Droperidol Morphine

Zimmermann AR, Kibblewhite D, Sleigh J. Comparison of morphine/droperidol and tramadoFdroperidol mixture for patient controlled analgesia (PCA) after cardiac surgery a prospective, randomised, double-blind study. J Acute Pain 2002 4 65-9. 

Fentanyl is 80 to 100 times as potent as morphine. Sufentanil (Sufenta) is 500- to 1,000-fold more potent than morphine, while alfentanil (Alfenta) is approximately 20 times more potent than morphine. Their onset of action is usually less than 20 minutes after administration. Dosage is determined by the lean body mass of the patient, since the drugs are lipophilic and tend to get trapped in body fat, which acts as a reservoir, prolonging their half-life. In addition, redistribution of the drugs from the brain to fat stores leads to a rapid offset of action. Droperidol, a neuroleptic agent, is generally administered in combination with fentanyl for IV anesthesia. 

Perhaps the most successful modification of the 4-phenylpiperidine derivatives of morphine is the 4-anilino compounds, such as fentanyl (3.15). This dmg is 50-100 times more active than morphine, owing mainly to its excellent transport across the blood-brain barrier and into the CNS as a result of its high lipophilicity. Spectacular activities ( 5000-6000 times that of morphine) have also been achieved by introducing ether or keto substituents (sufentanil), as in the meperidine or ketobemidone series. Fentanyl derivatives are very fast acting and of short duration. They are used in neuroleptanalgesia in surgery, in combination with neuroleptics or major tranquilizers like droperidol. 

Lo Y, Chia YY, Liu K, Ko NH. Morphine sparing with droperidol in patient-controlled analgesia. 

Several drugs are used intravenously, alone or in combination with other drugs, to achieve an anesthetic state (as components of balanced anesthesia) or to sedate patients in intensive care units who must be mechanically ventilated. These drugs include the following (1) barbiturates (thiopental, methohexital) (2) benzodiazepines (midazolam, diazepam) (3) opioid analgesics (morphine, fentanyl, sufentanil, alfentanil, remifentanil) (4) propofol (5) ketamine and (6) miscellaneous drugs (droperidol, etomidate, dexmedetomidine). Figure 25-2 shows the structures of... 

Fentanyl [FEN ta nil], which is chemically related to meperidine, has 80 times the analgesic potency of morphine, and is used in anesthesia. It has a rapid onset and short duration of action (15 to 30 minutes). When combined with droperidol (see p.117) it produces a neurolept anesthesia. Sufentanil [soo FEN ta nil], a related drug, is even more potent than fentanyl. 

Droperidol 0.5 micrograms reduced the need for postoperative morphine delivered via a patient-controlled analgesia device (31). At these doses it was non-sedating and caused no dyskinetic movements. 

Burduk P, Guzik P, Piechocka M, Bronisz M, Rozek A, Jazdon M, Jordan MR. Comparison of fentanyl and droperidol mixture (neuroleptanalgesia II) with morphine on clinical outcomes in unstable angina patients. Cardiovasc Drugs Ther 2000 14(3) 259-69. 

Sanansilp V, Areewatana S, Tonsukchai N. Droperidol and the side effects of epidural morphine after cesarean section. Anesth Analg 1998 86(3) 532-7. 

Intravenous ondansetron (4 mg at induction of anesthesia and 0.13 mg with each 1 mg bolus of morphine) has been compared with intravenous droperidol (0.5 mg at induction and 0.05 mg with each bolus of morphine) in a double-blind trial in 142 patients (22). The two regimens had similar efficacy in the prevention of postoperative nausea and vomiting. The most important adverse effect was sedation significantly more patients given droperidol (15%) had excessive sedation than patients given ondansetron (5%). 

Intravenous droperidol 1.25 mg and intravenous dexamethasone 8 mg, given at the end of cesarean section, have been compared in reducing the incidence of nausea and vomiting caused by epidural morphine 3 mg in 120... 

In another randomized, double-blind study, 140 patients undergoing cesarean section had anesthesia with epidural bupivacaine 100 mg and adrenahne to which was added morphine 2 mg and droperidol 0, 1.25, 2.5, or 5.0 mg (11). Previous evidence had suggested that intravenous droperidol reduces morphine-induced pruritus, but that the effect disappeared when the dose was increased from 2.5 mg to 5.0 mg (12). However, in this study, epidural droperidol caused a dose-dependent reduction in morphine-induced pruritus even at a dose of 5 mg. 

Nausea and vomiting are frequent adverse effects associated with the use of PCA opioids. Droperidol and tro-pisetron may reduce the incidence and severity of nausea and vomiting caused by morphine (SEDA-19, 84). 

A prospective, randomized, double-blind study of 97 women investigated whether droperidol alleviated the adverse effects of epidural morphine after cesarean section (54). All groups received morphine 5 mg epiduraUy on delivery, accompanied by no droperidol, or droperidol 2.5 mg epiduraUy, or droperidol 2.5 mg intravenously. Pruritus occurred in 70% of patients, starting at 6 hours... 

Tzeng JI, Wang JJ, Ho ST, Tang CS, Liu YC, Lee SC. Dexamethasone for prophylaxis of nausea and vomiting after epidural morphine for post-Caesarean section analgesia comparison of droperidol and saline. Br J Anaesth 2000 85(6) 865-8. 

