Budenofalk

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

Budenofalk: 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. Drug interactions
12. Analogs
13. Terms and conditions of storage
14. Terms of dispensing from pharmacies
15. Reviews
16. Price in pharmacies

Latin name: Budenofalk

ATX code: R.03. BA02

Active ingredient: budesonide (budesonide)

Manufacturer: Dr. FALK PHARMA GmbH (Germany)

Description and photo update: 2019-19-08

Prices in pharmacies: from 1602 rubles.

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Budenofalk is a glucocorticosteroid.

Release form and composition

Dosage forms of Budenofalk:

enteric capsules: hard gelatinous, size 1, body and lid - white, opaque; contents - pellets (granules) of round shape, white (10 pcs. in blisters, in a cardboard box 2, 5 or 10 blisters);
dosed foam for rectal use: creamy, persistent, almost white or white [14 doses in aerosol aluminum cans, in a cardboard box 1 can, complete with applicators (14 pcs.) and plastic bags (14 pcs.)].

The active substance is budesonide:

1 capsule - 3 mg;
1 dose of foam - 2 mg.

Additional components of capsules:

excipients: lactose monohydrate, sugar crumbs (starch syrup, sucrose), talc, povidone-K25, triethyl citrate, methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer (2: 0.2: 1) [Ammonio methacrylate tip A copolymer) RL], methacrylic acid and methyl methacrylate copolymer (1: 2) (Eudragit S), methacrylic acid and methyl methacrylate copolymer (1: 1) (Eudragit L), methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer (2: 0.1: 1) Ammonio-methacrylate copolymer (type B), Eudragit RS];
shell composition: gelatin, titanium dioxide, water.

Foam excipients: disodium edetate dihydrate, macrogol stearyl ether, water, propylene glycol, cetyl alcohol, citric acid monohydrate, emulsion wax (cetostearyl alcohol, polysorbate 60), propellants (under a pressure of about 2.5 bar: isobutane - 86.01% n-butane - 6.66% and propane - 7.24%).

The applicators supplied with rectal foam are coated with a lubricant consisting of a mixture of vaseline oil and white soft paraffin.

Pharmacological properties

Pharmacodynamics

Budesonide is a non-halogenated glucocorticosteroid with high biological activity. It exhibits anti-inflammatory, anti-exudative, anti-allergic and decongestant properties. Also, the drug is characterized by a membrane stabilizing and immunosuppressive effect.

Budesonide inhibits the release of mediators from macrophages, basophils and mast cells, and also leads to the redistribution and inhibition of the migration of inflammatory cells. One of the probable mechanisms of action of this substance is the induction of the production of specific proteins (for example, macrocortin). Macrocortin is an inhibitor of phospholipase A2, inhibits the formation of arachidonic acid from phospholipids of cell membranes and indirectly prevents the synthesis of inflammatory mediators - prostaglandins and leukotrienes.

When administered rectally, Budenofalk practically does not affect the functioning of the hypothalamic-pituitary-adrenal system and almost does not change the concentration of cortisol in the blood plasma. Rectal administration of budesonide does not have a clinically significant effect on the content of the bone fraction of alkaline phosphatase and osteocalcin in the blood serum, therefore, bone metabolism remains at the same level.

The local effect of budesonide on the intestines is to activate the processes of water absorption.

Pharmacokinetics

When taken orally, budesonide exhibits pronounced lipophilic properties and is absorbed in the intestine at a high rate due to good tissue permeability. Compared with classical glucocorticosteroids, this substance has a very high affinity for receptors. This determines the targeted local action of Budenofalk.

About 90% of the dose of budesonide taken is metabolized in the liver due to the "first pass" effect, and only about 10% has a systemic effect on the body. Of this amount, 90% of the active component of the drug binds to albumin and for this reason is in a biologically inactive form.

The systemic bioavailability of budesonide with rectal administration is higher compared to oral administration, which is explained by the direct entry of the substance from the rectum into the systemic circulation without participation in the processes of hepatic metabolism. The bioavailability of the drug with single and repeated use is 15.3% and 13.8%, respectively. There are no signs of cumulation of budesonide in the tissues after repeated administration.

