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PubMed2026

"It was good because they have a relationship with us": A qualitative study on low-threshold buprenorphine treatment at syringe services programs.

INTRODUCTION: Syringe service programs (SSPs) reach people who inject drugs with opioid use disorder (OUD) and are novel "low-threshold" venues to initiate buprenorphine treatment. The study investigated patients' experiences with SSP-initiated buprenorphine treatment, which could aid in improving buprenorphine treatment delivery at SSPs. METHODS: The study included 12 participants who completed qualitative exit interviews after a randomized controlled trial of buprenorphine treatment at SSPs. In the parent study, participants received buprenorphine treatment through an onsite model at an SSP or enhanced referral to a community health center based on the randomization sequence. Most participants started taking buprenorphine at home. Exit interviews included participants from both study arms, and the semi-structured interview guide focused on their experiences with clinicians, experiences initiating buprenorphine, prior experiences with OUD treatment, and perceptions about continuing buprenorphine treatment. Four researchers iteratively read, coded, and discussed each transcript, then they derived recurring themes using thematic analysis. RESULTS: Participants were mostly male, middle-aged, and 50% identified as Latino. Four main themes related to buprenorphine treatment initiation: 1) Onsite treatment facilitated buprenorphine prescription, but some participants also expressed a need for additional support; 2) Precipitated withdrawal complicated participants' buprenorphine initiation in both arms; 3) Participants largely experienced the SSPs as affirming and welcoming; and 4) Developing strong relationships with healthcare providers was critical to successful buprenorphine treatment initiation. CONCLUSIONS: The SSP-based model provided rapid access to buprenorphine prescriptions, but precipitated withdrawal was a common complication. Some participants desired additional support and guidance when they started taking buprenorphine at home. The findings point to a "low-threshold, high-touch" approach where participants receive expedited access to buprenorphine providers at SSPs but also additional support throughout the initiation process to avoid and/or manage precipitated withdrawal. Despite some challenges, SSP-based buprenorphine treatment was highly valued by study participants.

Humans↗

PubMed1977

Agonist and antagonist properties of buprenorphine, a new antinociceptive agent.

1. Buprenorphine is a highly lipophilic derivative of oripavine. In rodent antinociceptive assays (writhing, tail pressure), buprenorphine had an action which was rapid in onset and of long duration; it was 25-40 times more potent than morphine after parenteral injection and 7-10 times more potent after oral administration. 2. The log dose-response relationship for buprenorphine was curvilinear in mouse and rat tail flick tests with the antinociceptive effect decreasing at higher, non-toxic doses. 3. Tolerance developed to the antinociceptive activity of buprenorphine in mice. 4. No signs of abstinence were observed on naloxone challenge or after abrupt withdrawal in monkeys receiving buprenorphine chronically for one month. 5. Buprenorphine antagonized the antinociceptive actions of morphine in mouse and rat tail flick tests but was an ineffective antagonist in the rat tail pressure test. 6. Buprenorphine precipitated signs of abstinence in morphine-dependent mice and monkeys but not in morphine-dependent rats. 7. Buprenorphine produced Straub tails in mice. This effect was not antagonized when the animals were pretreated with naloxone. However, in the rat tail pressure test high doses of diprenorphine antagonized established antinociceptive effects of buprenorphine. 8. It is concluded that buprenorphine represents a definite advance in the search for a narcotic antagonist analgesic of low physical dependence potential.

Analgesics↗

PubMed2026

Differential impacts of exon 1-associated and exon 11-associated variants of the rat mu opioid receptor gene, Oprm1, on buprenorphine- and morphine-induced analgesia and respiratory depression in male rats.

