Tiotropium Bromide (Inhalation)
Brand Name: Spiriva
Common Dosage Forms:
Inhalation Powder: Available in HandiHaler and Respimat inhalers. Each dose delivers 18 mcg tiotropium
FDA Indications/Dosages:
For the long-term, once-daily, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema and for reducing exacerbations: The recommended dose is one inhalation daily.
Monitor: FEV
Pharmacology/Pharmacokinetics: Tiotropium is a long-acting antagonist of the action of acetylcholine at the M3-receptors in the smooth muscle of the bronchial tree. This antagonism results in bronchodilation which lasts for greater than 24 hours. Chemically, tiotropium is a synthetic, non-chiral, quaternary ammonium compound. Bioavailability is 20% via the inhaled route and 3% via the oral route. 74% of an intravenous dose is excreted unchanged in the urine which 25% is metabolized by cytochrome P450-dependant oxidation and subsequent glutathione conjugation. CYP2D6 and CYP3A4 appears to be the primary pathways for metabolism. The terminal elimination half-life following inhalation is between 5-6 days. Steady state levels are reached after 2-3 weeks with no accumulation thereafter.
Drug Interactions: Drugs which inhibit that CYP2D6 or CYP3A4 metabolic pathways may increase the plasma levels of tiotropium. However, since only a small amount of absorbed drug is metabolized, these interactions are not likely to be significant.
Contraindications/Precautions: Contraindicated in patients with known hypersensitivity to atropine or its derivatives. This medication is not indicated for the initial treatment of acute episodes of bronchospasm, I.e., rescue therapy. Use with caution in renally-impaired patients. Use with caution in patients with narrow-angle glaucoma, prostatic hyperplasia, or bladder neck obstruction. Pregnancy Category C.
Adverse Effects: The most common adverse effect is dry mouth (16%). Other adverse effects reported at a slightly higher rate than with placebo (≥2%) are accidents, chest pain, abdominal pain, constipation, vomiting, moniliasis, epistaxis, pharyngitis, sinusitis, upper respiratory tract infection, rash, dizziness, hoarseness, tachycardia, throat irritation, and urinary tract infection.
Patient Consultation:
Store in a cool, dry place away from sunlight and children. Unused capsules should remain in the blister strip and be used over the next consecutive days.
If a dose is missed, take it as soon as possible. If it is closer to the time of your next dose than the dose you missed, skip the missed dose and return to your dosing schedule.
Contact physician if the above side effects are severe or persistent.
This form is not intended for occasional use. Use daily for maximum effectiveness.
Directions for HandiHaler use: (1) Open one blister strip to expose one capsule only. (2) Open the dust cap and mouthpiece to expose the center chamber. (3) Place the capsule in the center chamber and close the mouthpiece until you hear a click. (4) Press the piercing button completely in once and release. (5) Exhale completely. Do not breath into the mouthpiece at any time. (6) Place your lips tightly around the mouthpiece and breath in slowly and deeply until your lungs are full. You should hear the capsule vibrate. (7) Remove the mouthpiece from your lips and exhale. (8) Repeat #6 and #7 up to 5 more times. (9) Open the mouthpiece and discard the empty capsule.