How and where to order Propranolol (Inderal, Inderal-LA, Innopran-XL) 10 mg, 20 mg, 40 mg, 80 mg tablets or capsules online:
INNOPRAN-XL (PROPRANOLOL HYDROCHLORIDE): PHARMACOKINETICS (see "References")
InnoPran-XL (Propranolol HCl) is highly lipophilic and is almost completely absorbed after oral administration. However, it undergoes high first-pass metabolism by the liver and on average, only about 25% of propranolol reaches the systemic circulation.
A single-dose, food-effect study in 36 healthy subjects showed that a high fat meal administered with InnoPran-XL at 10 p.m., increased the lag time from 3 to 5 hours and the time to reach the maximum concentration from 11.5 to 15.4 hours, under fed conditions, with no effect on the AUC.
Following multiple-dose administration of InnoPran-XL (Propranolol HCl) capsules at 10 p.m. under fasting conditions, the steady state lag time was between 4 and 5 hours and propranolol hydrochloride peak plasma concentrations were reached approximately 12 to 14 hours after dosing. Propranolol trough levels were achieved 24 to 27 hours after dosing, and persisted for 3 to 5 hours after the next dose. The elimination half-life of propranolol hydrochloride was approximately 8 hours.
The plasma levels of propranolol showed dose-proportional increases after single and multiple administrations of 80, 120, and 160 mg of InnoPran-XL (Propranolol Hydrochloride).
At steady state, the bioavailability of a 160 mg dose of InnoPran-XL and Propranolol Hydrochloride long-acting capsules did not differ significantly.
Approximately 90% of circulating propranolol is bound to plasma proteins (albumin and alpha1 acid glycoprotein). The binding is enantiomer-selective. The S-isomer is preferentially bound to alpha1 glycoprotein and the R-isomer preferentially bound to albumin. The volume of distribution of propranolol is approximately 4 liters.
Metabolism and Elimination
Propranolol is extensively metabolized with most metabolites appearing in the urine. InnoPran-XL (Propranolol Hydrochloride) capsules are metabolized through 3 primary routes: Aromatic hydroxylation (mainly 4-hydroxylation), N-dealkylation followed by further side-chain oxidation, and direct glucuronidation. It has been estimated that the percentage contributions of these routes to total metabolism are 42%, 41%, and 17%, respectively, but with considerable variability between individuals. The 4 major metabolites are propranolol glucuronide, naphthyloxylactic acid, and glucuronic acid and sulfate conjugates of 4-hydroxy propranolol.
In vitro studies have indicated that the aromatic hydroxylation of propranolol is catalyzed mainly by polymorphic CYP2D6. Side-chain oxidation is mediated mainly by CYP1A2 and to some extent by CYP2D6. 4-hydroxy propranolol is a weak inhibitor of CYP2D6.
Propranolol is also a substrate for CYP2C19 and a substrate for the intestinal efflux transporter, p-glycoprotein (p-gp). Studies suggest however that p-gp is not dose-limiting for intestinal absorption of propranolol in the usual therapeutic dose range.
In healthy subjects, no difference was observed between CYP2D6 extensive metabolizers (EMs) and poor metabolizers (PMs) with respect to oral clearance or elimination half-life. Partial clearance to 4-hydroxy propranolol was significantly higher and to naphthyloxylactic acid was significantly lower in EMs than PMs.
Of the 2 enantiomers of propranolol, the S-enantiomer blocks beta-adrenergic receptors. In normal subjects receiving oral doses of racemic propranolol, S-enantiomer concentrations exceeded those of the R-enantiomer by 40 to 90% as a result of stereoselective hepatic metabolism.
InnoPran-XL prescribing information
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