What is Propranolol?
Propranolol is used to treat arrhythmias caused by a variety of reasons, such as atrial and ventricular premature beats (good results), sinus and supraventricular tachycardia, atrial fibrillation, etc. Should be used with caution. Arrhythmia caused by antimony poisoning. When other drugs are not effective, try this product. In addition, it can also be used for angina pectoris, hypertension, pheochromocytoma (preoperative preparation), etc. When treating angina pectoris, it is often combined with nitrates. Can improve the efficacy and offset their adverse reactions. It has a certain effect on hypertension, and it is not easy to cause orthostatic hypotension.
- Drug type
- Essential medicines
- Drug name
- Propranolol
- English name
- Propranolol
- Chinese alias
- Naproxen; Enderol; Naphthyloxypropanolamine
- English alias
- Propranololum; AY-64043
- Propranolol is used to treat arrhythmias caused by a variety of reasons, such as atrial and ventricular premature beats (good results), sinus and supraventricular tachycardia, atrial fibrillation, etc. Should be used with caution. Arrhythmia caused by antimony poisoning. When other drugs are not effective, try this product. In addition, it can also be used for angina pectoris, hypertension, pheochromocytoma (preoperative preparation), etc. When treating angina pectoris, it is often combined with nitrates. Can improve the efficacy and offset their adverse reactions. It has a certain effect on hypertension, and it is not easy to cause orthostatic hypotension.
Introduction to propranolol compounds
Propranolol Basic Information
- Chinese name: Propranolol
- Chinese alias: 1-isopropylamino-3- (naphthalene-1-oxy) propan-2-ol; propranolol; naproxol; Inderal; AY-64043
- English name: Propranolol
- English alias: Disoprofol; 2-hydroxy-1,3-diisopropylbenzene; Fresofol; Diprivan; propofol
- CAS number: 525-66-6
- Molecular formula: C 16 H 21 NO 2
- Molecular weight: 259.34300
- Exact mass: 259.15700
- PSA: 41.49000
- LogP: 2.96840
Physical and chemical properties of propranolol
- Appearance and properties: white, odorless crystalline powder, usually its hydrochloride salt, is white or almost white crystalline powder; odorless, slightly sweet after bitter. Dissolved in water or ethanol, slightly soluble in chloroform.
- Density: 1.093 g / cm 3
- Melting point: 163-164ºC
- Boiling point: 434.9ºC at 760 mmHg
- Flash point: 216.8ºC
- Stability: stable to heat, unstable to light.
- Storage conditions: Keep in a dark, cool, dry and sealed container.
Propranolol Safety Information
- Customs code: 2922210000 [1]
Propranolol Pharmacopoeia Standard
- [Identification] (1) Take this product, make a solution containing 20 g per ml with methanol, and measure according to ultraviolet-visible spectrophotometry (Appendix IV A). It has maximum absorption at the wavelengths of 290 nm and 319 nm. (2) The infrared light absorption spectrum of this product should be consistent with the control spectrum (spectrum set 396). (3) Identification of chlorides in aqueous solution of this product (Appendix III).
