elavil dosage cats
The micellization behaviors of two amphiphilic drugs ((amitriptyline hydrochloride (AMT) and imipramine hydrochloride (IMP)) in presence of cationic surfactants (conventional as well as gemini) have been investigated conductometrically at four mole fractions and four temperatures. The critical micelle concentration (cmc) values come out to be lower than cmc(id) values (cmc(id) is the cmc value at ideal mixing state) indicating attractive interactions between the two components in mixed micelles. Micellar mole fractions of surfactants (X(1) and X(1)(M)), calculated by Rubingh and Motomura models, are always greater than X(1)(id) (micellar mole fraction at ideal mixing). The rigid structure of drugs decreases their contribution in mixed micelles as compared to that predicted by X(1)(id) values. Although α(1) (mole fraction of surfactant) is higher for DTAB than that of 12-4-12, the contribution of 12-4-12 is almost equal to that of DTAB. The interaction parameter (β) is negative at all temperatures and at all compositions indicating attractive interactions. Activity coefficients (f(1) and f(2)) are always less than unity suggesting nonideality in the systems. Thermodynamic parameters suggest dehydration of hydrophobic part of the drug at or above certain temperature which is different for the two drugs.
Combination therapy is often used to increase the clinical utility of analgesic agents. The coadministration of two compounds may achieve analgesia at doses lower than those required for either compound alone, leading to enhanced pain relief and reduction of adverse effects. Herein, the authors describe the effect of coadministration of morphine and amitriptyline on cutaneous orofacial inflammatory pain in rats.
We describe a gas chromatographic-chemical-ionization mass spectrometric procedure for determining concentrations of the tricyclic antidepressant drugs and their demethylated metabolites in plasma. The procedure requires 2.0 mL of plasma or serum and involves internal standard addition, extraction with a mixed organic solvent, and separation on a column packed with 0.5% potassium hydroxide and 2% Carbowax 20M. Between-assay and within-assay (n = 10) CVs were less than 11.0%. The procedure has been applied to several interesting cases, three of which are summarized.
elavil migraine dosage
Gas chromatography was used to determine plasma levels of amitriptyline, nortriptyline and their 10-hydroxy derivatives after conversion to the dehydro compounds by heating with acid. The primary amine 10-hydroxydesmethylnortriptyline is also dehydrated and the dehydro compound coincides on the chromatogram with dehydronortriptyline. Treatment of the extract with salicylaldehyde selectively removed the primary amine, which was determined by difference. Cis- and trans-hydroxydesmethylnortriptyline were isolated from urine by thin-layer chromatography and used to standardize the estimation. The stability of all the metabolites in plasma was investigated. Results are given for hydroxydesmethylnortriptyline levels in the plasma of 41 patients treated with amitriptyline.
elavil drug interactions
To review the tolerability and efficacy of amitriptyline in the management of depression.
elavil reviews depression
Actions on performance of dextropropoxyphene (DXP) alone and in combination with amitriptyline (AMI), indomethacin (IN), and placebo were compared in 15 patients with rheumatoid arthritis. The patients were on their prescribed maintenance regimen excluding analgesics. In four randomized test sessions at two-week intervals, they received double blind and crossover single oral doses of DXP 130 mg, IN 50 mg, DXP 65 mg + AMI 25 mg or placebo, each after two days' pretreatment with the same drug. Objective and subjective effects were measured at baseline and 2 and 4 hours after drug administration. DXP impaired critical flicker discrimination, symbol copying and body balance without modifying tracking, choice reactions or attention. It rendered the subjects elated, muzzy, mentally slow and calm. Actions of AMI + DXP were about the same. IN impaired body balance and critical flicker recognition. Plasma concentrations of DXP were moderate to high whilst those of IN and AMI were fairly low. We conclude that therapeutic doses of DXP and IN are relatively safe in regard to driving skills. Small doses of AMI may not enhance the mild psychomotor effects of DXP. Earlier single dose studies carried out with healthy volunteers might have overestimated the decremental effects of analgesics on psychomotor performance.
