tián ěr xīn
2 English Referencediltiazem hydrochloride
3 Tenarxin Instruction Manual 3.1 Name of the drugTenarxin
3.2 English NameDiltiazem
3.3 Diltiazem 3.4 Diltiazem hydrochloride 3.5 Diltiazem hydrochloride 3.3 Alias of Tenar XenicalTenazepam; Tenar Xenical? [1][Questionable] Alias for Tenerex; Thiazepinone; Thiaz? Ketone [1][challenge] Alias for Tenerexin; Hursin; Tildine; Diltiazem; Hoppexin; Hesinxin; Hazadrol; Haz? [1][QUESTION] Alias for Tenocardium; Urcon; Herbesser; Dilthiazem; Cardizem; CRD401
3.4 Classification
Circulatory Drugs > Antiarrhythmic Drugs > Calcium Channel Blockers
3.5 Dosage Forms1. (Hepcidin) 30mg, (Diltiazem) 30mg.
2. Extended-release tablets: (Tilden) 200mg.
3. Capsules: (Hebeishang) 90mg.
3.6 Pharmacological effects of TenaraxTenarax is a benzothiazide (phenothiazine) blocker. (phenothiazine) class of calcium antagonists, similar to the action of verapamil, through the inhibition of calcium current to make the 4-phase automatic depolarization slope decreased, inhibition of sinoatrial node and atrioventricular node autonomy, inhibition of atrioventricular node conduction, but no significant inhibition of the atrioventricular bypass. In addition, there are vasodilating effects and mild negative inotropic effects.
3.7 Pharmacokinetics of TenocinOral absorption is rapid and complete, and the absorption rate can be greater than 90% after prolonged administration, but the bioavailability is only about 45% due to the first-pass effect of the liver. After oral administration, the drug starts to take effect in 10~15min, Cmax is 1~2h, protein binding rate is 80%, and it is mainly distributed in various organs and tissues, such as heart, liver and kidney. After intravenous injection, the drug rapidly appeared in bile and gastrointestinal tract, indicating the existence of hepatic and intestinal circulation process. The half-life is 4-6h, 96%-99% is metabolized in the liver, and its metabolites are also active, 60% of the metabolites are excreted via feces and 40% via urine.
3.8 Indications for Tenocin1. Angina pectoris, including angina pectoris caused by coronary artery spasm or stenosis, such as resting angina pectoris, variant angina pectoris, or exertional angina pectoris.
2. Hypertension, either alone or in combination with other anti-hypertensive drugs.
3. Supraventricular tachyarrhythmias. Injections can be used to reverse paroxysmal supraventricular tachycardia, control ventricular rate in atrial fibrillation or atrial flutter.
4. Hypertrophic cardiomyopathy.
3.9 Contraindications to Tenocin1. Hypersensitivity to Tenocin or other calcium channel blocking agents.
2. Sick sinus syndrome, bradycardia due to second- or third-degree atrioventricular block and lack of effective artificial cardiac pacing.
3. Severe hypotension or cardiogenic shock.
4. Acute myocardial infarction with pulmonary congestion.
5. Intravenous administration is contraindicated in the presence of atrial fibrillation or atrial flutter in the presence of atrioventricular paraventricular tracts (e.g., WPW syndrome, LGL syndrome) or short PR syndrome.
6. Intravenous administration is contraindicated in ventricular tachycardia.
7. Injections containing benzyl alcohol are contraindicated in neonates.
8. Injectables are contraindicated in pregnant women.
3.10 Precautions1. (1) Congestive heart failure. (2) Left heart insufficiency in patients on beta-blockers. (3) Hypotension. (4) Hepatic or renal impairment. (5) Paroxysmal supraventricular tachycardia with caution with intravenous agents. (6) Intravenous preparations should be used with caution in atrioventricular block of the first degree. (7) Gastrointestinal motility increased or gastrointestinal obstruction with caution the use of slow-release agents.
