664
P A R T 8
Drugs acting on the cardiovascular system
TABLE 43.2
DRUGS IN FOCUS Antihypertensive agents
Drug name
Dosage/route
Usual indications
Angiotensin-converting-enzyme (ACE) inhibitors
captopril (Capoten,
Zedace)
50–100 mg PO t.d.s. for heart failure (HF);
50 mg PO t.d.s. for ventricular dysfunction;
25 mg PO t.d.s. for diabetic nephropathy;
reduce dose in people with renal impairment
and in geriatric people
Treatment of left ventricular dysfunction
after myocardial infarction (MI), diabetic
nephropathy; for use in adults
enalapril (Acetec,
Amprace, Renitec)
10–40 mg/day PO; reduce dose in geriatric
people and people with renal impairment;
2.5 mg PO b.d. for HF or left ventricular
dysfunction
Treatment of hypertension, HF, left
ventricular dysfunction in adults
fosinopril (Monace,
Monopril)
10–40 mg/day PO
Treatment of hypertension; adjunct therapy
for HF; for use in adults
lisinopril (Fibsol, Prinivil,
Zestril)
20–40 mg/day PO for hypertension;
5–20 mg/day PO for HF; 5–10 mg/day PO
after MI; decrease dose in geriatric people
and people with renal impairment
Treatment of hypertension, HF; treatment
of stable people within 24 hours after
acute MI to increase survival; for use in
adults
perindopril (Coversyl,
Indopril, Perindo)
4 mg/day PO; reduce dose in geriatric people
and people with renal impairment
Treatment of hypertension; may be used
alone or as combination drug to control
blood pressure; for use in adults
Many people require more than one type of
antihypertensive to achieve good control of their blood
pressure. There are now many fixed-combination drugs
available for treating hypertension. This allows for fewer
tablets or capsules each day, making it easier for the
person to comply with drug therapy. The person should
be stabilised on each drug first, and then an appropriate
combination product can be used.
amlodipine with valsartan (
Exforge
)
amlodipine with valsartan and hydrochlorothiazide
(
Exforge HCT
)
candesartan with hydrochlorothiazide (
Adesan HCT
,
Atacand Plus
)
eprosartan with hydrochlorothiazide (
Teveten Plus
)
fosinopril with hydrochlorthiazide (
Fosetic
,
Hyforil
Monoplus
)
irbesartan with hydrochlorothiazide (
Avapro HCT
,
Karvezide
,
KSART HCT
)
lercanidipine with enalapril (
Zan-Extra
)
olmesartan with amlodipine (
Sevikar
)
olmesartan with hydrochlorothiazide (
Olmetec Plus
)
perindopril with amlodipine (
Coveram
,
Reaptan
)
perindopril with indapamide (
Coversyl Plus
,
Perindo
Combo
,
Indosyl Combi
)
quinapril with hydrochlorothiazide (
Accuretic
)
telmisartan with amlodipine (
Twynsta
)
telmisartan with hydrochlorothiazide (
Micardis Plus
)
trandolapril with verapamil (
Tarka
)
valsartan with hydrochlorothiazide (
Co-Diovan
)
■■
BOX 43.2
Fixed-combination drugs for the
treatment of hypertension
In late 2001, bosentan (
Tracleer
) became the first
endothelin receptor antagonist to be approved for use in
the treatment of pulmonary arterial hypertension. This
drug specifically blocks receptor sites for endothelin
(ET
a
and ET
b
) in the endothelium and vascular smooth
muscles; these endothelins are chemicals that are
elevated in the plasma and lung tissues of people with
pulmonary arterial hypertension. Blockade of these
receptor sites allows the vessels to relax and dilate,
relieving the pressure in the arteries.
Tracleer
is an oral
drug that is given to adults, initially as 62.5 mg PO b.d.
for 4 weeks, and then increased to 125 mg PO b.d. if
the person’s exercise tolerance improves on the drug.
People need to be monitored closely for any change in
their respiratory function, signs of liver toxicity, or signs
of peripheral vasodilation, including flushing, headache,
hypotension and palpitations. The drug is pregnancy
category X and is known to interact with other drugs,
including ketoconazole, the statins, glyburide and oral
contraceptives.
In 2005, sildenafil, a drug known for the treatment
of erectile dysfunction, was approved for the treatment
of pulmonary arterial hypertension.
Revatio
is an oral
drug, with 20 mg given three times a day. The doses
should be at least 4–6 hours apart.
Revatio
inhibits
cGMP; this allows nitrous oxide in the blood vessel to
cause smooth muscle relaxation and decreases vessel
pressure (see Chapter 41).
■■
BOX 43.3
Treatment of pulmonary arterial
hypertension
