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John Bear Premier Opioid Research μor
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Mental force the bridge between conscious effort observed by neuronal metabolic changes Opioid Researcher You have to know were you been to get to were your going! ~ Jesus is God in the flesh! OPIOID ACTIVITY Mu Kappa Delta receptors NMDAR CBD BZD Channels Toxicology #P450 #OPRM1 #ABCB1 #Cytochrome #GABA Pathways
Mental force the bridge between conscious effort observed by neuronal metabolic changes Opioid Researcher You have to know were you been to get to were your going! ~ Jesus is God in the flesh! OPIOID ACTIVITY Mu Kappa Delta receptors NMDAR CBD BZD Channels Toxicology #P450 #OPRM1 #ABCB1 #Cytochrome #GABA Pathways

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Belbuca 150 mcg film BELBUCA 150 MCG FILM
Belbuca 75 mcg film BELBUCA 75 MCG FILM
Belbuca 900 mcg film BELBUCA 900 MCG FILM
Buprenex 0.3 mg/mL solution BUPRENEX 0.3 MG/ML AMPUL
buprenorphine HCl 2 mg tablet, sublingual BUPRENORPHINE 2 MG TABLET SL🐼uprenorphine HCl 8 mg tablet, sublingual BUPRENORPHINE 8 MG TABLET SL
buprenorphine HCl 2 mg tablet, sublingual BUPRENORPHINE 2 MG TABLET SL

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🐼Pharmacology
Mechanism of Action
Morphine is a pure opioid agonist, relatively selective for the mu-opioid receptor; inhibits ascending pain pathways, which causes alteration in response to pain; produces analgesia, respiratory depression, and sedation

Naltrexone is a centrally acting mu-opioid antagonist; only becomes active and antagonizes opioid agonsists when the tablet is either chewed, crushed, or dissolved

Pharmacokinetics
Pharmacokinetic parameters are for morphine unless otherwise stated

Bioavailability: 20-40%

Peak Plasma Time: 7.5 hr

Protein Binding: 30-35%

Half-Life: 29 hr

Volume of distribution: 3-4 L/kg

Metabolism: Glucuronidation and sulfation in the liver to produce including morphine-3-glucuronide, M3G (about 50%) and morphine-6-glucuronide, M6G (about 5 to 15%) or morphine-3-etheral sulfate; naltrexone extensively metabolized to 6-beta-naltrexol

Clearance: 20-30 mL/min/kg

Excretion: Morphine: 10% excreted unchanged in urine, 55-65 metabolites excreted in urine

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🐼 #OPIOIDAnalgesic #CYP3A4, #Hydromorphone #CIIPharmacology
Mechanism of Action
Mu opioid receptor agonist; interacts with other opioid receptors at higher doses; activates opioid receptors at sites in the peri-aquaductal and peri-ventricular gray matter, the ventro-medial medulla and the spinal cord to produce analgesia

Also elicits euphoric, respiratory depressant, and physiologic dependence properties of mu receptors within the CNS

Absorption
Zohydro ER

Extended-release provided by spheroidal oral drug absorption system (SODAS) technology (ie, multi-particulate formulation of coated carrier beads in hard gelatin capsules); contains rate-controlling polymers and drug release by diffusion
Peak plasma time: 5 hr
Peak plasma concentration increased by 27% when administered with a high fat meal
Hysingla ER

Peak plasma time (mean): 14-16 hr (range 6-30 hr)
AUC and peak plasma concentration increase linearly with doses
Peak plasma concentration (median): 14.6-110 ng/mL
AUC (median): 284-1787 ng•hr/mL
Peak plasma concentration increased by 20% when administered with a high fat meal
Vantrela ER

Peak plasma time: 8 hr (single dose); 5 hr (steady-state)
Peak plasma concentration (single doses): 12.6-62.5 ng/mL
AUC (single doses): 199-1189 ng•hr/mL
Distribution
Protein bound: ~19% (Zohydro ER); 36% (Hysingla ER); 19-45% (Vantrela ER)

Vd: 402 L (Hysingla ER); 1300-1400 L (Vantrela ER)

Metabolism
Metabolized in liver by CYP2D6 (minor) via O-demethylation, CYP3A4 (major) via N-demethylation, and 6-keto reduction

Metabolites: CYP3A4 mediated N-demethylation to norhydrocodone is the primary metabolic pathway; CYP2D6 to hydromorphone (active metabolite with higher binding capacity to mu opioid receptor)

Elimination
Half-life: 8 hr (Zohydro ER); 7-9 hr (Hysingla ER); 11-12 hr (Vantrela ER)

