Chlorpheniramine Maleate

Registered South African indications:

• Conditions responsive to antihistaminic therapy (syr, liq)
• Antitussive (liq)
• Allergic and anaphylactic conditions (tab)

Contraindications

South African recommendations

Oral (tab)

• Epilepsy
• Acute attacks of asthma
• Premature infants and newborn babies
• Safety in pregnancy has not yet been established

Oral (syr)

• In neonates
• Lactation
• Newborn or premature infants
• Epilepsy
• Acute attacks of asthma

Oral (liq)

• Epilepsy
• Premature infants or neonates
• Acute attacks of asthma
• Do not use in children under 2 years of age

Recommendations in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to antihistamines
• Patients who have been treated with monoamine oxidase inhibitors (MAOIs) within the last fourteen days

Cautions

• Pregnancy (syr, liq) (South African recommendations)
  Pregnancy (Recommendations in other jurisdictions)
• Breastfeeding (tab, liq) (South African recommendations)
  Breastfeeding (Recommendations in other jurisdictions)
• Renal impairment
• Hepatic impairment
• Elderly
• Children
• Prostatic hypertrophy
• Severe hypertension and cardiovascular disease
• Bronchitis
• Bronchiectasis
• Asthma
• Epilepsy
• Raised intraocular pressure, including glaucoma
• Diabetes mellitus (syr)
• Alcoholism (certain formulations) (syr)
• Galactose intolerance (tab)
• Lapp lactase deficiency (tab)
• Fructose intolerance (syr)
• Sucrose-isomaltase insufficiency (syr)
• Glucose-galactose malabsorption
• May impair ability to drive and operate machinery

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

Dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African registered indications and dosages

Allergic and anaphylactic conditions
- Such as hay fever, vasomotor rhinitis, urticaria, angioneurotic oedema, drug reactions, contact dermatitis, atopic dermatitis, insect bites, pruritus ani and pruritus vulvae

• Oral (tab): 4-16mg/day, in divided doses

Conditions responsive to antihistaminic therapy

• Oral (syr): 2-8mg/day, in divided doses
• Oral (liq): 4-16mg/day, in divided doses

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The oral (liq) formulation may also be used as an antitussive

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Indications and dosages registered in other jurisdictions

Symptomatic control of allergic conditions which respond to antihistamines
- This includes hay fever, vasomotor rhinitis, urticaria, angioneurotic oedema, food allergy, drug and serum reactions, insect bites
Symptomatic relief of itch associated with chickenpox

• Oral (tab, syr): 4mg, 4-6hrly; Max: 24mg/24hrs

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Do not exceed the stated dose or frequency of dosing. The minimum interval between the doses should be 4 hours

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Do not use continuously for more than 2 weeks without consulting a doctor

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

Dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African registered indications and dosages

Conditions responsive to antihistaminic therapy

Oral (syr)

• Neonates (newborns), or premature infants: Contraindicated
• Younger than 1 year: No information available
• Between 1-2 years: 1mg, 12hrly
• Between 2-5 years: 1mg, 4-8hrly; Max: 6mg/24hrs
• Between 6-12 years: 2mg, 4-8hrly; Max: 12mg/24hrs

Oral (liq)

• Younger than 2 years: Contraindicated
• Between 2-5 years: 1-2mg, 8hrly
• Between 6-12 years: 4mg, 6-8hrly

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The oral (liq) formulation may also be used as an antitussive

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Indications and dosages registered in other jurisdictions

Symptomatic control of allergic conditions which respond to antihistamines
- This includes hay fever, vasomotor rhinitis, urticaria, angioneurotic oedema, food allergy, drug and serum reactions, insect bites
Symptomatic relief of itch associated with chickenpox

Younger than 1 year

• Not recommended for use

Between 1-2 years

• Oral (syr): 1mg, 12hrly; Max: 2mg/24hrs

Between 2-6 years

• Oral (syr): 1mg, 4-6hrly; Max: 6mg/24hrs

Between 6-12 years

• Oral (tab, syr): 2mg, 4-6hrly; Max: 12mg/24hrs

Older than 12 years

• See adult dosage

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The tablets are not recommended for use in children under 6 years of age

