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Meperidine
Prepared by:
Nojoud al-tuwaijri
Definition:
• Meperidine or pethidine is a narcotic analgesic
Introduced in the 1930s, it produces effects that
are similar, but not identical, to morphine
(shorter duration of action and reduced
antitussive and antidiarrheal actions).
Uses:
• meperidine is used for the relief of moderate to
severe pain, most commonly in obstetrics and postoperative conditions.
• A unique characteristic to mepiridine over its opiate
family members is its ability to interrupt postoperative
shivering and shaking chills induced by amphotericin
B.
• it comes in both tablet and liquid form for oral
administration. The drug can also be administered by
injection into a large muscle or added to an
intravenous fluid.
Use of abuse:
• When abused, meperidine is taken orally,
injected and snorted .
• Street names: Pethidine, Demerol, and
Mepergan
Mechanism of action:
• Binds to opiate receptors in the CNS,
causing inhibition of ascending pain
pathways, altering the perception of and
response to pain; produces generalized CNS
depression
Effects of meperidine:
• The effects of meperidine are felt 10-15 minutes after
ingestion and typically last anywhere from 2-4 hours.
• mepiridine effects are very similar to morphine, with sedation,
respiratory depression and euphoria less intense than that of
morphine.
• nausea and vomiting are common with oral use, it is less likely
when administered via injection.
• Users of meperidine usually experience euphoria because the
medication triggers the brain's pleasure centers while it blocks
pain.
Side effects:
• The most frequent adverse reactions are:
lightheadedness, dizziness, sedation, nausea,
vomiting, and sweating.
• Less common side effects include: euphoria,
weakness, headache, tremor, severe convulsions,
transient hallucinations, disorientation, visual
disturbances, dry mouth, constipation,
palpitation, hypotension.
Is meperidine considered
addictive?
• Yes, meperidine is addictive. When the user
repeatedly uses it they build a tolerance to the
drug and this creates both a mental and physical
addiction.
Dependency
• meperidine can produce drug dependenc, giving it a
high abuse potential
• Signs of meperidine dependency:
- A strong desire or need to continue taking the
medicine.
-A need to increase the dose to maintain the effects of
the medicine.
- Withdrawal syndrome occurring after the medicine is
stopped.
withdrawal
• The length and severity of meperidine withdrawal is
directly related to how much and how often the drug
was used.
• "Cold turkey" withdrawal symptoms can occur four to
five hours after the last dose and usually lasts 7 to 10
days.
• meperidine withdrawal symptoms include but are not
limited to: severe anxiety, insomnia, profuse sweating,
muscle spasms, chills, shivering and tremors.
Analysis of meperidine:
1)Analysis of meperidine and normeperidine in
serum and urine by high-performance liquid
chromatography.
• A 1-ml sample aliquot is extracted into hexane, then backextracted into a small volume of dilute acid which is injected
onto a cyanopropyl analytical column. Absorbance of the
column effluent is monitored at 205 nm.
• Two internal standards are employed, diphenhydramine for
meperidine and nordiphenhydramine for normeperidine.
• Chromatography of the four compounds takes 4 min.
Analysis cont.
• 2) TLC identification and GLC determination of
meperidine and its metabolites in biological fluids.
• Meperidine, was extracted with ether from biological fluids at pH 10,
whereas meperidinic and normeperidinic acids and conjugated
metabolites remained in the aqueous phase.
• The residue, upon evaporation of the extract to dryness, was derivatized
with trifluoroacetic anhydride and gas chromatographed.
• Total (free and conjugated) meperidinic and normeperidinic acids in the
aqueous phase were converted and determined as meperidine and
normeperidine, respectively.
• A preliminary result of urinary disposition of meperidine and its
metabolites in the rat is presented. The identity of these metabolites was
confirmed with GLC-mass spectrometry.
Analysis cont.
3)Gas chromatographic analysis of meperidine and
normeperidine: determination in blood after a single
dose of meperidine.
• A method is described for the determination of meperidine and its
pharmacologically active metabolite, normeperidine, in blood, plasma,
and urine using gas chromatography with nitrogen-phosphorus
detection.
• Structural analogs of both meperidine and normeperidine were used as
internal standards.
• Unlike previously reported assays, this procedure was sensitive and
convenient enough for use in pharmacokinetic studies of both
meperidine and normeperidine following single doses of meperidine.
The assay was sensitive to 5 ng of meperidine/ml and 2.5 ng of
normeperidine/ml extracted from a 1-ml biological sample.