Pharmacopeia

CWP-0261

TRAMADOL

Neurology & Sedation · Neurology & Sedation · Level 2

Core pharmacology

Class Group

Opiate Analgesic

Legacy Cicm Level

Level 2

Introduction

Is a synthetic opioid – cyclohexanol derivative
Racemic mix.

Indications Uses

Analgesia

Presentation

immediate release, 12 hour release and 24 hour release
tablets, IV

Mechanism of action

mod affinity for μ receptors, weak κ, δ
-in spinal desc inh pathways by inh of neuronal reuptake of norad&serotonin
-presynaptic stim of seritonin release

Onset Peak Duration

onset / duration ~1 hour / 9 hours (immediate release)

Physiological effects

CNS:
- Analgesia
- Hallucinations
- Confusion
- Delirium
- Agitation
- Seizures
- Coma (Serotonin syndrome)

Respiratory depression and
constipation

Adverse Effects Toxicity

Dysphoria,Euphoria. Miosis (excitation of Edinger-Westphal nucleus)
N/V -CTZ stim. Serotonin syndrome with SSRI /SNRI/MAO/TCA
Less resp dep than morphine
analgesic effect in CYP2D6 deficiency

Absorption

Bioavailability- 75% PO

Distribution

Crosses placenta
Lipid soluble-crosses BBB

Metabolism

Extensively hepatic via demethylation ,
glucuronidation, and sulfation; active metabolite by CYP2D6 (M1; O-desmethyl tramadol)

Excretion

Urine 90% (30% unchanged), 10% faeces.

Half-life

T1/2: ~6-8 hrs;
Act metab:7-9hrs;
old, hepatic/renal imp.

Route And Dose

Route- PO/IV
Dose- 50-100mg QID for all routes
(Relative pot 0.2)

Main Action

mod affinity for μ receptors, weak κ, δ

Additional pharmacology

Protein binding

Prot bind-20%

Volume of distribution

Vd- 2.5-3L/kg