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Do not exceed the stated dose or frequency of dosing. The minimum interval between the doses should be 4hrs

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Do not use continuously for more than 2 weeks without consulting a doctor

Pregnancy

South African recommendations

• Oral (tab): Contraindicated
• Safety in pregnancy has not yet been established
   
• Oral (syr): Caution; positive evidence of risk in animal studies
• Chlorpheniramine maleate should not be administered during the early months of pregnancy because of foetal abnormalities in studies in animals
   
• Oral (liq): Caution
• Safety in pregnancy has not been established

Recommendations in other jurisdictions

• Caution; not recommended 
• There are no adequate data from the use of chlorpheniramine maleate in pregnant women. The potential risk for humans is unknown
• Use during the third trimester may result in reactions in the newborn or premature neonates. Therefore, chlorpheniramine maleate should not to be used during pregnancy unless considered essential by a physician

Breastfeeding

South African recommendations

• Oral (tab): Caution; no information available
   
• Oral (syr): Contraindicated
• Use of chlorpheniramine maleate is not recommended; it may cause unusual excitement or irritability in nursing infants
   
• Oral (liq): Caution
• Safety in lactation has not been established

Recommendations in other jurisdictions

• Caution; not recommended 
• Chlorpheniramine maleate and other antihistamines may inhibit lactation and may be secreted in breast milk; therefore it should not be used during breastfeeding unless considered essential

Renal Impairment

• Caution; no information available

Hepatic Impairment

• Caution; no information available
  Metabolized by the liver, a dose adjustment may be required

Elderly

• Caution; dose adjustment recommended 
  The elderly are more likely to experience neurological anticholinergic effects. Consider a lower daily dose (Max: 12mg/24hrs)

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Confusion
• Excitation, including paradoxical excitation
• Irritability
• Nightmares
• Depression
• Sedation
• Somnolence
• Disturbance in attention
• Abnormal coordination
• Dizziness  
• Headache
• Fatigue

Cardiovascular Disorders 

• Palpitations
• Tachycardia
• Arrhythmias
• Hypotension

Respiratory Disorders

• Thickening of bronchial secretions
• Tight chest

Gastrointestinal Disorders 

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

Hepatobiliary Disorders 

• Hepatitis
• Jaundice

Genitourinary Disorders 

• Urinary retention

Endocrine and Metabolic Disorders 

• Anorexia

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
• Tinnitus

• Hypnotics
• Anxiolytics
• Phenytoin
• Monoamine oxidase inhibitors
• Other antihistamine-containing products
• Alcohol

None routine

Chlorpheniramine, a potent antihistamine (H1-antagonist), acts to diminish or abolish the actions of histamine in the body by the competitive reversible blockade of histamine H1-receptor sites on tissues. Chlorpheniramine also has anticholinergic activity. Antihistamines act to prevent the release of histamine, prostaglandins and leukotrienes and have been shown to prevent the migration of inflammatory mediators. The actions of chlorpheniramine include inhibition of histamine on smooth muscle, capillary permeability and hence reduction of oedema and wheal in hypersensitivity reactions, such as allergy and anaphylaxis.

Tablet 4mg

• Allergex (Adcock Ingram) originator
• Rhineton (Ranbaxy)

Syrup (per 5ml) 2mg

• Allergex (Adcock Ingram) originator
• Chlorhist (Adcock Ingram)
• Rhineton (Ranbaxy)

COMBINATION PREPARATIONS

Phenylephrine/ Chlorpheniramine

Syrup (per 5ml) 2.5mg/1.25mg

• Demazin (Bayer) originator

Ascorbic acid/ Pseudoephedrine/ Chlorpheniramine

Syrup (per 5ml) 50mg/25mg/2mg

• Flusin C (Pharmacare)

