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PubMed2004

Treatment of ataxia in cortical cerebellar atrophy with the GABAergic drug gabapentin. A preliminary study.

The aim of this work was to investigate the efficacy of the GABAergic drug gabapentin in the treatment of the cerebellar signs caused by cortical cerebellar atrophy (CCA). Ten patients with CCA received gabapentin in single doses of 400 mg in an open-label study; thereafter, daily administration of 900-1,600 mg of gabapentin was continued during at least 4 weeks. An ataxia scale based on clinical findings was used to evaluate the cerebellar signs at baseline and after administration of the drug. A statistically significant improvement of the ataxia scores was found after single doses of 400 mg of gabapentin and after the administration of 900-1,600 mg of this drug during 4 weeks, as compared to the results obtained at baseline. An important clinical amelioration was also evident. Gabapentin has been demonstrated to be capable of improving the cerebellar signs in cases of CCA, after single doses and after continued administration of the drug during 4 weeks. GABAergic enhancement or supplementation could play an important role in the treatment of diseases of the cerebellar cortex associated with a deficit of GABA.

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PubMed2004

Analysis of interactions between serotonin and gabapentin or adenosine in the spinal cord of rats.

We evaluated the nature of the pharmacologic interaction after concurrent administration of 5-HT-gabapentin and 5-HT-adenosine at the spinal level. Intrathecal catheters were placed in the subarachnoid space of male Sprague-Dawley rats. Nociception was induced by subcutaneous injection of formalin solution (5%, 50 microl) into the hind paw. A fixed dose analysis and an isobolographic analysis were used to determine the properties of interaction. Intrathecal 5-HT dose-dependently suppressed the flinching response during phase 1 of the formalin test, while neither gabapentin nor adenosine affected the phase-1 flinching response. All three intrathecal drugs attenuated the phase-2 flinching response in a dose-dependent manner. The intrathecal combination of 5-HT with a fixed dose of gabapentin or adenosine in phase 1 had little effect or increased the antinociception of 5-HT alone. Isobolographic analysis in phase 2 revealed an additive or a synergistic interaction after intrathecal delivery of 5-HT-gabapentin or 5-HT-adenosine mixture. Taken together, the combination of 5-HT with either gabapentin or adenosine may offer a potential remedy in the treatment of the facilitated state as well as acute pain in the spinal cord.

Adenosine↗
PubMed2001

Single-dose gabapentin pharmacokinetics and safety in healthy infants and children.

Gabapentin (Neurontin) is a gamma-aminobutyric acid analogue indicated in adults for adjunctive treatment of partial seizures with or without secondary generalization. Two studies were conducted to determine the single-dose pharmacokinetics of gabapentin in healthy subjects age 1 month to 12 years and to guide dose selection in safety and efficacy trials in pediatric patients. Forty-eight subjects were given single oral doses of gabapentin (10 mg/kg) while fasting. Enrollment was homogeneously distributed throughout the age range. Plasma samples were drawn predose and then serially for 24 hours postdose. Single doses of gabapentin were well tolerated by healthy pediatric subjects. Plots of pharmacokinetic parameters versus age suggested significant differences between younger (1 month to < 5 years) and older (> or =5 to 12 years) subjects. Mean area under the plasma concentration-time curve from zero to infinity (AUC(0-infinity)) was 25.6 microg x h/mL in younger subjects and 36.0 microg x h/mL in older subjects (p < 0.001). Corresponding mean peak plasma concentrations (Cmax) were 3.74 and 4.52 microg/ml (p < 0.05). Oral clearance (normalized for body weight) was 7.40 and 4.41 mL/min/kg in younger subjects and older subjects, respectively (p < 0.001). It was concluded that children between 1 month and < 5 years of age require approximately 30% higher daily doses of gabapentin than those > or =5 to 12 years of age.

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PubMed1999

Gabapentin does not affect antipyrine clearance.