- [Check] Take 0.10g of this product for acidity, 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. Clarity and color of the solution is taken as 1.0 g of this product. After dissolving in 20 ml of water, the solution should be clear and colorless; if color is developed, it should not be deeper than the yellow colorimetric standard color solution (Appendix A first method). Take 20mg of free naphthol, add ethanol and 2ml of 10% sodium hydroxide solution, shake to dissolve, add 1ml of diphenylbenzenesulfonic acid test solution, shake well, and let stand for 3 minutes; if it develops color, Comparing 0.30 ml of ethanol solution (containing -naphthol 20 g per 1 ml) with the same method, it must not be deeper (0.03%). Relevant substances are taken from this product, and the mobile phase is dissolved and diluted to make a solution containing about 1 mg per 1 ml as the test solution; a precise amount is taken, and the mobile phase is quantitatively diluted to make a solution containing about 2 g per 1 ml. As a control solution. Tested according to high performance liquid chromatography (Appendix VD). Use octadecylsilicon bonded silica gel as filler; use acetonitrile-water-sulfuric acid (55: 45: 0.1) mixed solution (take 1.6g of sodium dodecyl sulfate and 0.31g of tetrabutyl dihydrogen phosphate) It was dissolved in 1000ml of mixed solution, and the pH was adjusted to 3.3) with 2mol / L sodium hydroxide solution as the mobile phase; the detection wavelength was 292nm. Take 20l of the test solution and inject it into the liquid chromatograph. The retention time of propranolol hydrochloride peak is about 5 minutes. The theoretical number of plates based on propranolol hydrochloride peak is not less than 3000, and the tailing factor should not be greater than 2.0; Then take 20l of the control solution and inject it into the liquid chromatograph to adjust the detection sensitivity so that the peak height of the main component chromatographic peak is about 10% of the full scale. Precisely measure 20 l each of the test solution and the control solution, and inject them into the liquid chromatograph respectively. Record the chromatogram to 7 times the retention time of the main component chromatographic peak. If there is an impurity peak in the chromatogram of the test solution, the area of a single impurity peak must not be greater than 0.5 times (0.1%) the area of the main peak of the control solution; the sum of the area of each impurity peak must not be greater than 2 times (0.4%) of the main peak area of the control solution. Loss on drying: Take this product and dry to constant weight at 105 ° C. Lose weight should not exceed 0.5% (Appendix L). Ignition residue shall not exceed 0.1% (Appendix N).
- [Content determination] Take about 0.25g of this product, accurately weigh, add 40ml of acetic anhydride-glacial acetic acid (7 3) mixed solution to dissolve, according to potentiometric titration (Appendix A), use perchloric acid titration solution (0. lmol / L) titration, and the titration results were corrected with a blank test. Each 1ml of perchloric acid titration solution (0.1mol / L) is equivalent to 29.58mg of C16H 21N02 · HCl.
- [Category] Beta adrenergic blockers.
- [Storage] Keep sealed.
Propranolol Drug Description
Pharmacological effects of propranolol
- Propranolol is a non-selective 1 and 2 adrenergic blocker, which slows down heart rate, weakens myocardial contractility, reduces cardiac output, and initially increases reflexivity due to peripheral resistance (enhancing the effect of receptors relatively ), So the antihypertensive effect is not obvious, renal blood flow and glomerular filtration rate, coronary blood flow and other internal organs decreased. Propranolol can affect the function of adrenergic neurons, the sensitivity of the central nervous system's blood pressure regulating baroreceptors, and it can compete against the effects of isoproterenol and norepinephrine. Plasma renin and renin activity is reduced due to 2 receptor blockade, which can also cause vasoconstriction and bronchospasm. It has the effect of enhancing insulin and lowering blood sugar, and it also affects the combination of prostaglandin E2. It can be summarized as mild, slow, long-lasting, can inhibit renin secretion, and has no orthostatic hypotension. The mechanism for treating tremor may be related to 2 receptors, or it may be a central effect.
Pharmacokinetics of propranolol
- After oral administration, the gastrointestinal absorption is relatively complete, and the absorption rate is about 90%. The blood drug concentration reached its peak in 1 to 1.5 hours, but a large amount of it was inactivated by the liver before entering the systemic circulation, the bioavailability was 30%, and the bioavailability increased after eating. The plasma protein binding rate is 93%. The drug's ability to bind to plasma proteins is genetically controlled and has stereoselectivity. Its active isomer, l-pronaprolol, has a low level with 1 acid glycoprotein, so it is not bound in plasma. The ratio of propranolol is higher than that of Europeans, so the Chinese are more sensitive to propranolol. It is lipophilic and can produce a central response through the blood-cerebrospinal fluid barrier. Propranolol can also enter the placenta. The distribution volume is about 6L / kg. Propranolol is extensively metabolized in the liver, and drug metabolism and body clearance are increased in patients with hyperthyroidism. Propranolol has a half-life of 2 to 3 hours and is mainly excreted by the kidney, including most metabolites and a small portion (less than 1%) of the original. Propranolol can be secreted in small amounts from milk. Propranolol cannot be cleared by dialysis.
