Pharmacokinetics of tramadol and metabolites after injective administrations in dogs

Giorgi, Mario; Carlo, S. Del; Łebkowska‐Wieruszewska, Beata; Kowalski, C.; Saccomanni, Giuseppe

doi:10.2478/v10181-010-0027-y

Cited by 17 publications

(28 citation statements)

References 12 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In humans, it was reported that the minimum effective plasma concentrations of tramadol was 287.7 ng/ml [16]. Giorgi et al [6] reported that the minimum effective plasma concentration of tramadol as calculated for humans had been maintained for about 6-7 hr following a single IV administration of 4 mg/kg tramadol in dogs. We previously reported [10] that the plasma concentration of tramadol gradually decreased over time from approximately 2,000 ng/ml at 5 min to 500 ng/ml at 120 min after a single IV dose of 4 mg/kg tramadol in older dogs (8-10 years old) anesthetized with sevoflurane 1.3 MAC.…”

Section: Discussionmentioning

confidence: 99%

“…Some authors, especially in human studies, use the plasma concentration of M1 to determine the analgesic effect of tramadol, because the evidence indicates that M1 is responsible for most of the therapeutic effects rather than the parent drug [4]. Giorgi et al [6] stated that M1 might not be responsible for the major clinical effectiveness in dogs, because M1 was detected at a lower concentration than the minimum effective plasma concentration (40 ng/ml) reported in humans [7]. However, a higher M1 concentration (65 ± 16 ng/ml) was detected in dogs infused tramadol at a rate of 1.3 mg/kg/hr CRI following 1.5 mg/kg IV [26].…”

Section: Discussionmentioning

confidence: 99%

“…On the other hand, it was reported that the minimum effective plasma concentration of tramadol as calculated for humans had been maintained for about 6-7 hr following an intravenous administration (IV) of tramadol in dogs [6].…”

mentioning

confidence: 99%

See 2 more Smart Citations

Effects of a Single Bolus Intravenous Dose of Tramadol on Minimum Alveolar Concentration (MAC) of Sevoflurane in Dogs

Itami

Kawase

Tamaru

et al. 2013

The Journal of Veterinary Medical Science

View full text Add to dashboard Cite

ABSTRACT. Tramadol is an atypical opioid analgesic widely used in small animal practice. This study was designed to determine the effect of a single intravenous (IV) dose of tramadol on the minimum alveolar concentration (MAC) of sevoflurane in dogs. Six beagle dogs were anesthetized twice to determine the sevoflurane MAC with or without an administration of tramadol (4 mg/kg, IV) at 7 days interval. The sevoflurane MAC was determined using a tail clamp method in each dog ventilated with positive pressure ventilation. The tramadol administration produced a significant reduction in the sevoflurane MAC by 22.3 ± 12.2% (1.44 ± 0.28% with tramadol versus 1.86 ± 0.30% without tramadol, P=0.010). This MAC reduction had been determined from 122 ± 19 to 180 ± 41 min following the tramadol administration. During this period, the plasma concentrations of tramadol and its metabolite, O-desmethyltramadol (M1), decreased from 429 ± 64 to 332 ± 55 ng/ml and from 136 ± 24 to 114 ± 68 ng/ml, respectively, but these changes were not statistically significant. There was no significant difference in heart rate, mean arterial blood pressure and SpO 2 between the control and tramadol treatment. The dogs that received tramadol treatment sometimes breathed spontaneously. Therefore, their respiratory rates significantly increased, and PETCO 2 decreased during the MAC determination. In conclusion, the single IV dose of tramadol produced a significant reduction in the sevoflurane MAC in dogs.

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Effects of a Single Bolus Intravenous Dose of Tramadol on Minimum Alveolar Concentration (MAC) of Sevoflurane in Dogs

Itami

Kawase

Tamaru

et al. 2013

The Journal of Veterinary Medical Science

View full text Add to dashboard Cite

show abstract

“…Although it has been used for some time now, our understanding and ability to predict the time course of its pharmacological effects in animals are still hampered by the presence of active metabolites and the coexistence of opioid and non-opioid mechanisms. Recently, T has been reported to be metabolized faster to inactive metabolites N-desmethyl tramadol (M2) and O,N-didesmethyl tramadol (M5), in goats (Sousa et al, 2008), dogs (McMillan et al, 2008;Giorgi et al, 2009a;2009b;2009c;2009d;2010a;Kukanich and Papich, 2011), horses (Giorgi et al, 2007;Shilo et al, 2008;Cox et al, 2010;Giorgi et al, 2010b), llamas , alpacas (Giorgi et al, 2010c), peafowl (Black et al, 2010), hawks than in cats (Pypendop and Ilkiw, 2008). The use of T has also been suggested for zoo animals .…”

Section: Tramadolmentioning

confidence: 99%

Tramadol Vs Tapentadol: Anew Horizon in Pain Treatment?

