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99% High Purity Pharmaceutical Raw Materials White Powder Quinidine CAS:56-54-2

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99% High Purity Pharmaceutical Raw Materials White Powder Quinidine CAS:56-54-2

Brand Name : TINGYI
Model Number : 56-54-2
Certification : GMP,SGS,ISO9001:2008,KOSHER
Place of Origin : China
MOQ : 100g
Price : Contact Us
Payment Terms : Western Union, MoneyGram, Bank Transfer, Bitcoin
Supply Ability : 5000kg/Month
Delivery Time : Within 7 Working Days
Packaging Details : Stealth And Discreet Packaging
Product Name : Quinidine
Purity : 99%
MF : C20H24N2O2
MW : 324.42
CAS : 56-54-2
Einecs no. : 200-279-0
Appearance : white powder
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99% High Purity Pharmaceutical Raw Materials White Powder Quinidine CAS:56-54-2 for antiarrhythmic drug


Product details:


Product Name: Quinidine
Synonym: (8R,9S)-6'-Methoxycinchonan-9-ol;6-METHOXY-A-(5-VINYL-2-QUINUCLIDINYL)-4-QUINOLINE-METHANOL;CONCHININE;CONQUININE;B-QUININE;(+)-QUINIDINE;QUINIDINE;(+)-QUINDINE
CAS: 56-54-2
MF: C20H24N2O2
MW: 324.42
EINECS: 200-279-0

Related categories: Antibiotics, alkaloids; Chinese herbal medicine ingredients; cell signaling and neurobiology; APIs; antiarrhythmic drugs; cell biology; chiral; Alkaloids; Alkoxyquinolines; plant extracts; cardiovascular and cerebrovascular research raw materials; pharmaceutical intermediates; Raw materials; intermediates; Biochemistry; for Resolution of Acids; Optical Resolution; Quinoline Alkaloids; Quinolines; Synthetic Organic Chemistry; Intermediates & Fine Chemicals; Pharmaceuticals; Cinchona Alkaloids Monovalent Ion Channels; Chiral Catalysts, Ligands, and Reagents; Other Sodium Channel Modulators; Privileged Ligands and Complexes; Sodium Channel Modulators; Chiral Reagents; Heterocycles; DURAQUIN
Melting Point: 168-172 °C(lit.)

Specific Rotation: 256 º (c=1, EtOH)

Boiling Point: 462.75°C (rough estimate)

Density: 1.1294 (rough estimate)

Refractive Index: 1.5700 (estimate)

Storage Conditions: Store at -20°C

PKa: 5.4, 10.0(at 20℃)

Optical Activity: α]20/D +265±5°, c = 0.8% in ethanol (dry matter)

Water solubility: 0.05 g/100 mL (20 ºC)

Sensitivity: Light Sensitive

Stability: Stable. Incompatible with strong oxidizing agents.
Appearance: white powder


Description:


Quinidine is an antiarrhythmic drug. It is commonly used in its sulfates but also in the hydrochloride and gluconate salts. Quinidine sulphate is a white crystalline powder, odorless, very bitter taste, melting point 175 ~ 176 ° C, soluble in water, slightly soluble in ethanol.
Quinidine is an alkaloid extracted from the bark of the genus Cinchona ledgeriana (Moens). It has a direct effect on the cell membrane, mainly inhibits the transmembrane movement of sodium ions, and is self-disciplined and conductive to the heart. Both stress and contractility have direct inhibitory effects, and both have anticholinergic effects on the heart. It is suitable for the treatment and prevention of atrial fibrillation, atrial flutter, supraventricular and ventricular tachycardia, and the treatment and prevention of malignant premature beats.
Quinidine is the right-handed body of quinine, which has similar pharmacological properties, but quinidine is 5 to 10 times stronger than quinine in the heart, and it binds to the lipoprotein of the sodium channel on the myocardial cell membrane, making the channel The gate narrows to prevent Na+ inflow, resulting in a decrease in the depolarization speed of the 0 phase and a slower conduction. The myocardial self-discipline is reduced due to the slowing of the depolarization rate of the fourth phase, and the ectopic rhythm point is suppressed. Slow down the 3-phase K+ outflow to extend the refractory period. It also inhibits myocardial contractility and has anti-parasympathetic and sympathetic effects. Quinidine blocks the alpha receptor and causes blood vessels to dilate, especially when intravenously, causing a sharp drop in blood pressure, so it cannot be administered intravenously.
The above information was compiled by Andy editor of ChemicalBook.


