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OPIOID
ANALGESICS
Assoc. Prof. Ivan Lambev
E-mail: itlambev@mail.bg
Pain is the most common symptom for which patients
see a doctor. Different types of drugs are used for
treatment of pain. In general, they include:
Morphine Poppy
Prof. Gay Lussac Morpheus
(1778–1850) and Iris
Opium contains two groups of alkaloids:
• with phenantrene structure
(morphine, codeine, thebaine)
• with isochinoline structure (papaverine, noscapine).
Problems are:
- Desire for the drug
- Want to experience the “rush” – positive
- Don’t want the withdrawal – negative
- Some opioids, e.g. codeine & pentazocine,
are much less likely to cause dependence
Principal uses of morphine and other opioids
•Relief of moderate to severe acute pain
(or chronic pain often in terminal illness)
•Brief relief of anxiety in serious and frightening
diseases accompanied by pain (e.g. traumas
but without commotio)
•Relief of dyspnoe in acute left ventricular failure,
and in terminal cases
•Premedication in surgery
•Treating of dry cough (usually codeine,
dextromethorphan).
Alcaloids
•Strong analgesics:
Morphine Hydrochloride
- 1% 1 ml (= 10 mg) i.m. with 1 mg Atropine
- Morphine Sulfate
1 tab./12 h p.o. in humans
•Antitussive and
week analgesic:
- Codeine
10–20 mg/dose
Semisynthetic derivative (opioid analogs)
Morphine derivatives
•Ethylmorphine, Heroin
Codeine derivatives
•Dextromethorphan (antitusive agent)
•Dihydrocodeine
(Dicodin®): 1 tab./12 h
•Hydrocodone (Vicodin®)
•Oxycodone: p.o.
Thebaine derivatives
•Buprenorphine, Etorphine
ETORPHINE
(strong μ/κ/δ-agonist) with remarkable
very high potency, more than 1000–3000 times
that of morphine. It is a semisynthetic derivative
of thebaine.
It is used im combination with
Acepromazine (phenothiazine derivative)
to immobilize large wild animals for trapping
and research purposes, since the required
dose, even for an elephant, is small enough
to be incorporated into a dart or pellet.
Targin® (oxycodone & naloxone)
Suboxone® (buprenorphine & naloxone)
Targin® (oxycodone & naloxone)
Suboxone® (buprenorphine & naloxone)
HEROIN
(diamorphine – BAN, diacetylmorphine)
Similar action to morphine
More active than morphine
More lipid soluble – crosses BBB faster to give
greater rush
Shorter duration of action than morphine
Synthetic derivatives
PHENYLPIPERIDINES
pethidine, fentanyl
METHADONES
methadone, dextropropoxyphene
BENZOMORPHANS
pentazocine
TRAMADOL
PETHIDINE
(Meperidine – USAN; Lydol® – Sopharma)
Sol. 5% 2 ml (= 100 mg/2 ml) s.c./i.m.
Almost identical to morphine
Tends to cause restlessness
rather than sedation
Antimuscarinic effects: dry mouth
blurred vision
Less antitussive
Shorter duration of action (4-6 h) –
preferred in labour
TRAMADOL
Tramadol provides moderate pain relief. Because of its dual
actions as a µ-agonist and monoamine transport inhibitor,
it produces less respiratory depression for a given analgesic
effect. Tramadol is a weak agonist at µ-receptors. Its
major metabolites are more potent agonists at µ-receptors.
Tramadol also inhibits monoamine transporters
(principally NA and 5-HT) which is thought to produce
analgesia synergistically
with µ-agonism.
FENTANYL
>80 times more potent than
morphine in analgesia
Actions similar to morphine
Main use is in anaesthesia, used in
conjunction with droperidol, a
neuroleptic, producing
neuroleptanalgesia
Durogesic® (Fentanyl):
TTS/72 h
Durogesic
Durogesic
TTS
NEUROLEPTANALGESIA
•Fentanyl 100 mcg +
•Droperidol 5 mg i.m.
Similar to Fentanyl:
•Alfentanil (NB: without “y”)
•Sufentanil (NB: without “y”)
METHADONE