Imipramine Propranolol

Alpharacid glycoprotein exists in concentrations that are 50 to 100 times lower than those of albumin. Basic drugs (quinidine, imipramine, propranolol, and lidocaine) bind to the single site present on alpharacid glycoprotein. 

Buspirone Imipramine Propranolol Verapamil SYR110155 SYR110180 SYR110182 SYR110184... 

VERAPAMIL DILTIAZEM PROMETHAZINE PHENAZOPYRIDINE DESIPRAMINE PROGESTERONE IMIPRAMINE CHLORPROMAZINE GRISEOFULVIN PROPRANOLOL CARBAMAZEPINE QUININE IBUPROFEN PIROXICAM PRIMAQUINE CAFFEINE ANTIPYRINE METOPROLOL NAPROXEN KETOPROFEN SULPIRIDE TERBUTALINE FUROSEMIDE SULPHASALAZINE RANITIDINE HYDROCHLOROTHIAZIDE ATENOLOL AMIOLORIDE... 

Fig. 4.3 CSF concentration/free (unbound) plasma concentration ratios for neutral and basic drugs 1, ritropirronium 2, atenolol 3, sulpiride 4, morphine 5, cimetidine 6, meto-prolol 7, atropine 8, tacrine 9, digoxin 10, propranolol 11, carbamazepine 12, ondansetron 13, diazepam 14, imipramine 15, digitonin 16, chlorpromazine and acidic drugs, a, salicylic acid b, ketoprofen c, oxyphenbutazone and d, indomethacin compared to log D.

Smoking cessation, with or without nicotine substitutes, may alter response to concomitant medication in ex-smokers. Smoking may affect alcohol, benzodiazepines, beta-adrenergic blockers, caffeine, clozapine, fluvoxamine, olanzapine, tacrine, theophylline, clorazepate, lidocaine (oral), estradiol, flecanide, imipramine, heparin, insulin, mexiletine, opioids, propranolol, catecholamines, and cortisol. 

Substrates Inhibitors Inducers CYP1A2 Acetaminophen, caffeine, clozapine, imipramine, theophylline, propranolol Most fluoroquinolone antibiotics, fluvoxamine, cimetidine Tobacco smoking, charcoal-broiled foods, cruciferous vegetables, omeprazole... 

Propranolol C 2 Nortriptyline 3 Doxepin 4 Imipramin 5 Amitriptyline 6 Trimipramin 7 Clomipramin... 

Drugs that may require dosage reduction with smoking cessation acetaminophen, caffeine, imipramine, oxazepam, penfazocine, propranolol, fheophylline, insulin, prazocin, labetalol... 

Cimetidine Lidocaine, propranolol, verapamil, imipramine Increased absorption... 

Cyt 2D6 metabolizes haloperidol, risperidone, thioridazine, sertindole, olanzapine and clozapine common substrates - fluoxetine, paroxetine, sertraline, venlafaxine, amitriptyline, clomipramine, desipramine, imipramine, nortriptyline, propranolol, metoprolol, timolol, codeine, encainide, flecanide. Common inhibitors - paroxetine, sertraline, fluoxetine. 

Fig. 4.5 Relationship between the Kp value of quinidine (A), propranolol (B), and imipramine (C) and the concentration of PS in rat tissue. 1, lung 2, spleen 3, kidney 4, pancreas 5, liver ...

Tab. 4.27 Binding parameters of propranolol, imipramine and quinidine to individual standard phospholipids3 (Adapted from Tab. 3 of ref. 92)...

Obach RS. 1997. Nonspecific binding to microsomes impact on scale-up of in vitro intrinsic clearance to hepatic clearance as assessed through examination of warfarin, imipramine, and propranolol. Drug Metab Dispos 25 1359-1369. 

Amitriptylline (B) Bupivacaine (B) Chlorpromazine (B) Diltiazem (B) Imipramine (B) Nortriptyline (B) Perazine (B) Propranolol (B) Quinidine (B)... 

Cancer and burn injury are associated with increased concentrations of AAG and decreased concentrations of albumin in plasma. For AAG-bound drugs, a 20-30 /o decrease in the unbound fractions of lidocaine, methadone,propranolol,and imipramine is observed, whereas the unbound fractions of albumin-bound drugs increase for tolbutamide (30 /o),f diazepam (180%),[12 1 and phenytoin (150%).[ 1... 