Application:


It has anticholinergic effect and can induce ventricular arrhythmia, that is, syncope.

Class IA antiarrhythmic drug; potassium channel blocker; also used as a chiral catalyst.

The pharmacological effects of quinidine against arrhythmia mainly extend the myocardial refractory period, reduce myocardial stress, self-discipline and conductivity, and are used to treat atrial or ventricular tachycardia, to convert atrial flutter and atrial fibrillation. And prevent its recurrence. In the use of quinidine, due to different causes and individual differences, the amount of quinidine treatment and tolerance in different cases are also inconsistent. Hyperthyroidism, chronic atrial fibrillation, and significant enlargement of the heart are more tolerated. Long-term heart failure, bundle branch block, coronary heart disease tolerance is low, sometimes the general treatment volume causes poisoning, although quinidine poisoning is related to the size of the dose, but a small amount of individual cases can lead to arrhythmia. It is currently considered to be the inhibitory effect of quinidine on conduction, which can induce the reentry agonism of the diseased myocardium. In order to reduce quinidine poisoning, changes in heart rate, rhythm, blood pressure and electrocardiogram must be strictly observed during the medication.


Usage and dosage:


Oral: 0.2g per day on the first day, once every 2 hours, 5 times, if there is no obvious adverse reaction, the next day increased to 0.3 g each time, 0.4 g on the third day, every 2 hours 1 Once, for 5 times, the daily total should not exceed 2 g. After returning to normal heart rhythm, change the amount to 0.2 to 0.4 g per day. If the patient is ineffective for 3 to 4 days or has adverse reactions, the drug should be discontinued. Children should be given a test dose of 2 mg/kg. If there is no adverse reaction, start treatment after 1-2 hours. On the first day, each time 6 mg/kg, once every 2 hours, take 4 to 5 times; if the effect is not obvious There is no symptoms of poisoning. On the second day, you can continue to use the original amount or increase the original amount by 20%. If necessary, the original amount can be maintained on the third day.
Intravenous or intravenous drip: 0.25 g each time, diluted to 50 ml with 5% glucose injection, and slowly injected. In children, the first dose is 2 mg/kg, diluted with 100 ml of 5% glucose injection, and then instilled for 1 hour. If there is no allergic reaction, each time 6 mg/kg, once every 3 hours, 1 day The total amount does not exceed 30 mg/kg.


Toxic reaction:


Quinidine can produce two toxic reactions, one related to the size of the dose. When daily oral administration of more than 3g of quinidine, the QRS complex is often broadened, sometimes more than 50%. Atrioventricular block and significant sinus bradycardia are indications for discontinuation. Another toxic reaction has nothing to do with the dose size. For example, when taking 0.2-2.0 g of quinidine per day, about 2% to 4% of patients have ventricular premature beats, ventricular tachycardia and even ventricular fibrillation and die. Ventricular ventricular tachycardia and ventricular fibrillation are often characterized by torsade ventricular tachycardia. It is currently believed that due to prolonged ventricular repolarization time (often QT interval is prolonged), repolarization time dispersion of various parts of the myocardium (dispersion) Increase, the widening of the vulnerable period plus the general conduction disorder of the myocardium, easy to cause continuous and disordered reentry agonism, especially in patients with poor myocardial conditions, or patients with electrolyte imbalance, should be more careful when using quinidine, When Q-Tc>0.50s, it should be administered cautiously. The side effects of quinidine have been shown to be dose-dependent, so the dose for clinical use should not be too large. Patients who are treated with quinidine cardioversion should be hospitalized to prevent accidents. Medical staff should closely observe the patient's heart rate, blood pressure, blood potassium, and monitoring ECG. One of the following conditions should be discontinued immediately: (1) the heart rate is significantly slowed down, less than 60 times/min; (2) the systolic blood pressure drops below 12.0 KPa (90 mmHg); (3) the Q-Tc interval is prolonged ≥30%; (4) QRS group time is extended by more than 25%; (5) T wave amplitude is reduced, and double peak occurs; (6) Frequent ventricular premature beats can be excluded for other reasons; (7) Tip torsion chamber speed.


