IV injection is appropriate if you want _____ effects but can cause ________. If a long term effect is desired when diazepam is used ___ route works. Absorption from the digestive system is more __ than absorption from an intramuscular site because drugs tend to bind to protein and do so more readily at an _____ than in the ___.
-rapid, local irritation, oral, rapid, injection sites, digestive system
BARBs and BDZs are both ___ acids. BDZs have a pka of about - and are readily absorbed from ____ and ____ administration
weak, 3.5-5, digestive, parenteral
Reports that flunitrazepam can cause very rapid effects when the tablets are what?
turned into a powder and taken intranasally.
Range of lipid solubility in the BDZs and a resulting difference in the _______ of _______. Diazepam on of the fastest acting BDZs peaks in about __-___ minutes. (midazolam, temazepam, flunitrazepam and triazepam). Oxazepam is ____ acting an may take ____ hours to peak.
-speed, absorption, 30-60, slower, several
Absorption from the digestive system may be greatly increased by what??? After small amounts are digested the blood lvls of BDZ can be nearly ___.
- doubled
Z drugs are readily absorbed from the _________ and reach a peak in ~__. There is considerable _____ of zaleplon.
-digestive tract, an hour, first pass metabolism
Once in the blood BDZs and BARBs, distribution and duration of action are determined by lipid solubility. The ____ lipid soluble drugs pass through the blood brain barrier very ____ and their effects on the brain are seen quickly.
-highly, quickly
Fast acting drugs tend to have a short duration because ??
The redistribution of BDZs through the body fat creates a two phase excretion phase. During first phase there is a ___ drop in blood lvl as its being redistributed.This phase has a half life of ___ hours. In the second phase, the blood lvls drop more ___ because the drug remaining in the blood is being ____ and as it is its being replaced by the drug slowly being released from body fat. Half life in this phase is ___-___ hours.
-rapid, 10, slowly , metabolized 27-48
The duration of the effect of the benzodiazepines however is not always determined by their 1/2 lives because the metabolites of some of the older BDZs (diazepam, chlordiazepozide and flurazepam) are also ____. These metabolites have longer ______ and may have somewhat diff effects. Newer BDZs do not have these metabolites (oxazepam, triazolam, alphrazolam, clonazepam and lorazepam).
active, half lives
BDZs and BARBs cross the ____ barrier easily and they appear in the ____ of nursing moms.
placental , milk
Metabolites of BDZs can be slowed by?
consumption of alcohol…half life increases by 60% in chlordiazepozide via small drink……
Zaleplons have life ?
1 hour