LEFLUNOMIDE (Arava)

Pharmacology.

Leflunomide’s active metabolite (M1) inhibits dihydro-oratate dehydrogenase, thereby inhibiting pyrimidine biosynthesis. M1 exhibits immunomodulating and anti-inflammatory effects.

Administration and Adult Dosage.

PO for rheumatoid arthritis 100 mg/day for 3 days, then 20 mg/day. Reduce dose to 10 mg if 20 mg is not tolerated.

Pediatric Dosage.

Safety and efficacy not established.

Geriatric Dosage.

Same as adult dosage.

Dosage Forms.

INFLIXIMAB (Remicade)

Pharmacology.

Infliximab is a chimeric monoclonal antibody that binds to soluble and transmembrane forms of TNF a, thereby neutralizing the activity of TNFa and inhibiting TNFa binding to its receptor sites. It has no effect on lymphotoxin (TNFa).Infliximab induces pro-inflammatory cytokines including interleukins 1 and 6 and increases endothelial cell permeability by enhancing leukocyte migration.

Administration and Adult Dosage.

SUMATRIPTAN SUCCINATE (Imitrex)

Pharmacology.

Sumatriptan is a serotonin (5-HT) analogue and a selective agonist at 5-HT1D receptors in cerebral vascular smooth muscle. Receptor activation results in migraine relief by vasoconstriction of intracranial blood vessels and attenuation of the release of vasoactive peptides responsible for inflammation of sensory nerves.

Administration and Adult Dosage.

Fluoxetene (anti-depressant)

Pharmacology.

Fluoxetine is a bicyclic antidepressant that is a selective and potent inhibitor of presynaptic reuptake of serotonin (an SSRI). It does not affect re-uptake of norepinephrine or dopamine and has a relative lack of affinity for muscarinic, histamine,


1- and


2-adrenergic, and serotonin receptors.

Administration and Adult Dosage.

CYCLOPHOSPHAMIDE

Pharmacology.
Cyclophosphamide is inactive in vitro and must be enzymatically activated in the liver to yield active alkylating compounds and toxic metabolites. Cell-cycle phase nonspecific.

Administration and Adult Dosage.
IV or PO alone or in combination regimens 250-500 mg/m2 q 3-4 weeks. IV (usually) or PO in high-dose intermittent regimens (including bone marrow transplant) maximum of 40-50 mg/kg given once or over 2-5 days, repeat q 2-4 weeks-these doses are not well tolerated orally.

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