Timolol Maleate (Page 4 of 4)

Potential Adverse Effects

In addition, a variety of adverse effects not observed in clinical trials with timolol maleate, but reported with other beta-adrenergic blocking agents, should be considered potential adverse effects of timolol. 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 timolol.

Clinical Laboratory Test Findings

Clinically important changes in standard laboratory parameters were rarely associated with the administration of timolol. 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.

OVERDOSAGE

Overdosage has been reported with timolol maleate tablets. A 30 year old female ingested 650 mg of timolol maleate (maximum recommended daily dose — 60 mg) and experienced second- and third-degree heart block. She recovered without treatment but approximately 2 months later developed irregular heart beat, hypertension, dizziness, tinnitus, faintness, increased pulse rate and borderline first degree heart block.

The oral LD50 of the drug is 1190 and 900 mg/kg in female mice and female rats, respectively.

An in vitro hemodialysis study, using 14 C timolol added to human plasma or whole blood, showed that timolol was readily dialyzed from these fluids; however, a study of patients with renal failure showed that timolol did not dialyze readily.

The most common signs and symptoms to be expected with overdosage with a beta-adrenergic receptor blocking agent are symptomatic bradycardia, hypotension, bronchospasm, and acute cardiac failure. Therapy with timolol should be discontinued and the patient observed closely. The following additional therapeutic measures should be considered:

(1) Gastric lavage.
(2) Symptomatic bradycardia: Use atropine sulfate intravenously in a dosage of 0.25 mg to 2 mg to induce vagal blockade. If bradycardia persists, intravenous isoproterenol hydrochloride should be administered cautiously. In refractory cases the use of a transvenous cardiac pacemaker may be considered.
(3) Hypotension: Use sympathomimetic pressor drug therapy, such as dopamine, dobutamine or norepinephrine. In refractory cases the use of glucagon hydrochloride has been reported to be useful.
(4) Bronchospasm: Use isoproterenol hydrochloride. Additional therapy with aminophylline may be considered.
(5) Acute cardiac failure: Conventional therapy with digitalis, diuretics, and oxygen should be instituted immediately. In refractory cases the use of intravenous aminophylline is suggested. This may be followed if necessary by glucagon hydrochloride which has been reported to be useful.
(6) Heart block (second- or third-degree): Use isoproterenol hydrochloride or a transvenous cardiac pacemaker.

DOSAGE AND ADMINISTRATION

Hypertension

The usual initial dosage of timolol maleate 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 to 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 7 days between increases in dosages.

Timolol maleate tablets 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 timolol maleate 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 to 8 weeks use of the maximum daily dosage, therapy with timolol should be discontinued.

HOW SUPPLIED

Timolol Maleate Tablets, USP are available containing 5 mg, 10 mg and 20 mg of timolol maleate, USP.

The 5 mg tablets are green, unscored, flat-faced round tablets debossed with M over 55 on one side of the tablet and blank on the other side. They are available as follows:

NDC 0378-0055-01
bottles of 100 tablets

NDC 69189-0496-1 single dose pack with 1 tablet as repackaged by Avera McKennan Hospital

Store at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]

Protect from light.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Keep container tightly closed.

Mylan Pharmaceuticals Inc.
Morgantown, WV 26505

REVISED AUGUST 2006

TIM:R15

Principal Display Panel

Timolol Maleate 5 mg tablets
(click image for full-size original)

TIMOLOL MALEATE
timolol maleate tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:69189-0496(NDC:0378-0055)
Route of Administration ORAL DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
TIMOLOL MALEATE (TIMOLOL ANHYDROUS) TIMOLOL ANHYDROUS 5 mg
Inactive Ingredients
Ingredient Name Strength
SILICON DIOXIDE
CROSCARMELLOSE SODIUM
MAGNESIUM STEARATE
CELLULOSE, MICROCRYSTALLINE
STARCH, CORN
SODIUM LAURYL SULFATE
FD&C BLUE NO. 2
D&C YELLOW NO. 10
Product Characteristics
Color GREEN Score no score
Shape ROUND Size 6mm
Flavor Imprint Code M;55
Contains
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:69189-0496-1 1 TABLET in 1 DOSE PACK None
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA072668 01/27/2016
Labeler — Avera McKennan Hospital (068647668)
Establishment
Name Address ID/FEI Operations
Avera McKennan Hospital 068647668 relabel (69189-0496), repack (69189-0496)

Revised: 03/2017 Avera McKennan Hospital

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