What Is Procainamide?

Procainamide is a class a antiarrhythmic drug. It has similar effects to quinidine as it has on cardiac autonomy, conductivity, excitability, and membrane response. It is suitable for the treatment of frequent pre-contraction, atrial and ventricular tachycardia, pre-excitation syndrome with atrial fibrillation and atrial flutter. This medicine mainly damages the heart, nervous system and produces allergic reactions.

Drug type: Essential medicines
Drug name: Procainamide

English name: Procainamide
Chinese alias: Procainamide
English alias: Amidoprocaine; Procan-SR

Introduction to Procaine Amines

Procainamide Basic Information

Chinese name: Procaine

Chinese alias: 4-amino-N- [2- (diethylamino) ethyl] benzamide; 4-amino-n- (2-diethylaminoethyl) benzamide; procainamide Novocainamide; Amishlin; Prostil; Procainamide hydrochloride; Procainamide hydrochloride

English name: procainamide; Pronestyl; Procaine Amide; procainamide; Amidoprocain; Cardiorytmin; Isoritmon

English alias: Benzamide, 4-amino-N- [2- (diethylamino) ethyl]-; 4-Amino-N- (2-diethylaminoethyl) benzamide; 4-amino-N- [2- (diethylamino) ethyl] benzamide; Amidoprocaine

CAS number: 51-06-9

Molecular formula: C ₁₃ H ₂₁ N ₃ O

Structural formula:

Molecular weight: 235.32500

Exact mass: 235.16800

PSA: 58.36000

LogP: 2.31250

Procaine amine physicochemical properties

Density: 1.06

Boiling point: 421.8ºC at 760mmHg

Flash point: 208.9ºC

Its hydrochloride is usually white or light yellow crystalline powder; odorless; hygroscopic. Melting point: 165-169 ° C, easily soluble in water, soluble in ethanol, slightly soluble in chloroform, and very slightly soluble in ether.

Procainamide Safety Information

Customs code: 2924299090 ^[1]

Procaine Pharmacopoeia Standard

[Identification] (1) Take 0.1g of this product, add 5ml of water, add 1 drop of ferric chloride test solution and concentrated hydrogen peroxide solution, slowly heat to boiling, the solution is purple, and then becomes dark brown Brown-black. (2) The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 398). (3) Identification of chlorides in aqueous solution of this product (Appendix).

[Inspection] Take 1.0g of this product, dissolve it by adding 10ml of water, and measure it according to law (Appendix VI H). The pH value should be 5.0 6.5. Loss on drying: Take this product and dry it at 105 to constant weight. The weight loss should not exceed 0.3% (Appendix L). Take the lignite residue of this product and check it according to law (Appendix N). The residual residue should not exceed 0.1%. The heavy metal shall be taken as the residue left under the burning residue, and shall be inspected in accordance with the law (Appendix H second method). The content of heavy metal shall not exceed 10 parts per million.

[Content determination] Take about 0.55g of this product, accurately weigh it, and titrate with sodium nitrite titration solution (0.1mol / L) according to the permanent stop titration method (Appendix A). Each 1 ml of sodium nitrite titration solution (0.1 mol / L) is equivalent to 27.18 mg of C13H21N30 · HC1.

[Category] Local anesthetics.

[Storage] shading and sealed.

Procaine Drug Description

Procainamide Classification

Circulatory Drugs> Antiarrhythmic Drugs> Class Antiarrhythmic Drugs

Procainamide dosage form

1. Injection: 0.1g, 0.2g, 0.5g, 1.0g;

2. Tablet: 0.25g.

Pharmacological effects of procainamide

Procainamide is a class a antiarrhythmic drug. It has similar effects to quinidine as it has on cardiac autonomy, conductivity, excitability, and membrane response. Inhibition of Na + influx in cardiomyocytes, reducing the speed and amplitude of phase 0 of the action potential, extending the time course and slowing the conduction. The slope of the zero division pole of the hippo system decreases, and the autonomy decreases. The anticholinergic effect is weak and does not block the? Receptor.

Procainamide pharmacokinetics

Oral absorption is fast and complete, the absorption rate can reach 75% to 100%, the peak plasma concentration reaches 45 to 90 minutes after oral administration, the peak concentration reaches 15 to 60 minutes after intramuscular injection, the bioavailability is 75%, and the effective plasma concentration is 4 to 12 g / ml, the drug-protein binding rate is about 15%, the half-life is about 3 to 3.5 hours, and the plasma drug concentration reaches about 5 to 7 half-lives. Almost all are metabolized by liver acetylation to acetylprocacine, which is almost entirely excreted from the urine.