2. The effect of drugs on the elderly: elderly patients should start with a low dose when using drugs.
3. The effect of the drug on breastfeeding: the effect of Tenocin on breastfeeding is still controversial, but Tenocin can be excreted from breast milk, and the concentration in breast milk is close to the blood concentration of the drug, so the use of Tenocin during breastfeeding is not recommended. Breastfeeding should be discontinued if the use of Tenocin is necessary in breastfeeding women.
4. Tenocin is metabolized in the liver and excreted by the kidneys and bile, long-term administration of the drug should be regularly monitored liver and kidney function. The use of injection should be continuous cardiac monitoring, frequent measurement of blood pressure, and should be equipped with cardioverter defibrillator and other emergency resuscitation equipment.
5. Dosage should be individualized. When taking the drug orally several times a day, it can be taken before meals or at bedtime, and the dose should be gradually increased every 1 to 2 days until a suitable effect is obtained. Discontinuation of the drug should be gradually reduced, can not suddenly stop the drug, to avoid hypertension rebound or angina pectoris.
6. Extended-release capsules should be swallowed whole, not separated, chewed or crushed.
7. The injection is dissolved in 5 ml of water for injection before use, and it is a clear colorless liquid after dissolution. If it is mixed with other agents with pH exceeding 8, it may precipitate crystals.
8. Before using injections to treat wide QRS wave tachycardia, it is important to carefully identify whether the tachycardia is ventricular or supraventricular with wide QRS waves.
9. Concomitant intravenous administration of Tenocardium with beta-blockers should be avoided. Beta-blocker injections should be given at least a few hours after the intravenous administration of phenazopyridine.
10. Skin reactions may be temporary and disappear with continued use of the drug, but the rash may progress to erythema multiforme and/or exfoliative dermatitis, and the drug should be discontinued if skin reactions persist.
11. Tenacin overdose can cause bradycardia, hypotension, conduction block and heart failure. Overdose reaction aggravation in addition to the application of gastrointestinal methods (such as gastric lavage, medicinal charcoal adsorption) to remove the exception, based on the pharmacological effects of Tenocardium and clinical experience, the following methods can be considered: (1) bradycardia: give atropine 0.6 ~ 1mg, if there is no vagal block reaction, can be careful to apply isoproterenol on the epinephrine. (2) High degree of AV block: place a pacemaker. (3) Heart failure: administer positive inotropic drugs (e.g., isoprenaline, dopamine, or dobutamine) and diuretics. (4) Hypotension: give antihypertensive drugs such as dopamine or norepinephrine.
3.11 Adverse reactions to TenaricinLess frequently, dizziness, headache, edema, flushing, insomnia, gastrointestinal discomfort, nausea, diarrhea, constipation, rash, bradyarrhythmia, sometimes atrioventricular block, upright hypotension, occasional hepatic damage (elevated GOT, GPT) and allergic reactions. Large doses administered intravenously can cause sinus bradycardia, sinus arrest, severe atrioventricular block and hypotension and other adverse reactions similar to verapamil.
3.12 Dosage and Administration of TenaricinHepcidol, ? to 2 tablets each time, 3 times a day; Hepcidol, 9 mg each time, 2 times a day; Tilden, 1 capsule each time, 1 time a day.
3.13 Drug InteractionsSynergistic effects may exist in combination with drugs that affect cardiac contraction and/or conduction, and the dose of Tilden should be carefully determined. Tenocin is biotransformed in vivo by cytochrome P450 oxidase, and combination with other drugs undergoing the same biotransformation pathway may result in competitive inhibition of metabolism; therefore, caution should be exercised in multi-drug therapy. When starting or discontinuing Tenocin, other drugs with the same metabolic pathway, especially those with a low therapeutic index, require dosage adjustments to maintain reasonable blood levels.
1. Tenocin may potentiate the effects of beta-blockers and may be beneficial in individuals with normal cardiac function. However, it may also cause hypotension, left heart failure and atrioventricular block. This is particularly likely to occur in the elderly, in patients with left heart insufficiency, and in patients with aortic stenosis. Tenormin may also increase plasma concentrations of beta-blockers metabolized by hepatic enzymes by approximately 30% to 40%. If combined, the patient's cardiac function should be carefully monitored and the dose of the drug should be adjusted.
