lBREAST FEEDINGManufacturer advises avoidance.
lRENAL IMPAIRMENTManufacturer advises caution.
lDIRECTIONS FOR ADMINISTRATIONGive through a central
venous catheter; incompatible with bicarbonate.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug.
Solution for injection
▶Esmolol hydrochloride (Non-proprietary)
Esmolol hydrochloride 10 mg per 1 mlEsmolol hydrochloride
100 mg/ 10 ml solution for injection vials| 5 vialP£ 38. 95 (Hospital
only)
▶Brevibloc(Baxter Healthcare Ltd)
Esmolol hydrochloride 10 mg per 1 mlBrevibloc Premixed
100 mg/ 10 ml solution for injection vials| 5 vialPs
Solution for infusion
▶Brevibloc(Baxter Healthcare Ltd)
Esmolol hydrochloride 10 mg per 1 mlBrevibloc Premixed
2. 5 g/ 250 ml infusion bags| 1 bagP£ 89. 69
eiiiiF 103
Metoprolol tartrate
lINDICATIONS AND DOSE
Hypertension
▶BY MOUTH USING IMMEDIATE-RELEASE MEDICINES
▶Child 1 month–11 years:Initially 1 mg/kg twice daily,
increased if necessary up to 8 mg/kg daily in
2 – 4 divided doses (max. per dose 400 mg)
▶Child 12–17 years:Initially 50 – 100 mg daily, increased if
necessary to 200 mg daily in 1 – 2 divided doses, high
doses are rarely necessary; maximum 400 mg per day
▶BY MOUTH USING MODIFIED-RELEASE MEDICINES
▶Child 12–17 years: 200 mg once daily
Arrhythmias
▶BY MOUTH USING IMMEDIATE-RELEASE MEDICINES
▶Child 12–17 years:Usual dose 50 mg 2 – 3 times a day,
then increased if necessary up to 300 mg daily in
divided doses
lUNLICENSED USENot licensed for use in children.
lINTERACTIONS→Appendix 1 : beta blockers, selective
lSIDE-EFFECTS
▶Common or very commonPalpitations
▶UncommonChest pain.drowsiness.dystrophic skin lesion
.insomnia.muscle cramps.oedema.weight increased
▶Rare or very rareAlertness decreased.arthritis.auditory
disorder.cardiac conduction disorder.conjunctivitis.eye
irritation.gangrene.hepatitis.personality disorder.
rhinitis
▶Frequency not knownPeyronie’s disease.retroperitoneal
fibrosis
lHEPATIC IMPAIRMENT
Dose adjustmentsReduce dose in severe impairment.
lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug. Forms available from special-order
manufacturers include: capsule, oral suspension, oral solution
Tablet
CAUTIONARY AND ADVISORY LABELS 8
▶Metoprolol tartrate (Non-proprietary)
Metoprolol tartrate 50 mgMetoprolol 50 mg tablets|
28 tabletP£ 3. 00 DT = £ 0. 69 | 56 tabletP£ 1. 38 – £ 1. 80
Metoprolol tartrate 100 mgMetoprolol 100 mg tablets|
28 tabletP£ 3. 00 DT = £ 0. 76 | 56 tabletP£ 1. 52 – £ 1. 78
Solution for injection
▶Betaloc(AstraZeneca UK Ltd)
Metoprolol tartrate 1 mg per 1 mlBetaloc I.V. 5 mg/ 5 ml solution for
injection ampoules| 5 ampouleP£ 5. 02 (Hospital only)
CALCIUM-CHANNEL BLOCKERS
Calcium-channel blockers
Overview
Calcium-channel blockers differ in their predilection for the
various possible sites of action and, therefore, their
therapeutic effects are disparate, with much greater
variation than those of beta-blockers. There are important
differences between verapamil hydrochloride p. 110 ,
diltiazem hydrochloride p. 144 , and the dihydropyridine
calcium-channel blockers (amlodipine p. 108 , nicardipine
hydrochloride p. 108 , nifedipine p. 109 , and nimodipine
p. 87 ). Verapamil hydrochloride and diltiazem hydrochloride
should usually beavoidedin heart failure because they may
further depress cardiac function and cause clinically
significant deterioration.
Verapamil hydrochloride is used for the treatment of
hypertension and arrhythmias. However, it is no longerfirst-
line treatment for arrhythmias in children because it has
been associated with fatal collapse especially in infants
under 1 year; adenosine p. 79 is now recommended forfirst-
line use.
Verapamil hydrochloride is a highly negatively inotropic
calcium channel-blocker and it reduces cardiac output, slows
the heart rate, and may impair atrioventricular conduction.
It may precipitate heart failure, exacerbate conduction
disorders, and cause hypotension at high doses and should
notbe used with beta-blockers. Constipation is the most
common side-effect.
Nifedipine relaxes vascular smooth muscle and dilates
coronary and peripheral arteries. It has more influence on
vessels and less on the myocardium than does verapamil
hydrochloride and unlike verapamil hydrochloride has no
anti-arrhythmic activity. It rarely precipitates heart failure
because any negative inotropic effect is offset by a reduction
in left ventricular work. Short-acting formulations of
nifedipine may be used if a modified-release preparation
delivering the appropriate dose is not available or if a child is
unable to swallow (a liquid preparation may be prepared
using capsules). Nifedipine may also be used for the
management of angina due to coronary artery disease in
Kawasaki disease or progeria and in the management of
Raynaud’s syndrome.
Nicardipine hydrochloride has similar effects to those of
nifedipine and may produce less reduction of myocardial
contractility; it should only be used for the treatment of life-
threatening hypertension in paediatric intensive care
settings and in postoperative hypertension.
Amlodipine also resembles nifedipine and nicardipine
hydrochloride in its effects and does not reduce myocardial
contractility or produce clinical deterioration in heart
failure. It has a longer duration of action and can be given
once daily. Nifedipine and amlodipine are used for the
treatment of hypertension. Side-effects associated with
vasodilatation such asflushing and headache (which become
less obtrusive after a few days), and ankle swelling (which
may respond only partially to diuretics) are common.
Nimodipine is related to nifedipine but the smooth muscle
relaxant effect preferentially acts on cerebral arteries. Its use
is confined to prevention and treatment of vascular spasm
following aneurysmal subarachnoid haemorrhage.
Diltiazem hydrochloride is a peripheral vasodilator and
also has mild depressor effects on the myocardium. It is used
in the treatment of Raynaud’s syndrome.
BNFC 2018 – 2019 Hypertension 107
Cardiovascular system
2