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BLOCADREN®
(timolol maleate)
BLOCADREN (Timolol Maleate) is a non-selective beta-adrenergic receptor blocking agent. The chemical name for timolol maleate is (S)-1-[(1,1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol (Z)-2-butenedioate (1:1) salt. It possesses an asymmetric carbon atom in its structure and is provided as the levo isomer. Its empirical formula is C13H24N4O3S•C4H4O4 and its structural formula is:
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Timolol maleate has a molecular weight of 432.50. It is a white, odorless, crystalline powder which is soluble in water, methanol, and alcohol.
BLOCADREN (timolol) is supplied as tablets in three strengths containing 5 mg, 10 mg or 20 mg timolol maleate for oral administration. Inactive ingredients are cellulose, FD&C Blue 2, magnesium stearate, and starch.
BLOCADREN (timolol) is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics.
BLOCADREN (timolol) is indicated in patients who have survived the acute phase of myocardial infarction, and are clinically stable, to reduce cardiovascular mortality and the risk of reinfarction.
BLOCADREN (timolol) is indicated for the prophylaxis of migraine headache.
The usual initial dosage of BLOCADREN (timolol) 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 (timolol) may be used with a thiazide diuretic or with other antihypertensive agents. Patients should be observed carefully during initiation of such concomitant therapy.
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).
The usual initial dosage of BLOCADREN (timolol) 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 (timolol) should be discontinued.
No. 3343 — Tablets BLOCADREN (timolol) , 5 mg, are light blue, round, compressed tablets, with code MSD 59 on one side and BLOCADREN (timolol) on the other. They are supplied as follows:
NDC 0006-0059-68 bottles of 100.
No. 3344 — Tablets BLOCADREN (timolol) , 10 mg, are light blue, round, scored, compressed tablets, with code MSD 136 on one side and BLOCADREN (timolol) on the other. They are supplied as follows:
NDC 0006-0136-68 bottles of 100
No. 3371 — Tablets BLOCADREN (timolol) , 20 mg, are light blue, capsule shaped, scored, compressed tablets, with code MSD 437 on one side and BLOCADREN (timolol) on the other. They are supplied as follows:
NDC 0006-0437-68 bottles of 100
Store at controlled room temperature, 15-30°C (59-86°F). Keep container tightly closed. Protect from light.
MERCK AND CO., INC., Whitehouse Station, NJ 08889, USA. Issued April 2001. FDA Rev date: 2/25/2003
BLOCADREN (timolol) 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:
| Timolol Maleate (n = 176) % |
Placebo (n = 168) % |
|
| BODY AS A WHOLE | ||
| fatigue/tiredness | 3.4 | 0.6 |
| headache | 1.7 | 1.8 |
| chest pain | 0.6 | 0 |
| asthenia | 0.6 | 0 |
| CARDIOVASCULAR | ||
| bradycardia | 9.1 | 0 |
| arrhythmia | 1.1 | 0.6 |
| syncope | 0.6 | 0 |
| edema | 0.6 | 1.2 |
| DIGESTIVE | ||
| dyspepsia | 0.6 | 0.6 |
| nausea | 0.6 | 0 |
| SKIN | ||
| pruritus | 1.1 | 0 |
| NERVOUS SYSTEM | ||
| dizziness | 2.3 | 1.2 |
| vertigo | 0.6 | 0 |
| paresthesia | 0.6 | 0 |
| PSYCHIATRIC | ||
| decreased libido | 0.6 | 0 |
| RESPIRATORY | ||
| dyspnea | 1.7 | 0.6 |
| bronchial spasm | 0.6 | 0 |
| rales | 0.6 | 0 |
| SPECIAL SENSES | ||
| eye irritation | 1.1 | 0.6 |
| tinnitus | 0.6 | 0 |
These data are representative of the incidence of adverse effects that may be observed in properly selected patients treated with BLOCADREN (timolol) , 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
| Adverse Reaction*** | Withdrawal† | |||
| Timolol (n=945) % |
Placebo (n=939) % |
Timolol (n=945) % |
Placebo (n=939) % |
|
| Asthenia or Fatigue | 5 | 1 | ||
