Phenyltoloxamine
Encyclopedia
Phenyltoloxamine is an antihistamine
with sedative
and analgesic
effects. It is a member of the ethanolamine
class of antihistaminergic agents and an anticholinergic
.
for some analgesics and antitussives (acetaminophen, dihydrocodeine
, codeine
, hydrocodone
). It is widely used in certain parts of the world as cough suppressant usually with codeine, and sometimes by itself or in addition to dextromethorphan
as it, like diphenhydramine
, possesses antitussive action of its own and is particularly useful in semi-productive coughs because of its moderate drying action.
Phenyltoloxamine has analgesic and anti-spasmodic properties of its own and is used in combination with paracetamol
, aspirin
and other salicylates and other drugs in proprietary preparations available over the counter for backache, muscle strains and similar conditions. In this respect, it is similar to a closely related antihistamine, orphenadrine
, and both drugs are very closely related to diphenhydramine
and to doxylamine
, the latter of which is the active ingredient in NyQuil and many other cough preparations.
Phenyltoloxamine is one of the more effective potentiators of codeine and derivatives such as ethylmorphine
, dihydrocodeine
, oxycodone
, nicocodeine
, hydrocodone
and similar drugs like tramadol
and propoxyphene for all indications, pain relief and cough suppression in particular.
Phenyltoloxamine, like diphenhydramine and doxylamine, is an effective non-narcotic anti-tussive on its own but tends to be effective only for productive coughs as the anticholinergic action will exacerbate dry, unproductive coughs, so it is often combined with dextromethorphan
, codeine
, ethylmorphine
, dihydrocodeine
, or hydrocodone
in cough suppressants both over the counter and prescription.
It is also used to discourage abuse
in certain opiate
analgesics due its unpleasant side effects at high doses. While therapeutic doses of phenyltoloxamine can generate mild to moderate euphoria as can many of its close chemical relatives, much higher doses have a side effect profile similar to that of atropine
, which is also used in this fashion for tablets of diphenoxylate
and morphine
for oral administration.
It is not a controlled substance
; however some preparations contain opiates such as codeine or hydrocodone and are controlled. When used in preparations with acetaminophen it is generally over the counter
.
Phenyltoloxamine combinations are sold under wide variety of preparations, brand names and dosages around the world:
Antihistamine
An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
with sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
effects. It is a member of the ethanolamine
Ethanolamine
Ethanolamine, also called 2-aminoethanol or monoethanolamine , is an organic chemical compound that is both a primary amine and a primary alcohol . Like other amines, monoethanolamine acts as a weak base...
class of antihistaminergic agents and an anticholinergic
Anticholinergic
An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine....
.
Common use
Phenyltoloxamine is widely used in preparations as an enhancing agentBiological agent
A biological agent — also called bio-agent or biological threat agent — is a bacterium, virus, prion, or fungus which may cause infection, allergy, toxicity or otherwise create a hazard to human health. They can be used as a biological weapon in bioterrorism or biological warfare...
for some analgesics and antitussives (acetaminophen, dihydrocodeine
Dihydrocodeine
Dihydrocodeine, also called DHC, Drocode, Paracodeine and Parzone and known by the brand names of Synalgos DC, Panlor DC, Panlor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin, Codidol, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DH-Codeine,...
, codeine
Codeine
Codeine or 3-methylmorphine is an opiate used for its analgesic, antitussive, and antidiarrheal properties...
, hydrocodone
Hydrocodone
Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from either of two naturally occurring opiates: codeine and thebaine. It is an orally active narcotic analgesic and antitussive...
). It is widely used in certain parts of the world as cough suppressant usually with codeine, and sometimes by itself or in addition to dextromethorphan
Dextromethorphan
Dextromethorphan is an antitussive drug. It is one of the active ingredients in many over-the-counter cold and cough medicines, such as Robitussin, NyQuil, Dimetapp, Vicks, Coricidin, Delsym, and others, including generic labels. Dextromethorphan has also found other uses in medicine, ranging...
as it, like diphenhydramine
Diphenhydramine
Diphenhydramine hydrochloride is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties which is mainly used to treat allergies. Like most other first-generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason...
, possesses antitussive action of its own and is particularly useful in semi-productive coughs because of its moderate drying action.
Phenyltoloxamine has analgesic and anti-spasmodic properties of its own and is used in combination with paracetamol
Paracetamol
Paracetamol INN , or acetaminophen USAN , is a widely used over-the-counter analgesic and antipyretic . It is commonly used for the relief of headaches and other minor aches and pains and is a major ingredient in numerous cold and flu remedies...
, aspirin
Aspirin
Aspirin , also known as acetylsalicylic acid , is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. It was discovered by Arthur Eichengrun, a chemist with the German company Bayer...
and other salicylates and other drugs in proprietary preparations available over the counter for backache, muscle strains and similar conditions. In this respect, it is similar to a closely related antihistamine, orphenadrine
Orphenadrine
Orphenadrine is an anticholinergic drug of the ethanolamine antihistamine class with prominent CNS and peripheral actions used to treat painful muscle spasms, other similar conditions, as well as the treatment...
, and both drugs are very closely related to diphenhydramine
Diphenhydramine
Diphenhydramine hydrochloride is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties which is mainly used to treat allergies. Like most other first-generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason...
and to doxylamine
Doxylamine
Doxylamine is one of the many sedating antihistamines used by itself as a short-term sedative, and in combination with other drugs as a night-time cold and allergy relief drug...
, the latter of which is the active ingredient in NyQuil and many other cough preparations.
