Stereochemistry | RACEMIC |
Molecular Formula | C15H25NO3 |
Molecular Weight | 267.3639 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COCCC1=CC=C(OCC(O)CNC(C)C)C=C1
InChI
InChIKey=IUBSYMUCCVWXPE-UHFFFAOYSA-N
InChI=1S/C15H25NO3/c1-12(2)16-10-14(17)11-19-15-6-4-13(5-7-15)8-9-18-3/h4-7,12,14,16-17H,8-11H2,1-3H3
Molecular Formula | C15H25NO3 |
Molecular Weight | 267.3639 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
Mrtoprolol is a beta-adrenergic receptor blocking agent. In vitro and in vivo animal studies have shown that it has a preferential effect
on beta-1 adrenoreceptors, chiefly located in cardiac muscle. Clinical pharmacology studies have confirmed the beta-blocking activity of metoprolol in man, as shown by (1) reduction in heart rate and cardiac output at rest and upon exercise, (2) reduction of systolic blood pressure upon exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia. Mrtoprolol is indicated for the treatment of hypertension, angina pectoris and myocardial infarction
CNS Activity
Originator
Approval Year
Doses
AEs
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
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Drug as perpetrator
Drug as victim
Tox targets
Sourcing
Sample Use Guides
Hypertension
The dosage of Lopressor should be individualized. Lopressor should be taken with or immediately following meals.
The usual initial dosage is 100 mg daily in single or divided doses, whether used alone or added to a diuretic. The dosage may be
increased at weekly (or longer) intervals until optimum blood pressure reduction is achieved. In general, the maximum effect of
any given dosage level will be apparent after 1 week of therapy. The effective dosage range is 100-450 mg per day. Dosages above
450 mg per day have not been studied. While once-daily dosing is effective and can maintain a reduction in blood pressure throughout
the day, lower doses (especially 100 mg) may not maintain a full effect at the end of the 24-hour period, and larger or more frequent
daily doses may be required. This can be evaluated by measuring blood pressure near the end of the dosing interval to determine
whether satisfactory control is being maintained throughout the day. Beta1 selectivity diminishes as the dose of Lopressor is increased.
Angina Pectoris
The dosage of Lopressor should be individualized. Lopressor should be taken with or immediately following meals.
The usual initial dosage is 100 mg daily, given in two divided doses. The dosage may be gradually increased at weekly intervals
until optimum clinical response has been obtained or there is pronounced slowing of the heart rate. The effective dosage range is
100-400 mg per day. Dosages above 400 mg per day have not been studied. If treatment is to be discontinued, the dosage should be
reduced gradually over a period of 1-2 weeks (see WARNINGS).
Myocardial Infarction
Early Treatment: During the early phase of definite or suspected acute myocardial infarction, treatment with Lopressor can be
initiated as soon as possible after the patient’s arrival in the hospital. Such treatment should be initiated in a coronary care or similar
unit immediately after the patient’s hemodynamic condition has stabilized.
Treatment in this early phase should begin with the intravenous administration of three bolus injections of 5 mg of Lopressor each; the
injections should be given at approximately 2-minute intervals. During the intravenous administration of Lopressor, blood pressure,
heart rate, and electrocardiogram should be carefully monitored.
In patients who tolerate the full intravenous dose (15 mg), Lopressor tablets, 50 mg every 6 hours, should be initiated 15 minutes after
the last intravenous dose and continued for 48 hours. Thereafter, patients should receive a maintenance dosage of 100 mg twice daily
(see Late Treatment below).
Patients who appear not to tolerate the full intravenous dose should be started on Lopressor tablets either 25 mg or 50 mg every
6 hours (depending on the degree of intolerance) 15 minutes after the last intravenous dose or as soon as their clinical condition
allows. In patients with severe intolerance, treatment with Lopressor should be discontinued (see WARNINGS).
Late Treatment: Patients with contraindications to treatment during the early phase of suspected or definite myocardial infarction,
patients who appear not to tolerate the full early treatment, and patients in whom the physician wishes to delay therapy for any other
reason should be started on Lopressor tablets, 100 mg twice daily, as soon as their clinical condition allows. Therapy should be
continued for at least 3 months. Although the efficacy of Lopressor beyond 3 months has not been conclusively established, data from
studies with other beta blockers suggest that treatment should be continued for 1-3 years.
Note: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration,
whenever solution and container permit.
Route of Administration:
Other