Monograph
N02AX02 - Tramadol |
Propably not porphyrinogenic |
PNP |
Rationale
Tramadol is metabolised by the cytochrome P450 isoenzymes, CYP 3A4 and CYP 2D6, but it is not an inducer or an inhibitor of the enzymes. Probably low PXR-affinity of the parent substance. Physiological effects on PXR/CAR-activation by serotonergic action is probably without relevance to acute porphyria. There are 12 reports (per February 2010) of safe use in carriers of acute porphyria.
Chemical description
(±)-trans-2-Dimethylaminomethyl-1-(3-methoxyphenyl)cyclohexanol hydrochloride. M=300. Terminal tertiary amine function.
Therapeutic characteristics
Tramadol is used for moderate to severe pain. It is a non-selective, complete agonist of µ-, δ- and κ opioid receptors with a higher affinity for µ-receptors. Other mechanisms contributing to the analgesic effect are the inhibition of the neural noradrenalin reuptake and an enhanced release of serotonine. Common confounding side-effects are nausea, vomiting, obstipation. Overdosage may give cardiovascular collapse or respiratory arrest.
Hepatic exposure
Probably significant.
Metabolism and pharmacokinetics
In humans the cytochrome P450 isoenzymes, CYP 3A4 and CYP 2D6 are involved in the metabolism of tramadol. It is a substrate of these enzymes (Rendic 2002 ; Martindale 2009)and clinical interaction studies give evidence of absence of significant capacity for CYP-induction or inhibition. Tramadol is mainly metabolised by means of N- and O-demethylation and conjugation of the O-demethylation products with glucuronic acid. Only O-desmethyltramadol is pharmacologically active (The electronic Medicines Compendium (eMC),UK). On oral administration it has relatively low first-pass effect, maximum of 30 per cent. High tissue affinity Vdb= around 203 l. After N-demethylation via CYP 3A4, the principal pharmacodynamically active O-demethylated metabolite is generated by CYP 2D6, which exhibits genetic polymorphism (Martindale 2009). The N-methylated parent drug is water soluble and thus probably of relatively low PXR-affinity.
Preclinical data
Observed to give rise to porphyrin accumulation in chicken embryo system, (Lambrecht,1999).
Personal communication
S.Thunell 2004, patient inquiry: tolerated (n=1).
Published experience
No observations of clinical porphyrogenicity published.
IPNet drug reports
Uneventful use reported in 15 patients with acute porphyria.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Lambrecht et al, Biochem Pharmacol 1999, Effects of antihypertenand analgesics on hepatic porphyrin accum, implic for clin porphyria.
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| 2. | Rendic S et al, Drug Metabolism Reviews 2002, Summary of information on human cyp enzymes Human P40 metabolism data.
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| * | Drug reference publications | |
| 3. | Martindale 2009 online.
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| * | Drug interaction databases | |
| 4. | LEXI-COMP online.
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| * | Summary of Product Characteristics | |
| 5. | The electronic Medicines Compendium (eMC),UK.
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Tradenames
This list comprises raw data collected from different countries.
In some cases, a more comprehensive list of available drug packages is included.
Consequently, very similar terms may therefore appear multiple times.
Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
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Tramadol HCl Aurobindo 50 mg, capsules, hard · Tramadol HCl Aurobindo Retard 100 mg, tabletten met gereguleerde afgifte · Tramadol HCl Aurobindo Retard 150 mg, tabletten met gereguleerde afgifte · Tramadol HCl Aurobindo Retard 200 mg, tabletten met gereguleerde afgifte · Tramadol HCl capsule CF 50 mg, capsules · Tramadol HCl druppels CF 100 mg/ml, druppels voor orale toediening · Tramadol HCL Duiven retard 100 mg, tabletten met gereguleerde afgifte · Tramadol HCL Duiven retard 150 mg, tabletten met gereguleerde afgifte · Tramadol HCL Duiven retard 150 mg, tabletten met gereguleerde afgifte · Tramadol HCL Duiven retard 200 mg, tabletten met gereguleerde afgifte · Tramadol HCl Nevik 50 mg, capsules · Tramadol HCl Prolepha Retard 100 mg, tabletten met gereguleerde afgifte · Tramadol HCl Retard 100 mg Teva, tabletten met gereguleerde afgifte · Tramadol HCl Retard 100 mg, tabletten met gereguleerde afgifte · Tramadol HCl Retard 150 mg Teva, tabletten met gereguleerde afgifte · Tramadol HCl Retard 150 mg, tabletten met gereguleerde afgifte · Tramadol HCl Retard 200 mg Teva, tabletten met gereguleerde afgifte · Tramadol HCL Retard 200 mg, tabletten met gereguleerde afgifte · Tramadol HCl Retard Viatris 100 mg, harde capsules met verlengde afgifte · Tramadol HCl Retard Viatris 100 mg, tabletten met verlengde afgifte · Tramadol HCl Retard Viatris 150 mg, harde capsules met verlengde afgifte · Tramadol HCl Retard Viatris 150 mg, tabletten met verlengde afgifte · Tramadol HCl Retard Viatris 200 mg, harde capsules met verlengde afgifte · Tramadol HCl Retard Viatris 200 mg, tabletten met verlengde afgifte · Tramadol HCl Retard Viatris 50 mg, harde capsules met verlengde afgifte · Tramadol HCl Sandoz bruis 50 mg, bruistabletten · Tramadol HCl Sandoz capsule 50 mg, capsules · Tramadol HCl Sandoz retard 100, tabletten met verlengde afgifte 100 mg · Tramadol HCl Sandoz retard 150, tabletten met verlengde afgifte 150 mg · Tramadol HCl Sandoz retard 200, tabletten met verlengde afgifte 200 mg · Tramadol HCl zetpil CF 100 mg, zetpillen · Tramadolhydrochloride capsules, capsules 50 mg · Tramal 100, injectievloeistof 100 mg/2 ml · Tramal, druppels voor oraal gebruik, oplossing 100 mg/ml 
Contramal · Contramal 100 mg/2 ml sol. inj./perf. i.v./i.m. amp. · Contramal 100 mg/ml gtts buv. sol. flac. compte-gouttes · Contramal 100 mg/ml sol. buv. pompe dos. · Contramal 50 mg g?l. · Contramal Retard 100 mg compr. lib. prol. · Contramal Retard 150 mg compr. lib. prol. · Contramal Retard 200 mg compr. lib. prol. · Contramal Retard 50 mg compr. lib. prol. · Tradonal · Tradonal 100 mg gtts buv. sol. · Tradonal 100 mg sol. inj./perf. i.v./i.m. amp. · Tradonal 50 mg g?l. · Tradonal Odis 50 mg compr. orodisp. · Tradonal Retard 100 mg g?l. lib. modif. · Tradonal Retard 150 mg g?l. lib. modif. · Tradonal Retard 200 mg g?l. lib. modif. · Tradonal Retard 50 mg g?l. lib. modif. · Tramadol · Tramadol EG 100 mg/2 ml sol. inj. s.c./i.v./i.m. amp. · Tramadol EG 100 mg/ml gtts buv. sol. flac. compte-gouttes · Tramadol EG 50 mg comp. · Tramadol Krka 100 mg compr. lib. prol. · Tramadol Krka 100 mg/2 ml sol. inj./perf. s.c./i.v./i.m. flac. · Tramadol Krka 150 mg compr. lib. prol. · Tramadol Krka 200 mg compr. lib. prol. · Tramadol Krka 50 mg g?l. · Tramadol Krka 50 mg/ml sol. inj./perf. s.c./i.v./i.m. flac. · Tramadol Retard EG 100 mg compr. lib. prol. · Tramadol Retard EG 150 mg compr. lib. prol. · Tramadol Retard EG 200 mg compr. lib. prol. · Tramadol Sandoz 100 mg compr. lib. prol. · Tramadol Sandoz 100 mg/ml gtts buv. sol. pompe dos. · Tramadol Sandoz 150 mg compr. lib. prol. · Tramadol Sandoz 200 mg compr. lib. prol. · Tramadol Sandoz 50 mg g?l. · Tramadol Uno Sandoz 200 mg compr. lib. prol. · Tramium · Tramium 100 mg g?l. lib. prol. · Tramium 150 mg g?l. lib. prol. · Tramium 200 mg g?l. lib. prol. 
