Procaine - instructions for use, dose, side effects, contraindications

It disrupts generation and conduction of nerve impulses mainly in non-mielin fibers. Local anesthetic (weak base) in non-ionized form (blood pH 7.4) penetrates through the cell membrane into the axon and ionizes there.Ionized molecules of matter interact with specific sites of binding of sodium channels from the inside of the membrane and, blocking sodium channels, interfere with Na + entry into the cell and depolarize the membrane. As a result, the generation of the action potential and the propagation of impulses along the nerve fiber are violated. Local anesthetics have an affinity for the sodium channel, which is in the inactivated state (potential-dependent sodium channels have three states: rest - closed, activation - open and inactivated - closed). Thus, local anesthetics block the passage of these channels into an open state.

It displaces calcium from receptors located on the inner surface of the membrane. Changes the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. Antiarrhythmic action is associated with an increase in the effective refractory period, a decrease in excitability and automatism of the myocardium.

When absorbed or directly injected into the blood reduces the formation of acetylcholine and the excitability of cholinergic systems, has a ganglion-blocking effect, reduces spasm of smooth muscles, inhibits the excitability of the myocardium and motor cortical areas of the brain.Has analgesic and antishock activity, antihypertensive and antiarrhythmic action. Eliminates the descending inhibitory effects of the reticular formation of the brain stem. Oppresses polysynaptic reflexes. In large doses can cause seizures.

Pharmacokinetics:

Poorly absorbed through mucous membranes. If parenteral administration is well absorbed, it is rapidly hydrolyzed in the bloodstream by the action of esterases and blood plasma cholinesterases to para-aminobenzoic acid and diethylaminoethanol. The elimination half-life is 0.7 minutes, 80% of the drug is excreted in the urine.

Has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h). To reduce the systemic effect, toxicity and prolongation of the effect is used in combination with vasoconstrictors (adrenaline). With increasing concentration of solutions, the total dose should be reduced. For the prevention of hypersensitivity reactions therapy begins with the administration of 2 ml of 2% solution after 3 days (in the absence of side effects) - 3 ml, and then proceeds to the introduction of a full dose of - 5 ml per injection.

Indications:

Infiltration, conductive, epidural and spinal anesthesia, intraosseous anesthesia, anesthesia of mucous membranes (in ENT practice); vagosympathetic and paranephalic blockade. Circular and paravertebral blockade in eczema, neurodermatitis, ishalgia.

Intravenously: to potentiate the action of fixed assets for anesthesia; for relief of pain syndrome of different genesis.

Intramuscularly: for the dissolution of penicillin in order to prolong its duration; as an adjuvant for some diseases more common in the elderly, including endarteritis, atherosclerosis, arterial hypertension, spasms of coronary vessels and cerebral vessels, joints of rheumatic and infectious genesis.

Rectal: hemorrhoids, spasms of smooth muscles of the intestine, anal fissures.

ICD-10

IX.I80-I89.I84 Hemorrhoids

XI.K55-K63.K60 Fissure and fistula of the anus and rectum area

XIII.M50-M54.M54.4 Lumbago with sciatica

XIII.M50-M54.M54.3 Sciatica

XII.L20-L30.L20.8 Other atopic dermatitis

XVIII.R50-R69.R52.2 Another constant pain

XVIII.R50-R69.R52.0 Acute pain

XII.L20-L30.L30.9 Dermatitis, unspecified

XVIII.R10-R19.R11 Nausea and vomiting

XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not elsewhere classified

Contraindications:

Hypersensitivity, including to other local anesthetics - esters PABK, parabenzu, p-phenylenediamine or other ingredients of the drug.

For anesthesia using the creeping infiltrate method, severe fibrous tissue changes are observed.

With subarachnoid and other types of anesthesia: complete atrioventricular blockade, profuse bleeding, severe hypotension and shock (possibly exacerbation due to cardiodepression and vasodilation, also slowed metabolism of amides), local infections in the area of presumed puncture (possible infection in the subarachnoid space, changes in the local pH reduce the effectiveness of anesthesia), sepsis (high risk of CNS stimulation).

Children under 12 years.

Carefully:

It should be borne in mind that when carrying out local anesthesia with the same total dose, the toxicity of procaine is higher the more concentrated the solution is.

Emergency operations, accompanied by acute blood loss.

