Sedatives: Herbal and Old School Insomnia Cures
To recapitulate, we are looking for a drug which will help dissolve insomnia without causing residual effects which turn into depression, and habit-formation is also a concern. A lot of things can help, and with respect to pharmacology, there are some places to start looking, which is why I point out the definitions:
Tranquillisers and anxiolytics can do their work without making the person sleep. Sedatives generally cause drowsiness and quiescence greater in degree than tranquillisers, but not necessarily sleep. Hypnotics put people to sleep. Other related definitions are (general) anesthetics, a drug or drugs which cause unconsciousness and insensibility, an analgesic is a drug which relieves pain without causing a loss of consciousness, and a narcotic analgesic is an analgesic which does its work in the central nervous system and often sedates, promotes sleep, and almost invariably causes anxiolysis (the dissolution of anxiety) An opioid narcotises the patient and does so by means of agonism and antagonism of mainly a set of four known receptor types and their subtypes (ζ, κ, μ, and δ opioid) of the central and peripheral nervous system (brain, spinal cord, GI tract and other tissues innervated with somatic neurons) Much of the differences amongst opioids and narcotics are caused by the relative and absolute numbers of receptors occupied and what is done to them, as well as receptors of other systems like up to a dozen suspected unconfirmed opioid receptors, opioid-like, σ, NMDA, nociceptin, PCP, cannabinoid, 5HT, cholinergic (muscarinic, nicotinic), histamine and many others.
As far as drugs which can help with insomnia, I know there are a lot. Zopiclone, lorazepam were on offer to the OP when she wrote to us. She also tried several others as well, listed in previous posts.
Here's most of the rest of which I can think, and I have detailed expositions of benzodiazepines, anticholinergics, and antihistamines in other threads . . .
Insomnia can be caused by tension and pain. Not surprisingly, skeletal muscle relaxants help. Does anyone use baclofen, cyclobenzaprine, or tizanidine for sleep? I pointed out orphenadrine in an earlier post and carisoprodol below. Methocarbamol is a pale imitation of carisoprodol, which the liver turns into meprobamate and is thus an excellent sleep aid but one which can be habit-forming. There are also smooth-muscle relaxants which work on things like the bladder, the intestines, and the arse. Most are anticholinergics mentioned below.
Baclofen is a weak gabapentinoid. It affects the parts of the CNS, peripheral nervous system, endocrine system and others also affected by benzodiazepines and sodium oxybate (Georgia Home Boy, Grievous Bodily Harm) The prototype of the class is Gabapentin (Neurontin) and a newer agent developed for pain management in particular, pregabalin (Lyrica) make up the most common other members of this class. The category has a number of uses as a psychological medicament and a CNS agent used for helping combat chronic pain of certain types, neuropathic like diabetic neuropathy and mechanical and infectious damage to nerves whether, by itself, or as a potentiator for opioids. Some doctors feel pressure to use especially Neurontin off-label as a means to reduce patient narcotic intake or stave off tolerance-required increases for reasons of concerns the doctor may actually have on clinical grounds, or as a political expedient to mollify management, regulators, patients and/or their family members or others, or put off a patient who wants an adjusted dose. Gabapentin was once the definitive example of a medication being used off label, a common and often ingenious and essential practise, for pain in general and especially nerve pain in this case, something the manufacturer encouraged greatly and doctors and patients and patient advocates researched this with enthusiasm.
Cyclobenzaprine is a first-generation anti-depressant used as a pharmacologically dirty skeletal muscle relaxant -- and it can have very long side effects of the anticholinergic type and drowsiness. Its mechanism of action is related to the prototype tricyclic anti-depressant amitriptyline (Elavil) and orphenadrine, the antihistamine with a cleaner side effect profile than the other two noted for creating slight to moderate, durable mood elevation in many users and modest but definite euphoria in some of those cases, which is used as a muscle relaxant, narcotic potentiator, and for dealing with symptoms of Parkinson's Disease and other disruptions of the neuroendocrine system. Cyclobenzaprine does cause euphoria in some folks of the sedative, tricyclic, and general anticholinergic type, so much so that it has the street name Cyclone and the DEA tells doctors that people are abusing it, an exaggeration or lie. Two other anticholinergics like this are hyoscine (scopolamine) and trihexyphenidyl. The latter, called Octane, and Sexy Trihexy, is used in close to normal doses for insomnia, anxiolysis in situations like combat and the post-war Iraq situation (and in fact may have been discovered by police and military around the world as part of a protocol with weak opiates, beta blockers, and anti-insomnia drugs, which also decreases the effects which can eventually add up and turn into PTSD) The street name Sexy Trihexy comes from the effect, also close to the normal dose, of trihexyphenidyl as an aphrodisiac for men, women, straight, gay, bi, and other members of the human family. The antispasmodic dicycloverine (Bentyl) also has been known to make people euphoric and horny and sleepy, as with other anticholinergics.
Tizanidine is a muscle relaxant related to clonidine. In fact, clonidine is also used for insomnia. Other beta-blockers like propranolol can also help, but are better for daytime tranquillisation and dissolving stage fright. Clonidine and propranolol are the most common beta blockers used for hypertension, but they are of different structural and chemical classes and have different mechanisms of action, They should never be mixed or taken in rapid succession as paradoxical hypertensive crisis is a possibility. Clonidine is used by itself by prisoners, young children, and others as a substitute narcotic-like euphoriant, and more commonly is used clinically to reduce the physical symptoms of narcotic withdrawal.
Anyone try bromides, valerates, chloral hydrate, or paraldehyde for insomnia any time recently? The latter two are made from hooch, and there are many bromide and valerate salts used especially in the past for sedation, sleep, and so forth. There are bromide and valerate salts of codeine, morphine, and dihydrocodeine have been used for medicinal purposes.
