Tiotropium Bromide

Registered South African indications:

• Chronic obstructive pulmonary disease

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients 
• Hypersensitivity to atropine or any of its derivatives, e.g. ipratropium or oxitropium

Cautions

• Pregnancy
• Breastfeeding 
• Moderate to severe renal impairment 
• Acute bronchospasm
• Narrow angle glaucoma
• Prostatic hyperplasia
• Bladder neck obstruction
• Inhalation-induced bronchospasm
• Recent myocardial infarction < 6 months
• Cardiac arrhythmia
• Hospitalisation for heart failure (NYHA Class III or IV) within the last 12 months
• Ocular contact
• Glaucoma
• Cystic fibrosis 
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• Lactose intolerance (caps)

Forms avail. in SA and covered in this monograph: inc, sol

Chronic obstructive pulmonary disease

• Inhaled (inc): 18μg, dly; Max: 18μg/24hrs  
• Inhaled (sol): 5μg, dly; Max: 5μg/24hrs

DO NOT swallow capsules

Only use Handihaler device to inhale capsule

Not established for use in children

Pregnancy 

• Caution
• There is a very limited amount of data from the use of tiotropium in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity at clinically relevant doses. As a precautionary measure, it is preferable to avoid the use of tiotropium during pregnancy

Breastfeeding 

• Caution; not recommended
• It is unknown whether tiotropium bromide is excreted in human breast milk. Despite studies in rodents which have demonstrated that excretion of tiotropium bromide in breast milk occurs only in small amounts, use of tiotropium is not recommended during breastfeeding. Tiotropium bromide is a long-acting compound. A decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with tiotropium bromide should be made taking into account the benefit of breastfeeding to the child and the benefit of tiotropium bromide therapy to the woman

Renal Impairment 

• CrCl >60ml/min: No dose adjustment recommended
• CrCl ≤60ml/min: Caution; no dose adjustment recommended

Hepatic Impairment 

• No dose adjustment recommended

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Dizziness
• Headache
• Insomnia

Cardiovascular Disorders

• Atrial fibrillation
• Supraventricular tachycardia
• Palpitations

Respiratory Disorders

• Pharyngitis
• Dysphonia
• Cough
• Bronchospasm
• Epistaxis
• Laryngitis
• Sinusitis

Gastrointestinal Disorders

• Dry mouth
• Gastro-oesophageal reflux disease
• Constipation
• Oropharyngeal candidiasis
• Gingivitis
• Glossitis
• Dysphagia
• Stomatitis
• Nausea
• Dental caries
• Intestinal obstruction

Genitourinary Disorders

• Dysuria
• Urinary retention
• Urinary tract infection

Endocrine and Metabolic Disorders

• Dehydration

Musculoskeletal Disorders

• Joint swelling

Skin and Subcutaneous Tissue Disorders

• Rash
• Urticaria
• Pruritus
• Skin infection
• Skin ulcer
• Dry skin

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity 
• Angioedema
• Anaphylactic reaction

Sensory Disorders

• Blurred vision
• Glaucoma
• Increased intraocular pressure 
• Taste disorders

• Anticholinergics

None routine  

Tiotropium bromide is a long-acting muscarinic receptor antagonist, which binds to muscarinic receptors in the bronchial smooth musculature. It competitively and reversibly inhibits the action of acetylcholine at type 3 muscarinic (M3) receptors in bronchial smooth muscle causing bronchodilation. The long duration is probably due to the very slow dissociation from the M3 receptor, exhibiting a significantly longer dissociation half-life than ipratropium bromide. It is topically broncho-selective when administered by inhalation, demonstrating an acceptable therapeutic range before systemic anticholinergic effects occur.

Inhalation capsule 10μg

• Tiores (Forrester Pharma)

Inhalation capsule 18μg

• Forvent (Ingelheim) originator
• Forvent refill (Ingelheim) originator
• Spiriva (Ingelheim) originator

Solution (per puff) 2,5μg

• Spiriva Respimat (Ingelheim) originator