Conditions accompanied by a decrease in hepatic blood flow (eg, in chronic heart failure, liver disease), progression of cardiovascular failure (usually due to the development of heart block and shock).

Inflammatory diseases or infection of the injection site.

Deficiency of pseudocholinesterase.

Renal failure.

Children from 12 to 18 years old and elderly patients (over 65 years), weakened patients, pregnancy and childbirth.

Pregnancy and lactation:

Recommendations FDA category C. Adequate and well-controlled studies in humans and animals have not been conducted. Penetrates through the placenta by diffusion. In retrospective studies on the use of local anesthetics during emergency surgical interventions, pregnant women have no adverse effect on the fetus.

There is no information on the penetration into breast milk, but the negative impact on the child is not described.

The drug should be used when the benefit exceeds the risk for the pregnant and the mother, for the fetus and the newborn.

Dosing and Administration:

Inside, intradermally, intramuscularly, intravenously, by electrophoresis, rectally. For infiltrative anesthesia, 0.25-0.5% solutions are used, conductor - 1-2% epi- or peridural - 2% (20-25 ml), spinal cord - 5% solution (2-3 ml). An appointment for intraosseous anesthesia is possible.

With paranephric blockade, 50-80 ml of a 0.5% solution is injected, vagosympathetic 30-100 ml of a 0.25% solution. To eliminate the pain syndrome used inside, in / m or / in. In a vein slowly inject from 1 to 10-15 ml of 0.25-0.5% solution.

Inside, use a 0.25-0.5% solution to 30-50 ml 2-3 times a day.

For circular and paravertebral blockade, eczema and neurodermatitis are recommended for injection of 0.25-0.5% solution.

Treatment of hypertension, atherosclerosis, coronary artery spasm - an / m 2% solution of 5 ml 3 times a week, course - 12 injections (4 courses are possible during the year).

Side effects:

Systemic adverse reactions develop immediately or within 30 minutes after administration.

Hematological: anemia, methemoglobinemia.

The cardiovascular system: bradycardia, arrhythmias, chest pain, hypertension (a consequence of the sympathomimetic effect with the addition of vasoconstrictors), hypotension, dizziness, tachycardia (provoked by the addition of a vasoconstrictor), peripheral vasodilation.

GIT: constipation, fecal incontinence, nausea and / or vomiting.

Respiratory system: a stop of independent breathing.

Urinary system: urinary incontinence, urethritis.

Nervous system: dizziness, confusion, headache, prolonged numbness or tingling of the lips, tongue and oral mucosa, paresis of the lower extremities, paresthesia, persistent anesthesia, anxiety, convulsions, loss of consciousness, visual disturbances, tremor, tinnitus, muscle twitching. After subarachnoidal administration or with the unintentional subarachnoid administration of local anesthetics during epidural anesthesia, motor and sensitive blockade may extend proximally than necessary. In rare cases, paralysis of the musculature of the chest is complicated by a stop in breathing. In some patients, after spinal anesthesia, transient neurologic disorders due to irritation of the roots of the spinal nerves are possible. The "horse tail" syndrome is possible with an uneven distribution of trimecaine injected under pressure. With transient stimulation of the spinal roots, neurological disorders spontaneously disappear within a few days or weeks,and with the syndrome of "pony tail" they can be irreversible.

Other: weakness, allergic reactions (anaphylactic shock is possible).

Overdose:Symtomas: when used in high doses, it is possible to have excessive absorption, accompanied by nausea, vomiting, sudden cardiovascular collapse, increased nervous excitability, tremor and convulsions, respiratory depression.
Other symptoms: pallor of the skin and mucous membranes, dizziness, "cold" sweat, quickening of respiration, tachycardia, apnea, methemoglobinemia. Action on the central nervous system is manifested by a sense of fear, hallucinations, motor excitement.
Treatment: general resuscitation measures. In case of intoxication after injection into the muscles of the arm or leg, urgent application of the tourniquet is recommended to reduce the further receipt of the drug in the total blood flow. Maintenance of adequate pulmonary ventilation, detoxification and symptomatic therapy.

Interaction:

With intravenous injection, it increases the inhibitory effect on the central nervous system for general anesthesia, hypnotics, sedatives, narcotic analgesics and tranquilizers.

