BA%, T1/2 duration etc. - brought in part by Lorne???

[Lorne???]

Ok people, time to update and expand upon information; may sticky this, at least temporarily- by all means those who can contribute should- the focus is on BA% via various routes, and T1/2, and corresponding duration. Also, SDU, that is, Standard Dosage Unit, used for conversion and equivalent purposes. Example? 10mg IV morphine is a SDU; ~20mg oxycodone (range(or R)=15-30mg) P.O., IV oxycodone SDU is 10-15mg.

Thank you For now have copy and pasted some shall get to it, I suppose

All bioavailabilies are relative to IV bioavailability (100% ). For those that do not know, the bioavailability of a substance is basically the percentage of the dose that gets absorbed. It changes drastically for each method of administration. A half-life is the amount of time it takes for your body to eliminate half of the substance that you took. There is a lot of conflicting data on the exact bioavailabilities of each substance so every thing thats listed here is the average.

Opiates
Methadone: Oral 84%.(range 40-95) Elimination half-life:12-40hrs
hours,
Ketobemiodone: Oral 34% +/-10%; Rectal 44% +/- 9%. Elimination half-life: 2.25- 2.45 hours
Meperidine: Rectal 55%, IM 80-85% Elimination half-life 3.0 h
Buprenorphine: Oral 10-22%, Sublingual 20-50%* IM 90-100%. Elimination half-life: 12-44 hours SL, 3-4hrs IV/IM/range 1.7-7
Hydromorphone: Oral-30-35%(can reach 50%); Intranasal 52.4%; Rectal 33%
Dihydrocodeine: Oral 20%. Elimination halflife 4 hours (inhibitors can dramatically increase effects)
Heroin: Oral Dose dependent and variable; 27-70% ; IM 85%
Fentanyl: Transdermal 92%; Sublingual and Buccal 50%; Intranasal 70%. Protein binding 80-85% Elimination half-life 3-12 hours
Sufentanil: Intranasal 78%,
Remifentanil: Protein binding 70%. Elimination half-life 1-20 minutes
Alfentanil: 92% Protein binding. Elimination half-life is 1.5-2 hours
Morphine: Oral 30%; Rectal 30%; Intranasal 15-20%, Chitosan(a linear polysaccharide that helps absorb drugs better) has been shown to increase nasal bioavailability of morphine from around 10-20% to over 60%, SC-60%, protein binding 30-40%, half-life is 2-3 hours
Oxycodone: Oral ~60%(35-90%) intranasal- 47-79%(?)
Hydrocodone: Oral bioavailability is not really known but it is around oxycodone bioavailability; Orally 70% of it is usually absorbed, half-life is 4-8 hours
Oxymorphone: Intranasal 43%; Orals 10-20%; Rectal 10%
BUTORPHANOL : Oral 5-17%
Tramadol: Oral 68-72%; Rectal 77%: Eliminatio half-life 5-7 hours
Codeine: Oral 90%; Rectal 90%
Diphenoxylate: Protein binding 74-95%. Elimination half-life 12-14 hours
Pethidine(meperidine): Oral 50-60%. Protein Binding 65-75%, Half Life 3-5 hours
Normeperidine Is about half as potent as meperidine, but it has twice the CNS stimulation effects.
Pentazocine: Oral 20%. Half-life 2 to 3 hours

xymorphone: Intranasal 43%; Orals 10-20%; Rectal 10%(Rectal provides longer duration, though slower onset and plasma levels, as with some other opioids)
BUTORPHANOL : Oral 5-17%
Tramadol: Oral 68-72%; Rectal 77%: Eliminatio half-life 5-7 hours (Prodrug for Nortramadol, ~50x more potent at Mu receptor)
Codeine: Oral 90%; Rectal 90%
Diphenoxylate: Protein binding 74-95%. Elimination half-life 12-14 hours
Pethidine(meperidine): Oral 50-60%. Protein Binding 65-75%, Half Life 3-5 hours
Normeperidine Is about half as potent as meperidine, but it has twice the CNS stimulation effects.
Pentazocine: Oral 20%. Half-life 2 to 3 hours

Opiate Antagonists
Naloxone: Oral 2-4%. Elimination half-life 1-1.5 hours
Naltrexone Oral 5-40%. Protein binding 21%, Half life-4 hours (naltrexone),
and 13 hours (6-β-naltrexol) (metabolite)

