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.
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.
The source material for this TV movie, the 1971 book Go Ask Alice, was first published by Prentice-Hall as non-fiction; the author was credited as "Anonymous" and the book was presented as a purportedly real diary of an actual teenage girl who fell into drug addiction and prostitution before dying of an overdose. However, almost from the book's first publication, there has been strong evidence that the book is actually fiction wholly invented by its purported "editor," Beatrice Sparks. Such suspicions only increased after Sparks "coincidentally" released a series of other books that were also supposedly the "real" diaries of other teenagers experiencing other then-currently controversial social ills (teen pregnancy, sexually transmitted infections, suicidal thoughts, and, during a period of heightened societal fear of the occult, even satanism).