Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effects of local anesthetics in depressing myocardial contractility were studied in isolated guinea pig right ventricular papillary muscles. Bupivacaine and etidocaine, 4 and 10 microM, showed reverse frequency-dependent depression of contractility, that is, less significant depression of contractility at higher stimulation frequencies (2-3 Hz) than at lesser frequencies (less than 1 Hz). Lidocaine, 40 microM, demonstrated a similar trend. In contrast, the normal action potential maximum rate of depolarization (Vmax), a measure of sodium channel conductance, was significantly more depressed at 2-3 Hz by bupivacaine and etidocaine than by lidocaine. Consequently, contractile depression could be overcome only at higher stimulation frequencies, at which conduction was depressed. To explore the mechanism of the contractile depression, local anesthetic effects were studied on slow (calcium channel-mediated) action potentials in partially depolarized papillary muscles. Etidocaine and bupivacaine, 4 and 10 microM, and lidocaine, 40 and 100 microM, caused a marked depression of the late-peaking contractile responses, attributed to Ca2+ release from the sarcoplasmic reticulum. In contrast, only 10 microM bupivacaine caused any significant depression of the slow action potential rate of depolarization (to 89% of control), consistent with a possible small depression of Ca2+ entry.
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PMID:Depression of myocardial contractility in vitro by bupivacaine, etidocaine, and lidocaine. 242 88

The differential sensitivities of A beta, A delta and C fibres of rat vagus nerve to bupivacaine, etidocaine and AL-381 were studied in vitro. In A beta fibres, at 35-37 degrees C, 50 mumole litre-1 of the drugs had similar effects on the action potential amplitude, while at greater concentrations (100 and 200 mumole litre-1) the greatest mean depression of amplitude was seen with etidocaine (n.s.). AL-381 had the most marked effect on the A delta potentials, and it appeared that it was about twice as potent as the others in blocking these fibres. Etidocaine 100 mumole litre-1 was more depressant than the same dose of bupivacaine. The C fibres were blocked most rapidly by AL-381, while etidocaine had the least effect.
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PMID:Differential sensitivity of A and C nerve fibres to long-acting amide local anaesthetics. 683 Jun 78

Postoperative pain is commonly treated with significant doses of narcotics, occasionally resulting in side effects including nausea, pruritus, and respiratory depression. One potential advantage of regional anesthesia is profound postoperative analgesia that reduces exposure to potent narcotics. To evaluate the efficacy of two long-acting local anesthetics, bupivacaine and etidocaine, in providing pain relief after major shoulder surgery, we randomized 20 patients to receive either bupivacaine or etidocaine for brachial plexus block as the primary anesthetic for shoulder surgery. Surgeons, patients, and the acute pain service were blinded as to drug selection. After the patient was sedated, an interscalene block was placed with the use of a nerve stimulator to facilitate proper needle placement. Forty milliliters of either 0.5% bupivacaine or 0.75% etidocaine containing 5 micrograms/mL epinephrine was injected into the brachial plexus sheath. An additional 8 mL of local anesthetic was administered for superficial cervical plexus blockade. Intraoperative sedation was accomplished with an intravenous infusion of methohexital as needed. After surgery, patients received a standard patient-controlled analgesia protocol providing incremental doses of morphine. The degree of postoperative analgesia resulting from residual local anesthetic effect was expressed as the time until first morphine requirement and the total dose of morphine required during the first 24 hours postoperatively. We found no statistically significant intergroup differences either in time of initial use of morphine or in the total dose of morphine required in the first 24 hours. Both etidocaine and bupivacaine provide prolonged analgesia after major shoulder surgery when injected into the brachial plexus. Bupivacaine, however, possesses significant cardiotoxicity and has a relatively delayed onset in peripheral neural blockade. Etidocaine is less cardiotoxic and also has a more rapid onset of effect. Thus etidocaine may be a preferable agent for interscalene block for major shoulder surgery.
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PMID:Postoperative analgesia after major shoulder surgery with interscalene brachial plexus blockade: etidocaine versus bupivacaine. 815 80

Large and equipotent doses of several local anesthetics were administered in a cardiac electrophysiologic model on closed-chest dogs. Five groups of pentobarbital-anesthetized dogs were each given intravenously 16 mg/kg lidocaine, 12 mg/kg mepivacaine, 4 mg/kg or 8 mg/kg etidocaine, and 4 mg/kg bupivacaine. Lidocaine induced bradycardia, slowing of atrioventricular node conduction (AH), and marked hemodynamic depression, represented by a decrease in mean aortic pressure (MAoP), in the peak of first derivative of left ventricular pressure (LVdP/dt(max)) and by an increase in left ventricular end-diastolic pressure (LVEDP). Atrial pacing at pacing cycle length (PCL) of 298 ms did not enhance the alteration of variables of ventricular conduction (His ventricle [HV] interval and QRS duration). Mepivacaine induced slight alteration of electrophysiologic variables. Atrial pacing at PCL of 312 ms did not enhance the alteration of HV and QRS duration. Mepivacaine induced transient hemodynamic depression. Etidocaine (4 mg/kg) induced electrophysiologic and hemodynamic alterations similar to mepivacaine but artrial pacing at PCL of 330 ms enhanced HV lengthening and QRS widening (P < 0.05). Etidocaine (8 mg/kg) induced marked impairment of PR, HV, QRS, and QT, and dramatic hemodynamic depression represented by a decrease in MAoP from 123.5 +/- 16.2 at baseline to 36.5 +/- 8.3 mm Hg at 1 min (P < 0.001) and of LVdP/dtmax) from 1446 +/- 379 to 333 +/- 93 mm Hg/s (P < 0.001). Bupivacaine induced dramatic impairment of electrophysiologic variables. Bupivacaine also decreased LVDP/dtmax (from 1333 +/- 347 to 617 +/- 299,P < 0.001) and increased LVEDP. We conclude that mepivacaine induced moderate cardiotoxicity. In contrast, lidocaine induced dramatic hemodynamic depression while etidocaine and bupivacaine markedly impaired both electrophysiologic and hemodynamic variables. This double impairment could explain the great difficulty in resuscitating patients who have had cardiotoxic accidents induced by etidocaine or bupivacaine.
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PMID:Comparative electrophysiologic and hemodynamic effects of several amide local anesthetic drugs in anesthetized dogs. 862 76