DRUGSforANGINA GROUP-1
DRUGSforANGINA GROUP-1
tachycardia.
• Monitor blood
pressure, especially
in those susceptible
to
hypotension.
• Methemoglobine
mia has occurred
in patients
receiving other
organic nitrates
and probably
could occur as
an adverse reaction.
Significant
methemoglobinemia
has occurred
with moderate
overdoses of
organic
nitrates. Suspect
methemoglobinemia
in patients who
exhibit signs
of impaired
oxygen delivery
despite adequate
cardiac
output and
adequate PaO2.
Classically,
methemoglobinemic
blood is
chocolate brown,
without
color change on
exposure to air.
Treatment of choice
for
methemoglobinemia
is methylene blue,
1 to
2 mg/kg
I.V. Breast-
feeding patients
•It isn’t known
whether drug
appears in breast
milk. Use cautiously
in breast-feeding
women. Pediatric
patients
• Safety and efficacy
in children haven’t
been established.
Adverse reactions
CNS: fatigue,
dizziness,
depressio n,
insomnia,
headaches,
nightmares,
drowsiness.
CV: bradycardia, h
ypotension, heart
failure, cold
limbs,
Raynaud’s
disease,
arrhythmi as.
GI: nausea,
diarrhea,
constipatio
n,
flatulence.
Respiratory:
dyspn ea,
bronchospasm
.
Skin: rash.
Other:
decreased
libido.
PROPRANOL Antihypertensive action: ExactAbsorption: Absorbed Hypertension, CNS: Do not
OL mechanism unknown. Mayalmost completely from GI cardiac depression discontinue
reduce blood pressure bytract; food enhances dysrhythmias, MI, , dizziness, abruptly,
blocking adrenergic absorption. hypertrophic drowsiness may
receptors (thus decreasingDistribution: Distributed subaortic stenosis , fatigue, precipitate
cardiac output), bywidely throughout body; Adjunctive lethargy, angina,
decreasing sympatheticmore than 90% protein- therapy of hallucinati sudden
outflow from the CNS, andbound. Metabolism: Almost pheochromocytom on s death;
by suppressing renin total hepatic a, migraine CV: reduce over
release. Antianginal action: metabolism; prophylaxis, bradycardi 1-2 weeks
Decreases myocardial oral dosage angina pectoris a, CHF, Propranolol
oxygen consumption by form Essential tremor cold also has been
blocking catecholamine undergoes extremities used to treat
access to beta-adrenergicextensive Adverse reactions , postural aggression
receptors, thus relieving first-pass CNS: fatigue, lethargy, hypotensio and rage,
angina. metabolism. vivid dreams, hallucinations, n, 2nd or stage fright,
Antiarrhythmic Excretion: About 96% tomental depression, light- 3rd degree recurrent GI
action: Decreases heart rate99% of given doseheadedness, insomnia, heart bleeding in
and prevents exercise-excreted in urine as fever. block, cirrhotic
induced increases in heartmetabolites; remainderCV: bradycardia, hypotension, he profound patients, and
rate. Also decreasesexcreted in feces asart failure, hypotensio menopausal
unchanged drug andintermittent claudication, n symptoms.
myocardial contractility,metabolites. Biologicalworsening of AV block. EENT: dry •Never
cardiac output, and SA andhalf-life about 4 hours. GI: nausea, vomiting, burning administer
AV nodal conduction diarrhea, eyes, sore propranolol
velocity. abdominal throat, as an
Migraine prophylactic cramping. visual adjunct in
action: Thought to result Hematologic: agranulocytosis. disturbance treatment of
from inhibition of Respiratory: bronchospasm. s pheochromocy
vasodilation. Skin: rash. to
MI prophylactic action: Exact GI: ma unless
mechanism unknown. diarrhea, patient has
dry mouth, been
elevated pretreated
LFT s, with alpha
ischemic blockers.
colitis, • Monitor
mesenteri serum
c arterial glucose level;
thrombosi drug may
s, nausea, mask signs of
vomiting hypoglycemia
GU: . Breast-
impotenc feeding
e, sexual patients
dysfuncti • Drug
on appears in
HEME: breast milk.
agranulocy An alternative
to sis, to breast-
thrombocy feeding is
to penia recommended
RESP: during
Bronchosp therapy.
as m, Pediatric
dyspnea, patients
wheezing • Safety
SKIN: and efficacy
alopecia, in children
pruritis, haven’t been
rash established;
use only if
potential
benefit
outweighs
risk. Geriatric
patients
•Elderly
patients may
need lower
maintenance
doses because
of increased
bioavailability
or delayed
metabolism;
they also may
experience
enhanced
adverse
effects.