Codeine, dihydrocodeine, morphine, and heroin methobromides are drugs having the effects of both the bromide and the narcotic. Bromides in general were used as sedatives and early anti-epileptic agents but have fallen out of favour as they can disrupt the endocrine system in various ways. Like the other stable halogens, some amount of bromine is needed buy the body for normal functioning and is acquired from the environment via food.
Valerian is a herb derived especially from the roots of a heliotrope-type flower originally found in Continental Europe and the Levant and now over much of the Northern Hemisphere and has also been carried to the Southern Hemisphere. Aside from things like heroin valerate elixir and morphine valerate injection, there was a popular pair of products in the 1920s used for headaches and insomnia with pain, namely Trivalin, a combination of morphine valerate, caffeine valerate, and cocaine valerate, and Tetravalin, which contained the three plus codeine valerate. The easiest way to get morphine and codeine valerate these days is to use valerian in various forms in the preparation of poppy seed and poppy pod/straw infusions and tea.
Poppy seed tea in particular may also be useful for occasional insomnia as a the phenanthrene alkaloids and other components can create anxiolysis, drowsiness, and other conditions important for sleep.
Other food or herbal substances used to combat insomnia include tryptophan, an amino acid which is a precursor to serotonin which is structurally similar in some ways to melatonin, and exogenous tryptophan, required for proper body function, is obtained from food from many animal sources ranging from poultry to some fish. The relation to serotonin does not make tryptophan a stimulant. In fact, the amount taken in from ingesting turkey, plus a drop in blood pressure from a rush of blood to the digestive tract is what makes people sleepy after large meals.
Kava is one of a number of preparations with active ingredients being various lactones from the Kava bush of the islands of the South Pacific. The herbal preparation has more than a dozen active compounds in it, and it has notable CNS and metabolic effects.
Chamomile is a plant in the daisy family along with ragweed and a somewhat distant valerian relative with a number of alkaloids and other components most often made into a tea for dealing with insomnia and anxiety.
The hormone precursor melatonin is found naturally in the human body, being made in the pineal gland, and it regulates Circadian rhythms and other bodily functions, and can be supplemented by exogenous melatonin, which comes from plants and animals. It has some connexion to melanin but is not the pigment nor closely tied up in how it functions. Melatonin is related tryptophan, which sound like tryptamine, and indeed there are precursor and other relations to these neurotransmitters and important biological substances endogenous and exogenous.
Does anyone get barbs for insomnia or anything anymore? Salts of barbituric acid have different uses depending on their speed of onset and how long they last. Their relative amount of CNS depression may also vary a bit. The shortest acting are for induction of anaesthesia and use as truth serum. Short-acting barbiturates and sedatives are hypnotics, generally. Intermediate-acting barbs are sedative-hypnotics, and the long-acting barbiturates are used for daytime sedation, potentiation of other drugs, and as part of tapering patients off of benzodiazepines. Certain barbiturates in the various classes, intermediate-acting and long-acting especially, are used as anti-convulsants for such cases, for epilepsy, poisoning and other such things,. Many barbiturates not only cause tolerance, but their effective dose rises, but the lethal dose does not, dangerously narrowing the therapeutic index over time.
Barbiturates with these problems led to the development of non-barbiturate agents in the 1940s to 1960s with similar profiles of action and some of which were also dangerous, especially their withdrawal syndromes. Benzodiazepines were a replacement for many of these, and off-label use of gabapentinoids has led to discovery of their usefulness in some of these things. All affect the Gaba-Glutamate-Glycine system in the human body. Another drug, GHB, was invented in the 1874 and developed for human use after about 1958 or so. They all have rebound or true withdrawal syndromes.
My favourite barbiturate is Codeonal, which is codeine diethylbarbiturate, the barbitone salt of codeine popular as a treatment for insomnia with pain and/or apprehension from 1912 to the 1960s,, and there were other ones too, along with morphine, DHC, DHM, and I think even one smack barbiturate. I am not aware of Codeonal being manufactured and sold as a proprietary pharmaceutical in recent times, but compounding pharmacists and other chemists can prepare it, so I have been able to use Codeonal, morphine diethylbarbiturate, and its nicomorphine and hydromorphone analogues on occasion for insomnia caused by pain in the XXI. Century.
I fondly remember another protocol for insomnia of drinking 100 ml of paregoric with three capsules of secobarbitone and chewing up an extended-release Pyribenzamine tablet with a Sprite chaser . . . It was my first introduction to Blue Velvet. Amobarbitone capsules are called Amys, and back in the day I'd bring a bottle of them with me, two young ladies both named Amy joined me in eating some of them, sniffing lots of amyl nitrite poppers, then whatever they call a 69 with three people in it. Secobarbitone and amobarbitone were combined in capsules called Tuinal, also known as Tuies or Twoeys, which we came to like even better and would somtimes eat along with some Bennys, White Crosses, Preludin, or Vitamin R . . . which often fueled a three on one instead.
I know that carisoprodol is used off-label for sleep very frequently, but does anybody actually get Miltown (meprobamate) for sleep anymore?
There were some great non-benzodiazepine hypnotics that were really great which are apparently all gone -- I've expounded up Doriden (glutethimide) and we all know about Mandrax and Quāāludes (methaqualone) . . . there are/were also clomethiazole, ethchlorvynol (Placidyl) and methyprylon (Noludar) as well as more obscure chemical relatives of the above like phenprobamate, tybamate, mecloqualone, and so on.
My opinion on cannabis for this is that especially depending on the cause for the insomnia, it could complicate it, or smash it like a million kilo shithammer. With something like 250 alkaloids and counting, it is just what one expects.
Good luck and hope you get to sleep.
