Diclofenac: instructions for use

Update: October 2018

Diclofenac – a drug from the group of NSAIDs, is a derivative
phenylacetic acid. In dosage forms is presented in the form
sodium salt. It is in the list of vital
drugs.

The drug was created in 1956 and was originally used in
treatment of rheumatological diseases, providing a powerful
analgesic and anti-inflammatory effects. Gradually sphere
use of the drug has expanded: today diclofenac is widely
used in traumatology, surgery, neurology, gynecology,
urology, sports medicine, oncology and ophthalmology.

Фармгруппа: НПВП.

Composition, physico-chemical properties, price

Diclofenac is available in 6 dosage forms: tablets for
oral administration, rectal suppositories, external ointment and gel,
solution for i / m administration and eye drops.

Main substance Вспомогательные вещества Physicochemical properties. Packaging. Price.
Solution Sodium Diclofenac – 25 mg in 1 ml of p-ra or 75 mg per 1
ampoule
sodium metabisulphite, benzyl alcohol, mannitol,
propylene glycol, water for injection, sodium hydroxide.
Transparent, colorless or light yellow solution with smell
benzyl alcohol. On 3 ml in ampoules and on 5 ampoules in planimetric
packaged. № 5: 35-45 rubles.
Pills 25, 50 и 100 мг  Diclofenac sodium 25, 50 and 100 mg per 1 tablet  milk sugar, sucrose, potato starch, povidone,
stearic acid.
 Pills белого цвета, покрытые кишечнорастворимой
shell. По 10 или 20 таблеток в ячейковых контурных packaged.
On 30 tablets in banks from polymer or dark glass. №20 100 each
mg: 33-35 rubles; № 20 50 mg: 15-20 rubles.
Candles 50 или 100 мг  Diclofenac sodium 50 mg or 100 mg per 1 suppository  semisynthetic glycerides, cetyl alcohol.  White or white-yellow suppositories that have
cylindrical shape. № 10 100 mg: 40-80 rubles.
Ointment 1 %  Sodium diclofenac – 0.3 g per 30 g ointment  polyethylene oxide – 1500, dimexide, polyethylene oxide – 400,
1,2-propylene glycol.
 Ointment белого цвета, имеющая специфический запах. 30 gr
ointment in an aluminum tube. 50-60 rubles
Gel 1 и 5 %  Sodium diclofenac 10 or 50 mg per 1 g of gel.  propylene glycol, rectified ethanol, carbopol, 
нипагин,  троламин, лавандовое масло, вода очищенная
 White or slightly yellow gel with a specific
the smell. 30 gr геля в алюминиевой тубе 1% -35- 90 руб; 5% – 40
rub.
 Drops 0,1 %  Diclofenac sodium 1 mg per 1 ml of drops  касторовое масло полиthisксилированное, динатрия эдетат
дигидрат,  трометамол, маннитол, хлористоводородная кислота
(1M solution), benzalkonium chloride, purified water.
 Transparent or almost transparent solution, light yellow
or colorless. On 5 ml in a special bottle dropper. 5 or
6 candles in the contour packaging. 25-60 rub.

pharmachologic effect

For the drug is characterized by pronounced anesthetic,
anti-inflammatory and antipyretic effect. In the focus of inflammation
indiscriminately inhibits cyclooxygenase 1 and 2, reduces the level
prostaglandins and disrupts the synthesis of arachidonic acid.

In the treatment of rheumatic diseases therapeutic effects
Diclofenac contribute to a significant reduction in pain,
stiffness, characteristic of the morning time, swelling
joints, which can significantly improve their functional
state.

Use of the drug after injury or in the postoperative period
allows to reduce inflammatory swelling and pain discomfort.

Pharmacokinetics

When i / m administration maximum plasma concentration
reached in 15-30 minutes (75 mg dose). After 3 hours
plasma concentration of the drug is 10% of the maximum.
Associated with plasma proteins by 99%.

With internal treatment, rapid and complete absorption occurs,
however, food slows down absorption by 1–4 h.

When applied topically, it is partially absorbed through the skin.
integument, bioavailability reaches 6%. When receiving local therapy
for the treatment of joints in synovial fluid there is a large
концентрация препарата, нежели в плазме blood.

In conjunctiva and cornea reaches maximum concentration
30 minutes after instillation, falls into the anterior chamber of the eye.
With treatment in therapeutic doses almost does not fall into
systemic blood flow.

About 65% of the administered drug in the form of metabolites is excreted.
kidneys, 1% is excreted unchanged, the rest
excreted in the bile also in the form of metabolites.

The instructions for use of diclofenac indicated that it penetrates
в грудное молоко – this следует учитывать при назначении
treatment.

Indications

Solution

Diclofenac shots are used for short-term pain therapy.
various etiology of moderate intensity:

  • sciatica, lumbago, neuralgia;
  • diseases of the musculoskeletal system: rheumatic lesions
    soft tissue, rheumatoid and psoriatic arthritis, chronic
    juvenile arthritis, gouty arthritis, spondylitis
    ankylosing, osteoarthritis of the joints and spine;
  • algomenorrhea;
  • pelvic inflammatory diseases, incl. adnexitis;
  • post-traumatic pain syndrome with inflammatory
    phenomena;
  • postoperative pain syndrome.