Poisoning performance


(1) Excessively easy to produce "Cinchona poisoning" syndrome, such as tinnitus, hearing impairment, vision loss, diplopia, blurred vision, color vision disorder, or temporary deafness, night blindness, headache, dizziness, anxiety, and even death. Generally related to the dose.
(2) Toxicity of the heart: There are various degrees of atrioventricular block and cardiac arrest, ventricular premature beats, ventricular tachycardia, and ventricular fibrillation. Patients with ventricular fibrillation or ventricular tachycardia may present with recurrent episodes of syncope, sometimes with convulsions or urinary incontinence, specifically known as "Quinidine syncope." A typical patient has no prodromal symptoms and suddenly loses consciousness. His face is gray or pale and his hair is persistent for 30 seconds to 3 to 4 minutes. It can recover naturally or recover after recovery, and it can die. When treated with a large amount of quinidine, the incidence rate is 3% to 4%, even if a therapeutic amount is administered.
(3) Electrocardiogram: QT interval is prolonged, ST segment is decreased, T wave is inverted; severe poisoning PR interval is prolonged, QRS complex is widened, QRS can be bundled conduction block type; or only the width is increased, and There is no change in the direction of each wave.
(4) Mental state: In severe cases, mental disorders, paralysis, hallucinations, etc. may occur.
(5) Blood system: subcutaneous hemorrhage, gastrointestinal bleeding, etc., as well as thrombocytopenia, leukopenia, neutropenia, hemolytic anemia, etc.
(6) Allergic reactions: high fever, rash, thrombocytopenic purpura, asthma, angioedema, acute hemolytic anemia. Severe cases can be manifested as decreased blood pressure, dizziness, cold sweat and syncope, and even dyspnea or peripheral circulatory failure, respiratory depression, and respiratory arrest.
(7) Others: such as occasional muscle weakness, lupus-like syndrome.


Poisoning First Aid:


1. Quinidine should be discontinued when premature beats or QRS waves are increased by 30% during the course of administration.
2. Atrioventricular block, especially in the A-S syndrome, should be given immediately 0.1-1.0 mg of isoproterenol and 200 ml of 5% glucose. If necessary, a pacemaker can be used.
3. When quinidine fainting occurs, in vitro cardiac massage and mouth-to-mouth resuscitation are usually performed, usually less than 2 to 3 minutes, and most episodes can be stopped spontaneously. Intravenous propranolol or propranolol may control ventricular fibrillation.
4. Severe progressive cardiac poisoning reaction, intravenous sodium bicarbonate or sodium lactate.
5. Hypotension caused by quinidine, intravenous rehydration and application of vasoconstrictors.
6. Respiratory depression and circulatory failure, optional central stimulants such as An Naca, Nicocam, Lobeline and so on. Perform artificial respiration if necessary.
7. Excessive patients can undergo hemodialysis, or blood perfusion, to accelerate drug excretion.


