metabolizers. Nebivolol is metabolized by a number of routes, including glucuronidation and hydroxylation by CYP D. The active isomer d-nebivolol has an Contraindications Interactions effective half-life of about hours in CYP D extensive metabolizers most Nebivolol is contraindicated in the following conditions: people , and hours in poor metabolizers and exposure to d-Nebivolol is Severe bradycardia Use caution when Nebivolol is co-administered with CYP D inhibitors substantially increased in poor metabolizers. Heart block greater than rst degree quinidine, propafenone, uoxetine, paroxetine, etc. . Tablets Patients with cardiogenic shock It is excreted in the urine and faeces, almost entirely as metabolites. Decompensated cardiac failure Do not use Nebivolol with other β-blockers. Closely monitor patients Sick sinus syndrome unless a permanent pacemaker is in place receiving catecholamine-depleting drugs, such as reserpine or PHARMACEUTICAL INFORMATION QUALITATIVE QUANTITATIVE COMPOSITION Patients with severe hepatic impairment Child-Pugh > B guanethidine, because the added β-blocking action of Nebivolol may Shelf Life Anvol tablets . mg: Patients who are hypersensitive to any component of this product produce excessive reduction of sympathetic activity. in patients who are years. Each tablet contains receiving Nebivolol and clonidine, discontinue Nebivolol for several days Nebivolol as HCl ...... . mg Warnings and Precautions before the gradual tapering of clonidine. Special Precautions for Storage Anvol tablets mg: To be sold on the prescription of a Each tablet contains Do not abruptly discontinue Nebivolol therapy in patients with coronary Both digitalis glycosides and β-blockers slow atrioventricular conduction registered medical practitioner only. Nebivolol as HCl ...... mg artery disease. Severe exacerbation of angina, myocardial infarction and and decrease heart rate. Concomitant use can increase the risk of Do not store above ºC. Anvol tablets mg: ventricular arrhythmias may occur in patients with coronary artery disease bradycardia. Protect from light and moisture. Each tablet contains following the abrupt discontinuation of therapy with β-blockers. Keep out of the reach of children. Nebivolol as HCl ...... mg Myocardial infarction and ventricular arrhythmias may occur with or Nebivolol can exacerbate the effects of myocardial depressants or without preceding exacerbation of the angina pectoris. Caution patients inhibitors of AV conduction, such as certain calcium antagonists Nature and contents of container DESCRIPTION without overt coronary artery disease against interruption or abrupt particularly of the phenylalkylamine verapamil and benzothiazepine Anvol Nebivolol . mg tablets are available in a blister of s xs . The chemical name for the active ingredient in Anvol is Nebivolol. discontinuation of therapy. As with other β-blockers, when discontinuation diltiazem classes , or antiarrhythmic agents, such as disopyramide. Anvol Nebivolol mg tablets are available in a blister of s xs . Chemically, it is RS,RS -,- RS, SR bis - uoro-,-dihydro - H-- of Nebivolol is planned, carefully observe and advise patients to minimize Anvol Nebivolol mg tablets are available in a blister of s xs . benzopyran- -yl - , - iminodiethanol hydrochloride. Anvol Nebivolol is physical activity. Taper Nebivolol over to weeks when possible. If the Pregnancy and Breastfeeding a racemate composed of d-Nebivolol and l-Nebivolol with the Category C stereochemical designations of SRRR-Nebivolol and RSSS nebivolol, angina worsens or acute coronary insufciency develops, re-start Nebivolol Use Nebivolol during pregnancy only if the potential benet justies the respectively. Nebivolols molecular formula is C H ClF NO HCl with the promptly, at least temporarily. potential risk to the fetus. following structural formula: Data regarding the use of Nebivolol is not available in patients with angina Because of the potential for β-blockers to produce serious adverse pectoris or who had a recent MI. reactions in nursing infants, especially bradycardia, Nebivolol is not recommended during nursing. In general, patients with bronchospastic diseases should not receive β-blockers. Adverse Reactions The most common adverse reactions that can lead to discontinuation of Because beta-blocker withdrawal has been associated with an increased Nebivolol are headache, nausea and bradycardia. asthenia. SRRR - or d-Nebivolol hydrochloride risk of MI and chest pain, patients already on beta-blockers should generally continue treatment throughout the perioperative period. If abdominal pain Nebivolol is to be continued perioperatively, monitor patients closely when hypercholesterolemia, increased BUN, increased triglycerides, decreased HDL and low platelets. anesthetic agents which depress myocardial function, such as ether, cyclopropane, and trichloroethylene, are used. If β-blocking therapy is paraesthesia withdrawn prior to major surgery, the impaired ability of the heart to respond to reex adrenergic stimuli may augment the risks of general Overdose anesthesia and surgical procedures. The most common