Anda di halaman 1dari 56

CARDIOVASCULAR

DRUGS
dr. Dian Nugrahenny, M.Biomed.
Department of Pharmacology
Faculty of Medicine
Universitas Brawijaya
diannugr2407@gmail.com

BASIC ANATOMY AND


PHYSIOLOGY
Functions of cardiovascular system:
Delivery of oxygen, nutrients, and hormones to
the various parts of the body
Transports waste products to the appropriate
waste removal system

COMPONENT OF
CARDIOVASCULAR SYSTEM
Cardiac
Blood vessels
Blood

Guyton Textbook of Medical Physiology, 11th ed.

BASIC ANATOMY AND


PHYSIOLOGY

Guyton Textbook of Medical Physiology, 11th ed.

CARDIAC SYMPATHETIC AND


PARASYMPATHETIC NERVES

Guyton Textbook of Medical Physiology, 11th ed.

ADRENERGIC SYSTEM
Receptor Subtype Tissue
Alpha 1
Beta 1

Vascular smooth
muscle
Heart

Effects
Contraction

Inc. Heart Rate


Inc. Force of

Contraction
Beta 2

Bronchial smooth
muscle

Relaxation

POSSIBLE MECHANISMS FOR


INFLUENCING HEART FUNCTION

Lllmann et al. 2000. Color Atlas of Pharmacology, 2nd


ed. Thieme.

HYPERTENSION
Primary (essential): 90%
Secondary
Virtually no symptoms
Treatment is usually life-long
Consequences of hypertension:
heart disease, kidney disease, blindness, stroke

INITIAL DRUG THERAPY CHOICES

DiPiro et al. 2005. Pharmacotherapy: A Pathophysiologic Approach, 6th ed. The McGraw-Hill
Companies, Inc.

COMPELLING INDICATIONS

DiPiro et al. 2005. Pharmacotherapy: A Pathophysiologic Approach, 6th ed. The McGraw-Hill
Companies, Inc.

DIURETICS
Drugs with a direct renal action.
Augment urine excretion (diuresis) by inhibiting the
reabsorption of NaCl and water.
Indications:
1. Mobilization of edemas: increase renal excretion of
Na+ and H2O.
2. Antihypertensive therapy: decrease peripheral
resistance.
3. Therapy of congestive heart failure: decrease
peripheral resistance, cure symptoms of venous
congestion.

ACTION OF
DIURETICS
1.Thiazides (e.g. HCT): act in the
intermediate segment of distal
tubules.
2.Loop diuretics (e.g.
furosemide): act in the thick
portion of the ascending limb of
Henles loop.
3.K+-sparing diuretics (e.g.
spironolactone): an aldosterone
antagonist, act in the distal
portion of the distal tubule and
the proximal part of the collecting
ducts.

SIDE EFFECTS OF DIURETICS


Side
effects
Increase
urine
output

Actions
Give in the early morning if
ordered daily

Rationale
Peak action will occur
during waking hours & not
interrupt with sleep

Keep a bedpan within reach.


Mainly to avoid fall
Assist to the bathroom anyone
who is elderly, weak, dizzy, or
unsteady in walking.
Postural
hypotensio
n

Assist the patient to get up


slowly

Possibility
Record fluid intake & output
of
regularly
dehydration

Avoid falling

Avoid fluid volume depletion


due to excessive diuresis

Hypo/Hyper Monitor serum potassium level Avoid K depletion due to


-kalemia
(within 3.5-5 mEq)
thiazide & loop diuretics or
Avoid K accumulation in
patient taking K-sparing
diuretics

CA2+-CHANNEL
BLOCKER (CCB)
Inhibit the influx of
Ca2+ ions without
affecting inward Na+ or
outward K+ currents to a
significant degree.
Inhibition of cardiac
functions by VERAPAMIL