ADOLONTA 100 mg/ ml SOLUCION ORAL · ADOLONTA 100 mg/2 ml SOLUCION INYECTABLE Y PARA PERFUSION · ADOLONTA 50 mg CAPSULAS DURAS · ADOLONTA RETARD 100 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ADOLONTA RETARD 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ADOLONTA RETARD 200 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ADOLONTA RETARD 50 mg COMPRIMIDOS DE LIBERACION PROLONGADA · Captor Simplex · Captor Simplex 100 mg Capsulas Duras de Liberacion Prolongada · Captor Simplex 150 mg Capsulas Duras de Liberacion Prolongada · Captor Simplex 200 mg Capsulas Duras de Liberacion Prolongada · CEPARIDIN 50 mg CAPSULAS EFG · Dolodol · DOLODOL 200 mg CAPSULAS DE LIBERACION PROLONGADA · DOLODOL FLAS 50 mg COMPRIMIDOS BUCODISPERSABLES · Mabron 100 mg/2 ml Solucion Inyectable y Para Perfusion efg · Tioner 100 mg/ml Solucion Oral · TIONER 50 mg CAPSULAS DURAS · TIONER RETARD 100 mg COMPRIMIDOS DE LIBERACION PROLONGADA · TIONER RETARD 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA · TIONER RETARD 200 mg COMPRIMIDOS DE LIBERACION PROLONGADA · TRADONAL RETARD 100 mg CAPSULAS DURAS DE LIBERACION PROLONGADA · TRADONAL RETARD 150 mg CAPSULAS DURAS DE LIBERACION PROLONGADA · TRADONAL RETARD 200 mg CAPSULAS DURAS DE LIBERACION PROLONGADA · TRADONAL RETARD 50 mg CAPSULAS DURAS DE LIBERACION PROLONGADA · Tramadol · Tramadol Almus 50 mg Capsulas Duras efg · Tramadol Andromaco 100 mg/2 ml Solucion Inyectable y Para Perfusion efg · Tramadol Andromaco 100 mg/ml Solucion Oral efg · Tramadol Andromaco 50 mg Capsulas Duras efg · TRAMADOL ARISTO 100 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL ARISTO 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL ARISTO 200 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · Tramadol Aristo 50 mg c?Psulas Duras efg · Tramadol Asta · TRAMADOL ASTA MEDICA 100 mg SOLUCION INYECTABLE EFG · Tramadol Asta Medica 100 mg/ml Gotas Orales en Soluci?n efg · TRAMADOL ASTA MEDICA 50 mg c?psulas EFG · Tramadol Aurovitas 50 mg Capsulas Duras efg · Tramadol Aurovitas 50 mg/ml Solucion Inyectable y Para Perfusion efg · Tramadol Basi 50 mg/ml Soluci?n Inyectable efg · TRAMADOL CINFA 50 mg CAPSULAS DURAS EFG · TRAMADOL CODRAMOL 50 mg CAPSULAS DURAS EFG · TRAMADOL FARMALIDER 100 mg/ml SOLUCION ORAL EFG · TRAMADOL KERN PHARMA 50 mg, CAPSULAS DURAS EFG · Tramadol Krka 100 mg/2 ml Solucion Inyectable y Para Perfusion efg · Tramadol Krka 100 mg/ml Gotas Orales en Solucion efg · Tramadol Krka 150 mg Comprimidos de Liberacion Prolongada efg · Tramadol Krka 200 mg Comprimidos de Liberacion Prolongada efg · Tramadol Krka 50 mg Capsulas Duras efg · Tramadol Krka 50 mg/1 ml Solucion Inyectable y Para Perfusion efg · Tramadol Mabo 50 mg Capsulas Duras efg · Tramadol Normon 100 mg Capsulas Duras · Tramadol Normon 50 mg c?Psulas Duras efg · Tramadol Retard Andromaco 100 mg Comprimidos de Liberacion Prolongada efg · TRAMADOL RETARD ANDROMACO 150 MG COMPRIMIDOS DE LIBERACIoN PROLONGADA EFG · Tramadol Retard Andromaco 200 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Andromaco 50 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Aurovitas Spain 100 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Aurovitas Spain 150 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Aurovitas Spain 200 mg Comprimidos de Liberacion Prolongada efg · TRAMADOL RETARD COMBIX 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL RETARD COMBIX 200 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL RETARD NORMON 100 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL RETARD NORMON 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · Tramadol Retard Stada 100 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Stada 150 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Stada 200 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Teva 