PHOLCODINE

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Created Dec 2020

PHOLCODINE

  • [COPHOLCO]
  • [ADAPHOL]
  • [CODISOL]
  • [LANTUSS]
  • [PHOLCOLIN]

Morpholinylethylmorphine | Homocodeine

DEA CODE 9314: Schedule 1 Narcotic

Pholcodine is not prescribed in the United States

Pholcodine is an opioid that has been widely used worldwide since 1950 for the treatment of non-productive cough in children and adults. Illicit drug. Additionally Pholcodine is a marker for sensitization to neuromuscular blocking agents (NMBA) and is intended for use as a diagnostic tool in NMBA-induced anaphylaxis.

What pholcodine is used for:

  • Pholcodine is used to relieve dry coughs.
  • Pholcodine is a cough suppressant that works selectively on the cough centre in the brain to control and help stop coughing.
  • Pholcodine does not cause an excited state when taking the recommended dose. There is no evidence of physical dependence after prolonged use.
  • There may be more than one active ingredient in your medicine, such as an anti-inflammatory, an antiseptic, a nasal decongestant or an antihistamine. If you are taking more than one cough and cold medicine, please read the packaging of each medicine carefully to ensure you are not taking the same active ingredient from 2 or more medicines. Taking the same active ingredient from more than one medicine could mean you are taking too much of that active ingredient.

Suppressing a dry, tickly, irritating, persistent cough, where you're not coughing up phlegm.

How does it work?
Galenphol linctus contains the active ingredient pholcodine (5mg per 5ml), which is a type of medicine called a cough suppressant. It works by blocking the cough reflex.

Coughing is a reflex response to irritation of the airways. It's normally useful for clearing mucus, dust and other particles from the throat and lungs. However, sometimes, coughing can become overstimulated even when there is no mucus to clear from the lungs or throat. In this situation coughing serves no purpose and can become painful and frustrating.

Pholcodine reduces the nerve signals that are sent from a part of the brain called the coughing centre to the muscles that produce coughing. This reduces the urge to cough and can be used to block the cough reflex in situations where the cough serves no purpose, ie when no plegm is being coughed up.

Contraindications:

  • Pholcodine should not be given to subjects in or at risk of developing respiratory failure as the sedative properties of pholcodine may exacerbate the condition.
  • Patients with chronic bronchitis, COPD, bronchiolitis or bronchiectasis due to sputum retention
  • Patients taking monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping such treatment (see also section 4.5).
  • Patients with hypersensitivity or idiosyncratic response to pholcodine or to any of the excipients.
  • Patients with liver disease since pholcodine is metabolised in the liver and the drug may accumulate.
  • Not to be used in children under the age of 6 years.

EMC PDF Pholcodine

What are pholcodine's side effects?

Side effects could include:

  • Nausea
  • Vomiting
  • Dizziness
  • Constipation
  • Drowsiness
This is not a complete list of side effects. It's essential that you call your doctor should you notice any severe or odd side effects.

What are the overdose symptoms?

Call a doctor or the ambulance immediately if you notice the following symptoms:

  • Restlessness
  • Excitement
  • Breathing difficulties
  • Inability to coordinate muscle movements (ataxia)

Action:
Description: Pholcodine is an antitussive agent that acts primarily on the CNS, causing depression of the medullary cough centre. It has mild sedative effect with little or no analgesic action.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 4-8 hours.
Distribution: Volume of distribution: 30-49 L/kg. Plasma protein binding: 23.5%.
Metabolism: Metabolised in the liver, with little conjugation. No transformation to morphine.
Excretion: Elimination half-life: 32-43 hours.

Food Interaction:
Increased CNS effects with alcohol.