Paracetamol/ Phenylephrine/ Chlorpheniramine

Capsule 300mg/5mg/2mg

• Famucaps (Brunel) originator

Paracetamol/ Pseudoephedrine/ Chlorpheniramine

Tablet 500mg/30mg/2mg

• Sinutab Sinus Allergy Congestion & Pain (Johnson & Johnson)

Caplet 500mg/30mg/2mg

• Sinumax Allergy Sinus (Janssen)

Liquid (per 5ml) 160mg/15mg/1mg

• Sinumax Allergy Sinus Paed (Janssen)

Paracetamol/ Chlorpheniramine/ Pseudoephedrine

Tablet effervescent 500mg/4mg/50mg

• Endcol Effervescent (Pharmacare)

Phenylpropanolamine/ Phenylephrine/ Chlorpheniramine

Syrup (per 5ml) 2.5mg/2.5mg/2mg

• Rinex Paed (Pharmacare)

Syrup (per 5ml) 5mg/5mg/4mg

• Rinex (Pharmacare)

Capsule 30mg/20mg/12mg

• Rinex Diffucaps (Pharmacare)

Paracetamol/ Pseudoephedrine/ Chlorpheniramine

Syrup (per 5ml) 120mg/15mg/2mg

• Corenza Cold & Flu (Adcock Ingram)

Aspirin/ Ascorbic acid/ Pseudoephedrine/ Chlorpheniramine

Tablet effervescent 600mg/330mg/50mg/4mg

• Coryx effervescent (Mirren)

Paracetamol/ Ascorbic acid/ Pseudoephrine/ Chlorpheniramine

Tablet effervescent 500mg/330mg/50mg/4mg

• Flusin S (Pharmacare)
• Flutex effervescent (Pharmacare)

Paracetamol/ Caffeine/ Ephedrine/ Chlorpheniramine

Tablet 200mg/20mg/6mg/2mg

• Flusin (Pharmacare)
• Sinucon (Ascendis)
• Sinuend (Akacia) originator

Chlorpheniramine/ Pseudoephedrine/ Dextromethorphan/ Ascorbic acid

Syrup (per 5ml) 2mg/25mg/7.5mg/50mg

• Flusin DM (Pharmacare)

Chlorpheniramine/ Paracetamol/ Phenylephrine/ Dextromethorphan

Syrup (per 5ml) 0.5mg/120mg/2.5mg/5mg

• Kiddyflu (Caps Pharm) originator

Chlorpheniramine/ Paracetamol/ Phenylephrine/ Caffeine

Syrup (per 5ml) 2mg/75mg/2.5mg/7.5mg

• Colcleer Paediatric (Adcock Ingram) originator

Codeine/ Chlorpheniramine/ Phenylephrine/ Cetylpyridinium/ Guaifenesin/ Sodium Salicylate

Syrup (per 5ml) 5mg/2mg/2mg/2mg/25mg/1500mg

• Colphen (Adcock Ingram) originator

Caffeine/ Paracetamol/ Chlorpheniramine/ Phenylephrine/ Guaifenesin/ Codeine/ Triprolidine

Syrup (per 5ml) 30mg/300mg/2mg/5mg/50mg/12mg/ 3mg/0.6mg

• Trifen Expectorant Paediatric (Be-tabs)

Paracetamol/ Salicylamide/ Ascorbic acid/ Caffeine/ Chlorpheniramine/ Phenylephrine

Capsule 100mg/75mg/50mg/30mg/2mg/2mg

• Flutex (Pharmacare)

Caffeine/ Chlorpheniramine Maleate/ Paracetamol/ Phenylephrine Hydrochloride/ Phenyltoloxamine Dihydrogen Citrate

Capsule 30mg/2mg/200mg/5mg/12.5mg

• Dequa-Flu (Pharmacare)

Salicylamide/ Paracetamol/ Ascorbic acid/ Caffeine/ Chlorpheniramine/ Phenylephrine

Capsule 150mg/125mg/100mg/30mg/2mg/2mg

• Adco-Histamed Co (Adcock Ingram)