What is the Recommended Atenolol Dosage?

Atenolol injection is indicated for acute myocardial infarction. Atenolol injection is suitable for hemodynamically stable patients with acute myocardial infarction to reduce the mortality of cardiovascular patients. Patients with a heart rate below 50 bpm, systolic blood pressure of less than 100 mmHg, or patients with other reasons who avoid the use of beta blockers are not suitable.

Drug Name: Atenolol injection
Drug type: prescription

Special medicine: Doping
Use classification: beta receptor blocker

Atenolol injection ingredients

The main ingredient of this product is atenolol. The chemical name of its main ingredient is: 4- [3-[(1-methylethyl) amino-2-hydroxy) propoxy] phenylacetamide. Chemical formula:

Molecular formula: C ₁₄ H ₂₂ N ₂ O ₃
Molecular weight: 266.34
The auxiliary materials are: sodium gasification, tartaric acid, and propylene glycol.

Atenolol injection properties

This product is a colorless clear liquid.

Atenolol injection indications

Acute myocardial infarction. Atenolol injection is suitable for hemodynamically stable patients with acute myocardial infarction to reduce the mortality of cardiovascular patients. Patients with a heart rate below 50 bpm, systolic blood pressure of less than 100 mmHg, or patients with other reasons who avoid the use of beta blockers are not suitable.

Atenolol injection specifications

10ml: 5mg

Atenolol injection dosage

When the patient is diagnosed or is about to be diagnosed with acute myocardial infarction, intravenous atenolol injection can be used for treatment. This product can only be treated in patients with coronary heart disease ward or similar ward if the patient is hemodynamically stable. Intravenous injection of 5mg was started slowly within 5 minutes, and 5mg was repeated after 10 minutes. The patient's blood pressure, rhythm, and electrocardiogram should be closely monitored during the injection. Dilution of atenolol injection: glucose injection or normal saline can be used.
Patients who can tolerate atenolol injection (10mg) intravenously should take atenolol tablets 50mg orally at 10min after injection, and then take 50mg after 12h; after that, take atenolol 100mg orally once a day or Take 50 mg twice daily for 6-9 days or until discharge from the hospital. If bradycardia, hypotension, or other side effects require treatment, atenolol tablets should be discontinued.
Results from studies with other beta-blockers indicate that if safety issues arise during the use of beta-blockers or contraindications in clinical evaluation, the drug should be discontinued immediately; patients who meet safety standards can be given altivar Lol tablets are given twice a day, 50 mg once or 100 mg once, for at least 7 days (excluding the intravenous dose).
Medication for patients with renal insufficiency: Since atenolol is metabolized by the kidneys, the dose should be adjusted for patients with severe renal insufficiency. When the rate of creatinine elimination drops to 35ml / min / 1.73m ² , atenolol appears clearly. Accumulation (normal range is 100-150ml / min / 1.73m ² ), so the maximum recommended oral dose for patients with renal insufficiency is as follows:
Creatinine elimination rate (ml / min / 1.73) Atenolol elimination half-life (h) Maximum dose 15-35 16-27 50mg per day
<15]> 27 50mg every other day
Patients undergoing hemodialysis should be given 50 mg of atenolol after each dialysis session. Patients' blood pressure should be closely monitored in the hospital after administration.

Adverse reactions of atenolol injection

Most side effects are mild and temporary.
Acute myocardial infarction: A series of studies have shown that atenolol, like other beta-blockers, is more commonly used for bradycardia and hypotension in the treatment of acute myocardial infarction than in the control group, but atropine is usually used or atenolol is discontinued. You can improve. Atenolol does not increase the incidence of heart failure and rarely uses positive inotropic drugs. The chances of such side effects in the study are shown in the table below:

The following adverse reactions occurred when intravenous and / or oral atenolol was administered to 477 patients:
In a subsequent international study on infarct survival (ISIS-I), there were 16,000 patients, of which 8037 were voluntarily treated with atenolol injection. The intravenous / oral atenolol was discontinued or reduced for the following reasons: the amount.