The effect of gabapentin on antipyrine clearance was assessed in 12 healthy male volunteers, using a known enzyme inducer, phenytoin, as control. Subjects received gabapentin 400 mg or phenytoin 100 mg three times daily for 2 weeks. Antipyrine tests were performed before, during, and after treatment with gabapentin or phenytoin. In contrast to phenytoin, chronic administration of gabapentin did not affect antipyrine clearance. Gabapentin appears to have little potential for drug interactions.

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PubMed2004

Gabapentin to control seizures in children undergoing cancer treatment.

Hepatic clearance of chemotherapy drugs is increased by many antiepilepsy drugs. At our institution, new-onset seizures in children on chemotherapy are treated with gabapentin, a nonhepatic enzyme inducer. The charts of all children given gabapentin for seizures were reviewed. At a median follow-up of 34 months, seizures were controlled in 74% of 50 children given gabapentin monotherapy as initial treatment: 91% of the leukemia group, 57% of the brain tumor group, and 75% of the other tumor group. Seizures were controlled in 49% of 59 children in whom gabapentin was added to other antiepilepsy drugs: 43% of the leukemia group, 53% of the brain tumor group, and 50% of the other tumor group. More than one seizure at presentation, focal neurologic deficits, high-dose methotrexate, brain irradiation, and T2-weighted signal abnormality around the brain tumor cavity predicted uncontrolled seizures. Only 8 children (7%) reported adverse effects, and the drug was discontinued in two. Gabapentin effectively controls seizures in children receiving chemotherapy and is well tolerated.

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PubMed2006

Gabapentin and breastfeeding: a case report.

The aim of this study was to describe the milk-plasma ratio and relative infant dose of gabapentin in a breastfeeding mother and to determine the well-being of her exposed infant. The mother-infant pair was studied over a 24-hour dose interval at steady state. Gabapentin concentrations were quantified by high-performance liquid chromatography. Infant exposure was calculated as concentration in milk multiplied by an estimated milk production of 0.15 L/kg/d and normalized to the weight-adjusted maternal dose. The milk-plasma ratio was 0.86; the relative infant dose was 2.34%. The absolute infant dose was approximately 3% of the children's dose for gabapentin, and the infant plasma level of 0.4 mg/L was approximately 6% of the maternal plasma drug concentration. No adverse effects attributable to gabapentin were noted in the infant. In combination with a previously published report, these limited data support the prescription of gabapentin to a breastfeeding mother after a careful individual risk-benefit analysis.

Adult↗
PubMed2003

Gabapentin in geriatric mania.

There is little available information on anticonvulsant treatment of mania in elderly patients. Seven elderly patients, each in a manic episode, were treated with gabapentin. All 7 patients experienced improvement in manic symptoms, with minimal to no side effects. They received gabapentin in combination with antipsychotic medications, and in 1 case in combination with valproate. Gabapentin appears to be a safe and effective treatment in geriatric mania when combined with antipsychotic medications or valproate. Gabapentin appears to be well tolerated with no major adverse drug interactions or side effects in elderly manic patients. This case series suggests that controlled studies are warranted to examine gabapentin's efficacy and side effects, particularly as an adjunctive medication, in geriatric mania.

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PubMed1994

Gabapentin: a new agent for the management of epilepsy.

OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, and safety of gabapentin, a new antiepileptic drug (AED). Gabapentin's potential role in the treatment of epilepsy also was assessed. DATA SOURCE: A MEDLINE search was performed to identify all published literature (manuscripts and abstracts). Abstracts presented at the American Epilepsy Society, International Epilepsy Congress, and American Academy of Neurology meetings from 1991 to 1993 also were reviewed. A copy of the proceedings from the Food and Drug Administration Peripheral and Central Nervous System Advisory Committee meeting and package insert were obtained from Parke Davis. STUDY SELECTION: All pertinent literature was reviewed. Emphasis was placed on published information, particularly placebo-controlled clinical trials. DATA SYNTHESIS: Gabapentin is effective as adjunctive treatment for patients with partial seizures with or without secondary generalization refractory to the standard AEDs. It has a unique pharmacokinetic profile for an AED, including no binding to plasma proteins, primary elimination by the kidney, and dose-dependent oral absorption at high dosages. No drug interactions occur with the other AEDs. The most frequent adverse reactions noted in patients receiving gabapentin have been mild and transient central nervous system effects. No serious hypersensitivity or systemic reactions have been observed. CONCLUSIONS: Gabapentin appears to be a useful new AED. Further studies evaluating its use as monotherapy, in higher dosages, and in pediatric and elderly patients are required to better delineate its therapeutic role relative to that of other AEDs.

