Propranolol Diltiazem

CLASS 1 (amphiphilic) 3 diltiazem antipyrine labetolol glucose captopril L-dopa enalapril metoprolol propranolol phenylalanine... 

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. 20.13. Potential H-bonding energy, released upon interaction with the transmembrane domains of P-gp (in arbitrary energy units, EU) for progesterone (1), propranolol (2), amitriptyline (3), diltiazem (4), amiodarone (5), colchicine (7), gramicidin S (8), daunorubicin (9), vinblastine (10), cyclosporin A, in comparison with verapamil...

If patients are hemodynamicaUy stable, the focus should be directed toward control of ventricular rate. Drugs that slow conduction and increase refractoriness in the AV node should be used as initial therapy. In patients with normal LV function (left ventricular ejection fraction >40%), IV j3-blockers (propranolol, metoprolol, esmolol), diltiazem, or verapamil is recommended. If a high adrenergic state is the precipitating factor, IV /J-blockers can be highly effective and should be considered first. In patients with left ventricular ejection fraction <40%, IV diltiazem and verapamil... 

All chemicals were used as received. PDADMAC and PAMPS were obtained from Aldrich Chemical Co. (Milwaukee, WI). Diclofenac sodium, sodium sulfathiazole, labetalol HCl, propranolol HCl, verapamil HCl, and diltiazem HCl were purchased from Sigma Chemical (St. Louis, MO). Dextrose USP was obtained from Amend Co. (Irvinton, NJ). Water was distilled and deionized using a Nanopure purihcation system (Fischer Scientihc, Fair Lawn, NJ). Simulated intestinal fluid was prepared using a O.OIM phosphate buffer (sodium phosphate monobasic and potassium phosphate dibasic) at pH 7 and 5.5 with different amounts of NaCl to vary the ionic strength. Simulated gastric fluid (pH 1.5) was prepared with concentrated HCl with different amounts of NaCl to vary the ionic strength. 

The release kinetics from the tablets of the drug-polymer complexes were carried out in buffered release media containing 0.01 M phosphate and NaCl ranging from 0.2 M to 0.02 M at 37°C by the USP basket method at 100 rpm. Drug release was monitored on a HP 8452A diode-array spectrophotometer at 250, 306, 306, 270, 278, 278, and 274 nm for sodium diclofenac and sulfathiazole, labetalol HCl, propranolol HCl, verapamil HCl, and diltiazem HCl, respectively. 

The main drngs nsed for myocardial ischema therapy and for relieving pain in angina pectoris are nitrates and nitrites (nitroglycerin, isosorbide dinitrate, and pentaerythritol tetranitrate) snbstances that snppress adrenergic systems of the heart—j3-adrenoblockers (atenolol, methoprolol, propranolol, and nadolol), and Ca + channel blockers (verapamil, diltiazem, nifedipine, and nicardipine) as well as a few older drugs, in particular papaverine and dipyridamole. 

Drugs that may affect HMG-CoA reductase inhibitors include alcohol, amiodarone, antacids, azole antifungals, bile acid sequestrants, cimetidine, cyclosporine, diltiazem, erythromycin, gemfibrozil, isradipine, nefazodone, niacin, nicotinic acid, omeprazole, phenytoin, propranolol, protease inhibitors, ranitidine, rifampin, St. John s wort, and verapamil. 

Propranolol and nadolol also have been used successfully in combination with certain calcium entry blockers, particularly nifedipine, for the treatment of secondary angina. Caution should be used, however, when combining a p-blocker and a calcium channel blocker, such as verapamil or diltiazem, since the negative inotropic and chronotropic effects of this combination may lead to severe bradycardia, arteriovenous nodal block, or decompensated congestive heart failure. 

B. Both diltiazem and propranolol would produce the effects listed in A, C, D, and E. Only diltiazem would dilate vessels in spasm. Propranolol would tend to produce vasoconstriction, not vasodilation. 

