Ibuprofen: instructions for use, tablets,suspension, ointment, gel, indications, contraindications, coursetreatment

Update: October 2018

Ibuprofen is a non-steroid drug that has three
effects: anti-inflammatory, antipyretic and analgesic,
indiscriminate enzyme blocker TsOG1 and TsOG2. Is one of
propionic acid derivatives. Ibuprofen is actively used in
pediatrics, starting at three months of age. Distinctive
characteristics of drugs in this group:

  • do not cause addiction and development of resistance;
  • affect the speed of the psychomotor reaction and do not depress
    CNS activity;
  • have a wide range of appointments with a variety of
    pathologies.

Pharmacological group: NSAIDs.

Composition, physico-chemical characteristics, price

Ibuprofen is available in several dosage forms that
intended for both oral and skin use
and rectal administration.

Main substance Excipients Physicochemical properties

Pills

10 tab. in cellular packages. 2-5 packs per pack
cardboard.

  • № 20 200 mg: 15-17 rubles;
  • № 20 400 mg: 30-40 rubles.

200 or 400 mg ibuprofen

Magnesium stearate, potato starch, silica, vanillin,
beeswax, dye azorubine, food gelatin, magnesium
hydroxycarbonate, wheat flour, low molecular weight povidone,
titanium dioxide, sucrose
Pills светло-розовые или розовые, с оболочкой,
biconvex, bilayer with transverse section

 Suspension Ibuprofen Children’s Day (syrup)

In a glass bottle of 100 ml with a measuring spoon, in a cardboard
a pack.

  • 85-95 rubles

 100 mg ibuprofen in 5 ml suspension

 Glycerol, Polysorbate, Sorbitol, Citric Acid,
sodium saccharinate, xanthan gum, acid solution
hydrochloric and sodium hydroxide, methyl parahydroxybenzoate,
propyl parahydroxybenzoate, fruit flavor, purified
water
 Homogeneous suspension having almost white color
viscous, fruit flavored

 Suppositories

On 5 suppositories in planimetric packing, in a cardboard pack on 2
packaging.

  • № 10: 60-70 rubles.

 60 mg ibuprofen in 1 suppositories

 Solid fat  Torpedo-shaped suppositories of white or almost white
colors with a smooth surface

 Ibuprofen gel

On 100, 50, 30, 20 g in an aluminum tuba, in a pack cardboard

  • 50 g: 80-90 rub.

 50 mg ibuprofen in 1 g of gel

 Ethanol, dimexide propylene glycol, carbomer,
methyl parahydroxybenzoate, triethanolamine, neroli oil,
лавандовое масло, water очищенная
 Colorless or with a yellowish sheen transparent gel,
having a peculiar smell

 Ibuprofen Ointment

On 15 and 25 g in an aluminum tuba, in a pack cardboard

  • 25 g: 30 rub.

 50 mg ibuprofen and 100 mg dimethyl sulfoxide in 1 g
ointment

 Macrogol 1500 and 400  White ointment with peculiar smell

pharmachologic effect

Provides analgesic, antipyretic and anti-inflammatory
action by indiscriminately blocking cyclooxygenase (1 and
2) and inhibiting the synthesis of prostaglandins (mediators
inflammatory reactions). The analgesic effect is more pronounced with
pain associated with inflammatory reactions. As for others
NSAIDs, antiplatelet activity is characteristic of ibuprofen
(inhibits the aggregation of blood cells – platelets). With long
treatment may have a desensitizing effect.

With outdoor use also has an active
analgesic and anti-inflammatory effect. Normalizes
vascular permeability reduces the liberation of inflammatory mediators.
Диметилсульфоксид, второй активный компонент ointment, оказывает
local non-specific anti-inflammatory effect and enhances
ibuprofen penetration into affected tissues.

Pharmacokinetics

With internal use of the drug is almost completely
absorbed from the digestive tract, but at the same time eating speed
suction slows down. When taken on an empty stomach, the maximum concentration in
blood is reached after 45 minutes, and after eating – in 90-150
minutes

Metabolism is carried out in the liver (up to 90%). After absorption
approximately 60% of the inactive R-form of the active substance
transformed into an S-form, which has pharmacological
activity. Excreted in the urine as inactive metabolites (up to 80
%), the rest is excreted by the intestines.

When applied externally does not penetrate into the system
blood flow. When released into the cavity of the joints accumulates in
synovial fluid.

