In
pharmacology, the term ceiling effect refers to the property of increasing doses of a given medication to have progressively smaller incremental effect (an example of
diminishing returns
In economics, diminishing returns are the decrease in marginal (incremental) output of a production process as the amount of a single factor of production is incrementally increased, holding all other factors of production equal ( ceteris parib ...
). Mixed
agonist-antagonist opioids, such as
nalbuphine
Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. It is given by injection into a vein, muscle, or fat.
Side effects of nalbuphine include sedation, sweatiness, clamm ...
, serve as a classic example of the ceiling effect; increasing the dose of a narcotic frequently leads to smaller and smaller gains in relief of
pain. In many cases, the severity of
side effects
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...
from a medication increases as the dose increases, long after its therapeutic ceiling has been reached.
The term is defined as "the phenomenon in which a drug reaches a maximum effect, so that increasing the drug dosage does not increase its effectiveness."
Sometimes drugs cannot be compared across a wide range of treatment situations because one drug has a ceiling effect.{{cn, date=September 2020
Sometimes the desired effect increases with dose, but
side-effects worsen or start being dangerous, and
risk to benefit ratio increases. This is because of occupation of all the receptors in a given specimen.
See also
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Agonist–antagonist opioids
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Buprenorphine
Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal ...
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Codeine
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Dose–response relationship
The dose–response relationship, or exposure–response relationship, describes the magnitude of the response of an organism, as a function of exposure (or doses) to a stimulus or stressor (usually a chemical) after a certain exposure tim ...
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Pain ladder
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Weber–Fechner law
The Weber–Fechner laws are two related hypotheses in the field of psychophysics, known as Weber's law and Fechner's law. Both laws relate to human perception, more specifically the relation between the actual change in a physical stimulus an ...
References
External links
Is there a ceiling effect of transdermal buprenorphine? Preliminary data in cancer patientsClinical evidence for an LH ‘ceiling’ effect induced by administration of recombinant human LH during the late follicular phase of stimulated cycles in World Health Organization type I and type II anovulationAnalgesic effect of i.v. paracetamol: possible ceiling effect of paracetamol in postoperative pain
Pharmacodynamics