Download DRUGS USED FOR ANGINA PECTORIS

DRUGS USED FOR
ANGINA PECTORIS
LAKSHMAN KARALLIEDDE
2011
ANGINA PECTORIS
SYMPTOM COMPLEX: CONSTITUTES A CLINICAL SYNDROME
RATHER THAN A DISEASE
CAUSE: TRANSIENT MYOCARDIAL ISCHAEMIA
OCCURS WHEN EVER THERE IS AN INBALANCE BETWEEN
MYOCARDIAL OXYGEN SUPPLY AND DEMAND
COMONEST CAUSE: ATHEROMATOUS DISEASE OF CORONARY
ARTERIES
MAY ALSO BE A MANIFESTATION OF OTHER FORMS OF HEART
DISEASE
e.g. Severe aortic valve disease, hypertrophic cardiomyopathy
DRUGS USED TO RELIEVE OR PREVENT THE
SYMPTOMS OF ANGINA
1.
2.
3.
4.
NITRATES
BETA BLOCKERS
CALCIUM ANTAGONISTS
POTASSIUM CHANEL ACTIVATORS
AS THE FUNDAMENTAL CAUSE OF ANGINA PECTORIS IS INSUFFICIENT
OXYGEN SUPPLY TO HEART MUSCLE, IT IS LOGICAL TO ATTEMPT TO
INCREASE THE OXYGEN SUPPLY BY ADMINISTERING OXYGEN- THAT IS
BY INCREASING THE INSPIRED OXYGEN CONCENTRATION SIMILARLY,
PATIENTS WITH ANGINA MAY SUFFER FROM SEVERE PAIN AND PAIN
RELIEF WITH A POTENT OPIATE
e.g. Morphine NEEDS TO BE CONSIDERED TO MAKE THE PATIENT
MORE
COMFORTABLE, LESS ANXIOUS.
NITRATES
MODE OF ACTION :
ACTS DIRECTLY ON VASCULAR SMOOTH MUSCLE TO
PRODUCE ARTERIAL AND VENOUS DILATATION
EFFECT DURING ANGINA
1.REDUCES MYOCARDIAL OXYGEN DEMAND (LOWERS
PRE-LOAD AND AFTER LOAD)
2. INCREASES MYOCARDIAL OXYGEN SUPPLY
(CORONARY VASODILATATION)
NITRATE PREPARATIONS
1.
2.
3.
4.
5.
6.
SUBLINGUAL GLYCERYL TRINITRATE (GTN)
BUCCAL GLYCERYL TRINITRATE
TRANSDERMAL GLYCERYL TRINITRATE
ORAL ISOSORBIDE DINITRATE
ORAL ISOSORBIDE MONONITRATE
INTRAVENOUS GTN- FOR ACUTE MYOCARDIAL
INFARCTION/LEFT VENTRICULAR FAILURE -10 -200 µg /MIN
INTRAVENOUS INFUSION, TITRATING TO CLINICAL RESPONSE
AND BLOOD PRESSURE.
DURATION OF ACTION OF SOME NITRTATE PREPARATIONS
PEAK ACTION
Sublingual GTN(Tablet 300500µg or metered dose
aerosol 400µg/spray)
4-8 minutes
DURATION OF
ACTION
10-30 minutes
Buccal GTN (1-5 mg tablet 6 4-10 minutes
hourly)
30-300 minutes
Transdermal. GTN (5-10
daily)
1-3 hours
Up to 24 hours
Oral isosorbidedinitrate.(1020 mg 8 hourly)
45-120 hours
2-6 hours
Oral isosorbide mononitrate
( 20-60 mg once or twice a
day)
45-120 hours
6-10 hours
SUBLINGUAL GTN- Administered
a. as a tablet – 300-500 µg to disolve under the tongue
b. As metered-dose aerosol (400 µg per spray)
RELIEVES AN ATTACK OF ANGINA IN 2-3 MINUTES
UNWANTED EFFECTS
 HEADACHE
 SYMPTOMATIC HYPOTENSION –DIZZINESS, POSTURAL GIDDINESS,
BLURRING OF VISION
 RARELY SYNCOPE – FAINTING
ASK PATIENT TO SPIT TABLET IF ABOVE EFFECTS OCCUR
 NOT HABIT FORMING
 TEACH PATIENTS TO USE PROPHYLACTICALLY e.g. Before exerting
 VIRTUALLY INEFFECTIVE IF SWALLOWED DUE TO EXTENSIVE FIRST PASS
METABOLISM IN THE LIVER
CONTINUOUS USE CAUSES PHARMACOLOGICAL TOLERANCE
THERFORE ATTEMPT TO INCLUDE A ‘NITRATE-FREE’ PERIOD OF 6-8 HOURS
A DAY
BETA BLOCKERS
MODE OF ACTION: LOWERS MYOCARDIAL OXYGEN DEMAND BY
A. REDUCING HEART RATE
B. REDUCING BLOOD PRESSURE
C. REDUCING MYOCARDIAL CONTRACTILITY
Can exaccerbate symptoms of peripheral vascular disease
May provoke bronchospasm in patients with obstructive airway disease
e.g asthma
Theoretically-Non- selective beta blockers may aggravate coronary vasospasm
by blocking the coronary artery beta 2 recetors.