Propranolol indication
- It is used to treat arrhythmias caused by a variety of reasons, such as atrial and ventricular premature beats (good results), sinus and supraventricular tachycardia, atrial fibrillation, etc., but ventricular tachycardia should be used with caution. Arrhythmia caused by antimony poisoning. When other drugs are not effective, try this product. In addition, it can also be used for angina pectoris, hypertension, pheochromocytoma (preoperative preparation), etc. When treating angina pectoris, it is often combined with nitrates. Can improve the efficacy and offset their adverse reactions. It has a certain effect on hypertension, and it is not easy to cause orthostatic hypotension.
Propranolol usage and dosage
- Due to different dosage forms and specifications, please read the drug instructions carefully or follow the doctor's advice.
Propranolol adverse reactions
- 1. Sinus bradycardia, atrioventricular block, hypotension, induce and aggravate heart failure;
- 2. Others: Exacerbation of asthma and chronic obstructive pulmonary disease, depression, fatigue, hypoglycemia, and elevated blood lipids. Visible drowsiness, dizziness, insomnia, nausea, bloating, rash, syncope, hypotension, bradycardia, etc., should be noted.
- 3. Long-term heavy use can cause severe depression and even suicide attempts.
- 4. Aggravate the hypoglycemic effect of hypoglycemic agents and mask the symptoms of hypoglycemia.
Contraindications of propranolol
- (1) It can cause bronchospasm and vasoconstriction of the nasal mucosa, so it is contraindicated in patients with asthma and allergic rhinitis. (2) Disabled in patients with sinus bradycardia, severe atrioventricular block, cardiogenic shock, hypotension. (3) This product has the effect of increasing the toxicity of digitalis, and it is contraindicated in patients who have digitalis, the heart is enlarged, and the heart rate is not stable.
Caution with propranolol
- 1. (1) history of allergies; (2) congestive heart failure; (3) first degree atrioventricular block; (4) diabetes; (5) emphysema or non-allergic bronchitis; (6) liver function Incompleteness; (7) Hypothyroidism; (8) Raynaud's syndrome or other peripheral vascular disease; (9) Renal dysfunction; (10) Patients under anesthesia or surgery; (11) Pregnant and lactating women.
- 2. The elderly have low metabolism and excretion capacity of propranolol, and the dosage should be adjusted appropriately.
- 3. The effect of the drug on the test value or diagnosis: (1) can increase blood urea nitrogen, lipoprotein, creatinine, potassium, triacylglycerol, uric acid, etc .; (2) can reduce blood sugar, and may increase blood sugar in patients with diabetes (3) The metabolites of propranolol can accumulate in the blood during renal insufficiency and interfere with the diazonium reaction of serum bilirubin, and false positives can occur.
- 4. Blood routine, blood pressure, heart function, liver function, kidney function should be checked or monitored before, after and during medication. Diabetics should check their blood glucose regularly.
- 5. In the case of gastrointestinal bleeding, taking propranolol may increase the risk of circulatory failure.
- 6. Propranolol can be taken on an empty stomach or with food. Food can slow down propranolol metabolism in the liver and increase bioavailability.
- 7. The dosage must emphasize individualization, and the dosage varies from individual to individual and from disease to disease.
- 8. The concentration of propranolol in the blood cannot fully predict the pharmacological effects, so clinical medication should be guided according to clinical signs such as heart rate and blood pressure.
- 9. A small number of patients may develop heart failure with long-term medication. If it occurs, it can be corrected with digitalis and / or diuretics, and gradually decline to stop.
- 10. Patients with coronary heart disease should not stop propranolol suddenly, otherwise angina pectoris, myocardial infarction or ventricular tachycardia may occur. Sudden withdrawal of medication in patients with hypertension can cause a rebound in hypertension. Therefore, long-term drug users should gradually reduce their withdrawal, and at the same time should limit physical activity as much as possible.
- 11. Patients with hyperthyroidism should not stop propranolol suddenly, otherwise the symptoms of hyperthyroidism will be aggravated. Because propranolol can reduce cardiac contraction, when hyperthyroidism is associated with cardiac insufficiency, it should be combined with heart-strengthening drugs.
- 12. Whether to discontinue medication before surgery is controversial, because discontinuation of medication can cause angina pectoris and / or high blood pressure rebound, which may be more dangerous than the cardiac depression caused by the surgery itself. Propranolol should be gradually reduced before surgery, but do not stop the medicine completely until the surgery.
