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Biotransformation begins either at substituents on the diazepine ring (diazepam: N-dealkylation at position 1; midazolam: hydroxylation of the methyl group on the imidazole ring) or at the diazepine ring itself. Hydroxylated midazolam is quickly eliminated following glucuronidation (t1/2 ~ 2 h).
The patient would thus experience motor paralysis and inability to breathe, while remaining fully conscious but incapable of expressing anything. For this reason, care must be taken to eliminate consciousness by administration of an appropriate drug (general anesthesia) before using a muscle relaxant. The effect of a single dose lasts about 30 min.


Inhibition of the renal actions of vasopressin leads to polyuria and thirst. Thyroid function is impaired, with compensatory development of (euthyroid) goiter. The mechanism of action of Li ions remains to be fully elucidated. Chemically, lithium is the lightest of the alkali metals, which include such biologically important elements as sodium and potassium.
Infertility is caused by suppression of spermatogenesis or follicle maturation. Most cytostatics disrupt DNA metabolism. This entails the risk of a potential genomic alteration in healthy cells (mutagenic effect). Conceivably, the latter accounts for the occurrence of leukemias several years after cytostatic therapy (carcinogenic effect).


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