Professional Documents
Culture Documents
Angina
pectoris is a characteristic
sudden severe pressing chest pain or
heaviness radiating to the neck, jaw,
back and arms. It is often associated
with diaphoresis, tachypnea and
nausea.
WHAT IS ANGINA???
Angina
Angina
The
Types of Angina
Angina occurs in
three overlapping
patterns:
Stable angina
Unstable angina
Prinzmetal (variant)
angina
Stable Angina
Unstable Angina
Vasospastic Angina
What is antianginal
drugs???
Antianginal drugs are those drugs
which improves the oxygen supply to
myocardium and reduce the oxygen
demand.
Those drugs which are used to treat the
episodes of angina.
Classification of
antianginals
Classification.
Beta-adrenergic blockers
Decrease heart rate and contractility
Decrease afterload 2 to a decrease in cardiac
output
Improve myocardial perfusion 2 to a
decrease in heart rate
Organic nitrates
Organic Nitrates
Effects of Nitrovasodilators
Peripheral vasodilation:
Dilation of veins predominates over that of arterioles
unstable angina
ORGANIC
NITRATES
Requires normal
vascular
endothelium
Diffuses to local
vascular smooth
muscle
Indications
Indications
Cyanide poisoning- Nitrates generate methhemoglobin which
Excreted in
urine
solution IV)
Thiosulphate
mlof
25%
Sod.
(50
Cyanide
has strong affinity for cyanide radical and form cyanomethemoglobin .This
may again dissociate to release cyanide .Therefore sod.thiosulphate is
given to form sod. Thiocyanate which is excreted in urine.
Sod.
Nitrate(10m
l of 3%
solution IV
NITRATES
CONTRAINDICATIONS
Previous hypersensitivity
Constrictive pericarditis
Intracranial hypertension
Hypertrophic cardiomyopathy
Pharmacokinetics
The difference between nitrate preparations
is mainly in time of onset of action.
1. Nitroglycerin suffers marked 1st pass
metabolism so administration is
sublingual (rapid absorption and onset
(<1 minute), t1/2 ~10 minutes.
Occasionally as nitroglycerin is
metabolized anginal symptoms will
return.
Transdermal administration either as
patch or paste provides a depot of agent
for a steady availability. Nitro-Bid is an
oral or topical preparation which
saturates the hepatic catabolic
pathways allowing a prolonged level of
nitroglycerine.
Isosorbide
mononitrate &
isosorbide dinitrate
are long acting
nitrates that are
relatively resistant
to hepatic
catabolism t1/2 ~ 1
hour.
Mechanism of Action
Nitrates decrease myocardial oxygen demand:
1. The primary effect is a reduction in venous tone
which results in venous pooling decreasing
venous return (decreased preload).
2. Arteriolar tone is less effectively reduced resulting
in a decrease in PVR (decreased afterload ) and
decreased blood pressure.
3. #s 1 & 2 decrease myocardial wall stress reducing
O2 demand.
4. Dilation of coronary vessels or exerts a ~minor
effect on increasing O2 supply.
Pharmacokinetic Properties of
Organic Nitrates
Hepatic first-pass metabolism is high and oral
bioavailability is low for nitroglycerin (GTN) and
isosorbide dinitrate (ISDN)
Sublingual or transdermal administration of these agents
Isosorbide mononitrate (ISMN) is not subject to firstpass metabolism and is 100% available after oral
administration
Hepatic blood flow and disease can affect the
pharmacokinetics of GTN and ISDN
Property
Half-life (min)
Plasma clearance (L/min)
Apparent volume of distribution (L/kg)
Oral bioavailability (%)
GTN
ISDN
3
50
3
<1
10
4
4
20
ISMN
280
0.1
0.6
100
Routes of Administration
Dosage
DRUG
DURATION OF ACTION
GTN(nitroglycerine)
0.5mg sublingual
5-15 mg oral
0.4-0.8 mg s.l. spray
10-30 min
4-8 hrs
10-30 min
Isosorbide dinitrate
5-10 mg sublingual
10-20 mg Oral
20-40 mg Oral(SR)
20-40 min
2-3 hrs
6-10 hrs
Isosorbide 5 mononitrate
20-40 mg Oral
6-10 hrs
Erthrityl-tetranitrate
15-60 mg Oral
4-6 hrs
3-5 hrs
8-12 hrs
Adverse Effects of
Nitrovasodilators
Orthostatic hypotension
Tachycardia
Severe throbbing headache
Dizziness
Flushing
Syncope
Adverse effects
1.
2.
3.
4.
5.
-Blockers
MECHANISM OF ACTION
afterload
Some b-blockers can cause vasodilation
directly or by acting as a-blockers
Improve myocardial perfusion by slowing heart rate
angina
Compound
Coronary
vasodilation
Suppression
of cardiac
contractility
Suppression
of
SA node
Suppression
of
AV node
Verapamil
++++
++++
+++++
+++++
Diltiazem
+++
++
+++++
++++
Nifedipine
+++++
Nicardipine
+++++
DOSAGE
Name of
drug
Action
Dose and
route
VERAPAMIL
DILITIAZEM
NIFEDIPINE
5-20 MG ORAL
FELODIPINE
5-10 MG ORAL
AMLODIPINE
40-60 MG ORAL
5 MG BY SLOW
IV INJ.
changes.
Encourage patients to keep a record of their anginal attacks,
including precipitating factors, number of pills taken, and
therapeutic effects.
Monitor for adverse reactions
Allergic reactions, headache, light-headedness, hypotension,
dizziness
Monitor for therapeutic effects
Relief of angina, decreased BP, or both
Instruct