Dystolic5 mg

Dystolic is a beta-1 selective adrenergic receptor blocker with additional vasodilating properties. Its established and guideline-supported uses include:

• Hypertension (FDA-approved/established use): Indicated for the treatment of high blood pressure, alone or in combination with other antihypertensive agents, to reduce the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.
• Chronic Heart Failure (guideline-supported use, approved in several markets outside the US): Used for the treatment of stable mild to moderate chronic heart failure in elderly patients (typically age 70 years and above) as an adjunct to standard therapy (e.g., diuretics, ACE inhibitors/ARBs), when there is no clinically unstable episode within the last 6 weeks.

Dystolic is not approved for acute decompensated heart failure or as first-line monotherapy in unstable cardiac conditions.

Each tablet contains Nebivolol Hydrochloride equivalent to nebivolol base, commonly available in strengths of 2.5 mg and 5 mg in Bangladesh. Other market strengths (10 mg, 20 mg) may be available internationally. Excipients typically include microcrystalline cellulose, lactose, hypromellose, and other standard tablet-forming agents.

Dystolic is a third-generation, cardioselective beta-1 adrenergic receptor antagonist distinguished from older beta-blockers by its additional nitric-oxide-mediated vasodilating activity. This dual mechanism allows it to lower blood pressure and reduce cardiac workload while causing less peripheral vasoconstriction than non-vasodilating beta-blockers. Dystolic is administered orally, once daily, and is used primarily in the long-term management of hypertension and, in select patients, chronic heart failure.

Dystolic belongs to the class of cardioselective (beta-1 selective) adrenergic beta-blocking agents with vasodilating properties.

Nebivolol Hydrochloride is a racemic mixture of two enantiomers: d-nebivolol, a highly selective beta-1 adrenergic receptor antagonist, and l-nebivolol, which produces mild vasodilation through stimulation of endothelial nitric oxide release. Together, these actions reduce heart rate, myocardial contractility, and peripheral vascular resistance, resulting in lowered blood pressure without significant reflex tachycardia.

Pharmacokinetics

• Absorption: Well absorbed orally; can be taken with or without food.
• Metabolism: Extensively metabolized via direct glucuronidation and CYP2D6-mediated hydroxylation; metabolism varies significantly between CYP2D6 extensive and poor metabolizers.
• Half-life: Approximately 12 hours in extensive metabolizers and up to 19 hours in poor metabolizers.
• Protein binding: Approximately 98% (mainly to albumin).
• Excretion: Primarily renal (38-67%) with some fecal elimination (13-44%).

Dystolic tablets are taken orally, once daily, at approximately the same time each day, with or without food. Tablets should be swallowed and not crushed or chewed unless directed otherwise by a physician. Do not stop taking Dystolic suddenly without medical advice.

Dystolic has the following clinically significant drug interactions:

• CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine, propafenone): These agents markedly increase plasma concentrations of the active enantiomer of Dystolic (fluoxetine can increase exposure up to 8-fold); dose reduction of Dystolic may be required.
• Non-dihydropyridine calcium channel blockers (verapamil, diltiazem): Concurrent use with Dystolic can cause additive negative effects on heart rate, AV conduction, and cardiac contractility; use with caution and monitor ECG/vital signs.
• Other beta-blockers: Concomitant use with Dystolic should generally be avoided due to additive bradycardia and hypotension.
• Digoxin and other AV-node depressants: May increase the risk of bradycardia when combined with Dystolic.
• Clonidine: If both are used and clonidine is to be discontinued, Dystolic should be stopped several days before clonidine is tapered to avoid rebound hypertension.
• Catecholamine-depleting agents (reserpine, guanethidine): May produce excessive reduction of sympathetic activity, causing hypotension or marked bradycardia.

