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The therapeutic index varies widely among substances, even within a related group. For instance, the opioid painkiller remifentanil is very forgiving, offering a therapeutic index of 33,000:1, while Diazepam, a benzodiazepine sedative-hypnotic and skeletal muscle relaxant, has a less forgiving therapeutic index of 100:1. [9]
Another use is in the therapeutic drug monitoring of drugs with a narrow therapeutic index. For example, gentamicin is an antibiotic that can be nephrotoxic (kidney damaging) and ototoxic (hearing damaging); measurement of gentamicin through concentrations in a patient's plasma and calculation of the AUC is used to guide the dosage of this drug ...
When a drug has a narrow therapeutic index, titration is especially important, because the range between the dose at which a drug is effective and the dose at which side effects occur is small. [2] Some examples of the types of drugs commonly requiring titration include insulin, anticonvulsants, blood thinners, anti-depressants, and sedatives.
A compound with a wide therapeutic index (greater than five) exerts its desired effect at a dose substantially below its toxic dose. Those with a narrow margin are more difficult to dose and administer, and may require therapeutic drug monitoring (examples are warfarin, some antiepileptics, aminoglycoside antibiotics).
Newer antidepressants are thought to have fewer and less severe side effects and are also thought to be less likely to result in injury or death if used in a suicide attempt, as the doses required for clinical treatment and potentially lethal overdose (see therapeutic index) are far wider in comparison.
Therapeutic drug monitoring (TDM) is a branch of clinical chemistry and clinical pharmacology that specializes in the measurement of medication levels in blood. Its main focus is on drugs with a narrow therapeutic range , i.e. drugs that can easily be under- or overdosed. [ 1 ]
Therefore, it is more useful to compare such substances by therapeutic index, which is simply the ratio of LD 50 to ED 50. [8] The following examples are listed in reference to LD 50 values, in descending order, and accompanied by LC 50 values, {bracketed}, when appropriate.
Also under development are site-specific conjugation (TDCs) [53] and novel conjugation techniques [54] [55] to further improve stability and therapeutic index, α emitting immunoconjugates, [56] antibody-conjugated nanoparticles [57] and antibody-oligonucleotide conjugates.