Procainamide indications

Procainamide has the same clinical indications as quinidine but it is not as good as quinidine in reversion of atrial fibrillation and atrial flutter, so it is mainly used in the treatment of ventricular arrhythmias such as pre-ventricular Contraction, ventricular tachycardia, etc. can also prevent ventricular tachycardia and ventricular fibrillation.

Procainamide contraindications

Those who are allergic to procainamide or procaine, severe hypotension, conduction dysfunction, sick sinus syndrome, history of lupus erythematosus, and myasthenia gravis are disabled.

Procainamide usage and dosage

1. For emergency cardioversion, 100 mg intravenously for 5 minutes, if necessary, repeat every 5 to 10 minutes until it is effective but the total amount should not exceed 1.0 to 2.0 g, and 1 to 4 mg intravenous infusion is maintained every minute after effective.

2. Intravenous injection: Adults: take a slow intravenous injection of 100mg, and repeat it every 5 to 10 minutes if necessary, the total amount does not exceed 10-15mg / kg, or intravenous drip at 10-15mg / kg for 1 hour, followed by 1.0 Maintained at 1.5 mg / kg. Children: 2mg / kg each time, dissolved in 50-100ml of glucose solution, slowly or intravenously.

3. Oral: 3 to 4 times a day, 0.5 to 0.75 g each time, and gradually reduced to 2 to 3 times a day, 0.25 g each time after a normal heart rhythm.

4. Intravenous drip: 0.5 1g, dissolved in 100ml of 5% 10% glucose solution, start dripping within 10-30 minutes, the speed can be appropriately increased, and dripping is completed within 1 hour. Ineffective, give it again after 1 hour, and the total amount should not exceed 2g within 24 hours. The intravenous drip is limited to emergency situations, such as ventricular paroxysmal tachycardia, especially in patients with acute myocardial infarction or other serious heart disease. People should always pay attention to changes in blood pressure and heart rate, after the heart rate is restored, you can stop dripping.

5. Intramuscular injection: 0.5 1g each time.

Procainamide adverse reactions

1. Nausea, vomiting, diarrhea and other gastrointestinal reactions occurred in high doses.

2. Long-term medication can lead to systemic lupus erythematosus-like syndrome. Patients appear positive for anti-DNA antibodies. Excessive doses can also lead to decreased white blood cells.

3. Other rare disorders include nervous, liver, kidney, and muscle system disorders.

Procainamide precautions

(1) Intravenous infusion can reduce blood pressure and prolapse, and the blood pressure, heart rate and heart rhythm should be closely observed. (2) In cases of atrial fibrillation and atrial flutter, if the ventricular rate is fast, it is advisable to first use digitalis cardiotonic drugs to control the ventricular rate after 70 to 80 times per minute before using this drug or quinidine. (3) If the sinus rhythm is not restored or the tachycardia does not stop after 3 days of medication, a change of medication should be considered. (4) When combined with neuromuscular blocking drugs (including depolarizing and non-depolarizing blocking drugs), the blocking effect of the neuromuscular junction is enhanced, and the aging time is prolonged.

Procaine Drug Interactions

1. Enhanced effect when combined with other antiarrhythmic drugs;

2. The combination of antihypertensive drugs during intravenous injection can increase the antihypertensive effect, and the drug should be discontinued if the blood pressure drops or the QRS time limit is extended> 50% during the administration;

3. Combined with cimetidine, the clearance rate can be reduced by 30% to 50% ^[2] .

Procaine poisoning

Procainamide (procainamide, norfocaine) is an effective drug for the treatment of arrhythmias, which is suitable for the treatment of frequent pre-phase contractions (the effect is better for pre-ventricular contractions), atrial and ventricular Tachycardia, pre-excitation syndrome, atrial fibrillation, and atrial flutter.

The drug is absorbed by the stomach and intestines and is quickly divided into the heart muscle. It reaches its peak in the blood for 1 hour after oral administration; it takes effect 10 to 15 minutes after intramuscular injection, maintaining the effect for 4 to 6 hours, and the effect is the strongest after 4 minutes after intravenous injection. The drug is excreted by the kidneys, 50% to 60% of which is excreted from the urine in its original form, with a half-life of 3.5 to 6 hours. During heart failure and renal insufficiency, excretion is slow and prone to accumulation poisoning. Large doses can cause atrioventricular block and ventricular premature contractions, and even ventricular fibrillation. Can inhibit myocardial contraction, intravenous administration of excessive or excessive speed can cause blood pressure to drop (and) ventricular insufficiency. May have cross-allergic reactions with procaine.

