Tiotropium bromide

When ATH:
R03BB04

Pharmacological action

Bronchodilator agent, blocks m-cholinergic receptors of the smooth muscle of the tracheobronchial tree. It has the same affinity for the different subtypes muscarinic receptors M1 to M5. The result of the inhibition of M3 receptors in the airways is the relaxation of smooth muscles. When inhaled route of administration has a selective effect of tiotropium, wherein at therapeutic doses do not cause systemic side effects of anticholinergic. Bronchodilatory effect depends on the dose and maintained for at least 24 no, due to the slow dissociation from the M3 receptors. The release of the M2 receptors is faster, than from M3. High affinity receptors and slow dissociation cause a pronounced and lasting bronchodilatory effects in patients with COPD. Significantly improves lung function (FJEL) after 30 minutes after a single dose of, increases the morning and evening peak expiratory flow. Pharmacodynamic balance is achieved within 1 Sun, and pronounced bronchodilator effect is observed in the 3 d.

Pharmacokinetics

When inhaled route of administration, the absolute bioavailability - 19,5 %. Poorly absorbed in the digestive tract. TCmax after inhalation - 5 m. Cmax in patients with COPD is 17-19 pg / ml after inhalation powder dose 18 mcg and decreases rapidly. The range of therapeutic dosages is linear pharmacokinetics. Relationship to plasma proteins - 72 %, volume of distribution - 32 l / kg, Css — 3-4 pg / ml. Do not cross the BBB. Metabolized slightly to ethanol-N-metilskopina and ditienilglikolievoy acid (pharmacologically inactive), less 20 % метаболизируется цитохромом P450 (изоферменты CYP2D6 и CYP3A4) to form various metabolites. Не ингибирует цитохром CYP1A1, CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 и CYP3A. T1 / 2 after inhalation - 5-6 days. Total clearance - 880 ml / min. Report the news (14 %) primarily by tubular secretion, and faeces. Not accumulates. In elderly patients with reduced renal clearance (7 %), However, plasma concentrations were not significantly changed. When CRF observed increase plasma concentrations and reduced renal clearance.

Testimony

As maintenance therapy in patients with COPD, including chronic obstructive bronchitis and emphysema, (when persistent dyspnea, and for the prevention of exacerbations).

Dosage regimen

Inhalation using a special inhaler, by 1 capsule per day at the same time. Capsules should not ingest. Elderly people, patients with compromised renal function or liver can use the drug in the recommended doses.

Contraindications

Increased sensitivity to the tiotropium bromide, as well as atropino or its derivatives (for example ipratropiju or ypratropiu oksitropiu), I trimester of pregnancy, Age to 18 years.

Side effect

For part of the intestine-dryness in the mouth (usually mild symptoms, often disappear if you continue treatment), constipation.

From the respiratory system: cough, Local irritation, It is possible to develop bronchospasm, as well as when taking other inhalation.

Other: tachycardia, difficulty or urinary retention (in men with benign prostatic hyperplasia), angioedema, blurred vision, ostraya glaucoma (associated with anticholinergic).

Cautions

Careful monitoring of patients with moderate or severe renal insufficiency, tiotropium bromide in combination with other drugs, egesting, primarily, kidney.

Be wary appoint patients with narrow-angle glaucoma, prostatic hyperplasia or bladder neck obstruction.

It can not be used as a means of emergency treatment for relief of bronchospasm attacks.

Do not allow to enter the powder into the eyes.

Contraindicated for use in the I trimester of pregnancy. The remaining stages of pregnancy and during lactation - only, if the expected benefits outweigh any possible risk to the fetus or infant.

Cautions

Not recommended simultaneous application with other anticholinergics.