The maximum concentration of the substance in the blood after rectal administration of 2 mg of Budenofalk on average reaches 0.8-0.9 ng / ml and is determined after 2-3 hours.

Rectal administration of Budenofalk in the form of foam leads to its spreading through the large intestine. Budenofalk is determined in the distal part of the sigmoid colon after about 2 hours, and in the proximal part after about 4 hours.

After entering the blood, budesonide is characterized by a large volume of distribution (about 3 l / kg). The degree of binding to blood plasma proteins is 85–90%.

After entering the body, approximately 90% of budesonide is intensively involved in biotransformation processes in the liver with the participation of cytochrome CYP3A. As a result, 16α-hydroxyprednisolone and 6β-hydroxybudesonide are formed - metabolites with low pharmacological activity, not exceeding 1% of the activity of budesonide itself.

Most of budesonide is excreted in urine, and only a small part of it is excreted in feces. With rectal administration, the average elimination half-life is about 3-4 hours. The clearance of budesonide reaches an average of 10 l / min.

In patients with liver dysfunctions, depending on the type and severity of the disease, the metabolism of budesonide in the cytochrome CYP3A system may decrease.

Indications for use

Enteric capsules

mild to moderate Crohn's disease involving the ileum and / or ascending colon;
autoimmune hepatitis without histological signs of liver cirrhosis.

Rectal foam

In the form of foam, Budenofalk is used for exacerbation of distal forms of ulcerative colitis with damage to the sigmoid and rectum.

Contraindications

Enteric capsules

Absolute:

intestinal infectious diseases (fungal, bacterial, viral, amoebic infections);
cirrhosis of the liver;
glucose-galactose malabsorption, lactase or sucrase / isomaltase deficiency, fructose, lactose or galactose intolerance;
children up to age 18;
lactation period;
hypersensitivity to the components of Budenofalk.

Relative:

peptic ulcer;
diabetes;
cataract;
glaucoma;
osteoporosis;
arterial hypertension;
tuberculosis;
a family history of diabetes or glaucoma;
pregnancy.

Rectal foam

Absolute:

intestinal infectious diseases (fungal, bacterial, viral, amoebic infections);
cirrhosis of the liver with signs of portal hypertension (for example, in the terminal stage of primary biliary cirrhosis);
pregnancy and lactation;
age up to 18 years;
hypersensitivity to the components of Budenofalk.

Relative:

peptic ulcer of the stomach and duodenum;
diabetes;
arterial hypertension;
tuberculosis;
cataract;
glaucoma;
osteoporosis;
a family history of diabetes or glaucoma.

Instructions for the use of Budenofalk: method and dosage

Enteric capsules

Budenofalk should be taken orally about 30 minutes before a meal, swallowing the capsules whole and drinking plenty of fluids.

For patients who have difficulty swallowing, you can open the capsules and take only the granules contained in them, without chewing and drinking a sufficient amount of liquid.

Recommended doses of Budenofalk for adults, depending on the indications:

Crohn's disease: 1 capsule 3 times a day for 8 weeks;
autoimmune hepatitis: 1 capsule 3 times a day, maintenance dose - 1 capsule 2 times a day (morning and evening). Duration of treatment - up to 6-12 months, maintenance therapy - up to 24 months.

At the end of the course of treatment, the dose should be gradually reduced: during the first week - up to 2 capsules per day (morning and evening), during the second week - up to 1 capsule once a day (in the morning). Only after that Budenofalk can be canceled.

Rectal foam

Budenofalk is applied rectally.

Unless otherwise prescribed by the doctor, the foam should be administered 1 dose once a day, in the morning or in the evening.

Rules for using Budenofalk foam:

place the applicator firmly on the cylinder head;
shake the can for 15 seconds to mix its contents;
remove the protective tab from the base of the dispensing head (in case of first use);
turn the cap so that the semicircular cutout on the safety ring is in line with the nozzle;
place your index finger on the cap and turn the balloon upside down;
insert the applicator as deep as possible into the rectum (for convenience, it is recommended to raise the leg, for example, put it on a chair);
inject 1 dose of the drug, to do this, press the cap all the way and slowly release it, wait 10-15 seconds and remove the applicator from the rectum (the temperature of Budenofalk at the time of injection should be 20-25 ºС);
remove the applicator, pack it in the supplied plastic bag and discard (a new applicator should be used for each injection);
Wash the hands.

