Chlorphenamine Maleate/ Phenylephrine Hydrochloride

Registered South African indications:

• Relief of nasal congestion and other symptoms associated with sinusitis, hay fever, nasal allergies or other respiratory allergies

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of the excipients in this combination product
• Children under 2 years of age
• Patients receiving monoamine oxidase inhibitors or within 14 days of termination of such treatment
• Pregnancy
• Lactation
• Severe hypertension
• Ischaemic heart disease

South African recommendations

Monitoring for renal or hepatic impairment

• Medical monitoring is necessary for patients with impaired renal or hepatic function. Adverse events related to propylene glycol, such as renal dysfunction (including acute tubular necrosis), acute renal failure, and liver dysfunction, have been reported

Elderly patients

• Higher susceptibility to dizziness, sedation, confusion, hypotension, and anticholinergic effects (e.g., dry mouth, urinary retention)

Use with caution in certain conditions

• Hyperthyroidism
• Cardiovascular disease (arrhythmia, tachycardia)
• Occlusive vascular disorders (arteriosclerosis, hypertension, aneurysms)
• Diabetes mellitus
• Closed-angle glaucoma
• Prostatic hypertrophy
• Phaeochromocytoma
• Emphysema or chronic bronchitis
• Porphyria
• Epilepsy
• During an acute asthma attack

Limited duration of use

• Should not be used for more than 7 days
• After 5 to 7 days tachyphylaxis may occur and the product loses effect

Consultation if symptoms persist

• Seek medical advice if symptoms persist or are accompanied by fever

Risks of exceeding recommended dosage

• Overdose can lead to nervousness, dizziness, insomnia, tremors, or cardiac arrhythmia
• Such symptoms can also occur in sensitive individuals even at lower doses

Potential adverse effects

• May cause paradoxical hyperexcitability, nervousness, irritability, and insomnia

Long-term use and oral health

• Prolonged use of antihistamines may reduce salivary flow, potentially leading to dental caries, periodontal disease, oral candidiasis, and oral discomfort

Impact on diabetes mellitus

• Contains sucrose, which may have an effect on the glycaemic control of patients with diabetes mellitus

Hereditary conditions

• Not suitable for patients with rare hereditary conditions like fructose intolerance, glucose-galactose malabsorption, or sucrase-isomaltase insufficiency

Risk in young children

• Co-administering with substrates for alcohol dehydrogenase, like ethanol, may cause adverse effects in children under 5 years old

Ability to drive and use machines

• This medication can cause drowsiness and reduced concentration
• These effects may worsen with alcohol or CNS depressants like sedatives and tranquillisers
• Exercise caution when driving, operating machinery, or performing tasks that require high concentration, as impaired focus could lead to accidents

Forms avail. in SA and covered in this monograph: syr

South African registered indications and dosages

Relief of nasal congestion and other symptoms associated with sinusitis, hay fever, nasal allergies or other respiratory allergies

Chlorphenamine Maleate/ Phenylephrine Hydrochloride
1.25/2.5 (mg)

• Oral (syr): 10ml, 3-4hrly; Max duration: 7 days

---

Chlorphenamine maleate/ phenylephrine hydrochloride syrup should not be taken for more than 7 days. After 5-7 days tachyphylaxis may occur and the product loses effect

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

South African registered indications and dosages

Relief of nasal congestion and other symptoms associated with sinusitis, hay fever, nasal allergies or other respiratory allergies

Chlorphenamine Maleate/ Phenylephrine Hydrochloride
1.25/2.5 (mg)

• Younger than 2 years: Contraindicated
• Between 2-3 years: Oral (syr): 2.5-5ml, 3-4hrly; Max duration: 7 days
• Between 3-6 years: Oral (syr): 5-10ml, 3-4hrly; Max duration: 7 days
• Older than 6 years: See adult dosage

---

Chlorphenamine maleate/ phenylephrine hydrochloride syrup should not be taken for more than 7 days. After 5-7 days tachyphylaxis may occur and the product loses effect

---

Co-administration with any substrate for alcohol dehydrogenase such as ethanol may induce adverse effects in children less than 5 years old

---

See additional prescribing points for precautions in paediatrics

Pregnancy 

South African recommendations

• Contraindicated
• Phenylephrine is best avoided in pregnancy, because of the potential promotion of uterine contractility and peripheral vasoconstriction, with the possibility of foetal hypoxia

Breastfeeding

South African recommendations

• Contraindicated
• Chlorphenamine maleate may inhibit lactation due to anticholinergic effects. Small amounts of antihistamines entering breast milk may cause drowsiness or excitement and/ or irritability in infants