Buprenorphine has long been recognized as a mu opioid agonist with a distinctive and intricate pharmacological profile. It is a partial agonist at the mu opioid receptor, an antagonist at the kappa and delta opioid receptors, and an agonist at the nociception opioid receptor. Similar to other mu agonists such as morphine and fentanyl, buprenorphine can produce side effects, including tolerance, physical dependence, respiratory depression, and addiction. The mu opioid receptor gene, OPRM1, undergoes extensive alternative splicing, generating an array of splice variants or isoforms, which are conserved from rodents to humans. These splice variants can be categorized into 2 main types, exon 1 (E1)-associated variants and exon 11 (E11)-associated variants. E1-associated variants primarily consist of full-length, 7-transmembrane C-terminal variants, whereas E11-associated variants are typically truncated 6-transmembrane variants. Previous studies established that buprenorphine analgesia in mice is dependent on both E1- and E11-associated variants. However, the role of these variants in buprenorphine analgesia and respiratory depression in rats remains unclear. In this study, we used CRISPR/Cas9 technology to develop 2 rat Oprm1 gene-targeting models in which E1- and E11-associated variants were selectively disrupted, aiming to investigate their roles in buprenorphine and morphine's actions. The results showed that both E1- and E11-associated variants are essential for buprenorphine's analgesic and respiratory depressional effects in rats, whereas morphine's effects are solely attributed to the E1-associated variants. These findings provide new and important insights into the distinct contributions of the E1- and E11-associated variants to the pharmacological actions of buprenorphine and morphine. SIGNIFICANCE STATEMENT: Differential dependences of buprenorphine and morphine analgesia and respiratory depression on Oprm1 exon 1- and exon 11-associated variants revealed in rat gene-targeting models provide new and important insights into unique contributions of these variants to buprenorphine and morphine actions.

Animals↗

PubMed1977

The animal pharmacology of buprenorphine, an oripavine analgesic agent.

1. The general pharmacology of buprenorphine, a potent analgesic agent derived from oripavine, is described. 2. After cute administration of buprenorphine, the spontaneous locomotor activity of mice was increased; rats displayed stereotyped licking and biting movements; behavioural depression was marked in guinea-pigs but mild in rhesus monkeys. The behaviour of cats was unchanged. 3. In general, buprenorphine reduced heart rate but had no significant effect on arterial blood pressure in conscious rats and dogs. 4. In anaesthetized, open-chest cats buprenorphine (0.10 and 1.0 mg/kg, i.v.) caused no major haemodynamic changes. 5. Buprenorphine (0.01-10 mg/kg i.a.) and morphine (0.30-30 mg/kg, i.a.) increased arterial PCO2 values and reduced PO2 values in conscious rats. With doses of buprenorphine greater than 0.10 mg/kg (a) the duration of respiratory depression became less, (b) ceiling effects occurred such that the maximum effects produced were less than those obtained with morphine. 6. Buprenorphine was a potent and long-lasting antagonist of citric acid-induced coughing in guinea-pigs. 7. At a dose level 20 times greater than the ED50 for antinociception (tail pressure), morphine suppressed urine output to a greater extent than the corresponding dose of buprenorphine in rats. 8. Over the range 0.01-1.0 mg/kg (s.c.), buprenorphine slowed the passage of a charcoal meal along the gastrointestinal tract in rats. After doses in excess of 1 mg/kg, the meal travelled increasingly further such that the distances measured at 10 and 30 mg/kg did not differ significantly from control values. In contrast, the morphine dose-response relationship was linear.

Analgesics↗

PubMed1979

Randomised trial comparing buprenorphine and diamorphine for chest pain in suspected myocardial infarction.

Buprenorphine, a new powerful analgesic agent, was used to treat chest pain in patients with suspected myocardial infarction. Initial studies showed no significant changes in systemic or pulmonary artery blood pressure or in heart rate after intravenous buprenorphine. Sublingual buprenorphine also appeared effective in relieving pain, but its onset of action was considerably delayed compared with the intravenous route. A randomised double-blind controlled trial of equivalent doses of buprenorphine and diamorphine showed no significant difference between the drugs in terms of pain relief and duration of action. The occurrence of nausea, vomiting, and other side effects was similar in the two groups. The onset of action of buprenorphine was slightly but significantly slower than that of diamorphine. Since buprenorphine seems to be comparable with diamorphine in action and is not a controlled drug, it may prove useful in both general and hospital practice.