To achieve the best effect, the introduction of Budenofalk is recommended after bowel movement.

After the procedure, you should try not to empty your bowels until morning.

The duration of the therapeutic course is determined by the doctor individually. The duration of treatment is at least 6-8 weeks.

Side effects

Enteric capsules

on the part of metabolism and nutrition: often (from> 1/100 to <1/10) - Cushing's syndrome, for example, abdominal obesity, moon face, hypertension, decreased glucose tolerance, diabetes mellitus, hypokalemia, sodium retention, edema, steroid acne, red striae, decreased function or atrophy of the adrenal cortex, disorder of the secretion of steroid hormones (eg, hirsutism, amenorrhea, impotence); very rarely (<1/10 000) - growth retardation in children;
from the musculoskeletal and connective tissue: often - muscle weakness, twitching, muscle and joint pain, osteoporosis; very rarely - aseptic necrosis of the femoral and humerus heads;
from the nervous system: often - headache; very rarely - idiopathic intracranial hypertension, including edema of the optic nerve head in adolescents;
on the part of the psyche: often - irritability, depression, euphoria; very rarely - behavior disorders, various psychiatric effects;
from the side of the immune system: often - infectious diseases;
on the vascular side: increased risk of thrombus formation, vasculitis (as one of the withdrawal symptoms in case of abrupt discontinuation of treatment after long-term therapy);
from the gastrointestinal tract: very rarely - dyspeptic disorders, constipation, gastroduodenal ulcers, pancreatitis;
on the part of the skin and subcutaneous tissues: ecchymosis, petechiae, contact dermatitis, impairment of wound healing, allergic eczema;
others: very rarely - malaise, weakness.

Rectal foam

general disorders and disorders at the injection site: often (from ≥ 1/100 to <1/10) - burning sensation and pain in the rectum; infrequently (from ≥ 1/1000 to <1/100) - weight gain, asthenia;
on the part of the blood and lymphatic system: infrequently - acceleration of the erythrocyte sedimentation rate, anemia, leukocytosis;
from the nervous system: infrequently - headache, dizziness, impaired perception of odors;
from the side of the psyche: infrequently - insomnia;
from the gastrointestinal tract: infrequently - aphthous stomatitis, flatulence, dyspepsia, abdominal pain, nausea, frequent urge to defecate, hemorrhoids, anal fissure, bleeding from the rectum, paresthesia in the abdominal region;
from the liver and biliary tract: infrequently - increased activity of liver enzymes, cholestasis;
from the side of the vessels: infrequently - increased blood pressure;
on the part of metabolism and nutrition: infrequently - increased appetite;
infectious and parasitic diseases: infrequently - urinary tract infections;
from the skin and subcutaneous tissues: infrequently - increased sweating, inflammation of the sebaceous glands (acne);
laboratory and instrumental data: infrequently - a change in the content of cortisol, an increase in amylase activity.

Possible side effects of systemic glucocorticosteroids (in very rare cases):

on the part of the organ of vision: glaucoma, cataract;
on the vascular side: increased blood pressure, increased risk of thrombosis, vasculitis (as one of the symptoms of withdrawal syndrome in case of abrupt discontinuation of treatment after long-term therapy);
from the nervous system: edema of the optic nerve head;
on the part of the psyche: irritability, depression, euphoria;
from the musculoskeletal and connective tissue: weakness, diffuse muscle pain, osteoporosis, aseptic necrosis of the femoral and humerus heads;
from the gastrointestinal tract: abdominal discomfort, constipation, duodenal ulcer, pancreatitis;
from the side of metabolism and nutrition: Cushing's syndrome;
on the part of the immune system: weakening of the body's defense systems and, as a result, increasing the risk of infection;
on the part of the skin and subcutaneous tissue: delayed wound healing, petechial and ecchymal hemorrhages, striae, allergic exanthema, contact dermatitis;
others: fatigue, discomfort.