NADOLOL Absorption: Oral doses Nadolol is indicated to treat
a light-headed Use nadolol
Nadolol is a nonselective of nadolol are angina pectoris and feeling, like you cautiously in
beta adrenal receptor approximately 30% hypertension. might pass out; patients with
blocker that is used to lower absorbed. slow heartbeats; diabetes
blood pressure. It has a long Distribution: In healthy shortness of
duration of action as it is subjects, the volume of breath (even with mellitus because it
usually taken once daily and distribution of nadolol is mild exertion), may prolong or
a wide therapeutic index as 147- 157L. swelling, rapid
patients start at doses of Metabolism: Nadolol is weight gain; or worsen
40mg daily but may be not metabolized by the bronchospasm hypoglycemia
increased to doses as high liver in humans. (wheezing, chest
as 240mg daily. Patients Elimination: Nadolol is tightness, trouble by
taking nadolol should not primarily eliminated in breathing). interfering
aburptly stop taking it as this the urine because it is numbness or cold
may lead to exacerbation ofnot metabolized in the feeling in your with glycogenolysis
ischemic heart disease liver. After 72 hours, 60 hands or feet;
percent of an intravenous dizziness;
dose is removed in the feeling
urine and 15 percent in tired;
the feces in healthy upset
patients. After that, the stomach,
remainder of the dose vomiting,
should be removed in the diarrhea,
stool. constipatio n;
vision problems;
or mood
changes,
confusion,
memory
problems.
ATENOLOL Antihypertensive Absorption: About 50% to Hypertension. Adults: Initially,Drug-drug. Alpha- Patient should take
action: Atenolol may reduce60% of an atenolol dose is25 to 50 mg P.O. as a singleadrenergic drugs oral single daily
blood pressure by adrenergicabsorbed. daily dose. May increase dose(such as those dose at same time
receptor blockade, therebyDistribution: Distributed to 100 mg daily after 7 to 14found in OTC cold each day.
decreasing cardiac output by into most tissues and days. Higher doses areremedies), • Drug may be
decreasing the sympatheticfluids except the brain unlikely to produce further indomethacin, taken without
outflow from the CNS and byand CSF; about 5% to NSAIDs: May food.
suppressing renin release. 15% is protein- benefit. antagonize • Monitor blood
At low doses, atenolol, likebound. Metabolism: Chronic stable anginaantihypertensiv pressure, heart rate,
metoprolol, selectivelyMetabolized minimally. pectoris. Adults: 50 mg P.O.e effects of and ECG during I.V.
inhibits cardiac beta1-Excretion: About 40% toonce daily; may be increasedatenolol. administration.
receptors; it has little effect50% of a given dose isto 100 mg daily after 7 daysMonitor patient • Dose may need to
on beta2-receptors inexcreted unchanged infor optimal effect. Maximumfor effect. be reduced in
bronchial and vascularurine; remainder isdaily dose is 200 mgAntihypertensives: patients with renal
smooth muscle. excreted as unchanged May potentiate insufficiency.
Antianginal action: Atenolol drug and metabolites in daily. antihypertensi • I.V. atenolol affords
aids in treating chronicfeces. In To reduce risk of CV mortality ve effect of a rapid onset of
stable patients with normal in patients with acute these the
renal MI. Adults: 5 mg I.V. over 5 protective effects of
minutes, followed by another beta blockade
5 mg against
angina by decreasingfunction, plasma half-life I.V. 10 minutes later. Startdrugs. Monitor reinfarction.
myocardial contractility andis 6 to 7 hours; half-life oral therapy (50 mg) 10blood pressure. • Patients who
heart rate (negativeincreases as renal function minutes after the final doseInsulin, oral can’t tolerate I.V.
