LOKTAFEN [Diclofenac] 75 mg/3 ml Solution for IM injection
![LOKTAFEN [Diclofenac] 75 mg/3 ml Solution for IM injection](https://livemedicine.biz/image/cache/catalog/upload/Loktafen_inj-1350x1350.jpg "LOKTAFEN [Diclofenac] 75 mg/3 ml Solution for IM injection")
LOKTAFEN
instructions for the medical use of the medicinal
product
Tradename
Lokatafen,
Локтафен
International
non-proprietary name or generic name
Diclofenac, Диклофенак
Composition
Each ampoule (3 ml solution) contains:
Active substance: diclofenac sodium 75 mg.
Excipients: sodium
metabisulfite, mannitol, propylene glycol, benzyl alcohol, sodium hydroxide,
water for injection.
Dosage form
Injection.
Pharmacotherapeutic group
Non-steroidal anti-inflammatory drugs (NSAIDs).
Pharmacodynamics
NSAIDs, a derivative of phenylacetic
acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic
effect. The mechanism of action is associated with inhibition of the activity
of COX, the main enzyme of the metabolism of arachidonic acid, which is a
precursor of prostaglandins, which play an important role in the pathogenesis
of inflammation, pain and fever. The analgesic effect is due to two mechanisms:
peripheral (indirectly, through suppression of prostaglandin synthesis) and
central (due to inhibition of prostaglandin synthesis in the central and
peripheral nervous system).
In vitro, at concentrations equivalent
to those achieved in the treatment of patients, does not inhibit the biosynthesis
of proteoglycans in cartilage tissue.
In rheumatic diseases, it reduces joint
pain at rest and during movement, as well as morning stiffness and swelling of
the joints, and helps to increase the range of motion. Reduces post-traumatic
and postoperative pain and inflammatory edema.
In case of post-traumatic and
postoperative inflammatory events, it quickly relieves pain (arising both at
rest and during movement), reduces inflammatory edema and edema of a
postoperative wound.
Suppresses platelet aggregation. With
prolonged use, it has a desensitizing effect.
After intramuscular
administration, the maximum concentration of the drug in the blood plasma is
2.5 μg / ml (8 μmol / L), the time to reach the maximum concentration is 20 minutes.
Diclofenac sodium binds to blood plasma proteins by 95 -98%, and most of the
drug binds to albumin.
The drug penetrates well into
the synovial fluid, where the maximum concentration of the active substance is
reached for 2 - 4 hours. later than plasma. The half-life of the synovial fluid
is 3 to 6 hours.
The systemic clearance of
diclofenac sodium is 260 ml / min, 60% of the drug is excreted as metabolites
by the kidneys, less than 1% is excreted unchanged, the rest - with bile.
In patients with severe renal
dysfunction (creatinine clearance less than 10 ml / min), the specific gravity
of excretion of metabolites with bile increases, therefore, an increase in
their concentration in the blood is not observed.
Indications for use
Inflammatory and degenerative
diseases of the musculoskeletal system, incl. rheumatoid, juvenile, chronic
arthritis; ankylosing spondylitis and other spondyloarthropathies;
osteoarthritis; gouty arthritis; bursitis, tendovaginitis; spinal pain syndrome
(lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, sciatica); pain
syndrome with trauma, accompanied by inflammation; pain syndrome after surgery,
accompanied by inflammation; pain syndrome in gynecological diseases,
accompanied by inflammation; renal colic; biliary colic.
Hypersensitivity to
diclofenac and excipients of the drug used; attacks of asthma, urticaria, or
acute coryza; stimulated with acetylsalicylic acid, or other drugs, with
inhibitory activity of prostaglandin synthetase; erosive and ulcerative lesions
of the gastrointestinal tract (GIT) in the exacerbation phase; severe renal
failure (CC <30 ml / min), progressive kidney disease; severe liver failure,
active liver disease; clinically confirmed coronary artery disease, peripheral
arterial and cerebrovascular disease, uncontrolled arterial hypertension,
decompensated heart failure; pregnancy and breastfeeding; children and
adolescents up to 18 years old.
