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Novocaine, solution for injection 2.5 mg/ml and 5.0 mg/ml

Overdose symptoms

In low doses, novocaine acts as a stimulant of the central nervous system; in high doses it leads to depression of central nervous system functions. Intoxication with novocaine hydrochloride occurs in 2 phases:

1. Stimulation

— CNS: paresthesia of the eyelids, feeling of numbness of the tongue, anxiety, delirium, convulsions (tonic-clonic).

- Cardiovascular system: increased cardiac output, increased blood pressure, redness of the skin.

2. Depression

— CNS: coma, respiratory arrest.

— Cardiovascular system: absence of pulse, pale skin, cardiac arrest.

Patients in the first stage of intoxication with local anesthetics exhibit symptoms of agitation. They are restless and complain of dizziness, visual and hearing disturbances, tingling and paresthesia, especially in the area of the tongue and lips. Paresthesia of the tongue, chills, and muscle cramps are warning signs of impending generalized seizures. Plasma concentrations of novocaine that do not reach the threshold for initiating seizures also often lead to drowsiness and sedation of the patient. At the first stage of intoxication, tonic-clonic convulsions develop. With progressive intoxication of the central nervous system, brain stem dysfunction develops with respiratory depression and symptoms of coma, which can lead to death.

A drop in blood pressure is often the first sign of cardiovascular toxicity. Hypotension is mainly due to depression or blockade of cardiac conduction. However, cardiovascular toxicity is of relatively little clinical significance.

In the case of accidental general spinal anesthesia, intoxication is manifested by initial signs of anxiety, then drowsiness, which can progress to unconsciousness and respiratory arrest.

Treatment of overdose:

If symptoms of toxic effects of novocaine on the central nervous system or cardiovascular system appear, you must:

- immediate cessation of administration of novocaine;

— ensuring airway patency;

- if necessary, oxygen inhalation or artificial respiration;

— careful monitoring of blood pressure, pulse rate and pupil diameter;

- in case of an acute and threatening drop in blood pressure, the patient is transferred to the so-called. “anti-shock” position (lying horizontally, with the head positioned below the level of the legs), beta-adrenergic agents (adrenaline) are administered intravenously slowly. In addition, crystalloid solutions are administered to replenish volume;

- when the tone of the vagus nerve increases with the development of bradycardia, atropine is administered (0.5 mg to 1.0 mg intravenously);

- in case of suspected cardiac arrest, it is necessary to carry out appropriate resuscitation measures;

- if seizures develop, diazepam is administered (about 0.1 mg/kg intravenously).

Analeptics of central action are contraindicated in case of intoxication with local anesthetics!

Publications in the media

(Procainum) INN

Synonyms. Novocaine.

Composition and release form. Powder; 0.25% and 0.5% solutions of procaine hydrochloride in ampoules of 1, 2, 5, 10 and 20 ml and 1% and 2% solutions of 1, 2, 5 and 10 ml; 0.25% and 0.5% sterile solutions of procaine hydrochloride in bottles of 200 and 400 ml; 5% and 10% ointment; suppositories containing 0.1 g of procaine hydrochloride.

Indications. Infiltration, conduction, epidural, spinal anesthesia; local anesthesia in dentistry, otorhinolaryngology, surgery (tracheal intubation, bronchoesophagoscopy, removal of polyps, etc.); spasms of intestinal smooth muscles.

Pharmachologic effect. Procaine has less strong anesthetic activity compared to modern local anesthetics. However, due to its relatively low toxicity, large therapeutic breadth and additional valuable pharmacological properties allowing its use in various fields of medicine, it is still widely used. Procaine, when absorbed and directly introduced into the bloodstream, has a general effect on the body: it reduces the formation of acetylcholine and reduces the excitability of peripheral cholinoreactive systems, has a blocking effect on the autonomic ganglia, reduces spasms of smooth muscles, excitability of the myocardium and motor areas of the cerebral cortex. The drug blocks the occurrence and conduction of nerve impulses, reducing the permeability of neuronal membranes to sodium ions, which leads to stabilization of the membrane and inhibits depolarization. To reduce absorption and prolong the action, procaine solutions for local anesthesia are usually combined with a solution of adrenaline hydrochloride (0.1% solution).

Pharmacokinetics. The rate of absorption is affected by the site of administration and the rate of administration of the drug. Protein binding is very low. In the body, procaine is hydrolyzed relatively quickly, forming para-aminobenzoic acid and diethylaminoethanol. T 1/2 is from 30 to 50 seconds. It is excreted from the body in the form of metabolites, 2% - unchanged.

Side effects. Dizziness, hypotension, weakness, allergic reactions.

Contraindications. Hypersensitivity to procaine.

Adverse reactions when interacting with other drugs. Procaine reduces the therapeutic effect of sulfonamide drugs. When cholinesterase inhibitors are taken simultaneously with procaine, antagonism of these drugs is noted due to the fact that procaine reduces the formation of acetylcholine and, thus, reduces the excitability of peripheral cholinoreactive systems. When used together with procaine, drugs that depress the central nervous system (droperidol, haloperidol, phenothiazines), additional depression of the central nervous system may occur. When using disinfectant solutions containing heavy metals, procaine can release heavy metal ions from these solutions, which leads to severe local irritation, the development of edema and pastiness.

