Propanolol, metabolism

Kinetic parameters of metabolism of fluorinated analogues of propanolol by a cytochrome enzyme (recombinant CYP1A2) have been determined. They clearly indicate that the A/-dealkylation was almost tenfold lower for the A/-CH2CF3... [Pg.568]

Fig. 12. Metabolism of fluorinated analogues of propanolol by recombinant CYP1A2 [52].

Kinetic parameters of metabolism of fluorinated analogues of propanolol by cytochrome enzyme (recombinant CYP1A2) have been determined. They clearly indicate that the A-dealkylation process was 10-fold lower for the N—CH2CF3 compound with respect to propanolol itself. Hydroxylation of the naphthalene ring process is not observed in the case of propanolol but it becomes the major process with the fluoro analogue (Figure 3.13)." The same decreased metabohsm trend has also been observed with lower pKa values for CYP2D6 cytochrome enzyme." ... [Pg.86]

Lately it has been found that it takes ten times as much haloperidol to relieve schizophrenic symptoms in Caucasians as it does in the inhabitants of Taiwan. And when using propanolol for the control of blood pressure, men of Chinese descent metabolize it more efficiently than Caucasians and could use lower doses for comparable effects. [Pg.52]

Upthagrove, A.L. and Nelson, W.L., Importance of amine pKa and distribution coefficient in the metabolism of fluorinated propanolol analogs metabolism by CYP1A2, Drug Metab. Disposition, 29, 1389-1395, 2001. [Pg.236]

MEXILETINE BETA-BLOCKERS Risk of bradycardia (occasionally severe), 1 BP and heart failure Additive negative inotropic and chronotropic effects. Also, mexiletine is known to inhibit CYP1 A2-mediated metabolism of propanolol Monitor PR, BP and ECG closely watch for development of heart failure... [Pg.24]

PROPAFENONE METOPROLOL, PROPANOLOL t plasma levels of propranolol and metoprolol Propafenone is extensively metabolized by CYP2D6 enzymes and interferes with the metabolism of propranolol and metoprolol Watch for propranolol and metoprolol toxicity 1 doses accordingly... [Pg.32]

VASODILATOR ANTIHYPERTENSIVES BETA-BLOCKERS t hypotensive effect Additive hypotensive effect with diazoxide, hydralazine, minoxidil and sodium nitroprusside. In addition, hydralazine may T the bioavailability of beta-blockers with a high first-pass metabolism (e.g. propanolol and metoprolol), possibly due to alterations in hepatic blood flow or inhibited hepatic metabolism Monitor BP closely... [Pg.47]

BETA-BLOCKERS OPIOIDS 1. Risk of t plasma concentrations and effects of labetalol, metoprolol and propranolol t systemic effects of timolol eye drops 2. t plasma concentrations of esmolol when morphine is added 3. t plasma concentrations of metoprolol and propranolol when dextro-propoxyphene is added 1. Methadone inhibits CYP2D6, which metabolizes these beta-blockers 2. Unknown 3. i hepatic clearance of metoprolol and propanolol 1. Monitor BP at least weekly until stable 2. Monitor BP closely 3. Monitor BP at least weekly until stable. Warn patients to report symptoms of hypotension (lightheadedness, dizziness on standing, etc.)... [Pg.65]

BETA-BLOCKERS RIFAMPICIN L plasma concentrations and efficacy of bisoprolol, carvedilol, celiprolol, metoprolol and propanolol Rifampicin induces hepatic enzymes (e.g. CYP2C19), which t metabolism of the beta-blockers in addition, it may also t P-gp expression Monitor PR and BP watch for poor response to beta-blockers... [Pg.66]

BETA-BLOCKERS CYTOTOXICS Imatinib may cause an t in plasma concentrations of metoprolol, propanolol and timolol, with a risk of toxic effects Imatinib is a potent inhibitor of CYP2D6 isoenzymes, which metabolize beta-blockers Monitor for clinical efficacy and toxicity of beta-adrenergic blockers... [Pg.66]

LABETALOL PROPANOLOL IMIPRAMINE T imipramine levels with labetalol and propanolol Uncertain at present. Postulated that imipramine metabolism 1 by competition at CYP2D6 and CYP2C8 Monitor plasma levels of imipramine when initiating beta-blocker therapy... [Pg.68]

BETA-BLOCKERS VENLAFAXINE T plasma concentrations and efficacy of metoprolol, propranolol and timolol Venlafaxine inhibits CYP2D6-mediated metabolism of metoprolol, propanolol and timolol Monitor PR and BP at least weekly watch for metoprolol toxicity (in particular, toss of its cardioselectivity) and propanolol toxicity... [Pg.68]

BETA-BLOCKERS BARBITURATES Regular barbiturate use may t elimination of those beta-blockers metabolized by the liver (metoprolol, propanolol, timolol) Barbiturates induce CYP1A2-, CYP2C9- and CYP2C19-mediated metabolism of propanolol Monitor BP at least weekly until stable and watch for t BP... [Pg.69]

PROPANOLOL, TIMOLOL CHLORPROMAZINE, HALOPERIDOL t plasma concentrations and efficacy of both chlorpromazine and propranolol during co-administration Propanolol and chlorpromazine mutually inhibit each other s hepatic metabolism. Haloperidol inhibits CYP2D6-mediated metabolism of propanolol and timolol Watch for toxic effects of chlorpromazine and propranolol 1 doses accordingly... [Pg.71]

BETA-BLOCKERS RITONAVIR, TIPRANAVIR t adverse effects of carvedilol, metoprolol, propanolol and timolol Inhibition of CYP2D6-mediated metabolism of these beta-blockers and CYP2C19-mediated metabolism of propanolol Use an alternative beta-blocker if possible if not, monitor closely... [Pg.72]

BETA-BLOCKERS VERAPAMIL 1. Risk of cardiac arrest when parenteral verapamil is given to patients on beta-blockers 2. Risk of bradycardias when both are given orally Additive effect. Also, verapamil inhibits CYP1 A2-mediated metabolism of propanolol 1. Do not administer intravenous verapamil to patients taking beta-blockers 2. Monitor ECG and BP carefully when both are given orally... [Pg.73]

PROPANOLOL 5-HT1 AGONISTS -RIZATRIPTAN Plasma levels of rizatriptan almost doubled during propranolol therapy Propanolol inhibits the metabolism of rizatriptan Initiate therapy with 5 mg rizatriptan and do not exceed 10 mg in 24 hours. The manufacturers recommend separating doses by 2 hours, although this has not been borne out by the studies... [Pg.74]

IMATINIB 1. ANTIARRHYTHMICS -flecainide, mexiletine, propafenone 2. ANTIDEPRESSANTS - fluoxetine, paroxetine, TCAs, trazodone, venlafaxine 3. ANTIPSYCHOTICS -clozapine, haloperidol, perphenazine, risperidone, thioridazine 4. BETA-BLOCKERS - metoprolol, propanolol, timolol 5. DONEPEZIL 6. METHAMPHETAMINE Imatinib may cause t plasma concentrations of these drugs, with a risk of toxic effects Inhibition of CYP2D6-mediated metabolism of these drugs Watch for early features of toxicity of these drugs... [Pg.312]

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