Rentibloc
Rentibloc Uses, Dosage, Side Effects, Food Interaction and all others data.
Rentibloc is a non-cardioselective beta-blocker. It increases sinus cycle length, slows heart rate, decreases AV nodal conduction and increases AV nodal refractoriness. It also prolongs AV monophasic action potentials. However, it lacks intrinsic sympathomimetic and membrane-stabilising properties.
Rentibloc is a competitive inhibitor of the rapid potassium channel. This inhibition lengthens the duration of action potentials and the refractory period in the atria and ventricles. The inhibition of rapid potassium channels is increases as heart rate decreases, which is why adverse effects like torsades de points is more likely to be seen at lower heart rates. L-sotalol also has beta adrenergic receptor blocking activity seen above plasma concentrations of 800ng/L. The beta blocking ability of sotalol further prolongs action potentials. D-sotalol does not have beta blocking activity but also reduces a patient's heart rate while standing or exercising. These actions combine to produce a negative inotropic effect that reduces the strength of contractility of muscle cells in the heart. Extension of the QT interval is also adversely associated with the induction of arrhythmia in patients.
Hyperglycemia is a greater risk for non insulin dependant diabetics than insulin dependant diabetics. Beta blockers inhibit insulin secretion which may cause hyperglycemia in type II diabetes mellitus. The risk of hypoglycemia is higher in insulin dependant diabetes than non insulin dependant diabetics. Beta blockers decrease secretion of insulin, which may mask hypoglycemia in an insulin dependant patient. Beta blockers also increase glucose uptake into cells which may prolong or potentiate hypoglycemia.
Further information regarding adverse reactions can be found here.
| Trade Name | Rentibloc |
| Availability | Prescription only |
| Generic | Sotalol |
| Sotalol Other Names | Sotalol, Sotalolo, Sotalolum |
| Related Drugs | propranolol, Xarelto, diltiazem, digoxin, rivaroxaban, flecainide, magnesium sulfate, propafenone, Multaq, esmolol |
| Type | |
| Formula | C12H20N2O3S |
| Weight | Average: 272.364 Monoisotopic: 272.119463206 |
| Protein binding | 0%. |
| Groups | Approved |
| Therapeutic Class | Anti adrenergic agent (Beta blockers) |
| Manufacturer | |
| Available Country | Germany |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Arrhythmias, Cardiac arrhythmias, Supraventricular and ventricular arrhythmias
Rentibloc is also used to associated treatment for these conditions: Atrial Fibrillation, Flutter, Atrial, Severe ventricular arrhythmias
How Rentibloc works
Rentibloc inhibits beta-1 adrenoceptors in the myocardium as well as rapid potassium channels to slow repolarization, lengthen the QT interval, and slow and shorten conduction of action potentials through the atria. The action of sotalol on beta adrenergic receptors lengthens the sinus node cycle, conduction time through the atrioventricular node, refractory period, and duration of action potentials.
Dosage
Rentibloc dosage
Oral (Adult)-
Supraventricular and ventricular arrhythmias: Initial: 80 mg/day in 1 -2 divided doses, increase gradually every 2-3 days. Usual: 160-320 mg/day in 2 divided doses. Max: 640 mg/day.
Life-threatening ventricular arrhythmias: 480-640 mg/day.
Acute arrhythmias: 20-120 mg, may repeat 6 hrly if needed.
For programmed electrical stimulation (to test antiarrhythmic efficacy): Initial: 1.5 mg/kg, then 0.2-0.5 mg/kg/hr infusion
Side Effects
Dyspnea, Dizziness, Fatigue, Bradycardia, Chest pain, Palpitation, Weakness, Lightheadedness, Nausea/vomiting, Edema, Headache, Sleep disturbances, Abnormal ECG, Diarrhea, Extremity pain, Hypotension, Mental confusion, Congestive heart failure, ltching/rash, Syncope, Anxiety, Depression, Torsades de pointes or new ventricular tachycardia / fibrillation in patients with supraventricular arrhythmia, Peripheral vascular disorders, Impotence, Proarrhythmic effect, Torsades de pointes with history of sustained ventricular tachycardia, Catechol hypersensitivity after abrupt withdrawal, Increased insulin requirement in diabetics
Toxicity
Patients experiencing an overdose may present with bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia. Larger intentional overdoses may present as hypotension, bradycardia, cardiac asystole, prolonged QT interval, torsade de pointes, ventricular tachycardia, and premature ventricular complexes. Stop administering sotalol and observe the patient until the QT interval returns to normal and the heart rate rises above 50 beats per minute. Hemodialysis may help lower plasma concentrations of sotalol as it is not bound to plasma proteins. Bradycardia and cardiac asystole may be treated with atropine, other anticholinergic drugs, beta adrenergic agonists, or transvenous cardiac pacing.. Second or third degree heart block may be treated with a transvenous cardiac pacemaker. Hypotension may be treated with epinephrine or norepinephrine. Bronchospasm may be treated with aminophylline or a beta-2 agonist, possibly at higher than normal doses. Torsade de pointes may be treated with DC cardioversion, transvenous cardiac pacing, epinephrine, or magnesium sulfate.