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PubMed1995

Potential treatment of amyotrophic lateral sclerosis with gabapentin: a hypothesis.

OBJECTIVE: To provide the biochemical rationale for the use of the new anticonvulsant agent gabapentin as a treatment for amyotrophic lateral sclerosis (ALS). BACKGROUND: ALS is a neuropathologic disorder of the central nervous system characterized by a progressive loss of upper and lower motor neurons. Although the etiopathology of ALS is incompletely known, it is hypothesized that glutamatergic neurotransmission is related to neuropathology. Glutamate is an excitatory amino acid neurotransmitter that is cytotoxic when overexpressed at synaptic terminals, probably through a calcium-related mechanism. The concentration of glutamate in cerebrospinal fluid is increased in patients with ALS. The increased extracellular concentrations of glutamate may be caused by a decreased capacity of glutamate transport in brain tissue and/or abnormal glutamate metabolism. Recent success with the glutamate release inhibitor riluzole in well-controlled clinical trials supports the excitotoxic mechanism of neuropathology in patients with ALS. POTENTIAL TREATMENT FOR ALS: Gabapentin has demonstrated neuroprotective properties in a model of chronic glutamate toxicity in vitro. Although the neuroprotective mechanism of action of gabapentin is currently unknown, it is hypothesized here that gabapentin decreases the rate of formation of glutamate derived from the branched-chain amino acids (BCAAs) leucine, isoleucine, and valine. The proposed decrease in formation of glutamate from BCAAs may decrease the pool of releasable glutamate and therefore compensate for diminished glutamate uptake capacity and/or abnormal glutamate metabolism in patients with ALS. CONCLUSIONS: Based on this rationale, it is proposed that gabapentin may provide a beneficial effect in the treatment of patients with ALS.

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PubMed1997

Use of gabapentin in pain management.

There have been many proposed uses for gabapentin, including midscapular pain secondary to radiation myelopathy, RSD, neuropathic pain, postherpetic neuralgia, and migraine prophylaxis. However, the published reports consist of a small number of patients and limited data. Limited data provided in published case reports do not allow adequate evaluation of expected adverse effects or efficacy. It is unclear whether gabapentin is more effective for a specific type of pain and how gabapentin may compare with placebo or other therapeutic alternatives. Therefore, randomized, double-blind, placebo-controlled, prospective studies are warranted to further elucidate gabapentin uses beyond what is recommended by the Food and Drug Administration. Gabapentin should only be considered for pain management after well-established therapies have failed to produce desired outcomes.

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PubMed2004

A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats.

