Blocadren

Blocadren is part of the drug class:

• Beta blocking agents, non selective

In the U.S.

• Blocadren

Available Dosage Forms:

• Tablet

Therapeutic Class: Cardiovascular Agent

Pharmacologic Class: Beta-Adrenergic Blocker, Nonselective

Timolol is used alone or together with other medicines (such as hydrochlorothiazide) to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled .

Timolol is also used after an acute heart attack to decrease its severity and prevent another heart attack. It may also be used to help prevent migraine headaches .

This medicine is a beta-blocker. It works by affecting the response to nerve impulses in certain parts of the body, like the heart. As a result, the heart beats slower and decreases the blood pressure. When the blood pressure is lowered, the amount of blood and oxygen is increased to the heart .

This medicine is available only with your doctor's prescription .

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects .

Timolol may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort; dilated neck veins; extreme fatigue; irregular breathing; an irregular heartbeat; shortness of breath; swelling of the face, fingers, feet, or lower legs; weight gain; or wheezing .

This medicine may cause changes in your blood sugar levels. Also, this medicine may cover up signs of low blood sugar, such as a rapid pulse rate. Check with your doctor if you have these problems or if you notice a change in the results of your blood or urine sugar tests .

Make sure any doctor or dentist who treats you knows that you are using this medicine. You may need to stop using this medicine several days before having surgery .

Blocadren is contraindicated in patients with bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS); sinus bradycardia; second and third degree atrioventricular block; overt cardiac failure (see WARNINGS); cardiogenic shock; hypersensitivity to this product.

Blocadren is usually well tolerated in properly selected patients. Most adverse effects have been mild and transient.

In a multicenter (12-week) clinical trial comparing timolol maleate and placebo in hypertensive patients, the following adverse reactions were reported spontaneously and considered to be causally related to timolol maleate:

These data are representative of the incidence of adverse effects that may be observed in properly selected patients treated with Blocadren, i.e., excluding patients with bronchospastic disease, congestive heart failure or other contraindications to beta blocker therapy.

In patients with migraine the incidence of bradycardia was 5 percent.

In a coronary artery disease population studied in the Norwegian multi-center trial (see CLINICAL PHARMACOLOGY), the frequency of the principal adverse reactions and the frequency with which these resulted in discontinuation of therapy in the timolol and placebo groups were:

The following additional adverse effects have been reported in clinical experience with the drug: Body as a Whole: anaphylaxis,extremity pain, decreased exercise tolerance, weight loss, fever; Cardiovascular: cardiac arrest, cardiac failure, cerebral vascular accident, worsening of angina pectoris, worsening of arterial insufficiency, Raynaud's phenomenon, palpitations, vasodilatation; Digestive: gastrointestinal pain, hepatomegaly, vomiting, diarrhea, dyspepsia; Hematologic:nonthrombocytopenic purpura; Endocrine: hyperglycemia, hypoglycemia; Skin:rash, skin irritation, increased pigmentation, sweating, alopecia; Musculoskeletal: arthralgia; Nervous System: local weakness, increase in signs and symptoms of myasthenia gravis; Psychiatric: depression, nightmares, somnolence, insomnia, nervousness, diminished concentration, hallucinations; Respiratory: cough; Special Senses: visual disturbances, diplopia, ptosis, dry eyes; Urogenital: impotence, urination difficulties.

There have been reports of retroperitoneal fibrosis in patients receiving timolol maleate and in patients receiving other beta-adrenergic blocking agents. A causal relationship between this condition and therapy with beta-adrenergic blocking agents has not been established.

Potential Adverse Effects: In addition, a variety of adverse effects not observed in clinical trials with Blocadren, but reported with other beta-adrenergic blocking agents, should be considered potential adverse effects of Blocadren: Nervous System: Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics; Cardiovascular:Intensification of AV block (see CONTRAINDICATIONS); Digestive: Mesenteric arterial thrombosis, ischemic colitis; Hematologic: Agranulocytosis, thrombocytopenic purpura; Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm with respiratory distress; Miscellaneous: Peyronie's disease.

There have been reports of a syndrome comprising psoriasiform skin rash, conjunctivitis sicca, otitis, and sclerosing serositis attributed to the beta-adrenergic receptor blocking agent, practolol. This syndrome has not been reported with Blocadren.

Clinical Laboratory Test Findings: Clinically important changes in standard laboratory parameters were rarely associated with the administration of Blocadren. Slight increases in blood urea nitrogen, serum potassium, uric acid, and triglycerides, and slight decreases in hemoglobin, hematocrit and HDL cholesterol occurred, but were not progressive or associated with clinical manifestations. Increases in liver function tests have been reported.

Hypertension

The usual initial dosage of Blocadren is 10 mg twice a day, whether used alone or added to diuretic therapy. Dosage may be increased or decreased depending on heart rate and blood pressure response. The usual total maintenance dosage is 20-40 mg per day. Increases in dosage to a maximum of 60 mg per day divided into two doses may be necessary. There should be an interval of at least seven days between increases in dosages.

Blocadren may be used with a thiazide diuretic or with other antihypertensive agents. Patients should be observed carefully during initiation of such concomitant therapy.

Myocardial Infarction

The recommended dosage for long-term prophylactic use in patients who have survived the acute phase of a myocardial infarction is 10 mg given twice daily (see CLINICAL PHARMACOLOGY).

Migraine

The usual initial dosage of Blocadren is 10 mg twice a day. During maintenance therapy the 20 mg daily dosage may be administered as a single dose. Total daily dosage may be increased to a maximum of 30 mg, given in divided doses, or decreased to 10 mg once per day, depending on clinical response and tolerability. If a satisfactory response is not obtained after 6-8 weeks use of the maximum daily dosage, therapy with Blocadren should be discontinued.

No. 3343 Tablets Blocadren, 5 mg, are light blue, round, compressed tablets, with code MSD 59 on one side and Blocadren on the other. They are supplied as follows:

NDC 0006-0059-68 bottles of 100.

No. 3344 Tablets Blocadren, 10 mg, are light blue, round, scored, compressed tablets, with code MSD 136 on one side and Blocadren on theother. They are supplied as follows:

NDC 0006-0136-68 bottles of 100

No. 3371 Tablets Blocadren, 20 mg, are light blue, capsule shaped, scored, compressed tablets, with code MSD 437 on one side and Blocadren on the other. They are supplied as follows:

NDC 0006-0437-68 bottles of 100

Storage

Store at controlled room temperature, 15-30°C (59-86°F). Keep container tightly closed. Protect from light.

MERCK & CO., INC., Whitehouse Station, NJ 08889, USA

Issued March 2002

Printed in USA

7901233