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Product: Subutex 28x 8 mg
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Active substance: Buprenorphine
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Buprenorphine (Subutex®, Buprenorphine mepha®)
Buprenorphine (Subutex®, buprenorphine mepha®) may provide advantages over methadone in certain situations for pharmacological reasons. In principle, the procedures for clarification / status and approval are the same as for methadone, see “SBG: Start in 1 Consultation” (best practice, suitable for experienced physicians) or “SGB Start in 2 Consultations”. Here you can find an aid for the differentiated indication for buprenorphine. Buprenorphine is much more expensive than methadone, but is also a compulsory health insurance.
Sublingual administration with rapid absorption (pronounced first-pass effect, therefore hardly bioavailable after ingestion and low risk of poisoning). After 3-5 minutes, the tablets dissolve under the tongue (to fully allow the effect of the tablets, do not swallow for 5 minutes).
sublingual bioavailability = 31-52%
Time to reach a clinical effect approximately 30 (-60) minutes
Time to reach maximum plasma levels approximately 90-150 minutes
Time to achieve maximum clinical effect approximately 1-4 hours
Rapid absorption from plasma and redistribution in different tissues (eg adipose tissue). Of the various tissues, there is a time-delayed, slow redistribution, which ensures constant plasma concentrations of buprenorphine (“depot effect”). Effective plasma levels: between 0.7 and 12 ng / ml; dose-dependent duration of action Permanent condition: approximately after 5-8 days; no significant daily fluctuations with regular intake. Most of the metabolism takes place via cytochrome P450 3A4. Because other enzymes are involved in the degradation of buprenorphine (CYP 2C8), the degradation metabolism of buprenorphine and its metabolites is relatively insensitive to interactions. Elimination half-life: 20-25 / 37hours. The elimination is mainly liver function through glucuronidation and N-dealkylation. The excretion is about 70-80% of the stool, the rest 20-30%, the kidneys.
Mechanism of action
Buprenorphine is a partial agonist of the mu opioid receptor (mediating effects such as euphoria, analgesia, respiratory depression and addiction) and an antagonist of the kappa receptor (mediating effects such as dysphoria and sedative treatment). Compared to methadone and heroin, buprenorphine shows important differences due to its special properties at the opioid receptors: Buprenorphine has a higher receptor affinity (heroin and methadone move) and a moderate inherent agonist activity with only partial stimulation of mu opioid receptors (high doses of a buprenorphine result in lighter, less euphoric and less sedative central nervous effect than high doses of other opioids such as heroin, methadone). Take effect: There is no linear dose-response relationship. With increasing doses, it will reach a Wirkplateaus. Buprenorphine, in combination with other central depressants, may contribute to a limited respiratory depressant effect. Buprenorphine shows a long receptor half-life with slow receptor dissociation and less receptor-down regulation.