Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Codeine”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 1,243 records · Page 69Linked to original sources
PubMedDate not supplied

Central action of narcotic analgesics. I. Catalepsy and stereotypy in rats and narcotic analgesics.

The action of four analgesics, belonging to various pharmacological groups (morphine, codeine, fentanyl, pentazocine), was investigated in rats in tests for catalepsy and stereotypy, the tests depending on dopaminergic brain mechanisms. Interactions of the analgesics with a number of compounds known to affect dopaminergic brain functions in tests of catalepsy and stereotypy were also studied. In some experiments nalorphine, an antagonist of narcotic analgesics, was used. Morphine, codeine and fentanyl produced catalepsy, while pentazocine, at doses up to 60 microgram/kg, did not produce this effect. Reserpine, 2 mg/kg 3 hr before drugs, potentiated catalepsy produced by analgesics, while haloperidol, 0.2 mg/kg, 2 hr earlier, did not influence morphine and codeine catalepsy, but moderately potentiated fentanyl-induced catalepsy. alpha-methyl-p-tyrosine potentiated the cataleptogenic action of fentanyl and codeine, and also, less markedly, the action morphine. D-amphetamine (2.5-10 mg/kg) and apomorphine (5 mg/kg) moderately antagonized the catalepsy induced by analgesics, while atropine did not affect it. Nalorphine, 5 mg/kg, effectively abolished the catalepsy produced by narcotic analgesics, but did not affect that produced by neuroleptics. Morphine, codeine and fentanyl slightly inhibited apomorphine stereotypy, and evidently antagonized stereotypy produced by amphetamine. Pentazocine did not affect or slightly potentiated the both types of stereotypy. It is concluded that morphine, codeine and fentanyl, in contrast to pentazocine, inhibit behavioral activities depending on central dopaminergic functions in the rat. The mechanism of this action is most probably indirect, and seems to be related to the dopaminergic presynaptic functions.

Animals↗
PubMed1981

Relationships between immunogen structure and antisera specificity in the narcotic alkaloid series.

We report the production and comparative specificities of antisera raised to different immunogens containing codeine, morphine, and oxycodone. Antisera raised to bovine serum albumin (BSA) conjugates of codeine-6-hemisuccinate, ethylmorphine-6-hemisuccinate, or oxycodone-6-carboxymethyloxime had greatest recognition of structural changes around the piperidine ring nitrogen atom and th 14-position. N-carboxypropylnormorphine-BSA, N-carboxypropylnorcodeine-BSA, and norcodeine-BSA (directly coupled) conjugates elicited antisera that recognized structural changes at the 3- and 6-positions best, but also clearly discerned changes in the 14-substituent. Attachment of codeine to BSA via the 8-position gave a conjugate that elicited antisera with specificity characteristics similar to those of the antiserum to N-carboxypropylnorcodeine-BSA. Thus clear relationships existed between immunogen structure and antiserum specificity. The utility of these antisera was illustrated by the application of antiserum to codeine-6-hemisuccinate-BSA and solvent extraction to a study of codeine disposition in the dog. The specific antisera of N-carboxypropylnormorphine-BSA and to norcodeine-BSA were applied directly to an examination of the distribution of codeine and metabolically produced morphine in the milk and plasma of a nursing mother.

Adult↗
PubMed1985

Opiate-induced inhibition of the visceral distension reflex by peripheral and central mechanisms.

Distension of the proximal ileum by elevation of the intraluminal pressure, caused a transient, reflex fall in blood pressure of urethane-anaesthetised rats. The threshold intraluminal pressure required to evoke a reflex response was increased by codeine, but not by the quaternary opiate agonist N-methylmorphine. The magnitude of the reflex hypotension was decreased by codeine, morphine and N-methylmorphine. The quaternary opiate antagonist N-methylnalorphine reduced the effects of N-methylmorphine, but not those of codeine or morphine. Codeine-induced inhibition of reflex depressor responses was reduced by pretreatment with naloxone. Bilateral vagotomy caused a significant decrease in effects of codeine on the threshold, but not the magnitude, of reflex depressor responses. Furthermore N-methylnalorphine antagonised both codeine- and morphine-induced inhibition of depressor responses following transsection of the vagus nerves. Effects of opiates on the threshold for the reflex appear to be centrally mediated and to require an intact vagal innervation. The magnitude of depressor responses is largely independent of vagal innervation and may be influenced by opiates acting via peripheral mechanisms.

Anesthesia↗
PubMed1998

A specific immunoassay for the determination of morphine and its glucuronides in human blood.

