NONMEM Users Guide Part V - Introductory Guide - Chapter 4
1. What This Chapter is About
2. General
3. Structural Parameter Models
3.1. Linear Models
3.2. Multiplicative Models
3.3. Saturation Models
3.4. Models with Indicator Variables
3.4.1. Combinations
3.4.2. Time Varying
3.5. Structural Kinetic Models
4. Population Random Effects Models
4.1. Models for Interindividual Errors
4.1.1. Additive/Multiplicative Models and theExponential Model
4.1.2. Other Models
4.1.3. General Form for the Parameter Model
4.2. Statistical Models for an Individual’sObservations
5. The Population Mixed Effects Model

NONMEM Users Guide Part V - Introductory Guide - Chapter 4

Chapter 4 - Models for Population Data

1. What This Chapter is About

In this chapter, models for data from (animal or human) populations will be discussed. These models describe observations from a number of individuals sampled from the population. The distinguishing feature of the data to which such models apply is that there is more than one observation from some (usually most) individuals. A population model includes the structural model of Chapter 3, but also a new model, which shall be called the parameter model, for each individual’s kinetic parameters. The parameter model can have both fixed and random effects. A population model also includes the error model of Chapter 3.

2. General

Individuals differ, and the types, degrees and causes of these differences are often what we want to learn. NONMEM was designed to help us learn these things. These individual differences can be due to fixed and/or random effects, but they all manifest themselves by affecting the value of an individual’s parameters,

Image grohtml-147484-2.png

. That is, first, each individual is regarded as having his own particular value of Image grohtml-147484-3.png . If the data come from Image grohtml-147484-4.png individuals, then we may rewrite the (not completely) general mixed effects model, (3.4) for Image grohtml-147484-5.png , the Image grohtml-147484-6.png observation from the Image grohtml-147484-7.png individual, as

Image grohtml-1474842.png

Eq (4.1) is now (part of) a population model because it explicitly recognizes, through the subscript, Image grohtml-147484-9.png , that the data come from distinct individuals. Note too that we have written Image grohtml-147484-10.png , rather than Image grohtml-147484-11.png . According to NONMEM conventions, when modeling data from a population, the random effects in the residual errors are denoted by Image grohtml-147484-12.png , their individual variances by Image grohtml-147484-13.png , and the collection of the variances by the matrix Image grohtml-147484-14.png , denoted SIGMA in NONMEM input and output. We also adopt the same convention here as we did for Image grohtml-147484-15.png : the Image grohtml-147484-16.png diagonal element of Image grohtml-147484-17.png is interchangeably denoted Image grohtml-147484-18.png or Image grohtml-147484-19.png .

When dealing with population data, the symbol Image grohtml-147484-20.png is reserved for random effects influencing the vectors Image grohtml-147484-21.png , as is now explained. We can write a general model (but not yet as general a model as we will present later) for Image grohtml-147484-22.png :

Image grohtml-1474843.png

It is called the parameter model. Here, Image grohtml-147484-24.png is a structural (though non-kinetic) type model (of which examples will be given shortly), which is a function of fixed effects, Image grohtml-147484-25.png , and fixed effects parameters, Image grohtml-147484-26.png . Note that since, in general, Image grohtml-147484-27.png is a vector, Image grohtml-147484-28.png must be a vector-valued function, and for the same reason, Image grohtml-147484-29.png is usually a vector. This will be discussed further later. All fixed effects, whether they are part of the kinetic structural model, or are part of the parameter model, are input to NONMEM in a uniform way. For the purposes of this discussion, the symbol Image grohtml-147484-30.png is used for the particular fixed effects in Image grohtml-147484-31.png , such as the individual’s height, weight, and so forth (this will be discussed further in a moment). Even though most often Image grohtml-147484-32.png is regarded as time invariant, as is done in most of the discussion in this document, fixed effects can change with time, and thus kinetic parameters within Image grohtml-147484-33.png can change with time. This will be discussed further in Section 3.4.2.

3. Structural Parameter Models

The symbol in (4.2) for the fixed effects parameter vector is Image grohtml-147484-34.png , not Image grohtml-147484-35.png . As mentioned in Chapter 3, we reserve the symbol Image grohtml-147484-36.png , in this document, for an individual’s fixed effect parameters and use the symbol Image grohtml-147484-37.png for a vector of population (fixed effects and possibly random effects) parameters.

