Pharmacy No. 84. Delivery of medicines to your home and office.

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What is special about Lidocaine?

Lidocaine injections act directly on the central nervous system, suppressing its conductivity. This happens because the components of the drug block sodium channels, which are located in nerve endings and fibers. After administering the solution, the drug begins to immediately act on the nerve endings. Effect up to 75 min.

Its properties are much superior to Procaine, to increase the duration of the anesthetic properties, it is used together with epinephrine.

The drug protects the body from arrhythmia. Its effect does not cause irritation on the skin and dilates blood vessels. In this case, calcium easily moves through the membranes, and the concentration of the solution reaches its maximum within 5 - 15 minutes after the antiseptic has been injected into the muscle.

Anesthetic composition

The active substance is lidocaine hydrochloride monohydrate. Its formula is supplemented with sodium chloride, and caustic soda acts as an auxiliary component. All these components are dissolved in water. Consequently, the solution itself does not have a characteristic odor and is colorless.

What is Lidocaine used for?

The drug is administered both intramuscularly and intravenously. But it can also be used as a dropper. This achieves maximum effect after 10 – 20 minutes.

The active substance of the drug, after the injection, begins to affect the membranes of neurons. This allows the movement of sodium ions to be blocked by the membrane. In this case, all exciting processes are inhibited. But complications may arise with calcium ions.

If an alkaline or slightly alkaline environment occurs, all components of the drug may dissolve. Lidocaine has two functions. It dilates blood vessels and reduces the pain threshold. Provided that the solution is administered via injection, it is quickly absorbed and the anesthetic begins to act immediately.

The active substance (Lidocaine hydrochloride) accumulates in the liver after the effect of the medicine ends. Then it is excreted naturally along with urine or bile. This process takes about 10 hours.

Storage

The storage temperature of the drug is from 8 to 25 ° C. In this case, all ampoules must be in the packaging. If any capsule is opened or the seal is broken, the solution is not suitable for injection. Always check the expiration date at the pharmacy. Usually it is 3 years from the date of issue. It is strictly prohibited to use expired goods.

Lidocaine in ampoules is an anesthetic that has been proven over the years. The only disadvantage of this drug is that it still remains toxic. But, nevertheless, many private clinics, dental offices and plastic surgeons order it for local anesthesia.

How to inject lidocaine

The instructions for Lidocaine injections state that Lidocaine is used as an anesthetic before any surgery. The dosage of the drug depends on the type of procedure. It is prescribed exclusively by a doctor with a medical education.

Shallow anesthesia. This procedure is done if it is necessary to treat the nasopharynx, oral cavity, gastrointestinal tract or rectum. Usually a solution (2%) is taken. The volume of the drug is calculated according to the following scheme (2 mg per 1 kg of weight). The effect of the injection lasts from 15 to 30 minutes. The maximum dose should not exceed 20 ml. solution.

Different types of anesthesia require different dosages:

for conduction anesthesia, take a 2% solution of Lidocaine in a volume of 5 - 10 ml, but in order to immobilize the fingers of the limbs, it is better to use 2 - 3 ml. solution;
to perform epidural anesthesia, take 10–20 mg. drug;
For spinal anesthesia, 3–4 ml is enough. anesthetic.

To prolong the effect of the drug, you need to add 0.1% adrenaline.

Intravenous route of drug administration. It is used very rarely. Typically, the solution is administered intravenously only when antiarrhythmic therapy is needed. First you need to dilute 25 ml. drug in 100 ml. saline solution to obtain an anesthetic concentration of 20 mg/ml. Only in this form can it be administered intravenously.

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The drug must be administered according to a specific schedule. The initial dose is 1 mg/kg. The drug must be administered at a certain speed. Typically this figure ranges from 25 to 50 mg/min. For example, if a patient weighs 95 kg, his dose of lidocaine should be 95 mg (or 0.095 g). And it will have to be administered in 1.9 minutes. (116 sec.).