Adverse Reactions:


The therapeutic index of this product is low, and about 1/3 of patients have adverse reactions.
1 cardiovascular: the occurrence of cardiac arrest and conduction block, more common in patients with structural heart disease, ventricular premature beats, ventricular tachycardia and ventricular fibrillation. This product can cause blood vessels to dilate to produce hypotension, and individual vasculitis can occur.
2 gastrointestinal adverse reactions are common, including nausea, vomiting, cramps and diarrhea, may be caused by direct stimulation.
3 cinchona reaction: can produce tinnitus, gastrointestinal disorders, palpitations, convulsions, headaches and flushing. Visual impairment such as blurred vision, photophobia, diplopia, color vision disorder, dilated pupils, dark spots and night blindness. Hearing impairment, fever, urticaria, local edema, dizziness, tremors, dizziness, excitement, coma, anxiety, and even death. Generally related to the dose.
4 idiosyncratic reactions: dizziness, nausea, vomiting, cold sweat, shock, bruising, respiratory depression or cessation. Not related to the dose.
5 allergic reactions: a variety of rash, especially urticaria, itching more common, fever, asthma, thrombocytopenia, neutropenia, anemia (regenerative or hemolytic), hepatitis, collapse, sudden death. Not related to the dose.
6 muscle: make myasthenia weakness worse.


Precautions:


1. Arrhythmia caused by digitalis poisoning, second to third degree atrioventricular block, sick sinus syndrome, cardiogenic shock, severe myocardial damage, allergy to quinine or its derivatives, thrombocytopenia patients and Pregnant women are banned. Severe heart failure, extreme bradycardia, hypotension (except for arrhythmia), hypokalemia or liver and kidney dysfunction in patients with caution.
2. Intravenous injection can often cause hypotension and respiratory depression, and non-critical patients should try not to inject.
3. Blood pressure and electrocardiogram should be monitored during medication (prolonged PR, QRS wave, T wave should be considered when discontinued), blood cell and platelet count, liver and kidney function (long-term medication), cardiac function, serum potassium concentration and Blood concentration. Those who remain inactive for 3 to 5 days should be discontinued.
4. For the correction of atrial fibrillation, atrial flutter should first give a strong heart sputum saturation, so as to avoid heart rate after heart rhythm change, causing heart failure. For patients with low blood pressure or in shock state, blood pressure should be increased first, and quinidine should be used after the shock is corrected.
5. The treatment of adverse reactions is as follows: ventricular arrest and conduction block can be intravenously administered isoproterenol or norepinephrine. For polymorphic ventricular tachycardia, it can be treated with isoproterenol, sodium bicarbonate or sodium lactate. After the visual impairment, nitrates and methacholine may be effective. Intravenous toxic black sputum can be relieved by intravenous sodium nitrate.


Medicine Interactions:


1. Quinidine has an additive effect when combined with other antiarrhythmic drugs.
2. When combined with anticoagulant drugs, the two drugs can affect each other. Care should be taken to adjust the two doses.
3. Phenobarbital and phenytoin can accelerate the intrahepatic metabolism of the product and reduce the blood concentration of quinidine.
4. In combination with digoxin, the blood concentration of digoxin can be increased.
5. Combined with anticholinergic drugs, it can increase the efficacy of anticholinergic drugs; combined with cholinergic drugs, can reduce the efficacy of cholinergic drugs; combined with neuromuscular blockers, especially myostatin and succinylcholine, can make them breathe The inhibition is enhanced.
6. Combined with potassium preparations can make this product more effective, while hypokalemia can make this product less effective.
7. In combination with beta blockers, the inhibitory effect on sinoatrial node and atrioventricular node can be aggravated.
8. Combined with antihypertensive drugs can enhance blood pressure and vasodilator.
9. In combination with rifampicin, the blood concentration of this product can be lowered.
10. Urine basifying agents such as acetazolamide, antacids or bicarbonate can increase the reabsorption of quinidine by the renal tubules and increase the blood concentration of the product, thereby causing poisoning reactions.


Toxicological Research:


Genotoxicity: bacterial mutation test, mouse lymphoma mutation test, bone marrow and in vitro human lymphocyte genetic test results in mice showed that there was no genotoxicity in sertraline in the presence or absence of metabolic activation.