Recall the phenobarbital example of Chapter 2. For the second run, the input contained the line of code

TVCL = THETA(1) + THETA(3)*WT

Translated into the symbols we are using here, this is

Image grohtml-1474844.png

In (4.3), Image grohtml-147484-39.png and Image grohtml-147484-40.png are the first and third elements of the parameter vector Image grohtml-147484-41.png , and Image grohtml-147484-42.png is an element of Image grohtml-147484-43.png (recall that this value of weight appears as a data item). The tilde over Image grohtml-147484-44.png is meant to distinguish this typical population value of clearance from the Image grohtml-147484-45.png individual’s actual value of clearance. According to this model, Image grohtml-147484-46.png will be the same for any two individuals both of whom have the same value of weight. Equation (4.3) defines an element (the one associated with clearance) of the vector-valued function Image grohtml-147484-47.png . Note that in (4.3), we use the subscript Image grohtml-147484-48.png to stress that this equation applies to the Image grohtml-147484-49.png individual, but there is no confusion when, as in the NM-TRAN input, and in the following, the subscript is omitted. It should always be understood that all variables and data items used in the parameter model definition refer to the same individual. Many different models are possible to describe the dependence of individual parameters on fixed effects. However, certain model forms are simple, easy to use, and cover most cases. An assortment of these will be discussed briefly next.

3.1. Linear Models

The simplest form that Image grohtml-147484-50.png can take, and the most common, is one that is linear in Image grohtml-147484-51.png . An example is (4.3): all elements of Image grohtml-147484-52.png appear as linear coefficients of terms involving data items. The data items themselves can appear nonlinearly, without affecting the linearity with respect to Image grohtml-147484-53.png . For example, if clearance is the sum of renal and non-renal components, and renal clearance is believed to be proportional to renal function as described according to a standard formula involving the elements of Image grohtml-147484-54.png : age ( Image grohtml-147484-55.png ), serum creatinine ( Image grohtml-147484-56.png ), and weight ( Image grohtml-147484-57.png ), then one might write

Image grohtml-1474845.png

Image grohtml-1474846.png

Image grohtml-1474847.png

Image grohtml-1474848.png

Clearly, Image grohtml-147484-62.png is a nonlinear function of Image grohtml-147484-63.png , for example, and so, therefore, is Image grohtml-147484-64.png , but Image grohtml-147484-65.png is linear in Image grohtml-147484-66.png , and (4.4 - 4.6) is still considered a linear model. (Do not worry about the non-consecutive numbering of the elements of Image grohtml-147484-67.png ; a model for Image grohtml-147484-68.png is being developed (an alternative to 4.3), and the missing elements Image grohtml-147484-69.png and Image grohtml-147484-70.png will appear presently.)

3.2. Multiplicative Models

Multiplicative models are linear models, but on a logarithmic scale. For example, if patients covering a very wide range of weights are studied, metabolic clearance might vary with weight, but not linearly, and a substitute for (4.4) might be

Image grohtml-1474849.png

Image grohtml-14748410.png

Note that the logarithm of Image grohtml-147484-73.png ( Image grohtml-147484-74.png ) is linear in Image grohtml-147484-75.png , but Image grohtml-147484-76.png itself is not. Of course, (4.4.1) can also be written

Image grohtml-14748411.png

Models (4.4.1) and (4.4.2) are equivalent so far as Image grohtml-147484-78.png is concerned, but Image grohtml-147484-79.png of (4.4.2) corresponds to Image grohtml-147484-80.png of (4.4.1).

3.3. Saturation Models

A useful model for processes reaching a maximum is a hyperbolic model. For example, if a second drug, (whose steady-state plasma concentration, Image grohtml-147484-81.png is known and available in the data set), is present in some individuals and it is believed that this second drug is an inhibitor of the metabolism of the study drug, one might wish to use

Image grohtml-14748412.png

This model is shown in figure 4.1. The inhibition is expressed by the ratio occurring within the brackets and is a concave hyperbola, asymptoting to a maximum value equal to Image grohtml-147484-83.png . It is identical in form to the familiar Michaelis-Menten model.

