Brand Name : Supermet™ XL 100
Generic Name : Metoprolol Succinate Extended Release Tablets IP 100 mg
| Bronchospastic Diseases: PATIENTS WITH BRONCHOSPASTIC DISEASES SHOULD, IN GENERAL, NOT RECEIVE BETA BLOCKERS, including metoprolol tartrate . Because of its relative beta1 selectivity, however, Metoprolol tartrate may be used with caution in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment. Since beta1 selectivity is not absolute, a beta2-stimulating agent should be administered concomitantly, and the lowest possible dose of Metoprolol tartrate should be used. In these circumstances it would be prudent initially to administer metoprolol tartrate in smaller doses three times daily, instead of larger doses two times daily, to avoid the higher plasma levels associated with the longer dosing interval. |
For the use of a Registered Medical Practitioner only
1. GENERIC NAMEAND BRAND NAME
Metoprolol Succinate Extended Release Tablets IP 25 mg
Supermet™ – XL 25
Metoprolol Succinate Extended Release Tablets IP 50mg
Supermet™ – XL 50
Metoprolol Succinate Extended Release Tablets IP 100 mg
Supermet™ XL 100
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Supermet™ XL 25
Each film-coated extended release tablet contains:
Metoprolol Succinate I.P. 23.75 mg
equivalent to Metoprolol Tartrate 25 mg
Colour: Titanium dioxide I.P.
Supermet™ – XL 50
Each film-coated extended release tablet contains:
Metoprolol Succinate I.P. 47.5 mg
equivalent to Metoprolol Tartrate 50 mg
(as extended release)
Excipients q.s.
Colour: Lake Sunset Yellow FCF & Lake Tartrazine
Supermet™ XL 100
Each film-coated extended release tablet contains:
Metoprolol Succinate IP 95mg
equivalent to Metoprolol Tartrate 100mg
Excipients q.s.
Colour: Ferric Oxide (Red) USP – NF
3. DOSAGE FORM AND STRENGTH
Kindly refer to section 1 & 2
4. CLINICAL PARTICULARS
4.1THERAPEUTIC INDICATION
Functional heart disorders,migraine prophylaxis, cardiac arrhythmias, prevention of cardiac death and reinfarction after the acute phase of myocardial infarction , stable symptomatic CHF.
4.2 POSOLOGY AND METHOD OF ADMINISTRATION Administer once daily. In some patients the dosages have to be individualized and titration may be required.
When switching from immediate release metoprolol tablet to metoprolol succinate extended-release tablet, for the treatment of hypertension and angina, the same total daily dose is recommended.
Hypertension
The usual initial dosage is 25 to 100 mg daily in a single dose. The dosage may be increased (up to 400 mg) at weekly (or longer) intervals until optimum blood pressure reduction is achieved. In general, the maximum effect of any given dosage level will be apparent after 1 week of therapy.
Angina Pectoris
The dosage of metoprolol succinate extended-release tablets should be individualized. The usual initial dosage is 100 mg once a day
The dosage may be gradually increased at weekly intervals until optimum clinical response has been obtained or there is a pronounced slowing of the heart rate.. For discontinuation of treatment, the dosage should be reduced gradually over a period of 1 or 2 weeks.
Heart Failure
Dosage must be individualized and closely monitored during up titration. If used, the dosing of diuretics, ACE inhibitors, and digitalis should be stabilized prior to initiation of metoprolol therapy
The recommended starting dose is 25 mg once daily for two weeks in patients with NYHA Class II heart failure and 12.5 mg once daily in patients with more severe heart failure. Every two weeks, the dose should be doubled to the highest dosage level tolerated by the patient.
If transient worsening of heart failure occurs, it may be treated with increased doses of diuretics, and it may also be necessary to lower or temporarily discontinue the dose of metoprolol succinate extended-release tablet.
Until symptoms of worsening heart failure have been stabilized, the dose of metoprolol succinate extended-release tablet should not be increased.
4.3 CONTRAINDICATIONS
Contraindicated in patients with
- Known hypersensitivity to metoprolol succinate or any component of this product.
- Severe bradycardia
- Cardiogenic shock
- Heart block greater than first degree
- Decompensated cardiac failure
- Sick sinus syndrome (unless a permanent pacemaker is in place) and
4.4 SPECIAL WARNINGS AND PRECAUTIONS FOR USE
Ischemic Heart Disease:
Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have been reported. Particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1–2 weeks and the patient should be carefully monitored, when discontinuing chronically administered metoprolol succinate extended-release tablets.
Metoprolol succinate extended-release tablet administration should be reinstated promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken, if angina markedly worsens or acute coronary insufficiency develops.