2. Synergistic effect with antiarrhythmic drugs, such as amiodarone hydrochloride, methicillin hydrochloride, etc.. The combination can further slow down the sinus heart rate and aggravate atrioventricular block. Combination with quinidine may also enhance quinidine toxicity. Therefore, electrocardiogram and patient response should be monitored, and if there is any abnormality, the dosage should be reduced or discontinued.
3. *** Inhibition of myocardial contraction, conduction, autonomic and vasodilatory effects, and calcium channel blockers have a synergistic effect, so the dose of coadministration should be carefully determined.
4. Nitrates have the effect of enhancing antihypertensive effect, when used in combination, blood pressure should be measured and the dosage should be adjusted appropriately.
5. Cimetidine can inhibit cytochrome P450, so that the blood concentration and the area under the curve of Tenocin increased, and therefore need to adjust the dose of Tenocin. Ranitidine can also increase the blood concentration of Tenocin, but not significantly.
6. Aplindin hydrochloride and Tenocin can affect each other *** the same metabolizing enzyme, so that the blood concentration increases, the combination should be reduced or discontinued.
7. HIV protease inhibitors, such as ritonavir, saquinavir, etc., can inhibit the metabolism of tenacin, so that tenacin blood concentration increased. When applied at the same time, should reduce the dosage of Tenacin or stop the drug.
8. Tenocin can significantly increase the peak blood concentration of alfuzosin, enhance the antihypertensive effect. Calcium channel blockers should be avoided in combination with alfuzosin.
9. Tenocin can impede the metabolizing enzyme of dihydropyridine calcium channel blockers, such as nifedipine, and increase the blood concentration of dihydropyridine calcium channel blockers, therefore, clinical symptoms should be observed and the dosage should be reduced or discontinued when used concomitantly.
10. Tenocin can inhibit the metabolizing enzymes of the alkaloids, delay the metabolism of the alkaloids, and enhance the effect of the alkaloids. Clinical symptoms should be observed regularly and the dosage of the alkaloid should be reduced or discontinued if abnormalities are found.
11. Tenocin can inhibit the metabolizing enzymes of immunosuppressive drugs, such as tacrolimus, resulting in an increase in blood concentration. When used in combination, the dosage of immunosuppressive drugs should be reduced or discontinued if abnormalities are found.
12. Tenocin can inhibit the metabolism of carbamazepine, so that carbamazepine blood concentration increases. Combined use should pay attention to the manifestations of carbamazepine poisoning, such as drowsiness, nausea, vomiting, dizziness, etc., and should be regularly tested carbamazepine blood concentration, found abnormal, should be reduced or discontinued.
13. Timothy can inhibit the metabolism of phenytoin sodium, so that the blood concentration of phenytoin sodium increases, causing movement disorders, vertigo and other symptoms. When used in combination, clinical symptoms should be observed, and when abnormalities are found, the dosage should be reduced or discontinued.
14. Timolol can inhibit the metabolism of triazolam and midazolam, increasing their blood concentration and enhancing their effects. Therefore, if used in combination, triazolam or midazolam should start with a small dose, and regularly observe the clinical symptoms, and need to reduce or stop the drug when abnormalities are found.
15. Tenocin can enhance the effect of muscle relaxants, when used in combination, the dosage should be reduced or discontinued.
16. Tenocin can enhance the cholesterol-lowering effect of simvastatin, but the risk of myopathy and rhabdomyolysis increased. If combined, patients should be closely observed for symptoms of myalgia or weakness, and the serum creatine kinase (CK) value should be checked regularly. Once the CK value increases significantly, the drug should be discontinued when myopathy or rhabdomyolysis is suspected or diagnosed.
17. Alfentanil is metabolized by cytochrome P450, and Tenocin can prolong the half-life of alfentanil, and alfentanil toxicity should be monitored if combined.