Image +chapt4/fig4.1.ubuntu.epsi.png

Figure 4.1. A hyperbolic model for metabolic clearance of drug on the ordinate, as inhibited by another drug at steady-state concentration Image grohtml-147484-85.png on the abscissa.

3.4. Models with Indicator Variables

Indicator variables were discussed in Chapter 3 in connection with the error model. They can be quite useful when modelling individual parameters. They are usually used in a linear model. For example, if the clinical condition, heart failure, is noted as "present" or "absent", one can define an indicator variable, Image grohtml-147484-86.png which equals 0 if heart failure is absent, and 1 if it is present. If metabolic clearance is thought to be affected by heart failure, one might choose

Image grohtml-14748413.png

Here, the non-heart-failure cases will have Image grohtml-147484-88.png , while the heart-failure cases will have Image grohtml-147484-89.png †.
----------

† Heart failure is expected to decrease metabolic clearance. If it does, using a minus sign in (4.4.4) allows the more pleasing result that Image grohtml-147484-90.png will be estimated as positive. The model is identical to one with a positive sign, but then Image grohtml-147484-91.png would probably be negative. If Image grohtml-147484-92.png were constrained to be non-negative, then the sign chosen in the model statement would, of course, be important.
----------

3.4.1. Combinations

Given the basic building blocks of linear, multiplicative and saturation models, these can be combined in the usual algebraic ways (usually by addition) to make more complex models. For example, one could use (4.4.3), (4.5), and (4.6) as a model for Image grohtml-147484-93.png . A non-additive example arises if plasma and urine concentrations are both observed and (kinetic) model (3.6) is to be used for the latter. The parameter Image grohtml-147484-94.png , the fraction of drug excreted unchanged into the urine might be modeled as

Image grohtml-14748414.png

where Image grohtml-147484-96.png is given by (4.5) and Image grohtml-147484-97.png by (4.6) (using any of the (4.4) variants).

3.4.2. Time Varying

As mentioned in Section 2, although most of the time the data items affecting an individual’s Image grohtml-147484-99.png do not change over the course of his data, they occasionally do, and PREDPP can handle this. For example, if an individual had heart failure for part of his observation period, but not the rest, Image grohtml-147484-100.png , according to (4.4.4) should change. Or, if acute renal failure occurred during a patient’s observation period, Image grohtml-147484-101.png would change, according to model (4.5).

PREDPP implements its kinetic model recursively: given the state of the system at time Image grohtml-147484-102.png (by state we mean the amounts of drug in all the compartments), it updates (i.e. advances) the state to that at time Image grohtml-147484-103.png , using the value of Image grohtml-147484-104.png (and in general, the value of Image grohtml-147484-105.png ) at time Image grohtml-147484-106.png to compute a value of Image grohtml-147484-107.png holding between times Image grohtml-147484-108.png and Image grohtml-147484-109.png . The value of Image grohtml-147484-110.png used to compute this Image grohtml-147484-111.png is that value found on the data record with time Image grohtml-147484-112.png . So, in order to have Image grohtml-147484-113.png change appropriately as Image grohtml-147484-114.png does, one places a value of Image grohtml-147484-115.png which is typical for the time period Image grohtml-147484-116.png to Image grohtml-147484-117.png on the data record associated with the time point Image grohtml-147484-118.png . This will not always be easy since the relevant element(s) of Image grohtml-147484-119.png may not be measured at, for example, the midpoint of the time interval (the value at the Image grohtml-147484-120.png of the time interval is a good choice for the Image grohtml-147484-121.png value for the interval). If not, one will have to use some interpolation method to arrive at the typical value. The important point is that the values of the independent variables at time Image grohtml-147484-122.png determine the values of the individual’s parameters applying to the entire period Image grohtml-147484-123.png to Image grohtml-147484-124.png .

3.5. Structural Kinetic Models

The kinetic models (i.e., the models for responses such as drug concentrations) used when performing a population analysis do not differ at all from those used for an individual analysis. One still needs a model for the relationship of Image grohtml-147484-125.png to Image grohtml-147484-126.png and Image grohtml-147484-127.png , and this relationship does not depend on whether Image grohtml-147484-128.png changes from individual to individual or with time within an individual.

