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[86] [50] [12] Roughly half of brain 5-HT 2A receptors are blocked by 1 mg of trazodone and essentially all 5-HT 2A receptors are saturated at 10 mg of trazodone, but the clinically effective hypnotic doses of trazodone are in the 25–100 mg range.
In pharmacokinetics, a loading dose is an initial higher dose of a drug that may be given at the beginning of a course of treatment before dropping down to a lower maintenance dose. [ 1 ] A loading dose is most useful for drugs that are eliminated from the body relatively slowly, i.e. have a long systemic half-life .
There is an important relationship between clearance, elimination half-life and distribution volume. The elimination rate constant of a drug K e l {\displaystyle K_{el}} is equivalent to total clearance divided by the distribution volume
In clinical practice, this means that it takes 4 to 5 times the half-life for a drug's serum concentration to reach steady state after regular dosing is started, stopped, or the dose changed. So, for example, digoxin has a half-life (or t 1 / 2 ) of 24–36 h; this means that a change in the dose will take the best part of a week to ...
An equianalgesic chart can be a useful tool, but the user must take care to correct for all relevant variables such as route of administration, cross tolerance, half-life and the bioavailability of a drug. [5] For example, the narcotic levorphanol is 4–8 times stronger than morphine, but also has a much longer half-life. Simply switching the ...
It was proposed to be used instead of AUC in animal-to-human dose translation, as computer simulation shows that it could cope better with half-life and dosing schedule variations than AUC. This is an example of a PK/PD model, which combines pharmacokinetics and pharmacodynamics. [13]
This is not to be confused with dose regimen, which is a type of drug therapy in which the dose [mg] of a drug is given at a regular dosing interval on a repetitive basis. Continuing the maintenance dose for about 4 to 5 half-lives (t 1/2 ) of the drug will approximate the steady state level. [ 1 ]
An effective half-life of the drug will involve a decay constant that represents the sum of the biological and physical decay constants, as in the formula: = + With the decay constant it is possible to calculate the effective half-life using the formula:
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