Kerlone
Brand names,
Kerlone
Analogs
Kerlone
Brand Names Mixture
Kerlone
Chemical_Formula
C18H29NO3
Kerlone
RX_link
http://www.rxlist.com/cgi/generic3/betaxolol.htm
Kerlone
fda sheet
Kerlone
msds (material safety sheet)
Kerlone
Synthesis Reference
No information avaliable
Kerlone
Molecular Weight
307.428 g/mol
Kerlone
Melting Point
70-72 oC
Kerlone
H2O Solubility
451 mg/L
Kerlone
State
Solid
Kerlone
LogP
3.265
Kerlone
Dosage Forms
Liquid; Solution; Suspension
Kerlone
Indication
For the management of hypertension.
Kerlone
Pharmacology
Betaxolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Betaxolol 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 betaxolol 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. Betaxolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.
Kerlone
Absorption
Absorption of an oral dose is complete. There is a small and consistent first-pass effect resulting in an absolute bioavailability of 89% ± 5% that is unaffected by the concomitant ingestion of food or alcohol.
Kerlone
side effects and Toxicity
Oral LD50s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats. Predicted symptoms of overdose include bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia.
Kerlone
Patient Information
Patients, especially those with evidence of coronary artery insufficiency, should be warned against interruption
or discontinuation of Kerlone therapy without the physician's advice.
Although cardiac failure rarely occurs in appropriately selected patients, patients being treated with
beta-adrenergic blocking agents should be advised to consult a physician at the first sign or symptom of failure.
Patients should know how they react to this medicine before they operate automobiles and machinery or engage in
other tasks requiring alertness. Patients should contact their physician if any difficulty in breathing occurs, and
before surgery of any type. Patients should inform their physicians or dentists that they are taking Kerlone.
Patients with diabetes should be warned that beta-blockers may mask tachycardia occurring with
hypoglycemia.
How to Use This Medicine:
Tablet
- Your doctor will tell you how much of this medicine to take and how often. Do not take more medicine or take it
more often than your doctor tells you to.
- You may take this medicine with or without food.
If a dose is missed:
- If you miss a dose or forget to use your medicine, use it as soon as you can. If your next regular dose is less
than 8 hours away, wait until then to use the medicine and skip the missed dose.
- Do not use extra medicine to make up for a missed dose.
How to Store and Dispose of This Medicine:
- Store the medicine at room temperature, away from heat, moisture, and direct light.
- Keep all medicine out of the reach of children and never share your medicine with anyone.
Kerlone
Organisms Affected
Humans and other mammals