Toprol XL drug interactions: Difference between revisions

Metoprolol
Clinical data
Trade names	Lopressor, Toprol-xl
AHFS/Drugs.com	Monograph
MedlinePlus	a682864
[[Regulation of therapeutic goods \|Template:Engvar data]]	US FDA: Metoprolol;
Pregnancy; category	AU: C ; US: C (Risk not ruled out) ; ;
Routes of; administration	Oral, IV
ATC code	C07AB02 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	12%
Metabolism	Hepatic via CYP2D6, CYP3A4
Elimination half-life	3-7 hours
Excretion	Renal
Identifiers
	IUPAC name (RS)-1-(Isopropylamino)-3-[4-(2-methoxyethyl)phenoxy]propan-2-ol;
CAS Number	51384-51-1 ;
PubChem CID	4171;
IUPHAR/BPS	553;
DrugBank	DB00264 ;
ChemSpider	4027 ;
UNII	GEB06NHM23;
KEGG	D02358 ;
ChEBI	CHEBI:6904 ;
ChEMBL	ChEMBL13 ;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C15H25NO3
Molar mass	267.364 g/mol
3D model (JSmol)	Interactive image;
Melting point	120 °C (248 °F)
	SMILES O(c1ccc(cc1)CCOC)CC(O)CNC(C)C;
	InChI 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 ; Key:IUBSYMUCCVWXPE-UHFFFAOYSA-N ;
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VisualWikitext

Revision as of 19:58, 13 March 2014

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Catecholamine Depleting Drugs

Catecholamine depleting drugs (eg, reserpine, monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents. Observe patients treated with TOPROL-XL plus a catecholamine depletor for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.

CYP2D6 Inhibitors

Drugs that inhibit CYP2D6 such as quinidine, fluoxetine, paroxetine, and propafenone are likely to increase metoprolol concentration. In healthy subjects with CYP2D6 extensive metabolizer phenotype, coadministration of quinidine 100 mg and immediate-release metoprolol 200 mg tripled the concentration of S-metoprolol and doubled the metoprolol elimination half-life. In four patients with cardiovascular disease, coadministration of propafenone 150 mg t.i.d. with immediate-release metoprolol 50 mg t.i.d. resulted in two- to five-fold increases in the steady-state concentration of metoprolol. These increases in plasma concentration would decrease the cardioselectivity of metoprolol.

Digitalis, Clonidine, and Calcium Channel Blockers

Digitalis glycosides, clonidine, diltiazem and verapamil slow atrioventricular conduction and decrease heart rate. Concomitant use with beta blockers can increase the risk of bradycardia.

If clonidine and a beta blocker, such as metoprolol are coadministered, withdraw the beta-blocker several days before the gradual withdrawal of clonidine because beta-blockers may exacerbate the rebound hypertension that can follow the withdrawal of clonidine. If replacing clonidine by beta-blocker therapy, delay the introduction of beta-blockers for several days after clonidine administration has stopped [see Warnings and Precautions (5.11)].^[1]

References

↑ "TOPROL XL (METOPROLOL SUCCINATE) TABLET, EXTENDED RELEASE [BRYANT RANCH PREPACK]".

Adapted from the FDA Package Insert.

[dailymed.nlm.nih.gov-1] "TOPROL XL (METOPROLOL SUCCINATE) TABLET, EXTENDED RELEASE [BRYANT RANCH PREPACK]".

[1]

@@ Line 9: / Line 9: @@
 ====CYP2D6 Inhibitors====
-Drugs that inhibit [[CYP]]2D6 such as [[quinidine]], [[fluoxetine]], [[paroxetine]], and propafenone are likely to increase metoprolol concentration. In healthy subjects with CYP2D6 extensive metabolizer phenotype, coadministration of quinidine 100 mg and immediate-release metoprolol 200 mg tripled the concentration of S-metoprolol and doubled the metoprolol elimination half-life. In four patients with cardiovascular disease, coadministration of propafenone 150 mg t.i.d. with immediate-release metoprolol 50 mg t.i.d. resulted in two- to five-fold increases in the steady-state concentration of metoprolol. These increases in plasma concentration would decrease the cardioselectivity of metoprolol.
+Drugs that inhibit [[CYP2D6]] such as [[quinidine]], [[fluoxetine]], [[paroxetine]], and propafenone are likely to increase metoprolol concentration. In healthy subjects with CYP2D6 extensive metabolizer phenotype, coadministration of quinidine 100 mg and immediate-release metoprolol 200 mg tripled the concentration of S-metoprolol and doubled the metoprolol elimination half-life. In four patients with cardiovascular disease, coadministration of propafenone 150 mg t.i.d. with immediate-release metoprolol 50 mg t.i.d. resulted in two- to five-fold increases in the steady-state concentration of metoprolol. These increases in plasma concentration would decrease the cardioselectivity of metoprolol.
 ====Digitalis, Clonidine, and Calcium Channel Blockers====