INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo CARDURA 1 mg Tablets
CARDURA 2 mg Tablets
CARDURA 4 mg Tablets
Doxazosin mesylate
Cardura
Tablets

        S3
        Prescription
        Required

SCHEDULING STATUS
Schedule 3.

PROPRIETARY NAMES
(and dosage form)

CARDURA 1 mg Tablets
CARDURA 2 mg Tablets
CARDURA 4 mg Tablets

COMPOSITION
Doxazosin mesylate is a quinazoline derivative, having the chemical name:
1-(4-amino-6, 7-dimethoxy-2-quinazolinyl )-4-(1, 4-benzodioxan-2-yl-carbonyl)piperazine methanesulphonate. It is a white powder, slightly soluble in methanol and sparingly soluble in water, ethanol, acetone and chloroform, and has a molecular weight of 547,6 (free base 451,5).
Each 1 mg, 2 mg and 4 mg Cardura tablet contains doxazosin mesylate equivalent to 1 mg, 2 mg, 4 mg free base respectively.
Cardura tablets contain the following inert ingredients: Sodium starch glycolate, microcrystalline cellulose, lactose, magnesium stearate, sodium lauryl sulphate.

PHARMACOLOGICAL CLASSIFICATION
A.7.1 Vasodilators, hypotensive medicines.

PHARMACOLOGICAL ACTION
Cardura exerts a vasodilator effect via selective and competitive blockade of post-junctional alpha 1-adrenoceptors.
Cardura has been shown to block the 1A subtype of the alpha-1-adrenoceptor which accounts for over 70% of the subtypes in the prostate.
After oral administration, Cardura is well absorbed with peak blood levels occurring at about 2 hours. The plasma elimination is biphasic with the terminal elimination half life being 19 to 22 hours, hence providing the basis for once daily dosing. Cardura is extensively metabolised with less than 5% excreted as the unchanged drug.
Maximum reduction in blood pressure normally occurs about 6 hours after dosing.
Most (98%) of plasma doxazosin is protein bound. In vitro data in human plasma indicates that Cardura has no effect on protein binding of the drugs tested (digoxin, phenytoin, warfarin or indomethacin).

INDICATIONS
Hypertension
Cardura is indicated for the treatment of mild to moderate hypertension.
Benign Prostatic Hyperplasia
Cardura is also indicated for the treatment of the urinary outflow obstruction and symptoms associated with benign prostatic hyperplasia (BPH). Cardura may be used in BPH patients who are either hypertensive or normotensive.

CONTRA-INDICATIONS
Cardura is contra-indicated in patients with a known hypersensitivity to quinazolines.
Use During Pregnancy and Lactation
Use during pregnancy or lactation has not yet been established.
Use for Children
No experience is available on usage of Cardura in children.

DOSAGE AND DIRECTIONS FOR USE
Hypertension
The initial dosage of Cardura is 1 mg given once daily. Depending on the individual patient's response, dosage may then be increased after 1-2 weeks of therapy to 2 mg and thereafter at similar intervals to 4 mg, 8 mg and 16 mg to achieve the desired reduction in blood pressure. In patients not adequately controlled on a single antihypertensive agent, Cardura may be used in combination with a thiazide diuretic or a beta-blocking agent.
Benign Prostatic Hyperplasia
The initial dosage of Cardura is 1 mg given once daily. Depending on the individual patient's urodynamics and BPH symptomatology, dosage may then be increased to 2 mg and thereafter to 4 mg and up to the maximum recommended dose of 8 mg. The recommended titration interval is 1-2 weeks. The usual recommended dose is 2-4 mg once daily. Blood pressure should be evaluated routinely in these patients.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
The most common reactions associated with Cardura therapy are dizziness, headache, fatigue, postural dizziness, vertigo, hypotension, oedema and asthenia. Other side-effects include abnormal vision, chest pain, depression, diarrhoea, dry mouth, dyspnoea, insomnia, nausea, nervousness, palpitation, rash, rhinitis, sexual dysfunction, somnolence, tachycardia and malaise.
Extremely rare cases of urinary incontinence were reported; this effect may be related to Cardura's pharmacological action.
Cases of priapism and impotence have been reported in association with Cardura.
The following have been reported in post-marketing experience: angina pectoris, myocardial infarction, cerebrovascular accidents, cardiac arrythmias and blurred vision. Rare cases of non-specific gastric complaints such as abdominal pain, diarrhoea and vomiting and rare cases of agitation and tremor have also been reported. Cases such as skin rashes, pruritis, thrombocytopenia, purpura, epistaxis, leukopenia, hematuria, cholestasis, hepatitis, jaundice and abormal liver function tests have also been reported.
Driving/Use of Machinery
The ability to engage in activities such as operating machinery or operating a motor vehicle may be impaired especially when initiating therapy.
Impaired Liver Function
Special precaution must be taken in patients with impaired liver function.
Interactions
No adverse drug interaction has been noted in clinical experience to date with thiazide diuretics, frusemide, beta-blocking agents, antibiotics, oral hypoglycaemic drugs, uricosuric agents or anticoagulants.
Administration of doxazosin may reduce plasma concentrations of triglycerides, total and LDL-cholestrol and increase HDL-cholestrol. These potentially favourable effects on lipids persist when a thiazide-type diuretic is given concurrently. The long-term consequences of these drug-induced changes in lipids are not known.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Since Cardura is highly protein bound, dialysis is not indicated. Treatment is symptomatic and supportive.

IDENTIFICATION
1 mg Tablet:        A white, round, biconvex tablet, embossed CN1 on one side and the Pfizer logo on the reverse.
2 mg Tablet: A white, oblong tablet embossed CN2 on one side and the Pfizer logo on the reverse.
4 mg Tablet: A white, rhombic tablet, embossed CN4 on one side and the Pfizer logo on the reverse.

PRESENTATION
1 mg Tablet:         Packs of 30
2 mg Tablet:         Packs of 30
4 mg Tablet:         Packs of 30

STORAGE INSTRUCTIONS
Store below 30°C. Protect from light. Keep out of reach of children.

REGISTRATION NUMBERS
1 mg Tablet:         U/7.1/68
2 mg Tablet:         U/7.1/69
4 mg Tablet:         U/7.1/70

NAME AND BUSINESS ADDRESS OF APPLICANT
Pfizer Laboratories (Pty) Limited
102 Rivonia Road
SANDTON
2196

DATE OF PUBLICATION OF THIS PACKAGE INSERT
13 March 1998

Updated on this site: February 2005
Source: Pharmaceutical Industry

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