Paracetamol/ Phenylephedrine/ Chlorpheniramine/ Caffeine

Registered South African indications:

• Colds and flu

Combination products may have additional pharmacological effects not accounted for by the action of the individual ingredients

Paracetamol
Contraindications

• Hypersensitivity to the active ingredient or any of the excipients in this combination product
• Severe hepatic impairment

Cautions

• Pregnancy
• Renal impairment
• Mild to moderate hepatic impairment

Phenylephrine
Contraindications

• Hypersensitivity to the active ingredient or any of the excipients in this combination product
• Cardiovascular disease
• Hypertension
• Diabetes mellitus
• Closed angle glaucoma
• Hyperthyroidism
• Prostatic hypertrophy
• Phaeochromocytoma
• Coadministration with monoamine oxidase inhibitors or within 14 days of use

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Occlusive vascular disease
• Prolonged use

Chlorpheniramine
Contraindications

• Hypersensitivity to the active ingredient or any of the excipients in this combination product
• Premature infants 
• Neonates 
• Coadministration with monoamine oxidase inhibitors or within 14 days of their use

Cautions

• Breastfeeding
• Renal impairment 
• Hepatic impairment 
• Elderly
• Narrow angle glaucoma 
• Urinary retention 
• Prostatic hypertrophy 
• Severe hypertension and cardiovascular disease 
• Bronchitis 
• Bronchiectasis 
• Asthma 
• Epilepsy 
• Acute exacerbation of asthma 
• May impair ability to drive and operate machinery 

Caffeine
Contraindications 

• Hypersensitivity to the active ingredient or any of the excipients in this combination product

Cautions 

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Anxiety 
• Cardiovascular disease
• History of peptic ulcer
• Gastroesophageal reflux
• History of seizure disorder
• Neonates
• Concommitant use with transcutaneous electrical nerve stimulation

Forms avail. in SA and covered in this monograph: tab, cap

Symptomatic relief of colds and flu 
- Nasal congestion
- Vasomotor rhinitis
- Sinusitis
- Hayfever
- Mild to moderate pain

Paracetamol/ Phenylephrine/ Chlorpheniramine/ Caffeine
200/5/2/30 (mg)

• Oral (cap): 1-2 cap, 6hrly

150/10/4/37.5 (mg)

• Oral (tab): 1-2 tab, 8hrly

150/5/2/15 (mg)

• Oral (tab): 2 tab, 8hrly

200/6/2/20 (mg) 

• Oral (tab): 2 tab, 4hrly 

Paed. forms avail. in SA and covered in this monograph: tab, syr

Symptomatic relief of colds and flu 
- Nasal congestion
- Vasomotor rhinitis
- Sinusitis
- Hayfever
- Mild to moderate pain

Paracetamol/ Phenylephrine/ Chlorpheniramine/ Caffeine 
75/2.5/2/7.5 (mg)

• Younger than 1 year: Not established for use
• Between 1-3 years: Oral (syr): 2.5ml, 8hrly
• Between 3-6 years: Oral (syr): 5ml, 8hrly
• Between 6-12 years: Oral (syr): 10ml, 8hrly
• Older than 12 years: Not established for use

150/5/2/50 (mg) 

• Younger than 6 years: Not established for use
• Between 6-12: Oral (tab): 1 tab, 8hrly
• Older than 12 years: See adult dosage 

Recommendations for this combination product as per highest risk category when comparing individual active ingredients

Pregnancy

• Caution; not recommended (Chlorpheniramine, Phenylephrine, Caffeine)

Breastfeeding

• Caution; not recommended  (Phenylephrine, Chlorpheniramine, Caffeine)

Renal impairment

• Mild to moderate: Caution; no dose adjustment recommended (Paracetamol, Phenylephrine, Caffeine, Chlorpheniramine)
• Severe: Contraindicated (Paracetamol)

Hepatic impairment

• Mild to moderate: Caution; no dose adjustment recommended (Paracetamol, Chlorpheniramine)
• Severe: Contraindicated (Paracetamol)

Elderly

• Caution; dose adjustment recommended (Chlorpheniramine)

Porphyria Information

• Not yet classified (NC) 

Drugs in Sport

• Permitted - No warning 

Combination products may have additional pharmacological effects not accounted for by the action of the individual ingredients

Paracetamol
Respiratory Disorders

• Bronchospasm

Hepatobiliary Disorders

• Hepatic dysfunction

Immune, Blood and Lymphatic System Disorders

• Anaphylaxis
• Cutaneous hypersensitivity reactions 
• Angiodema
• Stevens Johnson syndrome
• Thrombocytopenia 
• Agranulocytosis
• Methaemoglobinaemia

