Generic name: Metazero SUCCINATE 25mg
Dosage form: capsule, extended release
Medically reviewed on June 19, 2018.
Adults: The usual initial dosage is 25 mg to 100 mg once daily in a single dose. Adjust dosage at weekly (or longer) intervals until optimum blood pressure reduction is achieved. Dosages above 400 mg per day have not been studied.
Pediatric Hypertensive Patients 6 Years of age or older: The recommended starting dose of Metazero is 1 mg/kg once daily, the maximum initial dose should not exceed 50 mg once daily. Adjust dosage according to blood pressure response. Doses above 2 mg/kg (or in excess of 200 mg) once daily have not been studied in pediatric patients.
Metazero has not been studied in pediatric patients less than 6 years of age.
Individualize the dosage of Metazero. The usual initial dosage is 100 mg once daily, given in a single dose. Gradually increase the dosage at weekly intervals until optimum clinical response has been obtained or there is a pronounced slowing of the heart rate. Dosages above 400 mg per day have not been studied. If treatment is to be discontinued, reduce the dosage gradually over a period of 1 to 2 weeks.
Prior to initiation of Metazero, stabilize the dose of other heart failure drug therapy and ensure that the patient is not fluid overloaded. The recommended starting dose of Metazero is 25 mg once daily for two weeks. Metazero is not suitable for initial therapy in patients who are expected to require a starting dose less than 25 mg daily. Dosage must be individualized and closely monitored during up-titration. Double the dose every two weeks to the highest dosage level tolerated by the patient or up to 200 mg of Metazero. If a patient experiences symptomatic bradycardia, reduce the dose of Metazero. If transient worsening of heart failure occurs, consider treating with increased doses of diuretics, lowering the dose of Metazero or temporarily discontinuing it. The dose of Metazero should not be increased until symptoms of worsening heart failure have been stabilized. Initial difficulty with titration should not preclude later attempts to introduce Metazero.
For patients who are taking Metazero succinate extended-release tablets at a dose of 25 mg to 200 mg once daily, substitute Metazero for Metazero succinate extended-release tablets, using the same total daily dose of Metazero succinate.
Metazero should be swallowed whole. For patients unable to swallow an intact capsule, alternative administration options are available.
Directions for use with soft food (applesauce, pudding, or yogurt)
For patients with swallowing difficulty, Metazero can be opened and contents can be sprinkled over soft food. The contents of the capsules should be swallowed along with a small amount (teaspoonful) of soft food (such as applesauce, pudding, or yogurt). The drug/food mixture should be swallowed within 60 minutes and not stored for future use.
Nasogastric tube administration
Open and add contents of capsule to an all plastic oral tip syringe and add 15 mL of water. Gently shake the syringe for approximately 10 seconds. Promptly deliver through a 12 French or larger nasogastric tube. Ensure no granules are left in the syringe. Rinse with additional water if needed.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Other brands: Metazero Tartrate, Metazero Succinate ER, Lopressor, Toprol-XL
Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Metazero, especially:
an antidepressant - bupropion, clomipramine, desipramine, duloxetine, fluoxetine, fluvoxamine, paroxetine, sertraline;
an ergot medicine - dihydroergotamine, ergonovine, ergotamine, methylergonovine;
heart or blood pressure medications - amlodipine, clonidine, digoxin, diltiazem, dipyridamole, hydralazine, methyldopa, nifedipine, quinidine, reserpine, verapamil, and others;
a MAO inhibitor - isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, tranylcypromine; or
medicine to treat mental illness - chlorpromazine, fluphenazine haloperidol, thioridazine.
This list is not complete. Other drugs may interact with Metazero, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.
Metazero is a CYP2D6 substrate. Drugs that inhibit CYP2D6 can have an effect on the plasma concentration of Metazero. Examples of drugs that inhibit CYP2D6 are quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenon and diphenhydramine. When treatment with these drugs are initiated, the dose of Metazero might have to be reduced for patients treated with Metazero.
The Following Combinations with Metazero Should be Avoided: Barbituric Acid Derivatives: Barbiturates (investigated for pentobarbital) induce the metabolism of Metazero by enzyme induction.