Diclofenac Candles and Tablets

Used for symptomatic treatment, namely – to reduce
pain and severity of inflammation especially at the time
application, does not affect the progression
diseases.

  • pathologies of the musculoskeletal system inflammatory and
    degenerative, including psoriatic, rheumatoid,
    juvenile chronic arthritis, ankylosing spondylitis, arthritis
    gouty, osteoarthritis, tendovaginitis, bursitis;
  • pain syndrome, including migraine, cancer,
    ischialgia, ossalgia, lumbago, toothache, arthralgia, neuralgia,
    myalgia, radiculitis, biliary and renal colic, pain syndrome
    postoperative and post-traumatic;
  • algomenorrhea;
  • pelvic inflammatory disease, including adnexitis;
  • infectious and inflammatory pathologies of upper respiratory tract, occurring with
    pain syndrome, such as otitis media, pharyngitis, tonsillitis.

Additionally for candles: fever that accompanies ARVI and
flu.

Gel, ointment diclofenac

  • degenerative and inflammatory diseases of the musculoskeletal system
    the apparatus described above;
  • rheumatic and non-rheumatic muscle pains;
  • post-traumatic inflammatory processes of the locomotor system
    apparatus and soft tissues: dislocations of joints, bruises, damages
    bundles.

Drops

  • inhibition of miosis when operating cataracts;
  • inflammation after organ surgery
    view;
  • treatment and prevention of cystic edema of the yellow spot
    retina after cataract surgery;
  • noninfectious inflammatory processes: keratoconjunctivitis,
    conjunctivitis, corneal erosion, corneal inflammation and conjunctiva
    after injuries and others;
  • photophobia arising after keratotomy.

Contraindications

All Diclofenac dosage forms are not prescribed if available.
intolerance main or auxiliary in-in, as well as
the presence of hypersensitivity to other NSAIDs.

Diclofenac solution is contraindicated in the following
states

  • применение диклофенакexacerbation of gastrointestinal lesions
    (erosive and ulcerative);
  • bleeding from the digestive tract;
  • disorders of blood formation;
  • �”Aspirin Triad” – intolerance to NSAIDs
    patients with asthma and nasal polyps;
  • changes in hemostasis, including hemophilia;
  • children up to 18 years;
  • lactation;
  • pregnancy.

С осторожностью назначается при следующих states:
bronchial asthma, anemia, congestive heart failure,
edematous syndrome, arterial hypertension, hepatic or renal
insufficiency, inflammatory bowel disease, alcoholism,
erosive and ulcerative diseases of the gastrointestinal tract chronic (without exacerbation),
diabetes, diverticulitis, induced porphyria, condition after
serious surgical interventions, advanced age, systemic
connective tissue pathology.

Contraindications к применению таблеток

All indicated contraindications for solution plus
additionally:

  • inflammatory bowel disease;
  • severe kidney or liver failure;
  • condition after coronary artery bypass surgery;
  • 3 trimester of pregnancy;
  • children’s age up to 6 years for tablets 25 mg, other dosages –
    contraindicated to 18 years;
  • lactose intolerance, lactase deficiency, pathology
    suction glucose-galactose.

Contraindications к применению свечей диклофенака

All indicated contraindications for solution plus
additionally:

  • hemorrhoids, proctitis in the acute stage;
  • children under 16 years old.

Additional contraindications to the use of ointment, gel

  • violation of the integrity of the skin at the site of application of the gel;
  • history of asthma attacks on the background
    use of salicylates and NSAIDs;
  • 3 trimester of pregnancy;
  • lactation;
  • children up to 6 years;

With caution used for bleeding disorders
blood.

Contraindications к применению офтальмологических капель

  • children’s age up to 2 years;
  • 3 триместр беременности, lactation;

With care: bleeding disorders, herpetic
history of keratitis, “aspirin” asthma, gastrointestinal diseases in the stage
aggravations, elderly patients.

Dosage

Solution

Intramuscular deep introduction. Single dose for patients
is 75 mg, which corresponds to 1 ampoule of solution. Repeat
the introduction is permissible no earlier than after 12 hours. Duration
применения —  2 дня. Further, if necessary, continue
treatments are transferred to rectal or oral administration
drug.

Pills

Take half an hour before a meal, if you need fast
therapeutic effect. In other cases, tablets take
after or during the meal without chewing and drinking water.

Adult patients and adolescents: 25-50 mg twice or thrice a day
(max 150 mg daily). With the onset of a therapeutic effect
dosage is reduced to 50 mg per day.

In the case of juvenile rheumatoid arthritis, the daily dose
Diminishes to 3 mg / kg body weight.

At children’s age it is necessary to adhere to the following doses:

  • 6-7 years: 25 mg 1 time per day;
  • 8-11 years: 25 mg 2-3 times a day;
  • 12-14 years: 25-50 mg 3-4 times a day.