CYP2C19 Benzodiazepines diazepam Antidepressants imipramine, amitriptyline, clomipramine, citalopram Others propranolol, hexobarbital, mephobarbital, proguanil, omeprazole, S-mephenytoin 2 no activity 23%-39% in Asians 13% in Caucasians 25% in African Americans 3 no activity 6%-10% in Asians 0% in others... 

CYP2D6 Antidepressants amitriptyline, clomipramine, imipramine, desipramine, nortriptyline, trimipramine, N-desmethyl-clomipramine, fluoxetine, norfluoxetine, paroxetine, venlafaxine, sertraline Neuroleptics chlorpromazine, thioridazine, perphenazine, haloperidol, reduced haloperidol, risperidone, clozapine, sertindole Others codeine, opiate, propranolol, dextromethorphan 4 no activity 25% in Caucasians 0%-10% in others 5 no activity 2%-10% in all groups 10 reduced activity 47%-70% in Asians <5% in others 17 reduced activity 25%-40% in blacks 0% in others 2XN increased activity 19%-29% in Arabs and Ethiopians <5% in others... 

Clinically important, potentially hazardous interactions with acebutolol, amitriptyline, amoxapine, atenolol, betaxolol, carteolol, clomipramine, desipramine, dexmethylphenidate, doxepin, esmolol, imipramine, insulin detemir, insulin glulisine, metoprolol, nadolol, nortriptyline, oxprenolol, penbutolol, pindolol, propranolol, protriptyline, sulpiride, timolol, tricyclic antidepressants, trimipramine, verapamil... 

PAMPA-pKa fiux optimized design (pOD)-permeabiiity Iso-pH mapping unstirred PAMPA was used to measure the effective permeability, Pe, as a function of pH from 3 to 10, of five weak monoprotic acids (ibuprofen, naproxen, ketoprofen, salicylic acid, benzoic acid), an ampholyte (piroxicam), five monoprotic weak bases (imipramine, verapamil, propranolol, phenazopyridine, metoprolol), and a diprotic weak base (quinine). The intrinsic permeability, Po, the UWL permeability, Pu, and the apparent pKa (pKa.fiux) were determined from the pH dependence of log Pg. The underlying permeability-pH equations were derived for multiprotic weak acids, weak bases, and ampholytes. The average thickness of the UWL on each side of the membrane was estimated to be nearly 2000 p, somewhat larger than that found in Caco-2 permeability assays (unstirred). As the UWL thickness in the human intestine is believed to be about forty times smaller, it is critical to correct the in vitro permeability data for the effect of the UWL. Without such correction, the in vitro permeability coefficient of lipophilic molecules would be indicative only of the property of water. In single-pH PAMPA (e.g., pH 7.4), the uncertainty of the UWL contribution can be minimized if a specially selected pH (possibly different from 7.4) were used in the assay. From the analysis of the shapes of the log Pe-pH plots, a method to improve the selection of the assay pH, called pOD-PAMPA, was described and tested. From an optimally selected assay pH, it is possible to estimate Pg, as well as the entire membrane permeability-pH profile. 

Amitriptyline, barbiturates, chlorproguanil, citalopram, clomipramine, clozapine, cyclophosphamide, diazepam, hexobarbital, imipramine, pentamidine, phenobarbital, phenytoin, propranolol, quinine, (S)- and (Jf)-warfarin, zidovudine... 

Ajmaline, alprenolol, amiflamine, amphetamine, aprindine, captopril, chlorpheniramine, cinnarizine, citalopram, clomipramine, clozapine, codeine, desipramine, dolasteron, encainide, flecainide, fluoxetine, fluphenazine, haloperidol, hydrocordone, imipramine, loratidine, methoxyphenamine, 3,4-methylenedioxymethamphetamine, metoprolol, mexiletine, (S)- and (i )-mianserin, nifedipine, olanzapine, omeprazole, oxycodone, perhexiline, phenformin, propaphenone, propranolol, remoxipride, ritonavir, saquinavir, selegiline, tamsulosin, timolol, tomoxetine, tramadol, trifluperidol, zolpidem... 

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