The oral LD50 for rats is 3450mg/kg, intraperitoneal LD50 for rats is 680mg/kg, oral LD50 for mice is 2600mg/kg, and intraperitoneal LD50 for mice is 670mg/kg.
Pregnant rabbits given 6 times the maximum recommended human dose showed an increase in fetal death and maternal toxicity, while rats given 18 times the maximum recommended human dose had an increased number of fetal resorptions. Rentibloc is present in human breast milk so patients taking sotalol should not breast feed.
Rentibloc has not been found to be carcinogenic. No studies have been performed regarding mutagenicity or clastogenicity. In animal studies, sotalol was not associated with a reduction in fertility aside from smaller litter sizes.
Further information regarding adverse reactions can be found here.
Precaution
Patients with well-compensated heart failure, myasthenia gravis, DM, 1 st degree AV block. May mask symptoms of hyperthyroidism and hypoglycaemia. May worsen psoriasis. Patients undergoing major surgery requiring general anaesth. Avoid abrupt withdrawal as it may precipitate thyroid storm and exacerbate angina and Ml. Renal impairment. Pregnancy and lactation. Monitoring Parameters Monitor BP, heart rate, serum creatinine; Mg and K levels.
Interaction
May increase risk of bradycardia with digoxin. May increase risk of arrhythmias with diuretics. May potentiate rebound HTN with clonidine. May prolong refractoriness with disopyramide, quinidine, procainamide, amiodarone and bepridil. May prolong QT interval with TCAs, phenothiazines, terfenadine and astemizole. Increased risk of torsades de pointes with K-depleting diuretics, erythromycin IV, halofantrine, pentamidine, and quinolones. May prolong neuromuscular blockade of tubocurarine. May reduce response to insulin and oral hypoglycaemics.
Food Interaction
- Take with or without food. Oral sotalol with a meal reduces absorption by 20%.
Rentibloc Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Rentibloc Cholesterol interaction
[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.
Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.
Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.
Rentibloc multivitamins interaction
[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.
The exact mechanism of interaction is unknown.
In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.
The elimination half-life increased by 44%.
Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.
However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.
The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.
It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.
Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.
Rentibloc Drug Interaction
Moderate: furosemide, alprazolamMinor: aspirin, aspirin, levothyroxineUnknown: ubiquinone, warfarin, rosuvastatin, apixaban, omega-3 polyunsaturated fatty acids, atorvastatin, metoprolol, esomeprazole, clopidogrel, dabigatran, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, rivaroxaban
Rentibloc Disease Interaction
Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hypersensitivity, ischemic heart disease, PVD, asthma/COPD, hemodialysis, QT interval prolongation, renal dysfunctionModerate: cerebrovascular insufficiency, glaucoma, hyperlipidemia, hyperthyroidism, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, Prinzmetal's variant angina
Volume of Distribution
The apparent volume of distribution is 1.2-2.4L/kg.
Elimination Route
Rentibloc is 90-100% bioavailable. When taken with a meal, adsorption is lowered by 18%. In patients with a creatinine clearance >80mL/min, the maximum concentration is 6.25±2.19.
Half Life
The terminal elimination half life is 10-20 hours in healthy patients. In patients with a creatinine clearance >80mL/min, the half life is 17.5±0.97h. In patients with a creatinine clearance 30-80mL/min, the half life is 22.7±6.4h. In patients with a creatinine clearance 10-30mL/min, the half life is 64±27.2h. In patients with a creatinine clearance 1
Clearance
In patients with a creatinine clearance >80mL/min, the plasma clearance is 6.78±2.72L/h and the renal clearance is 4.99±1.43L/h. In patients with a creatinine clearance 30-80mL/min, the plasma clearance is 2.74±0.53L/h and the renal clearance is 2.00±0.67L/h. In patients with a creatinine clearance 10-30mL/min, the plasma clearance is 1.56±0.44L/h and the renal clearance is 0.65±0.31L/h. In patients with a creatinine clearance 1
Elimination Route
80-90% of a given dose is excreted in the urine as unchanged sotalol. A small fraction of the doses is excreted in the feces as unchanged sotalol.