Information for the patient. When procaine is administered, signs of discomfort may appear, which requires consulting a doctor.

Novocaine

Dosage form

Rectal suppositories

Compound:

one suppository contains:

Active substance

: Procaine hydrochloride (Novocaine) – 0.1 g.

Excipients

: Solid fat (Vitepsol (brands N 15, W 35), Supposir (brands NA 15, NAS 50)) – until a suppository weighing 1.2 g is obtained.

Description

Suppositories are white or white with a yellowish tint, torpedo-shaped.

Pharmacotherapeutic group

Local anesthetic.

ATX code

: C05AD05.

pharmachologic effect

Pharmacodynamics

A local anesthetic with moderate anesthetic activity and a wide range of therapeutic effects. Being a weak base, it blocks sodium channels, preventing the generation of impulses at the endings of sensory nerves and the conduction of impulses along nerve fibers. Changes the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. Suppresses the conduction of not only pain, but also impulses of other modalities.

Pharmacokinetics

Subject to complete systemic absorption. It is quickly hydrolyzed by plasma and liver esterases to form 2 main pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator effect) and para-aminobenzoic acid (is a competitive antagonist of sulfonamide chemotherapeutic drugs and can weaken their antimicrobial effect).

Indications for use

As a local anesthetic for hemorrhoids and anal fissures.

Contraindications

Hypersensitivity (including to para-aminobenzoic acid and other local anesthetic esters), children's age (up to 18 years).

Carefully

Emergency operations accompanied by acute blood loss, conditions accompanied by decreased hepatic blood flow (for example, with chronic heart failure, liver disease), progression of cardiovascular failure (usually due to the development of heart block and shock), proctitis, pseudocholinesterase deficiency, renal failure, in elderly patients ( over 65 years old), seriously ill, debilitated patients, pregnancy, childbirth.

Use during pregnancy and breastfeeding

During pregnancy and lactation, the drug should be used when the benefit to the mother outweighs the risk to the fetus or child.

Directions for use and doses

Rectally. The suppository is inserted deep into the anus (after a cleansing enema or spontaneous bowel movement), having previously freed the suppository from the contour packaging using scissors (cutting the packaging along the contour of the suppository). Use 1 suppository 1-2 times a day. The duration of treatment as a local anesthetic is no more than 5 days. If pain persists, you should consult a doctor.

Features of the action of the drug when first taken or when discontinued

No information available.

Side effect

From the nervous system

: headache, dizziness, drowsiness, weakness, motor restlessness, loss of consciousness, convulsions, trismus, tremor, visual and auditory disturbances, nystagmus, cauda equina syndrome (leg paralysis, paresthesia), paralysis of the respiratory center.

From the side of the heart

: bradycardia, arrhythmias, chest pain.

From the side of blood vessels

: increase or decrease in blood pressure, peripheral vasodilation, collapse.

From the kidneys and urinary tract

: involuntary urination.

From the gastrointestinal tract

: nausea, vomiting, involuntary defecation. Blood disorders: methemoglobinemia.

Allergic reactions

: itching of the skin, skin rash, other anaphylactic reactions (including anaphylactic shock), urticaria (on the skin and mucous membranes), dizziness, weakness, decreased blood pressure. In these cases, you should stop using the drug and consult a doctor.

Local reactions

: in the first days of using the drug, there may be a urge to defecate and a feeling of discomfort, which later go away on their own and do not require discontinuation of the drug. Rarely – hyperemia and itching in the anal area (when used in high doses).

Overdose

Symptoms

: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, “cold sweat”, increased breathing, tachycardia, decreased blood pressure, up to collapse, apnea, methemoglobinemia. The effect on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, and motor agitation.

Treatment

: maintaining adequate ventilation of the lungs with oxygen inhalation, intravenous administration of short-acting drugs for general anesthesia, in severe cases - detoxification and symptomatic therapy.

Interactions with drugs

Local anesthetics enhance the inhibitory effect of other drugs on the central nervous system. Anticoagulants (ardeparin sodium, dalteparin sodium, danaparoid sodium, enoxaparin sodium, heparin, warfarin) increase the risk of bleeding.

When used with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline), it increases the risk of lowering blood pressure. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect. Procaine reduces the antimyasthenic effect of anticholinesterase drugs, especially when used in high doses, which requires additional correction of the treatment of myasthenia gravis.

Cholinesterase inhibitors (antimyasthenic drugs, cyclophosphamide, demecaria bromide, ecothiopathy iodide, thiotepa) reduce the metabolism of local anesthetic drugs. The metabolite of procaine (para-aminobenzoic acid) is an antagonist of sulfonamides, which leads to a weakening of the antimicrobial effect.

special instructions

Patients require monitoring of the functions of the cardiovascular system, respiratory system and central nervous system. It is necessary to discontinue MAO inhibitors at least 10 days before using the drug.

Impact on the ability to drive vehicles and machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form

Rectal suppositories 100 mg.

5 suppositories in a blister pack.

Two contour blister packs, together with instructions for medical use of the drug, are placed in a box of cardboard.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Best before date

2 years. Do not use after the expiration date stated on the label.

Vacation conditions

Available without a prescription.