The development of specific antisera for immunochemical determination of morphine, morphine-3-glucuronide and morphine-6-glucuronide is described. Morphine was N-demethylated to normorphine and N-alkylated to give N-aminopropyl-normorphine as hapten for antisera against morphine. As haptens for antisera against morphine-3-glucuronide and morphine-6-glucuronide, N-aminopropyl-nor-morphine was glucuronidated in position 3 or 6 respectively. Each of these three haptens were coupled to BSA employing the glutaraldehyde method to obtain three different immunogens. Immunisation of rabbits with these conjugates gave anti-morphine, anti-morphine-3-glucuronide and anti-morphine-6-glucuronide antisera, which were tested in a competitive, heterogeneous radioimmunoassay. Tracers for this radioimmunoassay procedure were synthesised by substitution of morphine and morphine-6-glucuronide in position 2 with 125I and indirect iodination of the morphine-3-glucuronide hapten according to the method of Bolton and Hunter. The resulting antisera show very specific reactions with morphine, morphine-3-glucuronide and morphine-6-glucuronide. Cross reactivities of each antiserum with structurally related opiates and opioides are very low. The cross reactivities of the anti-morphine antiserum against morphine-3-glucuronide, morphine-6-glucuronide, codeine, codeine-6-glucuronide or dihydrocodeine were less than 0.3%, the anti-morphine-3-glucuronide antiserum against morphine, morphine-6-glucuronide, codeine, codeine-6-glucuronide or dihydrocodeine less than 0.1% and the anti-morphine-6-glucuronide antiserum against morphine, morphine-3-glucuronide, codeine or dihydrocodeine less than 0.1%, against codeine-6-glucuronide less than 2.3%. The determination of morphine, morphine-3-glucuronide and morphine-6-glucuronide in blood samples (limit of detection= 3, 1, 0.5 ng/g) of nine cases of fatal heroin overdose with this radioimmunoassay method and the comparison with a GC/MS method is described.

Animals↗
PubMed2004

Combination tramadol plus acetaminophen for postsurgical pain.

BACKGROUND: This multicenter, randomized, double-blind, active- and placebo-controlled trial evaluated tramadol plus acetaminophen (APAP) for orthopedic (n = 153) and abdominal (n = 152) postsurgical pain. METHODS: Patients with moderate pain or greater were randomized to an initial two tablets of 37.5 mg tramadol plus 325 mg APAP (n = 98), codeine 30 mg plus APAP 300 mg (n = 109), or placebo (n = 98); thereafter, they received 1 to 2 tablets every 4 to 6 hours as needed for pain for 6 days. Outcome measures were pain relief and pain intensity, total pain relief, sum of pain intensity differences, and sum of pain relief and pain intensity differences during 4 hours and the daily averages. RESULTS: Tramadol plus APAP was superior to placebo for total pain relief, sum of pain intensity differences, and sum of pain relief and pain intensity differences (P < or =0.015); tramadol plus APAP and codeine plus APAP did not separate (P > or=0.281). For average daily pain relief, average daily pain intensity, and overall medication assessment, tramadol plus APAP was superior to placebo (P < or =0.038); codeine plus APAP did not separate from placebo (P > or =0.125). Discontinuation because of adverse events occurred in 8.2% of tramadol plus APAP, 10.1% of codeine plus APAP, and 3.0% of placebo patients. Except for constipation (4.1% tramadol plus APAP vs 10.1% codeine plus APAP) and vomiting (9.2% vs 14.7%, respectively), adverse events were similar for active treatments. CONCLUSIONS: Tramadol plus APAP (mean dose 4.4 tablets) was effective and well tolerated for postsurgical pain and showed better tolerability than did codeine plus APAP.

Acetaminophen↗
PubMed1999

Enhancement mu opioid antinociception by oral delta9-tetrahydrocannabinol: dose-response analysis and receptor identification.