The Pharmacology of Pholcodine (1961):

  1. Pholcodine is an amino-alkylether of morphine resulting from the replacement of phenolic hydrogen by a morpholylethyl radical.
  2. The acute toxicity of pholcodine when administered to rats, mice and dogs is low and, except when administered orally to rats, is lower than that of codeine.
  3. Continued experiments with rats show the absence of any toxic action and of sensibilization phenomena after repeated doses.
  4. The clinic has established that pholcodine does not cause drug-addiction.
  5. Pholcodine administered intravenously lowers arterial pressure in a normo-tensive dog. Only a small part of this action is of central origin. It is due essentially to a peripheric vaso-dilation and to a freeing of histaminic substances. It is not of a cholinergic nature.
  6. Pholcodine differs from morphine and codeine in that it does not depress the respiratory volume or amplitude in dogs. On the contrary, it increases the amplitude and the respiratory volume per minute.
  7. Unlike morphine and codeine, pholcodine produces no intestinal spasm, and decreases neither the amplitude nor the peristaltic tonus in dogs. In rats the depressant action of the propulsive intestinal activity of pholcodine is ten times lower than that of morphine.
  8. Pholcodine has almost no analgesic action.
  9. Pholcodine is an anti-tussive like codeine and morphine.
  10. Pholcodine does not cause tail catatonus in mice, nor morphinic madness in cats.
  11. Pholcodine is an anti-convulsant, unlike morphine, codeine and morphine derivatives, which are all convulsants.
  12. Pholcodine responds positively to certain tests for ataraxics.

To sum up, pholcodine, as compared with morphine, appears, when administered in therapeutic doses, not to have any central stimulant action.

2010:
Pholcodine is an opiate with central antitussive action used for treatment of cough and cold symptoms in children and adults.

  • The first clinical studies on efficacy of pholcodine as an antitussive agent are dated 1950.
  • Pholcodine has been marketed for decades in the European Union.
  • Literature has been published suggesting a link between pholcodine consumption and cross sensitisation to NMBAs, resulting in anaphylactic reactions during surgery.
  • There has been extensive use of pholcodine-containing products over the course of several decades, which has allowed the collection of relevant safety data. The majority of the adverse events reported in clinical trials, literature and post-marketing experience are gastrointestinal disorders and psychiatric disorders, which are adverse events known and commonly reported with opiates. The existent data seems to indicate that pholcodine is at least as safe as codeine, with the advantage that it does not share the same potential for addiction.
  • CHMP concluded that the evidence of a link between pholcodine and NMBA-related anaphylaxis is circumstantial, not entirely consistent and does not support the conclusion that there is a significant risk of cross-sensitisation to NMBAs and subsequent development of anaphylaxis during surgery. Further data needs to be generated to clarify the possibility of an association between pholcodine use and NMBA-related anaphylaxis.
EMA PDF Pholcodine Annex II

EMA PDF Pholcodine Annex I

2012:
The Committee reviewed the available data on the safety and efficacy of pholcodine, particularly the data in support of a link between pholcodine use and development of NMBA-related anaphylaxis. The Committee considered that evidence of an association between pholcodine use and development of NMBA-related anaphylaxis is circumstantial, not entirely consistent and therefore does not support the conclusion that there is a significant risk of cross-sensitisation to NMBAs and subsequent development of anaphylaxis during surgery. The Committee also considered that data from clinical trials and extensive post marketing use has demonstrated the efficacy of pholcodine in the treatment of non productive cough. The Committee therefore concluded that, based on currently available data, the benefit-risk balance of pholcodine-containing products in the treatment of non-productive cough is positive under normal conditions of use.

EMA PDF Pholcodine

2012:
This review has illustrated that there remains considerable uncertainty regarding the validity of the 'pholcodine hypothesis' which suggests that consumption of pholcodine containing cough medicines increases the risk of NMBA-related anaphylactic reactions during surgery. Taken as a whole, the evidence for this hypothesis remains inconclusive and a causative link between the effects of pholcodine and differential rates of NMBA-associated anaphylaxis across international borders has not been established. Unless further evidence of causation is forthcoming, calls for restrictions on the availability of widely used cough medicines containing pholcodine cannot be justified.