elavil normal dosage
A multi-centre controlled trial of amitriptyline, dothiepin and mianserin in the treatment of depressive illness was undertaken in psychiatric inpatients over the age of 65. Despite the co-operation of many of the leading practitioners in this field in Great Britain, it proved impossible to recruit sufficient patients for firm conclusions to be drawn. Forty-five patients were entered into the trial, 13 withdrew because of lack of improvement, 4 because of intercurrent physical illness, 3 because of adverse effects of trial medication and 2 because of lack of compliance. Only 11 of the 23 patients completing had a final score on the Hamilton Depression Rating Scale of 10 or less. No treatment showed a significant superiority over the others, nor was there any difference in tolerance.
elavil overdose symptoms
One-hundred and twenty patients with chronic pain, who had all failed to obtain relief with traditional medical treatment, were given a standard psychotropic drug mixture consisting of amitriptyline 25 mg and perphenazine 2 mg. Of those who completed 2 months of treatment, 33.68% were pain free, while 8.3% had unacceptable side-effects. The best results were obtained in patients with postherpetic neuralgia and postoperative scar pain.
There is an art to prescribing medications to depressed patients. Both patient and therapist factors are important to a successful outcome with appropriate timing and prescribing of treatment. Two case reports are provided as examples. Specific strategies used by experienced clinicians are presented in the discussion.
elavil 30 mg
Dose-response association with QTc prolongation was identified for citalopram (adjusted beta 0.10 (SE 0.04), P<0.01), escitalopram (adjusted beta 0.58 (0.15), P<0.001), and amitriptyline (adjusted beta 0.11 (0.03), P<0.001), but not for other antidepressants examined. An association with QTc shortening was identified for bupropion (adjusted beta 0.02 (0.01) P<0.05). Within-subject paired observations supported the QTc prolonging effect of citalopram (10 mg to 20 mg, mean QTc increase 7.8 (SE 3.6) ms, adjusted P<0.05; and 20 mg to 40 mg, mean QTc increase 10.3 (4.0) ms, adjusted P<0.01).
elavil generic name
Palliative sedation (PS) is necessary in a significant percentage of patients dying on an acute palliative care unit (PCU). Common indications are terminal restlessness, pain and dyspnoea. On our PCU, terminal restlessness was the main indication for PS but pain was the most prevalent symptom during admission. Because delirium is often drug induced in terminal cancer patients and opioids are amongst the most frequently implicated drugs, we hypothesised that the underlying pain problem and its treatment might have been related to the need for sedation.
elavil dosage sleep
We studied the effect of alaproclate [2-(4-chlorophenyl)-1,1-dimethyl 2-aminopropanoate] on the N-methyl-D-aspartate (NMDA)-induced changes in membrane potential and intracellular free Ca++ in cerebellar granule cells by using the fluorescent indicators DiBaC4(3) and fura-2, respectively. The NMDA-induced responses were blocked by the 5-hydroxytryptamine reuptake blocker alaproclate in a noncompetitive manner with an IC50 value of 0.3 microM. The effect of alaproclate was stereoselective because the S-(-)-enantiomer was more potent than the R-(+)-enantiomer. The inhibitory response was rapidly reversed if alaproclate was removed by perfusion. The same was the case with the reversible noncompetitive NMDA receptor antagonists dextromethorphan, dextrorphan, amitriptyline and desipramine. The inhibition caused by the noncompetitive antagonist dizolcipine could not be reversed by perfusion. The glycine-sensitivity of the NMDA response was unaffected by alaproclate, and high concentrations of glycine were unable to reverse the inhibition of alaproclate. Alaproclate also did not affect the sensitivity of the responses to Mg++. The results suggest that alaproclate, which has previously been in clinical trials for depressive illness, acts as a reversible noncompetitive antagonist of the NMDA receptor.
elavil brand name
Low back pain (LBP) is responsible for more than 2.5 million visits to US emergency departments (EDs) annually. These patients are usually treated with nonsteroidal anti-inflammatory drugs, acetaminophen, opioids, or skeletal muscle relaxants, often in combination.