Nifedipine

Verapamil

used as an antiarrhythmic drug

SIDE EFFECTS OF CCB


Hypotension, dizziness, weakness, peripheral
edema, headache, heart failure, pulmonary
edema, nausea, constipation
Bradycardia (Verapamil, Diltiazem)
Tachycardia (Nifedipine & other
dihydropyridines)

RENIN-ANGIOTENSIN-ALDOSTERONE SYSTEM (RAAS)

ACE
Inhibitor
s

ACTION OF ANGIOTENSIN II
Angiotensin
II receptor
blocker
(ARB)

reabsorption

Adrenal cortex

ACE INHIBITORS
Used to treat hypertension, heart failure,
myocardial infarction, and nephropathy
Enalapril
Lisinopril
Perindopril
Ramipril

Angiotensin II receptor
blockers (ARBs)
Used for hypertension, may be used as an
alternative to ACE inhibitors in the
management of heart failure and diabetic
nephropathy.
Irbesartan
Losartan
Valsartan

ACE INHIBITOR ARB


Potential Adverse Effects

Nursing Actions

ACE inhibitors and ARBs may


cause first dose
hypotension

Instruct the patient to lie down


if hypotension develops

ACE inhibitors may produce


dry cough, due to
accumulation of bradykinin

Warn patients about the


possibility of cough.
Consult the doctor if the cough
is bothersome to the patient.

ACE inhibitors may cause


hyperkalemia

Avoid potassium
supplements, potassium
containing salt substitutes and
potassium-sparing diuretics

ACE inhibitors and ARBs are


Avoid these drugs in pregnancy
contra-indicated
in of ACE inhibitors and ARBs may be reduced
: The
intestinal absorption
ken pregnancy
with food.

BETA-BLOCKER
By blocking cardiac -receptors, -Blockers serve to lower
cardiac rate and lower the elevated blood pressure caused by
high cardiac output.
The mechanism
underlying their
antihypertensive
action via reduction
of peripheral
resistance is unclear.

Agonist

Antagonist

BETA BLOCKERS
Drug

Receptors
Blocked

Atenolol

Beta1

Metoprolol

Beta1

Carvedilol

Beta1 and 2

Labetolol

Beta1 and 2

Propranolol

Beta1 and 2

28

ADRENERGIC SYSTEM
Receptor Subtype Tissue
Alpha 1
Beta 1

Vascular smooth
muscle
Heart

Effects
Contraction

Inc. Heart Rate


Inc. Force of

Contraction
Beta 2

Bronchial smooth
muscle
Insulin secretion

Relaxation
Stimulation

BETA BLOCKERS
Side Effects:
Bradycardia
Hypotension
Bronchospasms
GI disturbances
Fatigue
Alerts:
Caution patients not to stop taking them abruptly
because that can precipitate angina and MI
Instruct diabetics to monitor blood glucose levels more
often at vulnerable times
Screen for asthma patients on beta blockers

TREATMENT OF CHRONIC HYPERTENSION IN


PREGNANCY

DiPiro et al. 2005. Pharmacotherapy: A Pathophysiologic Approach, 6th ed. The McGraw-Hill
Companies, Inc.

CONGESTIVE HEART FAILURE


Inadequate tissue perfusion from a failing pump, volume

overload
Major causes: hypertension, myocardial infarction
Right Heart Failure
Predominant: Sign:
venous congestion
Subcutaneous
edema
Abdominal effusion
(ascites)
Hepatomegaly
Splenomegaly

Left Heart
Failure
Predominan

t:
Symptom
Dyspnea,

orthopnea,
cough
(pulmonary
edema)

DRUGS FOR HEART


FAILURE
3D:
VasoDilators:
Venodilators
Arteriolar dilators
Diuretics
Digitalis

VASODILATORS
Venodilators: Reduces preload by trapping blood in the
venous circulation
Arteriolar dilators: Reduces afterload by reducing arterial
resistance
Potensial side effect:
hypotension

Lllmann et al. 2000. Color Atlas of


Pharmacology, 2nd ed. Thieme.

