nadolol.txt

CLINICAL USE

Beta-adrenoceptor blocker:Hypertension Angina Arrhythmias Migraine Thyrotoxicosis

DOSE IN NORMAL RENAL FUNCTION

Hypertension: 80–240 mg per day Angina, arrhythmias, migraine: 40–160 mg dailyThyrotoxicosis: 80–160 mg daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :309.4

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :30

%Excreted unchanged in urine &nbsp &nbsp : 73

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1.9

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :12–24/45

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Start with low dose and increase according to response

10 to 20 &nbsp &nbsp : Start with low dose and increase according to response

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start with low dose and increase according to response

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

HDF/high flux &nbsp :Dialysed. Dose as in GFR

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Dialysed. Dose as in GFR=10–20 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 MAOIsAntihypertensives; 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 mefloquineAntipsychotics 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 dobutamineTropisetron: increased risk of ventricular arrhythmias – use with caution

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

SPC guidelines for increasing dosing interval for patients with renal impairment may be impractical with respect to patient complianceUnlike most other beta-blockers, nadolol is not metabolised and is excreted unchanged mainly by the kidneys.

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