signs and symptoms associated with Nebivolol overdosage are bradycardia and hypotension. Other important adverse RSSS - or l-Nebivolol hydrochloride β-blockers may mask some of the manifestations of hypoglycemia, reactions that may occur with Nebivolol overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse reactions CLINICAL INFORMATION particularly tachycardia. Nonselective β blockers may potentiate associated with β-blocker overdose include bronchospasm and heart Indications insulin-induced hypoglycemia and delay recovery of serum glucose levels. block. Anvol Nebivolol is indicated for the treatment of hypertension, to lower It is not known whether Nebivolol has these effects. Because of extensive drug binding to plasma proteins, hemodialysis is not blood pressure. Anvol Nebivolol may be used alone or in combination expected to enhance Nebivolol clearance. If overdose occurs, provide with other antihypertensive agents. Lowering blood pressure reduces the β-blockers may mask clinical signs of hyperthyroidism, such as tachycardia. general supportive and specic symptomatic treatment. risk of fatal and nonfatal cardiovascular events, primarily strokes and Abrupt withdrawal of β-blockers may be followed by an exacerbation of the myocardial infarctions. symptoms of hyperthyroidism or may precipitate a thyroid storm. PHARMACOLOGICAL PROPERTIES Chronic Heart Failure: treatment of stable mild and moderate chronic Pharmacotherapeutic group: Beta blocking agent, selective. heart failure in addition to standard therapies in elderly patients ≥ years. β-blockers can precipitate or aggravate symptoms of arterial insufciency ATC code: CAB in patients with peripheral vascular disease. Nebivolol is a β-adrenergic receptor blocking agent. In extensive Dosage and Administration metabolizers most of the population and at doses less than or equal to Because of signicant negative inotropic and chronotropic effects in mg, Nebivolol is preferentially β selective. In poor metabolizers and at The dose of Anvol Nebivolol must be individualized to the needs of the patients treated with β-blockers and calcium channel blockers of the higher doses, Nebivolol inhibits both β - and β - adrenergic receptors. patient. For most patients, the recommended starting dose is mg once verapamil and diltiazem type, monitor the ECG and blood pressure in Nebivolol lacks intrinsic sympathomimetic and membrane stabilizing daily, with or without food, as monotherapy or in combination with other patients treated concomitantly with these agents. activity at therapeutically relevant concentrations. At clinically relevant agents. For patients requiring further reduction in blood pressure, the dose doses, Nebivolol does not demonstrate α-adrenergic receptor blockade can be increased at -week intervals up to mg. A more frequent dosing Nebivolol exposure increases with inhibition of CYP D. The dose of activity. various metabolites, including glucuronides, contribute to regimen is unlikely to be benecial. Nebivolol may need to be reduced. β-blocking activity. Mechanism of Action In patients with severe renal impairment ClCr less than mLmin the Renal clearance of Nebivolol is decreased in patients with severe renal The mechanism of action of the antihypertensive response of Nebivolol recommended initial dose is . mg once daily; titrate up slowly if needed. impairment. Nebivolol is not known in patients receiving dialysis. has not been denitively established. Possible factors that may be involved Anvol Nebivolol is not known in patients receiving dialysis. include: decreased heart rate, decreased myocardial contractility, Metabolism of Nebivolol is decreased in patients with moderate hepatic diminution of tonic sympathetic outow to the periphery from cerebral In patients with moderate hepatic impairment, the recommended initial impairment. Nebivolol is not known in patients with severe hepatic vasomotor centers, suppression of renin activity and vasodilation and dose is . mg once daily; titrate up slowly if needed. Anvol Nebivolol is impairment. decreased peripheral vascular resistance. not known in patients with severe hepatic impairment and therefore it is Pharmacokinetic Properties not recommended. While taking β-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated Nebivolol is rapidly absorbed after oral doses. Mean peak plasma Nebivolol Pediatric Use accidental, diagnostic, or therapeutic challenge. Such patients may be concentrations occur approximately . to hours post-dosing. Safety and effectiveness in pediatric patients have not been established. unresponsive to the usual doses of epinephrine used to treat allergic Geriatric Patients reactions. Human plasma protein binding of Nebivolol is approximately , mostly It is not necessary to adjust the dose in the elderly. to albumin, and is independent of Nebivolol concentrations. CYP2D6 Polymorphism In patients with known or suspected pheochromocytoma, initiate an No dose adjustments are necessary for patients who are CYP D poor α-blocker prior to the use of any β-blocker. 