According to the previous market experience of atenolol injection, the following conditions are temporarily related to medication: increased liver enzymes or bilirubin, hallucinations, headaches, impotence, Peynie's disease, orthostatic hypotension are usually accompanied by syncope, psoriasis Symptoms, exacerbation of psoriasis, psychosis, purpura, reversible hair loss, thrombocytopenia, visual impairment, sick sinus syndrome, dry mouth, etc. Like other beta-blockers, atenolol is associated with antinuclear antibodies, lupus syndrome, and Raynaud's phenomenon.
Possible side effects The side effects of other beta-blockers are also possible side effects of atenolol injection.
Hematological disorders: Granulocytic allergic reactions: fever, with body pain, sore throat, sore throat, and respiratory pain.
Central nervous system: reversible central nervous system depression can lead to tension: acute syndrome with disorientation of time and place; short-term memory loss; emotional instability with mild central sensory system disturbance; impaired function in neuropsychological testing .
Gastrointestinal tract: mesenteric arterial thrombosis, ischemic colitis, others: mixed erythema erythematosus: due to the use of beta receptor blockers, there have been reports of skin rashes and dry eyes, and they are reported to be less likely And in most cases the symptoms disappear after the treatment is over. When these symptoms cannot be explained by other reasons, the administration should be stopped immediately and closely monitored (see Dosage and Administration).
Ocular mucosa syndrome with beta-blocker propranolol did not occur with atenolol injection. In addition, some patients who had taken Xindering with obvious above-mentioned side effects switched to atenolol injection and their symptoms disappeared or the reaction stopped.

Atenolol injection contraindications

Sinus bradycardia, - degree cardiac block, cardiogenic shock, and significant heart failure. Patients who are allergic to atenolol or any component of this product are contraindicated.

Precautions for atenolol injection

1. Heart failure sympathetic nerve excitement is necessary to support circulatory function during congestive heart failure. Beta blockers have the potential to further inhibit myocardial contraction and cause more severe failure. Atenolol injection should be used with caution in patients with congestive heart failure treated with digitalis and diuretics. Both digitalis and atenolol can slow atrioventricular conduction.
In patients with acute myocardial infarction, if intravenous furosemide 80mg or equivalent treatment cannot be controlled, it is a contraindication to beta blocker treatment.
2. Patients without a history of heart failure may use -blockers to inhibit the heart muscle for a period of time, which may lead to heart failure. Once a patient develops symptoms of heart failure, the patient is required to receive existing recommended therapies and his response needs to be closely monitored. If the symptoms of heart failure cannot be controlled after adequate treatment is given, the intravenous injection of atenolol should be stopped (see Dosage and Administration).
3. Stop using atenolol. Patients with coronary artery disease should avoid abrupt withdrawal when using atenolol. The abrupt discontinuation of beta blockers leading to severe worsening angina pectoris and myocardial infarction and ventricular arrhythmias has been reported in patients with coronary artery disease. The latter two complications may occur with or without prior exacerbation of angina. As with other beta blockers, discontinuation of atenolol is planned, and patients should be closely monitored and minimized physical activity. If angina pectoris worsens or coronary dysfunction develops, then atenolol should be continued immediately, at least temporarily, because coronary artery disease is common and may not be diagnosed. Sudden discontinuation of atenolol should be used with caution even if the patient is being treated for hypertension alone (see Dosage and Administration).
4. Taking calcium channel blockers at the same time Taking calcium channel blockers such as verapamil or diltiazem may cause bradycardia and cardiac conduction block, and the diastolic pressure of the left ventricle may increase. Special attention should be paid to congenital heart conduction defects and ventricular dysfunction.
5. Bronchial spasm Patients with bronchospasm generally cannot use -blockers, but atenolol injection has a certain selectivity, so patients with bronchial asthma and no allergic reactions or other anti-cancer Patients with hypertension can use atenolol under doctor's order. Because of its incomplete selection of beta receptors, the initial therapeutic dose of atenolol is set at 50 mg and a beta ₂ agonist must be available as a backup bronchodilator. If it is necessary to increase the dose, multiple small doses can reach its smaller peak blood concentration.
6. Anesthesia and major surgery can not stop the use of -adrenergic receptors for most patients before surgery. Special care should be taken when using anesthetics that inhibit myocardium. If vagus nerve excitement occurs, 1-2mg of atropine can be given intravenously.
Similar to other beta blockers, atenolol has a strong competitive inhibitory effect on beta receptors. Taking the following drugs can reverse its effects on the heart, such as dobutamine or isoprenaline.
7. Diabetes and hypoglycemia patients should pay special attention when using atenolol. Beta receptor inhibitors may mask the symptoms of tachycardia in patients with hypoglycemia, but have no obvious effect on other symptoms such as dizziness and sweating. Atenolol at the recommended dose does not enhance insulin-induced hypoglycemia, and unlike other non-selective beta-blockers, it does not delay the return of blood glucose levels to normal levels.
8. Hyperthyroidism -adrenergic blockers may mask some clinical symptoms of hyperthyroidism, and patients with suspected thyroid disease should be closely monitored when intravenous atenolol is administered. Sudden discontinuation of beta blockers can lead to thyroid crisis, so patients who may be at risk of thyroid crisis should be closely monitored during the atenolol discontinuation process.
9. Patients with uncured pheochromocytoma should not receive atenolol intravenously.
10. Impaired renal function: Patients with impaired renal function should pay attention when taking this medicine (see Dosage and Administration for details).
11. Allergic reactions: Patients with a history of allergies may experience a more severe immune response when using beta blockers, which may be accidental, diagnostic or therapeutic. Such patients may have an allergic reaction to treatment. The regular dose of epinephrine did not respond.

