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Is this brief intervention a reliable way to decide whether
to develop the drug further?
You
answered:
This intervention
is a reliable way to decide whether to develop the drug further.
THIS
MAY BE INCORRECT. My answer is:
PROBABLY
NOT.
Although
analgesic effects of opioids and anti-inflammatory drugs
are readily assessed in single dose studies (Figure
6.1), below there is little information about other
classes of analgesics. Some drugs may work by slower mechanisms
and be missed in a single-dose study. For example, studies
in nerve-injured rats have shown that low-dose infusion
of some drugs that prevent central sensitization progressively
reduce pain behavior over five days of drug treatment. (JC
Hunter, personal communication). In order to minimize the
chance of missing a valuable clinical effect, the length
of an efficacy study might be the sum of the time required
to (1) titrate patients to optimal dose; (2) to reach pharmacokinetic
steady state after optimal doses are reached (that is, about
5 times the drug half-life); (3) cause the physiological
alterations required for pain relief; (4) collect enough
pain ratings to minimize the variance—one week of averaged
ratings may be optimal (Jensen
and McFarland, 1993). Given this caveat about potential
false negative results, a brief infusion study may still
be worth doing early in the development program because
a positive result would suggest that chronic treatment will
also be useful.
| Figure
6.1 Prediction of chronic opioid response by single-dose
infusion |
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| Dellemijn
et al., (1998) treated 44 patients with nonmalignant
neuropathic pain with a brief intravenous fentanyl
infusion followed by 12 weeks of transdermal fentanyl.
(Figure 6.1) Pain relief during the acute infusion
(x axis) was modestly predictive of relief during
chronic treatment (y axis), confirming that a
brief infusion is a reasonable "proof of
concept" study for a new morphine-like opioid.
This is not surprising, because the best studied
molecular analgesic mechanisms of opioids have
onset within seconds or minutes. Benefits of drugs
that affect slower processes might be missed,
however, unless chronic studies are done. |
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