inotropic and chronotropicdecreases. in patients who tolerate thehypoglycemics: atenolol after
effect), thus reducing full I.V. dose. Then, 50 mg Alte rs dosage an MI may be
myocardial oxygen P.O. 12 hours requirements in candidates for
consumption. later. Thereafter, 100stable diabetic oral atenolol
Cardioprotective action: The mg P.O. daily or 50 mg P.O. patients. Monitor therapy. Some
mechanism whereby b.i.d. for 6 to 9 days or untilserum glucose evidence suggests
atenolol improves survival in discharged from the hospital. level. that gastric
patients with MI is unknown. To slow rapid ventricular absorption of
However, it does reduce the response to atrial atenolol may
frequency of PVCs, chest tachyarrhythmias following be delayed in
pain, and enzyme elevation. acute MI without left ventricular Adverse reactions the early phase of
dysfunction and AVCNS: fatigue, MI. This may result
block ◇. Adults: 2.5 to 5 mg I.V.lethar gy, from the
over 2 minutes, p.r.n., tovertigo, physiologic
control rate; no more thandrowsiness, changes that
10 mg over a 10- to dizzine ss, mental accompany MI or
15-minute period.depression, from the effects
≡ Dosage adjustment. fever. of morphine,
For patients with renal failure,CV: bradycardia, h which is
adjust dosage if creatinineypotension, heart commonly
clearance is below 35failure, administered to
ml/minute. If patient has intermittent treat chest
creatinine clearance of 15 toclaudication, pain. However,
35 ml/minute, give 50 mgchanges in oral therapy alone
daily. If patient has creatinineexercise may still provide
clearance below 15 ml/tolerance and benefits.
minute, give 25 mg daily. IfECG. GI: nausea, • I.V. atenolol may
patient is undergoingdiarrhea, dry be given undiluted
hemodialysis, dosage is 25 to mouth. GU: renal or diluted no more
50 mg after each treatmentimpairment, than 1 mg/minute.
under close supervision. dysuria, nocturia, • Protect
oliguria, medication from
proteinuria. heat, direct light,
Hematologic: agra and moisture and
nulocytosis, store at room
nonthrombocytop temperature.
enic or • Caution against
thrombocytopenic abrupt withdrawal of
purpura, medication; it may
thrombocytopenia, precipitate MI and
anemia. increased
Hepatic: angina.
liver Pregnant patients
dysfunction • Atenolol can
. cause fetal harm
Metabolic: (intrauterine growth
hyperkal retardation).
Breast-feeding
patients
• Safety hasn’t
been established.
emia, Recommend
hyperglycemia,
hyp oglycemia. an alternative
Musculoskeletal: l feeding method
eg pain. during therapy.
Respiratory: Pediatric patients
dyspn ea, • Safety and efficacy
bronchospasm in children haven’t
. been established;
Skin: rash. use only if potential
benefit
outweighs
risk.
Geriatric patients
• Geriatric patients
may require
lower maintenance
doses of atenolol
because of
increased
bioavailability
or delayed
metabolism; they
also may
have
greater adverse
effects.
Antianginal and Absorption: About 80% ofManagement of Prinzmetal’s orDrug- S.L. nitroglycerin
III. CALCIUM DILTIAZEM antihypertensive actions: By a dose is absorbed rapidlyvariant angina or chronic stable drug. Anesthetics: may be
CHAN dilating systemic arteries, from the GI tract.angina pectoris. Adults: 30 mg May potentiate administered
NEL diltiazem decreases total However, only about 40%P.O. q.i.d. before meals andeffects. Monitor concomitantly, as
BLOC peripheral resistance and of drug enters systemich.s. Increase dose gradually topatient. needed, if patient
KERS afterload, slightly reduces circulation because of amaximum of 360 mg dailyBeta blockers: May has acute angina
blood pressure, and significant first-pass effectdivided into three to fourcause heart symptoms.
increases cardiac index in the doses, as indicated. Or, 120 orfailure, •Diltiazem has been
when given in high doses liver. 180 mg (extended-release)conduction used
(more than 200 mg). Distribution: About 70% toP.O. once daily. Adjust over a disturbances, investigationally to
Afterload reduction, which 85% of circulating drug is7- to 14-day period as neededarrhythmias, and prevent reinfarction
occurs at rest and with bound to plasma proteins.and tolerated up to ahypotension. Use after non-Q-wave
exercise, and the resulting Metabolism: Metabolized inmaximum dose of 480 mgtogether MI; as an adjunct in
decrease in myocardial the daily. cautiously. the treatment of
oxygen consumption liver. Hypertension. Adults: 60 Carbamazepine: Maperipheral vascular
account for the effectiveness Excretion: About 35% is y increase serum disorders; and in the
of diltiazem in controlling excreted in the urine and to carbamazepine treatment of several
chronic stable angina. about 65% in the bile as120 mg P.O. b.i.d. (sustained-levels, leading to spastic smooth-
Diltiazem also decreases unchanged drug andrelease). Adjust up totoxicity. Monitor muscle disorders,
myocardial oxygen demand inactive and activemaximum recommended doseserum levels. including
and cardiac work by metabolites. Eliminationof 360 mg daily, as needed.Cimetidine, esophageal spasm.