4. Population Random Effects Models

Under NONMEM conventions, there are two levels of random effects, and Image grohtml-147484-129.png and Image grohtml-147484-130.png are the symbols used for the vectors of first and second level random effects, respectively. With data from a single individual, only first-level random effects are needed. However, with data from a population of individuals, both first- and second-level random effects are needed. First-level effects are needed in the parameter model to help model unexplainable interindividual differences in Image grohtml-147484-131.png , and second-level effects are needed in the (intraindividual) error model. For example, in (4.2) there is an element of Image grohtml-147484-132.png , Image grohtml-147484-133.png , that is the difference between the individual value Image grohtml-147484-134.png (an element of Image grohtml-147484-135.png ) and Image grohtml-147484-136.png , the typical value of Image grohtml-147484-137.png . This is a first-level random effect. In (4.1) Image grohtml-147484-138.png is the error between Image grohtml-147484-139.png and Image grohtml-147484-140.png . This is a second-level random effect.

4.1. Models for Interindividual Errors

The difference between Image grohtml-147484-141.png and Image grohtml-147484-142.png is called an interindividual error. It arises from a few sources: the function Image grohtml-147484-143.png may be only approximate, and/or Image grohtml-147484-144.png may be measured with error. It is regarded as a random quantity, and it may be modeled in terms of Image grohtml-147484-145.png variables. As usual, each of these variables is assumed to have mean 0 and a variance denoted by Image grohtml-147484-146.png which may be estimated. This variance describes biological population variability.

The difference between Image grohtml-147484-147.png and Image grohtml-147484-148.png is called an intraindividual error. It has been discussed at some length in Chapter 3. Although in that discussion about individual data, this difference was modeled in terms of Image grohtml-147484-149.png variables, in this discussion about population data, it is modeled in terms of Image grohtml-147484-150.png variables. Each Image grohtml-147484-151.png variable is assumed to have mean 0 and a variance denoted by Image grohtml-147484-152.png which also may be estimated.

Each pair of elements in Image grohtml-147484-153.png has a covariance, and NONMEM can also estimate this, although often we choose to assume that the covariance is zero (we made this same assumption for the different elements of Image grohtml-147484-154.png in Chapter 3, Section 3.5.1).
A covariance between two elements of Image grohtml-147484-155.png , Image grohtml-147484-156.png and Image grohtml-147484-157.png , say, is a measure of statistical association between these two random variables. Their covariance is related to their correlation, Image grohtml-147484-158.png ( Image grohtml-147484-159.png ) by

Image grohtml-14748415.png

(Note that now that we are suppressing the subscript Image grohtml-147484-161.png on Image grohtml-147484-162.png , we may, without confusion, use the subscript position to designate elements of Image grohtml-147484-163.png .)

The variances and covariances among the elements of Image grohtml-147484-164.png are laid out in a covariance matrix, called Image grohtml-147484-165.png , and labeled OMEGA in NONMEM input and output. This matrix was defined in Chapter 3, Section 3.8, but some additional comment here may be helpful. If Image grohtml-147484-166.png has, for example, 3 elements, Image grohtml-147484-167.png has the following form:

Image grohtml-14748416.png

Here, as previously, Image grohtml-147484-187.png is another way of writing the variance Image grohtml-147484-188.png , and Image grohtml-147484-189.png ( Image grohtml-147484-190.png ) is the covariance between Image grohtml-147484-191.png and Image grohtml-147484-192.png .

The elements Image grohtml-147484-193.png , Image grohtml-147484-194.png , Image grohtml-147484-195.png are called the diagonal elements of the matrix. If the nondiagonal elements (the covariances) are all zero, i.e. the correlation among all pairs of Image grohtml-147484-196.png elements is zero, the matrix is called a diagonal matrix. The lower triangular elements of the matrix are the elements

Image grohtml-14748417.png

To specify the matrix only its lower triangular elements need be given (and these are all NONMEM does give), since from (4.8) it is clear that for all Image grohtml-147484-210.png , Image grohtml-147484-211.png .