Candles

Designed for rectal administration as deep as possible after
defecation: 50 mg twice a day or 100 mg once a day.
days The maximum dose for daily use is 150 mg.
Duration лечения определяется индивидуально.

For migraine: 100-150 mg for the first attacks.

Suppositories are administered whole, without cutting into pieces, because this
may lead to impaired absorption.

Gel

Put outwardly, with clean hands, gently distributing
painful area. Gel 1% — по 2-4 гр на однократное применение,
gel 5% – up to 2 grams.

Adults and children over 12 years old are applied the drug thrice-four times.
per day.

For children 6-12 years old, 1% gel is applied to the skin at a dose of up to 2 grams, not more than 2
once a day, gel 5% – up to 1 g for a single use maximum 2
раза per day.

Duration лечения определяется индивидуально.

Ointment

Apply externally, 2-4 grams, in a thin layer. The multiplicity is
трижды-четырежды в days

Drops

Before surgery, instilled in the conjunctival sac, 1
drop five times over 3 hours. After surgery in the early period
– 1 drop three times, then – 1 drop three times-five times
day.

For other diseases: 1 drop four to five times
day.

Treatment course, no more than 28 days.

Side effects

Systemic reactions Generally characteristic of the solution and
Diclofenac tablets, less often for suppositories and even less often for ointments,
drops and gel.

Digestive system: in more than 1% of patients – abdominal pain,
bloating, diarrhea, indigestion, constipation, flatulence, nausea,
peptic ulcers. Less often – jaundice, blood in the feces, vomiting, defeat
esophagus, dry mouth, hepatitis, liver necrosis, cirrhosis,
pancreatitis, colitis.

CNS: headache, dizziness. Less often – sleep disorders,
depression, drowsiness, aseptic meningitis, convulsions, nightmarish
dreams, anxiety.

Sense organs: tinnitus. Less – diplopia, blurred vision,
taste impairment, hearing loss.

Skin: rash, itching. Less common: eczema, alopecia, toxic dermatitis,
urticaria, erythema multiforme, hemorrhage
punctate, increased photosensitivity.

Genitourinary system: fluid retention. Less commonly, proteinuria,
oliguria, hematuria, interstitial nephritis, acute renal failure.

Blood system: anemia, leukopenia, eosinophilia,
thrombocytopenic purpura, thrombocytopenia, agranulocytosis.

Respiratory: bronchospasm, cough, laryngeal edema,
pneumonitis.

CAS: increased blood pressure, congestive heart failure,
extrasystole, chest pain, heart attack.

Allergic reactions: anaphylactoid reactions, lip swelling and
language, vasculitis.

Local reactions

When v / m introduction: infiltration, burning, aseptic necrosis,
necrosis of adipose tissue.

The use of suppositories: mucous rectal secretions with
blood admixture, local irritation, painful bowel movements,
allergic local reactions.

Treatment with drops can cause burning eyes, turbidity.
corneas, blurred vision, iritis.

Therapy with ointment or gel – allergic skin reactions.

Overdose

Possible in the treatment of pills, solution, candles:
dizziness, vomiting, clouding of consciousness, headache, shortness of breath.
Children are characterized by nausea, abdominal pain, myoclonic
convulsions, bleeding, vomiting, liver and kidney dysfunction.

Drug Interactions (for systemic drug
forms)

  • Increases the plasma concentration of methotrexate, digoxin,
    lithium and cyclosporine drugs.
  • Reduces the effectiveness of drugs from the group of diuretics, enhancing
    risk of hyperkalemia.
  • Increases the risk of bleeding, especially from the gastrointestinal tract when
    simultaneous treatment with thrombolytics.
  • Reduces the effectiveness of hypnotics, hypotensive and
    hypoglycemic agents.
  • Increases the risk of side effects of other NSAIDs.
  • Enhances the effect of drugs that cause
    photosensitization.
  • Paracetamol boosts nephrotoxic side effects.
    diclofenac
  • Aspirin reduces the plasma concentration of diclofenac in
    blood.
  • Cefamendol, cefotetan, cefoperazone, plicamycin and valproic
    acid increase the frequency of hypoprothrombinemia.
  • Cyclosporine and medicines containing gold increase
    нефрооксичность diclofenac
  • Colzicin, ethanol, corticotropin and Hypericum preparations
    increase the risk of bleeding from the digestive tract.
  • Drugs that block tubular secretion, increase
    токсичность diclofenac

Is it possible to diclofenac with the constant treatment of any other
drug, I must say the attending physician with all the available
risks.

Diclofenac – the opinion of doctors

Most medical practitioners describe diclofenac as
effective and fast-acting drug. Meanwhile
cardiovascular risk is higher in diclofenac than in its other
�”Relatives” from the group of NSAIDs.

The shorter the course of treatment, the less likely the development
negative side effects. Extremely important to comply
recommended dosage, take into account contraindications and do not resort
to self-treatment without prescription.

Analogs

Voltaren, Ortofen, Naklofen, Diklak, Diklovit, Diklogen,
Dikloberl.

Автор: врач-гигиенист, эпидемиолог

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