But here we must take into account the maximum dosage. No more than 300 mg of the drug can be administered in 1 hour, and this figure should not exceed 2000 mg per day. If a patient is administered an anesthetic of 2–10%, it is necessary to simultaneously monitor his electrocardiogram. It is also strictly forbidden to apply disinfectants at the injection site.

Indications of the drug

The drug can be used only as prescribed by a doctor. Self-use may adversely affect your health. Lidocaine is widely used in medicine. It is used to administer various methods of anesthesia.

Infiltration. It is commonly used to “freeze” certain tissues. This approach is mainly used in dentistry.
Terminal. Pain receptors are temporarily blocked. The effect is short-lived.
Conductor. Used during operations. Nerve impulses are blocked in a certain area.
Spinal. It is used if it is necessary to reduce the pain threshold in the spinal center. To do this, an injection is made into the subarachnoid space. In this case, the roots of the spinal center are blocked.
Epidural. In this case, it is necessary to give an injection into the epidural space.

The drug is indicated for the following types of pathologies:

when the patient begins to develop ventricular arrhythmia, the causative agent of which is considered to be glycoside intoxication;
for patients who suffer from coronary syndrome for preventive purposes;

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It is widely used in dentistry:

for removing baby teeth in preschool children;
when it is necessary to remove bones or apply sutures to wounds in the oral cavity;
if there is a need to perform an autopsy during sudden abscesses;
when installing a prosthesis or crown on the gum, to relieve pain in the gum itself;
to destroy the papilla on the tongue;
if there is a need to open a cyst in the salivary glands;
in children, when a frenulectomy is needed.

Doctors treating ENT diseases use lidocaine injections in the following cases:

when it is necessary to perform surgery to remove nasal polyps;
for the treatment of deviated nasal septum;
during electrocoagulation;
before performing an operation to open a peritonsillar abscess;
to administer anesthesia before performing a puncture of the maxillary sinuses;
analgesic effect before rinsing the nasopharynx;
before removing the tonsils (tonsillectomy);
before removing the adenoids (adenoidectomy).

Not only before surgery, injections of the drug are used. He is appointed:

when you need to numb the nasopharynx or mouth before inserting a probe;
before examining the rectum with a probe;
if there is a need to replace catheters.

This is only a small part of the procedures where the drug is used. Gynecology, ophthalmology, obstetrics, plastic surgery - its functions as an anesthetic are currently used in all areas of medicine.

Contraindications

The anesthetic has contraindications:

in the presence of atrioventricular block (in this case, the conduction of the drug is impaired);
diseases associated with the work of the heart (heart failure, decreased heart rate, low blood pressure);
porphyria, or as it is also called “scientific vampirism”;
the presence of neuromuscular malaise (myasthenia gravis) (striated and transverse muscles get tired very quickly);
problems with the liver and kidneys, which impairs the excretion of lidocaine hydrochloride;
allergic reactions to any of the components of the drug;

Allergies can cause anaphylactic shock. This is very dangerous as it can be fatal.

breastfeeding and any trimester of pregnancy;
low blood volume circulation rates.

Not only Lidocaine - drugs of similar action are strictly contraindicated for the patient.

Cefamed 0.5 g, solution 2 ml 1% lidocaine solution No. 1 por.d/sol.d/in.vial.