- 13. Intravenous administration can quickly control heart rate and myocardial contractility. Studies have shown that intravenous administration is better than oral administration within a few hours of the onset of myocardial infarction symptoms. After myocardial infarction, intravenous administration and then oral administration are better than one method alone.
- 14. Treatment of overdose: (1) give atropine or isoproterenol to bradycardia and install artificial pacemaker if necessary; (2) give lidocaine or phenytoin sodium to ventricular premature beats; (3) Heart failure is given oxygen, digitalis or diuretics; (4) infusion and hypotension in hypotension; (5) diazepam or phenytoin sodium; (6) bronchospasm to isoproterenol Adrenaline [2] .
Propranolol drug interactions
- 1. Quinidine can reduce the clearance of propranolol. If it must be used together, the heart function should be closely monitored, and the dosage of the two drugs should be adjusted if necessary.
- 2. Propafenone can increase the concentration of propranolol and cause a significant reduction in supine blood pressure. If it must be used together, the heart function, especially blood pressure, should be carefully monitored, and propranolol dosage should be adjusted if necessary.
- 3. Combined with amiodarone, obvious bradycardia and sinus arrest can occur. It can also cause bradycardia when used in combination with propionamine and flukanyl.
- 4. Combined with dihydropyridine calcium channel blockers, it is effective in treating angina pectoris or hypertension, but it can also cause severe hypotension or decreased heart reserve. Cardiac function should be carefully monitored in combination, especially for patients with impaired left ventricular function, arrhythmia, or aortic stenosis.
- 5. Diltiazem can enhance the pharmacological effects of beta-blockers and is beneficial to patients with normal cardiac function. However, it has also been reported to cause hypotension, left ventricular failure, and atrioventricular block after combined use. Therefore, cardiac function should be closely monitored when the two drugs are combined, especially when the elderly, left ventricular failure, aortic stenosis, and both drugs are used in large amounts.
- 6. Verapamil and propranolol have direct negative muscle strength and negative conduction, and combined use may cause hypotension, bradycardia, congestive heart failure, and conduction disorders. The risk increases with left ventricular dysfunction, aortic stenosis, or both doses. Therefore, cardiac function should be closely monitored when the two drugs are combined.
- 7. Combined with mibediril can cause hypotension, bradycardia or reduced heart reserve. Mbetidil should be discontinued for 7 to 14 days before starting beta blocker therapy. If combined, cardiac function should be monitored, especially in elderly patients with decreased left ventricular function, decreased cardiac conduction function, or aortic stenosis.
- 8. Although there is no report on the interaction between benzprodil, flunarizine, lidofloxazine, golopamide, peripoxiline, and propranolol, all of these drugs can reduce myocardial contraction and reduce Slow atrioventricular node conduction causes lower blood pressure, bradycardia, or decreased heart reserve. Therefore, if it must be used together, cardiac function should be monitored, especially in patients with decreased left ventricular function, decreased cardiac conduction function, or aortic stenosis.
- 9. Hydrazine can increase the bioavailability of propranolol, which is more common when taken on an empty stomach, but has less effect on sustained-release preparations.
- 10. Dexpropion may increase the risk of hypotension and bradycardia in propranolol. Pay attention to monitoring when combined.
- 11. Combined with oloflex, it can cause hypotension or hypertension with bradycardia. Patients' blood pressure and heart rate should be closely monitored.
- 12. During fentanyl anesthesia, the use of propranolol can cause severe hypotension.
- 13. Ritonavir can increase plasma concentration and toxicity of propranolol. When combined, the amount of propranolol should be reduced.
- 14. Zileuton can cause a significant increase in propranolol concentration. If it is used together, it should be closely monitored.
- 15. Cimetidine can reduce hepatic blood flow and liver metabolism of propranolol, which increases the concentration of propranolol in the blood. When combined use is needed, heart function such as blood pressure and heart rate should be closely monitored. If necessary, the dose should be adjusted.
- 16. Metoclopramide can enhance gastrointestinal motility and accelerate the absorption rate of propranolol, thus increasing the plasma concentration of propranolol.