4.1.1. Additive/Multiplicative Models and theExponential Model

Frequently, the model for an interindividual error is the simple additive one (as in (4.2)), such as

Image grohtml-14748418.png

A feature of (4.9) is that the resulting units for Image grohtml-147484-213.png depend on the units of the parameter ( Image grohtml-147484-214.png in this case). For example, this model was used in the theophylline problem of Chapter 2 (Figure 2.6). The final estimate of Image grohtml-147484-215.png is .286 (Figure 2.8). Assuming that the units of V are liters, we interpret this to mean that the standard deviation of V between individuals is .53 Liters ( .53 = Image grohtml-147484-216.png ).

Perhaps even more often, a multiplicative model equivalent to the Constant Coefficient of Variation (CCV) error model (3.5) is used, such as

Image grohtml-14748419.png

This model is also referred to as the proportional error model.
A feature of (4.10) is that the resulting units for Image grohtml-147484-218.png are independent of the units of the parameter ( Image grohtml-147484-219.png in this case). When this model is used in the theophylline problem instead of the additive model, so that Figure 2.6 contains the code V=TVVD*(1+ETA(2)) instead of V=TVVD+ETA(2), then NONMEM estimates Image grohtml-147484-220.png to be .146. We interpret this to mean that the coefficient of variation of V in the population is 38% (.38 = Image grohtml-147484-221.png ).

The exponential model is

Image grohtml-14748420.png

During simulation, (Chapter 12, Section 4.8), the exponential and proportional models give different results. During estimation by the first-order method, the exponential model and proportional models give identical results, i.e., NONMEM cannot distinguish between them. During estimation by a conditional estimation method, the exponential and proportional models for inter-individual variability give different results. The exponential model is preferred for conditional estimation methods. (See NONMEM User’s Guide Part VII, Conditional Estimation Methods.)

4.1.2. Other Models

Occasionally, a model for an individual’s pharmacokinetic parameter might involve scaling an Image grohtml-147484-223.png , as in (3.6), or two or more Image grohtml-147484-224.png ’s as in (3.10). For example, a study might involve patients in the intensive care unit (ICU) and others on non-acute care units. It might be reasonable to suppose that some aspects of the kinetics of ICU patients (e.g., metabolic clearance of drug) are more variable, due to unmeasured factors (e.g., hepatic function) that vary greatly among acutely ill patients. Even though the variation is, in reality, due to a potentially measurable fixed effect (hepatic function), if information on this fixed effect is not available, differences caused by it must be assigned to random factors ( Image grohtml-147484-225.png ). In this case, one might wish to use an indicator variable, Image grohtml-147484-226.png (which equals 1 if the patient is in the ICU, and 0, otherwise), and a model such as

Image grohtml-14748421.png

In addition to model (4.11) we might have, for example,

Image grohtml-14748422.png

Image grohtml-14748423.png

Models (4.11) and (4.12) together, along with suitable models for Image grohtml-147484-230.png and Image grohtml-147484-231.png , form a complete model for an individual’s Image grohtml-147484-232.png parameter, and involve 3 Image grohtml-147484-233.png ’s.

4.1.3. General Form for the Parameter Model

As we have just seen in (4.10) and in (4.11)-(4.12), an element of Image grohtml-147484-234.png need not act in a simple additive way and may act solely on an intermediate variable (e.g. Image grohtml-147484-235.png ). Indeed, there may be more or fewer elements in Image grohtml-147484-236.png than in Image grohtml-147484-237.png , the elements in Image grohtml-147484-238.png may act in nonlinear ways to influence Image grohtml-147484-239.png , and one element of Image grohtml-147484-240.png may influence more than a single element of Image grohtml-147484-241.png . We now give a more general form for the parameter model than (4.2) and then an example illustrating it.

The general form of the parameter model is

Image grohtml-14748424.png

Here, Image grohtml-147484-243.png is a very general function of fixed effects, Image grohtml-147484-244.png , fixed effects parameters, Image grohtml-147484-245.png , and a vector of Image grohtml-147484-246.png ’s, Image grohtml-147484-247.png . The dimensions of the vectors Image grohtml-147484-248.png and Image grohtml-147484-249.png need not be the same. An individual’s kinetic parameter may change with time. As explained in Section 1.6, with NONMEM-PREDPP changes can occur only at discrete time points. Therefore, the parameter actually can be regarded as being a number of parameters, each one applying to a different time period. The parameter Image grohtml-147484-250.png in (4.13), being a vector of all the kinetic parameters for the Image grohtml-147484-251.png individual, can be regarded as encompassing these time-interval-specific parameters.

