Detensiel
Detensiel - General Information
A cardioselective beta-1-adrenergic blocker. It is effective in the management of hypertension and angina pectoris. [PubChem]
Pharmacology of Detensiel
Detensiel is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Detensiel is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as Detensiel that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Detensiel is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.
Detensiel for patients
Patients especially those with coronary artery disease should be warned about discontinuing use of ZEBETA without a physician's supervision. Patients should also be advised to consult a physician if any difficulty in breathing occurs, or if they develop signs or symptoms of congestive heart failure or excessive bradycardia.
Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents should be cautioned that beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia, and bisoprolol fumarate should be used with caution. Patients should know how they react to this medicine before they operate automobiles and machinery or engage in other tasks requiring alertness.
Detensiel Interactions
ZEBETA should not be combined with other beta-blocking agents. Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be closely monitored, because the added beta-adrenergic blocking action of ZEBETA may produce excessive reduction of sympathetic activity. In patients receiving concurrent therapy with clonidine, if therapy is to be discontinued, it is suggested that ZEBETA be discontinued for several days before the withdrawal of clonidine.
ZEBETA should be used with care when myocardial depressants or inhibitors of AV conduction, such as certain calcium antagonists (particularly of the phenylalkylamine [verapamil] and benzothiazepine [diltiazem] classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
Concurrent use of rifampin increases the metabolic clearance of ZEBETA, resulting in a shortened elimination half-life of ZEBETA. However, initial dose modification is generally not necessary. Pharmacokinetic studies document no clinically relevant interactions with other agents given concomitantly, including thiazide diuretics, digoxin, and cimetidine. There was no effect of ZEBETA on prothrombin time in patients on stable doses of warfarin.
Risk of Anaphylactic Reaction: While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reactions.
Detensiel Contraindications
ZEBETA is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.
Additional information about Detensiel
Detensiel Indication: For the management of hypertension and prophylaxis treatment of angina pectoris and heart failure.
Mechanism Of Action: Detensiel selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Detensiel can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm.
Drug Interactions: Acetohexamide The beta-blocker decreases the symptoms of hypoglycemia
Chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia
Clonidine Increased hypertension when clonidine stopped
Dihydroergotamine Ischemia with risk of gangrene
Dihydroergotoxine Ischemia with risk of gangrene
Disopyramide The beta-blocker increases toxicity of disopyramide
Epinephrine Hypertension, then bradycardia
Ergonovine Ischemia with risk of gangrene
Ergotamine Ischemia with risk of gangrene
Fenoterol Antagonism
Formoterol Antagonism
Gliclazide The beta-blocker decreases the symptoms of hypoglycemia
Glipizide The beta-blocker decreases the symptoms of hypoglycemia
Glisoxepide The beta-blocker decreases the symptoms of hypoglycemia
Glibenclamide The beta-blocker decreases the symptoms of hypoglycemia
Glycodiazine The beta-blocker decreases the symptoms of hypoglycemia
Ibuprofen Risk of inhibition of renal prostaglandins
Indomethacin Risk of inhibition of renal prostaglandins
Insulin The beta-blocker decreases the symptoms of hypoglycemia
Insulin-aspart The beta-blocker decreases the symptoms of hypoglycemia
Insulin-detemir The beta-blocker decreases the symptoms of hypoglycemia
Insulin-glargine The beta-blocker decreases the symptoms of hypoglycemia
Insulin-glulisine The beta-blocker decreases the symptoms of hypoglycemia
Insulin-lispro The beta-blocker decreases the symptoms of hypoglycemia
Isoproterenol Antagonism
Lidocaine The beta-blocker increases the effect and toxicity of lidocaine
Methysergide Ischemia with risk of gangrene
Orciprenaline Antagonism
Pirbuterol Antagonism
Piroxicam Risk of inhibition of renal prostaglandins
Prazosin Risk of hypotension at the beginning of therapy
Procaterol Antagonism
Repaglinide The beta-blocker decreases the symptoms of hypoglycemia
Rifampin Rifampin decreases the effect of the metabolized beta-blocker
Salbutamol Antagonism
Salmeterol Antagonism
Terbutaline Antagonism
Tolazamide The beta-blocker decreases the symptoms of hypoglycemia
Tolbutamide The beta-blocker decreases the symptoms of hypoglycemia
Verapamil Increased effect of both drugs
Food Interactions: Take without regard to meals.
Generic Name: Bisoprolol
Synonyms: Bisoprolol Fumarate; Bisoprolol fumerate; Bisoprolol Hemifumarate
Drug Category: Sympatholytics; Antihypertensive Agents; Adrenergic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Bisoprolol: Cardicor; Concor; Condyline; Condylox; Detensiel; Emconcor; Emcor; Euradal; Isoten; Monocor; Soloc; Soprol; Zebeta;
Absorption: 80%
Toxicity (Overdose): Oral, mouse: LD50 = 100 mg/kg; Skin, rabbit: LD50 = 200 mg/kg; Skin, rat: LD50 = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat.
Protein Binding: Binding to serum proteins is approximately 30%
Biotransformation: Hepatic
Half Life: 9-12 hours
Dosage Forms of Detensiel: Tablet Oral
Chemical IUPAC Name: 1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol
Chemical Formula: C18H31NO4
Bisoprolol on Wikipedia: https://en.wikipedia.org/wiki/Bisoprolol
Organisms Affected: Humans and other mammals
