ATENOLOL tablet

Χώρα: Ηνωμένες Πολιτείες

Γλώσσα: Αγγλικά

Πηγή: NLM (National Library of Medicine)

Δραστική ουσία:

atenolol (UNII: 50VV3VW0TI) (atenolol - UNII:50VV3VW0TI)

Διαθέσιμο από:

McKesson Contract Packaging

INN (Διεθνής Όνομα):

atenolol

Σύνθεση:

atenolol 25 mg

Τρόπος διάθεσης:

PRESCRIPTION DRUG

Καθεστώς αδειοδότησης:

Abbreviated New Drug Application

Αρχείο Π.Χ.Π.

ATENOLOL- ATENOLOL TABLET
MCKESSON CONTRACT PACKAGING
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ATENOLOL TABLETS, USP
DESCRIPTION
Atenolol, a synthetic, beta -selective (cardioselective)
adrenoreceptor blocking agent, may be
chemically described as benzeneacetamide,
4-[2’-hydroxy-3’-[(1-methylethyl)amino]propoxy]-. It has
the following structural formula:
Atenolol (free base) has a molecular weight of 266.34. It is a
relatively polar hydrophilic compound
with a water solubility of 26.5 mg/mL at 37°C and a log partition
coefficient (octanol/water) of 0.23. It
is freely soluble in 1N HCl (300 mg/mL at 25°C) and less soluble in
chloroform (3 mg/mL at 25°C).
Atenolol is available as 25, 50 or 100 mg tablets for oral
administration. Inactive ingredients include
colloidal silicon dioxide, magnesium stearate, microcrystalline
cellulose, and sodium starch glycolate.
CLINICAL PHARMACOLOGY
Atenolol is a beta -selective (cardioselective) beta-adrenergic
receptor blocking agent without
membrane stabilizing or intrinsic sympathomimetic (partial agonist)
activities. This preferential effect is
not absolute, however, and at higher doses, atenolol inhibits beta
-adrenoreceptors, chiefly located in
the bronchial and vascular musculature.
PHARMACOKINETICS AND METABOLISM
In man, absorption of an oral dose is rapid and consistent but
incomplete. Approximately 50% of an oral
dose is absorbed from the gastrointestinal tract, the remainder being
excreted unchanged in the feces.
Peak blood levels are reached between two (2) and four (4) hours after
ingestion. Unlike propranolol or
metoprolol, but like nadolol, atenolol undergoes little or no
metabolism by the liver, and the absorbed
portion is eliminated primarily by renal excretion. Over 85% of an
intravenous dose is excreted in urine
within 24 hours compared with approximately 50% for an oral dose.
Atenolol also differs from
propranolol in that only a small amount (6%-16%) is bound to proteins
in the plasma. This kinetic profile
results in relatively consistent plasma drug levels with about a
fourfold interp