Atenolol injection for pregnant and lactating women

Attenolol in pregnant women can cause harm to the fetus. Atenolol can enter the cord blood through the placental barrier. Atenolol has been shown to cause premature birth in infants during birth and pregnancy from April to June. There are no studies using atenolol during the first trimester of pregnancy, so the possibility of fetal injury cannot be ruled out. If the patient uses the drug during pregnancy or if she becomes pregnant while taking the drug, the potential danger to the fetus should be reported.
Atenolol is excreted in breast milk and its plasma concentration is 1.5-6.8. It should be used with caution in lactating women. Breastfeeding infants have been reported to cause significant bradycardia. Premature babies or infants with impaired renal function may be more susceptible to adverse reactions. Infants whose mothers take atenolol during childbirth or breastfeeding may be at risk of hypoglycemia and bradycardia. Pregnant women and lactating women should pay attention to this.

Atenolol injection for children

The safety and effectiveness of medications for children have not been established.

Atenolol injection for the elderly

The clinical trial of atenolol injection did not include enough elderly subjects aged 65 years and older, so it is not possible to determine whether the response of the elderly to this drug is different from that of young subjects. Other reported clinical trials have not identified significant differences in efficacy and safety between older patients and younger patients, but are less favorable for older patients with systolic blood pressure <120mmHg. Taking into account the weakness of the heart, liver and kidney of elderly patients, may also suffer from other complications and be treated with other drugs at the same time, in general, the dosage of elderly patients should be carefully selected, usually starting from the smallest dose in the range use. Patients with hypotension and myocardial infarction are usually examined for renal function, and atenolol's metabolic capacity decreases with age.

Atenolol injection drug interactions

Catecholamine depletion drugs (eg, reserpine) may produce synergistic effects when used concurrently with beta blockers. Atenolol combined with catecholamine depletion drugs may cause dizziness, syncope, or orthostatic hypotension, and patients should be closely monitored for hypotension or significant bradycardia.
The combination of atenolol and thiazide diuretics has a hypotensive effect.
Beta-blockers may increase blood pressure rebound after clonidine is discontinued. If the two drugs are combined, beta-blockers should be discontinued for a few days before clonidine is gradually discontinued. If clonidine is replaced with a beta-blocker, start taking beta-blocker a few days after clonidine is discontinued.
Calcium channel inhibitors may also have a synergistic effect with atenolol. Beta-receptor inhibitors in combination with verapamil and diltiazem may exhibit bradycardia, cardiac depression, and increased left ventricular end diastolic blood pressure.
Combination with prostaglandin synthase inhibitor drugs (such as indomethacin) may reduce beta blockers and cause hypotension.
It should be noted when intravenous atenolol is combined with drugs that inhibit myocardial contraction. In rare cases, intravenous -blockers and verapamil can cause serious side effects, especially for patients with severe myocardium. Patients with disease, congestive heart failure, or recent myocardial infarction.
Information on the combination of atenolol and aspirin is very limited. Several clinical trials such as TIMI-II and ISIS-2 have not yet proven that aspirin and beta-blockers interact in acute myocardial infarction.