- 17. Ciprofloxacin can increase propranolol concentration, causing hypotension and bradycardia. Combined use should monitor blood pressure and cardiac function.
- 18. Cyanoxetine can cause increased plasma concentration of propranolol and increased toxicity. Therefore, the toxicity of propranolol should be monitored and the dosage should be reduced if necessary.
- 19. With the use of chlorpromazine, the blood concentration of both can be increased.
- 20. Fluvoxamine can inhibit propranolol metabolism, resulting in bradycardia and / or hypotension. When combined, it is recommended to start with a small dose and monitor heart rate and blood pressure, or switch to a cardiac selective beta blocker.
- 21. Angelica sinensis extract may inhibit the metabolism of propranolol by liver cytochrome P450 enzymes. If used in combination, attention should be paid to monitoring blood pressure.
- 22. Furosemide can increase the plasma concentration of propranolol, which may be related to diuretic reduction of extracellular fluid.
- 23. With the use of hydrochlorothiazide, it can cause increased blood sugar, triacylglycerol and uric acid levels. Patients with diabetes or hyperlipidemia should avoid both drugs.
- 24. Combination with digoxin can lead to prolonged atrioventricular conduction time, and propranolol can increase the blood concentration of digoxin. Careful monitoring of the electrocardiogram and blood concentration of digoxin should be performed when combined, and the dose should be adjusted accordingly.
- 25. When combined with epinephrine, it can cause hypertension and bradycardia.
- 26. It can aggravate the first dose response of 1 blockers. With the exception of prazosin, other 1 blockers are rare, but caution should be exercised when used with propranolol.
- 27. Propranolol can increase the blood concentration of lidocaine. Monitoring should be taken when combined, and the lidocaine dose should be adjusted accordingly.
- 28. It can enhance the efficacy of non-depolarizing muscle relaxants, such as cyproteronine and goradomide, and prolong the action time.
- 29. When combined with propranolol and clonidine, sudden withdrawal of clonidine can make hypertension worse. Therefore, when withdrawing clonidine, propranolol should be removed first, blood pressure should be closely monitored, and clonidine should be gradually stopped after a few days. Caution should be taken when using Mosulidine in combination with sudden withdrawal of Mosulidine.
- 30. When combined with methyldopa. Very few patients have abnormal responses to endogenous or exogenous catecholamines, such as hypertension, tachycardia, or arrhythmia.
- 31. Used in combination with ergotamine, dihydroergotine, and mesergox, due to the enhanced vasoconstriction effect, it can cause peripheral ischemia or hypertension. Monitor closely or switch to a cardiac selective beta-blocker.
- 32. It can increase the bioavailability of rizatriptan.
- 33. Increase plasma concentration of imipramine.
- 34. It can reduce the metabolism of bromazepam and increase its toxicity.
- 35. Zomitriptan metabolism can be inhibited and its adverse reactions can be increased.
- 36. It can inhibit the metabolism of thioridazine and increase the toxicity of the latter. Due to the possibility of severe arrhythmia, the simultaneous use of the two drugs is strictly prohibited.
- 37. Used with warfarin, it increases the risk of bleeding.
- 38. Used with cocaine, it can increase vascular resistance and reduce coronary blood flow.
- 39. When propranolol is used with diatrizoate-based contrast agents, care should be taken to aggravate the latter's allergic reaction.
- 40. Antacids can reduce the bioavailability of propranolol and should be taken separately as much as possible.
- 41. Colestipol can reduce the bioavailability of propranolol and reduce the efficacy of propranolol. If combined, they should be taken separately and the dose adjusted if necessary.
- 42. Rifampicin and rifabutin can induce liver cytochromease, accelerate the metabolism of propranolol, and reduce the efficacy. If combined, the propranolol dose should be increased.
- 43. Phenobarbital or pentobarbital can induce liver microsomal enzyme system, which can reduce the plasma concentration, bioavailability and efficacy of propranolol. The efficacy should be monitored when combined, and if necessary, the dose should be adjusted, or another beta-blocker that does not rely on liver metabolism, such as atenolol and timolol, should be used.
- 44. Combination with non-steroidal anti-inflammatory drugs can cause blood pressure to rise. If combined, the patient's blood pressure should be monitored and the propranolol dose adjusted accordingly.