elavil 75 mg
In users of tricyclic antidepressants (TCAs) the risk of switching to another antidepressant was significantly higher in poor metabolizers (PMs:*4/*4) compared with extensive metabolizers (EMs:*1/*1), with an adjusted OR of 5.77 (95% CI 1.59, 21.03; P = 0.01). In SSRI users there was no significant difference (OR 0.91; 95% CI 0.20, 4.15; P = 0.90). Heterozygous patients did not have an increased risk of switching in both TCA and SSRI users. The mean TCA dose was significantly lower in PMs than in EMs at the third and fourth prescription (difference 0.11 DDD, P = 0.03). In SSRI users the difference in mean dose between PMs and EMs was significant at the third prescription (0.17 DDD; P = 0.02).
elavil 50mg tablets
Amitriptyline may be effective in the treatment of diarrhoea-predominant irritable bowel syndrome and at low dose is well tolerated.
elavil overdose treatment
A pharmacokinetic analysis of a new antidepressant drug, mianserin (ORG GB-94), was undertaken in 4 male volunteers, each of whom received 15 mg mianserin on two occasions. Plasma levels peak at 2 h with a median level of 11.0 ng/ml, a median beta-phase half-life of 10.0 h, and a median apparent volume of distribution of 3.3 X 10(3) 1. EEG profile analysis shows mianserin to increase frequencies below 6 Hz, decrease those from 7.5 to 15 Hz, and increase frequencies above 18 Hz, a pattern similar to amitriptyline. Peak EEG effects range from 2 to 5 h with a pattern of measured changes that parallels plasma levels with varying latency. Decreases in vigilance measures and in critical flicker-fusion frequency show a similar time course. Mianserin is a putative thymoleptic on EEG profile analysis with high cerebral penetrance.
elavil lethal dose
Amitriptyline intoxication lowered cardiac output, peak left ventricular dP/dt, and mean arterial pressure (MAP). All doses of norepinephrine and the two higher doses of dopamine increased cardiac output, MAP, and peak left ventricular dP/dt during the intoxicated state. Both agents restored all variables to preintoxication values. Values obtained at the highest doses of the two drugs were not different for any variable.
Many adverse drug reactions are caused by the cytochrome P450 (CYP) dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-mediated toxicity and to improve safety of drug candidates, we developed two in vitro cell-based assays by combining an activating system (human CYP3A4) with target cells (HepG2 cells): in the first method we incubated microsomes containing cDNA-expressed CYP3A4 together with HepG2 cells; in the second approach HepG2 cells were transiently transfected with CYP3A4. In both assay systems, CYP3A4 catalyzed metabolism was found to be comparable to the high levels reported in hepatocytes. Both assay systems were used to study ten CYP3A4 substrates known for their potential to form metabolites that exhibit higher toxicity than the parent compounds. Several endpoints of toxicity were evaluated, and the measurement of MTT reduction and intracellular ATP levels were selected to assess cell viability. Results demonstrated that both assay systems are capable to metabolize the test compounds leading to increased toxicity, compared to their respective control systems. The co-incubation with the CYP3A4 inhibitor ketoconazole confirmed that the formation of reactive metabolites was CYP3A4 dependent. To further validate the functionality of the two assay systems, they were also used as a "detoxification system" using selected compounds that can be metabolized by CYP3A4 to metabolites less toxic than their parent compounds. These results show that both assay systems can be used to screen for metabolic activation, or de-activation, which may be useful as a rapid and relatively inexpensive in vitro assay for the prediction of CYP3A4 metabolism-mediated toxicity.
elavil overdose death
All RCTs comparing fluoxetine with any other AD (including non-conventional agents such as hypericum) for patients with unipolar major depressive disorder (regardless of the diagnostic criteria used) were included. For trials that had a cross-over design only results from the first randomisation period were considered.
elavil sleep dosage
We conclude that clinical response to antidepressive treatment precedes improvement of declarative memory. A low degree of impairment of declarative memory is associated with early complete remission of depression.
