Spiriva: Full Drug Profile
Spiriva - General Information
Spiriva is a long-acting, 24 hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Spiriva is a muscarinic receptor antagonist, on topical application it acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect.
Pharmacology of Spiriva
Spiriva is a long–acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3–receptors at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies prevention of methacholine–induced bronchoconstriction effects were dose–dependent and lasted longer than 24 hours. The bronchodilation following inhalation of tiotropium is predominantly a site–specific effect.
Spiriva for patients
PATIENT INFORMATION
Patient's Instructions for Use Spiriva® HandiHaler®
(tiotropium bromide inhalation powder)
FOR ORAL INHALATION ONLY
Read all instructions before use.
This leaflet provides summary information about SPIRIVA capsules and the HandiHaler inhalation device. Before you start to take SPIRIVA or use the HandiHaler, read this leaflet carefully and keep it for future use. You should read the leaflet that comes with your prescription every time you refill it because there may be new information.
For more information, ask your health-care provider or pharmacist.
What should you know about SPIRIVA and the HandiHaler?
Each SPIRIVA capsule contains a dry powder blend of active drug (18 mcg tiotropium) and lactose monohydrate as the carrier. The dry powder in the capsule is inhaled from the HandiHaler inhalation device. SPIRIVA capsules contain only a small amount of powder which makes the capsule appear almost empty. When disposing of the capsule, you may notice that a dusting of this powder is left in the capsule. This is normal.
SPIRIVA is a once daily maintenance bronchodilator medicine that opens narrowed airways and helps keep them open for 24 hours. SPIRIVA HandiHaler should not be used for immediate relief of breathing problems, i.e., as a rescue medication.
SPIRIVA CAPSULES ARE INTENDED FOR ORAL INHALATION ONLY AND ARE TO BE USED ONLY
WITH THE HANDIHALER INHALATION DEVICE.
SPIRIVA CAPSULES SHOULD NOT BE SWALLOWED.
The HandiHaler is an inhalation device that has been specially designed for use with SPIRIVA capsules. It must not be used to take any other medication.
Care must be taken not to allow the powder to enter into the eyes. If symptoms of eye pain, eye discomfort, blurred vision, visual halos, or colored images in association with red eyes occur, consult a physician immediately.
How do you take your dose of SPIRIVA using the HandiHaler?
Taking your dose of SPIRIVA, requires four main steps: Open the blister and the HandiHaler device, insert the SPIRIVA capsule, press the HandiHaler button, and inhale your medication. (See below for details.)
Become familiar with the components of the HandiHaler inhalation device:
- dust cap
- mouthpiece
- base
- piercing button
- center chamber
- Air intake vents
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Removing the SPIRIVA capsule from the blister.
A) SPIRIVA capsules are packaged in a blister card. Each blister card consists of two blister strips, each containing 3 capsules and joined along a perforated-cut line. Prior to removing the first capsule from the blister card, separate the blister strips by tearing along the perforation. (Figure A)
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B) The blister should be carefully opened to expose only one capsule at a time. Immediately before you are ready to use your dose of SPIRIVA, peel back the aluminum foil using the tab at the rounded edge until one capsule is fully visible. The foil lidding should only be peeled back as far as the STOPline printed on the blister foil to prevent exposure of more than one capsule. (Figure B) Turn the blister strip upside down and tip the capsule out, tapping the back of the blister pack, if necessary. DO NOT CUT THE FOIL OR USE SHARP INSTRUMENTS TO REMOVE THE CAPSULE FROM BLISTER. After using the first capsule, the 2 remaining capsules should be used over the next 2 consecutive days.
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Capsules should always be stored in the sealed blisters and only removed immediately before use. The drug should be used immediately after the packaging over an individual capsule is opened, or else its effectiveness may be reduced.
If additional capsules are inadvertently exposed to air, they should not be used and should be discarded.
Do not store capsules in the HandiHaler device.
Opening the HandiHaler device and inserting the SPIRIVA capsule.
1) OPEN: Open the dust cap by pulling it upwards. Then open the mouthpiece. (Figure 1)
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2) INSERT: Place the capsule in the center chamber. It does not matter which end of the capsule is placed in the chamber. (Figure 2)
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3) Close the mouthpiece firmly until you hear a click, leaving the dust cap open. Check to see that the mouthpiece is completely closed. Be sure that the mouthpiece sits firmly against the gray base so that there is no gap between the mouthpiece and the base. (Figure 3)
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Taking your dose of SPIRIVA.
4) PRESS: Hold the HandiHaler device with the mouthpiece upwards and press the piercing button completely in once until it is flush against the base, and release. This makes holes in the capsule and allows the medication to be released when you breathe in. (Figure 4)
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5) Breathe out completely. (Figure 5) Important: Do not breathe (exhale) into the HandiHaler mouthpiece at any time.
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6) INHALE: Holding the HandiHaler by only the gray base and without blocking the air intake vents, raise the HandiHaler device to your mouth and close your lips tightly around the mouthpiece. Keep your head in an upright position and breathe in slowly and deeply but at a rate sufficient to hear or feel the capsule vibrate. Breathe in until your lungs are full; then hold your breath as long as is comfortable and at the same time take the HandiHaler device out of your mouth. Resume normal breathing. (Figure 6)
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To ensure you get the full dose of SPIRIVA, you must repeat steps 5 and 6 once again.