18. The combination of Tenocin and aspirin can further inhibit ADP-induced platelet aggregation and prolong bleeding time.
19.Combination with NSAIDs or oral anticoagulants increases the risk of gastrointestinal bleeding.
20. Rifampicin can induce the metabolizing enzyme of Tenocin, which can decrease the blood concentration of Tenocin. At the same time, clinical symptoms should be observed, and if necessary, increase the dose of Pentoxifylline.
21. Ephedra contains ephedrine and pseudoephedrine, which can reduce the efficacy of antihypertensive drugs. Concomitant administration of ephedra preparations should be avoided in hypertensive patients treated with Tenocin.
22. Tenocin can increase digoxin blood levels by up to 20%, but no effect has been reported. Although the results are contradictory, digoxin blood levels should be monitored during initiation of Tenocin, dosage adjustment, or discontinuation of Tenocin in order to avoid overdose or underdose of digitalis.
3.14 Expert CommentaryExperimental evidence suggests that tenocardium increases subendocardial myocardial perfusion more than subepicardial myocardial perfusion. Therefore, in recent years, it has been reported that the use of tenocardial within 24-72h after myocardial infarction without Q-wave can help to prevent early reinfarction, but it is only beneficial to those who have normal left ventricular function after infarction, and on the contrary, it is harmful.
4 Tenor Heart ToxicityTenor Heart (Tenor Heartzine, Thiazepam, Diltiazem, Hazardzine, CRD401) is a new type of calcium antagonist. Similar to verapamil, it can be used to treat supraventricular arrhythmia, angina pectoris and hypertension in the elderly. Oral each time 30 ~ 60mg, 3 ~ 4 / d, the treatment of arrhythmia, angina pectoris; 120 ~ 240mg / d, divided into 3 ~ 4 oral, the treatment of hypertension patients. Oral absorption is complete, the effect occurs 15min after serving, 1 ~ 2h blood concentration peak, half-life of 4 ~ 5h, mainly metabolized by the liver, partially excreted by the gastrointestinal tract, and the remaining by the kidneys, long-term use of the drug can be accumulated, the smallest dose of human poisoning adults 420mg, the average of children for 5.7mg/kg, the oral LD50 in mice is 335.5mg/kg, via intravenous injection The LD50 of mice is 335.5mg/kg orally and 34.3/kg intravenously.
This drug mainly damages the digestive system (liver), heart and so on. [1]
4.1 Clinical manifestations[1]
1. Adverse reactions
Headache, dizziness, fatigue, bradycardia, gastric upset, lack of appetite, diarrhea, constipation, abdominal distension rash.
2. Poisoning manifestations
(1) Bradycardia, heart rate <40 beats/min, sinus arrest, III degree AV block.
(2) aggravate or induce cardiac insufficiency, heart failure, pulmonary edema can be fatal.
(3) Syncope, lethargy, convulsions, coma.
(4) Jaundice, hepatomegaly, elevated serum transaminases.
(5) Leukopenia, thrombocytopenia.
(6) Exfoliative dermatitis, pustular dermatitis.
4.2 TreatmentThe main points in the treatment of poisoning in Tenar are[2]:
1. In case of a large number of accidental doses, immediately induce vomiting, gastric lavage, and induce diarrhea.
2. 10% calcium chloride 10ml dextrose solution in 20ml, slow static injection, followed by every hour should be given 20 ~ 50mg/kg continuous static drip, in 30min after the drug and after every 2h measurement of blood calcium, so that the concentration of blood calcium to maintain at 2mmol / L.
3. Bradycardia or high degree of atrioventricular conduction block, the application of atropine, isoproterenol, the application of atropine, isopropyl epinephrine, and so on. If necessary, a temporary pacemaker can be installed.
4. Cardiac insufficiency, should limit the rate of infusion, can be applied to isoprenaline, dopamine, dobutamine and diuretics.
5. Hypotension, dopamine or norepinephrine, etc. can be given.