The prominent depressant action of verapamil and diltiazem at the SA and A-V nodes finds use in specific arrhythmias. They are of proven efficacy in acute control and long-term management of paroxysmal supraventricular tachycardia (see Chapter 16).Their ability to inhibit conduction at the A-V node is employed in protecting ventricles from atrial tachyarrhythmias, often in combination with digitalis or propranolol. 

During the acute phase of thyrotoxicosis, B-adrenoceptor blocking agents without intrinsic sympathomimetic activity are extremely helpful. Propranolol, 20-40 mg orally every 6 hours, will control tachycardia, hypertension, and atrial fibrillation. Propranolol is gradually withdrawn as serum thyroxine levels return to normal. Diltiazem, 90-120 mg three or four times daily, can be used to control tachycardia in patients in whom blockers are contraindicated, eg, those with asthma. Other calcium channel blockers may not be as effective as diltiazem. Adequate nutrition and vitamin supplements are essential. Barbiturates accelerate T4 breakdown (by hepatic enzyme induction) and may be helpful both as sedatives and to lower T4... 

Drugs insoluble in intestinal fluids (acid soluble basic drugs) chlordiazepoxide, chlorpheniramine, cinnarizine, diazepam, diltiazem, meto-prolol, propranolol, quinidine, salbutamol, and verapamil. 

It is obvious that drugs such as nifedipine and both isosorbide-5-mononitrate and isosorbide dinitrate, which have non-specific, wide absorption sites and so are well absorbed along the entire GI tract, may not be suitable candidates for GRDDS. Also, drugs that are irritant to the gastric mucosa " and those undergoing significant first-pass metabolism may have some limitations. Relevant examples of the latter type are nifedipine, propranolol, levodopa, diltiazem, metopro-lol and 5-fluorouracil. 

Propranolol, verapamil, nifedipine, diltiazem, metoprolol, nicardipine, or labetolol. 

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

Stone PH, Gibson RS, Glasser SP, DeWood MA, Parker JD, Kawanishi DT, Crawford MH, Messineo FC, Shook TL, Raby K, et al. Comparison of propranolol, diltiazem, and nifedipine in the treatment of ambulatory ischemia in patients with stable angina. Differential effects on ambulatory ischemia, exercise performance, and anginal symptoms. The ASIS Study Group. Circulation 1990 82(6) 1962-72. 

Rocha P, Baron B, Delestrain A, Pathe M, Cazor JL, Kahn JC. Hemodynamic effects of intravenous diltiazem in patients treated chronically with propranolol. Am Heart J 1986 lll(l) 62-8. 

Tateishi T, Ohashi K, Fujimura A, Ebihara A. The influence of diltiazem versus cimetidine on propranolol metabolism. J Chn Pharmacol 1992 32(12) 1099-104. 

In 33 patients with sjmptomatic and inducible supraventricular tachycardias single doses of placebo, flecainide 3 mg/kg, or dUtiazem 120 mg plus propranolol 80 mg were used to terminate the dysrhythmia (5). Conversion to sinus rhythm was achieved within 2 hours in 17 patients with placebo, in 20 with flecainide, and in 31 with diltiazem plus propranolol. Time to conversion was shorter with diltiazem plus propranolol (32 minutes) than with flecainide (74 minutes) or placebo (77 minutes). Of those who were given flecainide, two had hypotension and one had sinus bradycardia. 

Synthetic applications of AD which have already appeared and which are of potential industrial interest include the synthesis of propranolol (9) [48], diltiazem (10) [49], carnitine, and 4-amino-3-hydroxybutyric acid (11) [50], azole anti-fungals (12) [51], chloramphenicol (13) [52], reticuline intermediates (14) [53], camptothecin analogs (15) [54], khellactone (16) derivatives [55], taxol C-13 side chain (17) [56], halosarin [64], dehydro- xo-brevicomin [65], and antimalar-ial active cyclopenteno-l,2,4-trioxanes [57], as summarized in Figure 4. 

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