Reproductive toxicity: When the dose was 80 mg/kg (in terms of mg/m2, which is 4 times the maximum recommended dose of MRHD), one of the two rat experiments observed a decrease in fertility. Reproductive toxicity studies (up to 4 times the maximum recommended dose of humans in mg/m2) were performed on rats and rabbits at doses of 80 mg/(kg·d) and 40 mg/(kg·d), respectively. No teratogenic effects were observed at each test dose. Delayed ossification of the litter was observed in pregnant rats and rabbits when sertraline was administered at the organogenesis stage (10 mg/kg and 40 mg/kg, respectively, about 0.5 and 4 times the MRHD in mg/m2). Female rats were given sertraline in late pregnancy and lactation. The number of deaths in young rats born at the dose of 20 mg/kg and the first 4 days after birth increased, and the weight of young rats decreased in the first 4 days after birth. The rat has no effect dose of 10 mg/kg. The decrease in the survival rate of young rats is caused by the exposure of sertraline in the uterus. However, the clinical significance of these effects is unclear.


Carcinogenicity: The highest dose of 40 mg/(kg·d) was performed on CD-1 mice and Long-Evans rats (about 1 and 2 times, respectively, in mg/m2). At doses of 10 to 40 mg/(kg·d), dose-related hepatic adenomas increased in male mice, and no increase in hepatic adenomas was observed in female mice or rats treated with the same administration. No increase in hepatocellular carcinoma was observed. The spontaneous rate of liver adenomas in CD-1 mice is volatility, and the significance of this result to humans is still unclear. At 40 mg/(kg·d), female rats developed an increase in thyroid follicular adenomas without thyroid hyperplasia. Compared with the control group, the uterine adenoma increased in the 10-40 mg/(kg·d) administration group, but the correlation between the result and the drug was not clear.


Dependence: Animal studies have not shown the potential for excitatory effects or abuse of barbiturate (central inhibitors).


Adapt to symptoms:


Sertraline is used to treat symptoms associated with depression, including depression with or without history of mania. After satisfactory results, continued use of sertraline can effectively prevent recurrence and recurrence of depression. Sertraline is also used to treat obsessive-compulsive disorder. After initial treatment, sertraline maintains its effectiveness, safety and tolerability during the two years of treatment of obsessive-compulsive disorder.


Precautions:


1. Sertraline should be carefully considered in combination with drugs that increase serotonin neurotransmission, such as tryptophan or fenfluramine, to avoid possible pharmacodynamic interactions.
2. There is no experience in the optimal timing of conversion of other serotonin reuptake inhibitors, antidepressants or antiobsessive drugs to sertraline. Care should be taken when switching treatments, especially long-acting drugs such as fluoxetine, and should be carefully evaluated and monitored. The washout period from conversion of a selective serotonin reuptake inhibitor to another drug has not been determined.


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1,4-Butanediol(BDO)
EthylOleate(EO)
Grape Seed Oil(GSO)

Benzyl Alcohol(BA)
Benzyl benzoate(BB)
Guaiacol
PolyEthylene Glycol(PEG)
Polysorbate 80

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Methenolone Enanthate

Methenolone Acetate

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(Dehy droepiandrosterone)
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4-DHEA
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Epiandrosterone
Epiandrosterone Acetate

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Androstatrienedione

2, 4-Dinitrophenol
Dustasteride
Desonide
Triamcinolone
Finasteride
Cytomel, T3
L-Thyroxine, T4
Rimonabant
L-Carnitine

Sex Enhancer

Flibanserin
Cialis (Tadalafil)
Viagra (Silde nafil) Vardenafil (Levitra)

Acetildenafil (Hongdenafil)
Yohimbine Hcl

Maca Extract

Pain Killer

Benzocaine / Benzocaine hcl
Procaine / Procaine Hcl
Lidocaine HCL

Tetracaine / Tetracaine HCL
Bupivacaine/ Bupivacaine HCL
Articaine / Articaine hcl

Anti-Estrogen

Tamoxifen Citrate (Nolvadex)
Clomiphene citrate (Clomid)
Exemestane(Aromasin)

Anastrozole (Arimidex) Letrazole(Femara / For mestane)
Fulvestrant

Pharmaceuticals

Phenacetin

Dexamethasone Sodium Phosphate
Paracetamol
Pregabalin


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