In
pharmacology
Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur betwee ...
, 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 means 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 ('' ceter ...
). 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, clam ...
, 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
Pain is a distressing feeling often caused by intense or damaging Stimulus (physiology), stimuli. The International Association for the Study of Pain defines pain as "an unpleasant sense, sensory and emotional experience associated with, or res ...
. In many cases, the severity of
side effects
In medicine, a side effect is an effect of the use of a medicinal drug or other treatment, usually adverse but sometimes beneficial, that is unintended. Herbal and traditional medicines also have side effects.
A drug or procedure usually used ...
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, sold under the brand name Subutex among others, 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 a ...
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Codeine
Codeine is an opiate and prodrug of morphine mainly used to treat pain, coughing, and diarrhea. It is also commonly used as a recreational drug. It is found naturally in the sap of the opium poppy, ''Papaver somniferum''. It is typically use ...
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Dose–response relationship
The dose–response relationship, or exposure–response relationship, describes the magnitude of the Stimulus–response model, response of an organism, as a Function (mathematics), function of exposure (or Dose (biochemistry), doses) to a Sti ...
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Pain ladder
"Pain ladder", or analgesic ladder, was created by the World Health Organization (WHO) as a guideline for the use of drugs in the management of pain. Originally published in 1986 for the management of cancer pain, it is now widely used by medical p ...
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Weber–Fechner law
The Weber–Fechner laws are two related scientific law, scientific laws in the field of psychophysics, known as Weber's law and Fechner's law. Both relate to human perception, more specifically the relation between the actual change in a physica ...
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