Novocaine

I N S T R U C T I O N for medical use of the medicinal product NOVOCAINE (NOVOCAINUM)

Composition:

Active substance: procaine; hydrochloride of β-diethylaminoethyl ester of para-aminobenzoic acid;

1 suppository contains procaine hydrochloride (novocaine) 0.1 g (100 mg);

Excipient: hard fat.

Pharmaceutical form. Rectal suppositories.

Main physicochemical properties: white suppositories, or white with yellowish or creamy tint. Presence of a white coating on the surface of the suppository is permissible.

Pharmacotherapeutic group. Agents for treatment of hemorrhoids and anal fissures for local application. Local anesthetics. ATC code C05AD05.

Pharmacological properties.

Pharmacodynamics.

Disrupts the generation and conduction of nerve impulses, predominantly in unmyelinated fibers. Being a weak base, it interacts with membrane sodium channel receptors, blocks sodium ion influx, and displaces calcium from receptors located on the inner membrane surface. Alters the action potential in nerve cell membranes without significantly affecting the resting potential. Antiarrhythmic action is associated with an increase in the effective refractory period, reduction of myocardial excitability and automaticity. Eliminates descending inhibitory influences of the reticular formation of the brainstem. Suppresses polysynaptic reflexes. Reduces intestinal smooth muscle spasm.

Pharmacokinetics.

Well absorbed after rectal administration. During absorption, it is rapidly hydrolyzed, mainly in the systemic circulation, with the participation of esterases and plasma cholinesterases, forming para-aminobenzoic acid and diethylaminoethanol. Excreted in urine – 80%.

Clinical characteristics.

Indications.

Hemorrhoids, anal fissures.

Contraindications.

Hypersensitivity to the components of the drug.

Arterial hypotension.

Myasthenia.

Childhood age.

Interaction with other medicinal products and other forms of interaction. Should not be administered concurrently with drugs undergoing hepatic acetylation (sulfonamides, hydralazine, isoniazid, procainamide) and hypotensive agents. Concurrent use with monoamine oxidase inhibitors (MAOIs) (furazolidone, procarbazine, selegiline) increases the risk of developing arterial hypotension. Anticholinesterase drugs enhance procaine toxicity (by inhibiting its hydrolysis). The metabolite of procaine (para-aminobenzoic acid) acts as a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial activity. The medicinal product reduces the effect of anticholinesterase agents on neuromuscular transmission. Cross-sensitization is possible. Potentiates the effect of direct anticoagulants.

Special precautions for use.

Monitoring of cardiovascular, respiratory, and central nervous system functions is required during administration of the drug.

Due to possible depression of myocardial contractility and reduction of arterial blood pressure, the drug should be used with extreme caution in myocardial infarction. It is not recommended for use in severe atherosclerosis. Concomitant administration with drugs undergoing hepatic acetylation (sulfonamides, hydralazine, isoniazid, procainamide) should be avoided. If there is no therapeutic effect within 7 days of treatment, proctological examination is required.

Use during pregnancy or breastfeeding. The drug should not be used during pregnancy or breastfeeding.

Ability to affect reaction speed when driving or operating machinery. Use with particular caution when driving or operating complex machinery due to possible development of dizziness and weakness.

Administration and Dosage.

Administer rectally.

For adults – 1 suppository 1–2 times daily.

The duration of treatment is determined individually by a physician, taking into account the course and severity of the disease, the therapeutic effect achieved, and the overall treatment strategy.

Children. The drug must not be used in children.

Overdose.

When used in high doses, excessive absorption may occur, leading to nausea, vomiting, increased nervous excitability, tremor and convulsions, respiratory depression, and sudden cardiovascular collapse.

Treatment: symptomatic.

Side effects.

Immune system: allergic reactions, possible anaphylactic shock.

Cardiovascular system: arterial hypotension, bradycardia, arrhythmias.

Central nervous system: general weakness, dizziness, headache, drowsiness.

Gastrointestinal system: nausea, vomiting.

Blood system: methemoglobinemia.

Other: reactions at the site of administration.

Shelf life. 2 years.

Storage conditions.

In the original packaging at a temperature not exceeding 15 °C.

Keep out of reach of children.

Packaging. 5 suppositories in strips; 2 strips per carton.

Prescription status. Prescription only.

Manufacturer: JSC "Monfarm".

Manufacturer's address and location of business activity:

8, Zavodska Street, Avramivka, Uman district, Cherkasy region, 19161, Ukraine.