Horta ML, Ramos L, Goncalves ZR. The inhibition of epidural morphine-induced pruritus by epidural droperidol. Anesth Analg 2000 90(3) 638 1. 

Horta ML, Ramos L, Goncalves Zda R, de Ohveira MA, ToneUotto D, Teixeira JP, de Melo PR. Inhibition of epidural morphine-induced pruritus by intravenous droperidol. The effect of increasing the doses of morphine and of droperidol. Reg Anesth 1996 21(4) 312-17. 

One important analogue of morphine is fentanyl, a clinically used narcotic that is about 100 times more potent than morphine. Several analogues have been synthesised such as sufentanil, alfentanil, lofentanil and, even more interestingly, structurally related compounds with different activities such as astemizole (antihistaminic), droperidol (tranquillizing), loperamide (antidiarrheal) and lorcainide (antiarrhythmic) [50]. 

Also analyzed acebutolol, acepromazine, acetaminophen, acetazolamide, acetophenazine, albuterol, amitriptyline, amobarbital, amoxapine, antipsrrine, atenolol, atropine, azata-dine, baclofen, benzocaine, bromocriptine, brompheniramine, brotizolam, bupivacaine, buspirone, butabarbital, butalbital, caffeine, carbamazepine, cetirizine, chlorqyclizine, chlordiazepoxide, chlormezanone, chloroquine, chlorpheniramine, chlorpromazine, chlorpropamide, chlorprothixene, chlorthalidone, chlorzoxazone, cimetidine, cisapride, clomipramine, clonazepam, clonidine, clozapine, cocaine, codeine, colchicine, qyclizine, (yclo-benzaprine, dantrolene, desipramine, diazepam, diclofenac, diflunisal, diltiazem, diphenhydramine, diphenidol, dipheno late, dipyridamole, disopyramide, dobutamine, doxapram, doxepin, droperidol, encainide, ethidium bromide, ethopropazine, fenoprofen, fentanyl, flavoxate, fluoxetine, fluphenazine, flurazepam, flurbiprofen, fluvoxamine, fii-rosemide, glutethimide, glyburide, guaifenesin, haloperidol, homatropine, hydralazine, hydrochlorothiazide, hydrocodone, hydromorphone, hydro g chloroquine, hydroxyzine, ibuprofen, imipramine, indomethacin, ketoconazole, ketoprofen, ketorolac, labetalol, le-vorphanol, lidocaine, loratadine, lorazepam, lovastatin, loxapine, mazindol, mefenamic acid, meperidine, mephenytoin, mepivacaine, mesoridazine, metaproterenol, methadone, methdilazine, methocarbamol, methotrexate, methotrimeprazine, methoxamine, methyl-dopa, methylphenidate, metoclopramide, metolazone, metoprolol, metronidazole, midazolam, moclobemide, morphine, nadolol, nalbuphine, naloxone, naphazoline, naproxen, nifedipine, nizatidine, norepinephrine, nortriptyline, oxazepam, oxycodone, oxymetazo-line, paroxetine, pemoline, pentazocine, pentobarbital, pentoxifylline, perphenazine, pheniramine, phenobarbital, phenol, phenolphthalein, phentolamine, phenylbutazone, phenyltoloxamine, phenytoin, pimozide, pindolol, piroxicam, pramoxine, prazepam, prazosin, probenecid, procainamide, procaine, prochlorperazine, procyclidine, promazine, promethazine, propafenone, propantheline, propiomazine, propofol, propranolol, protriptyline, quazepam, quinidine, quinine, racemethorphan, ranitidine, remoxipride, risperidone, salicylic acid, scopolamine, secobarbital, sertraline, sotalol, spironolactone, sulfinpyrazone, sulindac, temazepam, terbutaline, terfenadine, tetracaine, theophylline, thiethyl-perazine, thiopental, thioridazine, thiothixene, timolol, tocainide, tolbutamide, tolmetin, trazodone, triamterene, triazolam, trifluoperazine, triflupromazine, trimeprazine, trimethoprim, trimipramine, verapamil, warfarin, xylometazoline, yohimbine, zopiclone... 

Also analyzed acebutolol, acetaminophen, alprazolam, amphetamine, atenolol, betaxolol, brotizolam, caffeine, camazepam, captopril, chloroquine, clobazam, clomipramine, cloth-iapine, clotiazepam, cloxazolam, cocaine, codeine, diclofenac, dihydralazine, dihydrocodeine, dihydroergotamine, diphenhydramine, domperidone, doxepin, droperidol, ergota-mine, ethyl loflazepate, fenethylline, fluoxetine, flupentixol, flurazepam, furosemide, gliclazide, hydrochlorothiazide, hydroxyzine, ibuprofen, imipramine, ketazolam, loprazo-1am, lorazepam, lormetazepam, maprotUine, medazepam, mepyramine, methadone, methaqualone, methyldopa, methylphenidate, metoclopramide, metoprolol, mexiletine, mianserin, midazolam, minoxidil, morphine, nadolol, nitrazepam, oxprenolol, papaverine, pentazocine, phenprocoumon, phenylbutazone, pipamperone, piritramide, practolol, pra-zepam, prazosin, promazine, promethazine, propoxyphene, propranolol, prothipendyl, quinine, sotalol, sulpride, thioridazine, trazodone, triazolam, trimipramine, tripelennamine, lyramine, verapeunil, yohimbine... 

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