elavil drug class
Hidradenitis Supprurativa (HS) is a painful chronic follicular disease. Few papers have addressed pain control for this debilitating condition. Possible topical agents include tricyclic antidepressants, opioids, anticonvulsants, NSAIDs, NMDA receptor antagonists, local anesthetics and other agents. The first line agents for the topical treatment of the cutaneous pain of HS are diclonefac gel 1% and liposomal xylocaine 4% and 5% cream or 5% ointment. The chief advantage of topical xylocaine is that is quick acting i.e. immediate however with a limited duration of effect 1-2 hours. The use of topical ketamine, which blocks n-methyl-D-aspartate receptors in a non-competitive fashion, might be a useful tool for the treatment of HS pain. Topical doxepin, which available in a 5% commercially preparation (Zonalon®) , makes patients drowsy and is not useful for controlling the pain of HS . Doxepin is available in a 3% or 3.3% concentration (which causes less drowsiness) from compounding pharmacies and can be used in compounded analgesic preparations with positive effect. Topical doxepin is preferred over use of topical amitriptyline because topical doxepin is more effective. Nevertheless, topical amitriptyline increase of the tactile and mechanical nociceptive thresholds and can be used for topical pain control in compound mixture of analgesics . Gabapentin and pregablin can also be used compounded with other agents in topical analgesic preparations with positive topical anesthetic effect. Capsaicin is not useful for topical treatment of the pain of HS. Sometimes compounded of anesthetics medications such as ketamine 10%, bupivacaine 1%, diclofenac 3%, doxepin 3% or 3.3%, and gabapentin 6% can extend the duration of effect so that medication only needs to be used 2 or 3 times a day. Still in my experience the easiest to get and most patient requested agent is topical diclonefac 1% gel.
elavil 200 mg
Tricyclic antidepressants (for example, amitriptyline) and other types of antidepressants (for example, amoxapine and maprotiline) are competitive antagonists of muscarinic acetylcholine receptors, the predominant class of acetylcholine receptors in the brain. Some evidence suggests that this muscarinic receptor blockade in brain alleviates depression. However, all tricyclic antidepressants appear to be equally effective in treating depression despite having differences in their antimuscarinic potencies while having similar ranges of therapeutic blood levels. It is more likely that the antimuscarinic potency of antidepressants is related mainly to the frequency with which they cause such symptoms as blurred vision, dry mouth, and urinary retention. Information on the antimuscarinic potency and other receptor-blocking potencies of antidepressant agents can be helpful in minimizing or avoiding certain side effects when these drugs are given to patients.
elavil type drugs
The efficacy of each antidepressant available has been found equal to that of amitriptyline in double-blind studies as far as mild to moderate depression is involved. However, it seems that some antidepressants are more effective than others in the treatment of severe types of depression (i.e., delusional depression and refractory depression). Following studies regarding the antinociceptive mechanisms of various antidepressants, we speculate that the involvement of the opioid system in the antidepressants' mechanism of action may be necessary, in order to prove effective in the treatment of severe depression. Among the antidepressants of the newer generations, that involvement occurs only with venlafaxine (a presynaptic drug which blocks the synaptosomal uptake of noradrenaline and serotonin and, to a lesser degree, of dopamine) and with mirtazapine (a postsynaptic drug which enhances noradrenergic and 5-HT1A-mediated serotonergic neurotransmission via antagonism of central alpha-auto- and hetero-adrenoreceptors). When mice were tested with a hotplate analgesia meter, both venlafaxine and mirtazapine induced a dose-dependent, naloxone-reversible antinociceptive effect following ip administration. Summing up the various interactions of venlafaxine and mirtazapine with opioid, noradrenergic and serotonergic agonists and antagonists, we found that the antinociceptive effect of venlafaxine is influenced by opioid receptor subtypes (mu-, kappa1- kappa3- and delta-opioid receptor subtypes) combined with the alpha2-adrenergic receptor, whereas the antinociceptive effect of mirtazapine mainly involves mu- and kappa3-opioid mechanisms. This opioid profile of the two drugs may be one of the explanations to their efficacy in severe depression, unlike the SSRIs and other antidepressants which lack opioid activity.
