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Bis Beta 2.5/5
Bis Beta
Systematic (IUPAC) name
(RS)-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}3-(isopropylamino)propan-2-ol
Bioavailability
>90%
Protein binding
30%[1]
Metabolism
Half-life
50% Hepatic
10–12 hours[2]
Therapeutic considerations
Licence data
Routes
US FDA:link
oral
Bis Beta is a drug belonging to the group of beta blockers, a class of drugs used
primarily in cardiovascular diseases. More specifically, it is a selective type β1
adrenergic receptor blocker. The FDA approved Oral Tablets (Bis Beta Fumarate) as a
new molecular entity on July 31, 1992.
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Clinical use
Bis Beta is a beta-adrenoceptor blocking drug (beta-blocker). It is approximately equally
hydrophilic and lipophilic, and is readily soluble in water, methanol, ethanol, and
chloroform. Bis Beta is available as 5 and 10 mg tablets for oral administration.
Many beta-blockers are now available and in general they are all equally effective.
There are, however, differences between them which may affect choice in treating
particular diseases or individual patients.
Beta-blockers with a relatively short duration of action have to be given two or three
times daily. Many of these are, however, available in modified-release formulations so
that administration once daily is adequate for hypertension. For angina twice-daily
treatment may sometimes be needed even with a modified-release formulation. Some
beta-blockers such as atenolol, Bis Beta, carvedilol, celiprolol, and nadolol have an
intrinsically longer duration of action and need to be given only once daily.
Cautions
Beta-blockers can precipitate asthma and this effect can be dangerous. Beta-blockers
should be avoided in patients with a history of asthma or bronchospasm; if there is no
alternative, a cardioselective beta-blocker can be used with extreme caution under
specialist supervision. Atenolol, Bis Beta, metoprolol, nebivolol, and (to a lesser extent)
acebutolol, have less effect on the beta2 (bronchial) receptors and are, therefore,
relatively cardioselective, but they are not cardiospecific. They have a lesser effect on
airways resistance but are not free of this side effect.
Side effects
Beta-blockers are also associated with fatigue, coldness of the extremities (may be less
common with those with ISA, see above), and sleep disturbances with nightmares (may
be less common with the water-soluble beta-blockers, see above).
Indications
Bis Beta can be used to treat cardiovascular diseases such as hypertension, coronary
heart disease, arrhythmias, ischemic heart diseases and treatment of myocardial
infarction after the acute event. Patients with compensated congestive heart failure may
be treated with Bis Beta as a comedication (usually together with an ACE inhibitor, a
diuretic and a digitalis-glycosid, if indicated). In patients with congestive heart failure, it
reduces the need for and the consumption of oxygen of the heart muscle. It is very
important to start with low doses, as Bis Beta reduces also the muscular power of the
heart, which is an undesired effect in congestive heart failure.
The drug is also used to treat other conditions, including dysautonomia, anxiety and
hyperthyroidism (over active thyroid gland).
Bis Beta will give a positive result in doping tests
Pharmacology and biochemistry
Selectivity of various β-blockers
β1 Selectivity
Bis Beta has a higher degree of β1-selectivity compared to other β1-selective βblockers such as atenolol, metoprolol and betaxolol. However Nebivolol is
approximately 3.5 times more β1-selective
Antihypertensive effect
Bis Beta has a stronger antihypertensive effect than propranolol
Cardioprotection
Bis Beta in animal models has been shown to be cardioprotective
Renin-angiotensin system
Bis Beta inhibits renin secretion by about 65% and tachycardia by about 35%
Pharmacology of side effects
In animal testing Bis Beta compared to propranolol has shown less sedative effects and
only slightly reduced glucose tolerance.
Overdosage
Acute overdosage is often manifested by nausea, emesis, asthenia, diarrhea,
bradycardia and hypotension. Plasma, serum or blood concentrations of Bis Beta may
be measured to confirm a diagnosis of poisoning in hospitalized patients or to aid in the
medicolegal investigation of fatalities.