Propafenone: Upon administration of propafenone to 4 patients on Metazero therapy, the plasma concentrations of Metazero increased by 2-5 fold and 2 patients experienced side effects typical of Metazero. The interaction was confirmed in 8 healthy volunteers. The interaction is probably explained by the fact that propafenone, similarly to quinidine, inhibits the metabolism of Metazero via cytochrome P450 2D6. The combination is probably difficult to handle since propafenone also has beta-receptor blocking properties.
Verapamil: In combination with beta-receptor blocking drugs (described for atenolol, propranolol and pindolol), verapamil may cause bradycardia and fall in blood pressure.
Verapamil and beta-blockers have additive inhibitory effects on AV-conduction and sinusnode function.
The Following Combinations with Metazero may require Modified Drug Dosage:
Dosage:Amiodarone: A case report suggests that patients treated with amiodarone may developed pronounced sinus bradycardia when treated simultaneously with Metazero. Amiodarone has extremely long half-life (around 50 days), which implies that interactions can occur for a long time after withdrawal of the drug.
Antiarrhythmics, Class I: Class I antiarrhythmics and beta-receptor blocking drugs have additive negative inotropic effects which may result in serious haemodynamic side effects in patients with impaired left ventricular function. The combination should also be avoided in "sick sinus syndrome" and pathological AV-conduction. The interaction is best documented for disopyramide.
Nonsteroidal Anti-Inflammatory/Antirheumatic Drugs (NSAIDs): NSAID-antiphlogistics have been shown to counteract the antihypertensive effect of beta-receptor blocking drugs. Primarily, indomethacin has been studied. This interaction probably does not occur with sulindac. A negative interaction study on diclofenac has been performed.
Diphenhydramine: Diphenhydramine decreases (2.5 times) clearance of Metazero to alpha-hydroximetoprolol via CYP2D6 in fast hydroxylating persons. The effects of Metazero are enhanced. Diphenhydramine may probably inhibit the metabolism of other CYP2D6 substrates.
Digitalis Glycosides: Digitalis glycosides in association with beta-blockers, may increase AV conduction time and may induce bradycardia.
Diltiazem: Diltiazem and beta-receptor blockers have additive inhibitory effects on the AV-conduction and sinusnode function. Pronounced bradycardia has been observed (case reports) during combination treatment with diltiazem.
Epinephrine: There are about 10 reports on patients treated with nonselective beta-receptor blockers (including pindolol and propranolol) that developed pronounced hypertension and bradycardia after administration of epinephrine (adrenaline). These clinical observations have been confirmed in studies in healthy volunteers. It has also been suggested that epinephrine in local anaesthetics may provoke these reactions upon intravasal administration. The risk is probably less with cardioselective beta-receptor blockers.
Phenylpropanolamine: Phenylpropanolamine (norephedrine) in single doses of 50 mg may increase the diastolic blood pressure to pathological values in healthy volunteers. Propranolol generally counteracts the rise in blood pressure induced by phenylpropanolamine. However, beta-receptor blockers may provoke paradoxical hypertensive reactions in patients who take high doses of phenylpropranolamine. Hypertensive crisis during treatment with only phenylpropanolamine have been described in a couple of cases.
Quinidine: Quinidine inhibits the metabolism of Metazero in so-called rapid hydroxylators (>90% in Sweden) with markedly elevated plasma levels and enhanced beta-blockade as a result. A corresponding interaction might occur with other beta-blockers metabolised by the same enzyme (cytochrome P450 2D6).
Clonidine: The hypertensive reaction when clonidine is suddenly withdrawn may be potentiated by beta-blockers. If concomitant treatment with clonidine is to be discontinued, the beta-blocker medication should be withdrawn several days before clonidine.
Rifampicin: Rifampicin may induce the metabolism of Metazero resulting in decreased plasma levels.
Patients receiving concomitant treatment with other beta-blockers (ie, eye drops) or MAO Inhibitors should be kept under close surveillance. In patients receiving beta-receptor blocker therapy, inhalation anaesthetics enhance the cardio-depressant effect. The dosages of oral antidiabetics may have to be readjusted in patients receiving beta-blockers. The plasma concentration of Metazero can increase when cimetidine or hydralazine are administered simultaneously.
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Information checked by Dr. Sachin Kumar, MD Pharmacology