Phenylephrine
Central Nervous System Disorders

• Headache

Cardiovascular Disorders

• Tachycardia
• Cardiac arrhythmia
• Palpitations
• Hypertension

Gastrointestinal Disorders

• Nausea and vomiting

Genitourinary Disorders

• Urinary retention

Chlorpheniramine
Central Nervous System Disorders

• Sedation
• Seizures
• Disturbances in attention
• Abnormal co-ordination
• Dizziness
• Headache
• Depression
• Nightmares
• Paradoxical stimulation

Cardiovascular Disorders 

• Palpitations
• Tachycardia
• Arrhythmias
• Hypotension

Respiratory Disorders

• Thickening of bronchial secretions
• Tight chest

Gastrointestinal Disorders

• Nausea and vomiting
• Dry mouth
• Abdominal pain
• Diarrhoea
• Constipation
• Dyspepsia

Hepatobiliary Disorders 

• Hepatitis
• Jaundice

Genitourinary Disorders

• Urinary retention
• Dysuria

Endocrine and Metabolic Disorder

• Anorexia
• Increased appetite

Musculoskeletal Disorders

• Muscle twitching
• Muscle weakness

Skin and Subcutaneous Tissue Disorders 

• Exfoliative dermatitis
• Rash
• Urticaria
• Photosensitivity

Immune, Blood and Lymphatic System Disorders 

• Haemolytic anaemia
• Blood dyscrasias
• Allergic reaction
• Angioedema
• Anaphylactic reactions

Sensory Disorders 

• Blurred vision
• Tinnitis

Caffeine
Central Nervous System Disorders

• Agitation
• Delirium
• Dizziness
• Hallucination
• Headache
• Insomnia
• Irritability
• Psychosis
• Restlessness

Cardiovascular Disorders

• Angina
• Chest pain
• Flushing
• Palpitations
• Sinus tachycardia
• Supraventricular tachycardia
• Vasodilarion
• Ventricular arrhythmis

Gastrointestinal Disorders

• Esophageal motility disorder
• Gastritis

Genitourinary Disorders

• Diuresis

Musculoskeletal Disorders

• Fasciculations

Skin and Subcutaneous Tissue Disorders

• Urticaria

Sensory Disorders

• Increased intraocular pressure
• Miosis

Combination products may have additional pharmacological effects not accounted for by the action of the individual ingredients

Paracetamol

• Metoclopramide 
• Domperidone
• Colestyramine
• Oral anticoagulants
• Chloramphenicol

Phenylephrine

• Monoamine oxidase inhibitors
• Anticholinergic agents
• Digoxin
• Sympathomimetic agents
• Tricyclic antidepressants
• Vasodilating agents
• Beta-blockers
• CYP450 inducers
• Linezolid
• Alcohol

Chlorpheniramine

• Phenytoin
• Monoamine oxidase inhibitors
• Anticholinergic agents
• Antihistamines
• Central nervous system depressants

Caffeine

• Adenosine
• Cocaine
• CYP1A2 inhibitors 
• Linezolid 
• Xanthines

None routine

Paracetamol
Paracetamol increases the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin synthesis. It does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects

Phenylephrine
Phenylephrine is a sympathomimetic agent which acts directly on adrenoreceptors. It has predominantly alpha adrenergic activity and does not cause stimulation of the central nervous system. It produces vasoconstriction which relieves nasal congestion

Chlorpheniramine
Chlorpheniramine acts as a competitive antagonist at H1-receptors. These histamine receptors are present in the respiratory tract, gastrointestinal tract and blood vessels thus allowing chlorpheniramine to perform its role in modulating the immune response and as a decongestant 

Caffeine
Caffeine is a nonspecific adenosine receptor antagonist and acts as a central nervous system stimulant

COMBINATION PREPARATIONS

Paracetamol/ Caffeine/ Phenylephedrine/ Chlorpheniramine

Tablet 150mg/15mg/5mg/2mg

• Grippon cold and flu (Adcock)

Tablet 150mg/37.5mg/10mg/4mg

• Degoran Plus (Novartis) originator

Capsule 200mg/30mg/5mg/2mg

• Histacon (Pharmacare) 

Syrup (per 5ml)  75mg/7.5mg/2.5mg/2.0mg

•  Colcleer Paed Syrup (Adcock)