Excretion: Primarily by kidneys

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🐼Pharmacology
Mechanism of Action
Mu opioid receptor agonist; interacts with other opioid receptors at higher doses; activates opioid receptors at sites in the peri-aquaductal and peri-ventricular gray matter, the ventro-medial medulla and the spinal cord to produce analgesia

Also elicits euphoric, respiratory depressant, and physiologic dependence properties of mu receptors within the CNS

Absorption
Zohydro ER

Extended-release provided by spheroidal oral drug absorption system (SODAS) technology (ie, multi-particulate formulation of coated carrier beads in hard gelatin capsules); contains rate-controlling polymers and drug release by diffusion
Peak plasma time: 5 hr
Peak plasma concentration increased by 27% when administered with a high fat meal
Hysingla ER

Peak plasma time (mean): 14-16 hr (range 6-30 hr)
AUC and peak plasma concentration increase linearly with doses
Peak plasma concentration (median): 14.6-110 ng/mL
AUC (median): 284-1787 ng•hr/mL
Peak plasma concentration increased by 20% when administered with a high fat meal
Vantrela ER

Peak plasma time: 8 hr (single dose); 5 hr (steady-state)
Peak plasma concentration (single doses): 12.6-62.5 ng/mL
AUC (single doses): 199-1189 ng•hr/mL
Distribution
Protein bound: ~19% (Zohydro ER); 36% (Hysingla ER); 19-45% (Vantrela ER)

Vd: 402 L (Hysingla ER); 1300-1400 L (Vantrela ER)

Metabolism
Metabolized in liver by CYP2D6 (minor) via O-demethylation, CYP3A4 (major) via N-demethylation, and 6-keto reduction

Metabolites: CYP3A4 mediated N-demethylation to norhydrocodone is the primary metabolic pathway; CYP2D6 to hydromorphone (active metabolite with higher binding capacity to mu opioid receptor)

Elimination
Half-life: 8 hr (Zohydro ER); 7-9 hr (Hysingla ER); 11-12 hr (Vantrela ER)

Excretion: Primarily by kidneys

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🐼Aptensio XR 10 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 10 MG CAPSULE
Aptensio XR 15 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 15 MG CAPSULE
Aptensio XR 20 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 20 MG CAPSULE
Aptensio XR 30 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 30 MG CAPSULE
Aptensio XR 40 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 40 MG CAPSULE
Aptensio XR 50 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 50 MG CAPSULE
Aptensio XR 60 mg cap,ER sprinkle,biphasic 40-60 APTENSIO XR 60 MG CAPSULE

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🐼Pharmacology
Mechanism of Action
Unknown; may block reuptake of norepinephrine and dopamine into presynaptic neurons; may stimulate CNS similar to amphetamines; may stimulate cerebral cortex and subcortical structures

Absorption
Bioavailability: ~30%; large individual differences (11-52%); 73.9% (Jornay PM)

Duration: 3-6 hr (IR); 3-8 hr (ER, SR); 8-12 hr (CD, LA, Concerta)

Peak plasma time: 6-8 hr (PO); 7.5-10.5 hr; (patch); 14 hr (Jornay PM)

Peak plasma concentration: 3.7 ng/mL (PO); 0-114 ng/mL (patch)

Onset of action

Immediate release: ~2hr
Sustained-release tablet: 4-7 hr
Extended-release tablet (Concerta): 1-2 hr
Transdermal: ~2 hr; applied heat may expedite onset
Distribution
Protein bound: 10-33%

VD: d-Methylphenidate (2.65 L/kg); l-methylphenidate (1.80 L/kg)

Metabolism
Metabolized mostly to a-phenyl-2-piperidine acetic acid (PPAA)

Elimination
Excretion: Urine (90%), mainly as PPAA

Half-life elimination

d-Methylphenidate: 3-4 hr
l-Methylphenidate: 1-3 hr
Jornay PM: 5.9 hr

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🐼dextroamphetamine 10 mg capsule, extended release DEXTROAMPHETAMINE ER 10 MG CAP
dextroamphetamine 15 mg capsule, extended release DEXTROAMPHETAMINE ER 15 MG CAP
dextroamphetamine 5 mg capsule, extended release DEXTROAMPHETAMINE ER 5 MG CAP
dextroamphetamine 10 mg tablet DEXTROAMPHETAMINE 10 MG TAB
dextroamphetamine 5 mg tablet DEXTROAMPHETAMINE 5 MG TAB
dextroamphetamine 10 mg tablet DEXTROAMPHETAMINE 10 MG TAB
dextroamphetamine 5 mg tablet
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