If you do not hear or feel the capsule vibrate, DO NOT PRESS THE GREEN BUTTON AGAIN, but instead tap the HandiHaler gently on a table, holding it in an upright position. Check to see that the mouthpiece is completely closed. Then breathe in again slowly and deeply. If you still do not hear or feel the capsule vibrate after repeating the above steps please consult your physician.
7) After you have finished taking your daily dose of SPIRIVA, open the mouthpiece again. Tip out the used capsule and discard. (Figure 7)
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8) Close the mouthpiece and dust cap for storage of your HandiHaler device. (Figure 8)
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When and how should you clean your HandiHaler Device?
Normally, during a one-month period of use, the HandiHaler device does not need to be cleaned. However, if cleaning is needed the HandiHaler device can be cleaned as described below:
Open the dust cap and mouthpiece. Open the base by lifting the piercing button. Rinse the complete inhaler with warm water to remove any powder. Do not use cleaning agents or detergents.
Dry the HandiHaler device thoroughly by tipping the excess water out on a paper towel and air-dry afterwards, leaving the dust cap, mouthpiece and base open. It takes 24 hours to air dry, so clean it right after you use it and it will be ready for your next dose. Do not use the HandiHaler device when it is wet.
If needed, the outside of the mouthpiece may be cleaned with a moist, but not wet tissue.
The HandiHaler device should not be placed in the dishwasher for cleaning.
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Where should you store SPIRIVA capsules and the HandiHaler Device?
Store at 25°C (77°F); excursions permitted to 15°—30°C (59°—86°F) [see USP Controlled Room Temperature].
The capsules should not be exposed to extreme temperature or moisture. Do not store capsules in the HandiHaler.
As with all prescription medications, keep this out of the reach of children.
Tell your doctor before you use SPIRIVA HandiHaler:
- if you may be pregnant or wish to become pregnant;
- if you are a breastfeeding mother;
- if you are taking any medications including eye drops, this includes those you can buy without a prescription;
- if you have any other medical problems such as difficulty urinating or an enlarged prostate;
- if you are allergic to any medications.
USE THIS PRODUCT AS DIRECTED, UNLESS INSTRUCTED TO DO OTHERWISE BY YOUR PHYSICIAN.
Spiriva Interactions
SPIRIVA has been used concomitantly with other drugs commonly used in COPD without increases in adverse drug reactions. These include sympathomimetic bronchodilators, methylxanthines, and oral and inhaled steroids. However, the co–administration of SPIRIVA with other anticholinergic–containing drugs (e.g., ipratropium) has not been studied and is therefore not recommended.
Spiriva Contraindications
SPIRIVA HandiHaler (tiotropium bromide inhalation powder) is contraindicated in patients with a history of hypersensitivity to atropine or its derivatives, including ipratropium, or to any component of this product.
Additional information about Spiriva
- Spiriva Indication
Used in the management of chronic obstructive pulmonary disease (COPD).
- Mechanism Of Action
- Spiriva is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, on topical application it acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect.
- Generic Name
- Tiotropium
- Synonyms
- Tiotropium bromide
- Drug Category
- Muscarinic Antagonists; Anticholinergic Agents
- Drug Type
- Small Molecule; Approved
- Other Brand Names containing Tiotropium
- Spiriva;
- Absorption
- Bioavailability is 19.5% following administration by inhalation. Oral solutions of tiotropium have an absolute bioavailability of 2-3%.
- Toxicity (Overdose)
- No mortality was observed at inhalation tiotropium doses up to 32.4 mg/kg in mice, 267.7 mg/kg in rats, and 0.6 mg/kg in dogs. These doses correspond to 7,300, 120,000, and 850 times the recommended human daily dose on a mg/m2 basis, respectively.
- Protein Binding
- 72% bound to plasma proteins.
- Biotransformation
- The extent of biotransformation appears to be small. This is evident from a urinary excretion of 74% of unchanged substance after an intravenous dose to young healthy volunteers. Tiotropium, an ester, is nonenzymatically cleaved to the alcohol N–methylscopine and dithienylglycolic acid, neither of which bind to muscarinic receptors. In vitro experiments with human liver microsomes and human hepatocytes suggest that a fraction of the administered dose (74% of an intravenous dose is excreted unchanged in the urine, leaving 25% for metabolism) is metabolized by cytochrome P450–dependent oxidation and subsequent glutathione conjugation to a variety of Phase II metabolites. Via inhibition studies, it is evident that CYP450 2D6 and 3A4 are involved in the metabolic pathway that is responsible for the elimination of a small part of the administered dose.
- Half Life
- 5-6 days
- Dosage Forms of Spiriva
- Capsule Respiratory (inhalation)
- Chemical Formula
- C19H22BrNO4S2
- Tiotropium on Wikipedia
- https://en.wikipedia.org/wiki/Tiotropium
- Organisms Affected
- Humans and other mammals