altiazem
Diltiazem HCl
CAS: 33286-22-5
Molecular Formula: C22H27ClN2O4S
altiazem - Names and Identifiers
| Name | Diltiazem HCl |
| Synonyms | masdil angizem anginyl altiazem Diltiazem HCl Diltiazem Hydrochloride Dilthiazem hydrochloride monohydrochloride,cis-(+)-yl)-2-(4-methoxyphenyl) 1,5-benzothiazepin-4(5h)-one,2,3-dihydro-3-(acetyloxy)-5-(2-(dimethylamino)eth 2,3-dihydro-3-(acetyloxy)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-5-benzothiazepin-4(5h)-one (2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate (2S-cis)-3-acetoxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one monohydrochloride |
| CAS | 33286-22-5 |
| EINECS | 251-443-3 |
| InChI | InChI=1/C22H26N2O4S.ClH/c1-15(25)28-20-21(16-9-11-17(27-4)12-10-16)29-19-8-6-5-7-18(19)24(22(20)26)14-13-23(2)3;/h5-12,20-21H,13-14H2,1-4H3;1H/t20-,21+;/m1./s1 |
altiazem - Physico-chemical Properties
| Molecular Formula | C22H27ClN2O4S |
| Molar Mass | 450.98 |
| Density | 1.30 g/cm3 |
| Melting Point | 212-214°C |
| Boling Point | 594.4°C at 760 mmHg |
| Specific Rotation(α) | D24 +98.3 ± 1.4° (c = 1.002 in methanol) |
| Flash Point | 2℃ |
| Water Solubility | soluble |
| Solubility | Freely soluble in water, in methanol and in methylene chloride, slightly soluble in anhydrous ethanol. |
| Vapor Presure | 4.27E-14mmHg at 25°C |
| Appearance | Powder |
| Color | White to off-white |
| Merck | 13,3226 |
| BRN | 4228706 |
| PH | pH (10g/l, 25℃) : 4.3～5.3 |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| Refractive Index | 118 ° (C=1, H2O) |
| MDL | MFCD00069252 |
| Physical and Chemical Properties | White Crystal or crystalline powder. Melting Point 187-188 °c. Soluble in water, methanol, chloroform, insoluble in ethanol, insoluble in benzene. Odorless and bitter. |
| Use | Calcium channel blockers for the treatment of supraventricular arrhythmias, angina pectoris, hypertension in the elderly |
altiazem - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R40 - Limited evidence of a carcinogenic effect R36/37/38 - Irritating to eyes, respiratory system and skin. R36 - Irritating to the eyes R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S36 - Wear suitable protective clothing. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37 - Wear suitable protective clothing and gloves. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S16 - Keep away from sources of ignition. |
| UN IDs | 3249 |
| WGK Germany | 3 |
| RTECS | DL0310000 |
| FLUKA BRAND F CODES | 8-10 |
| HS Code | 29349990 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 in male, female mice, male, female rats (mg/kg): 61, 58, 38, 39 i.v.; 260, 280, 520, 550 s.c.; 740, 640, 560, 610 orally (Nagao, 1972) |
altiazem - Reference Information
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| hypertension drug | diltiazem hydrochloride is a more common hypertension drug, which belongs to the national medical insurance catalogue class B drug and is a prescription drug. Diltiazem is a benzothiazepine calcium channel blocker. It is the third generation of anti-angina drugs and the fourth generation of anti-arrhythmic drugs. It is mainly used for coronary heart disease, angina pectoris, and mild to moderate hypertension. It is especially suitable for hypertensive patients with coronary heart disease and angina pectoris. Xinhua Pharmaceuticals (Gaomi) Diltiazem Hydrochloride Tablets (30mg) is the first to pass the consistency evaluation of this variety. The original research of this variety is Tianbian Pharmaceutical Co., Ltd., which belongs to the original research and production varieties in China and has been designated as reference preparations. In addition, Shanghai Xinyi Vientiane Pharmaceutical also submitted a supplementary application for consistency evaluation. |
| Pharmacological effects | The effect of diltiazem is related to the inhibition of calcium influx during depolarization of myocardium and vascular smooth muscle; this product can effectively expand the epicardium and The coronary arteries under the endocardium relieve spontaneous angina pectoris or angina caused by coronary artery spasm induced by ergonovine; by slowing down the heart rate and lowering blood pressure, reducing myocardial oxygen demand, increasing exercise tolerance and relieving labor angina pectoris. The product can relax vascular smooth muscle, reduce peripheral vascular resistance, and reduce blood pressure. The magnitude of its blood pressure reduction is related to the degree of hypertension, and those with normal blood pressure only slightly reduce blood pressure. This product has a negative inotropic effect and can slow down the conduction of the sinoatrial node and atrioventricular node. |
| adverse reactions | edema, headache, nausea, dizziness, rash and weakness may occur at higher doses. |
| taboo | 1. patients with sick sinus syndrome without pacemaker. 2. II or III degree atrioventricular block without pacemaker. 3. systolic blood pressure is lower than 12kPa(90mmHg) and heart rate is lower than 50 beats/min. 4. Those who are allergic to this product. 5. Patients with congestive heart failure. |
| drug overdose | drug overdose can lead to bradycardia, hypotension, heart block and heart failure. At this time, the following treatments can be given according to the pharmacological effects and clinical experience of this product while removing this product through the gastrointestinal tract: 1. bradycardia: atropine 0.6~1mg is given, and isoprenaline can be used cautiously if it is ineffective. 2. High-level atrioventricular block: The treatment is the same as before. If there is continuous high-level atrioventricular block, pacemaker will be used for treatment. 3. Heart failure: use inotropic drugs (isoproterenol, dopamine, dobutamine) and diuretics. 4. Hypotension: Use vasopressors (such as dopamine or norepinephrine). |
| uses | calcium channel blockers are used for supraventricular arrhythmia, angina pectoris, hypertension in the elderly, etc. This product is a coronary artery dilator, effective for angina pectoris. It is used for the treatment of angina pectoris caused by sports colic and old myocardial infarction. The oral LD50 of this product is 640 mg/kg for female mice and 560 mg/kg for male mice. calcium channel blocker, used to treat supraventricular arrhythmia, angina pectoris, hypertension in the elderly, etc. |
| Production method | 2-(4-methoxyphenyl) -3-hydroxy-1, 5-benzothiaza-4 (5H)-one is condensed from 2-aminothiophenol and ethyl p-methoxyphenylepoxypropionate. After acylation, condensation with dimethylaminochloroethane, and salt formation, thiazepine is prepared. |
Last Update：2024-04-10 22:29:15
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