100 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Teva 150 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Teva 200 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Teva-Ratiopharm 100 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Teva-Ratiopharm 150 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Teva-Ratiopharm 200 mg Comprimidos de Liberacion Prolongada efg · Tramadol Retard Viatris 100 mg Comprimidos de Liberaci?n Prolongada efg · Tramadol Retard Viatris 150 mg Comprimidos de Liberaci?n Prolongada efg · Tramadol Retard Viatris 200 mg Comprimidos de Liberaci?n Prolongada efg · TRAMADOL STADA 50 mg CAPSULAS DURAS EFG · Tramadol tad 100 mg Comprimidos de Liberacion Prolongada efg · Tramadol tad 150 mg Comprimidos de Liberacion Prolongada efg · Tramadol tad 200 mg Comprimidos de Liberacion Prolongada efg · TRAMADOL TARBIS 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL TARBIS 200 mg COMPRIMIDOS DE LIBERACION PROLONGADA EFG · TRAMADOL TEVA-RATIOPHARM 50 mg CAPSULAS DURAS EFG · TRAMADOL VIR 100 mg/ml GOTAS ORALES EN SOLUCION EFG · ZYTRAM 150 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ZYTRAM 200 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ZYTRAM 300 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ZYTRAM 400 mg COMPRIMIDOS DE LIBERACION PROLONGADA · ZYTRAM BID 75 mg COMPRIMIDOS DE LIBERACION PROLONGADA 
Contramal · Fortradol · Prontalgin · Tradogut · Tradonal · Traflash · Tralodie · Tramadolo · Tramalin 
CLORHIDRAT DE TRAMADOL BIOEEL 50 mg · MABRON 100 mg/2 ml · MABRON RETARD 100 mg · MABRON RETARD 150 mg · MABRON RETARD 200 mg · TRAMACALM 50 mg · TRAMADOL 100 mg/2 ml · TRAMADOL 50 mg · TRAMADOL 50 mg/1 ml · TRAMADOL ARENA 50 mg · TRAMADOL KALCEKS 50 mg/ml · TRAMADOL RETARD 100 mg · TRAMADOL RETARD 150 mg · TRAMADOL RETARD 200 mg · TRAMAG 50 mg · TRAMAL RETARD 100 mg · TRAMAL RETARD 150 mg · TRAMAL RETARD 200 mg 
Aceon · Brimisol · Brimisol PR · Dromadol SR · Dromadol XL · Invodol · Invodol SR · Larapam · Larapam SR · Mabron · Maneo · Marol · Maxitram · Maxitram SR · Nobligan · Oldaram · Tilodol · Tilodol SR · Tradorec · Tradorec XL · Tramadol · Tramake · Tramake Insts · Tramquel · Tramquel SR · Tramulief · Tramulief SR · Zamadol · Zamadol 24hr · Zamadol Melt · Zamadol SR · Zeridame · Zeridame SR · Zydol · Zydol SR · Zydol XL · Zytram 
Dolatramyl · Dolol · Dolol Retard UNO · Gemadol Retard · Mandolgin · Nobligan · Nobligan Retard · Tadol · Tradolan · Tradolan Retard · Tradonal Retard · Tramadol Actavis · Tramadol Krka · Tramadol Retard Actavis · Tramadol Retard Hexal · Tramadol Vitabalans · Tramadolhydrochlorid 2care4 
Nobligan · Nobligan Retard · Tramadol Actavis · Tramadol aliud · Tramadol Hexal · Tramadol panpharma · Tramadol stada · Tramadol-ratiopharm · Tramagetic OD · Tramagetic Retard · Tramal · Zytram BID · Zytram XL 
Poltram · Poltram 100 · Poltram 50 · Poltram Retard 100 · Poltram Retard 150 · Poltram Retard 200 · Tramadol Aurobindo · Tramadol Aurovitas · Tramadol Kalceks · Tramadol Krka · Tramadol Synteza · Tramadol Vitabalans · Tramal · Tramal Retard 100 · Tramal Retard 150 · Tramal Retard 200 · Tramal Retard 50 · Tramundin 
Contramal Retard-100 · Contramal Retard-150 · Contramal Retard-200 · Contramal Retard-50 · Tradonal · Tradonal Odis · Tradonal Retard · Tramadol eg · Tramadol Lannacher · Tramadol Retard eg · Tramal · Tramal Long · Tramium 
Tradolan · Tram?l-L · Tramadol Actavis · Tramadol Krka · Tramól-L 
Dolatramyl · Tradolan Retard · Tramadol Hexal · Tramadol Krka · Tramadol Retard Hexal · Tramadol Retard Sandoz · Tramadol Vitabalans · Tramal · Tramal Retard · Tramium 
Mabron · Mabron SR · Tramadol Basi · Tramadol Kalceks · Tramadol Krka · Tramadol Lannacher · Tramadol Vitabalans · Trametalin 
TramaFort® · Trodon
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