Phenyltoloxamine is one of the more effective potentiators of codeine and derivatives such as ethylmorphine
Ethylmorphine
Ethylmorphine is an opiate narcotic analgesic .Ethylmorphine was invented in Germany at Merck in 1884 and was used as a weaker alternative to heroin for all indications. Chemically, ethylmorphine is a morphine molecule with a -25 group substituted for the aromatic 3- group...
, dihydrocodeine
Dihydrocodeine
Dihydrocodeine, also called DHC, Drocode, Paracodeine and Parzone and known by the brand names of Synalgos DC, Panlor DC, Panlor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin, Codidol, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DH-Codeine,...
, oxycodone
Oxycodone
Oxycodone is an opioid analgesic medication synthesized from opium-derived thebaine. It was developed in 1916 in Germany, as one of several new semi-synthetic opioids in an attempt to improve on the existing opioids: morphine, diacetylmorphine , and codeine.Oxycodone oral medications are generally...
, nicocodeine
Nicocodeine
Nicocodeine is an opiate derivative, closely related to dihydrocodeine and the codeine analogue of nicomorphine developed as a cough suppressant and analgesic. It is not commonly used in most countries, but has activity similar to other opiates. Nicocodeine and nicomorphine were introduced in the...
, hydrocodone
Hydrocodone
Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from either of two naturally occurring opiates: codeine and thebaine. It is an orally active narcotic analgesic and antitussive...
and similar drugs like tramadol
Tramadol
Tramadol hydrochloride is a centrally acting synthetic opioid analgesic used in treating moderate pain. The drug has a wide range of applications, including treatment for restless legs syndrome and fibromyalgia...
and propoxyphene for all indications, pain relief and cough suppression in particular.
Phenyltoloxamine, like diphenhydramine and doxylamine, is an effective non-narcotic anti-tussive on its own but tends to be effective only for productive coughs as the anticholinergic action will exacerbate dry, unproductive coughs, so it is often combined with dextromethorphan
Dextromethorphan
Dextromethorphan is an antitussive drug. It is one of the active ingredients in many over-the-counter cold and cough medicines, such as Robitussin, NyQuil, Dimetapp, Vicks, Coricidin, Delsym, and others, including generic labels. Dextromethorphan has also found other uses in medicine, ranging...
, codeine
Codeine
Codeine or 3-methylmorphine is an opiate used for its analgesic, antitussive, and antidiarrheal properties...
, ethylmorphine
Ethylmorphine
Ethylmorphine is an opiate narcotic analgesic .Ethylmorphine was invented in Germany at Merck in 1884 and was used as a weaker alternative to heroin for all indications. Chemically, ethylmorphine is a morphine molecule with a -25 group substituted for the aromatic 3- group...
, dihydrocodeine
Dihydrocodeine
Dihydrocodeine, also called DHC, Drocode, Paracodeine and Parzone and known by the brand names of Synalgos DC, Panlor DC, Panlor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin, Codidol, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DH-Codeine,...
, or hydrocodone
Hydrocodone
Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from either of two naturally occurring opiates: codeine and thebaine. It is an orally active narcotic analgesic and antitussive...
in cough suppressants both over the counter and prescription.
It is also used to discourage abuse
Drug abuse
Substance abuse, also known as drug abuse, refers to a maladaptive pattern of use of a substance that is not considered dependent. The term "drug abuse" does not exclude dependency, but is otherwise used in a similar manner in nonmedical contexts...
in certain opiate
Opiate
In medicine, the term opiate describes any of the narcotic opioid alkaloids found as natural products in the opium poppy plant.-Overview:Opiates are so named because they are constituents or derivatives of constituents found in opium, which is processed from the latex sap of the opium poppy,...
analgesics due its unpleasant side effects at high doses. While therapeutic doses of phenyltoloxamine can generate mild to moderate euphoria as can many of its close chemical relatives, much higher doses have a side effect profile similar to that of atropine
Atropine
Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade , Jimson weed , mandrake and other plants of the family Solanaceae. It is a secondary metabolite of these plants and serves as a drug with a wide variety of effects...
, which is also used in this fashion for tablets of diphenoxylate
Diphenoxylate
Diphenoxylate is an opioid agonist used for the treatment of diarrhea that acts by slowing intestinal contractions and peristalsis allowing the body to consolidate intestinal contents and prolong transit time, thus allowing the intestines to draw moisture out of them at a normal or higher rate and...
and morphine
Morphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
for oral administration.
Adverse effects
Common adverse effects are those associated with most anticholinergics, effects are more pronounced in children and the elderly.Availability
Phenyltoloxamine is available in most countries, though it is rare in several western countries it remains widely used around the world, particularly in the developing world.It is not a controlled substance
Controlled substance
A controlled substance is generally a drug or chemical whose manufacture, possession, or use are regulated by a government. This may include illegal drugs and prescription medications ....
; however some preparations contain opiates such as codeine or hydrocodone and are controlled. When used in preparations with acetaminophen it is generally over the counter
Over-the-counter drug
Over-the-counter drugs are medicines that may be sold directly to a consumer without a prescription from a healthcare professional, as compared to prescription drugs, which may be sold only to consumers possessing a valid prescription...
.
Phenyltoloxamine combinations are sold under wide variety of preparations, brand names and dosages around the world:
- Ed-Flex, Dologesic, Duraxin, Flextra-650, Novagesic, Pain-gesic, Phenylgesic, Percogesic - North America
- Codipront - Europe/South America
- Codivis - Israel