Paracetamol / Codeine / Caffeine / Doxylamine

Brands of Paracetamol / Codeine / Caffeine / Doxylamine in Kenya

Betapyn® ,Adcock Ingram Ltd.

Fopyn®, Signature Healthcare Ltd

Pynstop® , Adcock Ingram Ltd.

Syndol®, Adcock Ingram Ltd.

Tamepyn® , Biopharma Ltd

MODE OF ACTION

Paracetamol

Paracetamol has a central analgesic effect that is mediated through activation of descending serotonergic pathways. Debate exists about its primary site of action, which may be inhibition of prostaglandin (PG) synthesis or through an active metabolite influencing cannabinoid receptors

Codeine

The precise mechanism of action of codeine is not known; however, like morphine, codeine binds to receptors in the brain (opioid receptors) that are important for transmitting the sensation of pain throughout the body and brain.

Caffeine

Caffeine increases intracellular concentrations of cyclic adenosine monophosphate (cAMP) by inhibiting phosphodiesterase enzymes in skeletal muscle and adipose tissues. These actions promote lipolysis via the activation of hormone-sensitive lipases with the release of free fatty acids and glycerol.

Doxylamine

As a member of the first-generation class of antihistamines, doxylamine exerts its effects by competitively antagonizing the binding of free histamine at the H1-receptor binding sites. It antagonizes the effects of histamine in the uterus, GI tract, large blood vessels, and bronchial muscles

INDICATIONS

For the short term treatment of acute moderate pain which is not relieved by paracetamol, ibuprofen or aspirin alone such as headache, tension headache, migraine, neuralgia, toothache, dysmenorrhoea, muscular and rheumatic aches and pains and post-operative analgesia following surgical or dental procedures.

Codeine is indicated in patients older than 12 years of age for the treatment of acute moderate pain which is not considered to be relieved by other analgesics such as paracetamol or ibuprofen (alone).

DOSAGE AND ADMINISTRATION

The duration of treatment should be limited to 3 days and if no effective pain relief is achieved the patients/carers should be advised to seek the views of a physician. Do not take continuously for more than 3 days without consulting your doctor.

Adults

One or two tablets every four to six hours as needed for relief. Total dosage over a 24 hour period should not normally exceed eight tablets.

Elderly and debilitated

Codeine should be used with caution in the elderly and debilitated patients as they may be more susceptible to the respiratory depressant effects.

Paediatric population

Children aged less than 12 years:

Codeine should not be used in children below the age of 12 years because of the risk of opioid toxicity due to the variable and unpredictable metabolism of codeine to morphine .

Children aged 16 years to 18 years

One to two tablets every 6 hours when necessary up to a maximum of 8 tablets in 24 hours.

Children aged 12 years to 15 years

One tablet every six hours when necessary to a maximum of 4 tablets in 24 hours

CONTRAINDICATIONS

Hypersensitivity to paracetamol, codeine or other opioid analgesics, doxylamine succinate, caffeine, or any of the other constituents.

Due to interaction with the doxylamine succinate component, the concomitant use of this drug with monoamine inhibitors (MAOIs) or within 14 days of stopping treatment with these medicines is contraindicated, as there is a risk of serotonin syndrome.

Conditions where morphine and opioids are contraindicated e.g:

  • Acute asthma (during an attack)
  • Acute respiratory depression and in chronic obstructive pulmonary disease
  • Acute alcoholism
  • Head injuries
  • Raised intra-cranial pressure
  • Following biliary tract surgery
  • Risk of paralytic ileus
  • Breast-feeding

In all paediatric patients (0-18 years of age) who undergo tonsillectomy and/or adenoidectomy for obstructive sleep apnoea syndrome due to an increased risk of developing serious and life-threatening adverse reactions .

In patients for whom it is known that they are CYP2D6 ultra-rapid metabolisers.

DRUG INTERACTION

The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by cholestyramine.

The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular daily use of paracetamol with increased risk of bleeding; occasional doses have no significant effect.

This may enhance the sedative effects of CNS depressants such as alcohol, barbiturates, anaesthetics, hypnotics, other opioid analgesics, anxiolytic sedatives, antipsychotics, tricyclic antidepressants and phenothiazines, resulting in increased CNS depression. It may also have an additive antimuscarinic action with other drugs, such as atropine and some antidepressants.

Benzodiazepines

The concomitant use of opioids with sedative medicines such as benzodiazepines or related drugs increases the risk of sedation, respiratory depression, coma and death because of additive CNS depressant effect. The dosage and duration of concomitant use should be limited .

Alcohol and opioids

The concomitant use of alcohol and opioids increases the risk of sedation, respiratory depression, coma, and death because of additive CNS depressant effect. Concomitant use with alcohol is not recommended .

The hypotensive actions of diuretics and anti-hypertensive agents may be potentiated when used concurrently with opioid analgesics. Concurrent use of hydroxyzine with codeine may result in increased analgesia as well as increased CNS depressant and hypotensive effects.

The respiratory depressant effect caused by neuromuscular blocking agents may be additive to the central respiratory depressant effects of opioid analgesics. Quinidine can inhibit the analgesic effect of codeine.