Advice: use a once daily cardio-selective preparation e.g atenolol 50-200mg
daily
slow release metoprolol 50-200mg daily
bisoprolol 5-10 mg daily
BETA BLOCKERS SHOULD NOT BE WITHDRAWN ABRUPTLY (SUDDENLY)
BECAUSE OF THE POSSIBILITY OF A REBOUND EFFECT AND THE RISK OF
PRECIPITATING ARRHYTHMIAS, WORSENING ANGINA OR CAUSING
MYOCARDIAL INFARCTION (THE ‘BETA-BLOCKER WITHDRAWAL SYNDROME).
CALCIUM ANTAGONISTS
MODE OF ACTION
1. DECREASES MYOCARDIAL OXYGEN DEMAND BY REDUCING BLOOD
PRESSURE AND MYOCARDIAL CONTRACTILITY
TYPES
A. DIHYDROPYRIDINE CALCIUM ANTAGONISTS-NIFEDIPINE, NICARDIPINE
OFTEN CAUSE REFLEX TACHYCARDIA-BEST USED IN COMBINATION WITH
BETA BLOCKER-not used or caution when using
B. VERAPAMIL AND DILITIAZEM-SUITABLE FOR PATIENTS WHO ARE NOT
RECEIVING BETA BLOCKERS AS THEY DECREASE THE HEART RATE (
DANGEROUS ADDITIVE EFFECT)
CALCIUM CHANNEL ANTAGONISTS MAY REDUCE MYOCARDIAL
CONTRACTILITY TO A DEGREE THAT CAN AGGRAVATEOR PRECIPITATE
HEART FAILURE
UNWANTED EFFECTS




PERIPHERAL OEDEMA
FLUSHING
HEADACHE
DIZZINESS
POTASSIUM CHANNEL ACTIVATORS
MODE OF ACTION: DILATES ARTERIES AND VEINS
DOES NOT EXHIBIT TOLERANCE SEEN WITH NITRATES
NICORANDIL- 10-30 mg 12 hourly
Caution in:
hypovolaemic patients
Patients with pulmonary oedema
Side effects:
a. Headache
b. Flushing
c. Dizziness
d. Weakness
e. May cause a dose dependent increase in heart rate
f. Myalgia
g. Angioedema
ANTIPLATELET DRUGS
ASPIRIN
CLOPIDOGREL
THROMBOLYTIC AGENTS
STREPTOKINASE
ALTEPLASE
RETEPLASE-
ASPIRIN
ANTIPLATELE T EFFECT BY INHIBITION OF THROMBOXANE A 2
NSAID, INHIBITS COX-1 AND COX -2 WHICH LEADS TO
DECREASED PROSTAGLANDIN SYNTHESIS
USES
THROMBO-EMBOLIC CVA, ISCHAEMIC HEART DISEASEPROPHYLAXIS (75MG/DAY) AND ACUTE TREAMENT (300 MG)
CONTRAINDICATIONS
1. THOSE UNDER AGE OF 16Y-CAN INCREASE INCIDENCE OF
REYE’S SYNDROME, LIVER/BRAIN DAMAGE
2. GASTRO-INTESTINAL ULCERS
3. BLEEDING DISORDERS
4. GOUT
5. HYPERSENSITIVITY TO ANY NSAID
6. GFR <10ML/MIN
ASPIRIN
CAUTION
1. ASTHMA
2. UNCONTROLLED HYPERTENSION
3. ANY ALLERGIC DISEASE
4. G6PD DEFICIENCY
5. DEHYDRATION