The antinociceptive effects of various mu opioids given p.o. alone and in combination with Delta-9-tetrahydrocannabinol (Delta9-THC) were evaluated using the tail-flick test. Morphine preceded by Delta9-THC treatment (20 mg/kg) was significantly more potent than morphine alone, with an ED50 shift from 28.8 to 13.1 mg/kg. Codeine showed the greatest shift in ED50 value when administered after Delta9-THC (139.9 to 5.9 mg/kg). The dose-response curves for oxymorphone and hydromorphone were shifted 5- and 12.6-fold, respectively. Methadone was enhanced 4-fold, whereas its derivative, l-alpha-acetylmethadol, was enhanced 3-fold. The potency ratios after pretreatment with Delta9-THC for heroin and meperidine indicated significant enhancement (4.1 and 8.9, respectively). Pentazocine did not show a parallel shift in its dose-response curve with Delta9-THC. Naloxone administration (1 mg/kg s.c.) completely blocked the antinociceptive effects of morphine p.o. and codeine p.o. The Delta9-THC-induced enhancement of morphine and codeine was also significantly decreased by naloxone administration. Naltrindole (2 mg/kg s.c.) did not affect morphine or codeine antinociception but did block the enhancement of these two opioids by Delta9-THC. No effect was seen when nor-binaltorphimine was administered 2 mg/kg s.c. before morphine or codeine. Furthermore, the enhancements of morphine and codeine were not blocked by nor-binaltorphimine. We find that many mu opioids are enhanced by an inactive dose of Delta9-THC p.o. The exact nature of this enhancement is unknown. We show evidence of involvement of mu and possibly delta opioid receptors as a portion of this signaling pathway that leads to a decrease in pain perception.

Analgesics, Non-Narcotic↗
PubMed1992

Differential influence of N-dealkylation on the stimulus properties of some opioid agonists.

The capacity of several opioid agonists and their N-dealkylated derivatives (normetabolites) to substitute for the discriminative and reinforcing stimulus properties of codeine was evaluated in rhesus monkeys, and the affinity of these compounds in binding to mu receptors in rhesus monkey brain membranes was determined. Heroin (0.1 mg/kg), 6-acetylmorphine (0.1 mg/kg), methadone (0.6 mg/kg), 3-acetylmorphine (1 mg/kg), morphine (1 mg/kg) and codeine (1.8 mg/kg) substituted for the codeine cue, but the normetabolites of heroin, 6-acetylmorphine, morphine and codeine did not (up to 10 mg/kg). l-alpha-Acetylmethadol (3 mg/kg) and its mono (0.1 mg/kg) and double (0.6 mg/kg) N-dealkylated derivatives all substituted. In self administration, subjects responded for morphine (0.1 mg/kg/injection) and codeine (0.3 mg/kg/injection), but not for norcodeine (up to 1 mg/kg/injection) or normophine (up to 3 mg/kg/injection). l-alpha-Acetylmethadol (up to 0.3 mg/kg/injection) did not maintain responding, but its mono (0.1 mg/kg/injection) and double (0.1 mg/kg/injection) normetabolites did. In receptor binding, the normetabolites of morphine and 6-acetylmorphine were less potent than their parent agonists in displacing [3H]Tyr-D-Ala-Gly-(Me)Phe-Gly-ol, but the normetabolites of l-alpha-acetylmethadol had greater affinity than their parent. Codeine and norcodeine were inactive in binding. If l-alpha-acetylmethadol is converted only slowly to its active normetabolites, this may explain the lack of efficacy found with this compound in the self administration procedure.

Animals↗
PubMed1998

[Actions of drugs affecting the cough reflex].

BACKGROUND AND AIM: Authors evaluated the part of some receptor systems in the antitussive activity of drugs. METHOD: The cough was induced by mechanical stimulation of the airways. Unanesthetized cats were used in this study. RESULTS: They followed: 1. statistically highly significant decrease of cough parameters after administration the drugs influencing the different types of opiate receptors--tramadol, tilidine, pentazocine, codeine and butorphanol. Every of these drugs were administered in a dose 10 mg/kg b.w. intraperitoneally, 2. the antitussive activity of codeine was decreased by pretreatment with naloxone only in part, 3. selective antagonist 5-HT2 receptors ketanserine (1 mg/kg b.w.) decreased antitussive effect of codeine by 10% and effect of tramadol by 20%, 4. the ability of codeine to reduce the cough parameters was unchanged after pretreatment with haloperidol (0.1 mg/kg b.w.), 5. whereas the pretreatment with reserpine decreased the cough-suppressing effect of codeine, 6. the application of gabaergic agent gabalid leads to the highly significant decrease the cough parameters. Results of these experiments showed that gaba-ergic mechanism might be involved in the mechanism of action of narcotic antitussives agents, 7. we showed, that inhibition of glutaminergic synaptic transmissions afferent impulses from cough receptors with dextromethorphan leads to suppressing cough reflex in cats. CONCLUSIONS: Antitussive activity of agents is not only mediated by means of mí opiate receptors. The results suggest, that gabaergic, serotoninergic systems and activity of NMDA receptors play an important role in the mechanism of action of antitussive drugs. Decrease in levels of brain monoamines modifies the cough-depressant effect of codeine. (Fig. 7, Ref. 23.)

