Twenty percent of modern pharmaceuticals contain fluorine.
One of these, the cholesterol-reducer atorvastatin (Lipitor), made more revenue than any other drug until it became generic in 2011.
The combination asthma prescription Seretide, a top-ten revenue drug in the mid-2000s, contains two active ingredients, one of which – fluticasone – is fluorinated.
Many drugs are fluorinated to delay inactivation and lengthen dosage periods because the carbon–fluorine bond is very stable.
Fluorination also increases lipophilicity because the bond is more hydrophobic than the carbon–hydrogen bond, and this often helps in cell membrane penetration and hence bioavailability.

Tricyclics and other pre-1980s antidepressants had several side effects due to their non-selective interference with neurotransmitters other than the serotonin target; the fluorinated fluoxetine was selective and one of the first to avoid this problem.
Many current antidepressants receive this same treatment, including the selective serotonin reuptake inhibitors: citalopram, its isomer escitalopram, and fluvoxamine and paroxetine.
Quinolones are artificial broad-spectrum antibiotics that are often fluorinated to enhance their effects.
These include ciprofloxacin and levofloxacin.
Fluorine also finds use in steroids: fludrocortisone is a blood pressure-raising mineralocorticoid, and triamcinolone and dexamethasone are strong glucocorticoids.
The majority of inhaled anesthetics are heavily fluorinated; the prototype halothane is much more inert and potent than its contemporaries.
Later compounds such as the fluorinated ethers sevoflurane and desflurane are better than halothane and are almost insoluble in blood, allowing faster waking times.
Twenty percent of modern pharmaceuticals contain fluorine. One of these, the cholesterol-reducer atorvastatin (Lipitor), made more revenue than any other drug until it became generic in 2011. The combination asthma prescription Seretide, a top-ten revenue drug in the mid-2000s, contains two active ingredients, one of which – fluticasone – is fluorinated. Many drugs are fluorinated to delay inactivation and lengthen dosage periods because the carbon–fluorine bond is very stable. Fluorination also increases lipophilicity because the bond is more hydrophobic than the carbon–hydrogen bond, and this often helps in cell membrane penetration and hence bioavailability.
Tricyclics and other pre-1980s antidepressants had several side effects due to their non-selective interference with neurotransmitters other than the serotonin target; the fluorinated fluoxetine was selective and one of the first to avoid this problem. Many current antidepressants receive this same treatment, including the selective serotonin reuptake inhibitors: citalopram, its isomer escitalopram, and fluvoxamine and paroxetine. Quinolones are artificial broad-spectrum antibiotics that are often fluorinated to enhance their effects. These include ciprofloxacin and levofloxacin. Fluorine also finds use in steroids: fludrocortisone is a blood pressure-raising mineralocorticoid, and triamcinolone and dexamethasone are strong glucocorticoids. The majority of inhaled anesthetics are heavily fluorinated; the prototype halothane is much more inert and potent than its contemporaries. Later compounds such as the fluorinated ethers sevoflurane and desflurane are better than halothane and are almost insoluble in blood, allowing faster waking times.
Fluorine