1 metabolizers. Nebivolol is metabolized by a number of routes, including glucuronidation and hydroxylation by CYP D. The active isomer d-nebivolol has an Contraindications Interactions effective half-life of about hours in CYP D extensive metabolizers most Nebivolol is contraindicated in the following conditions: people , and hours in poor metabolizers and exposure to d-Nebivolol is Severe bradycardia Use caution when Nebivolol is co-administered with CYP D inhibitors substantially increased in poor metabolizers. Heart block greater than rst degree quinidine, propafenone, uoxetine, paroxetine, etc. . Patients with cardiogenic shock It is excreted in the urine and faeces, almost entirely as metabolites. Decompensated cardiac failure Do not use Nebivolol with other β-blockers. Closely monitor patients Sick sinus syndrome unless a permanent pacemaker is in place receiving catecholamine-depleting drugs, such as reserpine or PHARMACEUTICAL INFORMATION QUALITATIVE QUANTITATIVE COMPOSITION Patients with severe hepatic impairment Child-Pugh > B guanethidine, because the added β-blocking action of Nebivolol may Shelf Life Anvol tablets . mg: Patients who are hypersensitive to any component of this product produce excessive reduction of sympathetic activity. in patients who are years. Each tablet contains receiving Nebivolol and clonidine, discontinue Nebivolol for several days Nebivolol as HCl ...... . mg Warnings and Precautions before the gradual tapering of clonidine. Special Precautions for Storage Anvol tablets mg: To be sold on the prescription of a Each tablet contains Do not abruptly discontinue Nebivolol therapy in patients with coronary Both digitalis glycosides and β-blockers slow atrioventricular conduction registered medical practitioner only. Nebivolol as HCl ...... mg artery disease. Severe exacerbation of angina, myocardial infarction and and decrease heart rate. Concomitant use can increase the risk of Do not store above ºC. Anvol tablets mg: ventricular arrhythmias may occur in patients with coronary artery disease bradycardia. Protect from light and moisture. Each tablet contains following the abrupt discontinuation of therapy with β-blockers. Keep out of the reach of children. Nebivolol as HCl ...... mg Myocardial infarction and ventricular arrhythmias may occur with or Nebivolol can exacerbate the effects of myocardial depressants or without preceding exacerbation of the angina pectoris. Caution patients inhibitors of AV conduction, such as certain calcium antagonists Nature and contents of container DESCRIPTION without overt coronary artery disease against interruption or abrupt particularly of the phenylalkylamine verapamil and benzothiazepine Anvol Nebivolol . mg tablets are available in a blister of s xs . The chemical name for the active ingredient in Anvol is Nebivolol. discontinuation of therapy. As with other β-blockers, when discontinuation diltiazem classes , or antiarrhythmic agents, such as disopyramide. Anvol Nebivolol mg tablets are available in a blister of s xs . Chemically, it is RS,RS -,- RS, SR bis - uoro-,-dihydro - H-- of Nebivolol is planned, carefully observe and advise patients to minimize Anvol Nebivolol mg tablets are available in a blister of s xs . benzopyran- -yl - , - iminodiethanol hydrochloride. Anvol Nebivolol is physical activity. Taper Nebivolol over to weeks when possible. If the Pregnancy and Breastfeeding a racemate composed of d-Nebivolol and l-Nebivolol with the Category C stereochemical designations of SRRR-Nebivolol and RSSS nebivolol, angina worsens or acute coronary insufciency develops, re-start Nebivolol Use Nebivolol during pregnancy only if the potential benet justies the respectively. Nebivolols molecular formula is C H ClF NO HCl with the promptly, at least temporarily. potential risk to the fetus. following structural formula: Data regarding the use of Nebivolol is not available in patients with angina Because of the potential for β-blockers to produce serious adverse pectoris or who had a recent MI. reactions in nursing infants, especially bradycardia, Nebivolol is not recommended during nursing. MANUFACTURED BY In general, patients with bronchospastic diseases should not receive β-blockers. Adverse Reactions The most common adverse reactions that can lead to discontinuation of Because beta-blocker withdrawal has been associated with an increased Nebivolol are headache, nausea and bradycardia. Aspin Pharma Pvt. Ltd. asthenia. Plot No. , Sector No. , SRRR - or d-Nebivolol hydrochloride risk of MI and chest pain, patients already on beta-blockers should generally continue treatment throughout the perioperative period. If abdominal pain Korangi Industrial Area, Karachi- , Pakistan. Nebivolol is to be continued perioperatively, monitor patients closely when hypercholesterolemia, increased BUN, www.aspin.com.pk increased triglycerides, decreased HDL and low platelets. anesthetic agents which depress myocardial function, such as ether, cyclopropane, and trichloroethylene, are used. If β-blocking therapy is paraesthesia REVISION DATE withdrawn prior to major surgery, the impaired ability of the heart to February respond to reex adrenergic stimuli may augment the risks of general