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Components:
Doxazosin
Method of action:
Alpha-Adrenergic Blocking, Alpha-Adrenolytic, Antihypertensive, Antispasmodic, Corrective Disorder Of Urination Or Dysuria, Hypotensive, Lipid-Lowering, Vasodilator
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Medically reviewed by Oliinyk Elizabeth Ivanovna, Pharmacy. Last updated on 2019.12.15

Name of the medicinal product

Lafedoxin

Qualitative and quantitative composition

Doxazosin

Therapeutic indications

The information provided in Therapeutic indications of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Therapeutic indications in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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- Essential hypertension

- Symptomatic treatment of benign prostatic hyperplasia.

Dosage (Posology) and method of administration

The information provided in Dosage (Posology) and method of administration of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Dosage (Posology) and method of administration in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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The tablets can be taken with or without food. The tablets must be swallowed whole with a sufficient amount of liquid. The tablets should not be chewed, divided or crushed.

The maximum recommended dose is 8 mg Lafedoxin once daily.

Essential hypertension:

Adults: Usually 4 mg Lafedoxin once daily. If necessary, the dosage may be increased to 8 mg Lafedoxin once daily.

Lafedoxin can be used as sole agent or in combination with another medicinal product e.g. a thiazide diuretic, beta-adrenoceptor blocking agent, calcium antagonist or an ACE-inhibitor.

Symptomatic treatment of prostatic hyperplasia:

Adults: Usually 4 mg Lafedoxin once daily. If necessary, the dosage may be increased to 8 mg Lafedoxin once daily.

Lafedoxin may be used in benign prostatic hyperplasia (BPH) patients who are either hypertensive or normotensive, as the blood pressure changes in normotensive patients are clinically insignificant. In hypertensive patients both conditions are treated concomitantly.

Elderly: Same dosage as for adults.

Patients with renal impairment: Since there is no change in pharmacokinetics in patients with impaired renal function, and since there are no signs that Lafedoxin aggravates existing renal impairment, the usual dose can be used in these patients.

Patients with hepatic impairment: Lafedoxin should be given with particular caution to patients with evidence of impaired liver function. In patients with severe hepatic impairment clinical experience is lacking and therefore the use of Lafedoxin is not recommended..

Children and adolescents: Lafedoxin is not recommended for patients under the age of 18 years.

Contraindications

The information provided in Contraindications of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Contraindications in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Lafedoxin is contraindicated in

- Patients with a known hypersensitivity to quinazolines (e.g. prazosin, terazosin, Lafedoxin), or any of the excipients

- Patients with a history of orthostatic hypotension

- Patients with benign prostatic hyperplasia and concomitant congestion of the upper urinary tract, chronic urinary tract infections or bladder stones

- Patients with a history of gastrointestinal obstruction, oesophageal obstruction, or any degree of decreased lumen diameter of the gastrointestinal tract1

- During lactation 2

- Patients with hypotension3

Lafedoxin is contraindicated as monotherapy in patients with either overflow bladder or anuria or without progressive renal insufficiency.

1 For patients taking the sustained release tablets only.

2 For the hypertension indication only

3 For the benign prostatic hyperplasia indication only

Special warnings and precautions for use

The information provided in Special warnings and precautions for use of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Special warnings and precautions for use in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Information to be given to the Patient: Patients should be informed that Lafedoxin tablets should be swallowed whole. Patients should not chew, divide or crush the tablets.

In Cardozo XL the active compound is surrounded by an inert, non absorbable coating that is designed to control the release of the drug over a prolonged period. After transit through the gastrointestinal tract, the empty tablet shell is excreted. Patients should be advised not to be concerned if they occasionally observe remains in their stools that look like a tablet

Abnormally short transit times through the gastrointestinal tract (e.g. following surgical resection) could result in incomplete absorption. In view of the long half life of Lafedoxin the clinical significance of this is unclear.

Initiation of Therapy: In relation with the alpha-blocking properties of Lafedoxin, patients may experience postural hypotension evidenced by dizziness and weakness, or rarely loss of consciousness (syncope), particularly with the commencement of therapy. Therefore, it is prudent medical practice to monitor blood pressure on initiation of therapy to minimise the potential for postural effects. The patient should be cautioned to avoid situations where injury could result should dizziness or weakness occur during the initiation of Lafedoxin therapy.

Use in Patients with Acute Cardiac Conditions:

As with any other vasodilatory anti-hypertensive agent it is prudent medical practice to advise caution when administering Lafedoxin to patients with the following acute cardiac conditions:

- pulmonary oedema due to aortic or mitral stenosis

- heart failure at high output

- right-sided heart failure due to pulmonary embolism or pericardial effusion

- left ventricular heart failure with low filling pressure.

Use in Hepatically Impaired Patients:

As with any drug wholly metabolised by the liver, Lafedoxin should be administered with particular caution to patients with evidence of impaired hepatic function. Since there is no clinical experience in patients with severe hepatic impairment use in these patients is not recommended.