Benzodiazepines
Alprazolam: Oral 80-90%. halflife 9-20 hours duration short/3-8hrs
Bromazepam: Oral 84% half life 10-20 hours
Cinolazepam: Oral 90-100%, Half life 9 hours
Clobazam: Oral 90%. Elimination half-life 18 hour half life
Clorazepate: Oral 91%. Elimination T1/2: Nordazepam ~20-150 hours (Prodrug for Nordazepam converted presystemically


hlordiazepoxide: Oral 100%; IM 90-95%. Elimination half-lives of its metabolites range from 14—100 hours
Clonazepam: Oral 90%; IM 93% intranasal (low) ~85 protein bound- Tmax 1-4hrs; Long acting Benzodiazepine, slow-intermediate onset
Diazepam: Oral 85-100%. Protein binding: 94% to 99% Tmax 1-2hrs P.O., Fast acting benzodiazepine, short- intermediate duration of action; Likely more effective with Chronic administration vs acute
Estazolam: Oral 93%. Elimination half-life 10-24 hours -Tribenzo
Lorazepam: Oral 85-90%; Intranasal 78%? Sublingual T1/2 10-20hrs, medium duration of action (longer than valium w/ acute dosing)

Midazolam: Oral 35-.40%; Intranasal 55%, IM 90%
Flurazepam: Oral 83%. Elimination half-life is 40-250 hours
Temazepam: Oral 96%. Elimination halflife is 8-20 hours
Quazepam: Oral 29-35% Half life 39 hours


Other GABA acting drugs/ analogs
Gabapentin (Neurontin): Oral: lower doses absorb better at 60% for .9g daily dosing; 27% for 4.8g daily dose. Food increases absorbtion by 14%. Protein binding 3%. Elimination Half life 5-7 hours

Gabapentin Enacarbil Provides improved absorption
Pregablin (Lyrica): Bioavailability 90%. Elimination Half life 5–6.5 hours
Vigabatrin: Oral 80-90%. Elimination half-life 5-8 hours in young adults, 12-13 hours in the elderly.

Buspirone:Oral 5%. Elimination half-life 2-3

 

[Lorne???]

Um these may need adjustment (tweakers, tweak)

xxthylphenidate: Oral 11–52%; Rectal is significantly higher, however an exact figure is not currently known. Elimination half-life 2–4 hours
Cocaine hcl: Oral 30%; Intranasal 40-60%. Elimination half-life .8-4 hours (depending on MOA)
Methamphetamine: Oral 62.7%; Intranasal 79%; Smoked 90.3%; 62.7%
Amphetamine: Oral 4L/kg; low binding to plasma proteins 20% Elimination half-life 10–13 hours
Ephedrine: Oral 85%. Elimination half-life 3–6 hours
Dextroamphetamine: Oral 75%. Elimination half-life 10-28 hours
Bupropron (Wellbrutrin: Oral 5-30%. Elimination half-life is 20 hours
Lisdexamfetamine: Prodrug for Dextroamphetamine, w/ non hepatic conversion
Dissociatives/psychedelics
PCP: Oral 65%; Smoked 50%
Ketamine's: Oral 20±7%; IM 93%; Intranasal 25-50%; IV dose 96% and or



D-depressants
Tianeptine: Oral 89 +/- 11%. Elimination half-life 2.5 hours
Trazodone: Oral 89 to 95%.

Muscle relaxants
Carisoprodol(soma): Oral 65%. 60% protein binding. Elimination half-life 8 hours
Meprobromate: Oral 60% protein binding. Elimination half-life is 10 hours
Baclofen: Protein binding 30%. Elimination half-life 1.5 hours
Dantrolene: Oral 70%

Sleep aids
Zolpidem: Oral 67%. 92% is bound in plasma
Zaleplon: Oral 30%. Elimination half-life is 1.1 hours
Diphenhydramine: Oral 86%. Protein binding 98 to 99%. Elimination half-life 1-4 hours
Eszopiclone (Lunesta): Protein binding 52-59%. Elimination half-life 6 hours
Zopiclone: Oral 52-59%. Bound to plasma protein. Elimination half-life 6 hours, and 9 hours for over 65