Instructions for use of the drug Cefamed Trade name Cefamed International nonproprietary name Ceftriaxone Dosage form Powder for solution for injection, 0.5 g or 1.0 g complete with solvent (lidocaine hydrochloride, 1% solution for injection 2.0 ml, 3.5 ml) Composition One bottle contains the active substance - ceftriaxone (in the form of ceftriaxone sodium) 500 mg or 1000 mg, solvent composition 1 ampoule of solvent contains the active substance - lidocaine hydrochloride 20 mg or 35 mg, excipients: sodium hydroxide or hydrochloric acid, water for injection Description White crystalline powder or yellowish in color, slightly hygroscopic. Solvent: colorless, transparent liquid. Pharmacotherapeutic group Antibacterial drugs for systemic use. Other beta-lactam antibacterial drugs. Third generation cephalosporins. Ceftriaxone. ATC code J01DD04 Pharmacological properties Pharmacokinetics When administered intramuscularly/intravenously, ceftriaxone penetrates well into tissues and body fluids. Bioavailability when administered intramuscularly is 100%. The maximum concentration in blood plasma after intramuscular administration is achieved after 2-3 hours. Reversibly binds to plasma albumin by 85-95% and this binding is inversely proportional to its concentration in the blood. Ceftriaxone quickly diffuses into the interstitial fluid, where it retains its bactericidal effect against microorganisms sensitive to it for 24 hours. Ceftriaxone penetrates well through the blood-brain barrier. The half-life in adults is about 8 hours, in elderly people over 75 years of age it is approximately 2-3 times longer, and in newborns it is 2-3 times longer than in young adults. In adults, 50-60% of ceftriaxone is excreted unchanged in the urine, 40-50% in the bile. In newborns, approximately 70% of the administered dose of ceftriaxone is excreted by the kidneys. In case of impaired renal or hepatic function in adults, the pharmacokinetics of ceftriaxone remains almost unchanged (possibly a slight prolongation of the half-life) due to the redistribution of functions: if renal function is impaired, biliary excretion increases, and if liver pathology occurs, renal excretion increases. Pharmacodynamics Cefamed is a broad-spectrum antibiotic of the third generation cephalosporin series. It has a bactericidal effect by inhibiting the synthesis of bacterial cell membranes. Active against most gram-negative, many gram-positive pathogens and some anaerobes. Resistant to the action of beta-lactamases produced by bacteria. Aerobic gram-negative bacteria sensitive to Cefamed: Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are resistant), E.coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (including Kl. pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are resistant), Salmonella spp. (including S. typhi), Serratia spp. (including S. marcescens), Shigella spp., Vibrio spp. (including V. cholerae), Yersinia spp. (including Y. enterocolitica). Many strains of the above microorganisms, which multiply steadily in the presence of other antibiotics, for example, penicillins, first and second generation cephalosporins and aminoglycosides, are sensitive to Cefamed. According to clinical data, good effectiveness of the drug is noted for primary and secondary syphilis. Aerobic gram-positive bacteria sensitive to Cefamed: Streptococcus agalactiae, Staphylococcus aureus (including penicillinase-producing strains), Streptococcus bovis, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans. Staphylococcus spp., resistant to methicillin, is also resistant to cephalosporins, including Cefamed. Most strains of Enterococcus spp. (for example, Streptococcus faecalis) are also resistant to the drug. Anaerobic pathogens: Bacteroides spp. (including some strains of B. fragilis), Clostridium spp. (including Cl. difficile), Fusobacterium spp. (except F. mortiferum and F. varium), Peptococcus spp., Peptostreptococcus spp. Some strains of Bacteroides spp. (for example, B. fragilis) that produce beta-lactamase are resistant to Cefamed. Indications for use Cefamed is effective for diseases caused by strains of bacteria that are sensitive to it: - diseases of the upper and lower respiratory tract (including pneumonia, lung abscess, pleural empyema) - infections of the abdominal organs (including cholangitis, gallbladder empyema ) -inflammatory diseases of the gastrointestinal tract, biliary tract, peritonitis -infections of bones and joints -infections of the skin and soft tissues -urinary tract infections (including pyelonephritis) -sexually transmitted infections (including gonorrhea) -infected wounds and burns - inflammation of the meningeal membranes, sepsis - for the prevention of postoperative infectious complications. Method of administration and dosage Cefamed is administered intramuscularly and intravenously by stream or drip. Usual doses for adults and children aged 12 years and older are 1-2 g of Cefamed once daily. The interval between