Fertility

South African recommendations

• No information available

South African recommendations

• Caution; no dose adjustment recommended

South African recommendations

• Caution; no dose adjustment recommended

South African recommendations

• Caution; dose adjustment recommended
  Dose reduction may be required
  Elderly patients are especially susceptible to dizziness, sedation, confusion, hypotension and anticholinergic effects such as dry mouth and urinary retention

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

Chlorphenamine Maleate

Central Nervous System Disorders

• Sedation
• Dizziness
• Fatigue
• Lassitude
• Incoordination
• Tremors
• Confusion
• Blurred vision
• Diplopia
• Tinnitus
• Euphoria
• Nervousness
• Tingling and weakness of the hands
• Irritability
• Nightmares
• Insomnia
• Hallucinations
• Convulsions

Anticholinergic Effects

• Dryness of the mouth and respiratory passages
• Thickening of mucous
• Cough
• Increased sweating
• Urinary retention or frequency
• Dysuria
• Headache
• Tight chest
• Palpitations
• Tachycardia
• Hypotension

Gastrointestinal Disturbances

• Loss of appetite
• Nausea
• Vomiting
• Epigastric distress
• Diarrhoea
• Reduction in tone and motility of the gastrointestinal tract, leading to gastric reflux and constipation

Hypersensitivity Reactions

• Allergic dermatitis
• Drug fever
• Photosensitisation

Blood Disorders

• Agranulocytosis
• Haemolytic anaemia
• Leukopenia
• Thrombocytopenia

Phenylephrine Hydrochloride

Central Nervous System Disorders

• Insomnia
• Fear
• Anxiety
• Restlessness
• Tremor
• Confusion
• Irritability
• Weakness
• Psychotic states

Gastrointestinal Disorders

• Nausea
• Vomiting
• Reduced appetite

Cardiovascular Disorders

• Vasoconstriction leading to hypertension
• Potential for cerebral hemorrhage
• Pulmonary edema
• Tachycardia or bradycardia
• Cardiac arrhythmias
• Palpitations
• Cardiac arrest
• Hypotension with dizziness and fainting
• Flushing
• Anginal pain (may be precipitated in patients with angina pectoris)

Renal and Urinary Disorders

• Difficulty in micturition
• Urinary retention

Respiratory Disorders

• Dyspnoea

Metabolic Disorders

• Altered metabolism, including disturbances of glucose metabolism

Other

• Sweating
• Hypersalivation
• Common occurrences of headache

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

Chlorphenamine Maleate/ Phenylephrine Hydrochloride

• Monoamine oxidase inhibitors
• Cardiac glycosides
• Quinidine
• Antihypertensives
• Alpha- and beta-blockers
• Guanethidine
• Reserpine
• Tricyclic antidepressants
• Digoxin
• Alpha-methyldopa
• Cyclopropane
• Halothane
• Other halogenated anaesthetics
• Ototoxic agents
• Aminoglycosides

Chlorphenamine Maleate

• Sedatives
• Alcohol
• Tricyclic antidepressants
• Maprotiline
• Monoamine oxidase inhibitors 
• Anticholinergic agents

Other interactions

• Skin testing procedures (See additional prescribing points)

None routine. Specific cases may require

• Renal function
• Hepatic function

Skin testing procedures

• The use of chlorpheniramine maleate/ phenylephrine hydrochloride should be discontinued several days prior to skin testing procedures since chlorphenamine maleate may prevent or diminish otherwise positive reactions to dermal reactivity indicators

Paediatric precautions

• Not recommended in newborn or premature infants. This age group has an increased susceptibility to anticholinergic side effects such as central nervous system excitation and an increased tendency towards convulsions
• Do not administer to children who have breathing problems such as chronic bronchitis, or who have glaucoma without prior consultation with a healthcare provider
• May induce drowsiness, which can be intensified by sedatives and tranquillisers
• Do not give this product to children who are taking sedatives and tranquillisers, without first consulting the child’s doctor

Chlorphenamine Maleate

Chlorphenamine maleate is a histamine H1 receptor antagonist that competes reversibly with histamine for H1 receptor sites on effector cells. It suppresses those symptoms due to histamine release. Antihistamines have anticholinergic properties and have a drying effect on the nasal mucosa.

Phenylephrine Hydrochloride

Phenylephrine hydrochloride is a sympathomimetic agent with mainly direct effects on adrenergic receptors. It has predominantly alpha-adrenergic activity and is without significant stimulating effects on the central nervous system at usual doses. Its pressor activity is weaker than that of ephedrine.

COMBINATION PREPARATIONS

Phenylephrine/ Chlorpheniramine

Chlorphenamine Maleate/ Phenylephrine Hydrochloride

Syrup (per 5ml) 1.25mg/2.5mg

• Demazin (iNova Pharmaceuticals) originator