Use with PDE-5 inhibitors:

Concomitant administration of Lafedoxin with phosphodiesterase-5-inhibitors (e.g. sildenafil, tadalafil, and vardenafil) should be done with caution as both drugs have vasodilating effects and may lead to symptomatic hypotension in some patients. To reduce the risk of orthostatic hypotension it is recommended to initiate the treatment with phosphodiesterase-5-inhibitors only if the patient is hemodynamically stabilized on alpha-blocker therapy. Furthermore, it is recommended to initiate phosphodiesterase-5-inhibitor treatment with the lowest possible dose and to respect a 6-hour time interval from intake of Lafedoxin. No studies have been conducted with Lafedoxin prolonged release formulations.

Use in Patients Undergoing Cataract Surgery:

The 'Intraoperative Floppy Iris Syndrome' (IFIS, a variant of small pupil syndrome) has been observed during cataract surgery in some patients on or previously treated with tamsulosin. Isolated reports have also been received with other alpha-1 blockers and the possibility of a class effect cannot be excluded. As IFIS may lead to increased procedural complications during the cataract operation current or past use of alpha-1 blockers should be made known to the ophthalmic surgeon in advance of surgery.

Effects on ability to drive and use machines

The information provided in Effects on ability to drive and use machines of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Effects on ability to drive and use machines in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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The ability to engage in activities such as operating machinery or operating a motor vehicle may be impaired, especially when initiating therapy.

Undesirable effects

The information provided in Undesirable effects of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Undesirable effects in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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The following undesirable effects have been observed and reported during treatment with Lafedoxin with the following frequencies: Very common >1/10; common >1/100, <1/10; uncommon >1/1,000, <1/100; rare >1/10,000, <1/1,000; very rare <1/10,000

System Organ Class

Very Common

(>1/10)

Common(>1/100 to <1/10)

Uncommon

(>1/1,000 to <1/100)

Rare

(>1/10,000 to <1/1,000)

Very rare (<1/10,000)

Unknown

Infections and infestations

Respiratory tract infection, urinary tract infection

Blood and the lymphatic system disorders

Leukopenia, thrombo-cytopenia

Immune system disorders

Allergic drug reaction

Metabolism and nutrition disorders

Anorexia, Gout,increased appetite

Psychiatric disorders

Anxiety, depression, insomnia

Agitation, nervousness

Nervous system disorders

Dizziness, headache, somnolence

Cerebrovascular accident, hypoesthesia, syncope, tremor

Dizziness postural, paresthesia

Eye disorders

Blurred vision

Introperative floppy iris syndrome

Ear and labyrinth disorders

Vertigo

Tinnitus

Cardiac disorders

Palpitation, tachycardia

Angina pectoris, myocardial infarction

Bradycardia, cardiac arrhythmias

Vascular disorders

Hypotension, postural hypotension

Flush

Respiratory, thoracic and mediastinal disorders

Bronchitis, cough, dyspnea, rhinitis

Epistaxis

Bronchospasm

Gastrointestinal disorders

Abdominal pain, dyspepsia, dry mouth, nausea,

Constipation, diarrhoea flatulence, vomiting, gastroenteritis,

Taste disturbances

Hepato-biliary disorders

Abnormal liver function tests

Cholestasis, hepatitis, jaundice,

Skin and subcutaneous tissue disorders

Pruritus

Skin rash

Alopecia, purpura urticaria,

Musculoskeletal, connective tissue and bone disorders

Back pain, myalgia

Arthralgia,

Muscle cramps, muscle weakness

Renal and urinary disorders

Cystitis, urinary incontinence

Dysuria, hematuria, micturition frequency

Micturition disorder, nocturia polyuria Increased diuresis

Reproductive system and breast disorders

Impotence

Gynecomastia, priapism

Retrograde ejaculation

General disorders and administration site conditions

Asthenia, chest pain, influenza-like symptoms, peripheral oedema,

Pain, facial oedema

Fatigue, malaise,

Investigations

Weight increase

Overdose

The information provided in Overdose of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Overdose in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Should overdosage lead to hypotension, the patient should be immediately placed in a supine, head down position. Other supportive measures should be performed if thought appropriate in individual cases. Since Lafedoxin is highly protein bound, dialysis is not indicated.

Pharmacodynamic properties

The information provided in Pharmacodynamic properties of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Pharmacodynamic properties in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Pharmacotherapeutic group: Alpha-adrenoceptor antagonists

ATC code: C02CA04

Hypertension:

Administration of Lafedoxin in hypertensive patients causes a clinically significant reduction in blood pressure as a result of a reduction in systemic vascular resistance. This effect is thought to result from selective blockade of the alpha-1-adrenoceptors located in the vasculature. With once daily dosing, clinically significant reductions in blood pressure are present throughout the day and at 24-hours post dose. The majority of patients are controlled on the initial dose of 4 mg Lafedoxin. In patients with hypertension, the decrease in blood pressure during treatment with Lafedoxin was similar in both the sitting and standing position.

