including cerebral hemorrhage) in rare cases can occur with the simultaneous use of anticoagulants and / or in patients with untreated arterial hypertension.

Caution should be exercised in patients with atypical symptoms of migraine or those who have it for the first time, it is necessary to exclude the presence of other potentially serious neurological disorders.

Askofen ULTRA should not be used if, during the relief of migraine attacks, patients vomit in more than 20% of episodes or the need for bed rest in more than 50% of episodes. If, after taking two pills, the migraine pain syndrome does not stop, you should consult a specialist.

It is recommended to stop taking the drug and consult a doctor if the headache has occurred over the past few (three or more) months more than 10 times a month.

It should be borne in mind that Askofen ULTRA can mask the signs and symptoms of infection.

The simultaneous use of alcoholic beverages is contraindicated. A special risk group for liver damage includes patients with a history of alcoholism.

Taking Askofen ULTRA can distort the results of a number of clinical and biochemical laboratory tests, including the determination of glycemia by the glucose oxidase or peroxidase method, and uric acid by the phosphotungstic acid method. When planning a study of coronary blood flow and assessment of myocardial function, it is necessary to stop taking the drug for 8-12 hours. In addition, the results of thyroid function tests may be distorted.

It should be borne in mind that the use of Askofen ULTRA may prolong the bleeding period during and after surgical interventions (including tooth extraction).

With metro or menorrhagia, special care should be taken.

When the first symptoms of the negative influence of Askofen ULTRA appear on the gastrointestinal tract, it must be canceled immediately. This is associated with a high risk of severe bleeding, ulceration and perforation of the gastrointestinal tract, including with a fatal outcome.

It should be borne in mind that concomitant therapy with other potentially hepatotoxic drugs or drugs that induce microsomal liver enzymes (including phenobarbital, phenytoin, carbamazepine and other anticonvulsants, rifampicin, isoniazid, chloramphenicol, hypnotics), the risk of paracetamol poisoning increases.

Taking the pills should be stopped at the first signs of hypersensitivity and consult a doctor. This is associated with the risk of developing serious skin reactions, including acute generalized exanthematous pustulosis, toxic epidermal necrolysis, and Stevens-Johnson syndrome.

During the period of administration of Askofen ULTRA, the intake of caffeine-containing products into the body can cause nervousness, insomnia, irritability, and increased heart rate in patients, therefore it is recommended to limit their consumption.

Influence on the ability to drive vehicles and complex mechanisms

Patients should refrain from driving vehicles or other complex mechanisms if the reception of Askofen ULTRA is accompanied by the occurrence of such undesirable phenomena as drowsiness or dizziness.

Application during pregnancy and lactation

The use of Askofen ULTRA is contraindicated during pregnancy and breastfeeding.

Pediatric use

The use of Askofen ULTRA is contraindicated as an anesthetic in children under 15 years of age and as an antipyretic - up to 18 years.

Taking the drug for febrile syndrome in patients under the age of 18 increases the risk of Reye's syndrome in case of a viral infection.

With impaired renal function

The use of Askofen ULTRA is contraindicated in patients with severe renal failure.

It is recommended to take ASCofen ULTRA with caution in case of mild to moderate renal failure.

For violations of liver function

The use of Askofen ULTRA is contraindicated in severe hepatic insufficiency.

It is recommended to take Ascofen ULTRA with caution in case of mild and moderate liver failure.

Use in the elderly

Ascofen ULTRA should be used with caution for the treatment of elderly patients (especially with low body weight).