- 45. Ephedra contains ephedrine and pseudoephedrine, which can reduce the efficacy of antihypertensive drugs. Patients with hypertension treated with propranolol should avoid using ephedra-containing preparations.
- 46. Propranolol can affect blood glucose levels, so when used with hypoglycemic drugs, the dose of the latter must be adjusted, and blood glucose should be monitored, or a cardiac selective beta blocker should be used.
- 47. Propranolol can reduce the efficacy of isoprenaline or theophylline.
- 48. Beta-blockers can antagonize the effects of ritodrine, and the combination of propranolol and ritodrine should be avoided.
- 49. Propranolol and adenosine, amotriptan, benazepril, cilapril, cyanvastatin, dofetilide, finasteride, lansoprazole, omeprazole, rao There is no obvious interaction between Laxipan and others [2] .
Propranolol poisoning
- Propranolol (propranolol, naphthol, naphthyloxypropanolamine) is a beta adrenal blocker, mainly used for the treatment of various arrhythmias, angina pectoris, hypertension, hyperthyroidism control and pheochromocytoma Caused by fast heart rate, thyroid crisis, etc. have a certain effect. The drug is easily absorbed by oral administration, and its blood concentration reaches a peak within 1 to 2 hours after taking it, and its half-life is 3 to 6 hours. 10 to 30 mg orally, 3 to 4 / d, 5 mg each intravenously, 20 to 40 ml with 5% glucose solution, and 0.5 to 1 mg / min injection. If it is ineffective for 10 ~ 15min, repeat intramuscular injection once, the total amount should not exceed 10mg. Intravenous drip 5mg each time, 100% 5% glucose solution diluted, adjust the drip rate as needed. The human lethal blood plasma concentration ranged from 0.8% to 1.2%.
- Clinical manifestation
- Adverse reaction
- Such as bradycardia, hypotension, dizziness, headache, dry mouth, gastrointestinal discomfort, nausea, lack of appetite, rash, etc.
- 2. Poisoning performance
- (1) Cardiovascular system performance: Congestive heart failure, heart failure can occur suddenly or slowly, bradycardia, hypotension, and cardiac arrest.
- (2) Respiratory system performance: bronchospasm, asthma, cough, dyspnea, and tidal breathing.
- (3) Nervous system performance: burnout, weakness, insomnia or drowsiness, hearing impairment, paresthesia, etc.
- (4) Digestive system performance: abdominal pain, diarrhea, bloating, constipation, etc.
- (5) Hematological manifestations: thrombocytopenic purpura, agranulocytosis, and eosinophilia.
- treatment
- The main treatment points of propranolol poisoning are:
- 1. Discontinue the drug when there are adverse reactions or poisoning manifestations, lavage the stomach with lukewarm 0.45% saline, reduce diarrhea, and inject 10% glucose solution intravenously to promote the excretion of the drug from the body.
- 2. Bradycardia: intramuscular or intravenous injection of 0.5 to 1 mg of atropine; or slow intravenous infusion of 200 to 300 ml of 5% glucose solution with isoproterenol 0.5 to 1 mg. If it is ineffective, a pacemaker can be given.
- 3. Blood pressure drops given booster drugs.
- 4. Improve heart function, can use glucagon 0.5 ~ 1mg, intramuscular injection, subcutaneous injection or intravenous injection. Or 60% to 80ml of 50% glucose solution, intravenous injection.
- 5. Bronchial spasm, inhaling oxygen, giving aminophylline, scopolamine or isoproterenol.
- 6. Other symptomatic treatments [3] .
Propranolol
- Tablet: 10mg
- [4-7]
Propranolol Expert Reviews
- Patients with coronary heart disease and hyperthyroidism should not be stopped suddenly. Withdrawal of long-term propranolol should gradually reduce the dose, at least after 3 days, usually 2 weeks.
Propranolol tablets
- Propranolol hydrochloride tablets
- Indications: 1. As a secondary prevention, reduce the mortality of myocardial infarction.
- 2. Hypertension (alone or in combination with other antihypertensive drugs).
- 3. Labor-type angina pectoris.