Bronchospastic Diseases
Patients having bronchospastic diseases should not receive beta-blockers. Metoprolol may be used with caution in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment because of its relative beta1-selectivity.
The lowest possible dose of metoprolol should be used and a beta2-stimulating agent should be administered concomitantly, since beta-selectivity is not absolute
Major Surgery
The impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures; the necessity or desirability of withdrawing beta-blocking therapy prior to major surgery is controversial.
With beta-blockers, difficulty in restarting and maintaining the heart beat has also been reported.
Diabetes and Hypoglycemia:
In diabetic patients Metoprolol succinate extended release tablets should be used with caution if a beta-blocking agent is required. Beta-blockers may mask tachycardia occurring with hypoglycemia, but other manifestations such as dizziness and sweating may not be significantly affected.
Thyrotoxicosis:
Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-blockade, which might precipitate a thyroid storm. Beta-adrenergic blockade may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism.
Peripheral Vascular Disease:
Beta-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease so caution should be exercised in such individuals.
Calcium Channel Blockers:
Caution should be exercised in patients treated with beta-blockers and calcium channel blockers of the verapamil and diltiazem type concomitantly, because of significant inotropic and chronotropic effects in patients treated with these agents.
Hepatic Function
In patients with impaired hepatic function Metoprolol succinate extended-release tablets should be used with caution.
Cardiac Failure
During up titration of metoprolol succinate extended release tablets, worsening cardiac failure may occur. If such symptoms occur, diuretics should be increased and until clinical stability is restored the dose of metoprolol succinate extended release tablets should not be advanced. It may be necessary to temporarily discontinue or lower the dose of metoprolol succinate extended-release tablet.
Carcinogenesis, Mutagenesis, Impairment of Fertility
In 2-year studies in rats at three oral dosage levels of up to 800 mg/kg/day there was no increase in the development of spontaneously occurring benign or malignant neoplasms of any type.
All genotoxicity tests performed on metoprolol succinate (a Salmonella/mammalian-microsome mutagenicity test) were negative.
Pregnancy
No adequate and well-controlled studies are done in pregnant women, hence, drug should be used during pregnancy only if clearly needed.
Nursing Mothers
Caution should be exercised when metoprolol succinate extended-release tablet is administered to a nursing woman as it is excreted in breast milk in very small quantities.
Pediatric Use
No clinically relevant differences in the adverse event profile were observed for pediatric patients (aged 6 to 16 years) as compared to adults. Safety and effectiveness have not been established in patients < 6 years of age of metoprolol succinate extended release tablets.
Geriatric Use
No established data is present for patients above 65 years of age.
4.5 DRUG INTERACTIONS
| No | Drug | Drug interaction | Remark |
| 1 | Catecholamine-depleting drugs e.g. Reserpine, Mono Amine Oxidase (MAO) Inhibitors |
Catecholamine-depleting drugs may have an additive effect when given with beta-blocking agents. | Closely observe patients for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension. |
| 2 | CYP2D6 Inhibitors E.g. Quinidine, Fluoxetine, Paroxetine, and Propafenone |
Metoprolol concentrations are likely to increase by drugs that inhibit CYP2D6. | |
| 3 | Digitalis | Digitalis | Concomitant use can increase the risk of bradycardia. |
| 4 | Clonidine | Beta-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. | If the two drugs are co administered, the beta blocker should be withdrawn several days before the gradual withdrawal of clonidine. If replacing clonidine by beta-blocker therapy, the introduction of beta blockers should be delayed for several days after clonidine administration has stopped. |
4.6 USE IN SPECIAL POPULATIONS (SUCH AS PREGNANT WOMEN, LACTATING WOMEN, PAEDIATRIC PATIENTS, GERIATRIC PATIENTS ETC.)
Pregnancy
No adequate and well-controlled studies are done in pregnant women, hence, drug should be used during pregnancy only if clearly needed.
Nursing Mothers
Caution should be exercised when metoprolol succinate extended-release tablet is administered to a nursing woman as it is excreted in breast milk in very small quantities.
Pediatric Use
No clinically relevant differences in the adverse event profile were observed for pediatric patients (aged 6 to 16 years) as compared to adults. Safety and effectiveness have not been established in patients < 6 years of age of metoprolol succinate extended release tablets.
Geriatric Use
No established data is present for patients above 65 years of age.
4.7 EFFECTS ON ABILITY TO DRIVE AND USE MACHINES
Patients should be advised to avoid operating automobiles and machinery or engaging in other tasks requiring alertness until the patient’s response to therapy with metoprolol succinate extended release tablets has been determined.
