The problem of tooth discoloration is emerging in our society because of the poor oral hygiene, physical agents, environmental chemicals, mouth rinses, some dental procedures, general systemic conditions, and drugs. Other common causes of tooth discoloration include excessive use of tea, coffee, tobacco smoking and chewing, chewing of betel morsel (piper betel, paan), and so on. Drug-induced tooth discoloration can be prevented by avoiding prescriptions of well-known offender drugs known to cause tooth discoloration during pregnancy and in young children. This review describes some important groups of drugs that cause tooth discoloration.