reducing heart rate, half-life is 3 to 9 hours.Or, give 180 to ranitidine: May •Diltiazem may be
relieving coronary artery Half-life may increase in240 mg (extended-release)increase diluted in D5W or
spasm (through coronary geriatric patients;P.O. once daily. Adjust dose diltiazem level. normal saline
artery vasodilation), and however, renalbased on patient response toMonitor solution. It’s
dilating peripheral vessels. dysfunction doesn’ta maximum dose ofpatient carefully. incompatible with
These effects appear to affect half-life. 480 mg daily. I.V. furosemide.
relieve ischemia and pain. In Atrial fibrillation or flutter,
patients with Prinzmetal’s paroxysmal supraventricular Cyclosporine: •If systolic blood
angina, diltiazem inhibits tachycardia. Adults: 0.25 Incre ases serum pressure is less
coronary artery spasm, mg/kg cyclosporine than 90 mm Hg or
increasing myocardial I.V. as a bolus injection over 2levels and heart rate is less
oxygen delivery. minutes. Repeat after 15cyclosporine- than 60
Antiarrhythmic action: By minutes if response isn’tinduced beats/minute, dose
impeding the slow inward adequate with a dose of 0.35nephrotoxicity. If should be withheld
influx of calcium at the AV mg/kg I.V. over 2 minutes.used together, until patient is
node, diltiazem decreases Follow bolus with continuousmonitor further evaluated.
conduction velocity and I.V. infusion at 5 to 15 mg/cyclosporine Breast-feeding
increases refractory period, hour (for up to 24 hours). levels. Digoxin: patients
thereby decreasing the Increases •Drug appears in
impulses transmitted to the digoxin breast milk;
ventricles in atrial fibrillation levels. Monitor women shouldn’t
or flutter. The result is a patient for breast-feed during
decreased ventricular rate. toxicity. Fentanyl: diltiazem therapy.
Cause severe Pediatric patients
hypotension; may • Safety and
increase fluid efficacy haven’t
volume been established.
requirements. Geriatric patients
Monit or vital •Use drug
signs. cautiously in elderly
Furosemide: Forms patients because
a precipitate the half-life may be
when mixed with prolonged.
diltiazem
injection. Give Patient education
drugs through •Tell patient that
separate I.V. nitrate therapy
lines. Lithium: May prescribed during
decrease lithium adjustment of
levels. Monitor diltiazem dosage
serum levels. may cause dizzi
Theophylline:
May enhance
drug actions.
Monitor patient
for increased or
adverse effects.
Adverse reactions
CNS: headache,
diz ziness,
asthenia,
somnolence,
insomnia, gait
abnormalities.
CV: peripheral
ede
ma,arrhythmias,
flu shing,
bradycardia,
hypotension,
conduction
abnormalities,
heart failure, AV
block, abnormal
ECG. EENT:
amblyopia, eye
irritation.
GI: nausea,
constipation,
abdom inal
discomfort.
Hepatic:
acute
hepatic
injury. Skin:
rash.
VERAPAMIL Antianginal action: ManagesAbsorption: AbsorbedManagement of Prinzmetal’s orDrug- If verapamil is
unstable and chronic stablerapidly and completelyvariant angina or unstable ordrug. Antihypertens started in patient
angina by reducingfrom GI tract after oralchronic stable anginaives, drugs that receiving
afterload, both at rest andadministration; however,pectoris. Adults: Initial dose, 80attenuate alpha- carbamazepine, a
with exercise, therebyonly about 20% to 35%to 120 mg P.O. t.i.d. Dosage adrenergic 40% to 50%
decreasing oxygenreaches systemicmay be increased at weeklyresponse (such as reduction in
consumption. Also decreasescirculation because ofintervals. Some patients maymethyldopa, carbamazepine
myocardial oxygen demandfirst- pass effect.need up to prazosin), quinidine dosage may be
and cardiac work by exertingTherapeutic serum levels480 mg (to treat needed. Monitor
a negative inotropic effect,are 80 to 300 ng/ml. daily. hypertrophic patient closely for
reducing heart rate, relievingDistribution: Steady state Supraventricular cardiomyopathy): C signs of toxicity.