Animals↗
PubMedDate not supplied

Analgesic efficacy of meclofenamate sodium in episiotomy pain.

Meclofenamate sodium was compared, double-blind, with codeine and placebo for the treatment of acute episiotomy pain. One hundred sixty-eight women with moderate or severe episiotomy pain after normal delivery were assigned randomly to one of four treatment groups: one received meclofenamate sodium 200 mg at dose 1 and 100 mg at doses 2 and 3; one received meclofenamate sodium 100 mg at dose 1 and 50 mg at doses 2 and 3; one received codeine 60 mg at all three doses; and one received placebo at all three doses. Efficacy measurements were evaluated periodically for 6 hours after medication. After the first administration, both doses of meclofenamate sodium were significantly superior to placebo and to codeine from 2-6 hours in pain intensity difference and pain relief. For second and third doses, data were available for too few patients to allow valid analysis and interpretation. Adverse effects occurred in 4 patients in each meclofenamate sodium group, and in 8 in the codeine group and in 6 in the placebo group. The study indicates that single 100- and 200-mg doses of meclofenamate sodium are as safe as, and significantly more effective than, codeine 60 mg or placebo for episiotomy pain.

Adolescent↗
PubMed1995

Modulation of endogenous opiate production: effect of fasting.

The endogenous opiate alkaloid content in tissues from fed, 24 h and 48 h fasted rats was determined. Plasma morphine and codeine concentrations did not change in response to fasting. Morphine levels in the spleen increased 3-fold after 24 h of fasting and were lower than fed rats by 48 h of fasting; no change was detected in spleen codeine levels. Brain morphine levels were elevated 5-fold after 24 h of fasting and were two-fold higher than those of fed rats after 48 h of fasting. Brain codeine levels did not change with fasting. These results indicate that opiate alkaloids are endogenously produced in rodent tissues, particularly in the spleen, liver, and adrenals. The synthesis of morphine, in the spleen and brain, is maximally stimulated after 24 h of fasting, without alterations in tissue codeine synthesis. These suggest differential regulation of the endogenous synthetic pathways of morphine and codeine in response to the stress of fasting.

Adrenal Glands↗
PubMed1987

Synthesis and pharmacologic properties of 6-succinylcodeine.

In our search for a ligand to be used for affinity chromatography in the separation of putative, codeine-specific receptors, we have synthesized a pharmacologically active codeine derivative, 6-succinylcodeine (Ib). The structure of the compound has been confirmed. It is markedly less toxic than the parent compound, codeine (Ia), and has significantly weaker antitussive properties in the cat. On the other hand, its antinociceptive properties in the mouse and effects on guinea pig ileum are comparable to those of codeine. An interesting pharmacological property of Ib is its hypotensive effect in both cats and rhesus monkeys. The compound has been successfully coupled to an aminoalkyl agarose matrix. When coupled to the matrix, the drug loses its capacity to cause contraction of the guinea pig ileum but this property is restored upon alkaline hydrolysis of the coupled beads. Whether the diminished antitussive properties, as compared to the parent compound, or the loss of capacity to inhibit guinea pig ileum contractility when coupled to agarose would limit its usefulness for affinity chromatography of codeine-specific receptors is being investigated.

Analgesics↗
PubMed1998

Selective effects of somatostatin analogs on human drug-metabolizing enzymes.

Pharmacologic or surgical manipulation with growth hormone secretion or with the physiologic release of somatostatin and growth hormone-releasing hormone affects some rat liver enzymes, especially the sex-differentiated ones. We investigated the effects of two somatostatin analogs on several enzyme functions in six patients with carcinoid syndrome, using codeine as a probe drug. Codeine was given intravenously and its N- and O-demethylation, as well as 6-glucuronidation catalyzed by CYP3A, CYP2D6, and uridine diphosphate-glucuronosyltransferase, respectively, were studied before and during treatment with somatostatins. After 3 days of treatment with somatostatins the partial metabolic clearance of codeine by N-demethylation decreased by 21% to 64% in all patients (mean change, 44%; p < 0.05), and the clearance by O-demethylation was decreased by 20% to 69% in five of the patients (mean change in all patients, 35%; p < 0.05). In contrast, the partial clearance by 6-glucuronidation and the total systemic clearance of codeine were unchanged. Our results may be caused by the inhibition of growth hormone secretion induced by the somatostatins, inasmuch as direct metabolic interactions with these peptide drugs are improbable. The decline in CYP3A4 and CYP2D6 activity might have clinical implications when substrates of these enzymes with low therapeutic indices are combined with somatostatin analogs. Because the formation of morphine from codeine was altered, the analgesic effect of this drug may be reduced during concomitant treatment with somatostatins.