- 4. Control supraventricular tachyarrhythmias, ventricular arrhythmias, especially those related to catecholamines or digitalis-induced arrhythmias. It can be used for the control of atrial flutter and atrial fibrillation ventricular rate with poor digitalis efficacy, and it can also be used for refractory premature contraction to improve patients' symptoms.
- 5. Reduce the differential pressure in the outflow tract of hypertrophic cardiomyopathy, and reduce the symptoms of angina pectoris, palpitations and syncope.
- 6. Combined with alpha blockers for tachycardia control in patients with pheochromocytoma.
- 7. Used to control the excessive heart rate of hyperthyroidism, can also be used to treat thyroid crisis.
- Dosage: 1. Hypertension: Oral, initial dose of 10mg, 3 to 4 times a day, can be used alone or in combination with diuretics. The dose should be gradually increased to a maximum daily dose of 200 mg.
- 2. Angina pectoris: 5 to 10 mg at the beginning, 3 to 4 times a day; 10 to 20 mg can be added every 3 days, and it can be gradually increased to 200 mg per day in divided doses.
- 3. Arrhythmia: 10 to 30 mg daily, 3 to 4 times daily. Take before meals and before bed.
- 4. Myocardial infarction: 30 to 240 mg daily, 2 to 3 times daily.
- 5. Hypertrophic cardiomyopathy: 10-20 mg, 3 to 4 times a day. Adjust the dose as needed and tolerated.
- 6. Pheochromocytoma: 10-20 mg, 3 to 4 times a day. For three days before surgery, alpha blockers should generally be used first, and propranolol should be added after the effect of the drug is stable.
- Dosage form: tablet
- Adverse reactions: Adverse reactions to the central nervous system such as dizziness, faintness (especially seen in the elderly), mental depression, and slow response; dizziness (caused by hypotension); slow heart rate (<50 times / minute) ; Rarely bronchospasm and dyspnea, congestive heart failure; Rarely fever and sore throat (granulocytosis), rash (allergic reaction), bleeding tendency (thrombocytopenia); When adverse reactions persist Special attention should be paid to cold limbs, diarrhea, burnout, dry eyes and skin, nausea, numbness of fingers and toes, and abnormal fatigue.
- Contraindications: 1. Bronchial asthma.
- 2. Cardiogenic shock.
- 3. Cardiac block (II-III degree AV block).
- 4. Severe or acute heart failure.
- 5. Sinus bradycardia.
- Precautions: 1. This product can be taken orally on an empty stomach or with food, which can delay metabolism in the liver and improve bioavailability.
- 2. The tolerance of -blockers varies widely, and the dosage must be individualized. When using this product for the first time, it is necessary to start with a small dose, gradually increase the dose and observe the response closely to avoid accidents.
- 3. Note that the blood concentration of this product cannot fully predict the pharmacological effects, so clinical medication should be guided according to clinical signs such as heart rate and blood pressure.
- 4. Patients with coronary heart disease should not use this product for sudden stop, otherwise angina pectoris, myocardial infarction or ventricular tachycardia may occur.
- 5. Patients with hyperthyroidism should not stop abruptly with this product, otherwise the symptoms of hyperthyroidism will be aggravated.
- 6. Long-term withdrawal of this product should gradually reduce the dose, at least after 3 days, usually 2 weeks.
- 7. Long-term application of this product can cause heart failure in a small number of patients. If it occurs, it can be corrected with digitalis and / or diuretics, and gradually reduce the dose, and finally stop using it.
- 8. This product can cause blood sugar reduction in diabetic patients, but non-diabetic patients have no hypoglycemic effect. Therefore, patients with diabetes should check blood glucose regularly.
- 9. Periodically check blood routine, blood pressure, heart function, liver and kidney function while taking this product.
- 10. Interference to diagnosis: When taking this product, the measurement of blood urea nitrogen, lipoprotein, creatinine, potassium, triglyceride, uric acid, etc. may be increased, and blood sugar will be reduced. But people with diabetes sometimes increase. Metabolites of this product can accumulate in the blood in patients with renal insufficiency, interfere with the determination of the diazonium response of serum bilirubin, and appear false positive.
- 11. Use this product with caution: history of allergies, congestive heart failure, diabetes, emphysema or non-allergic bronchial asthma, liver insufficiency, hypothyroidism, Raynaud's syndrome or other peripheral vascular disease, renal function decline, etc. .
