Bisoprolol

• (RS ) -1 - [4 - (2- Isopropoxyethoxymethyl ) phenoxy] - 3- isopropylamino -2-propanol (IUPAC)
• Bisoprololum (Latin )

• 66722-44-9
• 104344-23-2 (2:1 fumarate, also called " hemi " )

C07AB07

β -adrenergic receptor blocker

Selective blockade of β1 - receptors

100 ° C ( as hemifumarate )

Water: 2.24 g · l-1 (25 ° C)

Attention

Template: Infobox chemical / molecular formula search available

Bisoprolol is a 1:1 mixture of two chemical compounds from the groups of aromatic compounds, and phenol ethers of the alcohols. It is used in medicine as a drug of the group of selective β1 - adrenergic receptor ( beta-blockers ) for the treatment of hypertension, angina pectoris, chronic heart failure and tachycardia. The chiral compound is used as a racemate, i.e., as a 1:1 mixture of the two enantiomers. The active stereoisomer ( eutomer ) is the ( S)-form of bisoprolol.

Clinical information

Areas of application (indications )

Bisoprolol is used to treat arterial hypertension, angina pectoris and chronic heart failure. To improve compliance and simplification of therapy Bisoprolol is in a fixed combination with the diuretic hydrochlorothiazide in also graded potencies available.

Contraindications

The drug should not be used in bronchial asthma, with slow heart rhythm ( bradycardia), for the use of MAO inhibitors, with hypotension, in severe heart failure with incipient cardiogenic shock and in diabetes mellitus.

Adverse effects (side effects)

It can cause the following side effects: circulatory disorders, low blood pressure, headaches, psoriasis psoriasis, lowering of heart rate (bradycardia ), dizziness, fatigue, sleep disturbances, mood swings, confusion, hallucinations, bronchospasm, dry eyes, increased sweating, erectile dysfunction and Others

Pharmacological properties

Bisoprolol is a long-acting β - blocker, which preferentially binds to β1 - adrenergic receptors. It acts on the heart frequency lowering inotropic and negative. Because of its lipophilicity bisoprolol also has central nervous system effects. Such as carvedilol it has no intrinsic sympathomimetic activity (ISA).

After oral administration of β - blockers is rapidly absorbed with a bioavailability of about 90%. The ingestion of doses in the range of 10 to 100 mg lead after about 3 h to maximum plasma concentration. The half-life is 10 to 11 h, with half of the substance unchanged by the kidneys, and the rest is eliminated by decomposition in the liver. The active ingredient is used as a racemate, wherein the enantiomers of drugs usually have different pharmacological properties and effects.

Market significance

With around 515 million DDD was after metoprolol, bisoprolol in 2007, the second most frequently used β - blockers in Germany. Overall, the number of prescribed doses has almost tripled (after DDD) of beta-blockers 1998-2007.

Trade names

Bilol (CH), Bisacardiol (A), Bisocor (A), Concor (D, A, CH), Concor COR ( D, A), Jutabis (D), Rivacor (A ), numerous generics (D, A, CH )

In combination with hydrochlorothiazide: Concor Plus (D, CH), Bilol comp ( CH), bisoprolol comp ( D), bisoprolol generic HCT (D), Lodoz (CH), Rivacor plus (A)