BACKGROUND: Gabapentin and pregabalin have wide-ranging therapeutic actions, and are structurally related to the inhibitory neurotransmitter GABA. Gabapentin, pregablin and GABA can all modulate voltage-activated Ca2+ channels. In this study we have used whole cell patch clamp recording and fura-2 Ca2+ imaging to characterise the actions of pregabalin on the electrophysiological properties of cultured dorsal root ganglion (DRG) neurones from neonatal rats. The aims of this study were to determine whether pregabalin and gabapentin had additive inhibitory effects on high voltage-activated Ca2+ channels, evaluate whether the actions of pregabalin were dependent on GABA receptors and characterise the actions of pregabalin on voltage-activated potassium currents. RESULTS: Pregabalin (25 nM - 2.5 microM) inhibited 20-30% of the high voltage-activated Ca2+ current in cultured DRG neurones. The residual Ca2+ current recorded in the presence of pregabalin was sensitive to the L-type Ca2+ channel modulator, Bay K8644. Saturating concentrations of gabapentin failed to have additive effects when applied with pregabalin, indicating that these two compounds act on the same type(s) of voltage-activated Ca2+ channels but the majority of Ca2+ current was resistant to both drugs. The continual application of GABA, the GABAB receptor antagonist CGP52432, or intracellular photorelease of GTP-gamma-S had no effect on pregabalin-induced inhibition of Ca2+ currents. Although clear inhibition of Ca2+ influx was produced by pregabalin in a population of small neurones, a significant population of larger neurones showed enhanced Ca2+ influx in response to pregabalin. The enhanced Ca2+ influx evoked by pregabalin was mimicked by partial block of K+ conductances with tetraethylammonium. Pregabalin produced biphasic effects on voltage-activated K+ currents, the inhibitory effect of pregabalin was prevented with apamin. The delayed enhancement of K+ currents was attenuated by pertussis toxin and by intracellular application of a (Rp)-analogue of cAMP. CONCLUSIONS: Pregabalin reduces excitatory properties of cultured DRG neurones by modulating voltage-activated Ca2+ and K+ channels. The pharmacological activity of pregabalin is similar but not identical to that of gabapentin. The actions of pregabalin may involve both extracellular and intracellular drug target sites and modulation of a variety of neuronal conductances, by direct interactions, and through intracellular signalling involving protein kinase A.

Amines↗
PubMed2006

Effect of the administration of tiagabine and gabapentin on rabbit electroencephalogram activity.

New generation antiepileptic drugs, including gabapentin and tiagabine, are used in monotherapy or in combination with other drugs for specific seizure types. The multidirectional mechanism of activity and varied pharmacological properties of these drugs suggest that they could also be used in the therapy of other diseases. A possible limitation of new generation antiepileptic drugs is the incidence of CNS-related adverse effects. Few studies have assessed the effect of new antiepileptic drugs on electroencephalogram (EEG) recordings in subjects using these drugs for diseases other than epilepsy. The aim of this study was to determine the effects of tiagabine and gabapentin on EEG recordings from the midbrain reticular formation, dorsal hippocampus and frontal cortex in rabbits. Tiagabine was administered orally at a single dose of 5 and 20 mg kg(-1), or repeatedly at a dose of 5 mg kg(-1) (twice a day) for 14 days. Gabapentin was administered orally at a single dose of 25 and 100 mg kg(-1), or repeatedly at a dose of 25 mg kg(-1) (twice a day) for 14 days. Both tiagabine and gabapentin caused changes indicative of CNS inhibitory properties, which may be associated with the adverse effects of the drugs. After repeated doses of the drugs, the changes in EEG recordings were less pronounced than after single doses, which may indicate adaptive changes. The hippocampus was found to be the least sensitive to the effect of gabapentin.

Amines↗
PubMed2001

Rapid initiation of gabapentin: a randomized, controlled trial.

OBJECTIVE: To compare the tolerability of two different dose-initiation regimens of gabapentin for the adjunctive treatment of partial seizures. BACKGROUND: Patient compliance is a key feature of successful outpatient pharmacologic therapy for epilepsy, and one aspect of compliance is simplicity of initiation. By using a rapid titration rate, leading to a rapid therapeutic gabapentin dose, perhaps there could be an improvement with compliance. METHODS: Male or female patients, at least 12 years old, with a recent history of partial seizures with or without secondary generalization, were randomized to receive gabapentin (following a blinded placebo period of an undisclosed number of days) as either a Slow initiation (300 mg day 1, 600 mg day 2, then 900 mg/day) or a Rapid initiation (900 mg/day immediately following the placebo lead-in). RESULTS: Starting gabapentin therapy at an initial therapeutic dosage of 900 mg/day is well tolerated by patients with epilepsy and is as safe as initiating with a titration schedule over 3 days. Of the four most common adverse events (somnolence, dizziness, ataxia, fatigue), only one, dizziness, occurred more often in the nontitrated (Rapid initiation) group than in the titrated (Slow initiation) group. CONCLUSION: Initiation of gabapentin at 900 mg/day is as well tolerated as is a 3-day titration, except for a higher incidence of dizziness.