Buprenorphine↗

PubMed1979

Buprenorphine: a review of its pharmacological properties and therapeutic efficacy.

Buprenorphine, a derivative of the morphine alkaloid thebaine, is a strong analgesic with marked narcotic antagonist activity. In studies in relatively small groups of postoperative patients with moderate to severe pain, one or a few doses of buprenorphine parenterally (by intramuscular or slow intravenous injection) or sublingually were at least as effective as standard doses of other strong analgesics such as morphine, pethidine or pentazocine, and buprenorphine was longer acting than these agents. Only a small number of patients with chronic pain have received repeated doses, but in such patients there was no need for increased doses during several weeks to months of treatment. Buprenorphine appears to produce side effects which are similar to those seen with other morphine-like compounds, including respiratory depression. There is apparently no completely reliable specific antagonist for buprenorphine's respiratory depressant effect, since even very high doses of the antagonist drug naloxone may produce only a partial reversal. The respiratory stimulant drug doxapram has overcome respiratory depression in volunteers and in a few patients in a clinical setting, but such studies have not been done in an overdose situation. Animal studies and a direct addiction study in a few volunteers suggest that the dependence liability of buprenorphine may be lower than that of other older morphine-like drugs. However, a slowly emerging abstinence syndrome did occur on withdrawal after very high doses administered for 1 to 2 months. A definitive statement on the drug's dependence liability and abuse potential cannot be made until it has had much wider use for a longer period of time.

Animals↗

PubMed1979

The respiratory depressive effects of intravenous buprenorphine in patients in an intensive care unit.

Buprenorphine hydrochloride, a new, potent, long-acting synthetic opiate analgesic, with partial agonist-antagonist activity, was administered intravenously to two groups of patients in an intensive care unit. Arterial blood was drawn for blood gas analysis before (control) and at regular intervals after drug administration, to determine the effects of intravenous buprenorphine on respiration in critically ill patients, each acting as his or her own control. Intravenous buprenorphine 0,4 mg (group I -- 10 patients) caused a significant reduction in mean respiration rate and an increase in mean PaCO2, but did not alter heart rate, PaO2 or base excess values. Intravenous buprenorphine 0,2 mg (group II -- 10 patients) was associated with a less significant reduction in the rate of breathing and elevation of PaCO2. Both 0,4 mg and 0,2 mg buprenorphine produced effective relief of pain, sedation, and reduction in restlessness, and allayed anxiety. Our results suggest that intravenous buprenorphine 0,2 mg can be safely recommended for the prolonged relief of postoperative pain in adults.

Acid-Base Equilibrium↗

PubMed1978

Human pharmacology and abuse potential of the analgesic buprenorphine: a potential agent for treating narcotic addiction.

Buprenorphine was evaluated for its abuse potential and utility in treating narcotic addiction. The drug was morphine-like but was 25 to 50 times more potent than morphine and was longer-acting. Little if any physical dependence of clinical significance was produced by buprenorphine. The effects of morphine to 120-mg doses were blocked by buprenorphine, a blockade that persisted for 29 1/2 hours. In man, buprenorphine has less intrinsic activity than morphine, and as such, as a low abuse potential. Moreover, the drug has potential for treating narcotic addiction since it is acceptable to addicts, is long-acting, produces a low level of physical dependence such that patients may be easily detoxified, is less toxic than drugs used for maintenance therapy, and blocks the effects of narcotics.

Adult↗

PubMed1977

Buprenorphine hydrochloride: determination of analgesic potency.