Concurrent use of codeine with antidiarrhoeal and antiperistaltic agents such as loperamide and kaolin may increase the risk of severe constipation. Concomitant use of antimuscarinics or medications with antimuscarinic action may result in an increased risk of severe constipation which may lead to paralytic ileus and/or urinary retention.

Codeine may delay the absorption of mexiletine and thus reduce the antiarrhythmic effect of the latter. Codeine may antagonise the gastrointestinal effects of metoclopramide, cisapride and domperidone. Cimetidine inhibits the metabolism of opioid analgesics resulting in increased plasma concentrations.

Naxolone antagonises the analgesic, CNS and respiratory depressant effects of opioid analgesics. Naltrexone also blocks the therapeutic effect of opioids.

Doxylamine: Monamine oxidase inhibitors (MAOIs) or within 14 days of stopping treatment with these products as there is a risk of serotonin syndrome .

Concomitant administration of pethidine and possibly other opioid analgesics to patients taking MAOIs has been associated with very severe and sometimes fatal reactions such as severe CNS excitation or depression, including hypertension or hypotension. Although this has not been documented with codeine, it is possible that a similar interaction may occur and therefore the use of codeine should be avoided while the patient is taking MAOIs and for 2 weeks after MAOI discontinuation.

Incompatibilities: Codeine has been reported to be incompatible with phenobarbitone sodium forming a codeine-phenobarbitone complex, and with potassium-iodide, forming crystals of codeine periodide. Acetylation of codeine phosphate by aspirin has occurred in solid dosage forms containing the two drugs, even at low moisture levels.

Interference with laboratory tests: Opioid analgesics interfere with a number of laboratory tests including plasma amylase, lipase, bilirubin, alkaline phosphatase, lactate dehydrogenase, alanine aminotransferase and aspartate aminotransferase. Opioids may also interfere with gastric emptying studies as they delay gastric emptying and with hepatobiliary imaging using technetium Tc 99m disofenin as opioid treatment may cause constriction of the sphincter of Oddi and increase biliary tract pressure.

The metabolism of paracetamol is possibly accelerated by carbamazepine, phenytoin, phenobarbital, primidone (also there have been isolated reports of hepatotoxicity)”

ADVERSE EFFECTS

Adverse effects of doxylamine succinate:

Common side effects:

CNS effects: Drowsiness (usually diminishes within a few days), paradoxical stimulation, headaches, psychomotor impairment.

Antimuscarinic effects: Urinary retention, dry mouth, blurred vision, gastrointestinal disturbances, thickened respiratory tract secretions

Rare side effects:

Hypotension, extrapyramidal effects, dizziness, confusion, depression, sleep disturbances, tremor, convulsions, palpitation, arrhythmia hypersensitivity reactions, blood disorders and liver dysfunction.

Adverse effects of paracetamol:

Blood and lymphatic system disorders

Very rare: thrombocytopenia

Not known: agranulocytosis

Immune system disorders

Hypersensitivity including skin rash may occur.

Not known: Anaphylactic shock, angioedema.

Skin and subcutaneous tissue disorders

Very rare cases of serious skin reactions have been reported.

Adverse effects of Codeine:

The most frequent undesirable effects of codeine are constipation and drowsiness. Less frequent effects are nausea, vomiting, sweating, facial flushing, dry mouth, blurred or double vision, dizziness, orthostatic hypotension, malaise, tiredness, headache, anorexia, vertigo, bradycardia, palpitations, respiratory depression, dyspnoea, allergic reactions (itch, skin rash, facial oedema) and difficulties in micturition (dysuria, increased frequency, decrease in amount). Side effects, which occur rarely, include convulsions, hallucinations, nightmares, uncontrolled muscle movements, muscle rigidity, mental depression and stomach cramps. Very rare cases of pancreatitis have been reported.

Regular prolonged use of codeine is known to lead to addiction and symptoms of restlessness and irritability may result when treatment is stopped. Prolonged use of a painkiller for headaches can make them worse.

Adverse effects of Caffeine:

Side-effects include nausea, headache, insomnia, irritability and symptoms of anxiety neurosis. Large doses may cause restlessness, excitement, muscle tremor, tinnitus, scintillating scotoma, tachycardia and extrasystoles. Caffeine increases gastric secretions and may cause gastric ulceration.

Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:

Paracetamol / Codeine / Caffeine / Doxylamine in Kenya
Paracetamol / Codeine / Caffeine / Doxylamine in Kenya
Paracetamol / Codeine / Caffeine / Doxylamine in Kenya
Paracetamol / Codeine / Caffeine / Doxylamine in Kenya
Betapyn in Kenya
Betapyn prices in Kenya
Betapyn alternatives : Tamepyn, Pynstop, Syndol

Clinical | Pharmacokinetic data

Pregnancy Category: Not Recommended
Routes of Administration: Oral
Bioavailability:
Protein Binding:
Metabolosim:
Onset of Action:
Elimination Half life:
Excretion:

Legal Status | Dosage forms & Strengths

Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This is a controlled Schedule 1 Drug ,Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:

Drug Indentifiers:


Drug Images

References/ Citation:

What was the patient being treated for