Metabolite procaine PABA is a competitive antagonist of sulfonamides and can weaken their antimicrobial effect.

Disinfection solutions that contain heavy metals - local anesthetics can displace heavy metal ions from disinfection solutions, which causes severe local irritation and edema; It is not recommended to use such solutions for the chemical disinfection of containers containing local anesthetics, and when disinfected with skin or mucous membranes, anticipatory measures are necessary before anesthesia.

MAO inhibitors, including selegiline, procarbazine, furazolidone - with simultaneous application increases the risk of hypotension, therefore, 10 days before the planned surgical intervention under subarachnoid anesthesia, it is recommended to cancel MAO inhibitors.

Opioid (narcotic) analgesics - respiratory disorders caused by spinal or peridural anesthesia at a high level, can be added to the effects of opioids and cause changes in respiratory rate and alveolar ventilation. With epidural or spinal anesthesia at a high level, the vagal effects of alfentanil, fentanyl or sufentanil are more pronounced, which increases the risk of bradycardia and / or hypotension.

Cholinesterase inhibitors (antimiasthenic agents, demecaria, isofluorophate, insecticides, neurotoxic in large quantities, thiotepa, cyclophosphamide, ecotiophate) inhibit the metabolism of PABA esters, therefore, with an increase in the absorption of anesthetics, their toxicity may increase.

β-blockers, including topical preparations, in the presence of systemic absorption may slow down metabolism and increase the risk of toxicity of procaine due to decreased hepatic blood flow, and increase the risk of bradycardia.

In patients receiving anticoagulants (warfarin, heparin sodium, dalteparin sodium, danaparoid, adenoparin calcium, sodium enoxaparin), the trauma of blood vessels during epidural or subarachnoid administration of local anesthetics can lead to hemorrhage in the central nervous system or soft tissues.

Antimiasthenic drugs - local anesthetics, especially with rapid absorption in large quantities, inhibit the transmission of the nerve impulse, acting as antagonists of the action of antimiasthenic drugs on skeletal muscles. An adequate control of myasthenia gravis may require a temporary correction of the dose of antimiasthenic drugs.

Neuromuscular blockers - local anesthetics, especially with rapid absorption in large quantities, inhibit the transmission of a nerve impulse, which lengthens the action of neuro-muscular blockers.

Vasoconstrictors (methoxamine, phenylephrine, epinephrine) - it is not recommended to combine methoxamine and local anesthetics, since the effect of both drugs is prolonged, and prolonged exposure to methoxamine is accompanied by inhibition of circulation and skin debridement. When combining procaine with other vasoconstrictors, it is necessary to carefully observe the proportions, especially when anesthetizing areas of peripheral arteries (fingers, nose, penis), where blood supply to the gangrene is more likely.

In patients receiving ganglion blocking antihypertensives (guanagrel, guanethidine, meqamylamine, trimetafan), severe hypotension and / or bradycardia may develop with spinal or epidural anesthesia with procaine at a level sufficient for sympathetic blockade.

Special instructions:

To prepare a 0.25-0.5% solution for infiltration or conductive anesthesia, the procaine solution can be diluted with sterile water for injection at any concentration.

With intra- and subcutaneous administration, a 1% solution of procaine causes less pain than 1% solutions of lidocaine and lidocaine with epinephrine 1: 100,000, comparable to pain when a physiological solution of sodium chloride is administered.

It should be borne in mind that when carrying out local anesthesia with the same total dose, the toxicity of procaine is higher the more concentrated the solution is.

Prokaine penetrates slowly through undamaged mucous membranes, therefore it is not effective for surface anesthesia.

As an aid procaine apply IV in and in with hypertension, late toxicosis of pregnant women with hypertonic syndrome, spasms of blood vessels, phantom pains, peptic ulcer of stomach and duodenum, ulcerative colitis, itching, neurodermatitis, eczema, keratitis, iridocyclitis, glaucoma.

Patients need control over the functions of the cardiovascular, respiratory and central nervous systems. It is necessary to abolish monoamine oxidase inhibitors 10 days before the local anesthetic. Before use, mandatory sampling for individual sensitivity to the drug.

Impact on the ability to drive vehicles and manage mechanisms

When taking the drug should be abandoned driving vehicles or management mechanisms.

Instructions

Procain (Procainum)