The title comes from the Jefferson Airplane song from 1967, "White Rabbit", written by Grace Slick: "One pill makes you larger, and one pill makes you small/And the ones that mother gives you, don't do anything at all/Go ask Alice, when she's ten feet tall..."
This is the second movie that Charles Martin Smith worked on with Mackenzie Phillips. They both worked on American Graffiti (1973), and would also work on More American Graffiti (1979). In all three movies, they do not share any scenes together.
According to a New Yorker article, the book Go Ask Alice was completely fabricated by a Mormon housewife.
With the help of talk show host and anti-drug activist Art Linkletter, Beatrice Sparks who doubled as a ghostwriter for Linkletter and wrote the Manuscript for this made for TV movie, passed her book on to Linkletter's literary agent for production of this movie. Linkletter had a personal interest in this project due to the growing drug abuse among teenagers plus the suicide of his daughter Diane a few years earlier.