Drug interactions

GCS, other NSAIDs: contribute to an increase in the damaging effect on the gastrointestinal mucosa, increase the risk of developing gastrointestinal bleeding. In this regard, such combinations should be avoided or drugs should be taken in combination with gastroprotective agents in order to prevent NSAID-induced gastrointestinal ulcers;
coumarin derivatives and other oral anticoagulants: can enhance their effect, therefore, clinical and laboratory monitoring of bleeding time and prothrombin time is required;
thrombolytics, heparin, platelet aggregation inhibitors (paracetamol, clopidogrel, cilostazol, ticlopidine): concomitant therapy with each of these agents increases the risk of bleeding;
selective serotonin reuptake inhibitors: may affect blood clotting and increase the risk of bleeding;
phenytoin: monitoring of the plasma concentration of phenytoin should be ensured due to the high risk of its increase;
valproic acid: increased risk of valproic acid toxicity;
aldosterone antagonists (spironolactone, canrenoate): may reduce their activity, careful monitoring of blood pressure is required;
loop diuretics (including furosemide): they can reduce their clinical effect, therefore, when combined with Askofen ULTRA, it is necessary to control renal function and blood pressure, to ensure sufficient rehydration of the patient;
angiotensin-converting enzyme inhibitors, slow calcium channel blockers, angiotensin II receptor antagonists: may reduce their activity; it should be borne in mind that in dehydrated or elderly patients, concomitant therapy with each of these antihypertensive drugs increases the risk of developing acute renal failure;
probenecid, sulfinpyrazone: a decrease in the clinical effect of these and other uricosuric drugs is possible;
methotrexate (at a dose of less than 15 mg per week): its toxicity may increase, especially in patients with impaired renal function. Therefore, taking Askofen ULTRA is allowed only under medical supervision, control of a general blood test, liver and kidney function;
sulfonylurea derivatives, insulin: enhance their hypoglycemic effect; blood glucose levels should be monitored more often;
ethanol: the risk of gastrointestinal bleeding increases;
inducers of microsomal liver enzymes, hypnotics, antiepileptic drugs (including phenobarbital, phenytoin, carbamazepine), rifampicin, isoniazid, alcohol: potentially hepatotoxic substances contribute to a significant increase in paracetamol toxicity;
chloramphenicol: the risk of a clinically significant increase in the concentration of chloramphenicol increases;
zidovudine: a combination with zidovudine is allowed only on the recommendation of a doctor, an increase in the tendency to develop neutropenia is possible;
probenecid: against the background of concomitant therapy with probenecid, the clearance of paracetamol decreases;
indirect anticoagulants: it should be borne in mind that while taking Askofen ULTRA for more than one week, the effect of anticoagulants increases;
drugs that slow gastric emptying (including propantheline): may delay or reduce rapid pain relief;
drugs that accelerate evacuation from the stomach (including metoclopramide): promote faster absorption of Askofen ULTRA and the onset of its analgesic effect;
cholestyramine: the analgesic effect of paracetamol slows down, therefore, if it is necessary to use this combination, cholestyramine should be taken only 1 hour after taking the drug;
hypnotics (including barbiturates, benzodiazepines, H ₁ -histamine receptor blockers): may reduce their effect; the anticonvulsant effect of barbiturates decreases; it is advisable to avoid such combinations of drugs;
lithium: renal clearance of lithium increases;
disulfiram: the stimulating effect of caffeine on the cardiovascular and central nervous system increases the risk of exacerbating alcohol withdrawal syndrome; the combination of Askofen ULTRA with disulfiram is contraindicated;
ephedrine-like substances: concomitant therapy with ephedrine-like substances increases the risk of drug dependence;
sympathomimetics, levothyroxine: these agents should not be combined with the drug due to the possible increase in the chronotropic effect;
theophylline: theophylline excretion decreases;
terbinafine, cimetidine, fluvoxamine, quinolone antibacterial drugs, enoxacin, pipemidic acid, oral contraceptives: these agents increase the half-life of caffeine;
nicotine, phenytoin, phenylpropanolamine: the combination with each of the listed agents causes a decrease in the terminal half-life of caffeine;
clozapine: increases the serum concentration of clozapine.

Analogs

Askofen ULTRA analogues are Askofen-P, Aquacitramon, Kofitsil-plus, Migrenol Extra, Citramarine, Citramon P, Citramon P Forte, Citramon Ultra, Citramon-MFF, Citrapar, Excedrin, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C, protected from moisture.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Askofen ULTRA

Reviews about Askofen ULTRA are positive. Patients indicate a quick action of the drug in case of migraine, headache and high body temperature, good tolerance and absence of undesirable effects.

The disadvantages include a large list of contraindications.

Price for Askofen ULTRA in pharmacies

The price of Askofen ULTRA for a package containing 10 tablets can be from 78 rubles, 20 tablets - from 141 rubles.

Askofen ULTRA: prices in online pharmacies

Drug name

Price

Pharmacy

Askofen Ultra film-coated tablets 10 pcs.

RUB 68

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Askofen ultra tablets p.p. 250mg + 65mg + 250mg 10 pcs.

RUB 85

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Askofen Ultra film-coated tablets 20 pcs.

RUB 96

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Askofen ultra tablets p.p. 250mg + 65mg + 250mg 20 pcs.

146 r

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!