administrations is 24 hours. In severe cases or for infections caused by moderately sensitive bacteria, the daily dose of the drug can be increased to 4 g. For newborns (up to two weeks of age), Cefamed is prescribed at a dose of 20-50 mg/kg body weight once a day. Exceeding the dose is unacceptable due to the immaturity of the enzyme system in newborns. Ceftriaxone is contraindicated in neonates (≤8 days) who are already receiving or are expected to receive intravenous calcium-containing solutions, including continuous potassium-containing infusions, due to the formation of calcium salt precipitates. For infants and children under 12 years of age, the daily dose of Cefamed is 20-80 mg/kg body weight once a day. In children weighing over 50 kg or more, the usual doses for adults are used. Intravenous administration of the drug at a dose of more than 50 mg/kg body weight should be carried out by drip for at least 30 minutes. The duration of treatment depends on the nature and severity of the disease. It is recommended to continue administration of Cefamed for at least 3 days after body temperature normalizes. For bacterial meningitis in newborns and children, the drug is prescribed at an initial dose of 100 mg/kg body weight once a day. The maximum daily dose is 4 g. After identifying the pathogen, the dose can be reduced. When treating gonococcal infection (without complications), the recommended dose is 250 mg of Cefamed once intramuscularly. When treating gonorrhea (patients should be treated in a hospital setting). Treatment tactics depend on the nature of the clinical course of gonorrhea. Thus, in case of abscess formation of the paraurethral and large vestibular glands, along with antimicrobial drugs effective against N. gonorrhoeae, it is necessary to use appropriate pathogenetic, physiotherapeutic and surgical treatment methods. Etiological treatment of complicated gonococcal infection of the urinary system and pelvic organs: Cefamed -1.0 g intramuscularly every 24 hours. In patients with impaired renal function, provided that the liver function is normal, and in patients with impaired liver function, provided that renal function is preserved, there is no need to reduce the dose of the drug. In case of severe renal failure (creatinine clearance less than 10 ml/min), Cefamed should not exceed 2 g per day. With simultaneous impairment of liver and kidney function, as well as in patients on hemodialysis, it is necessary to regularly monitor the concentration of ceftriaxone in the blood serum. To prevent postoperative infections, a single injection of 1-2 g of Cefamed is recommended 30-90 minutes before surgery. Rules for preparation and administration of the drug For intramuscular administration, 500 mg or 1 g of powder is diluted in 2 or 3.5 ml of a 1% lidocaine solution, respectively, and injected deep into the gluteal muscle. Lidocaine is not used as a solvent in pediatric practice. For intravenous administration, the contents of one bottle of Cefamed 500 mg or 1 g are diluted in 5 or 10 ml of sterile distilled water, respectively, and injected slowly into a vein over 2-4 minutes. For intravenous infusion, 2 g of the drug is diluted in 40 ml of 0.9% sodium chloride solution, 5% glucose solution, 10% glucose solution, 5% fructose solution, 6% dextran solution. The duration of the intravenous infusion should be at least 30 minutes. The drug solution must be used immediately after its preparation! Side effects Possible: exanthema, allergic dermatitis, swelling, itching, urticaria, anaphylactic shock, erythema multiforme - diarrhea, nausea, vomiting, stomatitis, glossitis - eosinophilia, leukopenia, granulocytopenia, hemolytic anemia, agranulocytosis, thrombocytopenia - fever, chills Rarely: - headache, dizziness, - increased activity of liver transaminases, oliguria, increased serum creatinine In isolated cases: - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal syndrome (Lyell's syndrome) - pseudomembranous colitis - blood clotting disorder, with intravenous administration pain along the vein, phlebitis - arrhythmias (with rapid administration) - bleeding - dysbacteriosis, candidiasis - precipitation of ceftriaxone calcium salts in the gallbladder. Contraindications - hypersensitivity to cephalosporins and penicillins - hypersensitivity to the solvent - lidocaine (the solvent can be replaced with novocaine or water for injection) - first trimester of pregnancy - hyperbilirubinemia in newborns and premature infants - renal/liver failure - ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs - a history of bleeding - neonates (≤28 days) who are already prescribed or are expected to receive intravenous treatment with calcium-containing solutions, including continuous calcium-containing infusions, for example, with parenteral nutrition, due to the risk of the formation of precipitates of ceftriaxone calcium salts. interactions When used simultaneously with loop diuretics (for example, furosemide), renal dysfunction is not observed. Cefamed and aminoglycosides have synergism against many gram-negative bacteria. This combination is justified in the treatment of severe and life-threatening infections (for example, caused by a pathogen such as Pseudomonas aeroginosa). Cefamed should not be mixed in the same bottle or syringe with other antibiotics. Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. In vitro antagonism was found between chloramphenicol and ceftriaxone. Ceftriaxone is pharmaceutically incompatible with amsacrine, vancomycin, fluconazole and aminoglycosides. Special instructions When treating with Cefamed, the possibility of developing anaphylactic reactions must be taken into account; prescribe with caution if there is a history of allergic reactions to penicillin. During long-term treatment with the drug, regular monitoring of the peripheral blood picture is necessary. After the use of ceftriaxone, usually in doses exceeding the standard recommended, ultrasound examination of the gallbladder revealed shadows that were mistaken for stones. They are precipitates of the calcium salt of ceftriaxone, which disappear after completion or cessation of ceftriaxone therapy. Such changes rarely give any symptoms, but even in such cases only conservative treatment is recommended. If these phenomena are accompanied by clinical symptoms, then the decision to discontinue the drug is left to the discretion of the attending physician. Cases of pancreatitis are possible. Interaction with calcium ions Isolated fatal cases of the formation of precipitates in the lungs and kidneys have been described based on the results of autopsy studies in newborns receiving ceftriaxone and calcium-containing solutions. In some cases, a single venous access was used, and the formation of precipitates was observed directly in the intravenous system. At least one case of death has also been described using different venous approaches and at different times of administration of ceftriaxone and calcium-containing solutions. However, according to the results of the autopsy study, no precipitates were found in this newborn. Similar cases were observed only in newborns. Sporadic cases of agranulocytosis (<500/ml) have been reported, most of them observed after 10 days of treatment and against the background of total doses of more than 20 g. Sporadic cases of serious reactions have been reported (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis ( Lyell's syndrome)). Very rare cases of pseudomembranous colitis (<0.01%) and bleeding disorders, as well as the formation of kidney stones, have been described, mainly in children over 3 years of age who received either large daily doses of the drug (more than 80 mg/kg per day) or cumulative doses of more than 10 g, as well as those who had additional risk factors (limited fluid intake, bed rest, etc.). The formation of kidney stones can be asymptomatic or clinically manifest and can lead to renal failure. Use in pediatrics The drug should be prescribed with caution to newborns, especially premature infants, due to the high risk of developing hyperbilirubinemia. Pregnancy and lactation Safety of use during pregnancy has not been established. The use of Cefamed during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus (ceftriaxone crosses the placental barrier). If it is necessary to use the drug Cefamed during lactation, the issue of stopping breastfeeding should be decided (ceftriaxone is excreted in breast milk). Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms Considering the side effects of the drug, care must be taken when driving vehicles and working with mechanisms. Overdose Symptoms: increased side effects Treatment: symptomatic. Hemodialysis and peritoneal dialysis are not effective; there is no specific antidote. Release form and packaging 0.5 g and 1.0 g of the drug in a glass bottle, sealed with a rubber stopper and a crimped aluminum flip-off cap. 2.0 ml and 3.5 ml of solvent are packaged in glass ampoules. 1 bottle and 1 ampoule with solvent are placed in a blister pack. 1 contour package together with instructions for medical use in the state and Russian languages are placed in a cardboard box. Storage conditions Store at a temperature not exceeding 25°C. Keep out of the reach of children! Shelf life 3 years Do not use after expiration date Conditions for dispensing from pharmacies By prescription Manufacturer/packer E.I.P.I. Co., Egypt, Tenth of Ramadan City, First Industrial Area B1, PO Box 149 Tenth (“EIPICO.” Egypt, Tenth of Ramadan City, First Industrial Area B1, PO box: 149 Tenth) Owner of the registration certificate “WORLD MEDICINE” , Great Britain (“WORLD MEDICINE”, Great Britain) Address of the organization that accepts claims from consumers on the quality of products of the Republic of Kazakhstan on the territory of the Republic of Kazakhstan, Almaty, Turksib district, Suyunbay Ave., 222 b Tel/fax: 8(7272) 529090 www.worldmedicine .kz