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 yourbody 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.
Methadone: Oral 84%. Elimination half-life:24-36 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 22%; Sublingual 30%; IM 90-100%. Elimination half-life: 12-44 hours
Hydromorphone: Oral-30-35%; Intranasal 52.4%; Rectal 33%
Dihydrocodeine: Oral 20%. Elimination halflife 4 hours
Heroin: Oral 35%; 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 60-87%; intranasal- 55-70%
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
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)
Alprazolam: Oral 80-90%. halflife 9-20 hours
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 half-life 36-100 hours
Chlordiazepoxide: Oral 100%; IM 90-95%. Elimination half-lives of its metabolites range from 14—100 hours
Clonazepam: Oral 90%; IM 93%
Diazepam: Oral 85-100%. Protein binding: 94% to 99%
Estazolam: Oral 93%. Elimination half-life 10-24 hours
Lorazepam: Oral 85-90%; Intranasal 78%
Midazolam: Oral 36-40%; 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
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 2-3h
Methylphenidate: 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
PCP: Oral 65%; Smoked 50%
Ketamine’s: Oral 20±7%; IM 93%; Intranasal 25-50%; IV dose 96% and oral dose 20±7%. Ketamine is rapidly distributed into brain and other highly perfused tissues, and is 12% bound in plasma. The plasma half-life is 2.3 ± 0.5 hours.
MDMA: Elimnation half-life of the “S” isomer has a shorter half life (about 4 hours), whereas the “R” isomer has a much greater half life. (about 14hours)
Tianeptine: Oral 89 +/- 11%. Elimination half-life 2.5 hours
Trazodone: Oral 89 to 95%.
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%
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
Hexobarbital: Oral 25%. Protein binding
Methohexital: Rectal 17%. Elimination half-life is 5.6 hours
Phenobarbital: Oral 95%. Protein binding 20-45%. Elimination half-life is 53 to 118 hours
Primidone: Oral 90%. Protein binding 70%. Elimination half-life of Primidone 5-15 hours, active metabolite (Phenobarbital) Elimination half-life- 100 hours
Additive Makes Antibiotics Stand Up to MRSA
Researchers from North Carolina State Univ. have increased the potency of a compound that reactivates antibiotics against methicillin-resistant Staphylococcus aureus (MRSA), an antibiotic-resistant form of Staphylococcus that is notoriously difficult to treat. Their improved compound removes the bacteria’s antibiotic resistance and allows the antibiotic to once again become effective at normal dosage levels.
NC State chemist Christian Melander had previously proven the effectiveness of a 2-aminoimidazole compound in reactivating antibiotics against resistant bacterial strains. However, the original compound was not potent enough. In his latest work, described in a paper appearing in Angewandte Chemie, Melander, Assistant Prof. Roberta Worthington and graduate student Tyler Harris have solved the potency issue, bringing them one step closer to in vivo testing.
Read more: http://www.laboratoryequipment.com/news/2012/10/additive-makes-antibiotics-stand-mrsa
It is an anticoagulant normally used in the prevention of thrombosis and thromboembolism, the formation of blood clots in the blood vessels and their migration elsewhere in the body respectively. It was initially introduced in 1948 as a pesticide against rats and mice and is still used for this purpose, although more potent poisons such as brodifacoum have since been developed. In the early 1950s warfarin was found to be effective and relatively safe for preventing thrombosis andembolism (abnormal formation and migration of blood clots) in many disorders. It was approved for use as a medication in 1954 and has remained popular ever since; warfarin is the most widely prescribed oral anticoagulant drug in North America.
- Category A : No risk to fetus.
- Category B : Insufficient data to use in pregnancy
- Category C : Benefits of medication could outweigh the risks
- Category D: Risk to fetus exists but the benefits could outweigh the probable risks.
- Category X: Avoid use in pregnancy or in those who may become pregnant. Potential risks outweigh potential benefits.
Antibiotic.. Has a cool structure.. is an ionophore.. binds K+ ions which sit in the centre of the molecule and takes them across the cell membrane and deposits them outside of the cell screwing up the cells ionic equilibrium which kills the cell
But theyre not selective for bacteria and also have an effect on mammalian cells so theyre used for research purposes only and not therapeutically
Aspirin, ibuprofen, naproxen, and many other non-steroidal anti-inflammatory drugs (NSAIDs) work as COX inhibitors. They suppress the catalytic functions of the enzymes COX1 and COX2. COX2, which appears up injuries and other inflammatory stimuli, is deemed “bad”. It catalyzes the…
Doxorubicin (Adriamycin, hydroxydaunorubicin) also known as the Red Devil, is in a class of medications called anthracyclines. It works by slowing or stopping the growth of cancer cells in your body.
I’m going to be doing a new series of posts on drug facts. My pharmacy posts have been pretty boring and pointless in the past so please let me know if you would like me to continue with these.
The idea is that I can refresh my own knowledge while pick out key ‘take home messages’ about drugs…
Featured drug of the week-Pramipexole Dihydrochloride
Brand name: Mirapex
Available doses: .125, .25, .5, .75, 1, and 1.5mg. IR and ER formulations, tab.
Indication: Parkison’s Disease, Restless Leg Disorder (RLS, however, primarily prescribed for the aforestated), Off-label: Cluster headache, and to combat side-effect disorders stemming from SSRI administration (e.g. sexual dysfunction). Class: Non-ergoline dopamine agonist
Side-effects: Serious: exteme drowsiness, narcoleptic symptoms, hypotension-like symptoms (fainting, sweating, nausea), flu-like symptoms, heart arrhythmias, tremors or uncontrollable movements, behaviour fluctuations (complusive habits such as gambling, overeating, sexual frequency) Lesser: xerostomia, swelling, appetite changes, insomnia, blurred vision, forgetfulness, impotence.
Drug Interactions: Those indicated for hypertension (Diltiazem, Verapamil, and Triamterene namely), prescription anti-emetics or non-proton pump inhibitors (H-2 agonsit) indicated for stomach acid (metoclopramide, promethazine, cimetidine, ranitidine), or other dopamine agonist (haloperidol, thioridazine, chlorpromazine)