Overdose

Overdose cases of Budenofalk have not been registered at the moment. When taking high doses of the drug, symptomatic therapy is prescribed.

special instructions

Before exposure to any stress factor or surgery, additional use of systemic glucocorticosteroids is recommended.

Budenofalk can suppress the function of the hypothalamic-pituitary-adrenal system.

In patients with autoimmune hepatitis, the serum activity of transaminases (alanine aminotransferase and aspartate aminotransferase) should be monitored regularly during treatment: during the first month of therapy - every 2 weeks, then - at least 1 time in 3 months. According to the results of the study, if necessary, the dose of budesonide is adjusted.

Due to the fact that Budenofalk can cause side effects that affect the speed of reactions and the ability to concentrate (for example, weakness, headache and visual impairment), during treatment, care should be taken when driving and engaging in potentially hazardous activities.

Application during pregnancy and lactation

During pregnancy, the use of Budenofalk in the form of foam for rectal administration is contraindicated. Budenofalk in the form of enteric capsules is allowed to be used during gestation with caution, only in extreme cases, when the potential benefit to the mother significantly outweighs the possible risks to the fetus. In women of reproductive age, before starting treatment, possible pregnancy should be excluded, and during the course of therapy, reliable methods of contraception should be used.

It is not known whether budesonide passes into breast milk, therefore, during the use of Budenofalk, breastfeeding must be stopped.

Pediatric use

Age under 18 is a contraindication to the use of Budenofalk.

Drug interactions

grapefruit juice: the effectiveness of budesonide decreases (the use of juice during treatment is not recommended);
cardiac glycosides: their effect may increase due to potassium deficiency;
inhibitors of cytochrome P ₄₅₀ (troleandomycin, ketoconazole, erythromycin, clarithromycin, ritonavir, itraconazole, cyclosporin): the glucocorticosteroid effect of budesonide is enhanced;
saluretics: the risk of increased hypokalemia increases;
estrogens and oral contraceptives (with the exception of low-dose drugs): may increase the effect of budesonide;
antacids and resins that can bind steroids (for example, cholestyramine): the effectiveness of budesonide may decrease (at least 2-hour intervals should be observed between doses of these drugs).

Analogs

The analogues of Budenofalk are: Budekort, Tafen Nazal, Tafen Novolizer, Pulmicort, Pulmicort Turbuhaler, Pulmex, Novopulmon E Novolizer, Budesonid-Inteli.

Terms and conditions of storage

Store at temperatures up to 25 ° C out of reach of children.

The shelf life is 3 years. The foam after the first opening of the balloon can be stored for 4 weeks.

The cylinder is under high pressure, so it should not be opened, punctured, exposed to sunlight, or heated to temperatures above 50 ºС. Do not use near hot objects and fire. Do not incinerate used empty cylinders.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Budenofalk

Many patients with Crohn's disease leave positive reviews about Budenofalk compared to other drugs in this group. There are also reports that the drug helps with diarrhea of unclear etiology and loss of appetite, has a calming effect on the inflamed intestines and has virtually no side effects. However, to prevent the disease from returning, some patients are advised to follow a diet. Also, the advantages of Budenofalk include a convenient form of release, and the disadvantages are high cost.

Price for Budenofalk in pharmacies

The approximate price of Budenofalk in the form of enteric capsules is 1,474‒1755 rubles (the package contains 20 pcs.). Dosed foam for rectal administration costs about 5080-5840 rubles (the package includes 14 doses).

Budenofalk: prices in online pharmacies

Drug name

Price

Pharmacy

Budenofalk 3 mg capsules 20 pcs.

1602 RUB

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Budenofalk 2 mg / dose rectal foam dosed 14 doses 1 pc.

3658 RUB

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Budenofalk 9 mg enteric granules 20 pcs.

RUB 4189

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Budenofalk granules for enteric 9mg pack. 20 pcs.

4475 RUB

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Budenofalk foam rectal dosage. 2mg / 14 doses balloon

RUB 5158

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, 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!