Analgesics : opioid medication

Class Drug Pk PD CU Toxicity

Phenyl piperidines Fentanyl, sufentanil IV, epi, Intrathecal, transderm, Strong MOR agonist Anesthetic CNS
Fentanyl & co transbucal Potent analgesic - Short time to effect - N,V,D
- fentanyl Poor GIT absorption Minimal cardio-depressant - Rapid termination - Muscle rigidity
- Sufentanil Highly lipid soluble Don’t release histamine - Mini cardio depressant at high dose
- Remifentanil Cross BBB 100 X morphin - Reduced dose of - Rapid resp dep
- alfentanil Redistribution from plasma Sufentalil = 1000X morphine volatile agents - Neuroexcitation,
T1/2 = 3 hrs CVS surgery , pts with poor seizure – High D
M – hepatic cardiac function CVS
E - renal Post op - ↓ HR, BP
Labor analgesia
Chronic pain
Remifentanil Continuous iv infusion Short painful procedures Long term
M – plasma esterases Rapid recovery
remifentanil acid Cestein for methadone add
E - renal
More rapid actn than fentanyl
Age & weigh affect clearance
No prolongation of effect on
repeat dosing
T ½ = 10 min

Phenyl piperidines Pethidine Well abs orally Vs morphine Analgesic sub morphine Atropine like effects
- Pethidine/ IM, SC – longer acting - better oral abs Preanesthetic med Od - norpethidine
meperidine Bioav – 50% - similar efficacy Labour anesthetic – less - tremors
- Diphenoxylate T3 – 10-15 min - equal sedation, fetal resp depression - mydriasiss
- loperamides M – liver  meperidic acid + analgesia, resp dep, - delirium
norpethidine abuse - convulsion
Norpethidine accumulates - less muscle spasmodic
E - urine action – less miosis,
constipation 7 urinary
retention
- rapid short acting
- non antitussive
- less histamine release
Tramadol Tramadol Oral iv Centrally acting antianlgesic
100mg = 10mg morphine Low opioid receptor actn –
5HT, NA reuptake inh
Spinal inhibition
Class Drug PK PD Indications toxicity