Method of administration and dosage
Injected intramuscularly by
deep injection into the gluteus muscle. Do not use the drug as an injection for
more than 2 consecutive days. If necessary, treatment can be continued in
tablets or rectal suppositories.
The dose is usually 75 mg
(contents of 1 ampoule) 1 time per day. In severe cases, as an exception, 2
injections of 75 mg can be carried out, with an interval of at least 12 hours
(the second injection should be carried out in the opposite gluteal region).
Alternatively, one injection of the drug per day (75 mg) can be combined with
other dosage forms of diclofenac (tablets, rectal suppositories), while the
total daily dose should not exceed 150 mg.
The maximum daily dose is 150
mg.
Special instructions and precautions
Use with extreme caution in case of liver, kidney, gastrointestinal
tract diseases in history, dyspeptic symptoms, bronchial asthma, arterial
hypertension, heart failure, immediately after major surgical interventions, as
well as in elderly patients.
If there is a history of allergic reactions to NSAIDs and sulfites, the
drug is used only in urgent cases.
In the course of treatment, systematic monitoring of the function of the
liver and kidneys, and the picture of peripheral blood is necessary.
The drug should not be mixed with solutions of other drugs for
injection.
Influence on the ability to drive
vehicles and mechanisms
Due to the possibility of adverse reactions from the
nervous system, caution should be exercised when driving vehicles and engaging
in other potentially hazardous activities that require increased concentration
of attention and speed of psychomotor reactions.
Application during pregnancy and during breastfeeding
Contraindicated for use during pregnancy
and during breastfeeding.
Interaction with other medicinal products
Diclofenac may increase the
toxic effect of cyclosporine on the kidneys.
With simultaneous use with
anticoagulants, regular monitoring of blood coagulation indicators is
necessary.
With simultaneous use with
digoxin, phenytoin or lithium preparations, an increase in plasma
concentrations of these drugs is possible; with diuretics and antihypertensive
drugs - it is possible to reduce the effect of these drugs; with
potassium-sparing diuretics - the development of hyperkalemia is possible; with
acetisalicylic acid - a decrease in the concentration of diclofenac in the
blood plasma and an increase in the risk of side effects.
When using methotrexate within
24 hours before or after taking Loktafen, an increase in the concentration of
methotrexate and an increase in its toxic effect is possible.
Loktafen can cause hypo- or
hyperglycemia, therefore, when used simultaneously with hypoglycemic agents,
control of the concentration of glucose in the blood is required.
Side effect
From the digestive system: nausea,
vomiting, epigastric pain, anorexia, flatulence, constipation, gastritis up to
erosive with bleeding, increased transaminase activity, drug hepatitis,
pancreatitis.
From the urinary system: interstitial
nephritis.
From the nervous system: headache,
dizziness, disorientation, agitation, insomnia, irritability, fatigue, aseptic
meningitis.
From the respiratory system: bronchospasm.
From the hematopoietic system:
anemia,
thrombocytopenia, leukopenia, agranulocytosis.
Dermatological reactions: exanthema,
erythema, eczema, hyperemia, erythroderma, photosensitization.
Allergic reactions: erythema
multiforme, Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic reactions,
including shock.
Local reactions: burning
sensation, infiltration, necrosis of adipose tissue are possible at the
injection site.
Others: fluid
retention in the body, edema, increased blood pressure.
If
any of the side effects indicated in the instructions are aggravated, or you
notice any other side effects not listed in the instructions, inform your
doctor.
Symptoms: bleeding from the gastrointestinal tract, diarrhea,
vomiting, epigastric pain, dizziness, tinnitus, convulsions, rarely - increased
blood pressure, acute renal failure, hepatotoxic effect, respiratory
depression, coma.
Treatment: gastric lavage, activated charcoal, symptomatic
therapy aimed at eliminating an increase in blood pressure, impaired renal
function, seizures, irritation of the gastrointestinal tract, respiratory
depression. Forced diuresis, hemodialysis are ineffective.
Store in a dry and
dark place at temperatures below 30°C.
Keep out of the reach
of children!
2 years. Do not use
after the expiration date printed on the package.
Dispensed by
prescription.
Release form
5 ampoules of 3 ml in a blister strip packaging. 1
package with instructions for use in a cardboard box.