A wide range of physiological and hormonal changes occur during pregnancy. Most begin early in the first trimester and increase by the last trimester. These changes can significantly affect pharmacokinetics and pharmacodynamics of drugs and thus may alter their safety and efficacy. Approximately 5% of pregnant women are affected by some form of diabetes, with gestational diabetes being the most prevalent. Several classes of antidiabetic drugs are currently available for the treatment of diabetes, including human insulin, its short and long analogues, and oral hypoglycemic agents. Maternal and fetal responses to these drugs can be affected by changes in absorption, distribution, and elimination in both the mother and the placental-fetal unit. This can dictate the amount of drug that can cross and the amount that is metabolized or eliminated by the placenta. Further studies are needed on the safety of antidiabetic drugs in pregnancy to clarify the extent of their transplacental passage. Specifically, in vitro placental perfusion studies in combination with controlled trials and cord blood measurements can provide insight in to the pharmacokinetics of drug transport across the placenta. This article reviews common types of antidiabetic drugs, focusing on pharmacokinetic considerations that need to be incorporated into the decision on treatment in pregnancy.