Pregnancy & Breastfeeding use
Pregnancy Category- D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Contraindication
Bronchial asthma or history of COPD, sick sinus syndrome, symptomatic sinus bradycardia, cardiogenic shock. 2nd and 3rd degree AV block, untreated phaeochromocytoma, torsades de pointes, congenital or acquired long QT syndromes, uncontrolled cardiac failure, cardiogenic shock, metabolic acidosis, hypotension, severe peripheral arterial disease, Raynaud's disease, anaesthesia that causes myocardial depression. Renal impairment (CrCI <10 mL/min). Concomitant use with Ca channel blockers (e.g. verapamil and diltiazem).
Innovators Monograph
You find simplified version here Rentibloc
Rentibloc contains Sotalol see full prescribing information from innovator Rentibloc Monograph, Rentibloc MSDS, Rentibloc FDA label
FAQ
What is Rentibloc used for?
Rentibloc is used to treat atrial fibrillation and other conditions that cause an irregular heartbeat. This medicine is only available on prescription. It comes as tablets.
How safe is Rentibloc?
Rentibloc is generally safe to take for a long time. In fact, it works best when you take it for a long time.
How safe is Rentibloc?
Rentibloc works by changing the way your body responds to some nerve impulses, especially in the heart. It slows down your heart rate and makes it easier for your heart to pump blood around your body.
What are the common side effects of Rentibloc?
Tiredness, slow heartbeat, and dizziness may occur. Less common side effects include headache, diarrhea, and decreased sexual ability. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Is Rentibloc safe during breastfeeding?
Rentibloc is not usually recommended in pregnancy.
Is Rentibloc safe during pregnancy?
Some authors recommend using Rentibloc during breastfeeding only while monitoring the infant closely for signs of beta-blockade. Infants over 2 months of age have more mature kidney function and are less likely to be affected by sotalol in milk.
Can I drink alcohol with Rentibloc?
Drinking alcohol can increase the risk of side effects with Rentibloc. It can make you feel dizzy or lightheaded. During the first few days of taking Rentibloc or after an increase in your dose, it's best to stop drinking alcohol until you see how the medicine affects you.
Can I drive after taking Rentibloc?
Rentibloc can cause drowsiness. Do not drive a car or operate dangerous machinery until you know how the medication affects you. Always have enough of this medication on hand.
When is the best time to take Rentibloc?
Rentibloc is usual to take Rentibloc once or twice a day. Your doctor may advise you to take your first dose before bedtime, because it can make you feel dizzy.
How long does it take for your body to adjust to Rentibloc?
If you are taking the medication twice daily, it will take between two and three days for Rentibloc to maintain a steady concentration in your blood.
Does Rentibloc help with anxiety?
A number of clinical trials have shown the effectiveness of beta-blockers such as Rentibloc in the relief of anxiety symptoms both in comparison to placebo and benzodiazepines.
Can I eat bananas while taking Rentibloc?
People taking beta-blockers should therefore avoid taking potassium supplements, or eating large quantities of fruit (e.g., bananas), unless directed to do so by their doctor.
Should Rentibloc be taken on an empty stomach?
Taking it at the same time each day will have the best effect. It will also help you remember when to take it. Take your medicine on an empty stomach, preferably 1 to 2 hours before meals.
Does Rentibloc affect sleep?
Sleep disorders occur in one to eight per cent of Rentibloc users.
How much does Rentibloc affect blood pressure?
The side effects that you have to be aware of is, since it's a beta blocker and blocks the adrenaline to the heart, it can slow your heart rate, and it's a blood pressure medicine. It actually can drop your blood pressure a little bit.
Can you take Rentibloc long term?
Rentibloc incidence of side effects are high, patients appear to tolerate long-term sotalol therapy well.
Does Rentibloc cause depression?
Rentibloc may causes depression also with other side effects.
Is Rentibloc a high risk medication?
Rentibloc can lower your heart rate or cause a 'heart block,' which can be very dangerous. People who have sick sinus syndrome shouldn't take this medication.
Does Rentibloc affect kidney function?
Rentibloc is a betablocker with additional antiarrythmic properties. Its pharmacokinetic properties may lead to increased serum levels of the drug in patients with reduced kidney function.
Who should not take Rentibloc?
You should not use Rentibloc if you have asthma, low potassium, or a serious heart condition such as severe heart failure, long QT syndrome, slow heartbeats that have caused you to faint, "sick sinus syndrome" or "AV block" (unless you have a pacemaker).
What happens if I miss a dose of Rentibloc?
Skip the missed dose and use your next dose at the regular time. Do not use two doses at one time.
Try not to miss any doses. Get your prescription refilled before you run out of medicine completely.
Can I overdose on Rentibloc?
Seek emergency medical attention. An overdose of sotalol can be fatal.