coronary artery spasm (viadistribution volume intachyarrhythmias. Adults: auses • If verapamil is
coronary arteryhealthy adults ranges0.075 hypotension. added to therapy of
vasodilation), and dilatingfrom about 4.5 to 7 L/kg;to 0.15 mg/kg (5 to 10 mg)Monitor blood patient receiving
peripheral vessels. The netmay increase to 12 L/kg inI.V. push over 2 minutes. If nopressure digoxin, reduce
result of these effects ispatients with hepaticresponse occurs, give a closely. Adjust digoxin dosage by
relief of angina-relatedcirrhosis. About 90% ofsecond dose of 10 mg (0.15dosage of half and monitor
ischemia and pain. Incirculating drug is boundmg/kg) 15 to either drug as subsequent serum
patients with Prinzmetal’sto plasma30 minutes after the initial needed. drug levels.
variant angina, verapamil dose. Give over at least 3Beta • During long-term
inhibits coronary arteryproteins. Metabolism:minutes in geriatricblockers: Causes therapy with
spasm, resulting in increasedMetabolized in liver. additive effects verapamil and
myocardial oxygen delivery. Excretion: Excreted inpatients. leading to heart digoxin, monitor
Antihypertensive urine as unchanged drugChildren ages 1 to 15: 0.1 to 0.3failure, ECG periodically to
action: Reduces bloodand active metabolites.mg/kg (2 to 5 mg) as I.V.conduction observe for AV block
pressure mainly by dilatingElimination half- lifebolus over 2 minutes. Dosedisturbances, and
peripheral normally 6 to 12 hours; shouldn’t exceed 5 mg. Dosearrhythmias, bradycardia.
increases to as much as may be repeated in 30and • Reduce
16 minutes if no response verapamil
occurs (shouldn’t dosage in patients
exceed 10 with renal or
mg). hepatic
vessels. Drug’s negativehours in patients withChildren younger than age 1: hypotension, impairment, those
inotropic effect blocks reflexhepatic cirrhosis. In0.1 especially with with severely
mechanisms that lead toinfants, elimination half-to 0.2 mg/kg (0.75 to 2 mg) as high beta-blocker compromised
increased blood pressure.life may be 5 to 7 hours. I.V. bolus over 2 minutes.doses, drugs cardiac function, and
Antiarrhythmic action: Drug’s Dose may be repeated in 30administered I.V., those receiving beta
combined effects on the SA minutes if no responseor moderately blockers.
and AV nodes help manage severe to severe • Stop disopyramide
arrhythmias. Its primary occurs. heart failure, 48 hours before
effect is on the AV node; Control of ventricular rate in severe starting verapamil,
slowed conduction reduces digitalized patients with chroniccardiomyopathy, and don’t resume
the ventricular rate in atrial atrial flutter or or recent MI. until 24 hours after
tachyarrhythmias and blocks fibrillation. Adults: 240 to 320Monitor cardiac verapamil has been
reentry paths in paroxysmal mg status closely. stopped.
supraventricular P.O. daily in three to four Carbamazepine: • Generic
arrhythmias. divided doses. Inc reases serum sustained- release
Prophylaxis of repetitivecarbamazepine verapamil
paroxysmal supraventricularlevels and tablets may be
tachycardia. Adults: 240 to 480subsequent substituted only for
mg daily given in three to fourtoxicity. Use Isoptin SR and Calan
divided together SR, not Verelan
cautiously; capsules. The
doses. watch for signs of capsule form should
Hypertension. Adults: Usual toxicity. be given only once
starting dose is 80 mg P.O. Cyclosporine: Incre daily. When using
t.i.d. Daily dose may be ases serum
increased to cyclosporine sustained- release
360 to 480 mg. Initial dose oflevels. Monitor tablets, doses over
extended-release tablets ortherapeutic 240 mg should be
capsules is 120 to 240 mg effect; adjust given
daily in the morning. Initialcyclosporine b.i.d.
dose of Covera-HS is 180 mgdosage as • Obtain periodic
h.s. and of Verelan PM is 200needed. liver function
mg h.s. Start therapy withDantrolene: May tests.