Atenolol injection overdose

It is reported that patients can survive when taking atenolol in excess of 5 g. One patient died as a result of taking up to 10 g. Prominent symptoms when taking atenolol overdose are drowsiness, respiratory motility disorders, asthma, and intermittent sinus bradycardia. In addition, common adverse reactions using -blockers and possible adverse reactions when using atenolol are: congestive heart dysfunction, hypotension, bronchospasm and / or hypoglycemia. The treatment of overdose is mainly through the induction of vomiting, gastric lavage and the use of activated carbon to remove unabsorbed drugs. Atenolol can be removed from the bloodstream by hemodialysis. Other treatment options should be carefully considered by the doctor, mainly including: bradycardia: intravenous atropine. If there is no response to vagus nerve suppression, use isoproterenol or a venous pacemaker. Heart block (second or third degree): isoprenaline or pacemaker. Heart failure: use digitalis or diuretics. Glucagon has also been reported to be useful. Hypotension: Booster drugs such as dopamine or norepinephrine. Continuous control of blood pressure. Bronchial spasm: Give beta ₂ receptor agonists, such as isoprenaline, terbutaline and / or aminophylline. Hypoglycemia: Intravenous glucose. Given the severity of symptoms, treatment requires intensive care support and equipment that provides cardiovascular and respiratory support

Atenolol injection pharmacology and toxicology

It is a selective 1 adrenergic receptor blocker without membrane stabilization and endogenous sympathomimetic activity. But does not inhibit the bronchiectasis of isoproterenol. Its mechanism of lowering blood pressure and reducing myocardial oxygen consumption is the same as that of propranolol. High doses can also inhibit ₂ receptors in vascular and bronchial smooth muscle. Large-scale clinical trials have confirmed that atenolol can reduce mortality from 0 to 7 days in acute myocardial infarction. The treatment dose did not significantly inhibit myocardial contractility.
Animal Toxicology: Studies of long-term oral atenolol in animals have shown that duodenum of female and male dogs are duodenal at all tested doses (from 12 mg / kg / day or 7.5 times the maximum recommended anti-hypertensive dose in humans). Veinization of duodenal gland epithelial cells. A dose of 300 mg / kg / day instead of 150 mg / kg / day (150 and 75 times the maximum recommended dose for human antihypertensive drugs) can increase the incidence of cardiac anterior chamber degeneration in male rats. The maximum dose for a patient based on 50 kg is 100 mg / day.
Carcinogenic, mutant and reproductive toxicity in two long-term tests in rats (maximum dose, 18 and 24 months) and one long-term test in mice (maximum dose, 18 months), the applied doses are all higher than 300mg / kg / day or human resistance The recommended maximum dose of hypertension is 150 times, which does not show that atenolol is potentially carcinogenic. The other three rat trials (24 months) applied doses of 500 and 1500 mg / kg / day (250 and 750 times the recommended maximum dose of human antihypertensive drugs), benign adrenal medullary tumors in females and males, and female breast fibers. The incidence of adenoma and male thyroid medullary carcinoma is increasing. No major lethal test (mouse), in vivo cytogenetic test (Chinese voles) or Ames test (S typhoid fever virus) did not find that atenolol has the potential to induce mutations. Atenolol does not affect females or males. Fertility in rats (dose higher than 200 mg / kg / day or 100 times the maximum recommended human antihypertensive dose).

Pharmacokinetics of atenolol injection

Oral absorption is rapid, but incomplete. The oral absorption rate is about 50%, and most of it is excreted from the urine in its original form. The peak time of blood concentration is about 2 to 4 hours. Almost without liver metabolism, the absorbed part is mainly eliminated by renal excretion. 85% of the injected dose is excreted in the urine within 24 hours, while oral administration is about 50%. Its plasma protein binding rate is extremely low (6% to 16%).
The elimination half-life of oral atenolol is about 6-7 hours, and its kinetic characteristics do not change after long-term administration. Peak blood concentration was reached 5 minutes after intravenous injection. The peak decreases rapidly (5-10 times) during the first 7 hours, so its elimination half-life is the same as oral administration. Oral administration of 50mg or 100mg, -blocker effect and antihypertensive effect can be maintained for at least 24 hours. When renal function is impaired, the elimination of atenolol is closely related to glomerular filtration. If creatinine clearance is less than 15ml / (min.1.73m ² ), serious accumulation will occur.

Atenolol injection storage

Protected from light and sealed.

Atenolol injection packaging

Ampoules. 1 stick / box, 2 sticks / box.

Validity of atenolol injection

24 months

Atenolol injection standard

YBH05562009 ^[1]