4.8 UNDESIRABLE EFFECTS
Hypertension and Angina:
Central Nervous System: Tiredness, dizziness, Mental confusion, short-term memory loss, Headache, nightmares, somnolence, and insomnia
Cardiovascular: Shortness of breath, bradycardia, cold extremities; arterial insufficiency, usually of the Raynaud type, congestive heart failure palpitations, peripheral edema, syncope, chest pain and hypotension.
Respiratory: wheezing (bronchospasm) and dyspnea
Gastrointestinal: Diarrhea, nausea, dry mouth, constipation, gastric pain, flatulence, digestive tract disorders, and heartburn.
Hypersensitive Reactions: Pruritus o, rashes, worsening of psoriasis
Potential Adverse Reactions
In addition, there are a variety of adverse reaction not listed above, which have been reported with other beta adrenergic blocking agents and should be considered potential adverse reactions to metoprolol succinate extended release tablets.
Central Nervous System: Reversible mental depression progressing to catatonia; short-term memory loss, emotional lability, an acute reversible syndrome characterized by disorientation for time and place, slightly clouded sensorium, and decreased performance on neuropsychometrics.
Cardiovascular: Intensification of AV block.
Hematologic: Agranulocytosis, thrombocytopenic purpura, nonthrombocytopenic purpura.
Hypersensitive Reactions: Fever combined with sore throat and aching, laryngospasm, and respiratory distress.
Heart Failure: Dizziness, Vertigo, Bradycardia,
Other adverse events included myocardial infarction, diabetes mellitus/diabetes mellitus aggravated, pneumonia, cerebrovascular disorder, dyspnea/dyspnea aggravated, syncope, coronary artery disorder, chest pain, ventricular tachycardia/arrhythmia aggravated, hypotension, , abdominal pain, and fatigue.
Post-Marketing Experience
Cardiovascular: 2nd and 3rd degree heart block, cardiogenic shock in patients with acute myocardial infarction
Hematologic: thrombocytopenia.
Gastrointestinal: hepatitis, vomiting.
Musculoskeletal: arthralgia.
Reproductive, male: impotence.
Nervous System/Psychiatric: anxiety/nervousness, hallucinations, paresthesia.
Skin: increased sweating, photosensitivity, urticaria.
Special Sense Organs: taste disturbances.
4.9 OVERDOSAGE
Symptoms:
Overdosage of metoprolol succinate extended-release tablets may lead to
- Cardiac arrest
- Severe hypotension
- Atrioventricular block
- Bronchospasm
- Heart failure
- Cardiogenic shock
- Sinus bradycardia
- Impairment of consciousness/coma
- Nausea, vomiting, and cyanosis.
Treatment
Patients with acute or recent congestive heart or myocardial infarction failure may be more hemodynamically unstable than other patients and should be treated appropriately. The patient should be treated under intensive care conditions whenever possible. The following general measures should be employed on the basis of the pharmacologic actions of metoprolol:
Bradycardia: Atropine should be administered. Isoproterenol should be administered cautiously, if there is no response to vagal blockade.
Hypotension: A vasopressor should be administered, e.g., dopamine
Elimination of the Drug: Perform Gastric lavage.
Bronchospasm: A theophylline derivative and/or a beta-stimulating agent should be administered.
Cardiac Failure: A digitalis glycoside and diuretics should be administered. In shock resulting from inadequate cardiac contractility, administration of isoproterenol, dobutamine, or glucagon may be considered.
5.0 PHARMACOLOGIC PROPERTIES
5.1 MECHANISM OF ACTION
Metoprolol is a beta selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and metoprolol also inhibits beta adrenoreceptors at higher plasma concentrations, chiefly located in the vascular musculature and bronchial.
Metoprolol has no intrinsic sympathomimetic activity, and membrane stabilizing activity is detectable only at plasma concentrations much greater than required for beta blockade. Metoprolol slows the sinus rate and decreases AV nodal conduction indicated in animal and human experiments.
5.2 PHARMACODYNAMIC PROPERTIES
Beta-blocking activity of metoprolol in man, is shown by
1. Reduction in heart rate and cardiac output at rest and upon exercise,
2. Reduction of systolic blood pressure upon exercise,
3. Inhibition of isoproterenol-induced tachycardia, and
4. Reduction of reflex orthostatic tachycardia.
Although beta-adrenergic receptor blockade is useful in the treatment of hypertension, angina, and heart failure there are situations in which sympathetic stimulation is vital. Adequate ventricular function may depend on sympathetic drive in patients with severely damaged hearts. Beta-blockade may prevent the necessary facilitating effect of sympathetic activity on conduction in the presence of AV block.