sustained-release capsules atcause • If patient is
180 mg (240 mg for Verelan)hyperkalemia receiving verapamil
daily in the morning. Adjustand myocardial I.V., monitor ECG
dosage based ondepression. and blood
effectiveness 24 hours afterConsid er using a pressure
dosing. Increase by 120 mgdihydropyridine continuously. Breast-
daily until a maximum dose of calcium blocker. feeding patients
480 mg daily is given.Digoxin: May • Drug appears in
Sustained-release capsulesincrease serum breast milk. To avoid
should be given only oncedigoxin levels by possible
daily. Antihypertensive effects50% to 75% adverse effects in
are usually seen within theduring first week infants, mother
first week of therapy. Mostof therapy. shouldn’t breast-
patients respond to 240 mgAdjust digoxin feed during therapy.
daily. dosage; monitor Pediatric patients
cardiac •Currently, only the
status closely. I.V. form is
indicated
for
Disopyramide: use in children to
Caus es treat
combined supraventricular
negative tachyarrhythmias.
inotropic effects. Geriatric patients
Monitor patient • Elderly patients
closely. may need lower
Etomidate: May doses.
increase • Give I.V. doses
anesthetic effect over at least 3
of etomidate, minutes to minimize
with prolonged risk of adverse
respiratory effects.
depression and
apnea. Use
cautiously.
Flecainide: May
add to negative
inotropic effect
and prolong AV
conduction.
Monitor cardiac
status.
Hydantoins:
May decrease
serum
verapamil
levels.
Use
cautiousl
y.
Inhaled
anesthetics:
Causes excessive
CV depression.
Avoid use
together.
Lithium: May
increase lithium
effects. Adjust
lithium dosage,
as needed.
Neuromuscular
blockers: Drug
may potentiate
their action.
Adjust dosage of
neuromuscular
blockers, as
needed;
monitor
patient closely.
Phenobarbital:
May increase
verapamil
clearance.
Monitor cardiac
status.
Rifampin: May
substantially
reduce
verapamil’s oral
bioavailability.
Monit or
therapeutic
effect; adjust
dosage of
verapamil, as
needed.
Sulfinpyrazone: Ma
y increase
clearance of
verapamil.
Monitor patient
closely.
Theophylline: Caus
es increased
plasma
theophylline
levels. Monitor
patient closely;
adjust
theophylline
dosage as
needed. Vitamin
D: May reduce
therapeutic
effect of
verapamil.
Monitor patient
closely.
Drug-herb. Black
catechu: May
cause additive
effects.
Discourage use
together.
Yerba maté: May
decrease
clearance of
yerba maté
methylxanthines
and cause
toxicity.
Discourage
use together.
Drug-food. Any
food:
Increases
absorption.
Tell
patient to take
drug with food.
Drug-
lifestyle. Alcohol
use: Prolongs
intoxication
effect.
Discourage
alcohol use.
Adverse reactions
CNS: dizziness,
headache,
asthenia. CV:
transient
hypotension, heart
failure, pulmonary
edema,
bradycardia, AV
block, ventricular
asystole,
ventricular
fibrillation,
periphe ral
edema.
GI: constipation,
na usea.
Respiratory:
pulmo nary
edema.
Skin: rash.
AMLODIPINE After the administration of Absorption: The Indicated for - Swelling of - Monitor blood
therapeutic doses of gastrointestinal tract hypertension, to lower the hands, pressure while
amlodipine to patients absorbed amlodipine blood pressure feet, ankles, adjusting
diagnosed with hypertension, slowly and virtually Lowering blood pressure or lower legs dosage,
amlodipine causes entirely. 6-12 hours reduces the risk of fatal and - Headache especially in
vasodilation, which results in after oral dosing, nonfatal cardiovascular - Upset stomach patients with
a reduction of supine and peak plasma events, primarily strokes and - Nausea. heart failure or
standing blood pressure. concentrations are myocardial infarctions 5 - Stomach pain severe aortic
reached. mg/day PO initially; may be stenosis
increased by 2.5 mg/day because
every 7-
14 days; not to exceed 10
mg/day
Amlodipine's maintenance: 5-10 mg/day - Dizziness symptomatic
bioavailability is Adjust dosage according to or hypotension may
predicted to be blood pressure goals lightheadedn occur.
between 64 and 90 es s Use
percent. After 7- 8 days - Drowsiness
of regular dosage, Excessive amlodipine
steady-state plasma tiredness cautiously in
amlodipine levels are patients with heart
attained. Food has no block, heart failure,
effect onabsorption. impaired renal
Distribution: 21 L/kg function,
Metabolism: hepatic
Amlodipine is disorder, or severe
significantly converted aortic stenosis.
to inactive metabolites
by hepatic breakdown
(about 90%), with 10%
of the parent molecule
and 60% of the
metabolites eliminated
in the urine.