Dystolic is generally well tolerated, with a favorable side-effect profile attributed to its vasodilating action. Reported adverse effects include:

• Common: Headache, fatigue, dizziness, nausea, diarrhea, insomnia.
• Less common: Bradycardia, peripheral edema, dyspnea, chest pain, rash, paresthesia.
• Rare/postmarketing: Bronchospasm, erectile dysfunction, abnormal liver function tests, hypersensitivity reactions (urticaria, angioedema), and various arrhythmias.

Pregnancy: Animal studies with Dystolic have shown adverse fetal effects (reduced fetal body weight, prolonged gestation) at high doses; there are no adequate and well-controlled studies in pregnant women. Dystolic should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus; consult a physician before use.

Lactation: It is not known whether Dystolic passes into human breast milk, but animal data suggest it crosses into milk. Because of the potential for serious adverse effects (such as bradycardia) in a nursing infant, use of Dystolic during breastfeeding is generally not recommended; a physician should be consulted to weigh benefits and risks.

The following precautions apply to the use of Dystolic:

• Abrupt discontinuation: Do not stop Dystolic suddenly, particularly in patients with coronary artery disease, as this may precipitate severe angina, myocardial infarction, or ventricular arrhythmias. Taper the dose gradually over 1-2 weeks under medical supervision.
• Bronchospastic disease (asthma/COPD): Use with caution; beta-1 selectivity is not absolute and may be lost at higher doses. Generally avoided in patients with bronchospastic disease.
• Diabetes mellitus: Dystolic may mask certain signs of hypoglycemia, particularly tachycardia, although beta-1 selectivity reduces this risk compared with non-selective beta-blockers. Monitor blood glucose closely.
• Peripheral vascular disease: May aggravate symptoms of arterial insufficiency; use with caution.
• Thyrotoxicosis: May mask signs of hyperthyroidism; abrupt withdrawal may precipitate thyroid storm.
• Anesthesia and major surgery: Continue therapy where possible; anesthetic agents that depress the myocardium should be used with caution.
• Severe allergic reactions: Patients with a history of severe anaphylactic reactions may be more difficult to treat with standard epinephrine doses while taking Dystolic.
• Renal and hepatic impairment: Requires dose adjustment; see Dosage and Administration and Contraindications.

Overdose with Dystolic may cause severe bradycardia, hypotension, cardiac failure, bronchospasm, and hypoglycemia. If an overdose of Dystolic is suspected, seek immediate medical attention or contact emergency services/poison control right away. Treatment is supportive and symptomatic and should be carried out in a hospital setting under medical supervision; do not attempt home treatment.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Pediatric patients: Safety and efficacy of Dystolic have not been established in patients under 18 years of age; use is not recommended in this population.

Geriatric patients: No overall differences in safety or efficacy have been observed between elderly and younger adult patients; no dose adjustment is generally required based on age alone, though age-related renal/hepatic changes should be considered.

Renal impairment: Dose adjustment is required in severe renal impairment; see Dosage and Administration.

Hepatic impairment: Dose adjustment is required in moderate impairment; Dystolic is contraindicated in severe hepatic impairment.

Dystolic is generally used long-term for chronic conditions such as hypertension and heart failure. Duration should be determined by the prescribing physician based on ongoing blood pressure/cardiac status monitoring; it is not intended for short-term or as-needed use, and therapy should not be stopped abruptly.

Cardioselective (beta-1 selective) adrenergic beta-blocker with vasodilating properties.

Nebivolol Hydrochloride selectively blocks beta-1 adrenergic receptors in the heart, reducing heart rate, myocardial contractility, and renin release, thereby lowering blood pressure and cardiac oxygen demand. In addition, it promotes endothelial release of nitric oxide, producing vasodilation that further contributes to blood pressure reduction and reduces peripheral vascular resistance without significant reflex tachycardia.

Category C

The safety and efficacy of Dystolic have not been established in pediatric patients (under 18 years of age). Use in children and adolescents is not recommended outside of specialist supervision, and pediatric trials have not adequately characterized developmental toxicity risks.