elavil anxiety medication
A new method for the CE separation of nine tricyclic antidepressants (TCAs), viz. amitriptyline, clomipramine, desipramine, doxepin, fluphenazine, imipramine, nortriptyline, promazine, and thioridazine, is described. The capillary was statically coated with a layer of poly(N,N-dimethylacrylamide) (PDMA) to suppress the EOF, and beta-CD was used as an additive in the BGE solution. The optimal resolution of nine TCAs was obtained by using a 1% v/v PDMA-coated capillary and a BGE solution of 50 mM sodium phosphate buffer (pH 3.0) containing 0.5 mM beta-CD. Efficiencies were typically >10(5 )plates/m. Complete separation of nine TCAs could be achieved in about 28 min; the two diastereomers of doxepin and the two enantiomers of thioridazine could also be separated. The RSD values of migration time and peak area of the TCAs were in the ranges 0.5-0.8 and 3.3-4.9% (n = 10), respectively. In combination with a suitable sample clean-up technique, such as hollow fiber-based liquid phase microextraction (HF-LPME), the polymer-coated capillary can be employed for the CE-UV analysis of TCAs in human plasma.
elavil generic form
Analysis of routinely collected anonymised computerised patient records in 131 UK general practices (approximately 162,000 registered patients annually aged >or=65 years) providing data to the DIN-LINK database between 1994 and 2003. In each year, we identified patients prescribed drugs classified by the 2003 Beers criteria as potentially inappropriate for older people.
elavil 2 mg
Milnacipran's binding and uptake inhibition profile more closely resembles that of the tricyclic antidepressants than that of duloxetine. Whether these differences observed in vitro manifest themselves in vivo is not clear.
The cases of two borderline patients are presented, dexamethasone suppression test (DST) positive and refractory to many therapeutic interventions and treated successfully with high doses of amitriptyline (225 and 200 mg/day, respectively). During the therapeutic intervention, the psychopathological condition of the patients was evaluated using Hamilton's rating scale for depression and a constructed scale based on items 11, 12 and 13 (dysphoria, anger, sense of emptiness, boredom, anhedonia) of the diagnostic interview for borderline patients.
A three-dimensional molecular template has been generated for substrates of human debrisoquine 4-hydroxylase cytochrome P450 (CYP2D6). This template defines the stereochemical requirements for CYP2D6 substrates in terms of the volume occupied and positions of key atoms. The modelling was based on the X-ray crystallographic coordinates of the location of the attacked C5 atom of camphor in relation to the haem in cytochrome P450 cam. Interactive molecular graphics combined with energy calculations were used to identify allowed conformers to superpose known CYP2D6 substrates to yield a molecular template. This model takes into account the site of attack of the known substrates and the requirement for a protonated nitrogen atom to interact with an anion site of the protein. A nitrogen-anion distance of between 2.5 and 4.5 A was allowed for the interaction. The substrates modelled were cardiovascular drugs (debrisoquine, sparteine, guanoxan and perhexiline), beta-adrenergic blocking agents (bufuralol and propranolol), tricyclic anti-depressants (desipramine, amitriptyline and nortriptyline) and other miscellaneous compounds (phenformin, methoxy-amphetamine, codeine and dextromethorphan). The template generated in this manner was then used to determine the likelihood that certain other compounds were substrates for CYP2D6. A carcinogenic protein pyrolysate product, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), did not fit the template and is therefore unlikely to be activated by this enzyme. A potent carcinogen in tobacco smoke, 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone (NNK), fitted the template but could not be modelled to form a favourable nitrogen-anion interaction. Experimental substrate competition studies also showed that NNK is unlikely to be a CYP2D6 substrate. It was also shown that the widely used drug for treatment of breast cancer, trans-1-(4-beta-dimethylaminoethoxyphenyl)-,2-diphenyl-1-ene (tamoxifen), did not fit the molecular template and is unlikely to be metabolized by CYP2D6. Coordinates of the template are available.
elavil usual dosage
Interstitial cystitis is associated with substantial costs and health care resource utilization.
elavil maximum dosage
Psychomotor retardation, a general slowing of activity which is one of the central characteristics of depression, was investigated by measuring reaction time and movement duration in drawing tasks. Twenty depressive patients and 20 normal controls participated in two tasks in which either simple or more complex figures had to be copied as fast as possible on a digitizer. In general, patients needed more time to complete the drawing tasks than controls, and they performed them differently. Six patients, who could be tested before and after treatment, showed changes in drawing speed that correlated with clinical improvement. These results suggest that psychomotor retardation might be fruitfully studied by measuring the kinematic aspects of drawing and might provide objective parameters to measure progress in therapy.