Elimination: Elimination
from the plasma occurs
in a biphasic with a
terminal elimination
half-life of about 30–50
hours. Amlodipine is
10% excreted as
unchanged drug in the
urine. Amlodipine can
be initiated at normal
doses in patients
diagnosed with renal
failure
NIFEDIPINE Antianginal action: NifedipineAbsorption: About 90% ofManagement of Prinzmetal’sDrug-drug. Beta Nifedipine has been
dilates systemic arteries,a dose is absorbed rapidly(variant) angina or chronicblockers: May used
resulting in decreased totalfrom the GI tract after oralstable angina. Adults: Startingworsen angina, investigationally to
peripheral resistance andadministration; however,dose is 10 mg P.O. t.i.d. Usualheart failure, and treat Raynaud’s
modestly decreasedonly about 65% to 70% ofeffective dosage range is 10 hypotension. Use phenomenon
systemic blood pressure withdrug reaches the systemicto 20 mg t.i.d. Some patientstogether
a slightly increased heartcirculation because of amay need up to 30 mg q.i.d. cautiously. and
rate, decreased afterload,significant first-pass effectOr, 30 to 60 mg (extended-Cimetidine: May preterm
and increased cardiac index.in the liver. Therapeuticrelease) P.O. daily. Graduallydecrease labor.
Reduced afterload and theserum levels are 25 to 100increased at 7- to 14- daynifedipine ALERT Warn patient
subsequent decrease inng/ml. Distribution: Aboutintervals or more frequently, if metabolism. Use not to switch
myocardial oxygen92% to 98% of circulatingneeded. Maximum dose is 180together brands. Procardia XL
consumption probablynifedipine is mg daily for capsules, 120cautiously. and
account for the value of bound to plasma mg for Digoxin: May Adalat CC
nifedipine in treating proteins. extended-release increase serum aren’t
chronic digoxin therapeutically
tablets. equivalent because
of major
differences
in
their
pharmacokinetics.
stable angina. InMetabolism: Metabolized in Hypertension. Adults: Initially, levels. Monitor • Initial doses and
Prinzmetal’s angina,the 30 to 60 mg P.O. once dailyserum digoxin increased dosage
nifedipine inhibits coronary (extended-release). Adjustlevel. Fentanyl: may worsen angina
artery spasm, increasingliver. dosage at 7- to 14-dayMay cause briefly. Reassure
myocardial oxygen delivery. Excretion: Excreted inintervals based on patientexcessive patient that this
urine and feces as inactivetolerance and response.hypotension. Use effect is temporary.
metabolites. EliminationMaximum dose is 120 mgtogether • No advantage has
half- life is 2 to 5 hours. daily. cautiously. been found in S.L. or
Hypotensive intrabuccal
drugs: May nifedipine use.
precipitate • Monitor blood
excessive pressure regularly,
hypotension. especially if patient
Use is also taking beta
together blockers
cautiously. or
Phenytoin: May antihypertensives.
increase • Although
phenytoin levels. rebound effect
Monitor hasn’t been
phenytoin levels. observed when drug
Drug- is stopped,
herb. Melatonin: reduce
Int erferes with dosage
antihypertensive
effect of slowly.
nifedipine. Geriatric patients
Discoura ge use •Use drug cautiously
together. in geriatric
Drug- patients because
food. Grapefruit they may be more
juice: Increases sensitive to effects
bioavailability ofof drug and duration
drug. Advise of effect may be
patient to avoid prolonged.
taking drug with Orthostatic
grapefruit juice. blood pressures
should be
Adverse reactions monitored.
CNS: dizziness,
light-headedness,
headache,
weakness,
syncope,
nervousness,
fever. CV:
peripheral edema,
hypotension
, palpitations,
heart failure, MI,
flushing.
EENT: nasal
congestion.
GI: nausea,
diarrhe a,
constipation,
abdominal
discomfort.
Hepatic: liver
dysfunction.
Metabolic:
hypokal emia.
Musculoskeletal:
muscle cramps.
Respiratory:
dyspn ea, cough,
pulmonary
edema. Skin:
rash, pruritus.