OTHER VASODILATORS
Hydralazine:
Dilate arterioles
Treats hypertension
Less postural hypotension
Minoxidil:
Dilate arterioles
For severe hypertension
Diazoxide:
Given i.v. causes prominent arteriolar dilation
For hypertensive crises
Can be used in the management of insulin-secreting
pancreatic tumors.
Nitroprusside sodium:
Dilate venous and arterioles
Given i.v. for hypertensive crises

DIGITALIS, CARDIAC
GLYCOSIDES
In severe cases of myocardial insufficiency,
digitalis may be added to augment cardiac force
(positive inotrope) and to relieve the symptoms of
insufficiency.
Very narrow therapeutic index.
Very long half-life.
Digoxin has many drug interactions:
diuretics,verapamil, amiodarone, etc.

PROCESSES
IN
MYOCARDIA
L
CONTRACTI
ON AND
RELAXATION

Lllmann et al. 2000. Color


Atlas of Pharmacology, 2nd
ed. Thieme.

SIDE EFFECTS OF DIGITALIS


Dysrhythmias
Bradycardia
Toxicity very narrow therapeutic index
hypokalemia makes it easier for toxicity to
occur
Anorexia, nausea, vomiting
Disturbances of color vision
Fatigue

DIGITALIS: ALERTS
Withhold the drug & contact the physician if there are any
signs of digoxin toxicity or marked changes in the pulse
rate/rhythm (bradycardia)
Monitor digoxin levels closely: should be smaller than 2
ng/mL
Older adults are particularly prone to digoxin toxicity
Screen for factors that potentiate digitalis toxicity:
hypokalemia, impaired renal function, oral antibiotics,
quinidine, amiodarone, Ca++ channel blockers

HEMOSTASIS AND THROMBOSIS


C. SECONDARY HEMOSTASIS

latelets
adhesi
on

ADP, adenosine diphosphate; t-PA, tissue type


plasminogen activator

PARENTERAL
ANTICOAGULANTS
Heparin
Administered by injection
Helps inactivate thrombin, factor Xa and others
Half-life is short

Therapeutic Uses:
Open heart surgery
Deep Vein Thrombosis
Acute MI

PARENTERAL
ANTICOAGULANTS
Side Effects
Bleeding
Thrombocytopenia heparin induced
Hypersensitivity
Therapeutic effect is monitored by PTT (partial
thromboplastin time) every 6 hours and dose adjusted to
achieve PTT 1.5-2.0 times normal level

Alerts:
Monitor for signs and symptoms of bleeding: low HR,
hypotension, tachycardia, epistaxis
Avoid injuries
Hold injection sites longer than usual

ORAL
ANTICOAGULANTS
Warfarin
Act as false vitamin K and prevent regeneration of active
vitamin K from vitamin K epoxide, hence the synthesis of
vitamin K-dependent clotting factors.
Vitamin K promotes activation of factors II, VII, IX, and X.
Peak effects take several days.
Therapeutic Uses: Long-term prophylaxis of thrombosis, e.g.
in patients with prosthetic heart valves/atrial fibrillation.

ORAL
ANTICOAGULANTS
Warfarin has MANY drug and herb interactions
Hemorrhage
Warfarin is contraindicated in pregnancy
Must monitor PT (prothrombin time)/INR
(international normalized ratio, contains a
correction factor for PT)
Vitamin K can be given in case of overdose

DRUGS INTERACT WITH


WARFARIN
Abciximab
Acetaminophen
Alcohol
(acute and chronic)
Allopurinol
Aminodarone
Aminoglutethimide
Amobarbital
Anabolic steroids
Aspirin
Azathioprine
Butabarbital
Butalbital
Carbamazepine
Cefoperazone
Cefotetan
Cefoxitin
Ceftriaxone
Chenodiol
Chloral hydrate
Chloramphenicol
Chlorpropamide
Chlorthalidone
Cholestyramine
Cimetidine
Ciprofloxacin
Clarithromycin
Clofibrate

