OTC Meds of the Early 1900s
You’re probably aware of the old patent medicines- everything from harmless snake oils to very real, very dangerous concoctions of cocaine, morphine, belladonna, and alcohol that were sold without regulation by people who were more showmen than pharmacists.
And, likewise, you’re probably familiar with today’s over the counter (OTC) medications- the acetaminophen (paracetamol), ibuprofen, diphenhydramine, aspirin, loperamide, bismuth subsalysate- that you would find in the local pharmacy, drug or grocery store.Â
But you might not be aware that there was a period in between these. Where there was some government regulation, some knowledge that you probably didn’t need (and didn’t want) morphine for your cough, but where the pharmacy knowledge wasn’t quite where it is today as far as making medicine relatively safe for consumers to purchase without a prescription.
Well I recently went to an antique mall with a whole section devoted to early OTC drug packaging, and found it absolutely fascinating. I did some research on what I found for you guys- hope you find it as interesting as I did!
The first two are both marketed as “Laxative Cold Tablets” and contain a drug called “Acetanilide.” Acetanilide was first created in 1886, and first marketed under the brand name “Antifebrin” in 1887. It was one of the first non-aspirin, non-opioid painkillers/fever reducers available to consumers. Acetanilide is a prodrug of acetaminophen (AKA paracetamol, brand name Tylenol), meaning that while the chemical itself was not particularly helpful, the body would break it down into acetaminophen, which was responsible for the painkilling and fever-reducing effects.
Though effective, acetanilide and other similar acetamenophen prodrugs did have a significant drawback. Sometimes it would metabolize to a chemical called aniline along with acetaminophen (or aniline would be present in the drug all along due to defects in the production process). Aniline can be extremely toxic, causing a condition called methylglobinemia where the blood fails to adequately circulate oxygen. Due to this, once it was discovered that the metabolite acetaminophen could be synthesized and used without this risk, acetanilide was taken off the market.
The doses present in each tablet are measured in grains- typically 1 grain equals about 65mg. Instructions for such medications were usually to take 2 grains initially (130mg) and then 1 grain (65mg) every 3 hours as needed after that.
The term “laxative” appears in many different early OTC cold/pain medications. Oddly, the best I can find was that other ingredients were added to cause the laxative effect, not that bowel motility was a natural side effect of acetanilide. So basically people just really liked laxatives to the point where you could market your cold meds better if you made them laxatives as a perk…
The main painkiller in C-2223 is sodium salicylate- a chemical similar to aspirin that is used today primarily to treat acne topically (if you’ve ever read the bottle of an acne product and seen “salicylic acid” this is a salt version of that acid). It has all the same issues that aspirin does, including risk for bleeding, and reye’s syndrome in children. As such, the warning “not for children” on the bottle is very accurate.
Along with sodium salicylate, C-2223 also contained potassium iodide. While most people know potassium iodide as a preventative against certain aspects of radiation sickness, it is also an expectorant, or drug that loosens mucous to make it easier to cough up. Potassium iodide is still available as an expectorant, but usually this is by prescription for chronic bronchitis and other longer-term respiratory illnesses. Today potassium iodide has largely been replaced by the expectorant guafenesin due to severe allergy concerns for some patients (those allergic to shellfish, iodine, or contrast media may have a life-threatening reaction).
Another expectorant, usually used in combination with potassium iodide was ammonium chloride. Ammonium chloride works by irritating the respiratory tract, which encourages it to shed liquid, which loosens secretions. Ammonium chloride can still be found in some some cough medicines, but tends to also irritate the stomach and intestines, causing prohibitive side effects.
Antihistamines/Ye Olde NyQuil:Â
The concept of combining a painkiller, antihistamine, cough suppressant and expectorant into one convenient package for cold and flu is not new.
This tin of Tabcin was from sometime in the late 1930s. It contains the antihistamine thenylpyramine hydrochloride, the painkiller acetophenetidin, and caffeine.
Thenylpyramine hydrochloride is a very early first generation antihistamine. It has largely been replaced by doxylamine (the sedating/antihistamine part of NyQuil) and diphenhydramine (Benadryl).
Acetophenetidin is yet another acetaminophen prodrug- with a twist. Acetophenetidin has a major side effect of being a negative inotrope. Negative inotropes decrease the strength of the heart’s contractions, and so need to be packaged with a positive inotrope (something that strengthens heart muscle contractions), like the caffeine present in this preparation in order to be useful and not cause really serious problems. The caffeine may also have helped counter some of the sedating effect from the thenylpyramine.
Rahnous capsules, meanwhile, go all out. Pyrilamine as an antihistamine (this was taken off the market in the 1970s due to demonstrated risk of liver cancer in rats), acetophenetidin as a painkiller, belladonna as a positive inotrope, extract of lobelia as an expectorant (lobelia, fun fact, contains a drug extremely similar to nicotine), sodium salicylate as another painkiller, camphor (either as another expectorant or positive inotrope, possibly a stimulant to mitigate the sedation from the antihistamine), and magnesium oxide as, you guessed it, a laxative.
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