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LodozLodoz

Bisoprolol hemifumarate ....... 5.00 mg

Hydrochlorothiazide ............. 6.25 mg

 

Excipients

Silica colloidal anhydrous, magnesium stearate, microcrystalline cellulose, maize starch, anhydrous calcium hydrogen phosphate.

 

Product Description

Round, pastel pink, biconvex film coated tablet, with a heart embossed on one side and the figure 5 embossed on the other.

 

Indications

Mild to moderate hypertension.

 

Mode of administration

Lodoz is available in the following dosage strengths so that the dosage can be adjusted individually:

Lodoz 2.5 mg, film coated tablets,

Lodoz 5 mg, film coated tablets,

Lodoz 10 mg, film coated tablets,

The initial dosage is one tablet containing bisoprolol 2.5 mg + hydrochlorothiazide 6.25 mg once daily.

If an inadequate response to treatment is obtained, the dosage should be increased to one tablet containing bisoprolol 5 mg + hydrochlorothiazide 6.25 mg in a once daily dose. If the latter proves to be insufficiently effective, the dosage may be increased to one tablet containing bisoprolol 10 mg + hydrochlorothiazide 6.25 mg once daily.

Lodoz must be taken in the morning, and it may be taken with food. The film coated tablets must be swallowed with a little liquid and must not be chewed.

No alteration in dosage is required in patients with liver failure or mild to moderate renal failure (creatinine clearance > 30 ml/min). It is inadvisable to use Lodoz in children since there are no available data concerning its utilization in paediatrics.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamic properties

COMBINATION OF A BETA-BLOCKER (SELECTIVE β1) WITH A THIAZIDE DIURETIC.

ATC code: C07BB07

Clinical trials have demonstrated that the 2 active substances in the combination have an additive effect. The lowest dose, 2.5 mg + 6.25 mg, has been shown to be effective in the treatment of mild to moderate hypertension.

 

Pharmacodynamic effects such as hypokalaemia (hydrochlorothiazide) and bradycardia, asthenia and headaches (bisoprolol) are dose-dependent.

 

The use of a combination of the two active substances at one quarter or one half of the doses employed in monotherapy (2.5 mg + 6.25 mg) is designed to reduce these effects.

 

Bisoprolol is a powerful, highly selective β-adrenergic antagonist devoid of intrinsic sympathomimetic activity and without any significant membrane stabilizing effects.

 

As with other β-adrenergic-receptor antagonists, the mode of action of bisoprolol in hypertension is poorly understood, although it has been shown that this product markedly reduces the plasma renin concentration and slows the heart rate.

 

Hydrochlorothiazide is a thiazide diuretic which has an anti hypertensive action. Its diuretic effect is due to the inhibition of active Na+ transport from the renal tubules towards the blood, preventing the reabsorption of Na+.

 

Pharmacokinetic properties

Related to bisoprolol

Absorption: Tmax ranges from 1 to 4 hours.

Bioavailability is high (88 %) and unaffected by the intake of food, while little first-pass metabolism occurs in the liver. Pharmacokinetics are linear for doses between 5 and 40 mg.

Distribution: bisoprolol is 30 % bound to plasma proteins and the distribution volume is high (about 3 l/kg).

Metabolism: 40 % of bisoprolol is metabolized in the liver. The metabolites formed are inactive.

Elimination: the plasma elimination half-life is 11 hours. Renal and hepatic clearances are more or less equivalent and half of the dose administered is found unchanged in urine, along with the metabolites. Total clearance is about 15 l/h.

 

Related to hydrochlorothiazide

Absorption: the bioavailability of hydrochlorothiazide varies from 60 to 80 % in individual subjects. Tmax ranges from 1.5 to 5 hours, with a mean of about 4 hours.

Distribution: about 40 % is bound to plasma proteins.

Elimination: hydrochlorothiazide is not metabolized and is almost entirely excreted in unchanged form via glomerular filtration and active tubular secretion. The elimination half-life of hydrochlorothiazide is about 8 hours.

In patients with renal and heart failure, renal clearance of hydrochlorothiazide is reduced and the elimination half-life increased. This is also true in the elderly with, in addition, an augmentation in the peak plasma concentration (Cmax).

It crosses the placenta and is excreted in breast milk.

 

Preclinical safety data

Bisoprolol and hydrochlorothiazide did not prove to be harmful in man during the course of standard preclinical toxicity tests (long term toxicity, mutagenicity, genotoxicity and carcinogenicity). Like other beta-blockers, high doses of bisoprolol administered during animal studies produced toxic effects in the mother (decrease in food intake and weight gain), and in the embryo and/or foetus (increase in the number of late abortions, decrease in birth weight of progeny, delay in physical development up until the end of lactation). However, neither bisoprolol nor hydrochlorothiazide displayed any teratogenic effect. No aggravation in toxicity was noted when the two active substances were administered simultaneously.

 

Contraindications

Related to bisoprolol

This drug is contraindicated in the following cases:

- severe forms of asthma and chronic obstructive lung disease,

- heart failure uncontrolled by treatment,

- cardiogenic shock,

- sick sinus syndrome (including sinoatrial block),

- unpaced second- or third-degree atrioventricular block,

- major bradycardia (heart rate less than 50 beats/min),

- Prinzmetal variant of angina (pure forms and with monotherapy),

- pheochromocytoma (except after administration of alpha-blocker therapy),

- severe forms of Raynaud's phenomenon and peripheral arterial disorders,

- hypotension,

- hypersensitivity to bisoprolol,

- in combination with floctafenin (see heading 4.5 Interaction with other medicaments and other forms of interaction),

- in combination with sultopride (see heading 4.5 Interaction with other medicaments and other forms of interaction).

 

Related to hydrochlorothiazide

This drug is contraindicated in the following cases:

- hypersensitivity to sulphonamides,

- severe renal failure (creatinine clearance ≤ 30 ml/min),

- severe liver failure,

- lactation.

 

It is generally inadvisable to use this drug in combination with lithium and non antiarrhythmic drugs that give rise to atypical ventricular tachycardia (see heading 4.5 Interaction with other medicaments and other forms of interaction).

 

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