An open evaluation of relief from severe pain following major abdominal operations was carried out on at least ten patients, who had given written consent, with 0.1 to 0.4 mg doses of buprenorphine hydrochloride administered intramuscularly. Statistical analysis of the data showed that 0.3 mg of this compound provided quite satisfactory relief from pain for up to six hours. Seven more consenting patients were given buprenorphine hydrochloride 0.5 to 0.6 mg, but they did not receive much greater or longer pain relief than those receiving 0.3 to 0.4 mg. However, the latter patients were younger and heavier. It was concluded that buprenorphine hydrochloride 0.2 to 0.4 mg provided relief of severe pain probably as well as is observed with morphine 10 mg for the average-size patient, but the duration of pain relief with the new compound is substantially longer than with other strong analgesics previously tested. The only common side effect noted was drowsiness, which was observed during the analgesic action of the compound. No appreciable alterations were seen in the respiration, pulse rate and blood pressure. On the basis of these tests, buprenorphine hydrochloride appears to be a satisfactory analgesic for severe postoperative pain, and it deserves extensive study.

Adult↗

PubMed1979

[Comparative study about the analgesic effect of buprenorphine (author's transl)].

In that study we compared the analgesic effects of equianalgesic doses of buprenorphine and morphine taken as the narcotic of reference. The experiment has been undertaken in ten adults having severe cancer pain. The results have been analysed by statistical non parametric tests. We found that buprenorphine and morphine have the same pattern of action despite the fact that intramuscular buprenorphine has a clinical duration of approximately 9 hours.

Adolescent↗

PubMed1977

Buprenorphine: a new potent long-acting synthetic analgesic. Comparison with morphine.

A new thebaine derivative, buprenorphine, 0.6 mg, was compared with morphine 15 mg in a double-blind trial, in patients recovering from elective Caesarean section. Within 1 h of administration analgesia was obtained with both drugs and was sustained for 7-8 h with buprenorphine, and 3-4 h with morphine. Buprenorphine caused a greater decrease in diastolic arterial pressure than did morphine, but arterial systolic pressure and heart rate were not influenced by either drug. No serious side-effects were encountered in this study.

Cesarean Section↗

PubMed1978

A double-blind comparison of morphine and buprenorphine in the prevention of pain after operation.

A double-blind, between-patient comparison has been made of the effects of morphine 10 mg i.v. and buprenorphine 0.3 mg i.v. on the prevention of pain after operation. The drugs were given by the anaesthetist at the end of the operation, and the onset and severity of pain were assessed by a trained nurse. Both drugs caused a significant delay in the appearance of severe pain when compared with the control group, but with buprenorphine the mean delay of 10.5 h was more than twice that of morphine. The only side-effect to occur more frequently after administration of the analgesics was drowsiness, the incidence being greater after buprenorphine than after morphine.

Adult↗

PubMed2026

Relationships between cannabis and cocaine use in a randomized trial of combined buprenorphine and naltrexone for DSM-IV cocaine dependence.