Adult↗
PubMed1998

Effects of moguisteine on the cough reflex induced by afferent electrical stimulation of the superior laryngeal nerve in guinea pigs.

The study aimed to further demonstrate the peripheral antitussive properties of moguisteine. Firstly, the antitussive effect of moguisteine on the cough reflex induced by inhalation of citric acid aerosol was evaluated in conscious guinea pigs. Secondly, the effects of both moguisteine and codeine on the centrally mediated cough reflex induced by afferent electrical stimulation of the superior laryngeal nerve were investigated in anesthetized guinea pigs. Moguisteine (2.5-10 mg/kg, intravenously, i.v.) reduced the cough reflex induced by 7.5% citric acid aerosol in a dose-dependent manner, with an ED50 value of 0.55 mg/kg. Both i.v. (0.5-4 mg/kg) and intracerebroventricular (i.c.v., 5-20 microg) injection of codeine dose dependently inhibited the cough reflex induced by afferent electrical stimulation of the superior laryngeal nerve; the ED50 values were 0.91 mg/kg and 7.90 microg, respectively. The inhibitory effect of codeine (4 mg/kg i.v.) was abolished by pretreatment with naloxone (2 mg/kg intraperitoneally). In contrast to codeine, neither i.v. (4 and 20 mg/kg) nor i.c.v. (20 microg) injection of moguisteine affected the cough reflex. These results suggest that the antitussive effect of codeine is mediated by central opioid mechanisms, whereas the antitussive effect of moguisteine is mediated by peripheral mechanisms.

Aerosols↗
PubMed1976

Determination of nanogram amounts of aromatic compounds by spectrophotometry on thin-layer chromatograms.

A highly sensitive method is described for the simultaneous determination of codeine and chlorpheniramine in plasma. Thin-layer chromatography is used for the separation of the drugs. The spots are then rendered visible by nitration of the substances on the thin-layer plate. Codeine can be quantified by direct measurement of the resulting fluorescence. After reduction, the aromatic amines are diazotized and coupled with N-(1-naphthyl)ethylenediamine on the thin-layer plate. For codeine the fluorimetric measurement is more reliable than the colorimetric determination. The sensitivity limits are 8 ng/ml of plasma for codeine phosphate and 1-2 ng/ml of plasma for chlorpheniramine maleate. This procedure is also applicable to other aromatic compounds which can be nitrated by the described method. The method has been applied to compare a determination of the plasma levels of codeine and chlorpheniramine after administration in normal capsules and retard tablets.

Administration, Oral↗
PubMed1993

Efficacy of cough suppressants in children.

To test the hypothesis that codeine and dextromethorphan are effective in alleviating the symptoms of acute cough, we conducted a randomized, controlled trial. Eligible patients were children 18 months to 12 years of age, seen in private pediatric practices, with significant night cough of less than 14 days' duration. Study patients were randomly selected to receive codeine, dextromethorphan, or placebo at bedtime for 3 consecutive nights. Outcomes were assessed by the use of a parent questionnaire rating the severity of symptoms at the initiation of therapy, and after each night of the study. Every patient had a cough score (range 0 to 4) and composite symptom score (range 0 to 9) computed for each day of the study. One hundred forty-one doses of study medication were evaluated in 49 patients, including 13 children receiving placebo, 19 dextromethorphan, and 17 codeine. Mean cough and composite symptom scores decreased in each of the three treatment groups on each day of the study; there were no significant differences. Regression analysis, with reduction in cough score as the outcome of interest, showed that neither dextromethorphan nor codeine was significantly more effective than placebo (p = 0.41 and 0.70, respectively). Reduction in cough score was positively correlated with the severity of cough at the start of treatment (p = 0.007). Our data suggest that, in the doses used, neither codeine nor dextromethorphan is superior to placebo in treating night cough in children.

Child↗
PubMed1997

A comparison of patient-controlled and fixed schedule analgesia after orthognathic surgery.