Giorgi¹

2012

American Journal of Animal and Veterinary Sciences

View full text Add to dashboard Cite

Problem statement: Acute and chronic pain is a common presenting sign in animal species and human beings. Approach: Classical opioids provide very effective pain relief, although they may be less effective in the treatment of chronic pain due to their limited therapeutic windows and the induced opioid receptor down regulation. Atypical opioids, such as tramadol and tapentadol, have a dual mechanism of action and have been designed to overcome these issues through an opiate-sparing effect. Results: Tramadol activates mu opioid receptors and in addition, inhibits serotonin and noradrenalin reuptake. These actions are the result of the different enantiomers and tend to be reliant on their metabolism. Indeed, the O-desmethyltramadol phase I metabolite, is 200-300 times more potent for mu opioid receptor activation than the parental compound. For these reasons, the drug's effectiveness can vary among subjects. In veterinary medicine its effectiveness, especially after oral administration, is still uncertain and controversial. Tapentadol is a novel, atypical opioid with a unique mechanism of action. It was launched on the European drug market at the end of 2011. It has been proposed as the first representative of a new pharmacological class of centrally acting analgesics, namely, the mu opioid receptor agonist, noradrenalin reuptake inhibitors. The first human studies describe this molecule as safe and effective (equianalgesic to morphine). The drug has great potential for veterinary use because it exists as a single enantiomer only, it does not require metabolic activation to be effective and adverse effects triggered by the serotonin reuptake inhibition action are negligible. Conclusion/Recommendations: For these reasons, TAP is a promising compound however at this stage, more investigation is required before it can be recommended for regular use in veterinary medicine, the possibility of undesirable effects is yet to be entirely excluded.

show abstract

“…Ten min later (Giorgi et al 2010;Slingsby et al, 2015), anaesthesia was induced by intravenous (IV) administration of 2 mg/Kg propofol boluses (Cristalia Laboratories, Itapira, Brazil), repeated every 60 sec until loss of palpebral reflex. The total propofol induction dose (PID) was recorded.…”

Section: Experimental Designmentioning

confidence: 99%

Pre-emptive methadone or tramadol analgesia for mastectomy and ovariohysterectomy in bitches

Uscategui

Tiosso

Moro

et al. 2017

Rev Colomb Cienc Pecu

View full text Add to dashboard Cite

Analgesia preventiva con tramadol o metadona para mastectomia y ovario histerectomía en perrasAnalgesia preventiva com tramadol ou metadona para mastectomia e ováriohisterectomia em cadelas Abstract Background: mastectomy and ovariohysterectomy (OVH) in bitches are critical surgeries and pain control can be challenging. Objective: to evaluate the efficacy of pre-emptive analgesia with methadone (MET) or tramadol (TRA) in postoperative pain intensity, cardiorespiratory effects, and anaesthetic/analgesic consumption in female dogs undergoing mastectomy and OVH. Methods: a prospective randomized blind clinical trial was used to evaluate 48 bitches of various breeds, aged 10 ± 3.7 years, weighing 16 ± 12 Kg, and with multiple mammary tumours. The animals were distributed in two groups: TRA group received 5 mg/Kg tramadol and MET group 0.5 mg/Kg methadone intramuscularly, 10 min prior to anaesthesia induction with propofol followed by maintenance with isoflurane. Heart (HR) and respiratory (RR) rates, mean arterial pressure (MAP), propofol induction dose (PID), oxyhemoglobin saturation (SpO 2 ), end-tidal isoflurane concentration (EtISO), and carbon dioxide pressure (EtCO 2 ) were measured during the intra-operative period. Post-operative pain was evaluated for 12 h and rated according to the Melbourne scale. Rescue analgesia (0.5 mg/Kg methadone, 2 mg/Kg lidocaine, or 0.01 mg/Kg/min ketamine IV) was given when necessary and post-operative analgesic consumption recorded. Statistical tests were used to compare treatments. Results: rescue analgesia requirements, pain score, PID and analgesic consumption were significantly lower (p<0.05) in MET group. The HR was higher in TRA group, while EtCO 2 and MAP were higher in MET group (p<0.05). Conclusion: methadone was more effective than tramadol in pre-emptive analgesia but not completely adequate on controlling pain in bitches subjected to

show abstract

Pharmacokinetics of tramadol and metabolites after injective administrations in dogs

Cited by 17 publications

References 12 publications

Effects of a Single Bolus Intravenous Dose of Tramadol on Minimum Alveolar Concentration (MAC) of Sevoflurane in Dogs

Effects of a Single Bolus Intravenous Dose of Tramadol on Minimum Alveolar Concentration (MAC) of Sevoflurane in Dogs

Tramadol Vs Tapentadol: Anew Horizon in Pain Treatment?

Pre-emptive methadone or tramadol analgesia for mastectomy and ovariohysterectomy in bitches

Contact Info

Product

Resources

About