Timolol maleate.txt

CLINICAL USE

Beta-adrenoceptor blocker: Hypertension Angina Glaucoma Migraine prophylaxis

DOSE IN NORMAL RENAL FUNCTION

Hypertension: 10–60 mg daily, doses >30 mg in divided doses Angina: 5–30 mg twice daily Post MI: 5–10 mg twice daily Migraine:

10 to 20 &nbsp &nbsp : mg daily in 1–2 divided doses

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 432.5

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 10

%Excreted unchanged in urine &nbsp &nbsp : 5

Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 1.7

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : 4/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function. Start with lowest dose and titrate according to response

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Start with lowest dose and titrate according to response

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp: Not dialysed. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp : Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp: Unknown dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect

Analgesics: NSAIDs antagonise hypotensive effect

Anti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodarone

Antidepressants: enhanced hypotensive effect with MAOIs Antihypertensives: enhanced hypotensive effect; increased risk of withdrawal hypertension with clonidine; increased risk of first dose hypotensive effect with post-synaptic alpha-blockers such as prazosin

Antimalarials: increased risk of bradycardia with mefloquine Antipsychotics enhanced hypotensive effect with phenothiazines

Calcium-channel blockers: increased risk of bradycardia and AV block with diltiazem; hypotension and heart failure possible with nifedipine and nisoldipine; asystole, severe hypotension and heart failure with verapamil

Diuretics: enhanced hypotensive effect

Moxisylyte: possible severe postural hypotension

Sympathomimetics: severe hypertension with adrenaline and noradrenaline and possibly with dobutamine Tropisetron: increased risk of ventricular arrhythmias – use with caution

ADMINISTRATION

Reconstition

–

Route

Oral, topical

Rate of Administration

–

Comments

–

OTHER INFORMATION

Timolol is more hydrophilic than lipophilic

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