An example utilizing this generality is provided by a model for observations of both plasma and urine drug concentrations, similar to the one presented previously. Ignoring the details of the structural part of the model, consider the following model

Image grohtml-14748425.png

Image grohtml-14748426.png

Image grohtml-14748427.png

Image grohtml-14748428.png

Image grohtml-14748429.png

In this model, Image grohtml-147484-257.png ; the parameters Image grohtml-147484-258.png and Image grohtml-147484-259.png are regarded as intermediate parameters. We have Image grohtml-147484-260.png , where both Image grohtml-147484-261.png and Image grohtml-147484-262.png influence both Image grohtml-147484-263.png (linearly) and Image grohtml-147484-264.png (nonlinearly).

4.2. Statistical Models for an Individual’sObservations

Model (4.1) can be generalized by incorporating a model like those given in Chapter 3 for the residual errors, i.e. for the differences between the Image grohtml-147484-265.png and Image grohtml-147484-266.png , rather than using just the simple Additive model. A particular instance of such a model may have several types of Image grohtml-147484-267.png ’s, and as mentioned in Section 2, the variances of these Image grohtml-147484-268.png ’s are denoted by Image grohtml-147484-269.png ’s. With a population model these variances could change from individual to individual. With NONMEM, they are considered as constants over individuals. The Image grohtml-147484-270.png ’s can co-vary. A covariance matrix Image grohtml-147484-271.png , like the Image grohtml-147484-272.png matrix given in Section 4.1, gives the variances and covariances of the Image grohtml-147484-273.png ’s, as already discussed at the end of Chapter 3. This does not preclude the magnitudes of the errors from being affected by fixed effects. A model such as (3.8) can still be used. This is shown explicitly by the general model given in the next section.

5. The Population Mixed Effects Model

We have now presented all of the parts needed to fully define a population model. It may be useful to recap this information by stating the entire general model here:

Image grohtml-14748430.png

Image grohtml-14748431.png

Image grohtml-14748432.png

Image grohtml-147484-277.png , Image grohtml-147484-278.png independent for Image grohtml-147484-279.png
Image grohtml-147484-280.png , Image grohtml-147484-281.png independent for Image grohtml-147484-282.png
Image grohtml-147484-283.png , Image grohtml-147484-284.png independent for all Image grohtml-147484-285.png ,

where here, Image grohtml-147484-286.png is a vector, along with Image grohtml-147484-287.png , Image grohtml-147484-288.png , Image grohtml-147484-289.png and Image grohtml-147484-290.png , and Image grohtml-147484-291.png and Image grohtml-147484-292.png are square matrices with dimensions equal to those of Image grohtml-147484-293.png and Image grohtml-147484-294.png .

To try to represent the relationship between all the fixed and random effects of a population model graphically, consider figure 4.2. The model corresponding to this figure is

Image grohtml-14748433.png

Image grohtml-14748434.png

Image grohtml-14748435.png

Image grohtml-14748436.png

where the Image grohtml-147484-299.png are all equal to a constant Image grohtml-147484-300.png , i.e. there is no random interindividual variability in the volume of distribution, so that for the sake of this example, Image grohtml-147484-301.png is just a scalar.

Image +chapt4/fig4.2.ubuntu.epsi.png

Figure 4.2. Random and fixed effects influence observation, Image grohtml-147484-303.png , from the population point of view. Open circle, lower left, is population parameter predicted clearance, closed circle is true clearance for Image grohtml-147484-304.png individual which differs from population prediction by Image grohtml-147484-305.png , chosen randomly from a distribution (upper left) with mean 0 and SD Image grohtml-147484-306.png . Similarly, lower right, the observed Image grohtml-147484-307.png at time Image grohtml-147484-308.png (open square) differs by Image grohtml-147484-309.png from the true value (closed circle) by an error Image grohtml-147484-310.png , chosen independently from a distribution with mean 0 and SD Image grohtml-147484-311.png . The Image grohtml-147484-312.png corresponding to the population-based prediction is also shown (upper curve, open circle).

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