Patients treated with immediate release Lafedoxin tablets against hypertension can be transferred to Lafedoxin prolonged-release and the dose titrated upwards as needed, while maintaining effect and tolerability.

Habituation has not been observed during long-term treatment with Lafedoxin. Increase in plasma renin activity and tachycardia have rarely been seen during long-term treatment.

Lafedoxin has a beneficial effect on blood lipids with significant increase of HDL/total cholesterol ratio (app. 4-13% of base line values), and significant reduction in total glycerides and total cholesterol. The clinical relevance of these findings is still unknown.

Treatment with Lafedoxin has been shown to result in regression of left ventricular hypertrophy, inhibition of platelet aggregation as well as enhanced capacity of tissue plasminogen-activator. The clinical relevance of these findings is still uncertain.

Additionally, Lafedoxin improves insulin sensitivity in patients with impaired sensitivity to insulin, but also concerning this finding the clinical relevance is still uncertain.

Lafedoxin has shown to be free of metabolic adverse effects and is suitable for treatment of patients with coexistent asthma, diabetes, left ventricular dysfunction or gout.

Prostatic hyperplasia:

Administration of Lafedoxin to patients with prostatic hyperplasia results in a significant improvement in urodynamics and symptoms as a result of a selective blockade of alpha-adrenoceptors located in the prostatic muscular stroma, capsule and bladder neck.

Most of the patients with prostatic hyperplasia are controlled with the initial dose.

Lafedoxin has shown to be an effective blocker of 1A subtype of alpha-adrenoceptors which make up more than 70% of the adrenergic subtypes in prostate.

Throughout the recommended dosage range, Lafedoxin has only a minor or no effect on blood pressure in normotensive benign prostatic hyperplasia (BPH) patients.

Pharmacokinetic properties

The information provided in Pharmacokinetic properties of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Pharmacokinetic properties in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Absorption:

After oral administration of therapeutic doses, Lafedoxin in Cardozin XL 4mg Prolonged-release Tablets and associated names is well absorbed with peak blood levels gradually reached at 6 to 8 hours after dosing. Peak plasma levels are approximately one third of those of the same dose of immediate release Lafedoxin tablets. Trough levels at 24 hours are, however, similar. The pharmacokinetic properties of Lafedoxin lead to a minor variation in plasma levels. Peak/trough ratio of Lafedoxin prolonged-release is less than half that of immediate release Lafedoxin tablets.

At steady-state, the relative bioavailability of Lafedoxin from Lafedoxin prolonged-release compared to immediate release form was 54% at the 4 mg dose and 59% at the 8 mg dose.

Distribution:

App. 98% of Lafedoxin is protein-bound in plasma.

Biotransformation:

Lafedoxin is extensively metabolised with <5% excreted as unchanged product.

Lafedoxin is primarily metabolised by O-demethylation and hydroxylation.

Elimination:

The plasma elimination is biphasic with the terminal elimination half-life being 22 hours and hence this provides the basic for once daily dosing

Elderly:

Pharmacokinetic studies with Lafedoxin in the elderly have shown no significant alterations compared to younger patients.

Renal impairment:

Pharmacokinetic studies with Lafedoxin in patients with renal impairment also showed no significant alterations compared to patients with normal renal function.

Liver impairment:

There are only limited data in patients with liver impairment and on the effects of medicinal products known to influence hepatic metabolism (e.g. cimetidine). In a clinical study in 12 subjects with moderate hepatic impairment, single dose administration of Lafedoxin resulted in an increase of AUC of 43% and a decrease in oral clearance of app. 40%. Lafedoxin therapy in patients with hepatic impairment should be performed with caution.

Pharmacotherapeutic group

The information provided in Pharmacotherapeutic group of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Pharmacotherapeutic group in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Alpha-adrenoceptor antagonists

Preclinical safety data

The information provided in Preclinical safety data of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Preclinical safety data in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity and carcinogenicity. Studies in pregnant rabbits and rats at daily doses resulting in plasma concentrations 4 and 10 times the human exposure (Cmax and AUC), respectively, revealed no evidence of harm to the foetus. A dosage regime of 82 mg/kg/day (8 times the human exposure) was associated with reduced foetal survival.

Studies in lactating rats given a single oral dose of radioactive Lafedoxin gave an accumulation in the breast milk with a maximum concentration of about 20 times greater than the maternal plasma concentration. Radioactivity was found to cross the placenta following oral administration of labelled Lafedoxin to pregnant rats

Incompatibilities

The information provided in Incompatibilities of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Incompatibilities in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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Not applicable

Special precautions for disposal and other handling

The information provided in Special precautions for disposal and other handling of Lafedoxin is based on data of another medicine with exactly the same composition as the Lafedoxin of the medicine (Doxazosin). Be careful and be sure to specify the information on the section Special precautions for disposal and other handling in the instructions to the drug Lafedoxin directly from the package or from the pharmacist at the pharmacy.
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No special requirements.

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