Term
| Diisopropylphosphofluoridate (DIPF) |
|
Definition
| Irreversible enzyme inhibitor--binds to a serine residue in the active site of acetylcholinesterase |
|
|
Term
| Monoamine oxidase (MAO) inhibiting drugs |
|
Definition
Irreversible enzyme inhibitor; used for treatment of depression because prevents the degradation of norepinephrine and dihydroxyphenylalanine (DOPA) in the brain. This means that the activity of this enzyme does not return to normal rapidly after the patient is taken off the drug. One has to wait for the synthesis of new enzymes, and this takes about two weeks.
Tyramine is a sympathomimetic compound present in red wine and aged cheeses. When this enzyme is inhibited, the metabolism of tyramine is also inhibited. Eating of tyramine-rich food while taking this type of drug can result in hypertensive crisis (cheese reaction). |
|
|
Term
|
Definition
| Irreversible inhibitor of low and high Km aldehyde dehydrogenases. It is used for the aversive treatment of chronic alcoholism. Alcohol causes flushing, headache, nausea, vomiting, sweating, and hypotension soon after its consumption during treatment with this drug. |
|
|
Term
|
Definition
| Used as a competitive inhibitor to treat methanol and ethylene glycol poisoning. The Km of this "drug" to ADH is much lower than the Km's of either ethylene glycol or methanol. Thus, the enzyme prefers this "drug." |
|
|
Term
| Atorvastatin (Lipitor) and Simvastatin (Zocor) |
|
Definition
| These statin drugs are used to treat high cholesterol because they are competitive inhibitors of the enzyme hydroxymethylglutaryl-CoA reductase (HMG-CoA reductase), the enzyme that catalyzes the first committed step of cholesterol synthesis. As such, they inhibit de novo cholesterol synthesis, thereby lowering plasma cholesterol levels. |
|
|
Term
| Penicillin and Amoxicillin |
|
Definition
| These β-lactam antibiotics act by inhibiting enzymes involved in bacterial cell wall synthesis. |
|
|
Term
| Captopril, enalapril, and lisinopril |
|
Definition
| These angiotensin-converting enzyme (ACE) inhibitors act by inhibiting extracellular reactions. They lower blood pressure by blocking the enzyme that cleaves angiotensin I to form the potent vasoconstrictor angiotensin II. They cause vasodilation and a reduction in blood pressure. |
|
|
Term
| Aminoglycosides (e.g. gentamicin) |
|
Definition
| For this type of drug, the minimum effective concentration is HIGHER than the toxic concentration. In order to give this drug, you must make sure that there is a large difference between peak and trough levels in the steady state. |
|
|