SelfCare PDF Pholcodine

Pholcodine, also known as folcodina or ethnine, belongs to the class of organic compounds known as morphinans. Pholcodine is a very strong basic compound (based on its pKa). Pholcodine activity is the suppression of unproductive cough and it also has a mild sedative effect with little or no analgesic effects. Pholcodine is not prescribed in the United States where it is classed as a Schedule I drug. The therapeutic doses of pholcodine have been shown not to cause depression of respiration, CNS excitation or other side effects associated with narcotics.

Why is pholcodeine super duper illegal in the US?

  • It's not abusable, it's very hard to overdose, it has a use in a cough syrup (in as much as any cough syrup works), as far as I know it's not easy to chemically change into something more "interesting" - why is pholocodeine a schedule 1 chemical? Just cause it has the word codeine in it?
    • a real baffler of a schedule 1 drug. I've read some WHO studies where they gave this to addicts in WD in various doses and zip zero effect.
      • WHO has done studies where they gave pholcodine to druggies and opiate addicts in WD, none reported any effect or relief at any dose. I did some quick checking on druggie forums on the internet, no one claims any kind of narcotic effect from pholcodine, thats pretty remarkable. I can't find one claim that pholcodine produced any kind of effect.

Pholcodine is used as an antitussive agent in Australia, Belgium, Finland, France, Ireland, New Zealand, Norway, and the UK. It is a class B substance in the United Kingdom but can be purchased over-the-counter in most UK pharmacies. Pholcodine is not prescribed in the United States where it is classed as a Schedule I drug

  • An opioid cough suppressant (antitussive)
  • It helps suppress unproductive coughs
  • Has a mild sedative effect
  • Little or no analgesic effects
  • Found in cough lozenges and more commonly as an oral solution, typically 5 mg / 5 ml.
  • Adult dosage is 5-10 ml up to 3-4 times daily.

    Pholcodine now largely replaces the previously more common codeine linctus, as it has a much lower potential for dependence.

  • It acts primarily on the central nervous system (CNS), causing depression of the cough reflex, partly by a direct effect on the cough centre in the medulla.
  • It is metabolized in the liver and its action may be prolonged in individuals with hepatic insufficiency (i.e. liver problems). Its use is therefore contraindicated in patients with liver disease, while care is advised in patients with hepatic impairment.
  • Average half-life of approximately 2.3 days
  • Side effects are rare and may include dizziness and gastrointestinal disturbances such as nausea or vomiting. Adverse effects such as constipation, drowsiness, excitation, ataxia and respiratory depression have been reported occasionally or after large doses.

    The primary safety concerns with pholcodine revolve around death during general anaesthesia.

Administration of pholcodine causes production of antibodies linked with fatalities during surgery, when essential neuromuscular blocking agents (NMBAs) are administered to prevent patient movement under general anaesthesia. These antibody levels gradually fall to low levels several years after last dose of pholcodine. However, the presence of these antibodies causes a 300-fold increase in risk of anaphylaxis during anaesthesia. The link was suspected when neighbouring Norway and Sweden were found to have tenfold differences of surgical anaphylaxis deaths. Sweden had no products approved containing pholcodine, whereas 40% of the population in Norway had consumed the single approved pholcodine product. Norway withdrew pholcodine from the market in 2007, and the prevalence of anti-suxamethonium antibodies fell by over 80% in two years. A corresponding fall in anaesthesia deaths followed.

  
Researchers link common cough medicines such as Day Nurse to lethal allergic reactions in patients undergoing surgery - Experts suspect that when pholcodine, a cough suppressant that is found in popular products such as Day Nurse and some Covonia syrups, is combined with certain anaesthesia drugs, it sets off a ...
Saturday January 28, 2023 - dailymail.co.uk

Duro-Tuss Dry Cough Liquid plus Nasal Decongestant - Pholcodine works on the cough centre in the brain to control and stop coughing. Ask your pharmacist or doctor if you have any questions about this medicine. severe asthma, bronchitis or other ...
Monday January 06, 2020 - news-medical.net

EU bans cough syrup chemical over severe allergies - Cough medicines containing the chemical pholcodine should be banned due to the risk of potentially deadly allergic reactions in people under general anaesthetic, the European Union's drug ...
Thursday December 01, 2022 - timesofmalta.com

  
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