PURPOSE: The purpose of this prospective study was to compare the effectiveness of patient-controlled intravenous (i.v.) opioid analgesic administration (PCA) with fixed schedule and dosage oral/rectal administration of naproxen, and opioid analgesics intramuscularly/orally as needed (i.m./p.o. prn) for postoperative analgesia over a period of 48 to 56 hours after surgery. PATIENTS AND METHODS: There were 75 orthognathic patients aged 25.73 +/- 8.01 years, subdivided into three study groups of 25: codeine group (8 males, 17 females); naproxen group (5 males, 20 females) and PCA group (8 male, 17 females). The degree of analgesia was assessed every 4 hours from 8:00 AM to 8:00 PM hours on days 1 and 2 postsurgery using a visual analog scale (VAS). Mean daily and mean overall VAS scores were treated as parametric data and were analyzed accordingly. Mean daily VAS scores also were categorized as comfort days when mean scores were less than 3.0 cm, and as discomfort days when mean scores were equal to or greater than 3.0 cm. ANOVA were used to analyze patient demographics, pain scores, surgical time, fentanyl used during general anaesthesia, analgesic morphine equivalents, and vital signs. Chi-square tests were used to analyze sex, comfort (discomfort) days, and nausea and vomiting. Mean VAS ratings were analyzed using independent t-tests. RESULTS: The three groups were matched in demographics, surgical time, fentanyl used, and sex. The PCA group used less than half the amount of morphine equivalent as the codeine group (P = .0001). Both the naproxen and the PCA groups were significantly more comfortable than the codeine group during day 1 and day 2 postsurgery. The codeine group had significantly more episodes of nausea than either the naproxen or the PCA groups. CONCLUSION: In patients undergoing orthognathic surgery, the naproxen and PCA regimens provided better analgesia than the codeine regimen.

Adolescent↗
PubMed2005

Dextromethorphan differentially affects opioid antinociception in rats.

Opioid drugs such as morphine and meperidine are widely used in clinical pain management, although they can cause some adverse effects. A number of studies indicate that N-methyl-D-aspartate (NMDA) receptors may play a role in the mechanism of morphine analgesia, tolerance and dependence. Being an antitussive with NMDA antagonist properties, dextromethorphan (DM) may have some therapeutic benefits when coadministered with morphine. In the present study, we investigated the effects of DM on the antinociceptive effects of different opioids. We also investigated the possible pharmacokinetic mechanisms involved. The antinociceptive effects of the mu-opioid receptor agonists morphine (5 mg kg(-1), s.c.), meperidine (25 mg kg(-1), s.c.) and codeine (25 mg kg(-1), s.c.), and the kappa-opioid agonists nalbuphine (8 mg kg(-1), s.c.) and U-50,488H (20 mg kg(-1), s.c.) were studied using the tail-flick test in male Sprague-Dawley rats. Coadministration of DM (20 mg kg(-1), i.p.) with these opioids was also performed and investigated. The pharmacokinetic effects of DM on morphine and codeine were examined, and the free concentration of morphine or codeine in serum was determined by HPLC.It was found that DM potentiated the antinociceptive effects of some mu-opioid agonists but not codeine or kappa-opioid agonists in rats. DM potentiated morphine's antinociceptive effect, and acutely increased the serum concentration of morphine. In contrast, DM attenuated the antinociceptive effect of codeine and decreased the serum concentration of its active metabolite (morphine). The pharmacokinetic interactions between DM and opioids may partially explain the differential effects of DM on the antinociception caused by opioids.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMedDate not supplied

Sticky business: patterns of procurement and misuse of prescription cough syrup in Houston.

Reports of recreational codeine cough syrup use have increased in Houston and in the state of Texas. Occasional and polydrug users increasingly have consumed codeine cough syrup (with or without alcohol or other drugs) over the past three years, accounting for a $40 increase in the price of an eight-ounce bottle on the underground economy. News stories regarding syrup abuse and reports of deaths by codeine overdoses suggested the need to explore this emerging drug trend. The investigator conducted a literature search of scientific journals and news media, interviews with community authorities, and guided interviews with 25 adults who reported using codeine cough syrup in the 30 days preceding their interviews. Participants were recruited through snowball sampling; interview transcripts were coded and content analyzed. Polydrug users reported a penchant for codeine syrup because it carries fewer legal consequences, is perceived as "safer" than illegal drugs, and is either free or inexpensive for users with Medicaid or private insurance. Participants reported methods for procuring syrup from physicians and hospital emergency rooms which they consumed or traded for money, goods, or services. Consumption patterns for chronic and occasional users are described. Reported side effects include a drowsy relaxed high, fatigue, loss of coordination, constipation, and urinary retention.

Antitussive Agents↗