Corticotropin
Cortisone
Coumadin
Cyclophosphamid
e
Danazol
Dextran
Dextrothyroxine
Diazoxide
Diclofenac
Dicloxaxillin
Diflunsial
Disulfram
Doxycycline
Erythromycin
Ethacrynic acid
Ethchlorvynol
Fenoprofen
Fluconazole
Fluorouracil
Gemfibrozil
Glucagon
Glutethimide
Griseofulvin
Haloperidol
Halothane
Heparin

Ibuprofen
Ifosamide
Indomethacin
Influenza virus
vaccine
Itraconazole
Ketoprofen
Ketorolac
Levamisol
Levothyroxine
Liothyronine
Lovastatin
Mefenamic
Meprobamate
Methimazole
Methyldopa
Methylphenidate
Methylsalicylate
Miconzale
Metronidazole
Miconazole
Moricizine HCl
Nafcillin
Nalidixic acid
Naproxen
Neomycin
Norfloxacin

Ofloxacin
Olsalazine
Omeprazole
Oxaprozin
Oxymetholone
Paraldehyde
Paroxetine
Penicillin G
Pentobarbital
Pentoxifylline
Phenobarbital
Phenylbutazone
Phenytoin
Piperacillin
Piroxicam
Prednisone
Primidone
Propafenone
Propoxyphene
Propranolol
Propylthiouracil
Phytonadione
Quinidine
Quinine
Ranitidine
Rifampin

Secobarbital
Sertaline
Simvastatin
Spironolactone
Stanozolol
Streptokinase
Sucralfate
Sulfamethizole
Sulfamethoxazole
Sulfinpyrazone
Sulfinpyrazone
Sulfisoxazole
Sulindac
Tamoxifen
Tetracycline
Thyroid hormone
Ticacillin
Ticlopidine
t-PA
Tolbutamide
Trazodone
Trimethoprimsulfamethoxazole
Urokinase
Valproate
Vitamin C
Vitamin E

WARFARIN AND G
HERBS
Garlic (Allium sativum) 2 case reports. Continuing ingestion
of high levels of garlic or garlic oil can decrease platelet
aggregation.
Ginger (Zingiber officinalis) Inconclusive results in studies
in healthy volunteers but case reports exist.
Ginkgo (Ginkgo biloba) The extract inhibits thromboxane
and prostacyclin in diabetics. A case report suggests interaction.
Green tea (Camellia sinensis) Inhibits platelet synthesis of
thromboxane.
Chavez, Life Sci 2006; 78:2146-57

ORAL
ANTICOAGULANTS
Implications:
Teach the patients:
Observe for signs of bleeding and report bleeding
from gums/nose or in stool/urine
Use soft toothbrush
Avoid using aspirin or NSAIDS or any meds that
may potentiate bleeding
Frequent lab tests are necessary to monitor

ANTIPLATELET
DRUGS
Aspirin
Prevention of thrombosis in arteries
Suppresses platelet aggregation due to inhibition
of thromboxan (TXA2) synthesis
Therapeutic Uses: prophylaxis of MI, prevent
reinfarction in patients with acute MI, prevent
stroke
Low dose - not greater than 325 mg/day
Side Effects: GI bleeding, bronchospasm

ANTIPLATELET
DRUGS
Clopidogrel (Plavix)
Adenosine diphosphate receptor (ADP)
antagonist
Irreversible blocking of ADP receptors on the
platelet surface
Prevent ADP-stimulated aggregation
Therapeutic Uses: prevention of stroke,
vascular death & MI
Side Effects:
Hemorrhage (GI & Intracranial)
GI side effects

ANTIPLATELET
DRUGS
Implications:
Screen for asthma patients on aspirin
Teach the patients:
Drugs should be taken after meal due to GI irritation
Observe for signs of bleeding and report bleeding from
gums/nose or in stool/urine
Use soft toothbrush

SEMANGAT
BELAJAR!!!