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Betaxolol ; Uses, Dosage, Side Effects, Interactions, Pregnancy

Betaxolol is a racemic mixture and selective beta-1 adrenergic receptor antagonist with antihypertensive and anti-glaucoma activities and devoid of intrinsic sympathomimetic activity. Betaxolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. When applied topically in the eye, this agent reduces aqueous humor secretion and lowers the intraocular pressure (IOP). In addition, betaxolol prevents the release of renin, a hormone secreted by the kidneys that causes constriction of blood vessels.

Betaxolol also shows greater affininty for beta₁ receptors than metoprolol. It works by blocking the action of certain natural chemicals in your bodies such as epinephrine that affects the heart and blood vessels.

Mechanism of action of Betaxolol

Betaxolol 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. Betaxolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm.Betaxolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist . 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 lead to constriction of blood vessels. Betaxolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.

Indications of Betaxolol

Angina pectoris prophylaxis
To treatment of hypertension,
Arrhythmias,
Coronary heart disease,
Glaucoma,
To reduce non-fatal cardiac events in patients with heart failure.
Ophthalmic: for the management of glaucoma
the drug seems to have an effect of neuroprotection in glaucoma treatment
Reduction of elevated intraocular pressure in conditions such as ocular hypertension
Chronic open-angle glaucoma.

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Contra-Indications of Betaxolol

Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure
Sinus bradycardia, sick sinus syndrome, sino-atrial block
Cardiogenic shock;
Overt cardiac failure;
Pheochromocytoma
Diabetes
Depression
Complete heart block
Second-degree atrioventricular heart block
Sinus bradycardia
Suddenly serious symptoms of heart failure
Occasional Numbness
Prickling
Tingling of fingers and toes
Asthma
Asthma attack
Liver problems
kidney disease with the reduction in kidney function
Severe renal impairment
Psoriasis
Blood circulation failure due to the serious heart condition
Pregnancy
Anaphylactic shock due to Allergy Shots
Second or third degree AV block not controlled with pace-maker.;
Hypersensitivity to the active substance (betaxolol),
Reactive airway disease including severe bronchial asthma or a history of severe bronchial asthma, severe chronic obstructive pulmonary disease.

Dosage of Betaxolol

Intraocular Hypertension

0.25% suspension: One drop in the affected eye(s) twice a day
0.5% solution: One to two drops in the affected eye(s) twice a day

Glaucoma (Open Angle)

0.25% suspension: One drop in the affected eye(s) twice a day
0.5% solution: One to two drops in the affected eye(s) twice a day

Pediatric Dose for Intraocular Hypertension

0.25% suspension: One drop in the affected eye(s) twice a day

Side Effects of Betaxolol

The most common

Heart failure, chest pain, a slow heart rate, heart block, heart disease, or any other heart problems
Breathing disorders, such as bronchitis, asthma, sleep apnea, or chronic obstructive pulmonary disease (COPD)
A dry cough
Dizziness and light-headedness due to low blood pressure
Fatigue, especially in the early stages
Mouth dryness in the early stages
The most common (a burning feeling in the chest, behind the breastbone or gullet)
Abdominal or stomach pain
Constipation
High blood pressure
Nausea, vomiting,
painful or swollen gums
numbness or heavy feeling in the jaw
dull, aching pain in the hip, groin, or thigh
stomach pain,
a headache,
reversible hair loss or thinning, and
fever.

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Common

chills or fever
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
excessive sweating
sudden drowsiness or need to sleep
coughing up blood
liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
hallucinations
a headache
irritability
lightheadedness
cold and clammy skin
fast and shallow breathing
swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
fast or abnormal heart rate or palpitations
loss of appetite
lower back, side, or stomach pain
mental depression
muscle pain or cramps

Drugs interactions of Betaxolol

Betaxolol may interact with following drugs, supplements, & may change the efficacy of drugs

antidiabetes medications (e.g., insulin, metformin, gliclazide)
beta-2 agonists (e.g., formoterol, salmeterol, salbutamol)
bosutinib
Beta-blocker eye drops, betaxolol, carteolol, levobunolol , metipranolol,
Calcium channel blockers, such as Cardizem, diltiazem; nifedipine; and verapamil
Diabetes medication
bupropion
calcium channel blocking agents (e.g., diltiazem, verapamil)
cimetidine
cyclosporine
fluoxetine
MAO inhibitors (e.g., phenelzine, tranylcypromine)
medications that affect heart rhythm
medications that lower blood pressure
nitroglycerin
paroxetine
rituximab
tricyclic antidepressants (e.g., amitriptyline, nortriptyline)

Pregnancy & Lactation

Pregnancy

There are no adequate data for the use of betaxolol in pregnant women. Betaxolol should not be used during pregnancy unless clearly necessary.

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Epidemiological studies have not revealed malformative effects but show a risk for intra uterine growth retardation when beta-blockers are administered by the oral route. In addition, signs and symptoms of beta-blockade (e.g. bradycardia, hypotension, respiratory distress, and hypoglycemia) have been observed in the neonate when beta-blockers have been administered until delivery. If Betaxolol Eye Drops is administered until delivery, the neonate should be carefully monitored during the first days of life.

Lactation

Beta-blockers are excreted in breast milk, having the potential to cause serious undesirable effects in the infant of the nursing mother. However, at therapeutic doses of betaxolol in eye drops, it is not likely that sufficient amounts would be present in breast milk to produce clinical symptoms of beta-blockade in the infant.