Orally take 0.5 0.75g each time, 3 4 / d. Intravenous infusion of 0.5 to 1.0 g is dissolved in 100 ml of 5% glucose solution, and the drip rate can be appropriately accelerated within 10 to 30 minutes, and the drip is completed in 1 hour. The invalid person will be given again after 1h, and the total amount will not exceed 2g within 24h. This medicine mainly damages the heart, nervous system and produces allergic reactions.

Clinical manifestation

Adverse reaction

There may be anorexia, nausea, vomiting and diarrhea after oral administration.

2. Poisoning performance

(1) Large doses can cause atrioventricular block and ventricular premature contractions, and the latter can develop into ventricular fibrillation, which can progressively slow heart rate and cause cardiac arrest.

(2) Central nervous system symptoms: vertigo, hallucinations, hallucinations, depression, convulsions and other symptoms.

(3) Lupus erythematosus reaction, fever, rash, myopathy, arthritis, pericarditis, pleurisy, hepatosplenomegaly can be seen in long-term high-dose application. Most of them can be recovered after drug withdrawal.

(4) Intravenous injection is too fast, blood pressure drops due to dilation of surrounding blood vessels, and even shock.

(5) Allergic reactions, such as chills, fever, itching of the skin, urticaria, burning sensation in the palms and footpads, angioedema, arthralgia, myalgia, etc.

(6) Bone marrow suppression occurs in a small number of patients, leading to granulocytopenia, accompanied by fever, sore throat, difficulty swallowing, and cervical lymphadenopathy.

treatment

The main points of treatment for procainamide poisoning are:

1. Discontinue the drug immediately after discovering the above symptoms, and lavage the stomach with lukewarm 0.45% saline for those with large oral doses.

2. Allergic patients choose anti-amine drugs or prednisone, hydrocortisone, dexamethasone and so on.

3. If arrhythmia occurs, sodium lactate can be given, and corresponding antiarrhythmic drugs are selected according to the type of arrhythmia.

4. Shock, give vasoactive drugs such as dopamine, m-hydroxylamine and other anti-shock measures.

5. Other symptomatic treatments ^[3] .

Procainamide Expert Reviews

Procaine Procaine Procainamide, a class Ia drug, is a broad-spectrum antiarrhythmic drug. Procainamide has similar pharmacological and electrophysiological effects to quinidine, and its effect on ventricular arrhythmias is higher than that of atrial arrhythmias. It has been reported that ventricular tachycardia that is ineffective for lidocaine has no effect on proca Because amines are effective, cardioversion may occur for atrial fibrillation of short duration.

^[4-7]

Procainamide capsule preparation

Compound Procaine Hydrochloride Capsules

Indications: This product is used for neurasthenia, neurasthenia syndrome and autonomic disorders such as insomnia, fatigue, anxiety; headache, dizziness, memory loss, inattention, slow response and palpitations caused by cerebral arteriosclerosis, Improvement of symptoms such as insomnia, sweating, irritability, hot flashes.

Dosage: Oral. 1 capsule at a time, 2 times a day, even for 25 days as a course of treatment, after 5 to 6 days of withdrawal, continue to the next course of treatment.

Dosage form: capsule

Adverse reactions: Occasionally rash, dizziness, nausea, drowsiness, excitement, etc.

Contraindications: Those who are allergic to this product are prohibited.

Precautions:

1. To prevent allergic reactions, take 1 capsule once a day on the first day, once a day; 2 capsules once a day on the second day, once a day. Do not take if you have an allergic reaction such as a rash.

2. Patients with hemophilia should be cautious when taking medication, as pantothenic acid can prolong bleeding time.

Ingredients: This product is a compound preparation, and its components are: each capsule contains: procaine hydrochloride 100mg, calcium pantothenate 5mg.

Properties: This product is a capsule and the content is white or off-white powder.

Medication for pregnant and lactating women: It is not clear.

Drug Interactions: This product should not be taken at the same time as drugs such as sulfa, p-aminosalicylic acid, physostigmine salicylate and neostigmine.

Pharmacological effects: Procaine inhibits the central nervous system constant and excites excessively. Experiments have shown that procaine can increase the proliferation rate and saturation density of diploid cells and prolong the life of the cells (only affects cells that are actively dividing, and this effect is weakened or absent on senescent cells).

Calcium pantothenate is a precursor of coenzyme A and is necessary for a variety of metabolic links (including carbohydrates, proteins and lipids). It can participate in the synthesis of steroids, porphyrins, acetylcholine and other substances, and can maintain normal epithelial function ^{[8 ]} .