OTOTOXIC IN OVERDOSE
MAY INCREASE EFFECTS OF SULPHONYL UREAS AND OF METHOTREXATE
FOR ANALGESIA- 300-900 MG 4-6 HPOURLY –MAXIMUM DOSE4G/DAY
STOP 7 DAYS BEFORE SURGERY IF SIGNIFICANT BLEEDING IS EXPECTED
IF CARDIAC SURGERY OR PATIENT HAS ACUTE CORONARY SYNDROMECONSIDER CONTINUING
CLOPIDOGREL
ANTIPLATELET AGENT- ADP RECEPTOR ANTAGONIST
USE
PROPHYLAXIS OF ANTI-THROMBOTIC EVENTS IN NON—ST
ELEVATIONMYOCARDIAL INFARCTION AND IN ST ELEVATION
MYOCARDIAL INFARCTION-IN COMBINATION WITH ASPIRIN
MYOCARDIAL INFARCTION (WITHIN A ‘FEW’ TO35 DAYS)
ISCHAEMICCEREBROVASCULAR ACCIDENT- WITHIN 7 DAYS TO 6
MONTHS
PERIPHERAL ARTERIAL DISEASE
CONTRAINDICATION
ACTIVE BLEEDING
NOT RECOMMENDED WITH WARFARIN
CLOPIDOGREL
SIDE EFFECTS
 HAEMORRHAGE (ESPECIALLY GASTRO-INTESTINAL OR
INTRA-CRANIAL
 GASTRO-INTESTINAL UPSET
 PEPTIC ULCER
 PANCREATITIS
 HEADACHE
 FATIGUE
 DIZZINESS
 PARAESTHESIA
 RASH/PRURITUS
MONITOR FULL BLOOD AND FOR SIGNS OF OCCULT BLEEDING
STREPTOKINASE
THROMBOLYTIC AGENT
INCREASES PLASMINOGEN CONVERSION TO PLASMIN WHICH
INCREASES FIBRIN BREAKDOWN
USES
1. ACUTE MYOCARDIAL INFARCTION -1.5 MILLION UNITS
INTRAVENOUS INFUSION OVER 60 MIN
2. THROMBOEMBOLISM OF ARTERIES
3. PULMONARY EMBOLISM
4. CENTRAL RETINAL ARTERY THROMBOSIS
5. DEEP VEIN THROMBOSIS
OTHER DOSES-250,000 UNITS INTRAVENOUS INFUSION OVER
30 MIN, THEN 100,000 UNITS EVERYHOUR FOR UPTO12-72
HOURS
ALTEPLASE
(RECOMBINANT) TISSUE-TYPE PLASMINOGEN ACTIVATOR.
RECOMBINANT FIBRINOLYTIC
USE
ACUTE MYOCARDIAL INFARCTION (TOTAL DOSE 100MGREGIMEN DEPENDS ON TIME SINCE ONSET OF PAIN
0-6HOURS: 15 MG INTRAVENOUS BOLUS,FOLLOWED BY 50 MG
INTRAVENOUS INFUSION OVER 30 MINUTES AND 35 MG INTRAVENOUS
INFUSION OVER 60 MINUTES
6-12 HOURS-10 MG INTRAVENOUS BOLUS FOLLOWED BY 50 MG
INTRAVENOUS INFUSION OVER 60 MIN, AND FOUR FURTHER 10 MG
INTRAVENOUS INFUSIONS, EACH OVER 30 MIN)
DECREASE DOSE IF PATIENT WEIGHS LESS THAN 65 KG
RETEPLASE
RECOMBINANT PLASMINOGEN ACTIVATOR; THROMBOLYTIC
USED ONLY FOR MYOCARDIAL INFARCTION
DOSE-10 UNITS AS SLOW INTRAVENOUS INJECTION OVER 2 MINUTES,
REPEAT AFTER 30 MIN