Indications for use

  • Inflammatory diseases of the spine and joints, including
    ankylosing spondylitis, sciatica, rheumatoid arthritis, disease
    Ankylosing spondylitis, osteoarthritis, gouty arthritis.
  • Pain syndrome of moderate severity
    of origin: migraine, headache, neuralgia, toothache,
    postoperative and traumatic pains, algomenorrhea
    primary.
  • Fever accompanying infectious and colds
    diseases.
  • Symptomatic treatment of diseases (reduction of pain and
    inflammation), not affecting the progression
    pathology.
  • Dosage forms for external use are shown when
    lumbago, myalgia, tendinitis, bursitis, injuries occurring without
    tissue integrity disorders.

In pediatrics, the drug is used as an effective
antipyretic to help eliminate febrile
flu syndrome, childhood infections, acute respiratory infections, post-vaccination
reactions and other infectious and inflammatory changes. Effective in
as an anesthetic medicine for pain symptoms (moderate
and weak): headache, sore throat and ears, and toothache and
others

Contraindications

  • Hypersensitivity to any component in the composition
    ibuprofen dosage forms.
  • Hypersensitivity to other drugs from the group of NSAIDs
    (attacks of bronchial obstruction, urticaria, bronchial asthma and
    others).
  • Diseases of the digestive tract with ulcerative tissue in the stage
    exacerbations (ulcerative colitis, peptic ulcer,
    Crohn’s disease and others).
  • Inflammatory bowel changes.
  • Bleeding disorders, including hemophilia,
    hemorrhagic diathesis.
  • The recovery period after coronary artery
    shunting
  • Bleeding from the gastrointestinal tract, intracranial hemorrhage.
  • Hepatic insufficiency, acute
    liver disease.
  • Progressive kidney disease.
  • Severe renal failure, with clearance
    creatinine less than 30 ml / min and confirmed hyperkalemia.
  • Pregnancy.
  • Ibuprofen is contraindicated in children under the age of 3 months (suspension,
    suppositories), up to 6 years (tablets, gel), and up to 14 years (ointment).
  • Violation of the integrity of the skin (for external forms).

С осторожностью назначают для treatment следующих групп пациентов
and in the presence of pathologies:

  • Elderly age;
  • Bad habits (smoking, alcohol);
  • Hypertension, heart failure and coronary artery disease;
  • Cerebrovascular diseases;
  • Diabetes, dyslipidemia;
  • Peripheral artery disease;
  • Liver cirrhosis with portal-type hypertension;
  • Nephrotic syndrome;
  • Insufficiency of liver or kidney function with creatinine clearance
    less than 60 ml / min;
  • Hyperbilirubinemia;
  • Peptic ulcer disease (in remission);
  • H. pylori infection;
  • Gastropathy, enteritis, colitis;
  • Blood pathologies of unknown origin (anemia,
    leukopenia);
  • Long-term treatment with drugs from the group of NSAIDs;
  • Simultaneous treatment with hormonal drugs (contraceptives,
    prednisone), anticoagulants (warfarin inclusive),
    antiplatelet agents (clopidogrel, aspirin), selective inhibitors
    serotonin reuptake (paroxetine, citalopram,
    sertraline);
  • Severe somatic diseases;
  • Lactation period.

Dosage

  • Pills — в инструкция по применению таблеток ибупрофена
    It is indicated that the morning dose is taken before meals with water.
    The rest of the dose – after eating, drinking water.
  • Suspension – applied orally, after meals. Before taking
    Shake it carefully. The required amount of drug
    measured with a measuring spoon or syringe.
  • Suppositories — лекарственная форма применяется ректально,
    gently inserting the suppository into the anus.
  • Gel – a strip of gel 4-10 cm is applied to the problem area and
    carefully rubbed. When used in children from 6 to 12 liters (older than
    equal to adults) a strip of gel 2-4 cm applied to the skin in
    affected area and rubbed.
  • Мазь — небольшую полоску ointment (до 5-10 см) наносят на
    problem area and carefully rubbed until completely absorbed in
    skin

Pills

  • Adults-children from 12 years: 200 mg three times-four times
    day.
  • Первые приемы допускается по 400 мг трижды в day.
  • The maximum daily dose is 1200 mg.
Children 6 (more than 20 kg) -12 l: 200 mg three times or four times
day.

The intervals between receptions for adults and children over 12 l – not
less than 4 hours, for the category of children 6-12 liters – 6 hours

Course – no more than 5 days.

Suspension

Vaccine reactions:

Дети 3-6 мес (5-7.5 кг): по 2.5 мл два раза в day.