5.3 PHARMACOKINETIC PROPERTIES
| Parameters | Metoprolol succinate extended release |
| Absorption | The peak plasma concentrations (Cmax) of metoprolol is observed within 10-12 hours and 2.0 hours of dose intake, respectively
For AUC, the mean values were 0–24 (P<0.05) Metoprolol is a racemic mixture of R- and S- enantiomers, and is primarily metabolized by CYP2D6. When administered orally, it exhibits stereo selective metabolism that is dependent on oxidation phenotype.CYP2D6 can be inhibited by a number of drugs. Concomitant use of inhibiting drugs in poor metabolizers will increase blood levels of Metoprolol several-fold, decreasing Metoprolol's cardioselectivity |
| Distribution | Metoprolol crosses the blood-brain barrier and has been reported in the CSF in a concentration 78% of the simultaneous plasma concentration. Volume of distribution of 5.6 L/kg. |
| Metabolism | Metoprolol is a racemic mixture of R- and S- enantiomers, and is primarily metabolized by CYP2D6. When administered orally, it exhibits stereoselective metabolism that is dependent on oxidation phenotype.CYP2D6 can be inhibited by a number of drugs. Concomitant use of inhibiting drugs in poor metabolizers will increase blood levels of Metoprolol several-fold, decreasing Metoprolol’s cardioselectivity. |
| Excretion | Excretion Elimination is mainly by biotransformation in the liver, and the plasma half-life ranges from approximately 3 to 7 hours. Less than 5% of an oral dose of Metoprolol is recovered unchanged in the urine; the rest is excreted by the kidneys as metabolites that appear to have no beta-blocking activity. |
| Half life | The plasma half-life ranges from approximately 3 to 7 hours. |
| Plasma protein binding |
Plasma protein binding of metoprolol is about 5-10%. |
6. NONCLINICAL PROPERTIES
6.1 ANIMAL TOXICOLOGY OR PHARMACOLOGY
Carcinogenesis, Mutagenesis, Impairment of Fertility
In 2-year studies in rats at three oral dosage levels of up to 800 mg/kg/day there was no increase in the development of spontaneously occurring benign or malignant neoplasms of any type.
All genotoxicity tests performed on metoprolol succinate (a Salmonella/mammalian-microsome mutagenicity test) were negative.
7. DESCRIPTION
Supermet™ XL 25 :
SUPERMET XL 25 is supplied for oral administration, as an extended – release tablet of Metoprolol Succinate. Each extended – release tablet of SUPERMET XL 25 contains Metoprolol Succinate 23.75 mg, equivalent to Metoprolol Tartrate 25 mg.
Supermet™ – XL 50
SUPERMET XL 50 is supplied for oral administration, as an extended – release tablet of Metoprolol Succinate. Each extended – release tablet of SUPERMET XL 50 contains Metoprolol Succinate 47.5 mg, equivalent to Metoprolol Tartrate 50 mg.
Supermet™ XL 100
SUPERMET XL 100 is supplied for oral administration, as an extended – release tablet of Metoprolol Succinate. Each extended – release tablet of SUPERMET XL 100 contains Metoprolol Succinate 95 mg, equivalent to Metoprolol Tartrate 100 mg.
8. PHARMACEUTICAL PARTICULARS
8.1 INCOMPATIBILITIES
Not Applicable
8.2 SHELF-LIFE
Refer pack
8.3 PACKAGING INFORMATION
Refer pack
8.4 STORAGE AND HANDING INSTRUCTIONS
Refer pack
9. PATIENT COUNSELLING INFORMATION
Take metoprolol succinate extended-release tablets regularly and continuously, as directed, preferably with or immediately following meals.
If a dose should be missed, take only the next scheduled dose (without doubling it).
Do not interrupt or discontinue metoprolol succinate extended-release tablets without consulting the physician.
Avoid operating automobiles and machinery or engaging in other tasks requiring alertness until your response to therapy with metoprolol succinate extended release tablets has been determined
Contact your physician if any difficulty in breathing occurs
Inform the physician or dentist before any type of surgery that you are taking metoprolol succinate extended-release tablets.
If you are a heart failure patient, you should consult your physician if you experience signs or symptoms of worsening heart failure such as weight gain or increasing shortness of breath.
10. DETAILS OF MANUFACTURER
Refer Pack for manufacturer details.
MARKETED BY
Abbott Healthcare Pvt. Ltd.
Angel Space, Bldg. D-4, Gala No. 1 to 6 &
11 to 16 Ground Floor, 101 to 106 &
111 to 116 First Floor, 201 to 206 & 211 to 216
2nd Floor, Pimplas, Dist. Thane, Bhiwandi – 421 302, India.
11. DETAILS OF PERMISSION OR LICENCE NUMBER
Refer Pack for Permission/License details
12. DATE OF REVISION
Version 4.0, Dated 07th Nov 2023
TM – Trade Mark of Abbott Healthcare Pvt. Ltd.
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