- Ingredients: The main ingredient of this product is propranolol hydrochloride.
- Properties: This product is a white tablet.
- Medication for pregnant and lactating women: This product can enter the fetus through the placenta. It has been reported that those with high blood pressure during pregnancy can cause intrauterine fetal growth retardation, inability to cause dystocia during delivery, and newborns can produce hypotension, hypoglycemia, and respiratory depression. And heart rate slows down, although it has been reported that it has no effect on the mother and fetus, but it must be used with caution and should not be used as a first-line treatment for pregnant women. This product can be secreted from milk in small quantities, so it should be used with caution by lactating women.
- Medication for children: Not yet determined, generally 0.5 to 1.0 mg / kg daily by weight, orally in divided doses. Calculate the dosage for children based on body weight. The therapeutic range of this product is similar to that of adults. However, according to the body surface area of children, the therapeutic range of this product is higher than that of adults. It has been reported that when congenital stupid patients take this product, the blood concentration increases, thereby increasing bioavailability.
- Elderly medication: Due to the low metabolism and excretion ability of elderly patients, the dosage should be adjusted appropriately when using this product.
- Drug Interactions: 1. Interaction with antihypertensive drugs: This product combined with reserpine can cause orthostatic hypotension, bradycardia, dizziness, syncope. Combined with monoamine oxidase inhibitors, can cause extreme hypotension.
- 2. Combined with digitalis, atrioventricular block can occur and heart rate slows down. Close observation is required.
- 3. In combination with calcium antagonists, especially intravenous verapamil, be very vigilant against the inhibition of myocardium and the conduction system by this product.
- 4. Combination with epinephrine, phenylephrine or sympathomimetics can cause significant hypertension, slow heart rate, and atrioventricular block.
- 5. Combination with isoproterenol or xanthine can make the latter less effective.
- 6. Combination with haloperidol can cause hypotension and cardiac arrest.
- 7. Combination with aluminum hydroxide gel can reduce intestinal absorption of propranolol.
- 8. Alcohol can slow the absorption rate of this product.
- 9. Combined with phenytoin sodium, phenobarbital and rifampicin can speed up the removal of this product.
- 10. Combination with chlorpromazine can increase the blood concentration of both.
- 11. Combination with antipyrine, theophylline and lidocaine can reduce the clearance of this product.
- 12. Combination with thyroxine causes a decrease in T3 concentration.
- 13. Combination with cimetidine can reduce liver metabolism of this product, delay elimination, and increase plasma concentration of propranolol.
- 14. Can affect blood sugar levels, so when used with hypoglycemic drugs, the dose of the latter needs to be adjusted.
- Pharmacological effects: (1) Propranolol is a non-selective competitive inhibitor of epinephrine beta blockers. Block the 1 and 2 receptors on the heart, antagonize the sympathetic nerve excitation and catecholamine effect, reduce the contractile force and contraction speed of the heart, at the same time inhibit the contraction of vascular smooth muscle, reduce myocardial oxygen consumption, and make the oxygen supply and demand relationship of ischemic myocardium low Restores balance at the level and can be used to treat angina. (2) Adrenaline excitement that inhibits the cardiac pacing point potential is used to treat arrhythmias. This product can also be used in the treatment of hypertension by blocking the central and adrenergic neurons, inhibiting renin release, and reducing cardiac output. (3) Competitively antagonize the effects of isoproterenol and norepinephrine, block 2 receptors, and reduce plasma renin activity. Can cause bronchospasm. Inhibits insulin secretion, raises blood sugar, masks hypoglycemia symptoms, and delays the recovery of hypoglycemia. (4) It has obvious anti-platelet aggregation effect, which is mainly related to the drug's membrane stabilization effect and inhibition of platelet membrane Ca + -transport. 2. Carcinogenicity, mutagenicity, and reproductive toxicity Within 18 months, rats or mice were administered 150 mg / kg daily for 18 months. There was no significant toxic reaction and no drug-related carcinogenesis. Reproductive experiments showed no impaired fertility related to propranolol. When administered to animals at 10 times the dose for human use, this product shows embryo toxicity [8] .