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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.