  • Children 6-12 months (7-9 kg): 2.5 ml three times or four times
    day.
  • Children 12 months-3 l (10-15 kg): 5 ml three times during
    days.
  • Дети 3-6 л (16-20 кг): по 7.5 мл трижды в day.
  • Дети 6-9 л (21-29 кг): по 10 мл трижды в течение days.
  • Дети 9-12 л (30-40 кг): по 15 мл трижды в day.

The interval between receptions – 6 hours.

The course in the treatment of pain – no more than 5 days., Fever
– no more than 3 days.

 Suppositories

 Vaccine reactions:

  • children under 1 year – 1 candle;
  • children over 1 year old – 1 more candle 6 hours after administration
    first.
Elimination of pain and fever. Single dose: 5-10 mg
per 1 kg of body weight of a child with a frequency of three to four times a day.
  Максимальная доза — не более 30 мг на 1 кг веса в day.

  • Children 3-9 months (5.5-8.0 kg): 1 candle three times a day
    an interval between introductions of 6-8 h.
  • Дети 9-24 м (8.0-12.5 кг): по 1 свече четырежды в сутки с
    at intervals of 6 hours
  The interval between injections is 6-8 hours.

 Gel and ointment

Adults and children from 12 liters use the drug up to four times
сутки, дети 6-12 л – трижды в day.

 The interval between application – 4 hours

В инструкции к ointment и гелю Ибупрофен указан курс применения 2-3
of the week.

Side effects

  • Gastrointestinal tract: the phenomenon of gastropathy, expressed abdominal pain,
    dry mouth, heartburn, nausea, vomiting, loss of appetite,
    diarrhea, flatulence, constipation. Occasionally ulceration occurs
    mucous membrane of the stomach and intestines, with a possible, extremely rare
    complication in the form of bleeding and perforation, as well as pancreatitis
    (these reactions are most likely with long-term treatment). With
    side of the liver may develop hepatitis.
  • Respiratory: bronchospachm, shortness of breath.
  • Sense organs: hearing loss, ringing or tinnitus, unclear
    eyesight, double vision, dry cornea, eyelid edema and
    conjunctiva.
  • Central and peripheral NS: dizziness, headache,
    sleep disturbance, irritability, confusion, depression,
    psychomotor agitation. In rare cases, people with autoimmune
    pathology develops aseptic meningitis.
  • Cardiovascular system: hypertension, cardiac
    failure, tachycardia.
  • Excretory system: allergic type jade, acute
    renal failure, edema, cystitis, polyuria.
  • Allergic reactions that are also characteristic of external forms:
    skin rash on the type of erythema and urticaria, tingling, angioedema,
    itchy skin. Rarely – anaphylactic shock, erythema multiforme
    exudative type, bronchospasm, allergic rhinitis,
    eosinophilia.
  • Blood system: anemia, agranulocytosis,
    thrombocytopenic purpura, thrombocytopenia and leukopenia.
  • Other reactions – increased sweating.

Laboratory indicators:

  • Increase: bleeding time, creatinine concentration
    serum, activity of “liver” transaminases.
  • Decrease: concentrations of glucose, hemoglobin, hematocrit,
    creatinine clearance.

Overdose

With a significant excess of doses of the drug for internal use
The following symptoms develop: epigastric pain, drowsiness,
vomiting, headache, tinnitus, metabolic acidosis, coma,
pressure drop, tachycardia, atrial fibrillation. Treatment
stationary.

Drug interactions

  • Ibuprofen not recommended for simultaneous treatment
    other NSAIDs;
  • When prescribed with anticoagulants increases the risk
    bleeding;
  • When interacting with serotonin reuptake blockers
    increases the risk of bleeding from the gastrointestinal tract;
  • With simultaneous treatment with cephalosporins, the frequency increases.
    hypoprothrombinemia, increases the risk of nephrotoxic and hepatotoxic
    effects;
  • When treated with inducers of microsomal oxidation
    the risk of intoxication increases;
  • Barbiturates and preparations with ethanol increase the concentration
    ibuprofen in blood plasma;
  • Reduces the effect of vasodilators, furosemide and
    hydrochlorothiazide;
  • Increases antiplatelet activity, indirect
    anticoagulants, fibrinolitikov, hypoglycemic drugs and
    insulin, sulfonylurea derivatives;
  • Kolestiramin and antacids reduce the absorption of ibuprofen;
  • Caffeine enhances the analgesic effect of ibuprofen.

Analogs

Nurofen (tablets, gel, suppositories suspension), Nurofen Forte,
Mig 400, Dolgit, Advil, Ibufen.

Nurofen 200-300 rubles. Миг 400  80 руб. Long 100 rubles. Paspik 120 rub. Ibufen

Автор: врач-гигиенист, эпидемиолог

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