Overdose anesthesia and surgical procedures. The most common signs and symptoms associated with Nebivolol overdosage are bradycardia and hypotension. Other important adverse RSSS - or l-Nebivolol hydrochloride β-blockers may mask some of the manifestations of hypoglycemia, reactions that may occur with Nebivolol overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse reactions CLINICAL INFORMATION particularly tachycardia. Nonselective β blockers may potentiate associated with β-blocker overdose include bronchospasm and heart Indications insulin-induced hypoglycemia and delay recovery of serum glucose levels. block. Anvol Nebivolol is indicated for the treatment of hypertension, to lower It is not known whether Nebivolol has these effects. Because of extensive drug binding to plasma proteins, hemodialysis is not blood pressure. Anvol Nebivolol may be used alone or in combination expected to enhance Nebivolol clearance. If overdose occurs, provide with other antihypertensive agents. Lowering blood pressure reduces the β-blockers may mask clinical signs of hyperthyroidism, such as tachycardia. general supportive and specic symptomatic treatment. risk of fatal and nonfatal cardiovascular events, primarily strokes and Abrupt withdrawal of β-blockers may be followed by an exacerbation of the myocardial infarctions. symptoms of hyperthyroidism or may precipitate a thyroid storm. PHARMACOLOGICAL PROPERTIES Chronic Heart Failure: treatment of stable mild and moderate chronic Pharmacotherapeutic group: Beta blocking agent, selective. heart failure in addition to standard therapies in elderly patients ≥ years. β-blockers can precipitate or aggravate symptoms of arterial insufciency ATC code: CAB in patients with peripheral vascular disease. Nebivolol is a β-adrenergic receptor blocking agent. In extensive Dosage and Administration metabolizers most of the population and at doses less than or equal to Because of signicant negative inotropic and chronotropic effects in mg, Nebivolol is preferentially β selective. In poor metabolizers and at The dose of Anvol Nebivolol must be individualized to the needs of the patients treated with β-blockers and calcium channel blockers of the higher doses, Nebivolol inhibits both β - and β - adrenergic receptors. patient. For most patients, the recommended starting dose is mg once verapamil and diltiazem type, monitor the ECG and blood pressure in Nebivolol lacks intrinsic sympathomimetic and membrane stabilizing daily, with or without food, as monotherapy or in combination with other patients treated concomitantly with these agents. activity at therapeutically relevant concentrations. At clinically relevant agents. For patients requiring further reduction in blood pressure, the dose doses, Nebivolol does not demonstrate α-adrenergic receptor blockade can be increased at -week intervals up to mg. A more frequent dosing Nebivolol exposure increases with inhibition of CYP D. The dose of activity. various metabolites, including glucuronides, contribute to regimen is unlikely to be benecial. Nebivolol may need to be reduced. β-blocking activity. Mechanism of Action In patients with severe renal impairment ClCr less than mLmin the Renal clearance of Nebivolol is decreased in patients with severe renal The mechanism of action of the antihypertensive response of Nebivolol recommended initial dose is . mg once daily; titrate up slowly if needed. impairment. Nebivolol is not known in patients receiving dialysis. has not been denitively established. Possible factors that may be involved Anvol Nebivolol is not known in patients receiving dialysis. include: decreased heart rate, decreased myocardial contractility, Metabolism of Nebivolol is decreased in patients with moderate hepatic diminution of tonic sympathetic outow to the periphery from cerebral In patients with moderate hepatic impairment, the recommended initial impairment. Nebivolol is not known in patients with severe hepatic vasomotor centers, suppression of renin activity and vasodilation and dose is . mg once daily; titrate up slowly if needed. Anvol Nebivolol is impairment. decreased peripheral vascular resistance. not known in patients with severe hepatic impairment and therefore it is Pharmacokinetic Properties not recommended. While taking β-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated Nebivolol is rapidly absorbed after oral doses. Mean peak plasma Nebivolol Pediatric Use accidental, diagnostic, or therapeutic challenge. Such patients may be concentrations occur approximately . to hours post-dosing. Safety and effectiveness in pediatric patients have not been established. unresponsive to the usual doses of epinephrine used to treat allergic Geriatric Patients reactions. Human plasma protein binding of Nebivolol is approximately , mostly It is not necessary to adjust the dose in the elderly. to albumin, and is independent of Nebivolol concentrations. CYP2D6 Polymorphism In patients with known or suspected pheochromocytoma, initiate an No dose adjustments are necessary for patients who are CYP D poor α-blocker prior to the use of any β-blocker. AV-L- 2
Anvol Leaflet