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PubMed2002

Modulation of cerebral GABA by topiramate, lamotrigine, and gabapentin in healthy adults.

BACKGROUND: Anticonvulsant drugs have multiple mechanisms of action. Recent in vivo MRS studies suggest that cerebral gamma-aminobutyric acid (GABA) increases occur with the administration of certain anticonvulsants in humans. OBJECTIVE: To investigate the effect of topiramate, gabapentin, and lamotrigine on cerebral GABA concentrations in healthy volunteers and correlate the GABA concentrations with serum drug levels. METHODS: Seventeen healthy adults were randomly assigned to receive topiramate, gabapentin, and lamotrigine and underwent GABA measurements using a 4.1-T magnet from a 13.5-mL volume over the occipital region. GABA concentrations and serum levels were measured at 3 and 6 hours following administration of an acute single dose of one of the drugs. Thereafter, drugs were titrated over 4 weeks to target doses, with GABA measurements performed at 2 and 4 weeks. RESULTS: Cerebral GABA concentrations rose 70% in the acute phase compared with baseline for topiramate. GABA rose 48% at 6 hours with gabapentin but not with lamotrigine. With long-term dosing and once target doses were achieved at 4 weeks, significant elevations in GABA were observed compared with baseline for all three drugs (topiramate 46%, gabapentin 25%, lamotrigine 25%). CONCLUSION: This study demonstrates that single doses of topiramate and gabapentin increase cerebral GABA concentrations acutely (hours) in healthy individuals, but all drugs at clinically utilized doses increase cerebral GABA at 4 weeks. These results suggest that the mechanisms of action of anticonvulsant drugs are more complex and are likely to be multiple in nature.

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PubMed2002

Treatment of restless legs syndrome with gabapentin: a double-blind, cross-over study.

OBJECTIVE: To assess the effects of gabapentin on sensory and motor symptoms in patients with restless legs syndrome (RLS). METHODS: Patients with RLS (22 idiopathic, 2 secondary to iron deficiency) were randomized and treated for 6 weeks with either gabapentin or placebo. After a 1-week washout they crossed over to the alternative treatment for 6 weeks. Patients were rated at baseline and at scheduled intervals by the RLS Rating Scale, Clinical Global Impression, pain analogue scale, and Pittsburgh Sleep Quality Index. At the end of each treatment period, all-night polysomnography was performed. RESULTS: Compared to placebo, gabapentin was associated with reduced symptoms on all rating scales. In addition, sleep studies showed a significantly reduced periodic leg movements during sleep (PLMS) index and improved sleep architecture (increased total sleep time, sleep efficiency, and slow wave sleep, and decreased stage 1 sleep). Patients whose symptoms included pain benefited most from gabapentin. The mean effective dosage at the end of the 6-week treatment period was 1,855 mg, although therapeutic effects were already observed at the end of week 4 (1,391 mg). CONCLUSIONS: Gabapentin improves sensory and motor symptoms in RLS and also improves sleep architecture and PLMS.

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PubMed2006

Gabapentin: an alternative to the cyclooxygenase-2 inhibitors for perioperative pain management.

