Darifenacin (Darifenacinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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M-holinoblokatory

Spasmolytics myotropic

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    Aspen Pharma Trading Limited    
    • АТХ:

    G.04.B   Other drugs for the treatment of urological diseases (including antispasmodics)

    G.04.B.D.10   Darifenacin

    Pharmacodynamics:

    This drug is a selective blocker M3-muscarinic receptors, which are responsible for the regulation of the smooth muscle tone of the bladder and its detrusor. Darifenacin causes ylower frequency of urination, mandatory urination, episodes of urinary incontinence, and an increase in the average volume of urine when the bladder is emptied.

    Pharmacokinetics:

    Absorption 98% (does not depend on food intake). In men, bioavailability is lower by 23%. The connection with plasma proteins is 98%. Metabolized by the liver, eliminated by the kidneys - 60%, gastrointestinal tract - 40%. The half-life is 13-19 hours.

    Indications:

    Hyperactivity of the bladder, manifested persistent urge to urinate, urinary incontinence and frequent urination.

    ICD-10

    V.F90-F98.F98.0   Enuresis of inorganic nature

    XIV.N30-N39.N31   Neuromuscular dysfunction of the bladder, not elsewhere classified

    XIV.N30-N39.N31.1   Reflex bladder, not elsewhere classified

    XIV.N30-N39.N39.3   Involuntary urination

    XIV.N30-N39.N39.4   Other specified incontinence

    XVIII.R30-R39.R32   Urinary incontinence, unspecified

    XVIII.R30-R39.R39.1   Other difficulties associated with urination

    Contraindications:

    Urine retention, uncontrolled angle-closure glaucoma, slowing of gastric motility, hypersensitivity to the drug, children's age.

    Carefully:

    Clinically significant disorders of outflow from the bladder, the risk of urinary retention, obstructive diseases of the gastrointestinal tract, severe constipation.

    Pregnancy and lactation:

    Category FDA - C. Qualitative and well-controlled studies on humans and animals have not been conducted. Apply if the benefit to the mother exceeds the risk to the fetus.

    In experimental studies, excretion of darifenacin with breast milk was noted. It is not known whether darifenacin with human breast milk, so caution is required if lactation is required.

    Dosing and Administration:

    Take orally, swallow whole, without chewing, not dividing and not crushing. The drug is taken once a day, squeezed with liquid, long-term treatment. The initial recommended dose is 7.5 mg per day. If the effect is insufficient, after 2 weeks the dose can be increased to 15 mg per day.

    Side effects:

    From the nervous system: insomnia, dizziness, drowsiness, headache, violation of the thought process, violation of near vision, dry eye syndrome, violation of taste sensitivity.

    From the skin: dry skin, itching, rash, increased sweating, swelling of the face.

    On the part of the reproductive system: vaginitis, impotence.

    From the digestive system: constipation, dry mouth, indigestion, ulcerative stomatitis, flatulence, nausea, abdominal pain.

    From the side of the urinary system: urinary tract infection, dysuria, pain in the bladder.

    From the cardiovascular system: tachycardia, arterial hypertension.

    Overdose:

    Symptoms: shakiness, impaired vision, unstable walking, difficulty breathing, drowsiness, fever, hallucinations, severe muscle weakness.

    Treatment - administration of physostigmine or neostigmine methyl sulfate.

    Interaction:

    With simultaneous administration with inhibitors of isoenzyme CP3A4 (ketoconazole, itraconazole, miconazole, troleandomycin, nefazodone and ritonavir) - the maximum daily dose of the drug should not exceed 7.5 mg.

    The drug increases the bioavailability of digoxin when taken concomitantly with the drug.

    With simultaneous admission with m-holinoblokatorami - increase m-cholinoblocking effects of darifenacin (dry mouth, constipation, blurred vision).

    Caution should be applied darifenacin simultaneously with drugs that are metabolized predominantly by the CYP2D6 isoenzyme and have a narrow therapeutic range, for example, flecainide, thioridazine, tricyclic antidepressants (imipramine).

    Special instructions:

    Before starting to take, all organic causes of frequent urination should be ruled out.

    Influence on ability to drive a car and drive mechanisms

    Studies of the effect of the drug on the ability to drive vehicles and work with mechanisms have not been conducted. Some of the side effects of the drug, such as dizziness and blurred vision, can adversely affect the ability to drive and perform potentially dangerous activities requiring increased concentration and speed of psychomotor reactions.

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