BACKGROUND: Cannabis is the most commonly used drug in the United States, and among people who use cannabis, polysubstance use is common and understudied. We aimed to examine the association of tetrahydrocannabinol (THC) positive urine drug screen (+UDS) with the odds of submitting a cocaine + UDS during cocaine use disorder treatment. METHODS: We conducted a secondary data analysis of a previously reported double-blind, placebo-controlled clinical trial, CTN0048. Participants meeting criteria for opioid abuse/dependence were assigned to receive extended-release naltrexone and one of three conditions of buprenorphine (placebo, 4 mg/day, 16 mg/day) for 8 weeks. Generalized estimating equations (GEE) were used to analyze urine samples (Liu et al., 2018) collected over time, examining the association between THC + UDS and cocaine + UDS during treatment. RESULTS: Participants (n = 301) averaged 46 (SD = 8.64) years of age, were majority male (78.41 %), non-Hispanic (89.70 %), and African American (66.45 %). GEE results indicated that patients who submitted THC + UDS had significantly higher odds of submitting cocaine + UDS compared to participants who submitted THC-negative UDS across the 25 time points examined (OR = 1.47, 95 % CI = 1.21-1.79, p = 0.00). Time (OR = 0.9998, 95 % CI: 0.9997, 0.9999, p = 0.018) and the covariate of sex assigned at birth (OR = 1.77, 95 % CI = 1.13-2.77, p = 0.013) were also significant in the model, indicating very small decreases in the odds of submitting a cocaine + UDS over time for all patients and 77 % higher odds of submitting cocaine + UDS for females. CONCLUSION: THC + UDS was associated with increased odds of submitting a cocaine + UDS during treatment. Further investigation is needed to discern whether decreasing THC use will result in reduced cocaine use; however, these results suggest that it may be beneficial to counsel patients on cannabis use cessation both before and during treatment for cocaine use, as it is related to cocaine use treatment outcomes. TRIAL REGISTRATION: Secondary data analysis of ClinicalTrials.gov, TRN: NCT01402492 ("A randomized study to test the safety and effectiveness of buprenorphine in the presence of naltrexone for the treatment of cocaine dependence"; National Drug Abuse Treatment Clinical Trials Network (CTN) clinical trial: CTN0048), Registration date: 27 July 2011.

Humans↗

PubMed1979

Analgesic effects of sublingual buprenorphine.

The analgesic effects of sublingually administered buprenorphine 0.4 mg have been compared with morphine 10 mg given intramuscularly in patients following operation. The results indicate a slower onset of action for buprenorphine but of much longer duration than morphine. There were no serious side effects or difference in their incidence between the two drugs.

Administration, Oral↗

PubMed1979

Comparison of buprenorphine and pethidine given intravenously on demand to relieve postoperative pain.

In a double-blind study of on-demand intravenous analgesia buprenorphine was found to be about 600 times as potent as pethidine. The incidence of side effects was similar with both drugs. The quality of analgesia, subjectively assessed, was good with both drugs using this method of administration. Provided that its low potential for abuse is substantiated, buprenorphine appears to be a powerful analgesic that may successfully be given intravenously on demand.

Adolescent↗

PubMed1979

Electroencephalographic study of pentazocine and buprenorphine.

Both pentazocine and buprenorphine are hypnoanalgetics of the agonistic-antagonist group. They suppress the inhibitory effect of fentanyl upon the central nervous system. They show also secondary their own inhibitory properties (fig. 8). The agonistic-antagonists can be further divided in excitants (like pentazocine) and non-excitants (buprenorphine).

Animals↗

PubMed1977

Double-blind evaluation of buprenorphine hydrochloride for post-operative pain.

In a double-blind, random assignment study of four groups of 40 patients, relief of severe pain with buprenorphine hydrochloride 0.2 mg or 0.4 mg was evaluated and compared with morphine sulphate 5 or 10 mg. Evaluations included pain intensity, pain relief, sedation and other effects for up to 12 hours after drug administration, following recovery of wakefulness from anaesthesia for major abdominal surgery. Analyses of five parameters showed that the four groups were statistically comparable and that buprenorphine hydrochloride is at least 50 times more potent than morphine sulphate and has a substantially longer duration of analgesic action. Further clinical evaluation is, therefore, recommended.

Adolescent↗

PubMed1977

Comparison of buprenorphine, pethidine and pentazocine for the relief of pain after operation.

The analgesic effects of buprenorphine 2 microgram/kg--1 and 8 microgram. kg--1 were compared with those of pethidine 1 mg. kg--1 and pentazocine 0.6 mg.kg--1 in 172 patients recovering from surgery. The drugs were given by i.m. injection in the period immediately after operation and the quality of pain relief was assessed at intervals for at least 4h. Buprenorphine 4-8 microgram-kg-1 was shown to be an effective analgesic, superior in some cases to the other drugs in the doses employed in the study.

Adult↗