The cyclooxygenase-2 inhibitor, rofecoxib, was a popular analgesic adjuvant for improving perioperative pain management. We designed this placebo-controlled study to test the hypothesis that gabapentin could produce similar reductions in postoperative pain and opioid analgesic usage, thereby improving the recovery process. One hundred patients undergoing abdominal hysterectomy procedures were randomly assigned to one of four treatment groups: 1) control group received placebo capsules and pills before and for 2 days after surgery, 2) rofecoxib group received 50 mg/d PO and placebo capsules before and after surgery and, 3) gabapentin group received 1.2 g/d PO and placebo pills before and after surgery, and 4) combination group received rofecoxib 50 mg/d and gabapentin 1.2 g/d PO before and after surgery. The anesthetic technique was standardized and the postoperative assessments included verbal rating scales for pain and sedation, IV morphine usage, quality of recovery assessment, recovery of bowel function, resumption of normal activities, and patient satisfaction with their pain management. Postoperative pain scores were significantly reduced in all three analgesic treatment groups (versus control group). Compared with the control group, patient-controlled analgesia morphine usage was also significantly reduced in the 3 analgesic treatment groups at 1, 8, 24, and 30 h after surgery. Total PCA morphine usage was decreased by 43%, 24%, and 50% in groups 2, 3, and 4, respectively, compared with group 1. Oral analgesic consumption was also smaller in groups 2 and 4 when compared with the control group. The opioid-sparing effects of rofecoxib and gabapentin lead to a faster recovery of bowel function. Discharge eligibility scores in groups 2 and 4 were improved at 24 h when compared with group 1, and patient satisfaction with postoperative pain management was significantly higher at 24 h in all 3 analgesic treatment groups. At the 72 h follow-up, all of the patients in group 4 were completely satisfied with their pain management compared with only 32%, 64%, and 72% in groups 1, 2, and 3, respectively. Gabapentin (1.2 g/d PO) appears to be an acceptable alternative to rofecoxib (50 mg/d PO) for short-term use as an adjuvant to opioid analgesics in patients undergoing lower abdominal surgery.

Adult↗
PubMed2006

A single preoperative dose of gabapentin (800 milligrams) does not augment postoperative analgesia in patients given interscalene brachial plexus blocks for arthroscopic shoulder surgery.

BACKGROUND: Inadequate analgesia is common after shoulder arthroscopy. Both interscalene blocks and gabapentin are effective methods of pain management under various circumstances. We tested the hypothesis that gabapentin augments postoperative analgesia provided by interscalene brachial plexus block in patients having ambulatory arthroscopic shoulder surgery. METHODS: Sixty patients were randomly assigned to receive oral gabapentin, 800 mg, or placebo 2 h before surgery. An interscalene brachial plexus block with 0.3 mL/kg of 0.5% ropivacaine was performed. General anesthesia was maintained with sevoflurane and included a single 1-microg/kg dose of remifentanil. Postoperative analgesia was initially provided with morphine and subsequently with ketoprofene (150 mg orally twice daily) and a combination of 400 mg acetaminophen and 30 mg dextropropoxyphene as needed. Pain scores, analgesic requirements, and side effects were assessed in the ambulatory unit and at home for 48 h. RESULTS: Emergence from general anesthesia was similar in both groups. There were no significant differences in pain scores, first postoperative request for analgesia, or oral analgesic consumption. The incidence of side effects was comparable in both groups, except that headaches were less frequent in the gabapentin group. CONCLUSION: A single preoperative dose of gabapentin (800 mg) does not augment postoperative analgesia in patients given interscalene brachial plexus blocks for arthroscopic shoulder surgery.

Adult↗
PubMed2002

Gabapentin's effect on agitation in severely and persistently mentally ill patients.

OBJECTIVE: To study the effects of adjunctive gabapentin on agitation in severely and persistently mentally ill (SPMI) inpatients. METHOD: Eleven chronic SPMI inpatients on stable psychotropic medication regimens were evaluated before and after the initiation of adjunctive gabapentin for six months. The following psychometric tests were used: Brief Psychiatric Rating Scale (BPRS), Corrigan Agitated Behavior Scale (CABS), and Clinical Global Impression (CGI)-Severity. Data collection was accomplished via retrospective chart review. An internal reliability check indicated that a chart review BPRS is significantly predictive of one performed face-to-face. RESULTS: Statistically significant reductions were found at six months for each assessment instrument (p < 0.05, two-tailed). BPRS scores were reduced from 40.6 to 33.2, CABS from 34.4 to 25.0, and CGI-Severity from 5.9 to 5.3. The bulk of the BPRS reduction was accounted for by several subscores exclusive of those assessing affective/anxious symptomatology. Adverse effects were minimal. Two patients were discharged 12 and 17 months after implementation of gabapentin. CONCLUSIONS: Adjunctive gabapentin appears to be associated with a reduction in agitation in chronically hospitalized SPMI patients. Controlled, prospective trials are needed before any definitive conclusion can be drawn regarding the role of gabapentin in the treatment of this group of patients.

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